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Planta Med 1993; 59(2): 144-147
DOI: 10.1055/s-2006-959630
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© Georg Thieme Verlag Stuttgart · New York

Biochemical Evaluation of Colchicine and Related Analogs1,*

Jitka Ulrichová2 , Daniela Walterová2 , Veronika Lukič3 , Drahomíra Černochová4 , Ivana Chromcová2 , Vilím Šimánek2
  • 2Institute of Medical Chemistry, Medical Faculty, Palacký University, Hněvotínskáa 3, 77515 Olomouc, Czechoslovakia
  • 3Institute of Chemistry, Faculty of Sciences, University of Novi Sad, Novi Sad, Yugoslavia
  • 4Institute of Histology and Embryology, Medical Faculty, Palacký University, Olomouc, Czechoslovakia
1 Substances from the Plants of the Subfamily Wurmbaeoideae and their Derivatives; Part 109. For Part 108 see Ref. (13)* Dedicated to Professor Arnold Brossi on the Occasion of his 70th birthday.
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Publication History

1992

1992

Publication Date:
04 January 2007 (online)

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Abstract

Transformation of ten colchicinoids by isolated rat liver microsomes resulted in the mixture of C-2, C-3, and C-10 O-demethylated metabolites. Colchicinoids administered i.p. to rats (2.5 µmol/kg) increased serum and liver activities of alkaline phosphatase and decreased liver microsomal demethylase activity as well as cytochrome P-450 content. The changes of acid phosphatase level were less pronounced. The aspartate and alanine aminotransferase activities were significantly increased only in colchicine treated rats. No relations between enzyme activity changes and colchicinoid hydrophobicities quantified by partition coefficients (log P) were found. However, the enzyme activity changes were related to the type of substitution at C-3, C-7, and C-10 of colchicinoids. Particularly, O-demethylation at C-3 resulted into the fall of alkaline phosphatase response. On the other hand, the microsomal demethylation and cytochrome P-450 content were related to the modification of the nitrogen substituent at C-7.

Key words

Colchicinoids - rat liver microsomal transformation - aminotransferases - phosphatases - demethylase activity - cytochrome P-450 - hydrophobicity

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