As a member of the curcuminoid compound family,curcumin(Cur)has many interesting therapeutic properties.However,its low aqueous solubility and stability have resulted in poor bioavailability and restricted clinical ef...As a member of the curcuminoid compound family,curcumin(Cur)has many interesting therapeutic properties.However,its low aqueous solubility and stability have resulted in poor bioavailability and restricted clinical efficacy.Based on size matching,β-cyclodextrin polymer(β-CDP),with its hydrophilic polymer chains and hydrophobic cavities,can form an inclusion complex with Cur.To improve the water solubility and stability of Cur,a simple and eco-friendly grinding method was designed to formβ-CDP inclusion complexes.According to the Boltzmann-Hamel's method and Job's method,the molar ratio of theβ-CD unit inβ-CDP to Cur was determined to be 1:1.The diffusion coefficient and diffusion activation energy of Cur-β-CDP were calculated in an electrochemical study.This supramolecular complex worked well in vitro to inhibit the proliferation of hepatoma carcinoma cells HepG2.Remarkably,this method visibly reduced the undesirable side effects on normal cells,without weakening the anti-cancer activity of the drugs.We expect that the obtained host-vip complex will provide a new approach for delivering natural drug molecules,having low water solubility.展开更多
Objective:To investigate the biochemical constituents of the fruits of Terminalia bellerica(Gaertn.)Roxb.(hereafter termed T.bellerica)and estimate the anti-cancer activity of different polar extracts.Methods:To rapid...Objective:To investigate the biochemical constituents of the fruits of Terminalia bellerica(Gaertn.)Roxb.(hereafter termed T.bellerica)and estimate the anti-cancer activity of different polar extracts.Methods:To rapidly screen and identify the biochemical constituents of ethyl acetate(EA)extracts of T.bellerica,ultra performance liquid chromatography-electrospray ionization/mass spectrometry(UPLC-ESI-MSn)was done.The CellTiter-BlueTM cell-viability assay was used to ascertain the anti-cancer activity of different polar extracts in 10 human cancer cell lines.Results:Forty polyphenols of the EA extract of T.bellerica were characterized tentatively.The EA extract exhibited significant anti-cancer activity against ZR-75-1 cells(half-maximal inhibitory concentration=27.33(0.98)μg/mL)and Colo-205 cells(39.65(2.99)μg/mL)in vitro.Treatment of ZR-75-1 cells with 20 and 60μg/mL of the EA extract elicited dosedependent apoptosis percentages at an early stage of 17.58(0.74)%and at a late stage of 29.20(1.22)%;Colo-205 cells at the same concentration of EA extract had values of 21.33(1.03)%and 40.55(0.34)%,respectively.Western blotting suggested that ZR-75-1 and Colo205 cells treated with the EA extract showed a similar increasing tendency for expression of cleaved anti-poly adenosine diphosphate ribose polymerase I.Conclusion:We identified a total of 40 chemical constituents,of which 11 were first obtained from the Terminalia Linn.genus using UPLC-ESI-MSn.Meanwhile,we observe that the EA extract of T.bellerica possesses anti-cancer activity,especially against breast and colon cancers.展开更多
Objective： To study the isolated from the essential oil VIVO anti-tumor activities of furanodiene of the rhizome of Curcuma wenyujin （C15H200）, a primary sesquiterpene compound YH Chen et C. Ling（Wen Ezhu）, in vi...Objective： To study the isolated from the essential oil VIVO anti-tumor activities of furanodiene of the rhizome of Curcuma wenyujin （C15H200）, a primary sesquiterpene compound YH Chen et C. Ling（Wen Ezhu）, in vitro and in Methods： In vitro MTT assay was used to further study the effects of time and dosage on anti-proliferation of furanodiene against the sensitive Hela, Hep-2, HL-60, U251 cells, based on the cytotoxic effects of furanodiene on 12 human malignant tumor cell lines with the essential oil of Wen Ezhn as control., and the half-inhibitory concentration （IC50） was observed. In vivo uterine cervix （U14） tumor cell was selected and the conventional assay method of anti-tumor activity was employed. Furanodiene liposome was administered intraperitoneally, and tumor-inhibitory rate, thymus and spleen indexes were observed. Results： The inhibitive effects on cell proliferation were shown in all of the twelve cell lines and the cytotoxic effects of furanodiene against Hela, Hep-2, HL-60, U251 cells were observed after 12 h of administration, the effect could last for at least 48 h in a dose dependent manner, and the IC50 values were 0.6, 1.7, 1.8, 7.0μg/ml, respectively. Furanodiene was also found to show inhibitive effects on the proliferation of uterine cervix （U14） tumor induced in mice. The tumor inhibition rates were 36.09% （40 mg/kg）, 41.55% （60 mg/kg）, 58.29% （80 mg/kg）, respectively. Conclusion： Furanodiene is one of primary anti-cancer active components in the essential oil of Wen Ezhu, and also a very effective agent against uterine cervix cancer, and has protection effect on the immune function.展开更多
A series of ruthenium azopyridine complexes have recently been investigated due to their potential cytotoxic activities against renal cancer (A498), lung cancer (H226), ovarian cancer (IGROV), breast cancer (MCF-7) an...A series of ruthenium azopyridine complexes have recently been investigated due to their potential cytotoxic activities against renal cancer (A498), lung cancer (H226), ovarian cancer (IGROV), breast cancer (MCF-7) and colon cancer (WIDR). Thus, in order to predict the cytotoxic potentials of these compounds, quantitative structure-activity relationship studies were carried out using the methods of quantum chemistry. Five Quantitative Structure Activity Relationship (QSAR) models were obtained from the determined quantum descriptors and the different activities. The models present the following statistical indicators: regression correlation coefficient R2 = 0.986 - 0.905, standard deviation S = 0.516 - 0.153, Fischer test F = 106.718 - 14.220, correlation coefficient of cross-validation = 0.985- 0.895 and = 0.010 - 0.001. The statistical characteristics of the established QSAR models satisfy the acceptance and external validation criteria, thereby accrediting their good performance. The models developed show that the variation of the free enthalpy of reaction , the dipole moment μ and the charge of the ligand in the complex Ql, are the explanatory and predictive quantum descriptors correlated with the values of the anti-cancer activity of the studied complexes. Moreover, the charge of the ligand is the priority descriptor for the prediction of the cytotoxicity of the compounds studied. Furthermore, QSAR models developed are statistically significant and predictive, and could be used for the design and synthesis of new anti-cancer molecules.展开更多
Objective:To evaluate the potential immunomodulatory effects of an aqueous extract of Sesamum indicum seeds with regard to splenocyte proliferation,Th1/Th2 balance,macrophage function,and the cytotoxic activity of nat...Objective:To evaluate the potential immunomodulatory effects of an aqueous extract of Sesamum indicum seeds with regard to splenocyte proliferation,Th1/Th2 balance,macrophage function,and the cytotoxic activity of natural killer(NK)cells.Methods:Splenocyte proliferation was measured by[~3H]-thymidine incorporation.Griess assay was performed to evaluate the production of nitric oxide by macrophages.The levels of cytokines secreted by splenocytes and macrophages were measured by ELISA.JAM assay was performed to examine the cytotoxic activity of NK cells against YAC-1 tumor cells.Results:Sesamum indicum significantly enhanced splenocyte proliferation in a dose-dependent manner.Sesamum indicum also increased and suppressed the secretion of Th1 and Th2 cytokines,respectively,by splenocytes.The secretion of key pro-inflammatory mediators(IL-6,TNFα,and nitric oxide)by primary macrophages was significantly inhibited by Sesamum indicum.Moreover,Sesamum indicum increased the cytotoxic activity of NK cells against YAC-1 tumor cells.Conclusions:Sesamum indicum shows potent immunomodulatory,anti-inflammatory,and anti-cancer effects.Constituents of Sesamum indicum may be used as effective therapeutic agents in regulating immune reactions implicated in various infectious and noninfectious conditions including cancer.展开更多
