A new hTopo I isomerase inhibitor produced by a mangrove endophytic fungus no. 2240

• Published in: Journal of asian natural products research Vol. 10; no. 7; pp. 607 - 610
• Main Authors: Tan, Ni, Cai, Xiao-Ling, Wang, San-Yong, Pan, Jia-Hui, Tao, Yi-Wen, She, Zhi-Gang, Zhou, Shi-Ning, Lin, Yong-Cheng, Vrijmoed, Lilian L.P.
• Format: Journal Article
• Language: English
• Published: ABINGDON Taylor & Francis Group 01.07.2008; Taylor & Francis
• Subjects: (+)-3,3′,7,7′,8,8′-hexahydroxy-5,5′-dimethylbianthraquinone; 2240A; Anthraquinones - chemistry; Anthraquinones - pharmacology; Antibiotics, microbial producers, chemotherapic agents, antiseptics, disinfecting agents; Applied microbiology; Biological and medical sciences; Brackish; Chemistry; Chemistry, Applied; Chemistry, Medicinal; Chemotherapic agents; Fundamental and applied biological sciences. Psychology; Fungi - chemistry; hTopo I isomerase inhibitor; Humans; Life Sciences & Biomedicine; mangrove endophytic fungus; Microbiology; Molecular Structure; Pharmacology & Pharmacy; Physical Sciences; Plant Sciences; Science & Technology; Topoisomerase I Inhibitors; Asia; China; ISEW, South China Sea; SOUTH CHINA SEA; (+)-3,3 ',7 ',7 ',8 ',8 '-hexahydroxy-5,5 '-dimethylbianthraquinone; METABOLITES; COAST; hTopo I isomerase inhibitor; mangrove endophytic fungus; 2240A; XYLARIA SP; NUMBER-2508; Human; (+)-3,3',7,7',8,8'-hexahydroxy-5,5'-dimethylbian- thraquinone; Anthraquinone derivatives; Enzyme; Quinone; DNA topoisomerase; Enzyme inhibitor; Tricyclic compound; Condensed benzenic compound; Diphenols; In vitro; Biological activity; Fungi; Isomerases; Mangrove; Phenols; Endophyte; Isolation; Structural analysis
• ISSN: 1028-6020; 1477-2213
• DOI: 10.1080/10286020802133167

A new hTopo I isomerase inhibitor, (+)-3,3′,7,7′,8,8′-hexahydroxy-5,5′-dimethylbianthraquinone (2240A), was isolated from the mangrove endophytic fungus no. 2240 collected from an estuarine mangrove at the South China Sea coast. Its structure was elucidated by spectral analyses including two-dimensional NMR, HR-EI-MS, IR, and UV. The hTopo I isomerase inhibition experiment showed that 2240A (1) possessed strong inhibiting activity. When its inhibition concentration was 4.65 μmol/l, its percent inhibition rate was 59.1%, while the lowest inhibition concentration of the positive control camptothecin was 1.00 × 10 3  μmol/l.