• Bulletin of the Korean Chemical Society
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• 제23권7호
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• pp.1003-1010
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• 2002

Caspase 3, a member of cysteine protease family, is well known as a major apoptosis effector and is involved in cell death as a result of ischemic diseases such as stroke and myocardial infarction, therefore the inhibition of caspase 3 may protect those apoptotic cell damages. During the high-throughput screening of the compounds from the Korea Chemical Bank, berberine derivatives (A and B), an isoquinoline alkaloid, have been identified as potential inhibitors for caspase 3. Based on this finding we carried out molecular modeling study to identify the pharmacophoric elements of berberine structure which interact with a substrate-recognition binding site of caspase 3 and came up with several novel scaffolds. In this report, we will discuss the molecular modeling, syntheses and the enzyme inhibitory activities of these novel compounds.

• Journal of Microbiology and Biotechnology
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• 제9권1호
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• pp.119-121
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• 1999

Tumor cell interaction with the extracellular matrix is defined as the critical event of tumor invasion that signals the initiation of a metastatic cascade. Sesquicillin has been identified as an inhibitor of melanoma cell adhesion to the components of the extracellular matrix (ECM) in cultured broth of fungal strain F60063. Sesquicillin strongly inhibited the adhesion of B16 melanoma cells to laminin, fibronectin, and typeIV collagen. It also inhibited B16 melanoma cell invasion of reconstituted basement membrane Matrigel in vitro in a dose-dependent manner. These results suggest that sesquicillin is a new class of nonpeptidic ECM adhesion inhibitor having anti-invasive activity.