{"title":"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","authors":"Ram Chander, Ritesh Sharma, Vijai K Agnihotri","doi":"10.1080/14786419.2025.2572038","DOIUrl":null,"url":null,"abstract":"<p><p>Effective strategies for treating type-2 diabetes mellitus (T2DM) and Alzheimer's disease (AD) involve inhibition of <i>α</i>-amylase, <i>α</i>-glucosidase for T2DM and block acetylcholinesterase (AChE) enzymes for treating AD. To explore this potential natural <i>β</i>-citronellol, isolated from <i>Dracocephalum heterophyllum</i> 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 <i>α</i>-glucosidase and AChE inhibition. Parent compound 1, along with 3 and 4, displayed the highest <i>α</i>-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 <i>β</i>-carbon of <i>β</i>-citronellol is essential for activity. It highlights, a single <i>β</i>-citronellol derivative can manage dual T2DM and AD diseases.</p>","PeriodicalId":18990,"journal":{"name":"Natural Product Research","volume":" ","pages":"1-6"},"PeriodicalIF":1.6000,"publicationDate":"2025-10-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Natural <i>β</i>-citronellol derivatives as potential dual enzyme inhibitors for the treatment of type 2 diabetes and Alzheimer's diseases.\",\"authors\":\"Ram Chander, Ritesh Sharma, Vijai K Agnihotri\",\"doi\":\"10.1080/14786419.2025.2572038\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>Effective strategies for treating type-2 diabetes mellitus (T2DM) and Alzheimer's disease (AD) involve inhibition of <i>α</i>-amylase, <i>α</i>-glucosidase for T2DM and block acetylcholinesterase (AChE) enzymes for treating AD. To explore this potential natural <i>β</i>-citronellol, isolated from <i>Dracocephalum heterophyllum</i> 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 <i>α</i>-glucosidase and AChE inhibition. Parent compound 1, along with 3 and 4, displayed the highest <i>α</i>-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 <i>β</i>-carbon of <i>β</i>-citronellol is essential for activity. It highlights, a single <i>β</i>-citronellol derivative can manage dual T2DM and AD diseases.</p>\",\"PeriodicalId\":18990,\"journal\":{\"name\":\"Natural Product Research\",\"volume\":\" \",\"pages\":\"1-6\"},\"PeriodicalIF\":1.6000,\"publicationDate\":\"2025-10-14\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Natural Product Research\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://doi.org/10.1080/14786419.2025.2572038\",\"RegionNum\":3,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"CHEMISTRY, APPLIED\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Natural Product Research","FirstCategoryId":"92","ListUrlMain":"https://doi.org/10.1080/14786419.2025.2572038","RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, APPLIED","Score":null,"Total":0}
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.
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.