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Journal of Asian Natural Products Research Volume 14, 2012 - Issue 6
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Original Articles

Partial synthesis and biological evaluation of bisbenzylisoquinoline alkaloids derivatives: potential modulators of multidrug resistance in cancer

Ping He Department of Chemistry of Medicinal Natural Products, West China College of Pharmacy, Sichuan University, Chengdu, 610041, China
,
Hua Sun Department of Pharmacology, Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing, 100050, China
,
Xi-Xian Jian Department of Chemistry of Medicinal Natural Products, West China College of Pharmacy, Sichuan University, Chengdu, 610041, China
,
Qiao-Hong Chen Department of Chemistry of Medicinal Natural Products, West China College of Pharmacy, Sichuan University, Chengdu, 610041, China
,
Dong-Lin Chen Department of Chemistry of Medicinal Natural Products, West China College of Pharmacy, Sichuan University, Chengdu, 610041, China
,
Geng-Tao Liu Department of Pharmacology, Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing, 100050, China
&
Feng-Peng Wang Department of Chemistry of Medicinal Natural Products, West China College of Pharmacy, Sichuan University, Chengdu, 610041, ChinaCorrespondence[email protected]
 show all
Pages 564-576 | Received 04 Jan 2012, Accepted 26 Mar 2012, Published online: 15 May 2012
 
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Abstract

A series of new bisbenzylisoquinoline alkaloids was partially synthesized from tetrandrine and fangchinoline and evaluated for their ability to reverse P-glycoprotein-mediated multidrug resistance (MDR) in cancer cells. All the test compounds increased the intracellular accumulation rate of rhodamine 123 in MDR cells (Bel7402 and HCT8), and most exhibited more potent MDR-reversing activity relative to the reference compound verapamil. Compounds 8, 10, 13, and 14 enhanced intracellular accumulation of doxorubicin in Bel7402 and HCT8 cells.

Acknowledgments

We are grateful for financial support of this work by the National Natural Sciences Foundation of China (No. 30630069).

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