On December 31, 2018, Lee, Dong-Hwan; Hasanuzzaman, M.; Kwon, Daeho; Choi, Hye-Young; Kim, So Myoung; Kim, Dong Jin; Kang, Dong Ju; Hwang, Tae-Ho; Kim, Hyung-Hoi; Shin, Ho Jung; Shin, Jae-Gook; Oh, Sangtae; Lee, Seokjoon; Kim, So Won published an article.Recommanded Product: 5301-96-2 The title of the article was 10-Phenyltriazoyl Artemisinin is a Novel P-glycoprotein Inhibitor that Suppresses the Overexpression and Function of P-glycoprotein. And the article contained the following:
The effect of drugs on ATP-binding cassette transporters, especially permeability-glycoprotein (P-gp), is an important consideration during new anti-cancer drug development. 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. 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. 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. The results revealed that 5a can be classified as a type B P-gp inhibitor (with both substrate and inhibitor activities) with an addnl. function of suppressing P-gp overexpression. The results might be clin. useful in the development of anticancer drugs against cancers with multidrug resistance. The experimental process involved the reaction of 4-(p-Tolyl)-1H-1,2,3-triazole(cas: 5301-96-2).Recommanded Product: 5301-96-2
The Article related to glycoprotein inhibitor anticancer agent colon adenocarcinoma, artemisinin, immunoblotting techniques, p-glycoprotein, paclitaxel, rifampin, triazolyl artemisinin., Pharmacology: Effects Of Antimicrobials and Parasiticides and other aspects.Recommanded Product: 5301-96-2
Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics