3-和5-β-去斑蝥素偶联物的合成。

IF 1.9 3区 化学 Q3 CHEMISTRY, APPLIED Natural Product Research Pub Date : 2025-02-01 DOI:10.1080/14786419.2023.2269466
Han Lin , Weiwei Dong , Changkuo Zhao , Xianheng Wang
{"title":"3-和5-β-去斑蝥素偶联物的合成。","authors":"Han Lin ,&nbsp;Weiwei Dong ,&nbsp;Changkuo Zhao ,&nbsp;Xianheng Wang","doi":"10.1080/14786419.2023.2269466","DOIUrl":null,"url":null,"abstract":"<div><div>Using molecular hybridisation to develop conjugates of natural antitumor drugs is one of the research hotspots in recent drug development. In this study, <em>β</em>-anhydroicaritine with anticancer activity was conjugated to norcantharidine selectively to develop new antitumor lead candidates. In the condition of EDCI/DMAP/DCM, the C-3 and C-5 hydroxyl groups of <em>β</em>-anhydroicaritine was coupled with norcantharidin monoacid ester respectively, and the inhibitory activity of the synthesised conjugates against HepG2, MCF-7 and L-02 cells were tested by CCK-8 method. Most of these conjugates showed a better activity against HepG2 and MCF-7 cell lines compared to parent compound icaritin, but weaker than another parent compound norcantharidin.</div></div>","PeriodicalId":18990,"journal":{"name":"Natural Product Research","volume":"39 3","pages":"Pages 415-422"},"PeriodicalIF":1.9000,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Synthesis of 3- and 5-β-anhydroicaritine norcantharidin conjugates\",\"authors\":\"Han Lin ,&nbsp;Weiwei Dong ,&nbsp;Changkuo Zhao ,&nbsp;Xianheng Wang\",\"doi\":\"10.1080/14786419.2023.2269466\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><div>Using molecular hybridisation to develop conjugates of natural antitumor drugs is one of the research hotspots in recent drug development. In this study, <em>β</em>-anhydroicaritine with anticancer activity was conjugated to norcantharidine selectively to develop new antitumor lead candidates. In the condition of EDCI/DMAP/DCM, the C-3 and C-5 hydroxyl groups of <em>β</em>-anhydroicaritine was coupled with norcantharidin monoacid ester respectively, and the inhibitory activity of the synthesised conjugates against HepG2, MCF-7 and L-02 cells were tested by CCK-8 method. Most of these conjugates showed a better activity against HepG2 and MCF-7 cell lines compared to parent compound icaritin, but weaker than another parent compound norcantharidin.</div></div>\",\"PeriodicalId\":18990,\"journal\":{\"name\":\"Natural Product Research\",\"volume\":\"39 3\",\"pages\":\"Pages 415-422\"},\"PeriodicalIF\":1.9000,\"publicationDate\":\"2025-02-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Natural Product Research\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://www.sciencedirect.com/org/science/article/pii/S1478641923023276\",\"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://www.sciencedirect.com/org/science/article/pii/S1478641923023276","RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, APPLIED","Score":null,"Total":0}
引用次数: 0

摘要

利用分子杂交技术开发天然抗肿瘤药物缀合物是近年来药物开发的研究热点之一。本研究将具有抗癌活性的β-无氢羊藿碱选择性地与去甲斑蝥啶偶联,以开发新的抗肿瘤先导物。在EDCI/DMAP/DCM条件下,将β-无氢羊藿碱的C-3和C-5羟基分别与去甲斑蝥素单酸酯偶联,采用CCK-8法检测合成的偶联物对HepG2、MCF-7和L-02细胞的抑制活性。这些结合物对HepG2和MCF-7细胞系的抑制活性均优于亲本化合物去斑蝥素,但弱于亲本化合物去斑蝥素。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
查看原文
分享 分享
微信好友 朋友圈 QQ好友 复制链接
本刊更多论文
Synthesis of 3- and 5-β-anhydroicaritine norcantharidin conjugates
Using molecular hybridisation to develop conjugates of natural antitumor drugs is one of the research hotspots in recent drug development. In this study, β-anhydroicaritine with anticancer activity was conjugated to norcantharidine selectively to develop new antitumor lead candidates. In the condition of EDCI/DMAP/DCM, the C-3 and C-5 hydroxyl groups of β-anhydroicaritine was coupled with norcantharidin monoacid ester respectively, and the inhibitory activity of the synthesised conjugates against HepG2, MCF-7 and L-02 cells were tested by CCK-8 method. Most of these conjugates showed a better activity against HepG2 and MCF-7 cell lines compared to parent compound icaritin, but weaker than another parent compound norcantharidin.
求助全文
通过发布文献求助,成功后即可免费获取论文全文。 去求助
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.
期刊最新文献
In vitro and in vivo evaluation of the trypanocidal activity of the acetone extract of lichen Usnea steineri and its chemical constituents. Phenolic constituents from the roots of Strobilanthes sarcorrhiza C. Ling and their bioactivity. Therapeutic potential of Brazilian green propolis and oregano (Origanum vulgare) extracts in collagen hydrogel for pressure ulcer repair: an experimental study in an animal model. 1H NMR-based metabolomics study of the lipid profile of argan oil and investigation of possible adulterations in the market of this valuable herbal oil. Integrative dereplication and molecular networking reveal potential antimicrobial agents in Kielmeyera coriacea Mart.
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
现在去查看 取消
×
提示
确定
0
微信
客服QQ
Book学术公众号 扫码关注我们
反馈
×
意见反馈
请填写您的意见或建议
请填写您的手机或邮箱
已复制链接
已复制链接
快去分享给好友吧!
我知道了
×
扫码分享
扫码分享
Book学术官方微信
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术
文献互助 智能选刊 最新文献 互助须知 联系我们:info@booksci.cn
Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。
Copyright © 2023 Book学术 All rights reserved.
ghs 京公网安备 11010802042870号 京ICP备2023020795号-1