title: Anti-HIV-1 integrase activity of Mimusops elengi leaf extracts.
abstract: BACKGROUND
  Integrase (IN) is one of the three human immunodeficiency virus type 1 (HIV-1) enzymes that, together with a reverse transcriptase and protease, allow the virus to reproduce itself after infecting the host cells. Any new knowledge on inhibitors of this enzyme could provide essential clues for the development of anti-HIV drugs.
  
  
  OBJECTIVE
  To evaluate the anti-HIV-1 IN activity of some Thai medicinal plant extracts, and to isolate the active compounds from the extract that possessed the strongest anti-HIV-1 IN activity.
  
  
  METHODS
  Ethanol extracts of eight Thai medicinal plants (10-100 µg/mL) were evaluated for their inhibitory effect against HIV-1 IN. An extract of Mimusops elengi L. (Sapotaceae) leaves that possessed the strongest anti-HIV-1 IN activity was fractionated to isolate the active compounds by an anti-HIV-1 IN assay-guided isolation process.
  
  
  CONCLUSIONS
  The leaf extract from M. elengi had the strongest anti-HIV-1 IN activity with an IC₅₀ value of 62.1 µg/mL. A bioassay-guided isolation of the active compounds from M. elengi leaf extract resulted in the isolation of active compounds, identified as a mixture of gallocatechin and epigallocatechin. This mixture of gallocatechin and epigallocatechin showed satisfactory anti-HIV-1 IN activity with an IC₅₀ value of 35.0 µM. A flavanol glycoside, mearnsitrin was also isolated but was inactive at a concentration of 100 µM.
authors.affiliation: Department of Pharmacognosy and Pharmaceutical Botany and.
authors.forename: A
authors.initials: A
authors.lastname: Suedee
authors.forename: S
authors.initials: S
authors.lastname: Tewtrakul
authors.forename: P
authors.initials: P
authors.lastname: Panichayupakaranant
mesh_terms: D001681:Biological Assay; D002392:Catechin / Q000031:analogs & derivatives / Q000302:isolation & purification / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D019427:HIV Integrase / Q000187:drug effects* / Q000378:metabolism; D019428:HIV Integrase Inhibitors / Q000008:administration & dosage / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D032130:Mimusops / Q000737:chemistry*; D010078:Oxazines / Q000302:isolation & purification / Q000494:pharmacology; D010936:Plant Extracts / Q000008:administration & dosage / Q000494:pharmacology*; D010946:Plants, Medicinal / Q000737:chemistry; D013785:Thailand
chemical_list: D019428:HIV Integrase Inhibitors; D010078:Oxazines; D010936:Plant Extracts; D002392:Catechin; C007062:gallocyanine; D019427:HIV Integrase; C057580:gallocatechol; C514801:p31 integrase protein, Human immunodeficiency virus 1