RESUMO
Eight drimane sesquiterpenes (1-8), six isochromane derivatives (9-14), and three known compounds, daldinin B (15), 9alpha-hydroxy-6beta-[(2E,4E,6E)-octa-2,4,6-trienoyloxy]-5alpha-drim-7-en-11,12-olide (16), and pergillin (17), were isolated from the EtOAc extract of the marine-derived fungus Aspergillus ustus 094102. The structures of the new compounds were elucidated on the basis of spectroscopic analysis. The cytotoxic effects on A549 and HL-60 cell lines were evaluated by SRB and MTT methods. Ustusorane E (13) showed significant cytotoxicity against HL-60 cells with an IC50 value of 0.13 microM. Ustusolates C (6) and E (8) exhibited moderate cytotoxicity against A549 and HL-60 cells with IC50 values of 10.5 and 9.0 microM, respectively, and ustusolate A (4) showed weak cytotoxicity against HL-60 and A549 cells with IC50 values of 20.6 and 30.0 microM, respectively.
Assuntos
Antineoplásicos Fitogênicos/isolamento & purificação , Aspergillus/química , Benzofuranos/isolamento & purificação , Cromanos/isolamento & purificação , Sesquiterpenos/isolamento & purificação , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Benzofuranos/química , Benzofuranos/farmacologia , Cromanos/química , Cromanos/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Células HL-60 , Humanos , Concentração Inibidora 50 , Biologia Marinha , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Sesquiterpenos Policíclicos , Sesquiterpenos/química , Sesquiterpenos/farmacologia , EstereoisomerismoRESUMO
A new aflatoxin, aflatoxin B(2b) (1), together with six known compounds, were isolated from the marine-derived fungus Aspergillus flavus 092008 endogenous with the mangrove plant Hibiscus tiliaceus (Malvaceae). The structure of 1 was determined by the spectroscopic and chemical methods. Compound 1 exhibited a moderate antimicrobial activity against Escherichia coli, Bacillus subtilis and Enterobacter aerogenes, with MIC values of 22.5, 1.7 and 1.1 M, respectively. Compound 1 also showed a weak cytotoxicity against A549, K562 and L-02 cell lines, with IC(50) values of 8.1, 2.0 and 4.2 M, respectively. The results showed that hydration and hydrogenation of (8)-double bond significantly reduces the cytotoxicity of aflatoxins, while the esterification at C-8 increases the cytotoxicity.
Assuntos
Aflatoxinas/farmacologia , Antineoplásicos/farmacologia , Aspergillus flavus/química , Hibiscus/microbiologia , Aflatoxinas/administração & dosagem , Aflatoxinas/isolamento & purificação , Anti-Infecciosos/administração & dosagem , Anti-Infecciosos/isolamento & purificação , Anti-Infecciosos/farmacologia , Antineoplásicos/administração & dosagem , Antineoplásicos/isolamento & purificação , Aspergillus flavus/isolamento & purificação , Bacillus subtilis/efeitos dos fármacos , Linhagem Celular Tumoral , Enterobacter aerogenes/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Humanos , Concentração Inibidora 50 , Células K562 , Testes de Sensibilidade MicrobianaRESUMO
Six hundred and eight fungi strains were isolated from seventy-eight samples of mangrove plants and soil that collected from Qinglan harbor. Cyctotoxic activity was detected by observing the growth inhibition or killing of the tumor cells under microscope. The result showed that 81 strains (about 13.32% of the total strains isolated) displayed cytotoxic activity against B16 tumor cell. The most fungi strains were isolated from mangrove plant Sonneratia alba, and most of cytotoxic active fungi strains were isolated from mangrove plant Heritiera littoralis.