title: Inhibition of HIV-1 reverse transcriptase, toxicological and chemical profile of Calophyllum brasiliense extracts from Chiapas, Mexico.
abstract: Calophyllum species are sources of calanolides, which inhibit human immunodeficiency virus type 1 reverse transcriptase (HIV-1 RT). The hexane extract of the leaves from C. brasiliense collected in Soconusco, State of Chiapas, Mexico, analyzed by HPLC showed to contain apetalic acid, calanolides B, and C. It showed potent anti-HIV-1 RT inhibition (IC(50)=20.2 μg/ml), but was not toxic in mice (LD(50)=1.99 g/kg). The histological study of the mice treated at the highest dose revealed no alteration on hepatocytes, and an increase in the number of spleen megakaryocytes. These results suggest this extract is suitable to continue studies for developing a phytodrug against HIV-1.
authors: Instituto de Química, Universidad Nacional Autónoma de México, D.F., México.
authors: García-Zebadúa Julio
authors: GZ
authors: César
authors: Magos-Guerrero Gil
authors: MG
authors: Alfonso
authors: Mumbrú-Massip
authors: MM
authors: Marius
authors: Estrada-Muñoz
authors: EM
authors: Elizabeth
authors: Contreras-Barrios Miguel
authors: CB
authors: Angel
authors: Huerta-Reyes
authors: HR
authors: Maira
authors: Campos-Lara María
authors: CL
authors: Guadalupe
authors: Jiménez-Estrada
authors: JE
authors: Manuel
authors: Reyes-Chilpa
authors: RC
authors: Ricardo
mesh_terms: D000818:Animals; D029759:Calophyllum / Q000009:adverse effects / Q000737:chemistry*; D015658:HIV Infections / Q000188:drug therapy / Q000821:virology; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors*; D015497:HIV-1 / Q000201:enzymology; D022781:Hepatocytes / Q000187:drug effects; D006801:Humans; D007529:Isoflavones / Q000009:adverse effects / Q000032:analysis / Q000494:pharmacology*; D008297:Male; D008533:Megakaryocytes / Q000187:drug effects; D008800:Mexico; D051379:Mice; D008517:Phytotherapy; D010936:Plant Extracts / Q000009:adverse effects / Q000737:chemistry / Q000494:pharmacology*; D018515:Plant Leaves; D039681:Pyranocoumarins / Q000009:adverse effects / Q000032:analysis / Q000494:pharmacology*; D018894:Reverse Transcriptase Inhibitors / Q000009:adverse effects / Q000032:analysis / Q000494:pharmacology*; D013154:Spleen / Q000187:drug effects
chemical_list: D007529:Isoflavones; D010936:Plant Extracts; D039681:Pyranocoumarins; D018894:Reverse Transcriptase Inhibitors; C570384:apetalic acid; C570383:calanolide C; C075958:calanolide B; C514824:reverse transcriptase, Human immunodeficiency virus 1; D054303:HIV Reverse Transcriptase