11,13 - 脱氢内酯部分在妇科癌细胞中的情况。
11, 13-Dehydro Lactone Moiety in Gynecologic Cancer Cells.
作者信息
Liu Yibing, Meng Qingju, Jing Li, Feng Li, Zhou Zhiguo, Ni Zhiyu
机构信息
Department of Medical Oncology, Fourth Hospital of Hebei Medical University, Shijiazhuang, Hebei Province, China.
Department of Orthopedics, The First Hospital of Xingtai, Xingtai, Hebei Province, China.
出版信息
Iran J Public Health. 2020 Nov;49(11):2103-2110. doi: 10.18502/ijph.v49i11.4726.
BACKGROUND
To study the anti-cancer effect of isoalantolactone, a sesquiterpene lactoneisolated from the roots of on human gynecologic cancer cells.
METHODS
A structure-activity relationship experiment was designed to identify the functional moiety of isoalantolactone for its significant anti-cancer activity. Five gynecologic cancer cell lines were treated with isoalantolactone. Cell proliferation was determined by MTT assay in vitro and cell apoptosis by flow cytometry.
RESULTS
We found isoalantolactone strongly inhibited the cell proliferationofHEC-1, HAC-2, HOC-21, and HeLa cells. Its inhibitory effect was comparable to that of well-known chemotherapeutic agents, cisplatin and taxol. Furthermore, isoalantolactone induced apoptosis in HeLa cells via caspase. On the contrary, its 11, 13-dihydro derivatives had much weaker anti-proliferative activities than the parent compound.
CONCLUSION
Isoalantolactone exhibited strong anti-proliferative activities and apoptosis-inducing effects on gynecologic cancer cells. The 11, 13-dehydro lactone moiety was critical for its anti-proliferative activity.
背景
研究从土木香根中分离出的倍半萜内酯异土木香内酯对人妇科癌细胞的抗癌作用。
方法
设计结构-活性关系实验以确定异土木香内酯具有显著抗癌活性的功能基团。用异土木香内酯处理5种妇科癌细胞系。通过MTT法体外测定细胞增殖，通过流式细胞术测定细胞凋亡。
结果
我们发现异土木香内酯强烈抑制HEC-1、HAC-2、HOC-21和HeLa细胞的增殖。其抑制作用与著名化疗药物顺铂和紫杉醇相当。此外，异土木香内酯通过半胱天冬酶诱导HeLa细胞凋亡。相反，其11,13-二氢衍生物的抗增殖活性比母体化合物弱得多。
结论
异土木香内酯对妇科癌细胞表现出强烈的抗增殖活性和凋亡诱导作用。11,13-脱氢内酯基团对其抗增殖活性至关重要。
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