Untersuchungen zum Einfluß von Baldrinalen auf hämatopoetische Zellen in vitro, auf die metabolische Aktivität der Leber in vivo sowie zum Gehalt in Fertigarzneimitteln

Abstract

Baldrinal and homobaldrinal were described as degradation products of the cytotoxic and indirectly mutagenic valepotriates, valtrate and isovaltrate, respectively. The directly mutagenic baldrinals inhibit the in vitro colony growth of mouse bone marrow cells and human lymphocytes substantially less than the valepotriates. The in vivo metabolic degradation of ¹⁴ C-methacetin, however, is clearly inhibited after enteral (p.o.) administration of the baldrinals, which is not observed after p.o. administration of valepotriates. Thus, it can be concluded that the baldrinals are absorbed in the intestine. In pharmaceutical preparations standardized for valepotriate, contents of up to 0.988 mg/ dosage form of baldrinals were found. This concentration cannot be considered cytotoxically unobjectionable. However, further studies should be conducted in order to estimate the in vivo genotoxicity.