Department of Pharmacognosy and Pharmaceutical Botany, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat-Yai, Songkhla 90112, Thailand.
Pharm Biol. 2013 Oct;51(10):1256-61. doi: 10.3109/13880209.2013.786098. Epub 2013 Jul 11.
HIV-1 integrase (HIV-1 IN) is a key enzyme involved in the replication cycle of the retrovirus. Any new knowledge on inhibitors of this enzyme could provide essential clues for the development of anti-HIV drugs.
To evaluate anti-HIV-1 IN activity of some Thai medicinal plant extracts, and the extract that possessed the strongest anti-HIV-1 IN activity was subjected to isolation of the active compounds.
Ethanol extracts of eight Thai medicinal plants were evaluated for their inhibitory effect against HIV-1 IN. An extract of Pometia pinnata J. R. Forst. & G. Forst (Sapindaceae) leaves that possessed the strongest anti-HIV-1 IN activity was fractionated to isolate the active compounds by anti-HIV-1 IN assay-guided isolation process.
The leaf extract from P. pinnata had the strongest anti-HIV-1 IN activity with an IC50 value of 8.8 µg/mL. An anti-HIV-1 IN assay-guided isolation of the active compounds from a leaf extract of P. pinnata resulted in the isolation of one active compound, identified as proanthocyanidin A2. Proanthocyanidin A2 showed satisfactory anti-HIV-1 IN activity with an IC50 value of 30.1 µM. Three flavonoids, epicatechin, kaempferol-3-O-rhamnoside, quercetin-3-O-rhamnoside; a glycolipid, 1-O-palmitoyl-3-O-[α-.-galactopyranosyl-(1 → 6)-β-.-galactopyranosyl]-sn-glycerol; a steroidal glycoside; stigmasterol-3-O-glucoside; and a pentacyclic triterpenoid saponin, 3-O-α-.-arabinofuranosyl-(1 → 3)-[α-.-rhamnopyranosyl-(1 → 2)]-α-.-arabinopyranosyl hederagenin were also isolated but were inactive at a concentration of 100 µM.
HIV-1 整合酶（HIV-1 IN）是参与逆转录病毒复制周期的关键酶。任何关于该酶抑制剂的新认识都可能为抗 HIV 药物的开发提供重要线索。
评估八种泰国药用植物提取物的抗 HIV-1 IN 活性，对具有最强抗 HIV-1 IN 活性的提取物进行活性化合物的分离。
评估八种泰国药用植物的乙醇提取物对 HIV-1 IN 的抑制作用。具有最强抗 HIV-1 IN 活性的 Pometia pinnata J. R. Forst. & G. Forst（无患子科）叶提取物通过抗 HIV-1 IN 测定指导的分离过程进行分离以获得活性化合物。
P. pinnata 的叶提取物具有最强的抗 HIV-1 IN 活性，IC50 值为 8.8 µg/mL。抗 HIV-1 IN 测定指导的 P. pinnata 叶提取物中活性化合物的分离导致分离出一种活性化合物，鉴定为原花青素 A2。原花青素 A2 显示出令人满意的抗 HIV-1 IN 活性，IC50 值为 30.1 µM。分离出三种类黄酮，表儿茶素、山柰酚-3-O-鼠李糖苷、槲皮素-3-O-鼠李糖苷；一种糖脂，1-O-棕榈酰基-3-O-[α-.-半乳糖吡喃基-(1 ⁇ 6)-β-.-半乳糖吡喃基]-sn-甘油；一种甾体糖苷，豆甾醇-3-O-葡萄糖苷；和一种五环三萜皂苷，3-O-α-.-阿拉伯呋喃糖基-(1 ⁇ 3)-[α-.-鼠李吡喃糖基-(1 ⁇ 2)]-α-.-阿拉伯吡喃糖基齐墩果酸也被分离出来，但在 100 µM 浓度下没有活性。
