期刊
JOURNAL OF NATURAL PRODUCTS
卷 71, 期 1, 页码 22-27出版社
AMER CHEMICAL SOC
DOI: 10.1021/np070280x
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资金
- FOGARTY INTERNATIONAL CENTER [U01TW006634] Funding Source: NIH RePORTER
- NATIONAL CANCER INSTITUTE [R01CA100851] Funding Source: NIH RePORTER
- NATIONAL INSTITUTE OF ENVIRONMENTAL HEALTH SCIENCES [P30ES000210] Funding Source: NIH RePORTER
- NATIONAL INSTITUTE OF NEUROLOGICAL DISORDERS AND STROKE [R01NS053398] Funding Source: NIH RePORTER
- FIC NIH HHS [TW006634, U01 TW006634-05, U01 TW006634] Funding Source: Medline
- NCI NIH HHS [CA100851, R01 CA100851] Funding Source: Medline
- NIEHS NIH HHS [P30 ES00210, P30 ES000210] Funding Source: Medline
- NINDS NIH HHS [R01 NS053398-07, NS053398, R01 NS053398] Funding Source: Medline
Investigation of a Symploca sp. from Papua New Guinea has led to the isolation of symplocamide A (1), a potent cancer cell cytotoxin, which also inhibits serine proteases with a 200-fold greater inhibition of chymotrypsin over trypsin. The complete stereostructure of symplocamide A was determined by detailed NMR and MS analysis as well as chiral HPLC analysis of the component amino acid residues. The presence of several unusual structural features in symplocamide A provides new insights into the pharmacophore model for protease selectivity in this drug class and may underlie the potent cytotoxicity of this compound to H-460 lung cancer cells (IC50 = 40 nM) as well as neuro-2a neuroblastoma cells (IC50 = 29 nM).
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