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Potent Anti-HIV Activities and Mechanisms of Action of a Pine Cone Extract from Pinus yunnanensis
Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Science & Yunnan province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, China
School of Pharmaceutical Science, Kunming Medical University, Kunming 650500, China
Graduate School of the Chinese Academy of Science, Beijing 100039, China
School of Pharmacy, Dali University, Dali 671000, China
School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China
These authors contributed equally to the work.
* Author to whom correspondence should be addressed.
Received: 5 April 2012; in revised form: 26 May 2012 / Accepted: 31 May 2012 / Published: 6 June 2012
Abstract: The anti-HIV activities of a pine cone extract (YNS-PY-F) from Pinus yunnanensis have been evaluated, and its mechanisms of action were also explored. The pine cone extract, YNS-PY-F, potently inhibited HIV-1IIIB, HIV-1RF, HIV-1A17, HIV-1AO18 and HIV-2ROD and induced cytopathic effect in C8166 cells with EC50 values of 0.96 μg/mL, 1.53 μg/mL, 0.88 μg/mL, 7.20 μg/mL and 6.17 μg/mL, respectively. The quantification of a p24 production assay showed that YNS-PY-F significantly inhibited the acute replication of HIV-1IIIB, HIV-1RF, HIV-1A17 and HIV-1AO18 in C8166 cells. An MTT assay showed that YNS-PY-F also significantly inhibited the HIV-1IIIB induced cytolysis in MT-4 cells with an EC50 value of 2.22 μg/mL. The mechanism assays showed that YNS-PY-F had potent inhibitory effects on the fusion between infected cells and uninfected cells, and the activity of HIV-1 reverse transcriptase, with EC50 values of 7.60 μg/mL and 4.60 μg/mL, respectively. Overall, these data suggest that the pine cone extract from Pinus yunnanensis has potent inhibitory activities against HIV-1IIIB, HIV-1RF, RT inhibitor-resistant strains HIV-1A17 and HIV-1AO18, and HIV-2ROD, and its anti-HIV mechanisms include inhibition of HIV entry and inhibition of reverse transcriptase activity.
Keywords: Pinus yunnanensis; pine cone; anti-HIV activity; reverse transcriptase; fusion
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Zhang, X.; Yang, L.-M.; Liu, G.-M.; Liu, Y.-J.; Zheng, C.-B.; Lv, Y.-J.; Li, H.-Z.; Zheng, Y.-T. Potent Anti-HIV Activities and Mechanisms of Action of a Pine Cone Extract from Pinus yunnanensis. Molecules 2012, 17, 6916-6929.
Zhang X, Yang L-M, Liu G-M, Liu Y-J, Zheng C-B, Lv Y-J, Li H-Z, Zheng Y-T. Potent Anti-HIV Activities and Mechanisms of Action of a Pine Cone Extract from Pinus yunnanensis. Molecules. 2012; 17(6):6916-6929.
Zhang, Xuan; Yang, Liu-Meng; Liu, Guang-Ming; Liu, Ya-Juan; Zheng, Chang-Bo; Lv, Yong-Jun; Li, Hao-Zhi; Zheng, Yong-Tang. 2012. "Potent Anti-HIV Activities and Mechanisms of Action of a Pine Cone Extract from Pinus yunnanensis." Molecules 17, no. 6: 6916-6929.