Screening of Some Saponins and Phenolic Components of Tribulus terrestris and Smilax excelsa as MDR Modulators

• Published in: In vivo (Athens) Vol. 23; no. 4; pp. 545 - 550
• Main Authors: Ivanova, Antoaneta, Serly, Julianna, Dinchev, Dragomir, Ocsovszki, Imre, Kostova, Ivanka, Molnar, Joseph
• Format: Journal Article
• Language: English
• Published: Greece International Institute of Anticancer Research 01.07.2009
• Subjects: Animals; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; ATP Binding Cassette Transporter, Sub-Family B; ATP-Binding Cassette, Sub-Family B, Member 1 - genetics; ATP-Binding Cassette, Sub-Family B, Member 1 - metabolism; Cell Line, Tumor; Drug Design; Humans; Lymphoma, T-Cell; Mice; Phenols - chemistry; Phenols - pharmacology; Plant Extracts - chemistry; Plant Extracts - pharmacology; Saponins - chemistry; Saponins - pharmacology; Smilax - chemistry; Transfection; Tribulus - chemistry; Xenograft Model Antitumor Assays
• ISSN: 0258-851X; 1791-7549

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.