The synthesis and in vitro photodynamic anticancer activity of a new photosen- sitizer, tetra（trifluoroethoxy） germanium phthalocyanine （GePcF）, were studied. GePcF was characterized by UV-Vis, IR, MS and elementa...The synthesis and in vitro photodynamic anticancer activity of a new photosen- sitizer, tetra（trifluoroethoxy） germanium phthalocyanine （GePcF）, were studied. GePcF was characterized by UV-Vis, IR, MS and elemental analysis. The in vitro photodynamic activity of GePcF was studied by MTT. IC50 of GePcF for SW480 cells of human colonic adenocarcinoma and HeLa cells of cervical cancer were 36.53 and 45.78 μmol/L, respectively. GePcF as a photosensitizer may be used to treat cancers due to its photodyrmmic anticancer activity.展开更多
AIM： To investigate the anticancer activity of DT-13 under normoxia and determine the underlying mechanisms of action. METHODS： MDA-MB-435 cell proliferation, migration, and adhesion were performed to assess the ant...AIM： To investigate the anticancer activity of DT-13 under normoxia and determine the underlying mechanisms of action. METHODS： MDA-MB-435 cell proliferation, migration, and adhesion were performed to assess the anticancer activity of DT-13, a saponin from Ophiopogonjaponicus, in vitro. In addition, the effects of DT-13 on tumor growth and metastasis in vivo were evaluated by orthotopic implantation of MDA-MB-435 cells into nude mice; mRNA levels of vascular endothelial growth factor （VEGF）, C-C chemokine receptor type 5 （CCR5） and hypoxia-inducible factor 1a （HIF-1a） were evaluated by real-time quantitative PCR; and CCR5 protein levels were detected by Western blot assay. RESULTS： At 0.01 to 1 umol·L -1, DT-13 inhibited MDA-MB-435 cell proliferation, migration, and adhesion significantly in vitro. DT-13 reduced VEGF and CCR5 mRNAs, and decreased CCR5 protein expression by down-regulating HIF-1 a. In addition, DT-13 inhibited MDA-MB-435 cell lung metastasis, and restricted tumor growth slightly in vivo. CONCLUSION： DT-13 inhibited MDA-MB-435 cell proliferation, adhesion, and migration in vitro, and lung metastasis in vivo by reducing VEGF, CCR5, and HIF-la expression.展开更多
Prenylated flavonoids are mainly distributed in Leguminosae and Moraceae plants, and they have been reported to possess various biological activities. Previously, we have reported a prenylated isoflavonoid, isoangusto...Prenylated flavonoids are mainly distributed in Leguminosae and Moraceae plants, and they have been reported to possess various biological activities. Previously, we have reported a prenylated isoflavonoid, isoangustone A（IAA） from licorice（Glycyrrhiza uralensis）, which induces apoptosis in colorectal cancer cells by disrupting mitochondrial functions. In the present study, we compared a group of flavonoids from licorice with IAA for their anti-proliferation activities and effects on intracellular signaling. The results indicated that the isoprenyl groups on the A and B rings, the hydroxyl groups at the ortho position of isoprenyl on A ring and the conjugated plane of C ring might contribute to the anti-cancer activity of prenylated flavonoids. Based on the above structure-activity relationship, we further identified four prenylated flavonoids with similar anti-cancer activities from licorice. Taken together, our present study established a preliminary structure-activity relationship of anti-cancer prenylated flavonoids, and our data provided important leading compounds from licorice, which deserved further research and development.展开更多
This paper reports the preparation of three di‑iron complexes containing a thiazole moiety.Esterification of complex[Fe_(2)(CO)_(6)(μ‑SCH_(2)CH(CH_(2)OH)S)](1)with 4‑methylthiazole‑5‑carboxylic acid gave the correspo...This paper reports the preparation of three di‑iron complexes containing a thiazole moiety.Esterification of complex[Fe_(2)(CO)_(6)(μ‑SCH_(2)CH(CH_(2)OH)S)](1)with 4‑methylthiazole‑5‑carboxylic acid gave the corresponding ester[Fe_(2)(CO)_(6)(μ‑tedt)](2),where tedt=SCH_(2)CH(CH_(2)OOC(5‑C_(3)HNSCH_(3)))S.Further reactions of complex 2 with tri(ptolyl)phosphine(tp)or tris(4‑fluorophenyl)phosphine(fp)gave the phosphine‑substituted derivatives[Fe_(2)(CO)_(5)(tp)(μ‑tedt)](3)and[Fe_(2)(CO)_(5)(fp)(μ‑tedt)](4).The structures of the newly prepared complexes were elucidated by elemental analysis,NMR,IR,and X‑ray photoelectron spectroscopy.Moreover,single‑crystal X‑ray diffraction analysis confirmed their molecular structures,showing that they contain a di‑iron core ligated by a bridged dithiolate bearing a thiazole moiety and terminal carbonyls.The electrochemical and electrocatalytic proton reduction were probed by cyclic voltammetry,revealing that three complexes can catalyze the reduction of protons to H_(2) under the electrochemical conditions.For comparison,complex 4 possessed the best efficiency with a turnover frequency of 23.5 s^(-1)at 10 mmol·L^(-1)HOAc concentration.In addition,the fungicidal activity of these complexes was also investigated in this study.CCDC:2477511,2;2477512,3;2477513,4.展开更多
Chitosan(CTS)was grafted onto the surface of amino‑functionalized silver chloride silicon dioxide(AgCl@SiO_(2)‑NH_(2))cores to obtain AgCl@SiO_(2)/CTS hybrid nanoparticles.The as‑obtained AgCl@SiO_(2)/CTS nanoparticle...Chitosan(CTS)was grafted onto the surface of amino‑functionalized silver chloride silicon dioxide(AgCl@SiO_(2)‑NH_(2))cores to obtain AgCl@SiO_(2)/CTS hybrid nanoparticles.The as‑obtained AgCl@SiO_(2)/CTS nanoparticles were chlorinated by NaClO solution to get AgCl@SiO_(2)/CTS‑based chloramine nano‑hybrid materials,denoted as AgCl@SiO_(2)/CTS‑Cl.A transmission electron microscope was used to observe the morphology of the as‑prepared samples AgCl@SiO_(2)/CTS and AgCl@SiO_(2)/CTS‑Cl.At the same time,an X‑ray diffractometer and an infrared spectroscope were utilized to characterize their crystal and chemical structures.Besides,ζpotentials were measured to elucidate the surface modification of AgCl nanoparticles by—NH_(2),the antibacterial mechanism of AgCl@SiO_(2)/CTS‑Cl was investigated by scanning electron microscopy,and Escherichia coli(E.coli)and Staphylococcus aureus(S.aureus)were used as the to‑be‑tested strains to evaluate the antimicrobial activity of samples AgCl@SiO_(2)/CTS and AgCl@SiO_(2)/CTS‑Cl.Findings demonstrate that sample AgCl@SiO_(2)/CTS exhibits a chain‑like structure ascribed to the interaction between—NH_(2),and each AgCl@SiO_(2)/CTS hybrid nanoparticle contains several AgCl cores.In the meantime,sample AgCl@SiO_(2)/CTS‑Cl exhibits excellent antibacterial activity against E.coli and S.aureus,which is attributed to the synergistic antibacterial effect of Ag^(+)and Cl^(-).Sample AgCl@SiO_(2)/CTS‑Cl with a dosage of 640.00μg·mL^(-1) could completely kill the two kinds of tested bacteria in 12 h of incubation;it retains a high antibacterial efficiency even after 10 cycles of antibacterial tests.展开更多
