Cytotoxic Compounds from a Two-Sponge Association - Journal of

2: Synthesis of the GH-Ring System and a Structurally Simplified Macrolactone ... Metabolite Psammaplin A Activates PPARγ and Induces Apoptosis i...
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Journal of Natural Products

1722

Val. 58, NO.11,pp. 1722-1726, No~ember1995

CYTOTOXIC COMPOUNDS FROM A TWO-SPONGE ASSOCIATION JEE

H. JUNG,*

Marine Natural Products Labwatwy, Kwu Ocean Research and Deve(opment Institute, Seoul 425-600, Kuru CHLJNGJ. SIM,

Dtpartmmr of Biology, Han Nam University, Tatjmn, Kwu and CHONGOCKLEE

Phatnueutical Screening Center, Kwu Ruurch Institute of Chemical Technology, Taejeon, Kuru hsmff.-Investigation of the cytotoxic constituents of a two-sponge association (Pwrillartra sp. andJaspis sp.) led to the isolation ofpectenotoxin I1 [I] and psammaplin A as the active compounds. In an in vitro cell culture assay, 1 displayed very potent cytotoxic activities against human lung (A-549), colon (HT-29), and breast (MCF-7) cancer cell lines. Pectenotoxin I1 also exhibited selective cytotoxicity against several cell lines representing ovarian, renal, lung, colon, CNS, melanoma, and breast cancer, with differences in LC,, values between sensitive and resistant cell lines of 100-fold or more.

In our search for natural cytotoxic compounds, twenty-one marine sponges collected off Cheju and Komun islands, Korea, were screened for brine shrimp lethality (l),and significant brine shrimp (Artemia salina) lethality was detected (BST LC,, 61 kg/ml) in the crude extract of a two-sponge association. A cross-section of this sample showed two layers of morphologically distinct sponges. The thin and dirty yellow outer layer was identified as Poecillastra sp. (Pachastrellidae), the surface ofwhich was very rough. The light-grey inner layer was identified asJaspis sp. (Jaspidae), the surface of which was smooth. This twosponge association appears to be consistent as these sponges were always found in associated form regardless of collection site or collection period.

Bioactivity-directed fractionation of the sponges (1iquidAiquid partition followed by reversed-phase cc) afforded pectenotoxin I1 111 (BST LC,,