RESUMO
Three new cytochalasins Z(21) -Z(23) (1-3, resp.), together with five analogs, 4-8, were isolated from Spicaria elegans KLA03 by the OSMAC (one strain-many compounds) approach with adding L- and D-tryptophan during its cultivation. The structures of new cytochalasins were elucidated on the basis of comprehensive 1D- and 2D-NMR and HR-ESI-MS analyses. Cytochalasins Z(21) and Z(22) (1 and 2, resp.), and compound 5 showed cytotoxic activities against A-549 cell lines with IC(50) values of 8.2, 20.0, and 3.1â µM, respectively.
Assuntos
Antineoplásicos/química , Antineoplásicos/farmacologia , Citocalasinas/química , Citocalasinas/farmacologia , Fungos/química , Antineoplásicos/isolamento & purificação , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Citocalasinas/isolamento & purificação , Fungos/metabolismo , Humanos , Neoplasias/tratamento farmacológico , Triptofano/metabolismoRESUMO
An endophytic Streptomyces sp. (AC-2) was isolated from the root of Cistanches deserticola Y.C.Ma.. Chemical investigations of the culture broth of AC-2 afforded fifteen compounds including K1115 A (1), tyrosol (2), phenylethylamine derivatives (3, 4), cyclic dipeptides (5-8), nucleosides and their aglycones (9-13), N-acetyltryptamine (14), and pyrrole-2-carboxylic acid (15). Only tyrosol can promote an increase of intracellular cAMP special on GPR12 transfected cells, such as CHO and HEK293, which means it may be a possible ligand for GPR12.
Assuntos
Plantas Medicinais/química , Receptores Acoplados a Proteínas G/efeitos dos fármacos , Streptomyces/química , Animais , Células CHO , Cricetinae , Cricetulus , AMP Cíclico/metabolismo , DNA/biossíntese , DNA/genética , Dimetil Sulfóxido , Fermentação , Humanos , Espectroscopia de Ressonância Magnética , Álcool Feniletílico/análogos & derivados , Álcool Feniletílico/química , Álcool Feniletílico/isolamento & purificação , Extratos Vegetais/química , Plasmídeos/genética , RNA Ribossômico 16S/metabolismo , Espectrometria de Massas por Ionização por Electrospray , TransfecçãoRESUMO
Six new tetramic acids derivatives, penicillenols A(1), A(2), B(1), B(2), C(1), and C(2) (1-6), together with citrinin, phenol A acid, phenol A, and dihydrocitrinin, were identified from Penicillium sp. GQ-7, an endophytic fungus associated with Aegiceras corniculatum. Their structures were elucidated on the basis of comprehensive spectral analysis. All the new compounds were evaluated for their cytotoxic effects on four cell lines by the MTT method. Penicillenols A(1) and B(1) showed cytotoxicities against HL-60 cell line with IC(50) values of 0.76 microM and 3.20 microM, respectively.
Assuntos
Antifúngicos/isolamento & purificação , Antifúngicos/farmacologia , Penicillium/química , Primulaceae/microbiologia , Pirrolidinonas/isolamento & purificação , Pirrolidinonas/farmacologia , Cromatografia Líquida de Alta Pressão , Ensaios de Seleção de Medicamentos Antitumorais , Fermentação , Humanos , Espectroscopia de Ressonância Magnética , Espectrometria de Massas por Ionização por Electrospray , Espectrofotometria Ultravioleta , Sais de Tetrazólio , TiazóisRESUMO
In order to search for structurally novel and bioactive natural compounds from microorganisms, a halotolerant fungal strain, Penicillium citrinum B-57, which mainly produces citrinin derivatives, was isolated from sediments collected from the Jilantai salt field. From the ethyl acetate extract of P. citrinum B-57, two new citrinin dimers, pennicitrinone C ( 1) and penicitrinol B ( 2), and 11 known related compounds were isolated and identified by spectroscopic and chemical methods. These compounds showed antioxidative activity against DPPH radicals with IC 50 values ranging from 0.8 to 59 microM.
Assuntos
Antioxidantes/isolamento & purificação , Citrinina/isolamento & purificação , Penicillium/química , Antioxidantes/química , Antioxidantes/farmacologia , Compostos de Bifenilo , China , Citrinina/análogos & derivados , Citrinina/química , Citrinina/farmacologia , Estrutura Molecular , Picratos/farmacologiaRESUMO
Two new compounds, 2, 3, 5-trimethyl-6-(3-oxobutan-2-yl)-4H-pyran-4-one (1) and (2R)-2, 3- dihydro-7-hydroxy-6, 8-dimethyl-2-[(E)-prop-1-enyl] chromen-4-one (2), together with six known compounds (3-8), were isolated from a deep-sea fungus, identified as Aspergillus sydowi, by a bioassay-guided method. Their structures were elucidated by spectroscopic methods and the cytotoxicities were evaluated by SRB method.