Conductive materials(CM)can improve methane production(MP)efficiency in many methanogenic systems.However,several types of CM exist,and there are uncertainties regarding whether they all improve MP efficiency to the s...Conductive materials(CM)can improve methane production(MP)efficiency in many methanogenic systems.However,several types of CM exist,and there are uncertainties regarding whether they all improve MP efficiency to the same extent and modulate microbial communities in a similar way.To investigate that,different microbial enrichments with and without activated carbon(AC),magnetite(Mag),and zeolites(Zeo)(at 0.5 g/L)were developed.MP profiles and microbial composition changes were compared among enrichments.The behavior of all enrichments was different,although the initial inoculum sludge was the same.Lag phase duration was lower in AC enrichment,while the complete conversion of butyrate to methane was faster in Mag enrichment.Syntrophomonas was the most abundant bacterial genus in all enrichments,but changes in the methanogenic community were evident.Acetoclastic methanogens were more diverse in Mag enrichment,with microorganisms assigned to Methanosarcina and Methanothrix gener1,but Methanothrix was the only acetoclastic methanogen in the other enrichments.On the other hand,different species of hydrogenotrophic methanogens prevailed in distinct enrichments.The metatranscriptomics results revealed that the dominant mechanism of interspecies electron transfer in the AC enrichment utilized hydrogen as the electron carrier,and no evidences of direct interspecies electron transfer(DIET)could be found.These results showed how different CM modulate microbial communities and affect MP efficiency through mechanisms that do not necessarily involve DIET or mediation via CM.展开更多
Overweight and obesity are significant public health concerns worldwide due to their association with many chronic health conditions.This has resulted in the development of various interventions focused on weight loss...Overweight and obesity are significant public health concerns worldwide due to their association with many chronic health conditions.This has resulted in the development of various interventions focused on weight loss to reduce the associated health burden.Physical activity is an important lifestyle behavior associated with enhanced health.Evidence supports that many of the benefits of physical activity are realized independent of initial weight status or whether weight loss is achieved,with some benefits additive to what is achieved with weight loss alone.These benefits include enhanced cardiometabolic,brain,cognitive and psychological health,and others.Moreover,in adults with overweight or obesity,physical activity has independent effects on cardiorespiratory fitness,muscular strength,physical function,and mobility.There are also benefits to body composition,with physical activity improving the quality of key tissues,such as skeletal muscle,which may not occur with diet-induced weight loss.Therefore,physical activity is an important public health target for adults with overweight or obesity to provide a wide range of health benefits that extend beyond those of weight loss alone.However,physical activity recommendations and programming efforts should consider the unique characteristics of adults with overweight or obesity to be most effective,and should support a focus on mobility,physical function,and other health outcomes.展开更多
Conventional ultrasound(US)evaluation of enthesitis in psoriatic arthritis(PsA)is limited by its inability to quantify metabolic alterations such as hypoxia,a key driver of disease activity.We introduce an oxygenation...Conventional ultrasound(US)evaluation of enthesitis in psoriatic arthritis(PsA)is limited by its inability to quantify metabolic alterations such as hypoxia,a key driver of disease activity.We introduce an oxygenation-integrated multimodal photoacoustic/ultrasound(PA/US)imaging framework designed to quantify entheseal oxygen saturation(SO_(2))for assessing entheseal disease activity in PsA.In this cross-sectional study,25 PsA patients underwent bilateral PA/US imaging of 12 entheses,where ultrasound lesions were scored using the Outcome Measures in Rheumatology scoring system,and PA-derived SO_(2) levels,quantified via dual-wavelength PA imaging,were classified into hyperoxia or hypoxia groups using k-means clustering.This approach provides metabolic insights complementary to conventional ultrasonic assessment.A composite score integrating hypoxia with US parameters was validated against clinical disease activity indices(Disease Activity Score 28-C-reactive protein,DAS28-CRP;Disease Activity Index for Psoriatic Arthritis,DAPSA).Among 300 entheses,103(34.3%)exhibited PA positivity,with 40(38.8%)classified as hypoxia.Hypoxia scores independently predicted DAS28-CRP(β=0.618,p=0.001)and DAPSA(β=0.612,p<0:001).The hypoxia-optimized PAUS score demonstrated superior correlation with disease activity indices compared to conventional US(DAS28-CRP:r=0.615,p=0.001 versus r=0.474,p=0.017;DAPSA:r=0.743,p<0:001 versus r=0.567,p=0.003),alongside superior diagnostic accuracy for minimal disease activity(area under the curve,AUC 0.776 versus 0.614,p=0.008)and low disease activity(AUC 0.853 versus 0.772,p=0.009).This multimodal scoring system enhances the stratification of PsA disease activity by providing unique metabolic insights,offering a potential tool for therapeutic monitoring and guiding treat-to-target strategies.展开更多
Large-scale CO_(2)emissions have exacerbated the greenhouse effect,reinforcing the critical need for efficient CO_(2)mitigation methods.Plasma-catalytic technology enables CO_(2)conversion under mild conditions,especi...Large-scale CO_(2)emissions have exacerbated the greenhouse effect,reinforcing the critical need for efficient CO_(2)mitigation methods.Plasma-catalytic technology enables CO_(2)conversion under mild conditions,especially for CO_(2)methanation(the Sabatier reaction),which has attracted significant attention due to its economic benefits and the potential for safe energy transportation via existing natural gas pipelines.The development of high-performance CO_(2)methanation catalysts remains an ongoing and long-term objective,and there is a lack of adequate in-situ characterization techniques to investigate the mechanisms.This study focuses on the Ni/La_(2)O_(3)(LN)catalyst and introduces two CO_(2)activation strategies through F and Na modifications:the Ni-Ov-Ni site activation with electron transfer from Ni0 under low-power conditions and basic site activation under high-power conditions.The LN-NaF catalysts enhance CO_(2)methanation activity across the entire power range compared to LN,achieving a CO_(2)conversion of 86.3%and CH4 selectivity of 99.4%.Additionally,LN-F(h)reaches a CH4 yield 4.15 times higher than that of LN at low power.Furthermore,in-situ diffuse reflectance infrared Fourier transform(DRIFT)spectroscopy with a self-made reactor are performed under plasma-catalytic conditions to reveal the CO_(2)adsorption and conversion mechanisms,indicating that different dopants(F,Na,and NaF)exhibit promoting effects on different intermediates,resulting in variations in CO_(2)methanation activity.This study provides valuable insights for improving catalyst performance and a thorough comprehension of mechanisms in CO_(2)methanation.展开更多
Active inflammation in“inactive”progressive multiple sclerosis:Traditionally,the distinction between relapsing-remitting multiple sclerosis and progressive multiple sclerosis(PMS)has been framed as an inflammatory v...Active inflammation in“inactive”progressive multiple sclerosis:Traditionally,the distinction between relapsing-remitting multiple sclerosis and progressive multiple sclerosis(PMS)has been framed as an inflammatory versus degenerative dichotomy.This was based on a broad misconception regarding essentially all neurodegenerative conditions,depicting the degenerative process as passive and immune-independent occurring as a late byproduct of active inflammation in the central nervous system(CNS),which is(solely)systemically driven.展开更多
