Tags

Type your tag names separated by a space and hit enter

1,3-Benzodioxole-based fibrate derivatives as potential hypolipidemic and hepatoprotective agents.
Bioorg Med Chem Lett. 2021 Jul 01; 43:127898.BM

Abstract

A series of target compounds 1,3-benzodioxole-based fibrate derivatives were designed and synthesized. All the target compounds were preliminarily evaluated by hyperlipidemia mice induced by Triton WR-1339, in which compound 12 displayed a greater anti-hyperlipidemia activity than other compounds as well as positive drug fenofibrate (FF). 12 showed a significant reduction of plasma lipids, such as triglycerides (TG), total cholesterol (TC) and low-density lipoprotein cholesterin (LDL-C), in high fat diet (HFD) induced hyperlipidemic mice. In addition, hepatic transaminases (AST and ALT) were ameliorated after administration of 12, in particular the AST, and the histopathological examination showed that 12 improved the hepatic lipid accumulation. The expression of PPAR-α involved in lipids metabolism was up-regulated in the liver tissues of 12-treated group. Other significant activity such as antioxidant, and anti-inflammation was confirmed and reinforced the effects of 12 as a potential hypolipidemia and hepatoprotective agent.

Authors+Show Affiliations

College of Pharmacy, Shaanxi University of Chinese Medicine, Xi'an-xianyang New Ecomic Zone 712046, China.The People's Hospital of Yongcheng, 888 Ouya Road, Yongcheng City, Shangqiu City, Henan Province 476600, China.College of Pharmacy, Shaanxi University of Chinese Medicine, Xi'an-xianyang New Ecomic Zone 712046, China; Key Laboratory of Pharmacodynamics and Material Basis of Chinese Medicine, Shaanxi Administration of Traditional Chinese Medicine, Xianyang 712046, China; Subject Innovation Team of Shaanxi University of Chinese Medicine, China.College of Pharmacy, Shaanxi University of Chinese Medicine, Xi'an-xianyang New Ecomic Zone 712046, China; Key Laboratory of Pharmacodynamics and Material Basis of Chinese Medicine, Shaanxi Administration of Traditional Chinese Medicine, Xianyang 712046, China; Subject Innovation Team of Shaanxi University of Chinese Medicine, China.College of Pharmacy, Shaanxi University of Chinese Medicine, Xi'an-xianyang New Ecomic Zone 712046, China; Key Laboratory of Pharmacodynamics and Material Basis of Chinese Medicine, Shaanxi Administration of Traditional Chinese Medicine, Xianyang 712046, China; Subject Innovation Team of Shaanxi University of Chinese Medicine, China.College of Pharmacy, Shaanxi University of Chinese Medicine, Xi'an-xianyang New Ecomic Zone 712046, China.College of Pharmacy, Shaanxi University of Chinese Medicine, Xi'an-xianyang New Ecomic Zone 712046, China.College of Pharmacy, Shaanxi University of Chinese Medicine, Xi'an-xianyang New Ecomic Zone 712046, China.College of Pharmacy, Shaanxi University of Chinese Medicine, Xi'an-xianyang New Ecomic Zone 712046, China.Department of Pharmacy, Xi'an Jiaotong University, Xi'an 710061, China. Electronic address: bianxl@mail.xjtu.edu.cn.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

33684440

Citation

Xie, Yun-Dong, et al. "1,3-Benzodioxole-based Fibrate Derivatives as Potential Hypolipidemic and Hepatoprotective Agents." Bioorganic & Medicinal Chemistry Letters, vol. 43, 2021, p. 127898.
Xie YD, Xu YH, Liu JP, et al. 1,3-Benzodioxole-based fibrate derivatives as potential hypolipidemic and hepatoprotective agents. Bioorg Med Chem Lett. 2021;43:127898.
Xie, Y. D., Xu, Y. H., Liu, J. P., Wang, B., Shi, Y. H., Wang, W., Wang, X. P., Sun, M., Xu, X. Y., & Bian, X. L. (2021). 1,3-Benzodioxole-based fibrate derivatives as potential hypolipidemic and hepatoprotective agents. Bioorganic & Medicinal Chemistry Letters, 43, 127898. https://doi.org/10.1016/j.bmcl.2021.127898
Xie YD, et al. 1,3-Benzodioxole-based Fibrate Derivatives as Potential Hypolipidemic and Hepatoprotective Agents. Bioorg Med Chem Lett. 2021 Jul 1;43:127898. PubMed PMID: 33684440.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - 1,3-Benzodioxole-based fibrate derivatives as potential hypolipidemic and hepatoprotective agents. AU - Xie,Yun-Dong, AU - Xu,Yan-Hong, AU - Liu,Ji-Ping, AU - Wang,Bin, AU - Shi,Yong-Heng, AU - Wang,Wei, AU - Wang,Xiao-Ping, AU - Sun,Meng, AU - Xu,Xin-Ya, AU - Bian,Xiao-Li, Y1 - 2021/03/06/ PY - 2020/12/03/received PY - 2021/02/12/revised PY - 2021/02/16/accepted PY - 2021/3/9/pubmed PY - 2021/3/9/medline PY - 2021/3/8/entrez KW - 1,3-benzodioxole-based fibrate derivatives KW - Hepatoprotection KW - Hypolipidemia KW - PPAR-α SP - 127898 EP - 127898 JF - Bioorganic & medicinal chemistry letters JO - Bioorg Med Chem Lett VL - 43 N2 - A series of target compounds 1,3-benzodioxole-based fibrate derivatives were designed and synthesized. All the target compounds were preliminarily evaluated by hyperlipidemia mice induced by Triton WR-1339, in which compound 12 displayed a greater anti-hyperlipidemia activity than other compounds as well as positive drug fenofibrate (FF). 12 showed a significant reduction of plasma lipids, such as triglycerides (TG), total cholesterol (TC) and low-density lipoprotein cholesterin (LDL-C), in high fat diet (HFD) induced hyperlipidemic mice. In addition, hepatic transaminases (AST and ALT) were ameliorated after administration of 12, in particular the AST, and the histopathological examination showed that 12 improved the hepatic lipid accumulation. The expression of PPAR-α involved in lipids metabolism was up-regulated in the liver tissues of 12-treated group. Other significant activity such as antioxidant, and anti-inflammation was confirmed and reinforced the effects of 12 as a potential hypolipidemia and hepatoprotective agent. SN - 1464-3405 UR - https://www.unboundmedicine.com/medline/citation/33684440/13_Benzodioxole_based_fibrate_derivatives_as_potential_hypolipidemic_and_hepatoprotective_agents_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0960-894X(21)00124-4 DB - PRIME DP - Unbound Medicine ER -
Try the Free App:
Prime PubMed app for iOS iPhone iPad
Prime PubMed app for Android
Prime PubMed is provided
free to individuals by:
Unbound Medicine.