A new series of N-arylquinoline derivatives 5a-x bearing 2-morpholinoquinoline moiety has been synthesized by one pot base catalyzed cyclocondensation reaction of 2-morpholinoquinoline-3-carbaldehydes 2a-c,malononitri...A new series of N-arylquinoline derivatives 5a-x bearing 2-morpholinoquinoline moiety has been synthesized by one pot base catalyzed cyclocondensation reaction of 2-morpholinoquinoline-3-carbaldehydes 2a-c,malononitrile 3 andβ-enaminones 4a-h. All the synthesized compounds were screened for their in vitro antimicrobial activity against six bacterial pathogens,namely Streptococcus pneumoniae,Clostridium tetani,Bacillus subtilis,Salmonella typhi,Vibrio cholerae,Escherichia coli and against two fungal pathogens,Aspergillus fumigatus and Candida albicans using broth microdilution MIC method.Of the compounds studied,majority of the compounds were found to active against C.tetani,B.subtilis and C.albicans as compared to first-line standard drugs.展开更多
[Objective] This study aimed to analyze the in vitro inhibitory activity of Shisandra chinensis and Polygonatum sibiricum against Vibrio harveyi and its biofilms. [Result] By agar diffusion test, in vit...[Objective] This study aimed to analyze the in vitro inhibitory activity of Shisandra chinensis and Polygonatum sibiricum against Vibrio harveyi and its biofilms. [Result] By agar diffusion test, in vitro inhibitory activity of 5. chinensis and P. sibiricum against V. harveyi was investigated. The minimal inhibitory concentration （ MIC） and minimal bactericidal concentration （MBC） of 5. chinensis and P. sibiricum against V. harveyi were determined by doubling dilution meth-od. The inhibitory activity of 5. chinensis and P. sibiricum on the formation of V. harveyi biofilms was evaluated by modified MTT assay. [ Result ] Both 5. chinen-sis and P. sibiricum had inhibitory activity against V. harveyi. The inhibition zone diameter of 5. chinensis against V. harveyi was 17. 95 mm; MIC and MBC of 5. chinensis were both 3.125 mg/ml. The inhibition zone diameter of P. sibiricum against V. harveyi was 12. 22 mm; MIC and MBC of P. sibiricum were 3.125 and 6.250 mg/ml, respectively. When the concentration was higher than 6. 25 mg/ml, 5. chinensis decoction had extremely significant inhibitory activity against V. harveyi （P 〈 0. 01） ; when the concentration was higher than 3. 125 mg/ml, P. sibiricum had extremely significant inhibitory activity against V. harveyi （P 〈0. 01）. [ Conclusion] 5. chinensis and P. sibiricum could significantly inhibit V. harveyi and its biofilms.展开更多
A series of novel diaryl ureas containing 4-[（2-amino-6-trifluromethyl）pyrimidine-4-yl]piperazine-l-yl group were synthesized and evaluated for their cytotoxic activities in a panel of human cancer cell lines. Compa...A series of novel diaryl ureas containing 4-[（2-amino-6-trifluromethyl）pyrimidine-4-yl]piperazine-l-yl group were synthesized and evaluated for their cytotoxic activities in a panel of human cancer cell lines. Compared with the reference drug Sorafenib,some compounds showed more potent and a broader spectrum of anti-cancer activities.Among them,compound 2p demonstrated significant inhibitory activities against MDA-MB-231,HT-29 and MCF-7 cell lines with IC_（50） values of 0.016,0.63,0.001μmol/L, respectively.展开更多
Tumor-infiltrating lymphocytes (TIL) isolated from 11 gastric carcinoma were studied. TIL could grow for a long-term in medium containing recombi-nant interleukin-2(rlL-2). The mean expansion fold achieved in 6 long-t...Tumor-infiltrating lymphocytes (TIL) isolated from 11 gastric carcinoma were studied. TIL could grow for a long-term in medium containing recombi-nant interleukin-2(rlL-2). The mean expansion fold achieved in 6 long-term cultures of 11 specimens was 15.1. RIL-2 expanded gastric TIL exhibited significant cytotoxicity against K562, BGC823, MCF-7 and more effective antitumor cytotoxicity against fresh autologous tumor targets and human gastric cancer cell line. Peak cytotoxicity was shown in the third or fourth week after cultures. Cryopreservation of gastric TIL didn't influence their expansion capacity and antitumor activity. Phenotypic analysis was demonstrated in this study. The results of present study indicate that TIL from human gastric carcinoma could be expanded and reach high levels of antitumor effector function in long-term cultures with rIL-2. Their function may be of clinical importance.展开更多
Phenylalanine ammonia lyase(PAL)is the rate-limiting and pivotal enzyme of the general phenylpropanoid path-way,but few reports have been found on PAL genes in Pinus yunnanensis.In the present study,three PAL genes we...Phenylalanine ammonia lyase(PAL)is the rate-limiting and pivotal enzyme of the general phenylpropanoid path-way,but few reports have been found on PAL genes in Pinus yunnanensis.In the present study,three PAL genes were cloned and identified from P.yunnanensis seedlings for thefirst time,namely,PyPAL-1,PyPAL-2,and PyPAL-3.Our results indicated that the open-reading frames of PyPAL genes were 2184,2157,and 2385 bp.Phylogenetic tree analysis revealed that PyPALs have high homology with other known PAL genes in other plants.In vitro enzymatic analysis showed that all three PyPAL recombinant proteins could catalyze the deamination of L-phenylalanine to form trans-cinnamic acid,but only PAL1 and PAL2 can catalyze the conversion of L-tyrosine toρ-coumaric acid.Three PyPAL genes were expressed in different tissues in 1-year-old P.yunnanensis,and such genes had different expression patterns.This study lays a foundation for further understanding of the biosynthesis of secondary metabolites in P.yunnanensis.展开更多
BACKGROUND: The pharmacological action of traditional Chinese medicine compound is the comprehensive effect of the various ingredients, and the interactions of various ingredients are closely correlated with the final...BACKGROUND: The pharmacological action of traditional Chinese medicine compound is the comprehensive effect of the various ingredients, and the interactions of various ingredients are closely correlated with the final effect. In order to reveal the compatibility mechanism of BHD's prescription in treating and preventing ischemic cerebrovascular disease, we needed explore the effect and relation of ingredients in the prescription. OBJECTIVE: To observe the effect of Buyang Huanwu decoction (BHD) and Astragalus mongholicus on the activity of platelet activating factor receptor (PAFR) in the platelet of rabbits in vitro, and investigate the mechanism of Astragalus mongholicus. DESIGN: A decomposed recipes study. SETTING: Guangzhou University of Traditional Chinese Medicine. MATERIALS: Five New Zealand rabbits, weighing 2-3 kg, both sexes, were used. BHD was composed of Sheng Huang Qi 120 g, Dang Gui Wei 6 g, Chi Shao 4.5 g, Chuan Xiong 3 g, Di Long 3 g, Tao Ren 3 g, Hong Hua 3 g. The prescription for activating blood circulation consisted of Dang Gui Wei 6 g, Chi Shao 4.5 g, Chuan Xiong 3 g, Di Long 3 g, Tao Ren 3 g and Hong Hua 3 g. The prescription for invigorating qi consisted of 120 g Sheng Huang Qi. The prepared herbal pieces were purchased from the traditional Chinese medicine Dispensary of Foshan Second People's Hospital, and appraised by Professor Xu from Science of Chinese Materia Medica College, Guangzhou University of Traditional Chinese Medicine. 3H-PAF was supplied by Amersham Co., Ltd. (specific activity: 6. 