Compounds selectively binding and stabilizing G-quadruplex structures could inhibit the telomerase or down- regulate the oncogenes and may act as anti-cancer drugs. An alkaloid with non-flat structure, fangchinoline, ...Compounds selectively binding and stabilizing G-quadruplex structures could inhibit the telomerase or down- regulate the oncogenes and may act as anti-cancer drugs. An alkaloid with non-flat structure, fangchinoline, showed to strongly stabilize the intermolecular and intramolecular parallel stranded G-quadruplex structure, increasing melting temperature by 20 and 23℃, respectively. The binding mode was investigated by using NMR and molec- ular modelling methods. Four human cell lines （HL-60, BGC-823, Be1-7402 and KB） were taken to test the an- ti-proliferation effects of fangchinoline and the IC50 values were ranged from 16 to 32 μmol/L. These results showed that the fangchinoline or related moiety derivatives may represent a class of telomere-targeted agents as po- tential anti-cancer drugs.展开更多
Prof.Zhang Xiaokun’s laboratory at the School of Pharmaceutical Sciences,Xiamen University identified several new small molecule modulators of nuclear receptor RXRαwith unique binding mechanisms and anti-cancer acti...Prof.Zhang Xiaokun’s laboratory at the School of Pharmaceutical Sciences,Xiamen University identified several new small molecule modulators of nuclear receptor RXRαwith unique binding mechanisms and anti-cancer activity,which was recently published in Chemistry&Biology(2014,21:596-607)and ACS Med Chem Lett(2014,5:736—741).RXRα,a unique member of the nuclear receptor superfamily of transcription factors,is an important展开更多
Patients with hepatocellular carcinoma (HCC) often experience hepatic morbidity. Hepatitis B virus (HBV) reactivation is well documented as a serious hepatic morbidity during anti-cancer therapy. Reported rates of HBV...Patients with hepatocellular carcinoma (HCC) often experience hepatic morbidity. Hepatitis B virus (HBV) reactivation is well documented as a serious hepatic morbidity during anti-cancer therapy. Reported rates of HBV reactivation in chronic carriers with HCC undergoing chemotherapy range from 4%-67%. Apart from chemotherapy, HBV reactivation has been increasingly identified in settings of hepatectomy and local ablation therapies. The rates of HBV reactivation vary with different levels of immunosuppression and depend on treatment, viral factors, and patient characteristics. The principal concern relating to reactivation is that a substantial proportion of patients with reactivation suffer from liver dysfunction during therapy, which often leads to disruption of planned, potentially life-prolonging treatments, adversely affecting the patients’ final outcome. The first step in the management of HBV reactivation is identification of patients at risk of reactivation by testing for HBV serology prior to commencing anti-cancer therapy. Although it is a serious complication, HBV reactivation is preventable with prophylactic anti-HBV drugs. Multiple publications have shown the benefit of prophylactic or preemptive antiviral therapy in this setting and justified such an approach before the start of therapy. Given the tumors and underlying cirrhosis, long-term use of antivirals with high potency and low risk of resistance is recommended in patients with HCC. This topic review will summarize the epidemiology, pathogenesis, and clinical issues related to HBV reactivation in HCC patients, and will discuss proper management against HBV reactivation during anti-cancer therapy for HCC.展开更多
Paclitaxel(PTX),a valuable natural product derived from Taxus species,exhibits remarkable anti-cancer properties.It penetrates nanopores in microtubule walls,interacting with tubulin on the lumen surface and disruptin...Paclitaxel(PTX),a valuable natural product derived from Taxus species,exhibits remarkable anti-cancer properties.It penetrates nanopores in microtubule walls,interacting with tubulin on the lumen surface and disrupting microtubule dynamics,thereby inducing cytotoxic effects in cancer cells.PTX and its derivatives have gained approval for treating various diseases due to their low toxicity,high efficiency,and broad-spectrum application.The widespread success and expanding applications of PTX have led to increased demand,raising concerns about accessibility.Consequently,researchers globally have focused on developing alternative production methods and applying nanocarriers in PTX delivery systems to enhance bioavailability.This review examines the challenges and advancements in PTX sourcing,production,physicochemical properties,anti-cancer mechanisms,clinical applications,trials,and chemo-immunotherapy.It aims to provide a comprehensive reference for the rational development and effective utilization of PTX.展开更多
To expand the study on the structures and biological activities of the anthracyclines anticancer drugs and reduce their toxic side effects,the new anthraquinone derivatives,9‑pyridylanthrahydrazone(9‑PAH)and 9,10‑bisp...To expand the study on the structures and biological activities of the anthracyclines anticancer drugs and reduce their toxic side effects,the new anthraquinone derivatives,9‑pyridylanthrahydrazone(9‑PAH)and 9,10‑bispyridylanthrahydrazone(9,10‑PAH)were designed and synthesized.Utilizing 9‑PAH and 9,10‑PAH as promising anticancer ligands,their respective copper complexes,namely[Cu(L1)Cl_(2)]Cl(1)and{[Cu_(4)(μ_(2)‑Cl)_(3)Cl_(4)(9,10‑PAH)_(2)(DMSO)_(2)]Cl_(2)}_(n)(2),were subsequently synthesized,where the new ligand L1 is formed by coupling two 9‑PAH ligands in the coordination reaction.The chemical and crystal structures of 1 and 2 were elucidated by IR,MS,elemental analysis,and single‑crystal X‑ray diffraction.Complex 1 forms a mononuclear structure.L1 coordinates with Cu through its three N atoms,together with two Cl atoms,to form a five‑coordinated square pyramidal geometry.Complex 2 constitutes a polymeric structure,wherein each structural unit centrosymmetrically encompasses two five‑coordinated binuclear copper complexes(Cu1,Cu2)of 9,10‑PAH,with similar square pyramidal geometry.A chlorine atom(Cl_(2)),located at the symmetry center,bridges Cu1 and Cu1A to connect the two binuclear copper structures.Meanwhile,the two five‑coordinated Cu2 atoms symmetrically bridge the adjacent structural units via one coordinated Cl atom,respectively,thus forming a 1D chain‑like polymeric structure.In vitro anticancer activity assessments revealed that 1 and 2 showed significant cytotoxicity even higher than cisplatin.Specifically,the IC_(50)values of 2 against HeLa‑229 and SK‑OV‑3 cancer cell lines were determined to be(5.92±0.32)μmol·L^(-1)and(6.48±0.39)μmol·L^(-1),respectively.2 could also block the proliferation of HeLa‑229 cells in S phase and significantly induce cell apoptosis.In addition,fluorescence quenching competition experiments suggested that 2 might interact with DNA by an intercalative binding mode,offering insights into its underlying anticancer mechanism.CCDC:2388918,1;2388919,2.展开更多
基金supported by the National Natural Science Foundation of China(Nos.21703200 and 21773203)the Chey Institute for Advanced Studies International Scholar Exchange Fellowship for the Academic Year of 2021-2022China Scholarship Council Program(No.201908320084)。
文摘As a member of the curcuminoid compound family,curcumin(Cur)has many interesting therapeutic properties.However,its low aqueous solubility and stability have resulted in poor bioavailability and restricted clinical efficacy.Based on size matching,β-cyclodextrin polymer(β-CDP),with its hydrophilic polymer chains and hydrophobic cavities,can form an inclusion complex with Cur.To improve the water solubility and stability of Cur,a simple and eco-friendly grinding method was designed to formβ-CDP inclusion complexes.According to the Boltzmann-Hamel's method and Job's method,the molar ratio of theβ-CD unit inβ-CDP to Cur was determined to be 1:1.The diffusion coefficient and diffusion activation energy of Cur-β-CDP were calculated in an electrochemical study.This supramolecular complex worked well in vitro to inhibit the proliferation of hepatoma carcinoma cells HepG2.Remarkably,this method visibly reduced the undesirable side effects on normal cells,without weakening the anti-cancer activity of the drugs.We expect that the obtained host-vip complex will provide a new approach for delivering natural drug molecules,having low water solubility.
