云南松松果提取物的抗 HIV 活性及其作用机制。

Potent anti-HIV activities and mechanisms of action of a pine cone extract from Pinus yunnanensis.

机构信息

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.

出版信息

Molecules. 2012 Jun 6;17(6):6916-29. doi: 10.3390/molecules17066916.

DOI:10.3390/molecules17066916

PMID:22728366

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6268540/

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-1(IIIB), HIV-1(RF), HIV-1(A17), HIV-1(AO18) and HIV-2(ROD) 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-1(IIIB), HIV-1RF, HIV-1(A17) and HIV-1(AO18) in C8166 cells. An MTT assay showed that YNS-PY-F also significantly inhibited the HIV-1(IIIB) 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-1(IIIB), HIV-1(RF), RT inhibitor-resistant strains HIV-1(A17) and HIV-1(AO18), and HIV-2(ROD), and its anti-HIV mechanisms include inhibition of HIV entry and inhibition of reverse transcriptase activity.

摘要

从云南松的松果中提取的抗 HIV 活性物质（YNS-PY-F）进行了评估，并对其作用机制进行了探讨。松果提取物 YNS-PY-F 能有效抑制 HIV-1(IIIB)、HIV-1(RF)、HIV-1(A17)、HIV-1(AO18)和 HIV-2(ROD)，并在 C8166 细胞中产生细胞病变效应，其 EC₅₀ 值分别为 0.96μg/mL、1.53μg/mL、0.88μg/mL、7.20μg/mL 和 6.17μg/mL。p24 产量测定表明，YNS-PY-F 显著抑制 C8166 细胞中 HIV-1(IIIB)、HIV-1RF、HIV-1(A17)和 HIV-1(AO18)的急性复制。MTT 分析表明，YNS-PY-F 还显著抑制 HIV-1(IIIB)诱导的 MT-4 细胞裂解，EC₅₀ 值为 2.22μg/mL。机制研究表明，YNS-PY-F 对感染细胞与未感染细胞融合以及 HIV-1 逆转录酶活性均有很强的抑制作用，EC₅₀ 值分别为 7.60μg/mL 和 4.60μg/mL。综上所述，这些数据表明，云南松松果提取物对 HIV-1(IIIB)、HIV-1(RF)、RT 抑制剂耐药株 HIV-1(A17)和 HIV-1(AO18)以及 HIV-2(ROD)均具有较强的抑制活性，其抗 HIV 机制包括抑制 HIV 进入和抑制逆转录酶活性。