Anti-HIV-1 Activities of Hemslecins A and B
文献类型：期刊论文
| 作者 | Tian RR1,5; Chen JC2,4; Zhang GH1; Qiu MH2; Wang YH1,4; Du L3,4; Shen X3; Liu NF5; Zheng YT[*]1 |
| 刊名 | Chinese Journal of Natural Medicines
 |
| 出版日期 | 2008 |
| 卷号 | 6期号:3页码:214-218 |
| 通讯作者 | zhengyt@mail.kiz.ac.cn |
| 合作状况 | 其它 |
| 中文摘要 | 目的:研究从药用植物金佛山雪胆分离的雪胆素A和雪胆素B两个三萜类化合物的体外抗HIV活性。方法:应用合胞体抑制实验、p24抗原产生的抑制实验、慢性感染细胞和正常细胞间的细胞融合抑制实验等技术检测化合物的体外抗HIV-1活性;利用HIV-1逆转录酶、蛋白酶抑制实验,NCp7锌离子逐出实验探讨化合物的作用机制。结果:雪胆素A和雪胆素B在体外有较好的抑制HIV-1活性,其活性主要表现为:(1)抑制HIV-1诱导合胞体形成,EC50值分别为3.09μg.mL-1和2.53μg.mL-1;(2)抑制HIV-1急性感染的C8166细胞p24抗原产生,EC50值分别为3.97μg.mL-1和18.90μg.mL-1; (3)抑制HIV-1慢性感染H9与正常C8166细胞间融合, EC50分别为1.76μg.mL-1和11.95μg.mL-1。雪胆素A和雪胆素B对HIV-1逆转录酶、蛋白酶、NCp7锌离子逐出均没有抑制作用。雪胆素A对HIV-1整合酶有微弱的结合活性,而雪胆素B对HIV-1整合酶没有结合活性。在共培养实验中,雪胆素A和雪胆素B预处理C8166细胞组比未经预处理细胞组能够更有效的抑制HIV-1活性。结论:化合物雪胆素A和雪胆素B体外有较好的抗HIV-1活性,可能主要作用于HIV-1病毒进入细胞阶段。 |
| 英文摘要 | AIM: To study anti-HIV-1 activities of two triterpenoids, hemslecins A and B from a Chinese medicinal plant Hemsleya jinfushanensis. METHODS: The cellular inhibitory assays on syncytia formation induced by HIV-1, p24 antigen production in HIV-1 acutely infected C8166 cells, cell-to-cell fusion between HIV-1 chronically infected H9 cells and normal C8166 cells, and p24 production from HIV-1 chronically infected H9 cells were assayed. The effects on NCp7 zinc ejection and inhibitory activities against HIV-1 reverse transcriptase (RT) and protease (PR) were also detected. RESULTS: The hemslecins A and B with inhibitory effects on (1) syncytia formation induced by HIV-1 with EC50 values of 3.09 and 2.53 mu g.mL(-1) respectively, (2) p24 antigen production in HIV-1 acutely infected C8166 cells with EC50 of 3.97 and 18.90 mu g.mL(-1) respectively, and (3) fusion between HIV-1 chronically infected H9 cells and C8166 cells with EC50 of 1.76 mu g.mL(-1) and 11.95 mu g.mL(-1), respectively. But hemslecins A and B failed to show inhibitory activity against HIV-1 RT, PR, and NCp7 zinc ejection. Hemslecin A not hemslecin B showed slight interaction with HIV-1 integrase. In co-culture assay, hemslecins A and B showed more effect in pretreated C8166 cells group than no pretreated group. CONCLUSION: The hemslecins A and B are bioactive compounds against HIV-1 and their action mechanism might be correlated with virus entry. |
| 收录类别 | 其他 |
| 资助信息 | 国家“十五”科技攻关计划(2004BA719A14);云南省科技攻关计划(2004NG12);中国科学院知识创新工程重要方向(KSCX1-YW-R-4)项目 |
| 语种 | 英语 |
| 公开日期 | 2010-08-04 |
| 源URL | [http://159.226.149.42:8088/handle/152453/905]  |
| 专题 | 昆明动物研究所_分子免疫药理学 昆明动物研究所_动物模型与人类重大疾病机理重点实验室 |
| 作者单位 | 1.Laboratory of Molecular Immunopharmacology,Key Laboratory of Animal Models and Human Disease Mechanisms,Kunming Institute of Zoology,Chinese Academy of Sciences,Kunming 650223 2.State Key Laboratory of Phytochemistry and Plant Resources in West China,Kunming Institute of Botany,Chinese Academy of Sciences,Kunming 650204 3.State Key Laboratory of Drug Research,Shanghai Institute of Materia Medica,Chinese Academy of Sciences,Shanghai 201203 4.Graduate School of the Chinese Academy of Sciences,Beijing 100039 5.School of Life Science,Lanzhou University,Lanzhou 730000,China |
| 推荐引用方式 GB/T 7714 | Tian RR,Chen JC,Zhang GH,et al. Anti-HIV-1 Activities of Hemslecins A and B[J]. Chinese Journal of Natural Medicines,2008,6(3):214-218. |
| APA | Tian RR.,Chen JC.,Zhang GH.,Qiu MH.,Wang YH.,...&Zheng YT[*].(2008).Anti-HIV-1 Activities of Hemslecins A and B.Chinese Journal of Natural Medicines,6(3),214-218. |
| MLA | Tian RR,et al."Anti-HIV-1 Activities of Hemslecins A and B".Chinese Journal of Natural Medicines 6.3(2008):214-218. |
入库方式： OAI收割
来源：昆明动物研究所
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