475 TBq/mmol; batch number: 200402); PAF standard by Biomol Co., Ltd. (batch number: P1318V). METHODS: The experiments were carried out in the Laboratory of Nuclear Medicine, Guangzhou University of Traditional Chinese Medicine from September to December 2004. ① Injections of BHD, prescriptions for activating blood circulation and invigorating qi were prepared by the decoction and alcohol sedimentation technique. Rabbit common carotid artery blood (40 mL) was drawn via intubation to prepare platelet suspension of (0.8-1.0)×1010 L-1. ② Determination of 3H-PAF and washed PAFR binding: The general combination tube (T) contained washed platelet-rich plasma (WPRP) 380 μL + 3H-PAF (0.35 nmol/L)10 μL+distilled water 5 μL; The nonspecific binding tube (P) contained WPRP 380 μL+3H-PAF(0.35 nmol/L)10 μL+cold PAF (1 μmol/L) 5 μL; The sample tube (Y) contained WPRP 380 μL+3H-PAF(0.35 nmol/L)10 μL+experimental medicine (injection of BHD, prescriptions for activating blood circulation or invigorating qi) 5 μL. The test was conducted for three times for each sample in the same way as mentioned above. The samples were shaken on the oscillator for 30 s, then bathed at 25 ℃ for 40 minutes, and the reaction was terminated with cold Tris buffer containing 0.1% BSA, multichannel cell detachment separator was used for vacuum suction to filter the separated free 3H-PAF, and the filter paper was washed with cold Tris buffer for four times, then dried in the baking oven (80 ℃) for 1 hour, and placed in xylol liquid scintillator, and the radioactivity was determined automatically by the liquid scintillation detector. The mean of the three parallel tubes was calculated. The specific binging inhibition rate was calculated: SBIR=[(T-Y)/(T-P)]×100%]. ③ Univariate analysis of variance was conducted. And for comparison of each paired groups, the q test was adopted. MAIN OUTCOME MEASURES: Effect of BHD whole prescription, prescriptions for activating blood circulation and invigorating qi on the specific binding inhibition rate of 3H-PAF and PAFR. RESULTS: BHD, prescriptions for activating blood circulation and invigorating qi were all able to inhibit the specific binding of 3H-PAF to PAFR, the specific blinding inhibition rates were (45.90±7.50)%, (97.90±1.84)% and (26.75±2.48)%, respectively, and there were significant differences between every two groups (P < 0.01). CONCLUSION: Single Astragalus mongholicus (120 g) can inhibit the specific blinding of PAFR in the platelet of the rabbit with 3H-PAF, but the combination of Astragalus mongholicus with the drugs for activating blood circulation in BHD can significantly decrease the inhibiting action of the latter on PAFR activity of the platelet, reflecting the combined mechanism of 'removing blood stasis without injuring the vital qi' in BHD.展开更多
A series of 5-substitued-3-（5-（4-（furan-2-yl）-6-methyl-2-oxo/thioxo-1,2,3,4-tetrahydropyrimidin-5-yl）-1,3,4-thiadiazol-2- ylimino）indolin-2-one derivatives were synthesized,characterized and were screened for an...A series of 5-substitued-3-（5-（4-（furan-2-yl）-6-methyl-2-oxo/thioxo-1,2,3,4-tetrahydropyrimidin-5-yl）-1,3,4-thiadiazol-2- ylimino）indolin-2-one derivatives were synthesized,characterized and were screened for anti-bacterial,anti-fungal and antitubercular activity.展开更多
The effects of two different drying methods,namely hot-air drying and freeze drying,on the phenolic profiles,antioxidant and hypoglycemic activities of pulp extracts from two main Chinese bayberry cultivars(’Biqi’or...The effects of two different drying methods,namely hot-air drying and freeze drying,on the phenolic profiles,antioxidant and hypoglycemic activities of pulp extracts from two main Chinese bayberry cultivars(’Biqi’or’BQ’and’Dongkui’or’DK’)were evaluated.The results showed that’BQ’bayberry provided higher total phenolic(TPC),total flavonoid(TFC)and total anthocyanin(TAC)contents than’DK’bayberry after the same drying method,while its antioxidant and hypoglycemic activities were highly affected by drying method.Freeze-dried samples possessed significantly higher TPC,TFC and TAC,and exhibited more potent antioxidant and hypoglycemic activities than hot-air dried ones(P<0.05).Freeze-dried’DK’bayberry exhibited similar antioxidant activities and a-amylase inhibitory activity,but higher a-glucosidase inhibition than freeze-dried’BQ’bayberry(P<0.05).Compared with hot-air dried samples,freeze-dried samples had significantly higher contents of cyanidin-3-O-glucoside,myricitin-3-O-rhamnoside,quercetin-3-O-galactoside,quercetin-3-O-glucoside and quercetin-3-O-rhamnoside,which had been proved to be the main contributors to the in vitro hypoglycemic activities of bayberry pulp extract.All these results demonstrate that freeze drying is more suitable for the preservation of phenolic components in the pulp extract of Chinese bayberry,and the pulp extract of freeze-dried’DK’could be applied as a potential hypoglycemic food additive.展开更多
Two series of a-aminophosphonate derivatives containing a quinoline moiety have been designed and synthesized by introducing bioactive quinoline scaffold to a-aminophosphonate. The in vitro cytotoxic activities of tar...Two series of a-aminophosphonate derivatives containing a quinoline moiety have been designed and synthesized by introducing bioactive quinoline scaffold to a-aminophosphonate. The in vitro cytotoxic activities of target compounds were first investigated against two human cancer cell lines including Eca109 and Huh7 by MTT assay. Results revealed that most of target compounds exhibited moderate to high antitumor activities against the tested cancer cell lines and some demonstrated more potent inhibitory activities compared with Sunitinib. Among them, compounds 4b2 and 4b4 containing methylsubstituted aniline group were found to be more active than Sunitinib against both of two cancer cell lines, with IC50 in the range of 2.26 mmol/L–7.46 mmol/L.展开更多
The Deltanif E MoFe protein (Deltanif E Av1) was obtained by a chromatography on DE52, Sephacryl S-300 and Q-Sepharose columns from the unheated crude extract of nifE-deleted mutant strain (DJ35) of Azotobacter vinela...The Deltanif E MoFe protein (Deltanif E Av1) was obtained by a chromatography on DE52, Sephacryl S-300 and Q-Sepharose columns from the unheated crude extract of nifE-deleted mutant strain (DJ35) of Azotobacter vinelandii Lipmann. The analysis by SDS-PAGE showed that the Delta nif EAv1 was similar to OP MoFe protein (Av1) of A. vinelandii in the kinds and molecular weights of subunits (alpha and beta subunit). When complemented with nitrogenase Fe protein (M), the A nif EAv1 had hardly any proton-reduction activity, but could be significantly activated by FeMoco extracted from OP Av1. After the Delta nif E Av1 was treated with an excess o-phenanthroline (o-phen) and chromatographied on Sephadex G-25 column under atmosphere of Ar, Delta nif E Av1(C) was obtained. In the presence of both Av2 and MgATP regeneration system, the Delta nif EAv1(C), rather than A nif EAv1, was significantly activated in vitro by a reconstituent solution containing Mn which composed of KMnO4, ferric homocitrate, Na2S, Na2S2O4 (DT) and dithiothreitol (DTT). But in the absence of MgATP or Av2, the activation of Delta nifE Av1(C) did not happen. It indicates that activation of Delta nif EAv1 by RS-Mn requires the pretreatment with o-phen and the simultaneous presence of Av2 and MgATP.展开更多