基金supported by the National Natural Science Foundation of China:Surface Project(81274187)Longitudinal Research Project of the Beijing University of Chinese Medicine(2020072120043).
文摘Objective:To investigate the biochemical constituents of the fruits of Terminalia bellerica(Gaertn.)Roxb.(hereafter termed T.bellerica)and estimate the anti-cancer activity of different polar extracts.Methods:To rapidly screen and identify the biochemical constituents of ethyl acetate(EA)extracts of T.bellerica,ultra performance liquid chromatography-electrospray ionization/mass spectrometry(UPLC-ESI-MSn)was done.The CellTiter-BlueTM cell-viability assay was used to ascertain the anti-cancer activity of different polar extracts in 10 human cancer cell lines.Results:Forty polyphenols of the EA extract of T.bellerica were characterized tentatively.The EA extract exhibited significant anti-cancer activity against ZR-75-1 cells(half-maximal inhibitory concentration=27.33(0.98)μg/mL)and Colo-205 cells(39.65(2.99)μg/mL)in vitro.Treatment of ZR-75-1 cells with 20 and 60μg/mL of the EA extract elicited dosedependent apoptosis percentages at an early stage of 17.58(0.74)%and at a late stage of 29.20(1.22)%;Colo-205 cells at the same concentration of EA extract had values of 21.33(1.03)%and 40.55(0.34)%,respectively.Western blotting suggested that ZR-75-1 and Colo205 cells treated with the EA extract showed a similar increasing tendency for expression of cleaved anti-poly adenosine diphosphate ribose polymerase I.Conclusion:We identified a total of 40 chemical constituents,of which 11 were first obtained from the Terminalia Linn.genus using UPLC-ESI-MSn.Meanwhile,we observe that the EA extract of T.bellerica possesses anti-cancer activity,especially against breast and colon cancers.
基金supported by the Natural Science Foundation of Shandong Province of China (No Y2008C67)the Sci & Tech Development Plan Project of Shandong Provincial Education Department (No J07W01)
文摘Objective： To study the isolated from the essential oil VIVO anti-tumor activities of furanodiene of the rhizome of Curcuma wenyujin （C15H200）, a primary sesquiterpene compound YH Chen et C. Ling（Wen Ezhu）, in vitro and in Methods： In vitro MTT assay was used to further study the effects of time and dosage on anti-proliferation of furanodiene against the sensitive Hela, Hep-2, HL-60, U251 cells, based on the cytotoxic effects of furanodiene on 12 human malignant tumor cell lines with the essential oil of Wen Ezhn as control., and the half-inhibitory concentration （IC50） was observed. In vivo uterine cervix （U14） tumor cell was selected and the conventional assay method of anti-tumor activity was employed. Furanodiene liposome was administered intraperitoneally, and tumor-inhibitory rate, thymus and spleen indexes were observed. Results： The inhibitive effects on cell proliferation were shown in all of the twelve cell lines and the cytotoxic effects of furanodiene against Hela, Hep-2, HL-60, U251 cells were observed after 12 h of administration, the effect could last for at least 48 h in a dose dependent manner, and the IC50 values were 0.6, 1.7, 1.8, 7.0μg/ml, respectively. Furanodiene was also found to show inhibitive effects on the proliferation of uterine cervix （U14） tumor induced in mice. The tumor inhibition rates were 36.09% （40 mg/kg）, 41.55% （60 mg/kg）, 58.29% （80 mg/kg）, respectively. Conclusion： Furanodiene is one of primary anti-cancer active components in the essential oil of Wen Ezhu, and also a very effective agent against uterine cervix cancer, and has protection effect on the immune function.
文摘A series of ruthenium azopyridine complexes have recently been investigated due to their potential cytotoxic activities against renal cancer (A498), lung cancer (H226), ovarian cancer (IGROV), breast cancer (MCF-7) and colon cancer (WIDR). Thus, in order to predict the cytotoxic potentials of these compounds, quantitative structure-activity relationship studies were carried out using the methods of quantum chemistry. Five Quantitative Structure Activity Relationship (QSAR) models were obtained from the determined quantum descriptors and the different activities. The models present the following statistical indicators: regression correlation coefficient R2 = 0.986 - 0.905, standard deviation S = 0.516 - 0.153, Fischer test F = 106.718 - 14.220, correlation coefficient of cross-validation = 0.985- 0.895 and = 0.010 - 0.001. The statistical characteristics of the established QSAR models satisfy the acceptance and external validation criteria, thereby accrediting their good performance. The models developed show that the variation of the free enthalpy of reaction , the dipole moment μ and the charge of the ligand in the complex Ql, are the explanatory and predictive quantum descriptors correlated with the values of the anti-cancer activity of the studied complexes. Moreover, the charge of the ligand is the priority descriptor for the prediction of the cytotoxicity of the compounds studied. Furthermore, QSAR models developed are statistically significant and predictive, and could be used for the design and synthesis of new anti-cancer molecules.
文摘Objective:To evaluate the potential immunomodulatory effects of an aqueous extract of Sesamum indicum seeds with regard to splenocyte proliferation,Th1/Th2 balance,macrophage function,and the cytotoxic activity of natural killer(NK)cells.Methods:Splenocyte proliferation was measured by[~3H]-thymidine incorporation.Griess assay was performed to evaluate the production of nitric oxide by macrophages.The levels of cytokines secreted by splenocytes and macrophages were measured by ELISA.JAM assay was performed to examine the cytotoxic activity of NK cells against YAC-1 tumor cells.Results:Sesamum indicum significantly enhanced splenocyte proliferation in a dose-dependent manner.Sesamum indicum also increased and suppressed the secretion of Th1 and Th2 cytokines,respectively,by splenocytes.The secretion of key pro-inflammatory mediators(IL-6,TNFα,and nitric oxide)by primary macrophages was significantly inhibited by Sesamum indicum.Moreover,Sesamum indicum increased the cytotoxic activity of NK cells against YAC-1 tumor cells.Conclusions:Sesamum indicum shows potent immunomodulatory,anti-inflammatory,and anti-cancer effects.Constituents of Sesamum indicum may be used as effective therapeutic agents in regulating immune reactions implicated in various infectious and noninfectious conditions including cancer.
