title: Anti-HIV-1 integrase compound from Pometia pinnata leaves.
abstract: BACKGROUND
  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.
  
  
  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.
  
  
  CONCLUSIONS
  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.
authors.affiliation: Department of Pharmacognosy and Pharmaceutical Botany, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat-Yai, Songkhla 90112, Thailand.
authors.forename: Areerat
authors.initials: A
authors.lastname: Suedee
authors.forename: Supinya
authors.initials: S
authors.lastname: Tewtrakul
authors.forename: Pharkphoom
authors.initials: P
authors.lastname: Panichayupakaranant
mesh_terms: D005591:Chemical Fractionation; D000431:Ethanol / Q000737:chemistry; D019427:HIV Integrase / Q000378:metabolism*; D019428:HIV Integrase Inhibitors / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D008517:Phytotherapy; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D018515:Plant Leaves; D010946:Plants, Medicinal; D029631:Sapindaceae / Q000737:chemistry; D012997:Solvents / Q000737:chemistry
chemical_list: D019428:HIV Integrase Inhibitors; D010936:Plant Extracts; D012997:Solvents; D000431:Ethanol; D019427:HIV Integrase; C514801:p31 integrase protein, Human immunodeficiency virus 1