AIM： To evaluate the inhibitive effect of olmesartan to fibroblast proliferation and the anti-scarring effect in Tenon＇s capsule, both in vitro and in vivo.· METHODS： Human primary Tenon＇s capsule fibroblasts...AIM： To evaluate the inhibitive effect of olmesartan to fibroblast proliferation and the anti-scarring effect in Tenon＇s capsule, both in vitro and in vivo.· METHODS： Human primary Tenon＇s capsule fibroblasts were cultured in vitro, treated with up titrating concentrations of olmesartan. The rate of inhibition was tested with methyl thiazol tetrazolium（MTT） method.Real-time PCR was performed to analyze changes in m RNA expressions of the fibrosis-related factors： matrix metalloproteinase-2（MMP-2）, tissue inhibitor of metalloproteinase（TIMP-1,2） and proliferating cell nuclear antigen（PCNA）. Thirty rabbits were divided into5 groups（3, 7, 14, 21, and 28d）. A rabbit conjunctiva flap model was created in each eye. Olmesartan solution was injected subconjunctivally and then evaluated its anti-proliferation and anti-fibrosis effects through the histological morphology and immunohistochemistry of MMP-2 and PCNA in each group. Only the 7d group was treated with Masson＇s trichrome to compare the neovascularization in the subconjunctiva area.·RESULTS： In vitro, cultured Tenon＇s capsule human fibroblasts showed a dose dependent inhibition by olmesartan in MTT. Olmesartan reduced m RNA expressions of MMP-2 and PCNA but increased m RNA expressions of TIMP-1 and TIMP-2. In vivo, the rabbit eyes treated with olmesartan at 3rd, 7th, 14 thand 21stdays demonstrated a significant reduced expressions of MMP-2 and PCNA compared with control eye, no significant difference observed in 28 thday group. The cellular proliferation and neovascularization was suppressed by olmesartan in Masson＇s trichrome observation.·CONCLUSION： By inhibiting fibroblasts in vitro and in vivo, olmesartan prevents the proliferation and activity of fibroblasts in scar tissue formation, which might benefit glaucoma filtering surgery.展开更多
In this study, we evaluated the anti-proliferative activity of phlorotannins derived from brown algae Laminariajaponica Aresch extracts on the human hepatocellular carcinoma cell （BEL-7402） and on routine leukemic c...In this study, we evaluated the anti-proliferative activity of phlorotannins derived from brown algae Laminariajaponica Aresch extracts on the human hepatocellular carcinoma cell （BEL-7402） and on routine leukemic cells （P388） by MTT assay. Cells were incubated with 100 μg/mL of the phlorotannin extract （PE） for 48 h. The inhibitory rate of PE on BEL-7402 and P388 cells was 30.20±1.16% and 43.44±1.86%, respectively, and the half-inhibitory concentration of PE （IC50） on P388 and BEL-7402 cells was 120 μg/mL and 〉200 μg/mL, respectively. Microscopic observation shows that the morphologic features of tumor cells treated with PE and 5-fluorouracil are markedly different from the normal control group. The inhibitory rate of fraction A2 isolated from PE by sephadex LH-20 for BEL-7402 and P388 cells at the sample concentration of 70.42 μg/mL was 61.96±7.02% and 40.47±8.70%, respectively. The apoptosis peak for fraction A2 was the most profound of all fractions used in the flow cytometry assay. The results indicate that the anti-proliferative of this algal extract is associated with the total phlorotannin content.展开更多
Objective:To evaluate the in vitro anticancer activity of crude ethyl acetate extracts of the culture of four marine-derived fungi Aspergillus similanensis KUFA 0013(E1),Neosartorya paulistemis KUFC 7897(E2),Neosartor...Objective:To evaluate the in vitro anticancer activity of crude ethyl acetate extracts of the culture of four marine-derived fungi Aspergillus similanensis KUFA 0013(E1),Neosartorya paulistemis KUFC 7897(E2),Neosartorya siamensis KUFA 0017(E4) and Talaromyces trachyspermus KUFC 0021(E3) on a panel of seven human cancer cell lines.Methods:Effects on cell proliferation,induction of DNA damage and cell death were assessed by MTT and clonogenic assays,comet assay and nuclear condensation assay,respectively.Results:The proliferation of HepG2,HCTl 16 and A375 cells decreased after incubation with the extracts E2 and E4.The anti-proliterative effect was confirmed by morphologic alterations and by clonogenic assay.Both extracts also induced cell death in HepG2 and HCT116 cells.Doxorubicin was used as a positive control and showed in vitro anticancer activity.Conclusions:This study demonstrated,for the first time,that extracts of Neosartorya paulistensis and Neosartorya siamensis have selective anti-proliferative and cell death activities in HepG2,HCT16 and A375 cells.The bioactivity of these extracts suggests a potential for biotechnological applications and substantiates that both should be further considered for the elucidation of the molecular targets and signal transduction pathways involved.展开更多
Backgorund:Fruits and seed extracts of Annona montana have significant cytotoxic potential in several cancer cells.This study evaluates the effect of A.montana leaves hexane extract on several signaling cascades and g...Backgorund:Fruits and seed extracts of Annona montana have significant cytotoxic potential in several cancer cells.This study evaluates the effect of A.montana leaves hexane extract on several signaling cascades and gene expression in metastatic breast cancer cells upon insulin-like growth factor-1(IGF-1)stimulation.Methods:MTT assay was performed to determine the proliferation of cancer cells.Propidium iodide staining and flow cytometry analysis of Annexin V binding was utilized to measure the progression of the cell cycle and the induction of apoptosis.Protein expression and phosphorylation were determined by western blotting analysis to examine the underlying cellular mechanism triggered upon treatment with A.montana leaves hexane extract.Results:A.montana leaves hexane(subfraction V)blocked the constitutive stimulation of the PI3K/mTOR signaling pathways.This inhibitory effect was associated with apoptosis induction as evidenced by the positivity with Annexin V and terminal deoxynucleotidyl transferase dUTP nick end labeling(TUNNEL)staining,activation of caspase-3,and cleavage of PPAR.It also limited the expression of various downstream genes that regulate proliferation,survival,metastasis,and angiogenesis(i.e.,cyclin D1,survivin,COX-2,and VEGF).It increased the expression of p53 and p21.Interestingly,we also observed that this extract blocked the activation of AKT and ERK without affecting the phosphorylation of the IGF-1 receptor and activation of Ras upon IGF-1 stimulation.Conclusion:Our study indicates that A.montana leaves(sub-fraction V)extract exhibits a selective anti-proliferative and proapoptotic effect on the metastatic MDA-MB-231 breast cancer cells through the involvement of PI3K/AKT/mTOR/S6K1 pathways.展开更多
A series of novel derivatives of indirubin were synthesized and evaluated for their anti-proliferative activity against human cancer cell lines of SGC7901,A549,HL-60,SK-BR-3 and HCT116.Most of the compounds displayed ...A series of novel derivatives of indirubin were synthesized and evaluated for their anti-proliferative activity against human cancer cell lines of SGC7901,A549,HL-60,SK-BR-3 and HCT116.Most of the compounds displayed more potent activity than Sunitinib.In addition,the derivatives showed improved water solubility,which may be favorable to their pharmacokinetic performances.展开更多
Lectins are the carbohydrate-binding proteins of non-immune origin which have been the subject of intense investigation over the last few decades owing to the variety of interesting biological properties. Most of the ...Lectins are the carbohydrate-binding proteins of non-immune origin which have been the subject of intense investigation over the last few decades owing to the variety of interesting biological properties. Most of the lectins which have been purified and characterized from plants have been obtained from dicotyledons. In the present study a lectin was purified from tubers of a monocot plant Arisaema utile (AUL) Schott by affinity chromatography on asialofetuin-linked amino activated silica beads. AUL gave a single band in SDS-PAGE at pH 8.3 corresponding to subunit Mr 13.5 kDa. The native molecular mass of AUL was 54 kDa suggesting a homotetrameric structure. AUL gave multiple bands in isoelectric focusing and in native PAGE at pH 8.3. AUL was inhibited by N-acetyl-D-lactosamine (Lac NAc), a disaccharide and asialofetuin, a complex desialylated serum glycoprotein. When treated with denaturing agents, the lectin was stable in the presence of urea (3 M), thiourea (4 M) and guanidine HCl (4 M). AUL was a glycoprotein with a carbohydrate content of 1.2%. Complete loss of activity was observed upon modification of tryptophan residues of the lectin. The activity was reduced to 25% after modification of tyrosine. Chemical modification of arginine, histidine, serine and cysteine residues of AUL did not affect its activity. Using Far UV CD spectra the estimated secondary structure was 37% α-helix, 25% β-sheet and 38% random contributions. The lectin showed potent mitogenic response towards human lymphocytes. In vitro anti-proliferative assay using 11 human cancer cell lines resulted in 50% inhibition of six cell lines viz. SW-620, HCT-15, SK-N-SH, IMR-32, Colo-205 and HT-29 at 38, 42, 43, 49, 50 and 89 µg/ml, respectively.展开更多
Objective: This study focused on the antibacterial and anti-proliferative activity of extracts from Carica papaya and Cocos nucifera roots. Methodology: The minimum inhibitory concentration and the minimum bactericida...Objective: This study focused on the antibacterial and anti-proliferative activity of extracts from Carica papaya and Cocos nucifera roots. Methodology: The minimum inhibitory concentration and the minimum bactericidal concentration of the extracts on Escherichia coli, Pseudomonas aeruginosa, Streptococcus mutans, and Staphylococcus aureus were deduced by the microdilution method. The anti-biofilm activity was determined on all four strains and anti-quorum sensing activity by inhibition of violacein production in Chromobacterium violaceum. Anti-proliferative activity on prostate cultured cancer cells was evaluated by MTT assay. Sterols and triterpenes were also assayed in this study. Results: The methanolic extract of Carica papaya showed the best anti-biofilm effect with a percentage inhibition of 66.10 ± 1.79. The methanolic extract of Cocos nucifera had the strongest inhibition on the production of quorum sensing (61.42 ± 0.28). In addition, the methanolic extract of Cocos nucifera roots showed the best cytotoxic effect on prostate cancer LNCaP cell lines (IC<sub>50</sub> = 26.98 ± 2.6 μg/mL) and Carica papaya on the PC-3 lines (IC<sub>50</sub> = 127.20 ± 5.99 μg/mL). The extracts were also rich in triterpenes and sterols. Conclusion: This study provides support for the ethnomedical use of Carica papaya and Cocos nucifera roots as an antimicrobial and anticancer.展开更多
The in vitro anti-proliferative activity(pICi,i=hp,ca,hl)of fluoroquinolone(rhodanineα,β-unsaturated ketone)amide compounds,referred to as“fluoroquinolone amide derivatives(FQADs)”towards Hep-3B,Capan-1 and HL60 c...The in vitro anti-proliferative activity(pICi,i=hp,ca,hl)of fluoroquinolone(rhodanineα,β-unsaturated ketone)amide compounds,referred to as“fluoroquinolone amide derivatives(FQADs)”towards Hep-3B,Capan-1 and HL60 cells,was studied by the 3D-QSAR method of comparative molecular field analysis(CoMFA).Based on the training set of 14 compounds,the prediction model was established,which was further verified by the test set of 5 compounds with template molecule included.It is found that steric and electrostatic fields contribute 66.8%and 33.2%to pIChp,61.4%and 38.6%to pICca,and 61.5%and 38.5%to pIChl,respectively.The Rcv 2(i.e,cross-validation coefficient)is 0.324,0.381,and 0.421 for pIChp,pICca,and pIChl,respectively,while the corresponding R2(i.e,non-cross-validation coefficient)all reach 0.999.Then,the models were employed to estimate the activities of the training and test compounds,and the results show that the stability and predictability of developed models are very satisfactory.According to the contour maps of steric and electronic fields,bulky groups linked to 2-,3-,4-positions of phenyl ring,and electropositive groups near the 4-position and electronegative groups far away may increase the anti-proliferative activity.Using the information provided by the 3D contour maps,four new FQADs owing higher antiproliferative activity were designed,but their effectiveness should be further tested by experiments.展开更多
To explore the potential of crabapples as functional food, polyphenols in crabapples and ‘Fuji’ apples were extracted, and the phenolic profile,total polyphenols, antioxidant activity and anti-proliferative activity...To explore the potential of crabapples as functional food, polyphenols in crabapples and ‘Fuji’ apples were extracted, and the phenolic profile,total polyphenols, antioxidant activity and anti-proliferative activity against several human cancer cells were determined. The results indicated that crabapple extracts have more abundant phenols and higher total polyphenols(from 4.46 to 46.63 mg GAE·g-1 DW) compared to ‘Fuji’ apples.Crabapple extracts possessed higher antioxidant activity than apple by DPPH and ABTS analysis. All fruit extracts exhibited inhibitory effects on proliferation in different cancer cells;however, crabapple extracts performed significantly better, with half inhibitory concentration(IC50)values varied from 48.34 μg·m L-1 to 974.81 μg·m L-1 for colon cancer cells SW480, 64.67–1 466.35 μg·m L-1 for stomach cancer cells BGC-803,78.88–910.64 μg·m L-1 for esophageal cancer cells CaEs-17. Besides, the red crabapples had higher antioxidant activity and anti-proliferative activity than yellow fruits. These results showed that crabapples, especially red crabapples, have great potential as a healthy food, as they are rich in phenolic compounds with high antioxidant and anti-proliferative activities to cancer cells.展开更多
Agro-wastes contribute major social,economic,and environmental challenges for food production and circular economy systems.The current increasing demand for clean label food production and use of natural bioactive com...Agro-wastes contribute major social,economic,and environmental challenges for food production and circular economy systems.The current increasing demand for clean label food production and use of natural bioactive compounds could turn these challenges into opportunities providing avenues for proper utilization of agro-wastes to produce valuable products.This study aimed to investigate the potential use of kiwifruit(Actinidia chinensis)leaves as a source of proanthocyanidins(PAs)bioactive phenolic phytochemicals.Kiwifruit leaves PAs were extracted,purified,identified,and evaluated for their antioxidant and anti-proliferative activities.The structural composition of the purified PAs was characterized using HPLC-QTOF-MS/MS and MALDI-TOF-MS.The results showed that purified kiwifruit leaves PAs(PKLPs)comprised mainly procyanidins,propelargonidins,and prodelphindins ranging from dimers to hexamers with(epi)catechin as terminal units and(epi)afzelechin or(epi)gallocatechin as dominant extension units.This study reports the structure of novel PKLPs monomer fractions was unique compared to the PAs that extracted from the other plant sources.The PKLPs exhibited higher phenolic content than the skin and flesh of several kiwifruit cultivars.Moreover,the PKLPs exhibited higher in vitro antioxidant activity in chemical-based(DPPH,ABTS,and FRAP)assays and H2O2-induced injury cell model than ascorbic,Trolox,and catechin(p<0.01).A remarkable dose-dependent anti-proliferation activity(IC_(50)=186.04±2.61μg/mL)against HepG2 cells was observed.In conclusion,this study demonstrated that kiwifruit leaves waste could serve as a sustainable and low-cost source of PAs,a group of multi-functional bioactive compounds that plays a key role in the food and pharmaceutical industries.展开更多