The methanolic extract obtained from the root portion of Caltha palustris var. alba was evaluated for its anthelmintic efficacy against gastrointestinal nematodes of sheep under both in vitro and in vivo conditions us...The methanolic extract obtained from the root portion of Caltha palustris var. alba was evaluated for its anthelmintic efficacy against gastrointestinal nematodes of sheep under both in vitro and in vivo conditions using worm motility inhibition(WMI) assay and fecal egg count reduction(FECR) assay, respectively. The extract was subjected to antimicrobial activity using agar-well diffusion method against different bacterial strains. In addition the extract was evaluated for cytotoxic and antioxidant activity against cultured THP-1(Leukemia), A-549(Lung), HCT-15(Colon), Cervix(HeLa) and PC-3(Prostrate) cell lines by SRB and DPPH radical scavenging assays. The extract used resulted in mean %WMI of 94.44%, as observed when the worms were put in lukewarm buffer for 30 min after exposure to different treatments. The mean mortality index of the sample was 0.95. The lethal concentration(LC50) was 0.11 mg·mL-1. Cell lines were exposed to concentration of 100 μg·mL-1 of extract for 48 h, which reduced the viability of these cell lines. The same plant extract also showed 55.58% DPPH radical scavenging activity.展开更多
The activation and development of primordial follicles is the key to the maturation of female gametes.Premature ovarian insufficiency(POI)patients are unable to complete the primordial follicle activation and developm...The activation and development of primordial follicles is the key to the maturation of female gametes.Premature ovarian insufficiency(POI)patients are unable to complete the primordial follicle activation and development due to follicular dormancy and unbalanced developmental regulation in the body,leading to female infertility.Ovarian tissue in vitro activation(IVA)technology has become a new way to solve the problem of patients who cannot auto-activate primordial follicles to obtain their own mature oocytes.In IVA research,signaling pathways such as PI3K/PTEN/Akt and Hippo have become the focus of current research.This review will describe the relevant research progress and clinical application of the IVA mechanism,and provide a reference for clinical research on ovarian tissue culture and activation in vitro.展开更多
A two-dimensional supramolecular compound di-n-butyltin piperonylate, {（μ3-O）（μ2-OMe）（n-Bu2Sn）2[O2CAr（C2H4O）]}2 constructed by hydrogen bonds with a Sn4O4 ladder-like framework, was obtained by the microwave...A two-dimensional supramolecular compound di-n-butyltin piperonylate, {（μ3-O）（μ2-OMe）（n-Bu2Sn）2[O2CAr（C2H4O）]}2 constructed by hydrogen bonds with a Sn4O4 ladder-like framework, was obtained by the microwave-assisted solvothermal reaction of di-n-butyltin oxide precursor with the piperonylic acid in methanol environments. The composite was characterized by elemental analysis and IR（~1H, ^（13）C and ^（119）Sn） NMR spectra. The compound crystallizes in monoclinic system, space group P21/n with a = 13.3690（12）, b = 14.1442（14）, c = 16.4022（16） A, β = 107.191（6）°, V = 2963.0（5） A^3, Z = 2, Dc = 1.520 g/cm^3, F（000） = 1368, μ = 1.719 mm^（-1）, Mo Kα radiation（λ = 0.71073 A）, the final R = 0.0495 and w R = 0.1260 for 6780 observed reflections with I 〉 2σ（I）. Its X-ray crystallography diffraction analyses show a Sn4O4 ladder-like skeleton, in which two endocyclic tin and one exo tin atoms are bonded to the μ3-O atom. In addition, one endocyclic tin and one exo tin atoms are respectively bonded to the μ2-O atom from methanol. The ladder-like molecule has a three-ring fused skeleton, which is almost coplanar. The endocyclic and exocyclic tin atoms were all five-coordinated with distorted trigonal bipyramidal geometry. The antitumor activity showed that the compound had higher activities than cisplatin in HT-29, HepG2, MCF-7, KB and A549 cell line in vitro.展开更多
This study aimed to explore the anti-bacterial and anti-fungal activities of extracts from different parts of plants in the Zingiberaceae family.The inhibitory rate,minimum inhibitory concentration(MIC),and minimum ba...This study aimed to explore the anti-bacterial and anti-fungal activities of extracts from different parts of plants in the Zingiberaceae family.The inhibitory rate,minimum inhibitory concentration(MIC),and minimum bactericidal concentration(MBC)of leaf and stem,and root and rhizome extracts from Alpinia katsumadai Hayata,Alpinia oxyphylla Miq×Alpinia henryi K.Schumann,Alpinia oblongifolia Hayata,Alpinia nigra(Gaertn.)Burtt,Amomum villosum Lour,Alpinia zerumbet(Pers.)Burtt.et Smith and Alpinia oxyphylla Miq were determined using the fungus cake method and double dilution method.The seven Zingiberaceae plants exhibited characteristic antibacterial activities against pathogenic bacteria and fungi.At a 1.5 mg mL^(−1),A.zerumbet root and rhizome extracts exhibited strong inhibitory activity against S.aureus and E.coli,with 83.23%and 79.62%,respectively.In addition,A.zerumbet leaf and stem extracts had an inhibitory rate of 90.85%against P.aeruginosa.At the same concentration,the leaf and stem,root and rhizome extracts of A.katsumadai had the best anti-bacterial effect against F.oxysporum,with inhibition rates of 84.46%and 84.73%,respectively.Moreover,A.katsumadai and A.zerumbet leaf and stem extracts had the most significant antibacterial effect against S.aureus,with a MIC of 0.063 mg mL^(−1).Thus,both A.katsumadai and A.zerumbet extracts had significant antibacterial activity.In addition,by comparing the inhibitory effect of extracts from different parts,it was found that the inhibitory rate and average inhibitory rate of extracts from leaf and stem were higher than those from root and rhizome.The chemical constituents of A.katsumadai and A.zerumbet,determined by the high-performance liquid chromatography-tandem mass spectrometry(UPLC-MS/MS),revealed that citric acid(CA),alpinetin,and pinocembrin(PNCB)were the functional constituents yielding the antibacterial activity.Overall,A.katsumadai and A.zerumbet have the potential to be developed as new plant fungicides and bactericides.展开更多
Objective: To study the effect of fluconzole derivatives from a side chain containing 4-substituted acyl piperazin-1-yl on antifungal activity. Methods: Fourteen title compounds were synthesized and confirmed by the e...Objective: To study the effect of fluconzole derivatives from a side chain containing 4-substituted acyl piperazin-1-yl on antifungal activity. Methods: Fourteen title compounds were synthesized and confirmed by the elementary analysis, 1HNMR and IR spectra. Five deep fungal strains and 3 shallow fungal strains were chosen as the experimental strains.Minimum inhibitory concentrations(MICs) of all title compounds were determined by the method recommended by the National Committee for Clinical Laboratory Standards (NCCLS) using RPMI 1640 test medium. Results: Among the 14 title compounds, 12 were first reported. The results of preliminary antifungal test showed that all the title compounds exhibited potent antifungal activities to a certain extent. The activity of 4 compounds were more than 4 times as high as that of fluconazole and equal to that of ketoconazole against Candida albicans in vitro(MIC 80 value≤0.125 μg/ml). Conclusion: Introduction of a side chain containing 4-substituted acyl piperazin-1-yl into the main part of fluconazole has important influence on antifungal activities of title compounds.展开更多
