天然β-香茅醇衍生物作为治疗2型糖尿病和阿尔茨海默病的潜在双酶抑制剂

IF 1.6 3区 化学 Q3 CHEMISTRY, APPLIED
Ram Chander, Ritesh Sharma, Vijai K Agnihotri
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引用次数: 0

摘要

2型糖尿病(T2DM)和阿尔茨海默病(AD)的有效治疗策略包括抑制α-淀粉酶、α-葡萄糖苷酶治疗T2DM和阻断乙酰胆碱酯酶(AChE)治疗AD。从龙脑油中分离得到3个化合物(化合物2 ~ 4),利用NMR和GC-MS技术对其进行了分析。结果表明,化合物2和4对α-葡萄糖苷酶和乙酰胆碱酯酶的抑制作用最显著。亲本化合物1、3和4对α-淀粉酶的抑制作用最强。网络药理学鉴定出CXCR4(得分:14)和PIK3CA(得分:12)是最重要的靶点。这些发现表明,PIK3CA调节葡萄糖代谢、胰岛素信号传导和细胞存活,而CXCR4可能具有神经保护和抗炎作用。构效关系表明,β-香茅醇β-碳烷氧基官能团化是其活性的关键。它强调,一种β-香茅醇衍生物可以治疗双重T2DM和AD疾病。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Natural β-citronellol derivatives as potential dual enzyme inhibitors for the treatment of type 2 diabetes and Alzheimer's diseases.

Effective strategies for treating type-2 diabetes mellitus (T2DM) and Alzheimer's disease (AD) involve inhibition of α-amylase, α-glucosidase for T2DM and block acetylcholinesterase (AChE) enzymes for treating AD. To explore this potential natural β-citronellol, isolated from Dracocephalum heterophyllum Benth essential oil, was derivatized to yield three derivatives (Compounds 2-4), analysed using NMR and GC-MS techniques. The results showed that compounds 2 and 4 had the most significant α-glucosidase and AChE inhibition. Parent compound 1, along with 3 and 4, displayed the highest α-amylase inhibition. Network pharmacology identified CXCR4 (score: 14) and PIK3CA (score: 12) as top-ranked targets. These findings suggest that PIK3CA, which regulates glucose metabolism, insulin signalling, and cell survival, while CXCR4 suggests potential for neuroprotective and anti-inflammatory roles. Structure-activity relationship indicated that alkoxy group functionalization at β-carbon of β-citronellol is essential for activity. It highlights, a single β-citronellol derivative can manage dual T2DM and AD diseases.

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来源期刊
Natural Product Research
Natural Product Research 化学-医药化学
CiteScore
5.10
自引率
9.10%
发文量
605
审稿时长
2.1 months
期刊介绍: The aim of Natural Product Research is to publish important contributions in the field of natural product chemistry. The journal covers all aspects of research in the chemistry and biochemistry of naturally occurring compounds. The communications include coverage of work on natural substances of land and sea and of plants, microbes and animals. Discussions of structure elucidation, synthesis and experimental biosynthesis of natural products as well as developments of methods in these areas are welcomed in the journal. Finally, research papers in fields on the chemistry-biology boundary, eg. fermentation chemistry, plant tissue culture investigations etc., are accepted into the journal. Natural Product Research issues will be subtitled either ""Part A - Synthesis and Structure"" or ""Part B - Bioactive Natural Products"". for details on this , see the forthcoming articles section. All manuscript submissions are subject to initial appraisal by the Editor, and, if found suitable for further consideration, to peer review by independent, anonymous expert referees. All peer review is single blind and submission is online via ScholarOne Manuscripts.
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