Aim:This study was conducted to assess the in vivo and in vitro anti-tumor effects of diallyl disulfi de(DADS)against Ehrlich ascites carcinoma(EAC)and to suggest its probable mechanism of action.Methods:EAC was induc...Aim:This study was conducted to assess the in vivo and in vitro anti-tumor effects of diallyl disulfi de(DADS)against Ehrlich ascites carcinoma(EAC)and to suggest its probable mechanism of action.Methods:EAC was induced in female mice by intraperitoneal injection of EAC-cells from stock mice.EAC-bearing mice were orally treated with 100 mg/kg body weight for 2 weeks beginning from the 1st day of EAC intraperitoneal transplantation.Cytotoxicity effects of DADS against EAC-cells in vitro were investigated at different concentrations(0,6.25,12.5,25,50,and 100μg/mL)of DADS using trypan blue exclusion assay.Results:Data from this study exhibited a signifi cant decrease in EAC-aliquot volume as well as total and alive EAC-cell number and a marked increase in dead EAC-cell number and percent in EAC-bearing mice treated with DADS as compared with EAC-bearing control.These changes were consistent with increased number of cells which exhibited phenotypic apoptotic signs marked by a decrease in the expression of anti-apoptotic protein Bcl-2,an increase of pro-apoptotic and cell cycle arrest mediator p53 and an elevation of DNA fragmenting indicator terminal deoxynucleotidyl transferase in EAC-bearing mice treated with DADS.In addition,the tumor marker sialic acid level was markedly decreased in plasma and Ehrlich ascites in EAC-bearing mice treated with DADS.In vitro,DADS also produced anti-proliferative and anti-tumor cytotoxic potentials against EAC.Conclusion:DADS may have anti-cancer effects which may be mediated via modulation of apoptosis and cell cycle arrest.展开更多
In this study,novel micro and nanoparticle complexes of Ag(Ⅰ),Ni(Ⅱ),and Pd(Ⅱ)ion with new asymmetrical Schiff base triazole ligand(4-(((3-mercapto-5-(naphthalen-1-ylmethyl)-4H-1,2,4-triazol-4-yl)imino)methyl)phenol...In this study,novel micro and nanoparticle complexes of Ag(Ⅰ),Ni(Ⅱ),and Pd(Ⅱ)ion with new asymmetrical Schiff base triazole ligand(4-(((3-mercapto-5-(naphthalen-1-ylmethyl)-4H-1,2,4-triazol-4-yl)imino)methyl)phenol)were prepared.The Schiff base micro complexes were identified using Fourier-transform infrared spectroscopy(FTIR),Ultraviolet-visible spectroscopy(UV-Vis),flame atomic absorption,elemental analysis C.H.N.S,conductivity measurements and magnetic susceptibility.New nanoparticles Schiff base triazole ligand(4-(((3-mercapto-5-(naphthalen-1-ylmethyl)-4H-1,2,4-triazol-4-yl)imino)methyl)phenol)ligand and Ag(Ⅰ),Ni(Ⅱ)and Pd(Ⅱ)complexes were synthesized as a novel compounds by using sonication method,and were fully characterized by using FTIR,atomic force microscopy(AFM),scanning electron microscope(SEM),and X-ray powder diffraction(XRD).The antioxidant activity of tested compounds was tested using DPPH assay.The effect of synthetic novel compounds on cancer cell line MCF-7 proliferation was measured by MTT assay.The ability of synthetic novel compounds in induction of apotosis was achieved using acridine orange/ethidium bromide(AO/EB)stains.We found that the synthetic novel compounds had the potential to inhibit growth of cancer cell at low concentrations.The effect of synthetic compounds on cell growth and proliferation of MCF-7 cells was associated with cell cycle arrest,and increased apoptosis.Our results showed that the synthetic novel compounds inhibited cancer cell line proliferation with a mechanism of action similar to that of other tubulin inhibitors.In conclusion,the results of this study indicate that synthetic novel compounds represent a new chemo type with a novel mechanisms of action and that it has the potential to be developed for tumor therapy.展开更多
The non-coding RNAs(ncRNAs)are a family of single-stranded RNAs that have become recognized as crucial gene expression regulators in normal and cancer cell biology.The gut microbiota,which consists of several differen...The non-coding RNAs(ncRNAs)are a family of single-stranded RNAs that have become recognized as crucial gene expression regulators in normal and cancer cell biology.The gut microbiota,which consists of several different bacteria,can actively contribute to the regulation of host metabolism,immunity,and inflammation.Roles of ncRNAs and gut microbiota could significantly interact with each other to regulate the growth of various types of cancer.In particular,a causal relationship among ncRNAs,gut microbiota,and immune cells has been shown for their potential importance in the development of breast cancer.Alteration of ncRNA expression and/or gut microbiota profiles could also influence several intracellular signaling pathways with the function of anti-proliferative(APRO)family proteins associated with the malignancy.Targeting ncRNAs and/or APRO family proteins for the treatment of various cancers has been revealed with novel immune therapies.Here,the most recent studies to underline the key role of ncRNAs,APRO family proteins,and gut microbiota in breast cancer progression have been discussed.For more effective breast cancer therapy,it would be imperative to figure out the collective mechanism of ncRNAs,APRO family proteins,and gut microbiota.展开更多
Saposhnikoviae divaricata(Turcz.) Schischk(SD) is a traditional Chinese herb commonly used to treat clinical conditions such as rheumatism and allergic rhinitis. This review article evaluates a collection of works on ...Saposhnikoviae divaricata(Turcz.) Schischk(SD) is a traditional Chinese herb commonly used to treat clinical conditions such as rheumatism and allergic rhinitis. This review article evaluates a collection of works on in vitro and biochemical studies of SD. The discourse on the diverse class of chromones and coumarins in SD offers an insight to the pharmacological effects of these bioactive constituents as anti-inflammatory, analgesic, immunoregulatory, antioxidative, and anti-proliferative agents. It is highlighted that there is a structural relationship between the constituents and bioactive activities, which in effect provides a valid reasoning and reaffirm the use of SD in the treatment of the pathologies in Chinese medicine.展开更多
Aiming to better understand the physiochemical properties of lignite, we select Zhaotong lignite as object and adopt simulation and experiment data to construct its molecular structure. Firstly, the important paramete...Aiming to better understand the physiochemical properties of lignite, we select Zhaotong lignite as object and adopt simulation and experiment data to construct its molecular structure. Firstly, the important parameters including carbon skeleton, valence state and functional group of the sample are obtained by ultimate analysis, 13 C NMR, XPS and Py-GC/MS. Results indicate that the ratio of aromatic carbon and aromatic bridge carbon to surrounding carbon of the sample are 40.32% and 0.14, respectively. Such results imply that the aromatic structure of the sample is dominated by benzene and naphthalene. Moreover, the ratio of aliphatic carbon is 51.55%, and the aliphatic structure is mainly comprised by methyl, methylene, quaternary carbon and oxygen-aliphatic carbon. Oxygen atoms principally exist in ether, carbonyl and carboxyl groups, of which ether accounts for 70.2%. Additionally, the contents of pyridine, pyrrole and quaternary nitrogen are 25.2%, 46.3% and 13.0%, respectively. Based on the aforementioned results, the molecular structure model of Zhaotong lignite is constructed by the method of computer-aided molecular design. Subsequently, the molecular formula of Zhaotong lignite is calculated as C;H;O;N;. Finally, in order to verify the reasonability of the constructed model, the 13 C NMR of the molecular structure model is simulated by employing the basis set of GIAO/6-31G at the Gaussian 09 computing platform. These simulated results agree well with the experimental ones, which suggests that the molecular structure model of Zhaotong lignite is accurate and reasonable.展开更多
