Guggulsterone regulates the function and expression of P-glycoprotein in rat brain microvessel endothelial cells

• Published in: European journal of pharmacology 2013-10, Vol.718 (1-3), p.24-29
• Main Authors: Chen, Xian-Zhen, Xu, Hong-Bin, Xu, Lu-Zhong, Mao, Xia-Ping, Li, Ling
• Format: Article
• Language: English
• Subjects: Adenosine Triphosphatases - metabolism; adenosinetriphosphatase; Animals; ATP-Binding Cassette, Sub-Family B, Member 1 - metabolism; brain; breast neoplasms; endothelial cells; Endothelial Cells - drug effects; Endothelial Cells - metabolism; Gene Expression Regulation - drug effects; Guggulsterone; Humans; Microvessels - cytology; multiple drug resistance; P-glycoprotein; pharmacology; Pregnenediones - pharmacology; Rat brain microvessel endothelial cell; Rats
• ISSN: 0014-2999; 1879-0712
• DOI: 10.1016/j.ejphar.2013.09.010

Our previous studies found that guggulsterone could inhibit P-glycoprotein-mediated multidrug resistance in P-glycoprotein over-expressed human cancer cell lines. However, the effects of guggulsterone on the ;P-glycoprotein function and expression in rat brain microvessel endothelial cells (rBMECs) are poorly understood. In the present study, we investigated whether guggulsterone has a modulative effect on the function and expression of P-glycoprotein in rBMECs. rhodamine 123 acts as a good substrate for P-glycoprotein, and agents that block P-glycoprotein have been found to increase the retention of rhodamine in cells. The results showed that the accumulation of rhodamine 123 in rBMECs was potentiated in a time-dependent manner after incubation with 30, 100μM guggulsterone (P