RESUMO
Four new norterpene cyclic peroxides (1-4), together with three known norterpene cyclic peroxides were isolated from the Xisha Islands Sponge Diacarnus megaspinorhabdosa. Their structures were elucidated on the basis of spectroscopic analyses and comparison with the related model compounds. The compounds (1-7) were evaluated for the inhibitory activity against the malaria parasite Plasmodium falciparum, all of them showed significant antimalarial activity with IC50 values in the range of 1.6-8.6 µM.
Assuntos
Antimaláricos/farmacologia , Peróxidos/farmacologia , Plasmodium falciparum/efeitos dos fármacos , Poríferos/química , Animais , Antimaláricos/síntese química , Antimaláricos/química , Antimaláricos/isolamento & purificação , Relação Dose-Resposta a Droga , Estrutura Molecular , Testes de Sensibilidade Parasitária , Peróxidos/síntese química , Peróxidos/química , Peróxidos/isolamento & purificação , Relação Estrutura-AtividadeRESUMO
Five new norditerpene endoperoxides, named diacarperoxides H-L (1-5), and a new norditerpene diol, called diacardiol B (6), were isolated from the South China Sea sponge, Diacarnus megaspinorhabdosa. Their structures, including conformations and absolute configurations, were determined by using spectroscopic analyses, computational approaches and chemical degradation. Diacarperoxides H-J (1-3) showed some interesting stereochemical issues, as well as antimalarial activity.
Assuntos
Antimaláricos/química , Diterpenos/química , Peróxidos/química , Poríferos/química , Animais , Antimaláricos/farmacologia , Linhagem Celular Tumoral , China , Diterpenos/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais/métodos , Humanos , Estrutura Molecular , Oceanos e Mares , Peróxidos/farmacologia , Plasmodium falciparum/efeitos dos fármacos , EstereoisomerismoRESUMO
Four novel phenolic compounds (1-4) were isolated from the leaves of Crataegus pinnatifida, along with three known ones (5-7). Their structures were elucidated as: methyl 4-O-ß-D-glucopyranosyl-3-[(2E,6E)-8-O-ß-D-glucopyranosyl-3,7-dimethyl-2,6-octadienyl] benzoate (1), biphenyl-5-ol-3-O-ß-D-glucoside (2), 3,4'-dimethoxy-biphenyl-5-ol-4-O-ß-D-glucoside (3), (E)-6-(benzoyloxy)-1-hydroxyhex-3-en-2-O-ß-D-glucoside (4), shanyenoside A (5), eriodectyol (6), and 2â³-O-rhamnosyl vitexin (7), using a combination of mass spectroscopy, 1D and 2D NMR spectroscopy, and chemical analysis. The antithrombotic activity of the isolated compounds was investigated on the transgenic zebra fish system. Among them, eriodectyol (6) potently inhibited the production of thrombus.
Assuntos
Crataegus/química , Fibrinolíticos/isolamento & purificação , Fibrinolíticos/farmacologia , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Folhas de Planta/química , Trombose/prevenção & controle , Animais , Animais Geneticamente Modificados , Fibrinolíticos/química , Estrutura Molecular , Fenóis/isolamento & purificação , Fenóis/farmacologia , Extratos Vegetais/química , Peixe-ZebraRESUMO
Seven new formamido-diterpenes, cavernenes A-D (1-4), kalihinenes E and F (5-6), and kalihipyran C (7), together with five known compounds (8-12), were isolated from the South China Sea sponge Acanthella cavernosa. Structures were established using IR, HRESIMS, 1D and 2D NMR, and single X-ray diffraction techniques. The isolated compounds were assessed for their cytotoxicity against a small panel of human cancer cell lines (HCT-116, A549, HeLa, QGY-7701, and MDA-MB-231) with IC(50) values in the range of 6-18 µM. In addition, compound 9 showed weak antifungal activity against Trichophyton rubrum and Microsporum gypseum with MIC values of 8 and 32 µg/mL, respectively, compound 10 displayed weak antifungal activity against fungi Candida albicans, Cryptococcus neoformans, T. rubrum, and M. gypseum with MIC values of 8, 8, 4, and 8 µg/mL, respectively.