Objective: To explore the potential of essential oil, as therapeutic molecule source, from olibanum of Boswellia papyrifera(Burseraceae), leafy stems of Cymbopogon schoenanthus(Poaceae) and Croton zambesicus(Euphorbia...Objective: To explore the potential of essential oil, as therapeutic molecule source, from olibanum of Boswellia papyrifera(Burseraceae), leafy stems of Cymbopogon schoenanthus(Poaceae) and Croton zambesicus(Euphorbiaceae) and rhizome of Cyperus rotundus(Cyperaceae) found in Sudan. Respective essential oil was evaluated for antiproliferative, antibacterial and antioxidant activity. Methods: Essential oils were extracted by hydrodistillation and then analysed by gas chromatography coupled to mass spectrometry(GCMS). Anti-proliferative activity was determined against human cell lines(MCF7 and MDAMB231, HT29 and HCT116) by the thiazolyl blue tetrazolium bromide(MTT) procedure. Antioxidant activity was evaluated by diphenyl 2 pycril hydrazil(DPPH) assay. Antibacterial activity was determined against two Gram-positive and two Gram-negative bacteria by microdilution method. Results: The essential oil from olibanum of Boswellia papyriferacontained mainly alcohol and ester derivatives(46.82%) while monoterpenes(69.84%) dominated in Corton zambesicus oil. Sesquiterpenes were the most highly represented classes of terpene derivatives in Cyperus schoenanthus(71.59%) and Cyperus rotundus(44.26%). Oil of Cymbopogon schoenanthus revealed the best anti-proliferative activity against HCT116 cell line with IC50 value at(19.1 ± 2.0) μg/m L. Oil of Croton zambesicus showed the best antioxidant activity [EC50(4.20 ± 0.19) mg/m L]. All oils showed good antibacterial activity against Escherichia coli, Bacillus subtilis and Staphylococcus aureus with minimum inhibitory concentration(MIC) value ranged from 16 to 250 μg/m L. Conclusions: The results suggest that the essential oils of these plants could be used as a source of natural anti-proliferative, antioxidant and antibacterial agents.展开更多
Objective: To examine the proapoptotic properties of Oroxylum indicum methanol extract on cervical cancer cells. Methods: Methylene blue assay was used to determine the IC50 value of the extract. Western blotting assa...Objective: To examine the proapoptotic properties of Oroxylum indicum methanol extract on cervical cancer cells. Methods: Methylene blue assay was used to determine the IC50 value of the extract. Western blotting assays were done to analyze the expression of HPV oncoproteins (HPV18 E6 and E7) and apoptotic molecules (caspase-3 and caspase-8). Reverse transcriptase PCR assays were performed to determine genetic alteration of tumor suppressors p53 and pRb and apoptosis markers Fas and FasL. Enzyme-linked immunosorbent assay (ELISA) was done to determine the expression of cytokine levels (IL-6 and IL-12). Results: The determination of IC50 value indicated a higher anti-proliferative activity of the extract compared to cisplatin. After 24 hours of treatment, Western blot analysis showed that treated HeLa cells exhibited a significant down-regulation of HPV18 oncoproteins E6 and E7, and a significant induction of caspase-8 and caspase-3 activation level. Meanwhile, the mRNA expressions of p53, pRb, Fas and FasL were significantly upregulated in treated cells. Moreover, ELISA showed an increased IL-12 and decreased IL-6 production after Oroxylum indicum treatment. Conclusions: The methanol extract of Oroxylum indicum has an anti-proliferative activity and proapoptotic potential. It induces localized-immunity improvements by altering cytokine production in HPV-positive cervical cancer cells.展开更多
Prodigiosin is a red pigment with a pyrrolylpyrromethane skeleton.It is mainly produced by bacterial strains belonging to the Serratia genus,but also by some other genera,including Streptomyces and Vibrio.Within the g...Prodigiosin is a red pigment with a pyrrolylpyrromethane skeleton.It is mainly produced by bacterial strains belonging to the Serratia genus,but also by some other genera,including Streptomyces and Vibrio.Within the genus Serratia,the pigment is generally produced as a virulence factor.However,it also has many important beneficial biological activities such as immunosuppressive and anti-proliferative activities.Moreover,the pigment has many industrial applications in textile and cosmetics.In this mini-review,we discuss the genetic and molecular mechanisms supporting prodigiosin synthesis and production from the Serratia genus,as well as its potential applications.展开更多
Three matrine-derived alkaloids, alopecuroidine A(1), alopecuroidine B(2 a) and alopecuroidine C(2 b)were isolated from the seeds of Sophora alopecuroides. Their structures were elucidated by extensive spectroscopic a...Three matrine-derived alkaloids, alopecuroidine A(1), alopecuroidine B(2 a) and alopecuroidine C(2 b)were isolated from the seeds of Sophora alopecuroides. Their structures were elucidated by extensive spectroscopic analyses and X-ray diffraction. Three compounds possess an unprecedented rearranged fused7/6/5/6 tetracyclic skeleton with a diazacycloheptane structure. Their plausible biosynthetic pathway was also proposed. The anti-proliferative activities of compounds 1 and 2 a were examined by the MTT assay.Compound 1 inhibited the viability of human lung cancer A549 cells, having a half maximal inhibitory concentration(IC50) of 7.58 ± 2.47 μmol/L at 72 h. The flow cytometric analysis suggested that 1 inhibited A549 cell growth by inducing apoptosis and cell-cycle arrest. Additionally, 1 induced the loss of mitochondrial membrane potential, elevated intracellular reactive oxygen species, increased the Bax/Bcl-2 ratio, stimulated cleaved-caspase-3 and P53 protein levels, and suppressed the pro-caspase-3 level. Thus,1 appeared to induce A549 cells apoptosis through a mitochondria-mediated apoptotic pathway.展开更多
Objective: To evaluate the antimicrobial, antioxidant, cytotoxicity and anticancer activity of fractions from Jatropha zeyheri roots and to explore the phytochemical profile of the most biologically active fraction.Me...Objective: To evaluate the antimicrobial, antioxidant, cytotoxicity and anticancer activity of fractions from Jatropha zeyheri roots and to explore the phytochemical profile of the most biologically active fraction.Methods: Fractions from Jatropha zeyheri ethyl acetate extract were investigated for antimicrobial activity against a plethora of pathogenic microorganisms of different origins. The cytotoxicity studies of fractions were evaluated in vitro using tetrazolium-based calorimetric assay against human dermal fibroblast, colon adenocarcinoma(Caco-2), breast cancer(MCF-7) and lung cancer(A547) cell lines. The anti-oxidant activity of fractions was determined in vitro against 2,2-diphenyl-1-picrylhydrazyl(DPPH), 2,2′-azino-bis-(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt(ABTS) and chelation of iron(Fe2+). Gas chromatography mass spectrometry analysis was performed to detect phytochemical constituents in fraction with potent biological activity.Results: Fraction 2 of Jatropha zeyheri roots exhibited the lowest minimum inhibitory concentration of 40 μg/mL against Klebsiella pneumoniae and 80 μg/mL against Candida albicans, Staphylococcus aureus and Mycoplasma hominis. The fractions revealed some varying degrees of cytotoxicity against human dermal fibroblasts yielding LC50 values ranging from 28.96 to 166.52 μg/mL. Fraction 3 exhibited the highest selectivity index value of 2.08 against Klebsiella pneumoniae. Moreover, fraction 2 selectively inhibited the growth of Caco-2 with LC50 of 8.83 μg/mL, compared to other cancerous cell lines. Fraction 2 of Jatropha zeyheri further exhibited IC50 of 19.66, 22.63 and 1.82 μg/mL against DPPH, ABTS and Fe2+, respectively. Gas chromatography mass spectrometry analysis revealed the presence of cyclotetracosane(10.08%), 9-hexacosene(9.40%), hexadecanoic acid(3.90%),(Z)-9-octadecenamide(3.63%), octacosane(2.27%), 11-n-decylheneicosane(2.23%), ethyl vallesiachotamate(2.17%), heneicosanoic acid(2.10%), and octadecanoic acid(2.08%) in fraction 2 of Jatropha zeyheri.Conclusions: These identified compounds, particularly cyclotetracosane(hydrocarbon), may well explain the biological activity of fraction 2 of Jatropha zeyheri, which possesses higher biological activity than other fractions. These compounds can be further investigated for use in treating various bacterial and fungal opportunistic infections associated with HIV-AIDS and related cancers.展开更多
