PMID- 23844583 OWN - NLM STAT- MEDLINE DCOM- 20140324 LR - 20181202 IS - 1744-5116 (Electronic) IS - 1388-0209 (Linking) VI - 51 IP - 10 DP - 2013 Oct TI - Anti-HIV-1 integrase compound from Pometia pinnata leaves. PG - 1256-61 LID - 10.3109/13880209.2013.786098 [doi] AB - CONTEXT: 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. OBJECTIVE: 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. MATERIALS AND METHODS: 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. RESULTS AND DISCUSSION: The leaf extract from P. pinnata had the strongest anti-HIV-1 IN activity with an IC50 value of 8.8 microg/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 microM. Three flavonoids, epicatechin, kaempferol-3-O-rhamnoside, quercetin-3-O-rhamnoside; a glycolipid, 1-O-palmitoyl-3-O-[alpha-.-galactopyranosyl-(1 --> 6)-beta-.-galactopyranosyl]-sn-glycerol; a steroidal glycoside; stigmasterol-3-O-glucoside; and a pentacyclic triterpenoid saponin, 3-O-alpha-.-arabinofuranosyl-(1 --> 3)-[alpha-.-rhamnopyranosyl-(1 --> 2)]-alpha-.-arabinopyranosyl hederagenin were also isolated but were inactive at a concentration of 100 microM. FAU - Suedee, Areerat AU - Suedee A AD - Department of Pharmacognosy and Pharmaceutical Botany, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat-Yai, Songkhla 90112, Thailand. FAU - Tewtrakul, Supinya AU - Tewtrakul S FAU - Panichayupakaranant, Pharkphoom AU - Panichayupakaranant P LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't DEP - 20130711 PL - England TA - Pharm Biol JT - Pharmaceutical biology JID - 9812552 RN - 0 (HIV Integrase Inhibitors) RN - 0 (Plant Extracts) RN - 0 (Solvents) RN - 3K9958V90M (Ethanol) RN - EC 2.7.7.- (HIV Integrase) RN - YY6481J2FF (p31 integrase protein, Human immunodeficiency virus 1) SB - IM MH - Chemical Fractionation MH - Ethanol/chemistry MH - HIV Integrase/*metabolism MH - HIV Integrase Inhibitors/chemistry/isolation & purification/*pharmacology MH - Phytotherapy MH - Plant Extracts/chemistry/isolation & purification/*pharmacology MH - Plant Leaves MH - Plants, Medicinal MH - *Sapindaceae/chemistry MH - Solvents/chemistry EDAT- 2013/07/13 06:00 MHDA- 2014/03/25 06:00 CRDT- 2013/07/13 06:00 PHST- 2013/07/13 06:00 [entrez] PHST- 2013/07/13 06:00 [pubmed] PHST- 2014/03/25 06:00 [medline] AID - 10.3109/13880209.2013.786098 [doi] PST - ppublish SO - Pharm Biol. 2013 Oct;51(10):1256-61. doi: 10.3109/13880209.2013.786098. Epub 2013 Jul 11.