The Identification of Phenylalanine Ammonia-Lyase(PAL)Genes from Pinus yunnanensis and an Analysis of Enzyme Activity in vitro

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.

In vitro Inhibitory Activity of Shisandra chinensis and Polygonatum sibiricum against Vibrio harveyi and Its Biofilms

[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.

Research progress of in vitro activation mechanism and clinical application of female ovarian tissue

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.

In Vitro Anti-Bacterial and Anti-Fungal Activities of Extracts from Different Parts of 7 Zingiberaceae Plants

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.

IN VITRO ANTITUMOR ACTIVITY OF TUMOR-INFILTRATING LYMPHOCYTES FROM HUMAN GASTRIC CARCINOMA

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.

Effects of Buyang Huanwu decoction and Astragalus mongholicus on platelet activating factor receptor activity in rabbits in vitro

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.

Influence of sodium fluoride on alkaline phosphatase activity and bone gla protein synthesis in human yellow ligament cells in vitro

Objective To investigate the influence of sodium fluoride(NaF)on alkaline phosphatase(ALP)activity and bone gla protein(BGP)synthesis in yellow ligament cells from different surgical simples in vitro.Methods The human ligament cells

Synthesis and antifungal activity of 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-(4-substituted acyl piperazin-1-yl)-2-propanols

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.

Effects of different drying methods on phenolic components and in vitro hypoglycemic activities of pulp extracts from two Chinese bayberry(Myrica rubra Sieb.et Zucc.)cultivars

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.

Purification and Activation In Vitro of MoFe Protein from a nifE Deleted Mutant Strain of Azotobacter vinelandii

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.

Microwave Solvothermal Synthesis, Crystal Structures and in Vitro Antitumor Activities of Di-n-butyltin Piperonylate with a Sn4O4 Ladder Framework

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.

Therapeutic Activity of Partially Purified Fractions of Emblica officinalis （Syn, Phyllanthus embfica） Dried Fruits against Trypanosoma evansi

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.

Physicochemical properties,antioxidant and anti-inflammatory activities of coumarin-carbonodithioate hybrids

Objective:To study physicochemical properties,antioxidant and anti-inflammatory activities of coumarin-carbonodithioate hybrids.Methods:The substituted 4-bromomethyl coumarins were synthesized in first step by the cyclization.Then the reaction of substituted coumarins(a-e)with potassium O-ethyl/methyl carbonodithioate(1)by using absolute ethanol as solvent,afforded coumarin-carbonodithioate(1a-1j)derivatives under microwave irradiation and the conventional method.The spectroscopic analysis was used for the characterization of coumarin derivatives.The title(1a-1j)compounds were confirmed by spectroscopic methods.Antioxidant property was evaluated by using DPPH free radical-scavenging ability assay method and anti-inflammatory activity was evaluated by protein denaturation procedure using diclofenac sodium as a standard.Drug-likeness.In-silico toxicity was predicted with LD_(50)value and bioactivity score was also calculated for all the compounds.Results:All coumarin(1a-1j)compounds exhibited promisingin-vitro antioxidant and anti-inflammatory properties in comparison to standard drugs.All tested compounds were used for evaluating their physicochemical properties as set by Lipinski rule.It was observed that the synthesized compounds followed rule of five,indicating more'drug-like'nature.Conclusions:All the screened coumarin-carbonodithioates display promising in vitro antioxidant and antiinflammatory activities.From the physicochemical properties of coumarin derivatives,it is found that none of the compounds violate the Lipinski rule and they fall well in the range of rule of five.It is concluded that the coumarin-carbonodithioate hybrids act with more'drug-like'nature.

Antioxidant Activities of Crude Phlorotannins from Sargassum hemiphyllum

Brown algae are well known as a source of biologically active compounds, especially those having antioxidant activities, such as phlorotannins. In this study we examined the antioxidant activities of crude phlorotannins extracts（CPEs） obtained from Sargassum hemiphyllum（SH） and fractionated according to the molecular weights. When CPEs were administrated at a dose of 30 mg/kg to Kunming mice pre-treated with carbon tetrachloride（CCl4）, the levels of oxidative stress indicators in the liver, kidney and brain were significantly reduced in vivo. All the components of various molecular weight fractions of CPEs exhibited greater scavenging capacities in clearing hydroxyl free radical and superoxide anion than the positive controls gallic acid, vitamin C and vitamin E. Particularly, the components greater than 30 k D obtained from ethyl acetate phase showed the highest antioxidant capacities. These results indicated that SH is a potential source for extracting phlorotannins, the algal antioxidant compounds.

Synthesis and in vitro antitumor activity of novel diaryl urea derivatives

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.

Synthesis and in vitro antimicrobial activity of N-arylquinoline derivatives bearing 2-morpholinoquinoline moiety

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.

Study of Aldo-keto Reductase 1C3 Inhibitor with Novel Framework for Treating Leukaemia Based on Virtual Screening and In vitro Biological Activity Testing

Aldo-keto reductase 1C3(AKR1C3)is a potential target for the treatment of acute myeloid leukaemia and T-cell acute lymphoblastic leukaemia.In this study,pharmacophore models,molecular docking and virtual screening of target prediction were used to find a potential AKR1C3 inhibitor.Firstly,eight bacteriocin derivatives(Z1-Z8)were selected as training sets to construct 20 pharmacophore models.The best pharmacophore model MODEL_016 was obtained by Decoy test(the enrichment degree was 21.5117,and the fitting optimisation degree was 0.9668).Secondly,MODEL_016 was used for the virtual screening of ZINC database.Thirdly,the hit 83256 molecules were docked into the AKR1C3 protein.Compared to the total scores and interactions between compounds and protein,16532 candidate compounds with higher docking scores and interactions with important residues PHE306 and TRP227 were screened.Lastly,eight compounds(A1-A8)that had good absorption,distribution,metabolism,excretion and toxicity(ADMET)properties were obtained by target prediction.Compounds A3 and A7 with high total score and good target prediction results were selected for in vitro biological activity test,whose IC_(50) values were 268.3 and 88.94µmol/L,respectively.The results provide an important foundation for the discovery of novel AKR1C3 inhibitors.The research methods used in this study can also provide important references for the research and development of new drugs.

Synthesis and structure-activity relationships study ofα-aminophosphonate derivatives containing a quinoline moiety

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.

Secondary metabolites of rice sheath blight pathogen Rhizoctonia solani Kühn and their biological activities

Eight compounds were isolated from the fermentation cultures of rice sheath blight pathogen Rhizoctonia solani Kuhn. They were identified as ergosterol （1）, 6β-hydroxysitostenone （2）, sitostenone （3）, m-hydroxyphenylacetic acid （4）, methyl m-hydroxyphenylacetate （5）, m-hydroxymethylphenyl pentanoate （6）, （Z）-3-methylpent-2-en-1,5-dioic acid （7） and 3-methoxyfuran-2-carboxylic acid （8） by means of physicochemical and spectroscopic analysis. Among them, 2, 3, 5-8 were isolated from R. solani for the first time. All the compounds were evaluated for their biological activities. 4-6 and 8 showed their inhibitory activities on the radical and germ elongation of rice seeds. 1,4 and 7 showed moderate antibacterial activity to some bacteria. 4, 7 and 8 exhibited weak inhibitory activities on spore germination of Magnaporthe oryzae. 8 showed moderate antioxidant activity with the 1,1-diphenyl-2-picryhydrazyl （DPPH） andβ-carotene-linoleic acid assays. This is the first time to reveal compounds 5, 6 and 8 from rice sheath blight pathogen R. solani to have in vitro phytotoxic activity.