Studies on the Chemical Constitutents and Their Biological Activities of Fromosan Soft Corals - Sarcophyton trocheliophorum and Sinularia sp.

• Main Author: 謝珮文
• Other Authors: 吳永昌
• Format: Others
• Language: zh-TW
• Published: 1993
• Online Access: http://ndltd.ncl.edu.tw/handle/88498895758968977001

碩士 === 高雄醫學大學 === 藥學研究所 === 81 === 　　As a result of our search for biologically active substances from marine organisms, the methanolic extract of the marine Formosan soft corals, Sarcophyton trocheliophorum and Sinularia sp., were found to show significant cytotoxicity against in. vitro tissue culture cells in human KB, A-549 lung carcinoma, HT-29 colon tumor and HL-60 human promyelocytic leukemia, as well as in murine P-388 lymphocytic leukemia and antiplatelet aggregation activity against in vitro collegen factor. Bioactivity- guided chromatographic fractionation led to the isolation and character ization of nine cembranoids, (+)-isosarcophytoxide (1), (+)- isosarcophine (2), norcembranolide (3), 11-epi-sinulariolide acetate (4), 11- dehydrosinulariolide (5), sinulariolide (6), sarcophytoxide (7),norcembranolide (8) and dihydrosinularin (9); three nucleosides, 2'- de-oxyadenosine (10), thymidine (11) and thymine (12) as as well as a new cembranoid sinurolide A (13). The structure elucidations of the isolates were established by spectroscopic analysis and chemical methods. Compounds 10, 11 and 12 were isolated for the first time from marine soft corals, compound 2 was isolated for the first time from the genues Sarcophyton. 　　In addition to compounds 1, 2, 3, 4, 5, 6, 7, 9 and 13 showed significant cytotoxicity against KB, A-549, P- 388, HT-29 HL-60 cancer cells, compounds 3, 5, 6, and 7 exhibited antiplatelet aggregation effect against collegen and PAF factors. 　　Seven cembranoids derivatives were prepared by semisythesis for studies the Structure- Activity Relationships owing to the isolated cembranoids showed strong significant cytotoxicity. The structures and biological activities of these seven compounds will be also discussed.