基金Supported by the Natural Science Foundation of Fujian Province(2012J01368)
文摘The synthesis and in vitro photodynamic anticancer activity of a new photosen- sitizer, tetra（trifluoroethoxy） germanium phthalocyanine （GePcF）, were studied. GePcF was characterized by UV-Vis, IR, MS and elemental analysis. The in vitro photodynamic activity of GePcF was studied by MTT. IC50 of GePcF for SW480 cells of human colonic adenocarcinoma and HeLa cells of cervical cancer were 36.53 and 45.78 μmol/L, respectively. GePcF as a photosensitizer may be used to treat cancers due to its photodyrmmic anticancer activity.
基金supported by the National Natural Science Foundation(Nos.81102853,81071841)the 2011’Program for Excellent Scientific and Technological Innovation Team of Jiangsu Higher Education
文摘AIM： To investigate the anticancer activity of DT-13 under normoxia and determine the underlying mechanisms of action. METHODS： MDA-MB-435 cell proliferation, migration, and adhesion were performed to assess the anticancer activity of DT-13, a saponin from Ophiopogonjaponicus, in vitro. In addition, the effects of DT-13 on tumor growth and metastasis in vivo were evaluated by orthotopic implantation of MDA-MB-435 cells into nude mice; mRNA levels of vascular endothelial growth factor （VEGF）, C-C chemokine receptor type 5 （CCR5） and hypoxia-inducible factor 1a （HIF-1a） were evaluated by real-time quantitative PCR; and CCR5 protein levels were detected by Western blot assay. RESULTS： At 0.01 to 1 umol·L -1, DT-13 inhibited MDA-MB-435 cell proliferation, migration, and adhesion significantly in vitro. DT-13 reduced VEGF and CCR5 mRNAs, and decreased CCR5 protein expression by down-regulating HIF-1 a. In addition, DT-13 inhibited MDA-MB-435 cell lung metastasis, and restricted tumor growth slightly in vivo. CONCLUSION： DT-13 inhibited MDA-MB-435 cell proliferation, adhesion, and migration in vitro, and lung metastasis in vivo by reducing VEGF, CCR5, and HIF-la expression.
基金National Natural Science Foundation of China(Grant No.81472657 and 81272468)
文摘Prenylated flavonoids are mainly distributed in Leguminosae and Moraceae plants, and they have been reported to possess various biological activities. Previously, we have reported a prenylated isoflavonoid, isoangustone A（IAA） from licorice（Glycyrrhiza uralensis）, which induces apoptosis in colorectal cancer cells by disrupting mitochondrial functions. In the present study, we compared a group of flavonoids from licorice with IAA for their anti-proliferation activities and effects on intracellular signaling. The results indicated that the isoprenyl groups on the A and B rings, the hydroxyl groups at the ortho position of isoprenyl on A ring and the conjugated plane of C ring might contribute to the anti-cancer activity of prenylated flavonoids. Based on the above structure-activity relationship, we further identified four prenylated flavonoids with similar anti-cancer activities from licorice. Taken together, our present study established a preliminary structure-activity relationship of anti-cancer prenylated flavonoids, and our data provided important leading compounds from licorice, which deserved further research and development.
文摘This paper reports the preparation of three di‑iron complexes containing a thiazole moiety.Esterification of complex[Fe_(2)(CO)_(6)(μ‑SCH_(2)CH(CH_(2)OH)S)](1)with 4‑methylthiazole‑5‑carboxylic acid gave the corresponding ester[Fe_(2)(CO)_(6)(μ‑tedt)](2),where tedt=SCH_(2)CH(CH_(2)OOC(5‑C_(3)HNSCH_(3)))S.Further reactions of complex 2 with tri(ptolyl)phosphine(tp)or tris(4‑fluorophenyl)phosphine(fp)gave the phosphine‑substituted derivatives[Fe_(2)(CO)_(5)(tp)(μ‑tedt)](3)and[Fe_(2)(CO)_(5)(fp)(μ‑tedt)](4).The structures of the newly prepared complexes were elucidated by elemental analysis,NMR,IR,and X‑ray photoelectron spectroscopy.Moreover,single‑crystal X‑ray diffraction analysis confirmed their molecular structures,showing that they contain a di‑iron core ligated by a bridged dithiolate bearing a thiazole moiety and terminal carbonyls.The electrochemical and electrocatalytic proton reduction were probed by cyclic voltammetry,revealing that three complexes can catalyze the reduction of protons to H_(2) under the electrochemical conditions.For comparison,complex 4 possessed the best efficiency with a turnover frequency of 23.5 s^(-1)at 10 mmol·L^(-1)HOAc concentration.In addition,the fungicidal activity of these complexes was also investigated in this study.CCDC:2477511,2;2477512,3;2477513,4.
文摘Chitosan(CTS)was grafted onto the surface of amino‑functionalized silver chloride silicon dioxide(AgCl@SiO_(2)‑NH_(2))cores to obtain AgCl@SiO_(2)/CTS hybrid nanoparticles.The as‑obtained AgCl@SiO_(2)/CTS nanoparticles were chlorinated by NaClO solution to get AgCl@SiO_(2)/CTS‑based chloramine nano‑hybrid materials,denoted as AgCl@SiO_(2)/CTS‑Cl.A transmission electron microscope was used to observe the morphology of the as‑prepared samples AgCl@SiO_(2)/CTS and AgCl@SiO_(2)/CTS‑Cl.At the same time,an X‑ray diffractometer and an infrared spectroscope were utilized to characterize their crystal and chemical structures.Besides,ζpotentials were measured to elucidate the surface modification of AgCl nanoparticles by—NH_(2),the antibacterial mechanism of AgCl@SiO_(2)/CTS‑Cl was investigated by scanning electron microscopy,and Escherichia coli(E.coli)and Staphylococcus aureus(S.aureus)were used as the to‑be‑tested strains to evaluate the antimicrobial activity of samples AgCl@SiO_(2)/CTS and AgCl@SiO_(2)/CTS‑Cl.Findings demonstrate that sample AgCl@SiO_(2)/CTS exhibits a chain‑like structure ascribed to the interaction between—NH_(2),and each AgCl@SiO_(2)/CTS hybrid nanoparticle contains several AgCl cores.In the meantime,sample AgCl@SiO_(2)/CTS‑Cl exhibits excellent antibacterial activity against E.coli and S.aureus,which is attributed to the synergistic antibacterial effect of Ag^(+)and Cl^(-).Sample AgCl@SiO_(2)/CTS‑Cl with a dosage of 640.00μg·mL^(-1) could completely kill the two kinds of tested bacteria in 12 h of incubation;it retains a high antibacterial efficiency even after 10 cycles of antibacterial tests.
