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Wikstroelide M potently inhibits HIV replication by targeting reverse transcriptase and integrase nuclear translocation 期刊论文

编号：

0778e7d6-09a9-4cf0-9b31-0b0374fac7d1
作者：

Zhang Xuan(张旋)#^[1,3,4]Huang ShengZhuo^[2];Gu WanGang^[5];Yang LiuMeng^[1];Chen Huan^[1];Zheng ChangBo(郑昌博)^[6]Zhao YouXing^[2];Wan David ChiCheong^[5];Zheng YongTang*^[1]
语种：

英文
期刊：

CHINESE JOURNAL OF NATURAL MEDICINES ISSN：2095-6975 2014 年 12 卷 3 期 (186 - 193) ; MAR
收录：
关键词：

Wikstroelide M Daphnane diterpene Daphne acutiloba Rehder HIV Reverse trascriptase integrase Nuclear translocation Lens epithelium-derived growth factor (LEDGF/p75) Molecular docking
摘要：

AIM: To evaluate the anti-HIV activity and mechanism of action of wikstroelide M, a daphnane diterpene from Daphne acutiloba Rehder (Thymelaeaceae).
METHOD: The anti-HIV activities of wikstroelide M against different HIV strains were evaluated by cytopathic effect assay and p24 quantification assay with ELISA. The inhibitory effect of wikstroelide M on HIV reverse transcription was analyzed by real-tithe PCR and ELISA. The effect of wikstroelide M on HIV-1 integrase nuclear translocation was observed with a cell-based imaging assay. The effect of wikstroelide M on LEDGF/p75-IN interaction was assayed by molecular docking.
RESULTS: Wikstroelide M potently inhibited different HIV-1 strains, including HIV-1(IIIB), HIV-1(A17), and HIV-1(9495), induced a cytopathic effect, with EC50 values ranging from 3.81 to 15.65 ng.mL(-1). Wikstroelide M also had high inhibitory activities against HIV-2(ROD) and HIV-2(CBL-20)-induced cytopathic effects with EC50 values of 18.88 and 31.90 ng.mL(-1). The inhibitory activities of wikstroelide M (on) the three HIV-1 strains were further confirmed by p24 quantification assay, with EC50 values ranging from 15.16 to 35.57 ng.mL(-1). Wikstroelide M also potently inhibited HIV-1(IIIB) induced cytolysis in MT-4 cells, with an EC50 value of 9.60 ng.mL(-1). The mechanistic assay showed that wikstroelide M targeted HIV-1 reverse transcriptase and nuclear translocation of integrase through disrupting the interaction between integrase and LEDGF/p75.
CONCLUSION: Wikstroelide M may be a potent HIV-1 and HIV-2 inhibitor, the mechanisms of action may include inhibition of reverse trascriptase activity and inhibition of integrase nuclear translocation through disrupting the interaction between integrase and LEDGF/p75.
推荐引用方式
GB/T 7714：

Zhang Xuan,Huang Sheng-Zhuo,Gu Wan-Gang, et al. Wikstroelide M potently inhibits HIV replication by targeting reverse transcriptase and integrase nuclear translocation [J].CHINESE JOURNAL OF NATURAL MEDICINES,2014,12(3):186-193.
APA：

Zhang Xuan,Huang Sheng-Zhuo,Gu Wan-Gang,Yang Liu-Meng,&Zheng Yong-Tang.(2014).Wikstroelide M potently inhibits HIV replication by targeting reverse transcriptase and integrase nuclear translocation .CHINESE JOURNAL OF NATURAL MEDICINES,12(3):186-193.
MLA：

Zhang Xuan, et al. "Wikstroelide M potently inhibits HIV replication by targeting reverse transcriptase and integrase nuclear translocation" .CHINESE JOURNAL OF NATURAL MEDICINES 12,3(2014):186-193.
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