Proksa B, Uhrin D, Adamcová J, Fuska J
Institute of Chemistry, Slovak Academy of Sciences, Bratislava.
Pharmazie. 1992 Aug;47(8):582-4.
Oxidation of the macrolide antibiotic brefeldin A with pyridinium chlorochromate adsorbed on alumina afforded [6S, 10E, 11aS, 14E]-6-methyl-2,3,6,7,8,9,11a,12-octahydro-4 H-cyclopent[f]oxacyclotridecin-1,4,13-trione together with 13-oxobrefeldin. These compounds showed higher cytotoxic activity on P388 leukemia cells than brefeldin A, brefeldin A-1,13-diacetate, brefeldin A-13-acetate, tetrahydrobrefeldin or tetrahydrobrefeldin-1,13-dione. 13-Oxobrefeldin exceeded brefeldin A in antifungal activity on Candida albicans.
用吸附在氧化铝上的氯铬酸吡啶鎓氧化大环内酯类抗生素布雷菲德菌素A，得到[6S, 10E, 11aS, 14E]-6-甲基-2,3,6,7,8,9,11a,12-八氢-4H-环戊[f]氧杂环十三烷-1,4,13-三酮以及13-氧代布雷菲德菌素。这些化合物对P388白血病细胞的细胞毒性活性高于布雷菲德菌素A、布雷菲德菌素A-1,13-二乙酸酯、布雷菲德菌素A-13-乙酸酯、四氢布雷菲德菌素或四氢布雷菲德菌素-1,13-二酮。13-氧代布雷菲德菌素对白色念珠菌的抗真菌活性超过了布雷菲德菌素A。