基金supported by the Portuguese Foundation for Science and Technology(FCT)under the scope of the strategic funding of UIDB/04469/2020 unit and by the CM4Methane project(Ref:PTDC/BTA-BTA/2249/2021,DOI 10.54499/PTDC/BTABTA/2249/2021)FCT and European Union(EU),through the Portuguese State Budget and the European Social Fund under the scope of Norte2020-Programa Operacional Regional do Norte,also funded the SFRH/BD/132003/2017 and COVID/BD/152431/2022 grants held by Cátia S.N.Braga.,and the SFRH/BD/147271/2019 grant held by João C.Sequeira.M.SaloméDuarte acknowledges FCT for the Junior Research contract obtained under the scope of the Scientific Stimulus Employment 2022(ref:2022.06569.CEECIND/CP1718/CT0004,doi:https://doi.org/10.54499/2022.06569.CEECIND/CP1718/CT0004)PhD M.Fernando R.Pereira and PhD O.SaloméG.Soares from the Laboratory of Separation and Reaction Engineering-Laboratory of Catalysis and Materials,Faculty of Engineering(University of Porto),for providing the AC used in this study.
文摘Conductive materials(CM)can improve methane production(MP)efficiency in many methanogenic systems.However,several types of CM exist,and there are uncertainties regarding whether they all improve MP efficiency to the same extent and modulate microbial communities in a similar way.To investigate that,different microbial enrichments with and without activated carbon(AC),magnetite(Mag),and zeolites(Zeo)(at 0.5 g/L)were developed.MP profiles and microbial composition changes were compared among enrichments.The behavior of all enrichments was different,although the initial inoculum sludge was the same.Lag phase duration was lower in AC enrichment,while the complete conversion of butyrate to methane was faster in Mag enrichment.Syntrophomonas was the most abundant bacterial genus in all enrichments,but changes in the methanogenic community were evident.Acetoclastic methanogens were more diverse in Mag enrichment,with microorganisms assigned to Methanosarcina and Methanothrix gener1,but Methanothrix was the only acetoclastic methanogen in the other enrichments.On the other hand,different species of hydrogenotrophic methanogens prevailed in distinct enrichments.The metatranscriptomics results revealed that the dominant mechanism of interspecies electron transfer in the AC enrichment utilized hydrogen as the electron carrier,and no evidences of direct interspecies electron transfer(DIET)could be found.These results showed how different CM modulate microbial communities and affect MP efficiency through mechanisms that do not necessarily involve DIET or mediation via CM.
基金supported by the National Institutes of Health for the Kansas Center for Metabolism and Obesity Research(award No.P20GM144269)support from the Center for Advancing Translational Sciences of the National Institutes of Health(award No.KL2TR002367)supported by the National Center for Advancing Translational Sciences of the National Institutes of Health(award No.TL1TR002368)。
文摘Overweight and obesity are significant public health concerns worldwide due to their association with many chronic health conditions.This has resulted in the development of various interventions focused on weight loss to reduce the associated health burden.Physical activity is an important lifestyle behavior associated with enhanced health.Evidence supports that many of the benefits of physical activity are realized independent of initial weight status or whether weight loss is achieved,with some benefits additive to what is achieved with weight loss alone.These benefits include enhanced cardiometabolic,brain,cognitive and psychological health,and others.Moreover,in adults with overweight or obesity,physical activity has independent effects on cardiorespiratory fitness,muscular strength,physical function,and mobility.There are also benefits to body composition,with physical activity improving the quality of key tissues,such as skeletal muscle,which may not occur with diet-induced weight loss.Therefore,physical activity is an important public health target for adults with overweight or obesity to provide a wide range of health benefits that extend beyond those of weight loss alone.However,physical activity recommendations and programming efforts should consider the unique characteristics of adults with overweight or obesity to be most effective,and should support a focus on mobility,physical function,and other health outcomes.
基金supported by the National Natural Science Foundation of China(62325112)the National Key Research and Development Program of China(2023YFC2411700,2023YFC2411705)+2 种基金the National Natural Science Foundation of China(U22A2023)the National High-Level Hospital Clinical Research Funding(2022-PUMCH-C-009,2022-PUMCH-B-064,2022-PUMCH-D-002)the National Basic Research Program of China(973 Program,2014CB541801).
文摘Conventional ultrasound(US)evaluation of enthesitis in psoriatic arthritis(PsA)is limited by its inability to quantify metabolic alterations such as hypoxia,a key driver of disease activity.We introduce an oxygenation-integrated multimodal photoacoustic/ultrasound(PA/US)imaging framework designed to quantify entheseal oxygen saturation(SO_(2))for assessing entheseal disease activity in PsA.In this cross-sectional study,25 PsA patients underwent bilateral PA/US imaging of 12 entheses,where ultrasound lesions were scored using the Outcome Measures in Rheumatology scoring system,and PA-derived SO_(2) levels,quantified via dual-wavelength PA imaging,were classified into hyperoxia or hypoxia groups using k-means clustering.This approach provides metabolic insights complementary to conventional ultrasonic assessment.A composite score integrating hypoxia with US parameters was validated against clinical disease activity indices(Disease Activity Score 28-C-reactive protein,DAS28-CRP;Disease Activity Index for Psoriatic Arthritis,DAPSA).Among 300 entheses,103(34.3%)exhibited PA positivity,with 40(38.8%)classified as hypoxia.Hypoxia scores independently predicted DAS28-CRP(β=0.618,p=0.001)and DAPSA(β=0.612,p<0:001).The hypoxia-optimized PAUS score demonstrated superior correlation with disease activity indices compared to conventional US(DAS28-CRP:r=0.615,p=0.001 versus r=0.474,p=0.017;DAPSA:r=0.743,p<0:001 versus r=0.567,p=0.003),alongside superior diagnostic accuracy for minimal disease activity(area under the curve,AUC 0.776 versus 0.614,p=0.008)and low disease activity(AUC 0.853 versus 0.772,p=0.009).This multimodal scoring system enhances the stratification of PsA disease activity by providing unique metabolic insights,offering a potential tool for therapeutic monitoring and guiding treat-to-target strategies.
基金supported by the National Natural Science Foundation of China(No.51878292).
文摘Large-scale CO_(2)emissions have exacerbated the greenhouse effect,reinforcing the critical need for efficient CO_(2)mitigation methods.Plasma-catalytic technology enables CO_(2)conversion under mild conditions,especially for CO_(2)methanation(the Sabatier reaction),which has attracted significant attention due to its economic benefits and the potential for safe energy transportation via existing natural gas pipelines.The development of high-performance CO_(2)methanation catalysts remains an ongoing and long-term objective,and there is a lack of adequate in-situ characterization techniques to investigate the mechanisms.This study focuses on the Ni/La_(2)O_(3)(LN)catalyst and introduces two CO_(2)activation strategies through F and Na modifications:the Ni-Ov-Ni site activation with electron transfer from Ni0 under low-power conditions and basic site activation under high-power conditions.The LN-NaF catalysts enhance CO_(2)methanation activity across the entire power range compared to LN,achieving a CO_(2)conversion of 86.3%and CH4 selectivity of 99.4%.Additionally,LN-F(h)reaches a CH4 yield 4.15 times higher than that of LN at low power.Furthermore,in-situ diffuse reflectance infrared Fourier transform(DRIFT)spectroscopy with a self-made reactor are performed under plasma-catalytic conditions to reveal the CO_(2)adsorption and conversion mechanisms,indicating that different dopants(F,Na,and NaF)exhibit promoting effects on different intermediates,resulting in variations in CO_(2)methanation activity.This study provides valuable insights for improving catalyst performance and a thorough comprehension of mechanisms in CO_(2)methanation.
