Bioorganic & Medicinal Chemistry Letters 2001-08-06

Antimalarial halorosellinic acid from the marine fungus Halorosellinia oceanica.

M Chinworrungsee, P Kittakoop, M Isaka, A Rungrod, M Tanticharoen, Y Thebtaranonth

Index: Bioorg. Med. Chem. Lett. 11(15) , 1965-9, (2001)

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Abstract

Three known compounds, 2-hexylidene-3-methylsuccinic acid (1), cytochalasin Q (2), and 5-carboxymellein (3), together with two new derivatives, 2-hexylidene-3-methylsuccinic acid 4-methyl ester (4) and an ophiobolane sesterterpene named halorosellinic acid (5), were isolated from culture broth of the marine fungus Halorosellinia oceanica BCC 5149. Compounds 1-3 exhibited moderate cytotoxicity against KB and BC-1 cell lines with IC(50) values of 1-13 microg/mL, while compounds 2, 3, 5, and 6 showed antimalarial activity with respective IC(50) values of 17, 4, 13, and 19 microg/mL. Halorosellinic acid (5) possessed only weak antimycobacterial activity with the minimum inhibitory concentration of 200 microg/mL.