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The Identification of Phenylalanine Ammonia-Lyase(PAL)Genes from Pinus yunnanensis and an Analysis of Enzyme Activity in vitro
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作者 Dejin Mu Lin Chen +6 位作者 Heze Wang Zhaoliu Hu Sihui Chen Shi Chen Nianhui Cai Yulan Xu Junrong Tang 《Phyton-International Journal of Experimental Botany》 SCIE 2024年第3期503-516,共14页
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
关键词 Pinus yunnanensis phenylalanine ammonia-lyase enzyme activity in vitro functional analysis secondary metabolites
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In vitro Inhibitory Activity of Shisandra chinensis and Polygonatum sibiricum against Vibrio harveyi and Its Biofilms 被引量:4
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作者 Zhifeng HUANG Huanying PANG +3 位作者 Yang HUANG Yucong HUANG Yishan LU Jichang JIAN 《Agricultural Biotechnology》 CAS 2016年第4期57-60,共4页
[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
关键词 Shisandra chinensis Polygonatum sibiricum Vibrio harveyi in vitro inhibitory activity BIOFILM
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Research progress of in vitro activation mechanism and clinical application of female ovarian tissue
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作者 WU Bang-yong YI Hong-yan +1 位作者 MA Yan-lin HUANG Yuan-hua 《Journal of Hainan Medical University》 2023年第4期69-73,共5页
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
关键词 Ovarian tissue Primordial follicle in vitro activation PI3K/PTEN/Akt HIPPO
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In Vitro Anti-Bacterial and Anti-Fungal Activities of Extracts from Different Parts of 7 Zingiberaceae Plants
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作者 Lixian Wu Yongquan Li +5 位作者 Qiaoguang Li Jingxuan Li Qinghua Lao Yucheng Zhong Hui Zhang Xiu Hu 《Journal of Renewable Materials》 SCIE EI 2023年第2期975-989,共15页
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
关键词 ZinGIBERACEAE PATHOGENS in vitro antibacterial activity minimum inhibitory concentration(MIC) minimum bactericidal concentration(MBC) high-performance liquid chromatography-tandem mass spectrometry(UPLC-MS/MS)
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IN VITRO ANTITUMOR ACTIVITY OF TUMOR-INFILTRATING LYMPHOCYTES FROM HUMAN GASTRIC CARCINOMA
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作者 王宏志 黄信孚 +2 位作者 林本耀 阳兰桂 姚丽华 《Chinese Journal of Cancer Research》 SCIE CAS CSCD 1991年第2期21-24,共4页
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
关键词 TIL LAK in vitro ANTITUMOR activity OF TUMOR-inFILTRATinG LYMPHOCYTES FROM HUMAN GASTRIC CARCinOMA
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Effects of Buyang Huanwu decoction and Astragalus mongholicus on platelet activating factor receptor activity in rabbits in vitro
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作者 Hui Yao1, Jiping Zhang2, Zhixi Chen3, Yongjie Wu4, Zhiqiang Li3 1Department of Pharmacy, 2Department of Science Education, Foshan Second People’s Hospital, Foshan 528000, Guangdong Province, China 3Laboratory of Nuclear Medicine, Guangzhou University of Traditional Chinese Medicine, Guangzhou 510405, Guangdong Province, China 4Department of Pharmacology, College of Pharmaceutical Science, Lanzhou University, Lanzhou 730000, Gansu Province, China 《Neural Regeneration Research》 SCIE CAS CSCD 2006年第7期634-637,共4页
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
关键词 PAFR Effects of Buyang Huanwu decoction and Astragalus mongholicus on platelet activating factor receptor activity in rabbits in vitro
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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 被引量:3
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作者 Zhe Liu Jiagan Zhang +3 位作者 Shengmin Lu Weimin Tang Yibin Zhou Siew Young Quek 《Food Science and Human Wellness》 SCIE 2022年第2期366-373,共8页
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
关键词 Chinese bayberry Drying Phenolic components Antioxidant activities in vitro hypoglycemic activities
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Microwave Solvothermal Synthesis, Crystal Structures and in Vitro Antitumor Activities of Di-n-butyltin Piperonylate with a Sn4O4 Ladder Framework
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作者 邝代治 冯泳兰 +3 位作者 蒋伍玖 朱小明 庾江喜 张复兴 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2018年第8期1265-1271,共7页
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
关键词 di-n-butyltin piperonylate microwave solvothermal synthesis ladder-likeframework in vitro antitumor activity
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Effects of Ages of Donors and Conditions of Preserving Ovaries on Porcine Oocytes Maturation in vitro and Efficiency of Parthenogenetic Activation
