辣椒素的新型衍生物是一种有效的降血脂和抗肥胖剂。

IF 3.9 2区化学 Q2 CHEMISTRY, APPLIED

Molecular Diversity Pub Date : 2024-10-24 DOI:10.1007/s11030-024-10971-0

Feng Li, Yingwei Hou, Haipeng Pang, Xiaofeng Song, Wenbao Li

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引用次数: 0

摘要

辣椒素是一种天然产品，具有多种生物活性，如消炎、镇痛、减肥、抗癌和预防心血管疾病等。然而，由于其刺激性强、水溶性差、药理作用不理想等原因，其进一步应用受到了限制。为了改善这一问题，我们设计并合成了一系列辣椒素及其类似物的衍生物。三个候选化合物（HJ-1-3、HJ-1-4 和 HJ-1-6）在体外和体内的生物学评价表明，它们在不同指标上都具有减少体内脂肪堆积和减肥的潜力。

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Novel derivatives of capsaicin as a potent hypolipidemic and anti-obesity agent.

Capsaicin is a natural product with multiple biological activities, such as anti-inflammatory, analgesic, weight loss, anti-cancer and cardiovascular disease prevention. However, its further applications have been limited by its strong irritation, poor water solubility, and unsatisfied pharmacological effects. To ameliorate the problem, a series of derivatives of capsaicin and its analogues were designed and synthesized. Three candidate compounds (HJ-1-3, HJ-1-4, HJ-1-6) have shown the potential to reduce body fat accumulation and lose weight on different indicators with biological evaluation in vitro and in vivo.

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来源期刊

Molecular Diversity 化学-化学综合

CiteScore

7.30

自引率

7.90%

发文量

219

审稿时长

2.7 months

期刊介绍： Molecular Diversity is a new publication forum for the rapid publication of refereed papers dedicated to describing the development, application and theory of molecular diversity and combinatorial chemistry in basic and applied research and drug discovery. The journal publishes both short and full papers, perspectives, news and reviews dealing with all aspects of the generation of molecular diversity, application of diversity for screening against alternative targets of all types (biological, biophysical, technological), analysis of results obtained and their application in various scientific disciplines/approaches including: combinatorial chemistry and parallel synthesis; small molecule libraries; microwave synthesis; flow synthesis; fluorous synthesis; diversity oriented synthesis (DOS); nanoreactors; click chemistry; multiplex technologies; fragment- and ligand-based design; structure/function/SAR; computational chemistry and molecular design; chemoinformatics; screening techniques and screening interfaces; analytical and purification methods; robotics, automation and miniaturization; targeted libraries; display libraries; peptides and peptoids; proteins; oligonucleotides; carbohydrates; natural diversity; new methods of library formulation and deconvolution; directed evolution, origin of life and recombination; search techniques, landscapes, random chemistry and more;