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穿心莲内酯衍生物的合成及初步抗高血脂活性评价。

Synthesis and preliminary antihyperlipidaemic activities evaluation of andrographolide derivatives.

机构信息

School of Pharmacy, China Pharmaceutical University, Nanjing 210009, People's Republic of China.

出版信息

Med Chem. 2012 Mar;8(2):293-8. doi: 10.2174/157340612800493629.

DOI:10.2174/157340612800493629
PMID:22385174
Abstract

Recent studies indicated that andrographolide was a potential antihyperlipidaemic therapeutic agent. In the paper, the synthesis of a series of andrographolide derivatives was described and their antihyperlipidaemic activities were evaluated in vivo. As compared with TG, TC, HDL-C and LDL-C concentrations, some of the derivatives exhibited better antihyperlipidaemic effects than positive control atromide. Therein, compound 6i, which was the most potent compound, could serve as a new lead for further development of antihyperlipidaemic agents.

摘要

最近的研究表明,穿心莲内酯是一种有潜力的抗高血脂治疗药物。本文描述了一系列穿心莲内酯衍生物的合成,并在体内评估了它们的抗高血脂活性。与 TG、TC、HDL-C 和 LDL-C 浓度相比,一些衍生物的抗高血脂效果优于阳性对照阿托伐他汀。其中,活性最强的化合物 6i 可以作为进一步开发抗高血脂药物的新先导化合物。

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引用本文的文献

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Identification of Andrographolide as an Agonist of Bile Acid TGR5 Receptor in a Cell Line to Demonstrate the Reduction in Hyperglycemia in Type-1 Diabetic Rats.穿心莲内酯作为细胞系中胆汁酸TGR5受体激动剂的鉴定,以证明1型糖尿病大鼠高血糖的降低。
Pharmaceuticals (Basel). 2023 Oct 5;16(10):1417. doi: 10.3390/ph16101417.
2
Synthesis, In Vitro, In Vivo and In Silico Antidiabetic Bioassays of 4-Nitro(thio)phenoxyisobutyric Acids Acting as Unexpected PPARγ Modulators: An In Combo Study.作为意外的PPARγ调节剂的4-硝基(硫代)苯氧基异丁酸的合成、体外、体内和计算机辅助抗糖尿病生物测定:一项联合研究。
Pharmaceuticals (Basel). 2022 Jan 15;15(1):102. doi: 10.3390/ph15010102.
3
Andrographolide, a New Hope in the Prevention and Treatment of Metabolic Syndrome.
穿心莲内酯,代谢综合征防治的新希望。
Front Pharmacol. 2017 Aug 23;8:571. doi: 10.3389/fphar.2017.00571. eCollection 2017.