{"title":"从Euphorbia antiquorum块茎中提取的具有多药耐药性逆转活性的鳞茎二萜类化合物。","authors":"","doi":"10.1016/j.phytochem.2024.114233","DOIUrl":null,"url":null,"abstract":"<div><p>Nine previously unreported lathyrane diterpenoids named euphorantesters A−I, along with 16 known analogues, have been separated from the tubers of <em>Euphorbia antiquorum</em>. Their structures were established by means of spectroscopic analyses, time-dependent density functional theory based electronic circular dichroism calculation and single crystal X-ray crystallography. Their reversal ability against P-glycoprotein-mediated multidrug resistance (MDR) in MCF-7/ADR cell line was then evaluated, and 15 ones exhibited moderate MDR reversal activity with reversal fold falling in the range of 1.12–13.15. The most active euphorantester B could effectively increase the sensitivity of MCF-7/ADR cell to adriamycin comparably to the reference drug verapamil.</p></div>","PeriodicalId":20170,"journal":{"name":"Phytochemistry","volume":null,"pages":null},"PeriodicalIF":3.2000,"publicationDate":"2024-08-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Lathyrane diterpenoids with multidrug resistance reversal activity from the tubers of Euphorbia antiquorum\",\"authors\":\"\",\"doi\":\"10.1016/j.phytochem.2024.114233\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>Nine previously unreported lathyrane diterpenoids named euphorantesters A−I, along with 16 known analogues, have been separated from the tubers of <em>Euphorbia antiquorum</em>. Their structures were established by means of spectroscopic analyses, time-dependent density functional theory based electronic circular dichroism calculation and single crystal X-ray crystallography. Their reversal ability against P-glycoprotein-mediated multidrug resistance (MDR) in MCF-7/ADR cell line was then evaluated, and 15 ones exhibited moderate MDR reversal activity with reversal fold falling in the range of 1.12–13.15. The most active euphorantester B could effectively increase the sensitivity of MCF-7/ADR cell to adriamycin comparably to the reference drug verapamil.</p></div>\",\"PeriodicalId\":20170,\"journal\":{\"name\":\"Phytochemistry\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":3.2000,\"publicationDate\":\"2024-08-05\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Phytochemistry\",\"FirstCategoryId\":\"99\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S003194222400270X\",\"RegionNum\":2,\"RegionCategory\":\"生物学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"BIOCHEMISTRY & MOLECULAR BIOLOGY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Phytochemistry","FirstCategoryId":"99","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S003194222400270X","RegionNum":2,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"BIOCHEMISTRY & MOLECULAR BIOLOGY","Score":null,"Total":0}
引用次数: 0
摘要
从 Euphorbia antiquorum 的块茎中分离出了 9 种以前未报道过的被命名为 euphorantesters A-I 的 lathyrane 二萜类化合物,以及 16 种已知的类似物。通过光谱分析、基于时间相关密度泛函理论的电子圆二色性计算和单晶 X 射线晶体学,确定了它们的结构。然后评估了它们对 MCF-7/ADR 细胞系中 P 糖蛋白介导的多药耐药性(MDR)的逆转能力,其中 15 种具有中等程度的 MDR 逆转活性,逆转倍数在 1.12-13.15 之间。与参考药物维拉帕米相比,活性最强的 euphorantester B 能有效提高 MCF-7/ADR 细胞对阿霉素的敏感性。
Lathyrane diterpenoids with multidrug resistance reversal activity from the tubers of Euphorbia antiquorum
Nine previously unreported lathyrane diterpenoids named euphorantesters A−I, along with 16 known analogues, have been separated from the tubers of Euphorbia antiquorum. Their structures were established by means of spectroscopic analyses, time-dependent density functional theory based electronic circular dichroism calculation and single crystal X-ray crystallography. Their reversal ability against P-glycoprotein-mediated multidrug resistance (MDR) in MCF-7/ADR cell line was then evaluated, and 15 ones exhibited moderate MDR reversal activity with reversal fold falling in the range of 1.12–13.15. The most active euphorantester B could effectively increase the sensitivity of MCF-7/ADR cell to adriamycin comparably to the reference drug verapamil.
期刊介绍:
Phytochemistry is a leading international journal publishing studies of plant chemistry, biochemistry, molecular biology and genetics, structure and bioactivities of phytochemicals, including ''-omics'' and bioinformatics/computational biology approaches. Phytochemistry is a primary source for papers dealing with phytochemicals, especially reports concerning their biosynthesis, regulation, and biological properties both in planta and as bioactive principles. Articles are published online as soon as possible as Articles-in-Press and in 12 volumes per year. Occasional topic-focussed special issues are published composed of papers from invited authors.