CALPHOSTINS (UCN-1028), NOVEL AND SPECIFIC INHIBITORS OF PROTEIN KINASE C I. FERMENTATION, ISOLATION, PHYSICO-CHEMICAL PROPERTIES AND BIOLOGICAL ACTIVITIES

EIJI KOBAYASHI; KATSUHIKO ANDO; HIROFUMI NAKANO; TAKAO IIDA; HIROE OHNO; MAKOTO MORIMOTO; TATSUYA TAMAOKI

doi:10.7164/antibiotics.42.1470

CALPHOSTINS (UCN-1028), NOVEL AND SPECIFIC INHIBITORS OF PROTEIN KINASE C

I. FERMENTATION, ISOLATION, PHYSICO-CHEMICAL PROPERTIES AND BIOLOGICAL ACTIVITIES

EIJI KOBAYASHI, KATSUHIKO ANDO, HIROFUMI NAKANO, TAKAO IIDA, HIROE OHNO, MAKOTO MORIMOTO, TATSUYA TAMAOKI

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JOURNAL FREE ACCESS

1989 Volume 42 Issue 10 Pages 1470-1474

DOI https://doi.org/10.7164/antibiotics.42.1470

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Abstract

A novel complex of calphostin (UCN-1028), which specifically inhibits protein kinase C (PKC) has been isolated from the culture broth of a fungi Cladosporium cladosporioides. Purification of individual components was carried out by silica gel, non-porus resin Diaion HP-20SS and Sephadex LH-20 chromatography, leading to isolation of five closely related components, A, B, C, D and I. Calphostins showed cytotoxic activities against various tumor cells, and these cytotoxicities were proportional to their inhibitory activities against PKC.

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