RESUMEN
A new indole alkaloid strychnosinol (1) and a new phenolic-glycoside (2) were isolated from the bark and leaves of Strychnos fendleri Sprague & Sandwith, together with six known compounds reported for the first time in this species. The structures of these compounds were determined on the basis of spectroscopic data; mainly those obtained by using (1)H and (13)C NMR (1D and 2D) and mass spectrometry. Strychnosinol (1) and the phenolic glycoside (2) together with compounds 3-8 were evaluated for cytotoxicity against a panel of five tumour cell lines; IC50 values between 0.090 and 0.227 µM for the human tumour cell lines were observed for compound 2.
Asunto(s)
Alcaloides/aislamiento & purificación , Alcaloides/farmacología , Antineoplásicos Fitogénicos/farmacología , Glicósidos/aislamiento & purificación , Glicósidos/farmacología , Indoles/aislamiento & purificación , Indoles/farmacología , Strychnos/química , Línea Celular Tumoral , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Espectroscopía de Resonancia Magnética , Fenoles/aislamiento & purificación , Fenoles/farmacología , Corteza de la Planta/química , Extractos Vegetales/química , Extractos Vegetales/farmacología , Hojas de la Planta/química , Sales de Tetrazolio , TiazolesRESUMEN
A series of caracasine acid (1) derivatives were synthesized and evaluated for their in vitro cytotoxicity on human cancer-derived cell lines MCF-7 and PC-3, as well as for other activities such as antibacterial, antileishmanial and antitrypanosomal activity. Compound 1 was more effective than any of its derivatives against tested human cancer cell lines. PC-3 cells were more sensitive than MCF-7 to all compounds, particularly the methyl ester (2), the amide (9) and the epoxide (10). The evaluation of antiparasitic activity revealed that ester derivatives (2-8) and the amide derivative (9) were the most effective antileishmanial and antitrypanosomal compounds, even though their effect on Trypanosoma cruzi was modest. Finally, compound 1 and the derivatives evidenced a broad spectrum of antibacterial activity, as assayed against Gram-positive and Gram-negative bacteria.
Asunto(s)
Antibacterianos/síntesis química , Antineoplásicos/síntesis química , Antiprotozoarios/síntesis química , Ácidos Carboxílicos/síntesis química , Fenantrenos/síntesis química , Amidas/química , Antibacterianos/farmacología , Antineoplásicos/farmacología , Antiprotozoarios/farmacología , Bacillus cereus/efectos de los fármacos , Bacillus cereus/crecimiento & desarrollo , Ácidos Carboxílicos/farmacología , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Compuestos Epoxi/química , Escherichia coli/efectos de los fármacos , Escherichia coli/crecimiento & desarrollo , Ésteres/química , Humanos , Concentración 50 Inhibidora , Leishmania mexicana/efectos de los fármacos , Leishmania mexicana/crecimiento & desarrollo , Células MCF-7 , Fenantrenos/farmacología , Pseudomonas aeruginosa/efectos de los fármacos , Pseudomonas aeruginosa/crecimiento & desarrollo , Staphylococcus aureus/efectos de los fármacos , Staphylococcus aureus/crecimiento & desarrollo , Relación Estructura-Actividad , Trypanosoma cruzi/efectos de los fármacos , Trypanosoma cruzi/crecimiento & desarrolloRESUMEN
The essential oil from leaves of Croton gossypiifolius Vahl. (Euphorbiaceae) was obtained by hydrodistillation, and analyzed by GC/FID and GC/MS. The constituents were identified by their mass spectra and Kovats' indices. Fifty-one compounds accounting for 92% of the oil were detected, and 47 of them were identified. The oil was dominated by oxygenated sesquiterpenes with the major presence of alpha-cedrene oxide (18.6%), spathulenol (16.3%), valencene (5.8%), geranyl-pentanoate (5.3%), alpha-cadinol (4.0%), germacrene D (3.5%) and longifolene (3.3%).
Asunto(s)
Croton/química , Aceites Volátiles/análisis , Hojas de la Planta/química , Sesquiterpenos/análisis , Sesquiterpenos de Germacrano/análisis , Terpenos/análisis , VenezuelaRESUMEN
El extracto acuoso de las hojas de Bauhinia megalandra ha sido muy empleado en Venezuela en el tratamiento empírico de la diabetes mellitus. En el presente trabajo se estudió el efecto del extracto acuoso de B. megalandra sobre la glucogenolísis hepática estimulada por adrenalina o dibutiril AMPc. La administración oral del extracto de la planta, a ratas alimentadas, disminuyó de una manera estadísticamente significativa el incremento de la glicemia promovido por la adrenalina. De igual manera, rebanadas de hígado de ratas alimentadas incubadas en presencia del extracto de B. megalandra produjeron menos glucosa en respuesta a la adrenalina o al dibutiril AMPc que los controles. Estos resultados indican una disminución de la glucogenolísis hepática por efecto del extracto acuoso de hojas de B. megalandra, probablemente por inhibición de la enzima glucosa-6-fosfatasa.
Asunto(s)
Animales , Ratas , Bucladesina/administración & dosificación , Bucladesina/uso terapéutico , Diabetes Mellitus , Epinefrina/efectos adversos , /efectos adversosRESUMEN
Croton malambo (K.) bark aqueous extract, popularly known in Venezuela as "palomatias" or "torco" was tested for acute toxicity and for its anti-inflammatory and antinociceptive effects using tail flick and writhing syndrome tests models, respectively. Croton malambo aqueous extract (6.15 mg/kg i.p.) administered intraperitoneally had a significant antinociceptive and anti-inflammatory effects compared to acetylsalicylic acid (200mg/kg p.o.) and sodium diclofenac (5.64 mg/kg p.o.). Studies to determine correlation between chemical composition and pharmacological activity are underway.