基金the Scientific Research and Laboratory Center of the Second Affiliated Hospital of Xi'an Jiaotong University for the technical support
文摘AIM： To evaluate the inhibitive effect of olmesartan to fibroblast proliferation and the anti-scarring effect in Tenon＇s capsule, both in vitro and in vivo.· METHODS： Human primary Tenon＇s capsule fibroblasts were cultured in vitro, treated with up titrating concentrations of olmesartan. The rate of inhibition was tested with methyl thiazol tetrazolium（MTT） method.Real-time PCR was performed to analyze changes in m RNA expressions of the fibrosis-related factors： matrix metalloproteinase-2（MMP-2）, tissue inhibitor of metalloproteinase（TIMP-1,2） and proliferating cell nuclear antigen（PCNA）. Thirty rabbits were divided into5 groups（3, 7, 14, 21, and 28d）. A rabbit conjunctiva flap model was created in each eye. Olmesartan solution was injected subconjunctivally and then evaluated its anti-proliferation and anti-fibrosis effects through the histological morphology and immunohistochemistry of MMP-2 and PCNA in each group. Only the 7d group was treated with Masson＇s trichrome to compare the neovascularization in the subconjunctiva area.·RESULTS： In vitro, cultured Tenon＇s capsule human fibroblasts showed a dose dependent inhibition by olmesartan in MTT. Olmesartan reduced m RNA expressions of MMP-2 and PCNA but increased m RNA expressions of TIMP-1 and TIMP-2. In vivo, the rabbit eyes treated with olmesartan at 3rd, 7th, 14 thand 21stdays demonstrated a significant reduced expressions of MMP-2 and PCNA compared with control eye, no significant difference observed in 28 thday group. The cellular proliferation and neovascularization was suppressed by olmesartan in Masson＇s trichrome observation.·CONCLUSION： By inhibiting fibroblasts in vitro and in vivo, olmesartan prevents the proliferation and activity of fibroblasts in scar tissue formation, which might benefit glaucoma filtering surgery.
基金Supported by the National Key Technology Research & Development Program of the 11th Five Year Plan of China (No. 2006BAD30B01)the National Natural Science Foundation of China (No. 30871945)
文摘In this study, we evaluated the anti-proliferative activity of phlorotannins derived from brown algae Laminariajaponica Aresch extracts on the human hepatocellular carcinoma cell （BEL-7402） and on routine leukemic cells （P388） by MTT assay. Cells were incubated with 100 μg/mL of the phlorotannin extract （PE） for 48 h. The inhibitory rate of PE on BEL-7402 and P388 cells was 30.20±1.16% and 43.44±1.86%, respectively, and the half-inhibitory concentration of PE （IC50） on P388 and BEL-7402 cells was 120 μg/mL and 〉200 μg/mL, respectively. Microscopic observation shows that the morphologic features of tumor cells treated with PE and 5-fluorouracil are markedly different from the normal control group. The inhibitory rate of fraction A2 isolated from PE by sephadex LH-20 for BEL-7402 and P388 cells at the sample concentration of 70.42 μg/mL was 61.96±7.02% and 40.47±8.70%, respectively. The apoptosis peak for fraction A2 was the most profound of all fractions used in the flow cytometry assay. The results indicate that the anti-proliferative of this algal extract is associated with the total phlorotannin content.
基金supported by project MARBIOTECH,grant NORTE-07-0124-FEDER-000047-BPD-2013-06partially funded by project MARBIOTECH(reference NORTE-070124-FEDER-000047)+6 种基金co-financed by the North Portugal Regional Operational Programme(ON.2-O Novo Norte)the National Strategic Reference Framework(NSRF)the European Regional Development Fund(ERDF)the ERDF,through the Competitiveness and TradeExpansion Program(COMPETE)national funds provided by the Foundation for Science and Technology(FCT)project PEst-C/MARL-1A0015/2013the financial aid provided by the Master of Marine Sciences-Marine Recourses,of the Institute of Biomedical Sciences Abel Salazar,University of Porto
文摘Objective:To evaluate the in vitro anticancer activity of crude ethyl acetate extracts of the culture of four marine-derived fungi Aspergillus similanensis KUFA 0013(E1),Neosartorya paulistemis KUFC 7897(E2),Neosartorya siamensis KUFA 0017(E4) and Talaromyces trachyspermus KUFC 0021(E3) on a panel of seven human cancer cell lines.Methods:Effects on cell proliferation,induction of DNA damage and cell death were assessed by MTT and clonogenic assays,comet assay and nuclear condensation assay,respectively.Results:The proliferation of HepG2,HCTl 16 and A375 cells decreased after incubation with the extracts E2 and E4.The anti-proliterative effect was confirmed by morphologic alterations and by clonogenic assay.Both extracts also induced cell death in HepG2 and HCT116 cells.Doxorubicin was used as a positive control and showed in vitro anticancer activity.Conclusions:This study demonstrated,for the first time,that extracts of Neosartorya paulistensis and Neosartorya siamensis have selective anti-proliferative and cell death activities in HepG2,HCT16 and A375 cells.The bioactivity of these extracts suggests a potential for biotechnological applications and substantiates that both should be further considered for the elucidation of the molecular targets and signal transduction pathways involved.
基金supported by the National Institutes of Health Grant SC1DK084343(to MAB)by Mass Spectrometry Research and Education Center must cite funding from NIH S10 OD021758-01A1.
文摘Backgorund:Fruits and seed extracts of Annona montana have significant cytotoxic potential in several cancer cells.This study evaluates the effect of A.montana leaves hexane extract on several signaling cascades and gene expression in metastatic breast cancer cells upon insulin-like growth factor-1(IGF-1)stimulation.Methods:MTT assay was performed to determine the proliferation of cancer cells.Propidium iodide staining and flow cytometry analysis of Annexin V binding was utilized to measure the progression of the cell cycle and the induction of apoptosis.Protein expression and phosphorylation were determined by western blotting analysis to examine the underlying cellular mechanism triggered upon treatment with A.montana leaves hexane extract.Results:A.montana leaves hexane(subfraction V)blocked the constitutive stimulation of the PI3K/mTOR signaling pathways.This inhibitory effect was associated with apoptosis induction as evidenced by the positivity with Annexin V and terminal deoxynucleotidyl transferase dUTP nick end labeling(TUNNEL)staining,activation of caspase-3,and cleavage of PPAR.It also limited the expression of various downstream genes that regulate proliferation,survival,metastasis,and angiogenesis(i.e.,cyclin D1,survivin,COX-2,and VEGF).It increased the expression of p53 and p21.Interestingly,we also observed that this extract blocked the activation of AKT and ERK without affecting the phosphorylation of the IGF-1 receptor and activation of Ras upon IGF-1 stimulation.Conclusion:Our study indicates that A.montana leaves(sub-fraction V)extract exhibits a selective anti-proliferative and proapoptotic effect on the metastatic MDA-MB-231 breast cancer cells through the involvement of PI3K/AKT/mTOR/S6K1 pathways.
