RESUMO
A new indolinepeptide (3) was isolated, together with two known compounds, a cerebroside (1) and an alloxazine (2), from silkworm larvae infected with Paecilomyces sp. J300. On the basis of spectroscopic data, their structures were elucidated as (4E, 8E, 2S, 2'R, 3R)-N-2'-hydroxyhexadecanoyl-1-O-beta-D-glucopyranosyl-9-methyl-4, 8-sphingadienine (1), 7,8-dimethylalloxazine (2) and 3beta,5-dihydroxy-1-N-methyl-indoline-2beta-carbonyl amino-D-alanyl-erythro-beta-hydoxyisoleucinyl-glycine (3).
Assuntos
Indóis/química , Oligopeptídeos/química , Oligopeptídeos/isolamento & purificação , Paecilomyces/química , Peptídeos/química , Animais , Bombyx/microbiologia , Indóis/isolamento & purificação , Peptídeos/isolamento & purificaçãoRESUMO
The anti-tumor and immuno-stimulating activities of the fruiting bodies of Paecilomyces japonica (PJ), grown on silk-worm larvae and of Cordyceps sinensis (CS), a wild form of Cordyceps Fungi, were investigated. Ethanol extracts of both fungi, when administered for 9 consecutive days, at 50 and 100 mg/kg i.p., caused a significant increase in life span and a significant decrease in tumor weights and volumes, in mice inoculated with Sarcoma-180 tumor cells. Both fungal extracts were demonstrated to exhibit phagocytosis enhancing activity as measured by carbon clearance in mice. PJ extracts, when administered i.p. at 50 mg/kg/day for 3 consecutive days, exhibited a significant enhancement of phagocytosis, its potency as expressed by the regression coefficient ratio, RCtr/RCc, being 1.64 (the phagocytosis index = 2). This was approximately the same for that of zymosan (RCtr/RCc = 1.55, PI = 2), a typical phagocytosis enhancer, whereas CS extracts exhibited a moderate phagocytosis enhancing activity at the same dose level (RCtr/RCc = 1.30, PI = 1). Both fungal extracts caused a significant increase in an acid phosphatase activity, representing lysosomal enzymes, in macrophages at 20 and 100 micro g/ml in vitro, in compliance with in vivo results. These results suggest that the anti-tumor activity of both fungi might be related to an immuno-stimulating function.
Assuntos
Adjuvantes Imunológicos/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Paecilomyces , Fitoterapia , Extratos Vegetais/farmacologia , Adjuvantes Imunológicos/administração & dosagem , Adjuvantes Imunológicos/uso terapêutico , Animais , Antineoplásicos Fitogênicos/administração & dosagem , Antineoplásicos Fitogênicos/uso terapêutico , Carbono/metabolismo , Relação Dose-Resposta a Droga , Frutas , Macrófagos/efeitos dos fármacos , Macrófagos/enzimologia , Masculino , Camundongos , Camundongos Endogâmicos ICR , Fagocitose/efeitos dos fármacos , Extratos Vegetais/administração & dosagem , Extratos Vegetais/uso terapêutico , Sarcoma 180/prevenção & controle , Organismos Livres de Patógenos EspecíficosRESUMO
Three new (2-4) and one known (1) sphingolipid were identified in the MeOH extract of Bombycis Corpus 101A. Their structures were elucidated as (4E,2S,3R)-2-N-octadecanoyl-4-tetradecasphingenine (1), (4E,6E,2S,3R)-2-N-eicosanoyl-4,6-tetradecasphingadienine (2), (4E,2S,3R)-2-N-eicosanoyl-4-tetradecasphingenine (3), and (4E,6E,2S,3R)-2-N-docosanoyl-4,6-tetradecasphingadienine (4) on the basis of spectroscopic data. Their neurotrophic effects were evaluated by examining PC12 cell neurite outgrowth.
Assuntos
Bombyx/química , Fatores de Crescimento Neural/isolamento & purificação , Esfingolipídeos/isolamento & purificação , Animais , Coreia (Geográfico) , Larva/química , Estrutura Molecular , Fatores de Crescimento Neural/química , Fatores de Crescimento Neural/farmacologia , Ressonância Magnética Nuclear Biomolecular , Células PC12/efeitos dos fármacos , Ratos , Esfingolipídeos/química , Esfingolipídeos/farmacologia , EstereoisomerismoRESUMO
Seven ergosterol derivatives (1-7) were isolated from silkworm larvae infected with Paecilomyces sp. J300. On the basis of spectroscopic means, their structures have been elucidated as 3beta,5alpha-dihydroxy-ergosta-7,22-diene (1), 5alpha,6alpha-epoxy-(22E,24R)-ergosta-8(14), 22-diene-3beta, 7alpha-diol (2), 5alpha,6alpha-epoxy-(22E,24R)-ergosta-8,22-diene-3beta,7alpha-diol (3), ergosta-4,6,8(14),22-tetraene-3-one (4), ergosterol (5), ergosterol endoperoxide (6), 3beta,5alpha-dihydroxy-6beta-methoxyergosta-7,22-diene (7). Compounds 3-7 showed moderate cytotoxicity against five tumor cells.