Emblica officinalis （E. oJficinalis） dried fruits were evaluated for its antitrypanosomal activity and cytotoxic effects. Vero cell line maintained in DMEM （Dubecco＇s Modified Eagle Medium） and incubated with Try...Emblica officinalis （E. oJficinalis） dried fruits were evaluated for its antitrypanosomal activity and cytotoxic effects. Vero cell line maintained in DMEM （Dubecco＇s Modified Eagle Medium） and incubated with Trypanosoma evansi for more than 12 h. MPE was added to the Vero cell culture medium at different concentrations （250-1,000 μg/mL） with trypanosomes concentration （1 × 106 trypanosomes/mL in each ELISA plate well） and incubated at appropriate conditions for 72 h. In-vitro cytotoxieity of MPE of E. officinalis was determined on Vero cells at concentrations （（1.56-100 ~tg/mL）. Acute toxicity and in-vivo infectivity tests were done in mice. Obtained MPE ofE. officinalis underwent process of purification via column chromatography, preparative chromatography and HPLC （higher performance liquid chromatography） with bioassay at different strata on Alsever＇s medium. In-vivo assay for trypanocidal activity, MPE and PPFs （partially purified fractions） of E. officinalis with two sets of mice, each mouse was inoculated with 1 × 104/mL oftrypanosomes and treated （48 h post inoculation） at concentrations （12.5, 25, 50, 100 and 200 mg/kg body weight） were administered at dose rate of 100 [tL per mouse via intraperitoneal route （in treating parassitemic mice） to different groups of mice, 6 mice per concentration. HPLC of partially purified fractions ofE. officinalis was carried out with mobile phase ofacetonitdle： water （40：60） in gradient mode. In vitro, MPE induced immobilization and killing of the parasites in concentration-time dependent manner. Significant reduction of trypanosomes counts from concentration of 250μg/mL and complete killing of trypanosomes at 5th hour of observation, which was statistically equivalent to 4th hour of Diminazine Aceturate （Berenil）, standard reference drug used. HPLC of the partially purified fractions revealed two major prominent peaks at retention time of 1-4 min. In vivo, both MPE and PPFs of test material did prolong lives of mice by 6-9 days but could not cure them. At concentration of 2,000 kg/kg body weight of MPE in acute test, all mice survived. For in-vivo infectivity test, mice injected with immobilized trypanosomes developed parasitemia and died while, the other group survived. MPE, PPFs and Diminazine Aceturate were toxic to Vero cells at all concentrations exception of 1.56, 1.56-3.13 and 1.56-6.25 μg/mL, respectively. From this report, PPFs ofE. officinalis dried fruits demonstrated potential pathway for a new development oftrypanocide in near future if additional investigations are put in place.展开更多
Seed treatment with endophytic fungi has been regarded as an effective method for plant parasitic nematode control.Endophytic fungi from cucumber seedlings were isolated and screened for their potential to be used as ...Seed treatment with endophytic fungi has been regarded as an effective method for plant parasitic nematode control.Endophytic fungi from cucumber seedlings were isolated and screened for their potential to be used as seed treatment agents against Meloidogyne incognita.Among the 294 isolates screened,23 significantly reduced galls formed by M.incognita in greenhouse test.The 10 most effective isolates were Fusarium(5),Trichoderma(1),Chaetomium(1),Acremonium(1),Paecilomyces(1),and Phyllosticta(1) .Their control efficacies were repeatedly tested and their colonizations as well as in vitro activity against M.incognita were studied.They reduced the number of galls by 24.0%-58.4%in the first screening and 15.6%-44.3%in the repeated test,respectively.Phyllosticta Ph511 and Chaetomium Ch1001 had high colonizations on both the roots and the aboveground parts of cucumber seedlings.Fusarium isolates had colonization preference on the roots,their root colonizations ranging from 20.1%to 47.3%of the total root area.Trichoderma Tr882,Paecilomyces Pa972,and Acremonium Ac985 had low colonizations on both the roots and the aboveground parts.Acremonium Ac985,Chaetomium Ch1001,Paecilomyces Pa972,and Phyllosticta Ph511 produced compounds affecting motility of the second stage juveniles of M.incognita.Based on these results,Chae-tomium Ch1001 was considered to have the highest potential as a seed treatment agent for M.incognita biocontrol.展开更多
In the present study, the zinc oxide nanoparticles(ZnO NPs) were prepared by using a sol-gel method. The characterization of ZnO NPs, such as particle size, morphology, crystal form, optical properties and p H-respons...In the present study, the zinc oxide nanoparticles(ZnO NPs) were prepared by using a sol-gel method. The characterization of ZnO NPs, such as particle size, morphology, crystal form, optical properties and p H-responsive behavior, was carried out. The in vitro anti-tumor activity of ZnO NPs was evaluated on PC-3M and 4T1 cell lines. The results indicated that ZnO NPs were spherical NPs with uniform particle size, excellent fluorescence properties, and p H-responsive behavior. The in vitro anti-tumor activity of ZnO NPs was observed on PC-3M and 4T1 cell lines. Considering to above characteristics, Zn O NPs could be used as drug delivery carries for loading active compound performing therapeutic and diagnostic effect.展开更多
This article demonstrates the synthesis, characterization and the study of in vitro antitubercular activities of twenty four new N-（4-（5-aryl-3-（5-methyl-1,3,4-oxadiazol-2-yl）-1H-pyrazol-1-yl）phenyl）-4-amide der...This article demonstrates the synthesis, characterization and the study of in vitro antitubercular activities of twenty four new N-（4-（5-aryl-3-（5-methyl-1,3,4-oxadiazol-2-yl）-1H-pyrazol-1-yl）phenyl）-4-amide derivatives（8a–x）. The antitubercular activity of the compounds against Mycobacterium tuberculosis H37Rv（MTB） revealed that 2-chloro-N-（4-（5-（4-chlorophenyl）-3-（5-methyl-1,3,4-oxadiazol-2-yl）-1H-pyrazol-1-yl）phenyl）benzamide（8n） is the most promising lead molecule with a MIC of1.56 mg/m L, while the corresponding unsubstituted benzamide derivative（8o） is the next most active molecule with a MIC of 3.13 mg/m L. Interestingly, the pyrazole intermediate 5b containing chlorophenyl and N-acylcarbohydrazide substituents also showed significant activity（MIC = 3.13 mg/m L）. Further, the active molecules did not show toxicity against a normal NIH 3T3 cell line, signifying their suitability for further drug development.展开更多
文摘A new series of N-arylquinoline derivatives 5a-x bearing 2-morpholinoquinoline moiety has been synthesized by one pot base catalyzed cyclocondensation reaction of 2-morpholinoquinoline-3-carbaldehydes 2a-c,malononitrile 3 andβ-enaminones 4a-h. All the synthesized compounds were screened for their in vitro antimicrobial activity against six bacterial pathogens,namely Streptococcus pneumoniae,Clostridium tetani,Bacillus subtilis,Salmonella typhi,Vibrio cholerae,Escherichia coli and against two fungal pathogens,Aspergillus fumigatus and Candida albicans using broth microdilution MIC method.Of the compounds studied,majority of the compounds were found to active against C.tetani,B.subtilis and C.albicans as compared to first-line standard drugs.
