Publications
Product
| 지원과제 | cPMTb |
| 저자명 | Lee DH, Hasanuzzaman MD, Kwon DH, Choi HY, Kim SM, Kim DJ, Kang DJ, Hwang TH, Kim HH, Shin HJ, Shin JG, Oh S, Lee SJ, Kim SW |
| 학회정보 | Curr Pharm Des. 24(46):5590-5597 / 2019.02 |
| 제 목 | 10-Phenyltriazoyl artemisinin is a novel P-glycoprotein inhibitor that suppresses the overexpression and function of P-glycoprotein. |
| LINK | www.ncbi.nlm.nih.gov/pubmed/30799787/ |
| 게시일 | 2025-03-17 11:12:44 |
| 년도 | |
| 내용 | Background: The effect of drugs on ATP-binding cassette transporters, especially permeabilityglycoprotein (P-gp), is an important consideration during new anti-cancer drug development.
Objective: In this context, the effects of a newly synthesized artemisinin derivative, 10-(4-phenyl-1H-1,2,3- triazol)-artemisinin (5a), were evaluated on P-gp expression and function. Methods: Reverse transcript polymerase chain reaction and immunoblotting techniques were used to determine the effect of 5a on P-gp expression in LS174T cells. In addition, the ability of 5a to work as either a substrate or an inhibitor of P-gp was investigated through different methods. Results: The results revealed that 5a acts as a novel P-gp inhibitor that dually suppresses the overexpression and function of P-glycoprotein. Co-treatment of LS174T cell line, human colon adenocarcinoma cell line, with 5a and paclitaxel recovered the anticancer effect of paclitaxel by controlling the acquired drug resistance pathway. The overexpression of P-gp induced by rifampin and paclitaxel in a colorectal cell line was suppressed by 5a which could be a novel inhibitory substrate inhibiting the transport of paclitaxel by P-gp. Conclusion: The results revealed that 5a can be classified as a type B P-gp inhibitor (with both substrate and inhibitor activities) with an additional function of suppressing P-gp overexpression. The results might be clinically useful in the development of anticancer drugs against cancers with multidrug resistance. Keywords: Artemisinin; immunoblotting techniques; p-glycoprotein; paclitaxel; rifampin; triazolyl artemisinin. |
