RESUMEN
An anticancer-bioassay guided isolation of the ethanol extract and fractions of two plants from the Peruvian rainforest, Mikania decora and Cremastosperma microcarpum, led to the characterization of one abundant diterpene, ent-pimara-8(14),15-dien-19-oic acid (1), three thymol derivatives, 10-acetoxy-8,9-dehydro-6-methoxythymol butyrate (2), 10-acetoxy-8,9-epoxy-6-methoxythymol isobutyrate (3), and acetylschizoginol (4), as well as one neolignan, (±)-trans-dehydrodiisoeugenol (5). Only the latter was isolated from C. microcarpum. These compounds exhibited significant cytotoxic activity against a panel of human tumor cell lines. Compounds 3 and 4 were also investigated for their in vitro antileishmanial and trypanocidal activity against Leishmania amazonensis axenic amastigotes and Trypanosoma cruzi trypomastigotes.
Asunto(s)
Annonaceae/química , Antiinfecciosos/farmacología , Mikania/química , Extractos Vegetales/química , Animales , Antiinfecciosos/química , Línea Celular Tumoral , Supervivencia Celular , Diterpenos/química , Diterpenos/farmacología , Femenino , Humanos , Leishmania/efectos de los fármacos , Lignanos/química , Lignanos/farmacología , Macrófagos/efectos de los fármacos , Masculino , Ratones , Pruebas de Sensibilidad Parasitaria , Perú , Hojas de la Planta/química , Raíces de Plantas/química , Tallos de la Planta/química , Timol/química , Timol/farmacología , Árboles , Trypanosoma cruzi/efectos de los fármacosRESUMEN
A pharmacological screening of the ethanol extract and fractions of two Peruvian medicinal plants, Plagiochila disticha and Ambrosia peruviana, led to the isolation and characterization of three ENT-2,3-secoaromadendrane-type sesquiterpenoids, named plagiochiline A ( 1), I ( 2), and R ( 3), as well as of two pseudoguaianolids, damsin ( 4) and confertin ( 5), which exhibited significant cytotoxic activity against a panel of human tumor cell lines. Compounds 1, 4, and 5 were also investigated for their in vitro antileishmanial, trypanocidal, and antituberculosis activity against Leishmania amazonensis axenic amastigotes and Trypanosoma cruzi trypomastigotes, as well as against MDR and sensitive strains of Mycobacterium tuberculosis, respectively.
Asunto(s)
Antiinfecciosos/aislamiento & purificación , Antineoplásicos Fitogénicos/aislamiento & purificación , Asteraceae/química , Azulenos/aislamiento & purificación , Compuestos Epoxi/aislamiento & purificación , Piranos/aislamiento & purificación , Sesquiterpenos/aislamiento & purificación , Línea Celular Tumoral , Evaluación Preclínica de Medicamentos , Humanos , Perú , Plantas Medicinales/químicaRESUMEN
A multidisciplinary and international team of scientists was assembled in the early 1990s to conduct an ethnobotanical study of plants used by the Aguaruna people of the Peruvian Amazon forest. The initial ethnobotanical project, carried out under the auspices of an International Cooperative Biodiversity Grant (ICBG), led to the collection of approximately 4000 plant species. Some members of the original team of scientists have continued this collaboration by focusing on potential sources of new anticancer, anti-infective, and wound-healing agents. This effort has uncovered several secondary metabolites representing a wide variety of chemical diversity. In this short review we describe some bioactive compounds of interest as part of our continuing collaboration.
Asunto(s)
Plantas Medicinales/química , Etnobotánica , Humanos , Medicina Tradicional , Estructura Molecular , PerúRESUMEN
The antiproliferative bioassay-guided fractionation of five Peruvian plants, Doliocarpus dentatus, Picramnia sellowii, Strychnos mitscherlichii, Iryanthera juruensis, and Croton alnifolius, led to the isolation and identification of their different major cytotoxic constituents, betulinic acid (1), nataloe-emodin (2), bisnordihydrotoxyferine (4), 2',4'-dihydroxy-6'-methoxy-3,4-methylenedioxydihydrochalcone (5), and 2',4'-dihydroxy-4,6'-dimethoxydihydrochalcone (6) and 12-O-tetradecanoylphorbol-13-acetate (7), respectively. Eight human tumor cell lines and two nontumorigenic cell lines were used in this investigation. Their in vitro activity against Mycobacterium tuberculosis is also reported.