基金Supported by Project of Enhancing School with Innovation of Guangdong Ocean University(GDOU2015050216)Major Program for the Fundamental Research of the Department of Education of Guangdong Province(2014GKXM046)International Cooperation Innovation Platform Project of Universities in Guangdong Province(2013gjhz0008)
文摘[Objective] This study aimed to analyze the in vitro inhibitory activity of Shisandra chinensis and Polygonatum sibiricum against Vibrio harveyi and its biofilms. [Result] By agar diffusion test, in vitro inhibitory activity of 5. chinensis and P. sibiricum against V. harveyi was investigated. The minimal inhibitory concentration （ MIC） and minimal bactericidal concentration （MBC） of 5. chinensis and P. sibiricum against V. harveyi were determined by doubling dilution meth-od. The inhibitory activity of 5. chinensis and P. sibiricum on the formation of V. harveyi biofilms was evaluated by modified MTT assay. [ Result ] Both 5. chinen-sis and P. sibiricum had inhibitory activity against V. harveyi. The inhibition zone diameter of 5. chinensis against V. harveyi was 17. 95 mm; MIC and MBC of 5. chinensis were both 3.125 mg/ml. The inhibition zone diameter of P. sibiricum against V. harveyi was 12. 22 mm; MIC and MBC of P. sibiricum were 3.125 and 6.250 mg/ml, respectively. When the concentration was higher than 6. 25 mg/ml, 5. chinensis decoction had extremely significant inhibitory activity against V. harveyi （P 〈 0. 01） ; when the concentration was higher than 3. 125 mg/ml, P. sibiricum had extremely significant inhibitory activity against V. harveyi （P 〈0. 01）. [ Conclusion] 5. chinensis and P. sibiricum could significantly inhibit V. harveyi and its biofilms.
基金supported by a grant from the National Natural Science Foundation of China(No.21002065)
文摘A series of novel diaryl ureas containing 4-[（2-amino-6-trifluromethyl）pyrimidine-4-yl]piperazine-l-yl group were synthesized and evaluated for their cytotoxic activities in a panel of human cancer cell lines. Compared with the reference drug Sorafenib,some compounds showed more potent and a broader spectrum of anti-cancer activities.Among them,compound 2p demonstrated significant inhibitory activities against MDA-MB-231,HT-29 and MCF-7 cell lines with IC_（50） values of 0.016,0.63,0.001μmol/L, respectively.
文摘Tumor-infiltrating lymphocytes (TIL) isolated from 11 gastric carcinoma were studied. TIL could grow for a long-term in medium containing recombi-nant interleukin-2(rlL-2). The mean expansion fold achieved in 6 long-term cultures of 11 specimens was 15.1. RIL-2 expanded gastric TIL exhibited significant cytotoxicity against K562, BGC823, MCF-7 and more effective antitumor cytotoxicity against fresh autologous tumor targets and human gastric cancer cell line. Peak cytotoxicity was shown in the third or fourth week after cultures. Cryopreservation of gastric TIL didn't influence their expansion capacity and antitumor activity. Phenotypic analysis was demonstrated in this study. The results of present study indicate that TIL from human gastric carcinoma could be expanded and reach high levels of antitumor effector function in long-term cultures with rIL-2. Their function may be of clinical importance.
基金This study received financial support from the Youth Talents Special Project of Yunnan Province,“Xingdian Talents Support Program”(XDYC-QNRC-2022-0203)Southwest Forestry University Scientific Research Start-Up Funds(112116).
文摘Phenylalanine ammonia lyase(PAL)is the rate-limiting and pivotal enzyme of the general phenylpropanoid path-way,but few reports have been found on PAL genes in Pinus yunnanensis.In the present study,three PAL genes were cloned and identified from P.yunnanensis seedlings for thefirst time,namely,PyPAL-1,PyPAL-2,and PyPAL-3.Our results indicated that the open-reading frames of PyPAL genes were 2184,2157,and 2385 bp.Phylogenetic tree analysis revealed that PyPALs have high homology with other known PAL genes in other plants.In vitro enzymatic analysis showed that all three PyPAL recombinant proteins could catalyze the deamination of L-phenylalanine to form trans-cinnamic acid,but only PAL1 and PAL2 can catalyze the conversion of L-tyrosine toρ-coumaric acid.Three PyPAL genes were expressed in different tissues in 1-year-old P.yunnanensis,and such genes had different expression patterns.This study lays a foundation for further understanding of the biosynthesis of secondary metabolites in P.yunnanensis.
