ABSTRACT
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.
Subject(s)
Aflatoxins/pharmacology , Antineoplastic Agents/pharmacology , Aspergillus flavus/chemistry , Hibiscus/microbiology , Aflatoxins/administration & dosage , Aflatoxins/isolation & purification , Anti-Infective Agents/administration & dosage , Anti-Infective Agents/isolation & purification , Anti-Infective Agents/pharmacology , Antineoplastic Agents/administration & dosage , Antineoplastic Agents/isolation & purification , Aspergillus flavus/isolation & purification , Bacillus subtilis/drug effects , Cell Line, Tumor , Enterobacter aerogenes/drug effects , Escherichia coli/drug effects , Humans , Inhibitory Concentration 50 , K562 Cells , Microbial Sensitivity TestsABSTRACT
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.
Subject(s)
Antineoplastic Agents, Phytogenic/isolation & purification , Aspergillus/chemistry , Benzofurans/isolation & purification , Chromans/isolation & purification , Sesquiterpenes/isolation & purification , Antineoplastic Agents, Phytogenic/chemistry , Antineoplastic Agents, Phytogenic/pharmacology , Benzofurans/chemistry , Benzofurans/pharmacology , Chromans/chemistry , Chromans/pharmacology , Drug Screening Assays, Antitumor , HL-60 Cells , Humans , Inhibitory Concentration 50 , Marine Biology , Molecular Structure , Nuclear Magnetic Resonance, Biomolecular , Polycyclic Sesquiterpenes , Sesquiterpenes/chemistry , Sesquiterpenes/pharmacology , StereoisomerismABSTRACT
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.