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作者 XINGFeng-ying WUZhong-hong +4 位作者 ZENGShen-ming LIUGuo-shi ZHUShi-en ZHANGZhong-cheng CHENXue-jin 《Agricultural Sciences in China》 CAS CSCD 2004年第6期475-480,共6页
Effects of different ages of donors and different conditions of preserving ovaries onporcine oocytes maturation in vitro and efficiency of parthenogenetic activation werestudied. The experiments included: 1) effects o... Effects of different ages of donors and different conditions of preserving ovaries onporcine oocytes maturation in vitro and efficiency of parthenogenetic activation werestudied. The experiments included: 1) effects of different temperatures (22, 30, 37, 38.5and 40℃) of preserving ovaries on porcine oocytes maturation in vitro and developmentalpotential; 2) effects of periods of preserving ovaries on porcine oocytes maturation invitro and development in vitro; 3) effects of different ages of donors on porcine oocytesmaturation in vitro and developmental potential. The results of the experiment showed:1) There were no statistical differences (p>0.05) of the parthenogenetic cleavage rate(79.64% vs 76.18%) and blastocyst rate (18.11% vs 33.82%) between oocytes from ovariespreserved at 38.5℃ and those preserved at 37℃. When the preserving temperature wasincreased to 40℃, the cleavage rate (21.68%) and the blastocyst rate (0) were greatsignificantly lower than those at 37℃(p<0.01). The cleavage rate (80.79% vs 76.18%) andblastocyst rate (29.61% vs 33.82%) were not different between 30 and 37℃(p>0.05). Whenthe preserving temperature was decreased to 22℃, the rate of cleavage was not different,but the rate of blastocyst was significantly lower, compared with that at 37℃; 2) Thecleavage and blastocyst rates of the porcine oocytes collected after slaughter 2 or 6hwere not different (p>0.05); 3) The cleavage rate of oocytes from gilts and sows aftermaturation was not different, but the blastocyst rate of the sow group was significantlyhigher than that of gilt group (p<0.05). The blastocyst cell number of sows and giltshowed no difference (p>0.05). 展开更多
关键词 Porcine Oocytes Maturation in vitro Parthenogenetic activation
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Introduction of NKT cell,a novel immunoregulatory subset and in vitro studies in lving activated NKT cell
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作者 Deming Sun 《中国输血杂志》 CAS CSCD 2001年第S1期301-305,共5页
关键词 NKT introduction of NKT cell a novel immunoregulatory subset and in vitro studies in lving activated NKT cell
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Physicochemical properties,antioxidant and anti-inflammatory activities of coumarin-carbonodithioate hybrids
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作者 Suresh S.Kumbar Kallappa M.Hosamani Arun K.Shettar 《Asian Pacific Journal of Tropical Biomedicine》 SCIE CAS 2018年第4期201-206,共6页
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 cyc... 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. 展开更多
关键词 Physicochemical properties Coumarin-carbonodithioates in vitro antioxidant activity in vitro anti-inflammatory activity
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Antioxidant Activities of Crude Phlorotannins from Sargassum hemiphyllum
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作者 赵智丽 杨小青 +3 位作者 龚忠勤 潘明珠 韩雅莉 刘义 《Journal of Huazhong University of Science and Technology(Medical Sciences)》 SCIE CAS 2016年第3期449-455,共7页
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 phlorotanni... 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. 展开更多
关键词 Sargassum hemiphyllum phlorotannins antioxidant activities in vitro in vivo
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Synthesis and in vitro antimicrobial activity of N-arylquinoline derivatives bearing 2-morpholinoquinoline moiety 被引量:2
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作者 Jigar A.Makawana Manish P.Patel Ranjan G.Patel 《Chinese Chemical Letters》 SCIE CAS CSCD 2012年第4期427-430,共4页
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
关键词 N-arylquinoline 2-Morpholinoquinoline-3-carbaldehyde in vitro antimicrobial activity MCR
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Synthesis and in vitro antitumor activity of novel diaryl urea derivatives 被引量:3
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作者 Yan-Fang Zhao Zi-Jian Liu +3 位作者 Xin Zhai Dan-Dan Ge Qiang Huang Ping Gong 《Chinese Chemical Letters》 SCIE CAS CSCD 2013年第5期386-388,共3页
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
关键词 Diaryl ureas SYNTHESIS Antitumor activity in vitro
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Study of Aldo-keto Reductase 1C3 Inhibitor with Novel Framework for Treating Leukaemia Based on Virtual Screening and In vitro Biological Activity Testing
