[CNS, cytotoxicity and antimicrobial activities of [+]-dihydroperfamine and its derivatives]

ABSTRACT

In this work [+]-dihydroperfamine was isolated from Haplophyllum tuberculatum and several derivatives, namely, anhydroperforine, dihydroperfaminole, haplophyllidine, [-]-perforine and [+]-perforine were prepared. Dihydroperfamine and its derivatives were investigated for prolongation of sleeping time of pentobarbitone. Their cytotoxic activity was performed using a mechanism-based bioassay utilizing genetically engineered mutants of the yeast Saccharomyces cerevisiae. In addition, their antimicrobial activity was also tested using agar dilution method. The results showed that dihydroperfamine and its derivatives except haplophyllidine prolonged the hypnotic duration of pentobarbital. Dihydroperfamine was the only compound that possessed cytotoxic activity against strain I. On the other hand, all compounds were antimicrobially inactive