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Molecules 2012, 17(6), 6916-6929; doi:10.3390/molecules17066916

Potent Anti-HIV Activities and Mechanisms of Action of a Pine Cone Extract from Pinus yunnanensis

1 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 2 School of Pharmaceutical Science, Kunming Medical University, Kunming 650500, China 3 Graduate School of the Chinese Academy of Science, Beijing 100039, China 4 School of Pharmacy, Dali University, Dali 671000, China 5 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 / Revised: 26 May 2012 / Accepted: 31 May 2012 / Published: 6 June 2012
(This article belongs to the Section Natural Products)
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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 Pinus yunnanensis; pine cone; anti-HIV activity; reverse transcriptase; fusion
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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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.

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