文摘A series of novel derivatives of indirubin were synthesized and evaluated for their anti-proliferative activity against human cancer cell lines of SGC7901,A549,HL-60,SK-BR-3 and HCT116.Most of the compounds displayed more potent activity than Sunitinib.In addition,the derivatives showed improved water solubility,which may be favorable to their pharmacokinetic performances.
文摘Lectins are the carbohydrate-binding proteins of non-immune origin which have been the subject of intense investigation over the last few decades owing to the variety of interesting biological properties. Most of the lectins which have been purified and characterized from plants have been obtained from dicotyledons. In the present study a lectin was purified from tubers of a monocot plant Arisaema utile (AUL) Schott by affinity chromatography on asialofetuin-linked amino activated silica beads. AUL gave a single band in SDS-PAGE at pH 8.3 corresponding to subunit Mr 13.5 kDa. The native molecular mass of AUL was 54 kDa suggesting a homotetrameric structure. AUL gave multiple bands in isoelectric focusing and in native PAGE at pH 8.3. AUL was inhibited by N-acetyl-D-lactosamine (Lac NAc), a disaccharide and asialofetuin, a complex desialylated serum glycoprotein. When treated with denaturing agents, the lectin was stable in the presence of urea (3 M), thiourea (4 M) and guanidine HCl (4 M). AUL was a glycoprotein with a carbohydrate content of 1.2%. Complete loss of activity was observed upon modification of tryptophan residues of the lectin. The activity was reduced to 25% after modification of tyrosine. Chemical modification of arginine, histidine, serine and cysteine residues of AUL did not affect its activity. Using Far UV CD spectra the estimated secondary structure was 37% α-helix, 25% β-sheet and 38% random contributions. The lectin showed potent mitogenic response towards human lymphocytes. In vitro anti-proliferative assay using 11 human cancer cell lines resulted in 50% inhibition of six cell lines viz. SW-620, HCT-15, SK-N-SH, IMR-32, Colo-205 and HT-29 at 38, 42, 43, 49, 50 and 89 &#181;g/ml, respectively.
文摘Objective: This study focused on the antibacterial and anti-proliferative activity of extracts from Carica papaya and Cocos nucifera roots. Methodology: The minimum inhibitory concentration and the minimum bactericidal concentration of the extracts on Escherichia coli, Pseudomonas aeruginosa, Streptococcus mutans, and Staphylococcus aureus were deduced by the microdilution method. The anti-biofilm activity was determined on all four strains and anti-quorum sensing activity by inhibition of violacein production in Chromobacterium violaceum. Anti-proliferative activity on prostate cultured cancer cells was evaluated by MTT assay. Sterols and triterpenes were also assayed in this study. Results: The methanolic extract of Carica papaya showed the best anti-biofilm effect with a percentage inhibition of 66.10 ± 1.79. The methanolic extract of Cocos nucifera had the strongest inhibition on the production of quorum sensing (61.42 ± 0.28). In addition, the methanolic extract of Cocos nucifera roots showed the best cytotoxic effect on prostate cancer LNCaP cell lines (IC<sub>50</sub> = 26.98 ± 2.6 μg/mL) and Carica papaya on the PC-3 lines (IC<sub>50</sub> = 127.20 ± 5.99 μg/mL). The extracts were also rich in triterpenes and sterols. Conclusion: This study provides support for the ethnomedical use of Carica papaya and Cocos nucifera roots as an antimicrobial and anticancer.
基金supported by the National Natural Science Foundation of China (21676292, 21075138)special fund of State Key Laboratory of Structure Chemistry (2016028)
文摘The in vitro anti-proliferative activity(pICi,i=hp,ca,hl)of fluoroquinolone(rhodanineα,β-unsaturated ketone)amide compounds,referred to as“fluoroquinolone amide derivatives(FQADs)”towards Hep-3B,Capan-1 and HL60 cells,was studied by the 3D-QSAR method of comparative molecular field analysis(CoMFA).Based on the training set of 14 compounds,the prediction model was established,which was further verified by the test set of 5 compounds with template molecule included.It is found that steric and electrostatic fields contribute 66.8%and 33.2%to pIChp,61.4%and 38.6%to pICca,and 61.5%and 38.5%to pIChl,respectively.The Rcv 2(i.e,cross-validation coefficient)is 0.324,0.381,and 0.421 for pIChp,pICca,and pIChl,respectively,while the corresponding R2(i.e,non-cross-validation coefficient)all reach 0.999.Then,the models were employed to estimate the activities of the training and test compounds,and the results show that the stability and predictability of developed models are very satisfactory.According to the contour maps of steric and electronic fields,bulky groups linked to 2-,3-,4-positions of phenyl ring,and electropositive groups near the 4-position and electronegative groups far away may increase the anti-proliferative activity.Using the information provided by the 3D contour maps,four new FQADs owing higher antiproliferative activity were designed,but their effectiveness should be further tested by experiments.
基金supported by the National Natural Science Foundation of China (31570697)Basic Research Foundation of Northwest A&F University (Z109021563)
文摘To explore the potential of crabapples as functional food, polyphenols in crabapples and ‘Fuji’ apples were extracted, and the phenolic profile,total polyphenols, antioxidant activity and anti-proliferative activity against several human cancer cells were determined. The results indicated that crabapple extracts have more abundant phenols and higher total polyphenols(from 4.46 to 46.63 mg GAE·g-1 DW) compared to ‘Fuji’ apples.Crabapple extracts possessed higher antioxidant activity than apple by DPPH and ABTS analysis. All fruit extracts exhibited inhibitory effects on proliferation in different cancer cells;however, crabapple extracts performed significantly better, with half inhibitory concentration(IC50)values varied from 48.34 μg·m L-1 to 974.81 μg·m L-1 for colon cancer cells SW480, 64.67–1 466.35 μg·m L-1 for stomach cancer cells BGC-803,78.88–910.64 μg·m L-1 for esophageal cancer cells CaEs-17. Besides, the red crabapples had higher antioxidant activity and anti-proliferative activity than yellow fruits. These results showed that crabapples, especially red crabapples, have great potential as a healthy food, as they are rich in phenolic compounds with high antioxidant and anti-proliferative activities to cancer cells.
基金This study was supported by the National Key Research and Development Program of China(grant no:2017YFD0400704).
