Screening of some saponins and phenolic components of Tribulus terrestris and Smilax excelsa as MDR modulators

Antoaneta Ivanova, Julianna Serly, Dragomir Dinchev, Imre Ocsovszki, Ivanka Kostova, Joseph Molnar

Research output: Contribution to journalArticle

23 Citations (Scopus)

Abstract

Background: Cytotoxic activity of saponins and phenolic compounds have been described in the literature, but no reports were found on their multidrug resistance (MDR)-modulating effects on human mdr1 gene-transfected mouse lymphoma cell line. Materials and Methods: Methylprototribestin, structurally related compounds and a mixture of 3 acetylated isomers of methylprotodioscin were investigated for antiproliferative effect and modulation of drug accumulation. Results: The growth inhibitory dose (ID50) of the compounds ranged from 12.64 to 20.62 μg/ml. Methylprototribestin was the most effective resistance modifier. However, methylprotodioscin, pseudoprotodioscin, prosapogenin A of dioscin, tribestin and 5-O-caffeoylshikimic acid showed moderate MDR reversal activity. In a checkerboard method, methyloprototribestin and the mixture of the 3 acetylated isomers enhanced the antiproliferative effects on MDR cells in combination with doxorubicin. Conclusion: Based on these results, methylprototribestin and the mixture of the 3 acetylated isomers can be recommended for further in vivo experiments in combination with anthracyclines in human MDR-cancer xenograft transplanted mice.

Original languageEnglish
Pages (from-to)545-550
Number of pages6
JournalIn Vivo
Volume23
Issue number4
Publication statusPublished - Jul 1 2009

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Keywords

  • Efflux pump
  • MDR reversal
  • Multidrug resistance
  • P-glycoprotein
  • Smilax excelsa
  • Steroidal saponins
  • Tribulus terrestris

ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Pharmacology

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