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作者 LIU Fei LI Ren +5 位作者 YE Jing REN Yujie TANG Zhipeng LI Rongchen ZHANG Cuihua LI Qunlin 《Chemical Research in Chinese Universities》 SCIE CAS CSCD 2021年第3期778-786,共9页
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 ... 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. 展开更多
关键词 Virtual screening in vitro biological activity test Absorption distribution metabolism excretion and toxicity(ADMET)prediction Aldo-keto reductase 1C3(AKR1C3)inhibitor LEUKAEMIA
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Design,synthesis,in vitro evaluation of tetrahydropyrimidine-isatin hybrids as potential antibacterial,antifungal and anti-tubercular agents 被引量:7
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作者 Tarunkumar Nanjibhai Akhaja Jignesh Priyakant Raval 《Chinese Chemical Letters》 SCIE CAS CSCD 2012年第4期446-449,共4页
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
关键词 Tetrahydropyrimidines ISATin 1 3-Dihydro-2H-indol-2-ones Biginelli reaction CaCl_2 catalyst in vitro antituberculer activity Antibacterial and antifungal activity
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Secondary metabolites of rice sheath blight pathogen Rhizoctonia solani Kühn and their biological activities 被引量:4
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作者 XU Liang WANG Xiao-han +5 位作者 LUO Rui-ya LU Shi-qiong GUO Ze-jian WANG Ming-an LIU Yang ZHOU Li-gang 《Journal of Integrative Agriculture》 SCIE CAS CSCD 2015年第1期80-87,共8页
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-hydroxy... 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. 展开更多
关键词 rice sheath blight Rhizoctonia solani Kuhn secondary metabolites BIOACTIVITIES in vitro phytotoxic activity
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Study on Targeting and in vitro Anti-oxidation of Baicalin Solid Lipid Nanoparticles 被引量:4
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作者 MIYAMURA Mitsuhiko +3 位作者 YOKOTA Junko YOSHIOKA Saburo 《Chinese Herbal Medicines》 CAS 2012年第4期335-339,共5页
Objective To prepare liver-targeted baicalin solid lipid nanoparticles(BSLNs) and to study their in vitro anti-oxidative activity.Methods BSLNs were prepared by emulsification ultrasonic dispersion method and characte... Objective To prepare liver-targeted baicalin solid lipid nanoparticles(BSLNs) and to study their in vitro anti-oxidative activity.Methods BSLNs were prepared by emulsification ultrasonic dispersion method and characterized by transmission electron microscopy and laser particle size distribution;The tissue in vivo distribution was detected by pharmacokinetics;In vitro anti-superoxide dismutase(SOD) activity and reduction capacity of BSLNs were determined;The ability of removing hydroxyl radical was determined by phenanthroline-Fe2+ oxidation.Results The best prescription was baicalin-soybean lecithin-glyceryl monostearate-poloxamer 188(1:5:15:30);The encapsulation efficiency and drug loading were 84.7% and 5.65%,respectively,mean size of particles was(68.6 ± 8) nm,Zeta potential was 22.13 mV;The in vitro anti-oxidant results showed that BSLNs had a significant inhibitory effect on SOD and a strong reducing capacity as well as a removing hydroxide radical ability.The targeting rate of BSLNs was 6.931 for liver.Conclusion The results demonstrate that BSLNs could enhance the liver targeting ability and in vitro anti-oxidative activity significantly. 展开更多
关键词 BAICALin in vitro anti-oxidative activity liver-targeted solid lipid nanoparticals tissue distribution
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Synthesis and structure-activity relationships study ofα-aminophosphonate derivatives containing a quinoline moiety 被引量:1
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作者 Xi-Feng Zhu Jing Zhang +3 位作者 Shuo Sun Yan-Chun Guo Shu-Xia Cao Yu-Fen Zhao 《Chinese Chemical Letters》 SCIE CAS CSCD 2017年第7期1514-1518,共5页
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
关键词 Quinoline a-Aminophosphonate Synthesis Antitumor activity in vitro
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Anthelmintic, antimicrobial, antioxidant and cytotoxic activity of Caltha palustris var. alba Kashmir, India 被引量:1
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作者 Sofi Mubashir Mohd Yousuf Dar +2 位作者 Bashir A.Lone M.Iqbal Zargar Wajaht A.Shah 《Chinese Journal of Natural Medicines》 SCIE CAS CSCD 2014年第8期567-572,共6页
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
关键词 Caltha palustris var.alba Anthelmintic activity(in vivo and in vitro) Antimicrobial activity Cytotoxic activity Radical scavenging activity
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