基金grants from Scientific Planning Program of Guangdong Province, No. 2004B36001009Scientific Research Funds of Guangdong Bureau of Traditional Chinese Medicine, No. 30002+1 种基金 Scientific Development Special Planning Funds of Foshan City, No. 200124Medical Scientific Research Program of Foshan City, No. 2000096
文摘BACKGROUND: The pharmacological action of traditional Chinese medicine compound is the comprehensive effect of the various ingredients, and the interactions of various ingredients are closely correlated with the final effect. In order to reveal the compatibility mechanism of BHD's prescription in treating and preventing ischemic cerebrovascular disease, we needed explore the effect and relation of ingredients in the prescription. OBJECTIVE: To observe the effect of Buyang Huanwu decoction (BHD) and Astragalus mongholicus on the activity of platelet activating factor receptor (PAFR) in the platelet of rabbits in vitro, and investigate the mechanism of Astragalus mongholicus. DESIGN: A decomposed recipes study. SETTING: Guangzhou University of Traditional Chinese Medicine. MATERIALS: Five New Zealand rabbits, weighing 2-3 kg, both sexes, were used. BHD was composed of Sheng Huang Qi 120 g, Dang Gui Wei 6 g, Chi Shao 4.5 g, Chuan Xiong 3 g, Di Long 3 g, Tao Ren 3 g, Hong Hua 3 g. The prescription for activating blood circulation consisted of Dang Gui Wei 6 g, Chi Shao 4.5 g, Chuan Xiong 3 g, Di Long 3 g, Tao Ren 3 g and Hong Hua 3 g. The prescription for invigorating qi consisted of 120 g Sheng Huang Qi. The prepared herbal pieces were purchased from the traditional Chinese medicine Dispensary of Foshan Second People's Hospital, and appraised by Professor Xu from Science of Chinese Materia Medica College, Guangzhou University of Traditional Chinese Medicine. 3H-PAF was supplied by Amersham Co., Ltd. (specific activity: 6. 475 TBq/mmol; batch number: 200402); PAF standard by Biomol Co., Ltd. (batch number: P1318V). METHODS: The experiments were carried out in the Laboratory of Nuclear Medicine, Guangzhou University of Traditional Chinese Medicine from September to December 2004. ① Injections of BHD, prescriptions for activating blood circulation and invigorating qi were prepared by the decoction and alcohol sedimentation technique. Rabbit common carotid artery blood (40 mL) was drawn via intubation to prepare platelet suspension of (0.8-1.0)×1010 L-1. ② Determination of 3H-PAF and washed PAFR binding: The general combination tube (T) contained washed platelet-rich plasma (WPRP) 380 μL + 3H-PAF (0.35 nmol/L)10 μL+distilled water 5 μL; The nonspecific binding tube (P) contained WPRP 380 μL+3H-PAF(0.35 nmol/L)10 μL+cold PAF (1 μmol/L) 5 μL; The sample tube (Y) contained WPRP 380 μL+3H-PAF(0.35 nmol/L)10 μL+experimental medicine (injection of BHD, prescriptions for activating blood circulation or invigorating qi) 5 μL. The test was conducted for three times for each sample in the same way as mentioned above. The samples were shaken on the oscillator for 30 s, then bathed at 25 ℃ for 40 minutes, and the reaction was terminated with cold Tris buffer containing 0.1% BSA, multichannel cell detachment separator was used for vacuum suction to filter the separated free 3H-PAF, and the filter paper was washed with cold Tris buffer for four times, then dried in the baking oven (80 ℃) for 1 hour, and placed in xylol liquid scintillator, and the radioactivity was determined automatically by the liquid scintillation detector. The mean of the three parallel tubes was calculated. The specific binging inhibition rate was calculated: SBIR=[(T-Y)/(T-P)]×100%]. ③ Univariate analysis of variance was conducted. And for comparison of each paired groups, the q test was adopted. MAIN OUTCOME MEASURES: Effect of BHD whole prescription, prescriptions for activating blood circulation and invigorating qi on the specific binding inhibition rate of 3H-PAF and PAFR. RESULTS: BHD, prescriptions for activating blood circulation and invigorating qi were all able to inhibit the specific binding of 3H-PAF to PAFR, the specific blinding inhibition rates were (45.90±7.50)%, (97.90±1.84)% and (26.75±2.48)%, respectively, and there were significant differences between every two groups (P < 0.01). CONCLUSION: Single Astragalus mongholicus (120 g) can inhibit the specific blinding of PAFR in the platelet of the rabbit with 3H-PAF, but the combination of Astragalus mongholicus with the drugs for activating blood circulation in BHD can significantly decrease the inhibiting action of the latter on PAFR activity of the platelet, reflecting the combined mechanism of 'removing blood stasis without injuring the vital qi' in BHD.
文摘A series of 5-substitued-3-（5-（4-（furan-2-yl）-6-methyl-2-oxo/thioxo-1,2,3,4-tetrahydropyrimidin-5-yl）-1,3,4-thiadiazol-2- ylimino）indolin-2-one derivatives were synthesized,characterized and were screened for anti-bacterial,anti-fungal and antitubercular activity.
基金financially supported by the Science and Technology Department of Zhejiang Province under Key Research and Development Project(2017C02004)。
文摘The effects of two different drying methods,namely hot-air drying and freeze drying,on the phenolic profiles,antioxidant and hypoglycemic activities of pulp extracts from two main Chinese bayberry cultivars(’Biqi’or’BQ’and’Dongkui’or’DK’)were evaluated.The results showed that’BQ’bayberry provided higher total phenolic(TPC),total flavonoid(TFC)and total anthocyanin(TAC)contents than’DK’bayberry after the same drying method,while its antioxidant and hypoglycemic activities were highly affected by drying method.Freeze-dried samples possessed significantly higher TPC,TFC and TAC,and exhibited more potent antioxidant and hypoglycemic activities than hot-air dried ones(P<0.05).Freeze-dried’DK’bayberry exhibited similar antioxidant activities and a-amylase inhibitory activity,but higher a-glucosidase inhibition than freeze-dried’BQ’bayberry(P<0.05).Compared with hot-air dried samples,freeze-dried samples had significantly higher contents of cyanidin-3-O-glucoside,myricitin-3-O-rhamnoside,quercetin-3-O-galactoside,quercetin-3-O-glucoside and quercetin-3-O-rhamnoside,which had been proved to be the main contributors to the in vitro hypoglycemic activities of bayberry pulp extract.All these results demonstrate that freeze drying is more suitable for the preservation of phenolic components in the pulp extract of Chinese bayberry,and the pulp extract of freeze-dried’DK’could be applied as a potential hypoglycemic food additive.
基金financial support of this work by the National Natural Science Foundation of China(Nos.21105091,21172201)
文摘Two series of a-aminophosphonate derivatives containing a quinoline moiety have been designed and synthesized by introducing bioactive quinoline scaffold to a-aminophosphonate. The in vitro cytotoxic activities of target compounds were first investigated against two human cancer cell lines including Eca109 and Huh7 by MTT assay. Results revealed that most of target compounds exhibited moderate to high antitumor activities against the tested cancer cell lines and some demonstrated more potent inhibitory activities compared with Sunitinib. Among them, compounds 4b2 and 4b4 containing methylsubstituted aniline group were found to be more active than Sunitinib against both of two cancer cell lines, with IC50 in the range of 2.26 mmol/L–7.46 mmol/L.