文摘Agro-wastes contribute major social,economic,and environmental challenges for food production and circular economy systems.The current increasing demand for clean label food production and use of natural bioactive compounds could turn these challenges into opportunities providing avenues for proper utilization of agro-wastes to produce valuable products.This study aimed to investigate the potential use of kiwifruit(Actinidia chinensis)leaves as a source of proanthocyanidins(PAs)bioactive phenolic phytochemicals.Kiwifruit leaves PAs were extracted,purified,identified,and evaluated for their antioxidant and anti-proliferative activities.The structural composition of the purified PAs was characterized using HPLC-QTOF-MS/MS and MALDI-TOF-MS.The results showed that purified kiwifruit leaves PAs(PKLPs)comprised mainly procyanidins,propelargonidins,and prodelphindins ranging from dimers to hexamers with(epi)catechin as terminal units and(epi)afzelechin or(epi)gallocatechin as dominant extension units.This study reports the structure of novel PKLPs monomer fractions was unique compared to the PAs that extracted from the other plant sources.The PKLPs exhibited higher phenolic content than the skin and flesh of several kiwifruit cultivars.Moreover,the PKLPs exhibited higher in vitro antioxidant activity in chemical-based(DPPH,ABTS,and FRAP)assays and H2O2-induced injury cell model than ascorbic,Trolox,and catechin(p<0.01).A remarkable dose-dependent anti-proliferation activity(IC_(50)=186.04±2.61μg/mL)against HepG2 cells was observed.In conclusion,this study demonstrated that kiwifruit leaves waste could serve as a sustainable and low-cost source of PAs,a group of multi-functional bioactive compounds that plays a key role in the food and pharmaceutical industries.
文摘Aim:This study was conducted to assess the in vivo and in vitro anti-tumor effects of diallyl disulfi de(DADS)against Ehrlich ascites carcinoma(EAC)and to suggest its probable mechanism of action.Methods:EAC was induced in female mice by intraperitoneal injection of EAC-cells from stock mice.EAC-bearing mice were orally treated with 100 mg/kg body weight for 2 weeks beginning from the 1st day of EAC intraperitoneal transplantation.Cytotoxicity effects of DADS against EAC-cells in vitro were investigated at different concentrations(0,6.25,12.5,25,50,and 100μg/mL)of DADS using trypan blue exclusion assay.Results:Data from this study exhibited a signifi cant decrease in EAC-aliquot volume as well as total and alive EAC-cell number and a marked increase in dead EAC-cell number and percent in EAC-bearing mice treated with DADS as compared with EAC-bearing control.These changes were consistent with increased number of cells which exhibited phenotypic apoptotic signs marked by a decrease in the expression of anti-apoptotic protein Bcl-2,an increase of pro-apoptotic and cell cycle arrest mediator p53 and an elevation of DNA fragmenting indicator terminal deoxynucleotidyl transferase in EAC-bearing mice treated with DADS.In addition,the tumor marker sialic acid level was markedly decreased in plasma and Ehrlich ascites in EAC-bearing mice treated with DADS.In vitro,DADS also produced anti-proliferative and anti-tumor cytotoxic potentials against EAC.Conclusion:DADS may have anti-cancer effects which may be mediated via modulation of apoptosis and cell cycle arrest.
文摘In this study,novel micro and nanoparticle complexes of Ag(Ⅰ),Ni(Ⅱ),and Pd(Ⅱ)ion with new asymmetrical Schiff base triazole ligand(4-(((3-mercapto-5-(naphthalen-1-ylmethyl)-4H-1,2,4-triazol-4-yl)imino)methyl)phenol)were prepared.The Schiff base micro complexes were identified using Fourier-transform infrared spectroscopy(FTIR),Ultraviolet-visible spectroscopy(UV-Vis),flame atomic absorption,elemental analysis C.H.N.S,conductivity measurements and magnetic susceptibility.New nanoparticles Schiff base triazole ligand(4-(((3-mercapto-5-(naphthalen-1-ylmethyl)-4H-1,2,4-triazol-4-yl)imino)methyl)phenol)ligand and Ag(Ⅰ),Ni(Ⅱ)and Pd(Ⅱ)complexes were synthesized as a novel compounds by using sonication method,and were fully characterized by using FTIR,atomic force microscopy(AFM),scanning electron microscope(SEM),and X-ray powder diffraction(XRD).The antioxidant activity of tested compounds was tested using DPPH assay.The effect of synthetic novel compounds on cancer cell line MCF-7 proliferation was measured by MTT assay.The ability of synthetic novel compounds in induction of apotosis was achieved using acridine orange/ethidium bromide(AO/EB)stains.We found that the synthetic novel compounds had the potential to inhibit growth of cancer cell at low concentrations.The effect of synthetic compounds on cell growth and proliferation of MCF-7 cells was associated with cell cycle arrest,and increased apoptosis.Our results showed that the synthetic novel compounds inhibited cancer cell line proliferation with a mechanism of action similar to that of other tubulin inhibitors.In conclusion,the results of this study indicate that synthetic novel compounds represent a new chemo type with a novel mechanisms of action and that it has the potential to be developed for tumor therapy.
文摘The non-coding RNAs(ncRNAs)are a family of single-stranded RNAs that have become recognized as crucial gene expression regulators in normal and cancer cell biology.The gut microbiota,which consists of several different bacteria,can actively contribute to the regulation of host metabolism,immunity,and inflammation.Roles of ncRNAs and gut microbiota could significantly interact with each other to regulate the growth of various types of cancer.In particular,a causal relationship among ncRNAs,gut microbiota,and immune cells has been shown for their potential importance in the development of breast cancer.Alteration of ncRNA expression and/or gut microbiota profiles could also influence several intracellular signaling pathways with the function of anti-proliferative(APRO)family proteins associated with the malignancy.Targeting ncRNAs and/or APRO family proteins for the treatment of various cancers has been revealed with novel immune therapies.Here,the most recent studies to underline the key role of ncRNAs,APRO family proteins,and gut microbiota in breast cancer progression have been discussed.For more effective breast cancer therapy,it would be imperative to figure out the collective mechanism of ncRNAs,APRO family proteins,and gut microbiota.
文摘Saposhnikoviae divaricata(Turcz.) Schischk(SD) is a traditional Chinese herb commonly used to treat clinical conditions such as rheumatism and allergic rhinitis. This review article evaluates a collection of works on in vitro and biochemical studies of SD. The discourse on the diverse class of chromones and coumarins in SD offers an insight to the pharmacological effects of these bioactive constituents as anti-inflammatory, analgesic, immunoregulatory, antioxidative, and anti-proliferative agents. It is highlighted that there is a structural relationship between the constituents and bioactive activities, which in effect provides a valid reasoning and reaffirm the use of SD in the treatment of the pathologies in Chinese medicine.
基金supported by the National Natural Science Foundation of China (21766013)Analysis and Testing Foundation of Kunming University of Science and Technology (2020M20192208021)
文摘Aiming to better understand the physiochemical properties of lignite, we select Zhaotong lignite as object and adopt simulation and experiment data to construct its molecular structure. Firstly, the important parameters including carbon skeleton, valence state and functional group of the sample are obtained by ultimate analysis, 13 C NMR, XPS and Py-GC/MS. Results indicate that the ratio of aromatic carbon and aromatic bridge carbon to surrounding carbon of the sample are 40.32% and 0.14, respectively. Such results imply that the aromatic structure of the sample is dominated by benzene and naphthalene. Moreover, the ratio of aliphatic carbon is 51.55%, and the aliphatic structure is mainly comprised by methyl, methylene, quaternary carbon and oxygen-aliphatic carbon. Oxygen atoms principally exist in ether, carbonyl and carboxyl groups, of which ether accounts for 70.2%. Additionally, the contents of pyridine, pyrrole and quaternary nitrogen are 25.2%, 46.3% and 13.0%, respectively. Based on the aforementioned results, the molecular structure model of Zhaotong lignite is constructed by the method of computer-aided molecular design. Subsequently, the molecular formula of Zhaotong lignite is calculated as C;H;O;N;. Finally, in order to verify the reasonability of the constructed model, the 13 C NMR of the molecular structure model is simulated by employing the basis set of GIAO/6-31G at the Gaussian 09 computing platform. These simulated results agree well with the experimental ones, which suggests that the molecular structure model of Zhaotong lignite is accurate and reasonable.
