College of Pharmacy, Chungnam National University, Daejeon, Korea.
Pharm Biol. 2011 Oct;49(10):1046-51. doi: 10.3109/13880209.2011.563316. Epub 2011 May 20.
Acquired immune deficiency syndrome (AIDS) is a severe pandemic disease especially prevalent in poor and developing countries. Thus, developing specific, potent antiviral drugs that restrain infection by human immunodeficiency virus type 1 (HIV-1), a major cause of AIDS, remains an urgent priority.
This study evaluated 32 extracts and 23 compounds from Vietnamese medicinal plants for their inhibitory effects against HIV-1 ribonuclease H (RNase H) and their role in reversing the cytopathic effects of HIV.
The plants were air-dried and extracted in different solvent systems to produce plant extracts. Natural compounds were obtained as previously published. Samples were screened for RNase H inhibition followed by a cytopathic assay. Data were analyzed using the Microsoft Excel.
At 50 μg/mL, 11 plant extracts and five compounds inhibited over 90% of RNase H enzymatic activity. Methanol extracts from Phyllanthus reticulatus and Aglaia aphanamixis leaves inhibited RNase H activity by 99 and 98%, respectively, whereas four extracts showed modest protection against the cytopathic effects of HIV.
The screening results demonstrated that the butanol (BuOH) extract of Celastrus orbiculata leaves, methanol (MeOH) extracts of Glycosmis stenocarpa stems, Eurya ciliata leaves, and especially P. reticulatus leaves showed potential RNase H inhibition and protection against the viral cytopathic effects of HIV-1. Further chemical investigations should be carried out to find the active components of these extracts and compounds as potential anti-HIV drug candidates.
获得性免疫缺陷综合征（AIDS）是一种严重的流行疾病，尤其在贫穷和发展中国家普遍存在。因此，开发能够特异性抑制感染人类免疫缺陷病毒 1 型（HIV-1）的抗病毒药物仍然是当务之急，HIV-1 是 AIDS 的主要病因。
本研究评估了 32 种来自越南药用植物的提取物和 23 种化合物对 HIV-1 核糖核酸酶 H（RNase H）的抑制作用及其逆转 HIV 细胞病变作用的能力。
将植物风干后，用不同溶剂系统提取，得到植物提取物。天然化合物如前所述获得。样品经 RNase H 抑制筛选后，进行细胞病变测定。数据使用 Microsoft Excel 进行分析。
在 50μg/mL 时，有 11 种植物提取物和 5 种化合物对 RNase H 酶活性的抑制率超过 90%。叶下珠和乌墨的甲醇提取物对 RNase H 活性的抑制率分别为 99%和 98%，而有 4 种提取物对 HIV 的细胞病变有一定的保护作用。
筛选结果表明，三叶苦的正丁醇（BuOH）提取物、桃金娘科糯米条的甲醇（MeOH）提取物、黄瑞木的叶、特别是叶下珠的提取物具有潜在的 RNase H 抑制和保护 HIV-1 病毒细胞病变的作用。应进一步进行化学研究，以发现这些提取物和化合物的活性成分，作为潜在的抗 HIV 药物候选物。