文摘The Deltanif E MoFe protein (Deltanif E Av1) was obtained by a chromatography on DE52, Sephacryl S-300 and Q-Sepharose columns from the unheated crude extract of nifE-deleted mutant strain (DJ35) of Azotobacter vinelandii Lipmann. The analysis by SDS-PAGE showed that the Delta nif EAv1 was similar to OP MoFe protein (Av1) of A. vinelandii in the kinds and molecular weights of subunits (alpha and beta subunit). When complemented with nitrogenase Fe protein (M), the A nif EAv1 had hardly any proton-reduction activity, but could be significantly activated by FeMoco extracted from OP Av1. After the Delta nif E Av1 was treated with an excess o-phenanthroline (o-phen) and chromatographied on Sephadex G-25 column under atmosphere of Ar, Delta nif E Av1(C) was obtained. In the presence of both Av2 and MgATP regeneration system, the Delta nif EAv1(C), rather than A nif EAv1, was significantly activated in vitro by a reconstituent solution containing Mn which composed of KMnO4, ferric homocitrate, Na2S, Na2S2O4 (DT) and dithiothreitol (DTT). But in the absence of MgATP or Av2, the activation of Delta nifE Av1(C) did not happen. It indicates that activation of Delta nif EAv1 by RS-Mn requires the pretreatment with o-phen and the simultaneous presence of Av2 and MgATP.
文摘The methanolic extract obtained from the root portion of Caltha palustris var. alba was evaluated for its anthelmintic efficacy against gastrointestinal nematodes of sheep under both in vitro and in vivo conditions using worm motility inhibition(WMI) assay and fecal egg count reduction(FECR) assay, respectively. The extract was subjected to antimicrobial activity using agar-well diffusion method against different bacterial strains. In addition the extract was evaluated for cytotoxic and antioxidant activity against cultured THP-1(Leukemia), A-549(Lung), HCT-15(Colon), Cervix(HeLa) and PC-3(Prostrate) cell lines by SRB and DPPH radical scavenging assays. The extract used resulted in mean %WMI of 94.44%, as observed when the worms were put in lukewarm buffer for 30 min after exposure to different treatments. The mean mortality index of the sample was 0.95. The lethal concentration(LC50) was 0.11 mg·mL-1. Cell lines were exposed to concentration of 100 μg·mL-1 of extract for 48 h, which reduced the viability of these cell lines. The same plant extract also showed 55.58% DPPH radical scavenging activity.
基金Major Science and Technology Projects in Hainan Province(ZDKJ2017007)Hainan Natural Science Foundation(2019CXTD408)。
文摘The activation and development of primordial follicles is the key to the maturation of female gametes.Premature ovarian insufficiency(POI)patients are unable to complete the primordial follicle activation and development due to follicular dormancy and unbalanced developmental regulation in the body,leading to female infertility.Ovarian tissue in vitro activation(IVA)technology has become a new way to solve the problem of patients who cannot auto-activate primordial follicles to obtain their own mature oocytes.In IVA research,signaling pathways such as PI3K/PTEN/Akt and Hippo have become the focus of current research.This review will describe the relevant research progress and clinical application of the IVA mechanism,and provide a reference for clinical research on ovarian tissue culture and activation in vitro.
基金Supported by the Innovation Platform Open Foundation for Colleges and Universities of Hunan Province(No.16k011)Key Laboratory of Functional Organometallic Materials of Hengyang Normal University(No.GN16K01)Scientific&Technological Projects of Hengyang(No.2016KJ03)
文摘A two-dimensional supramolecular compound di-n-butyltin piperonylate, {（μ3-O）（μ2-OMe）（n-Bu2Sn）2[O2CAr（C2H4O）]}2 constructed by hydrogen bonds with a Sn4O4 ladder-like framework, was obtained by the microwave-assisted solvothermal reaction of di-n-butyltin oxide precursor with the piperonylic acid in methanol environments. The composite was characterized by elemental analysis and IR（~1H, ^（13）C and ^（119）Sn） NMR spectra. The compound crystallizes in monoclinic system, space group P21/n with a = 13.3690（12）, b = 14.1442（14）, c = 16.4022（16） A, β = 107.191（6）°, V = 2963.0（5） A^3, Z = 2, Dc = 1.520 g/cm^3, F（000） = 1368, μ = 1.719 mm^（-1）, Mo Kα radiation（λ = 0.71073 A）, the final R = 0.0495 and w R = 0.1260 for 6780 observed reflections with I 〉 2σ（I）. Its X-ray crystallography diffraction analyses show a Sn4O4 ladder-like skeleton, in which two endocyclic tin and one exo tin atoms are bonded to the μ3-O atom. In addition, one endocyclic tin and one exo tin atoms are respectively bonded to the μ2-O atom from methanol. The ladder-like molecule has a three-ring fused skeleton, which is almost coplanar. The endocyclic and exocyclic tin atoms were all five-coordinated with distorted trigonal bipyramidal geometry. The antitumor activity showed that the compound had higher activities than cisplatin in HT-29, HepG2, MCF-7, KB and A549 cell line in vitro.
基金funded by the Forestry Science and Technology Innovation Project of Guangdong Province,China(2020KJCX010).
文摘This study aimed to explore the anti-bacterial and anti-fungal activities of extracts from different parts of plants in the Zingiberaceae family.The inhibitory rate,minimum inhibitory concentration(MIC),and minimum bactericidal concentration(MBC)of leaf and stem,and root and rhizome extracts from Alpinia katsumadai Hayata,Alpinia oxyphylla Miq×Alpinia henryi K.Schumann,Alpinia oblongifolia Hayata,Alpinia nigra(Gaertn.)Burtt,Amomum villosum Lour,Alpinia zerumbet(Pers.)Burtt.et Smith and Alpinia oxyphylla Miq were determined using the fungus cake method and double dilution method.The seven Zingiberaceae plants exhibited characteristic antibacterial activities against pathogenic bacteria and fungi.At a 1.5 mg mL^(−1),A.zerumbet root and rhizome extracts exhibited strong inhibitory activity against S.aureus and E.coli,with 83.23%and 79.62%,respectively.In addition,A.zerumbet leaf and stem extracts had an inhibitory rate of 90.85%against P.aeruginosa.At the same concentration,the leaf and stem,root and rhizome extracts of A.katsumadai had the best anti-bacterial effect against F.oxysporum,with inhibition rates of 84.46%and 84.73%,respectively.Moreover,A.katsumadai and A.zerumbet leaf and stem extracts had the most significant antibacterial effect against S.aureus,with a MIC of 0.063 mg mL^(−1).Thus,both A.katsumadai and A.zerumbet extracts had significant antibacterial activity.In addition,by comparing the inhibitory effect of extracts from different parts,it was found that the inhibitory rate and average inhibitory rate of extracts from leaf and stem were higher than those from root and rhizome.The chemical constituents of A.katsumadai and A.zerumbet,determined by the high-performance liquid chromatography-tandem mass spectrometry(UPLC-MS/MS),revealed that citric acid(CA),alpinetin,and pinocembrin(PNCB)were the functional constituents yielding the antibacterial activity.Overall,A.katsumadai and A.zerumbet have the potential to be developed as new plant fungicides and bactericides.