文摘Objective: To explore the potential of essential oil, as therapeutic molecule source, from olibanum of Boswellia papyrifera(Burseraceae), leafy stems of Cymbopogon schoenanthus(Poaceae) and Croton zambesicus(Euphorbiaceae) and rhizome of Cyperus rotundus(Cyperaceae) found in Sudan. Respective essential oil was evaluated for antiproliferative, antibacterial and antioxidant activity. Methods: Essential oils were extracted by hydrodistillation and then analysed by gas chromatography coupled to mass spectrometry(GCMS). Anti-proliferative activity was determined against human cell lines(MCF7 and MDAMB231, HT29 and HCT116) by the thiazolyl blue tetrazolium bromide(MTT) procedure. Antioxidant activity was evaluated by diphenyl 2 pycril hydrazil(DPPH) assay. Antibacterial activity was determined against two Gram-positive and two Gram-negative bacteria by microdilution method. Results: The essential oil from olibanum of Boswellia papyriferacontained mainly alcohol and ester derivatives(46.82%) while monoterpenes(69.84%) dominated in Corton zambesicus oil. Sesquiterpenes were the most highly represented classes of terpene derivatives in Cyperus schoenanthus(71.59%) and Cyperus rotundus(44.26%). Oil of Cymbopogon schoenanthus revealed the best anti-proliferative activity against HCT116 cell line with IC50 value at(19.1 ± 2.0) μg/m L. Oil of Croton zambesicus showed the best antioxidant activity [EC50(4.20 ± 0.19) mg/m L]. All oils showed good antibacterial activity against Escherichia coli, Bacillus subtilis and Staphylococcus aureus with minimum inhibitory concentration(MIC) value ranged from 16 to 250 μg/m L. Conclusions: The results suggest that the essential oils of these plants could be used as a source of natural anti-proliferative, antioxidant and antibacterial agents.
基金supported by Fundamental Research Grant Scheme Grant 203/PPSK/6171191
文摘Objective: To examine the proapoptotic properties of Oroxylum indicum methanol extract on cervical cancer cells. Methods: Methylene blue assay was used to determine the IC50 value of the extract. Western blotting assays were done to analyze the expression of HPV oncoproteins (HPV18 E6 and E7) and apoptotic molecules (caspase-3 and caspase-8). Reverse transcriptase PCR assays were performed to determine genetic alteration of tumor suppressors p53 and pRb and apoptosis markers Fas and FasL. Enzyme-linked immunosorbent assay (ELISA) was done to determine the expression of cytokine levels (IL-6 and IL-12). Results: The determination of IC50 value indicated a higher anti-proliferative activity of the extract compared to cisplatin. After 24 hours of treatment, Western blot analysis showed that treated HeLa cells exhibited a significant down-regulation of HPV18 oncoproteins E6 and E7, and a significant induction of caspase-8 and caspase-3 activation level. Meanwhile, the mRNA expressions of p53, pRb, Fas and FasL were significantly upregulated in treated cells. Moreover, ELISA showed an increased IL-12 and decreased IL-6 production after Oroxylum indicum treatment. Conclusions: The methanol extract of Oroxylum indicum has an anti-proliferative activity and proapoptotic potential. It induces localized-immunity improvements by altering cytokine production in HPV-positive cervical cancer cells.
文摘Prodigiosin is a red pigment with a pyrrolylpyrromethane skeleton.It is mainly produced by bacterial strains belonging to the Serratia genus,but also by some other genera,including Streptomyces and Vibrio.Within the genus Serratia,the pigment is generally produced as a virulence factor.However,it also has many important beneficial biological activities such as immunosuppressive and anti-proliferative activities.Moreover,the pigment has many industrial applications in textile and cosmetics.In this mini-review,we discuss the genetic and molecular mechanisms supporting prodigiosin synthesis and production from the Serratia genus,as well as its potential applications.
基金supported by grants from CAMS Innovation Fund for Medical Sciences (No. 2016-I2M-1-010, China)the Drug Innovation Major Project (No. 2018ZX09711001-008, China)。
文摘Three matrine-derived alkaloids, alopecuroidine A(1), alopecuroidine B(2 a) and alopecuroidine C(2 b)were isolated from the seeds of Sophora alopecuroides. Their structures were elucidated by extensive spectroscopic analyses and X-ray diffraction. Three compounds possess an unprecedented rearranged fused7/6/5/6 tetracyclic skeleton with a diazacycloheptane structure. Their plausible biosynthetic pathway was also proposed. The anti-proliferative activities of compounds 1 and 2 a were examined by the MTT assay.Compound 1 inhibited the viability of human lung cancer A549 cells, having a half maximal inhibitory concentration(IC50) of 7.58 ± 2.47 μmol/L at 72 h. The flow cytometric analysis suggested that 1 inhibited A549 cell growth by inducing apoptosis and cell-cycle arrest. Additionally, 1 induced the loss of mitochondrial membrane potential, elevated intracellular reactive oxygen species, increased the Bax/Bcl-2 ratio, stimulated cleaved-caspase-3 and P53 protein levels, and suppressed the pro-caspase-3 level. Thus,1 appeared to induce A549 cells apoptosis through a mitochondria-mediated apoptotic pathway.
文摘Objective: To evaluate the antimicrobial, antioxidant, cytotoxicity and anticancer activity of fractions from Jatropha zeyheri roots and to explore the phytochemical profile of the most biologically active fraction.Methods: Fractions from Jatropha zeyheri ethyl acetate extract were investigated for antimicrobial activity against a plethora of pathogenic microorganisms of different origins. The cytotoxicity studies of fractions were evaluated in vitro using tetrazolium-based calorimetric assay against human dermal fibroblast, colon adenocarcinoma(Caco-2), breast cancer(MCF-7) and lung cancer(A547) cell lines. The anti-oxidant activity of fractions was determined in vitro against 2,2-diphenyl-1-picrylhydrazyl(DPPH), 2,2′-azino-bis-(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt(ABTS) and chelation of iron(Fe2+). Gas chromatography mass spectrometry analysis was performed to detect phytochemical constituents in fraction with potent biological activity.Results: Fraction 2 of Jatropha zeyheri roots exhibited the lowest minimum inhibitory concentration of 40 μg/mL against Klebsiella pneumoniae and 80 μg/mL against Candida albicans, Staphylococcus aureus and Mycoplasma hominis. The fractions revealed some varying degrees of cytotoxicity against human dermal fibroblasts yielding LC50 values ranging from 28.96 to 166.52 μg/mL. Fraction 3 exhibited the highest selectivity index value of 2.08 against Klebsiella pneumoniae. Moreover, fraction 2 selectively inhibited the growth of Caco-2 with LC50 of 8.83 μg/mL, compared to other cancerous cell lines. Fraction 2 of Jatropha zeyheri further exhibited IC50 of 19.66, 22.63 and 1.82 μg/mL against DPPH, ABTS and Fe2+, respectively. Gas chromatography mass spectrometry analysis revealed the presence of cyclotetracosane(10.08%), 9-hexacosene(9.40%), hexadecanoic acid(3.90%),(Z)-9-octadecenamide(3.63%), octacosane(2.27%), 11-n-decylheneicosane(2.23%), ethyl vallesiachotamate(2.17%), heneicosanoic acid(2.10%), and octadecanoic acid(2.08%) in fraction 2 of Jatropha zeyheri.Conclusions: These identified compounds, particularly cyclotetracosane(hydrocarbon), may well explain the biological activity of fraction 2 of Jatropha zeyheri, which possesses higher biological activity than other fractions. These compounds can be further investigated for use in treating various bacterial and fungal opportunistic infections associated with HIV-AIDS and related cancers.