文摘Active inflammation in“inactive”progressive multiple sclerosis:Traditionally,the distinction between relapsing-remitting multiple sclerosis and progressive multiple sclerosis(PMS)has been framed as an inflammatory versus degenerative dichotomy.This was based on a broad misconception regarding essentially all neurodegenerative conditions,depicting the degenerative process as passive and immune-independent occurring as a late byproduct of active inflammation in the central nervous system(CNS),which is(solely)systemically driven.
基金We thank the National Natural Science Foundation of China （Nos. 21472197, 91027033, 81072576, 21205121, 21305145 and 31200576）, the Major National Basic Research Projects （973） （No. 2013CB733701）, the ＂Strategic Priority Research Program＂ of the Chinese Academy of Sciences （No. XDA09030307）, and the Key Program of the Chinese Academy of Sciences （No. KJCX2-EW-N06-01）.
文摘Compounds selectively binding and stabilizing G-quadruplex structures could inhibit the telomerase or down- regulate the oncogenes and may act as anti-cancer drugs. An alkaloid with non-flat structure, fangchinoline, showed to strongly stabilize the intermolecular and intramolecular parallel stranded G-quadruplex structure, increasing melting temperature by 20 and 23℃, respectively. The binding mode was investigated by using NMR and molec- ular modelling methods. Four human cell lines （HL-60, BGC-823, Be1-7402 and KB） were taken to test the an- ti-proliferation effects of fangchinoline and the IC50 values were ranged from 16 to 32 μmol/L. These results showed that the fangchinoline or related moiety derivatives may represent a class of telomere-targeted agents as po- tential anti-cancer drugs.
基金support by the National Natural Science Foundation of China(Grant Nos.91129302 and21332007)
文摘Prof.Zhang Xiaokun’s laboratory at the School of Pharmaceutical Sciences,Xiamen University identified several new small molecule modulators of nuclear receptor RXRαwith unique binding mechanisms and anti-cancer activity,which was recently published in Chemistry&Biology(2014,21:596-607)and ACS Med Chem Lett(2014,5:736—741).RXRα,a unique member of the nuclear receptor superfamily of transcription factors,is an important
文摘Patients with hepatocellular carcinoma (HCC) often experience hepatic morbidity. Hepatitis B virus (HBV) reactivation is well documented as a serious hepatic morbidity during anti-cancer therapy. Reported rates of HBV reactivation in chronic carriers with HCC undergoing chemotherapy range from 4%-67%. Apart from chemotherapy, HBV reactivation has been increasingly identified in settings of hepatectomy and local ablation therapies. The rates of HBV reactivation vary with different levels of immunosuppression and depend on treatment, viral factors, and patient characteristics. The principal concern relating to reactivation is that a substantial proportion of patients with reactivation suffer from liver dysfunction during therapy, which often leads to disruption of planned, potentially life-prolonging treatments, adversely affecting the patients’ final outcome. The first step in the management of HBV reactivation is identification of patients at risk of reactivation by testing for HBV serology prior to commencing anti-cancer therapy. Although it is a serious complication, HBV reactivation is preventable with prophylactic anti-HBV drugs. Multiple publications have shown the benefit of prophylactic or preemptive antiviral therapy in this setting and justified such an approach before the start of therapy. Given the tumors and underlying cirrhosis, long-term use of antivirals with high potency and low risk of resistance is recommended in patients with HCC. This topic review will summarize the epidemiology, pathogenesis, and clinical issues related to HBV reactivation in HCC patients, and will discuss proper management against HBV reactivation during anti-cancer therapy for HCC.
基金supported by the National Natural Science Foundation of China(Nos.82225047,82170274,82304665)the National Key Research and Development Program of China(No.2022YFC3501703)+3 种基金Zhejiang Provincial Natural Science Foundation of China(Nos.LZ24H280003,LQ23H280016)the Postdoctoral Fellowship Program of CPSF(No.GZC20233561)the Basic Medical Research Project of Naval Medical University(No.2023QN022)the Key Project at Central Government Level:The Ability Establishment of Sustainable Use for Valuable Chinese Medicine Resources(No.2060302).
文摘Paclitaxel(PTX),a valuable natural product derived from Taxus species,exhibits remarkable anti-cancer properties.It penetrates nanopores in microtubule walls,interacting with tubulin on the lumen surface and disrupting microtubule dynamics,thereby inducing cytotoxic effects in cancer cells.PTX and its derivatives have gained approval for treating various diseases due to their low toxicity,high efficiency,and broad-spectrum application.The widespread success and expanding applications of PTX have led to increased demand,raising concerns about accessibility.Consequently,researchers globally have focused on developing alternative production methods and applying nanocarriers in PTX delivery systems to enhance bioavailability.This review examines the challenges and advancements in PTX sourcing,production,physicochemical properties,anti-cancer mechanisms,clinical applications,trials,and chemo-immunotherapy.It aims to provide a comprehensive reference for the rational development and effective utilization of PTX.
文摘To expand the study on the structures and biological activities of the anthracyclines anticancer drugs and reduce their toxic side effects,the new anthraquinone derivatives,9‑pyridylanthrahydrazone(9‑PAH)and 9,10‑bispyridylanthrahydrazone(9,10‑PAH)were designed and synthesized.Utilizing 9‑PAH and 9,10‑PAH as promising anticancer ligands,their respective copper complexes,namely[Cu(L1)Cl_(2)]Cl(1)and{[Cu_(4)(μ_(2)‑Cl)_(3)Cl_(4)(9,10‑PAH)_(2)(DMSO)_(2)]Cl_(2)}_(n)(2),were subsequently synthesized,where the new ligand L1 is formed by coupling two 9‑PAH ligands in the coordination reaction.The chemical and crystal structures of 1 and 2 were elucidated by IR,MS,elemental analysis,and single‑crystal X‑ray diffraction.Complex 1 forms a mononuclear structure.L1 coordinates with Cu through its three N atoms,together with two Cl atoms,to form a five‑coordinated square pyramidal geometry.Complex 2 constitutes a polymeric structure,wherein each structural unit centrosymmetrically encompasses two five‑coordinated binuclear copper complexes(Cu1,Cu2)of 9,10‑PAH,with similar square pyramidal geometry.A chlorine atom(Cl_(2)),located at the symmetry center,bridges Cu1 and Cu1A to connect the two binuclear copper structures.Meanwhile,the two five‑coordinated Cu2 atoms symmetrically bridge the adjacent structural units via one coordinated Cl atom,respectively,thus forming a 1D chain‑like polymeric structure.In vitro anticancer activity assessments revealed that 1 and 2 showed significant cytotoxicity even higher than cisplatin.Specifically,the IC_(50)values of 2 against HeLa‑229 and SK‑OV‑3 cancer cell lines were determined to be(5.92±0.32)μmol·L^(-1)and(6.48±0.39)μmol·L^(-1),respectively.2 could also block the proliferation of HeLa‑229 cells in S phase and significantly induce cell apoptosis.In addition,fluorescence quenching competition experiments suggested that 2 might interact with DNA by an intercalative binding mode,offering insights into its underlying anticancer mechanism.CCDC:2388918,1;2388919,2.