文摘Objective: To study the effect of fluconzole derivatives from a side chain containing 4-substituted acyl piperazin-1-yl on antifungal activity. Methods: Fourteen title compounds were synthesized and confirmed by the elementary analysis, 1HNMR and IR spectra. Five deep fungal strains and 3 shallow fungal strains were chosen as the experimental strains.Minimum inhibitory concentrations(MICs) of all title compounds were determined by the method recommended by the National Committee for Clinical Laboratory Standards (NCCLS) using RPMI 1640 test medium. Results: Among the 14 title compounds, 12 were first reported. The results of preliminary antifungal test showed that all the title compounds exhibited potent antifungal activities to a certain extent. The activity of 4 compounds were more than 4 times as high as that of fluconazole and equal to that of ketoconazole against Candida albicans in vitro(MIC 80 value≤0.125 μg/ml). Conclusion: Introduction of a side chain containing 4-substituted acyl piperazin-1-yl into the main part of fluconazole has important influence on antifungal activities of title compounds.
文摘Emblica officinalis （E. oJficinalis） dried fruits were evaluated for its antitrypanosomal activity and cytotoxic effects. Vero cell line maintained in DMEM （Dubecco＇s Modified Eagle Medium） and incubated with Trypanosoma evansi for more than 12 h. MPE was added to the Vero cell culture medium at different concentrations （250-1,000 μg/mL） with trypanosomes concentration （1 × 106 trypanosomes/mL in each ELISA plate well） and incubated at appropriate conditions for 72 h. In-vitro cytotoxieity of MPE of E. officinalis was determined on Vero cells at concentrations （（1.56-100 ~tg/mL）. Acute toxicity and in-vivo infectivity tests were done in mice. Obtained MPE ofE. officinalis underwent process of purification via column chromatography, preparative chromatography and HPLC （higher performance liquid chromatography） with bioassay at different strata on Alsever＇s medium. In-vivo assay for trypanocidal activity, MPE and PPFs （partially purified fractions） of E. officinalis with two sets of mice, each mouse was inoculated with 1 × 104/mL oftrypanosomes and treated （48 h post inoculation） at concentrations （12.5, 25, 50, 100 and 200 mg/kg body weight） were administered at dose rate of 100 [tL per mouse via intraperitoneal route （in treating parassitemic mice） to different groups of mice, 6 mice per concentration. HPLC of partially purified fractions ofE. officinalis was carried out with mobile phase ofacetonitdle： water （40：60） in gradient mode. In vitro, MPE induced immobilization and killing of the parasites in concentration-time dependent manner. Significant reduction of trypanosomes counts from concentration of 250μg/mL and complete killing of trypanosomes at 5th hour of observation, which was statistically equivalent to 4th hour of Diminazine Aceturate （Berenil）, standard reference drug used. HPLC of the partially purified fractions revealed two major prominent peaks at retention time of 1-4 min. In vivo, both MPE and PPFs of test material did prolong lives of mice by 6-9 days but could not cure them. At concentration of 2,000 kg/kg body weight of MPE in acute test, all mice survived. For in-vivo infectivity test, mice injected with immobilized trypanosomes developed parasitemia and died while, the other group survived. MPE, PPFs and Diminazine Aceturate were toxic to Vero cells at all concentrations exception of 1.56, 1.56-3.13 and 1.56-6.25 μg/mL, respectively. From this report, PPFs ofE. officinalis dried fruits demonstrated potential pathway for a new development oftrypanocide in near future if additional investigations are put in place.
基金Project supported by the German Academic Exchange Agency (DAAD),the China Scholarship Council(CSC),the Special Fund for Agro-scientific Research in the Public Interest(No.nyhezx07-050-6)the Science and Technology Department of Zhejiang Province of China(No.2008C22062)the Zhejiang Provincial Natural Science Foundation of China(No.R307396)
文摘Seed treatment with endophytic fungi has been regarded as an effective method for plant parasitic nematode control.Endophytic fungi from cucumber seedlings were isolated and screened for their potential to be used as seed treatment agents against Meloidogyne incognita.Among the 294 isolates screened,23 significantly reduced galls formed by M.incognita in greenhouse test.The 10 most effective isolates were Fusarium(5),Trichoderma(1),Chaetomium(1),Acremonium(1),Paecilomyces(1),and Phyllosticta(1) .Their control efficacies were repeatedly tested and their colonizations as well as in vitro activity against M.incognita were studied.They reduced the number of galls by 24.0%-58.4%in the first screening and 15.6%-44.3%in the repeated test,respectively.Phyllosticta Ph511 and Chaetomium Ch1001 had high colonizations on both the roots and the aboveground parts of cucumber seedlings.Fusarium isolates had colonization preference on the roots,their root colonizations ranging from 20.1%to 47.3%of the total root area.Trichoderma Tr882,Paecilomyces Pa972,and Acremonium Ac985 had low colonizations on both the roots and the aboveground parts.Acremonium Ac985,Chaetomium Ch1001,Paecilomyces Pa972,and Phyllosticta Ph511 produced compounds affecting motility of the second stage juveniles of M.incognita.Based on these results,Chae-tomium Ch1001 was considered to have the highest potential as a seed treatment agent for M.incognita biocontrol.
基金National Natural Science Foundation of China(Grant No.81773646)the National Key Research and Development Program of China(Grant No.2017YFA0205600)the Innovation Team of the Ministry of Education(Grant No.BMU2017TD003)。
文摘In the present study, the zinc oxide nanoparticles(ZnO NPs) were prepared by using a sol-gel method. The characterization of ZnO NPs, such as particle size, morphology, crystal form, optical properties and p H-responsive behavior, was carried out. The in vitro anti-tumor activity of ZnO NPs was evaluated on PC-3M and 4T1 cell lines. The results indicated that ZnO NPs were spherical NPs with uniform particle size, excellent fluorescence properties, and p H-responsive behavior. The in vitro anti-tumor activity of ZnO NPs was observed on PC-3M and 4T1 cell lines. Considering to above characteristics, Zn O NPs could be used as drug delivery carries for loading active compound performing therapeutic and diagnostic effect.
基金National Institute of Technology Karnataka,India for the financial support and laboratory facility
文摘This article demonstrates the synthesis, characterization and the study of in vitro antitubercular activities of twenty four new N-（4-（5-aryl-3-（5-methyl-1,3,4-oxadiazol-2-yl）-1H-pyrazol-1-yl）phenyl）-4-amide derivatives（8a–x）. The antitubercular activity of the compounds against Mycobacterium tuberculosis H37Rv（MTB） revealed that 2-chloro-N-（4-（5-（4-chlorophenyl）-3-（5-methyl-1,3,4-oxadiazol-2-yl）-1H-pyrazol-1-yl）phenyl）benzamide（8n） is the most promising lead molecule with a MIC of1.56 mg/m L, while the corresponding unsubstituted benzamide derivative（8o） is the next most active molecule with a MIC of 3.13 mg/m L. Interestingly, the pyrazole intermediate 5b containing chlorophenyl and N-acylcarbohydrazide substituents also showed significant activity（MIC = 3.13 mg/m L）. Further, the active molecules did not show toxicity against a normal NIH 3T3 cell line, signifying their suitability for further drug development.
