Kazusamycin B is a minor component of the leptomycin complex produced from the fermentation of the broth of a Streptomyces sp.. The compound is a hydroxylated analogue of Leptomycin A (sc-203102), a nuclear export inhibitor, and highly lipophillic. In vitro antitumor activity of Kazusamycin B on tumors L1210, P388/S, B16, HeLa S3, L5178Y-ML or L929 was ascertained to have an IC50 of 1.8, 2.0, 0.7, 1.8, 10.0 and l.0 ng/ml when cultured in the presence of Kazusamycin B for 72 hours. The compound has also displayed broad antitumor activity in mice with effectiveness being more dependent on dosing regimen than dosing concentration both in vivo and in vitro. Kazusamycin B also possesses antibacterial and antifungal activity.
1. Yoshida, E., et al. 1987. J. Antibiot. 40: 1596-1604. PMID: 3693127 2. Funaishi, K., et al. 1987. J. Antibiot. 40: 778-785. PMID: 3610834 3. Takamiya, K., et al. 1988. J. Antibiot. 41: 1854-1861. PMID: 3209477
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YoshidaYoshida, E. et al. (PubMed 3693127) studied the antitumor effect of Kazusamycin B, that displays broad antitumor activity along with antibacterial and antifungal activity, on experimental tumors. IC50 against the growth of tumor cells was around 1 ng/ml at 72 hours exposure in vitro. -SCBT Publication Review
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