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薯蓣皂苷元季铵衍生物的合成及其抗肿瘤活性。

Synthesis of diosgenyl quaternary ammonium derivatives and their antitumor activity.

机构信息

Key Laboratory of Basic Chemistry of the State Ethnic Affairs Commission, School of Chemistry and Environment, Southwest Minzu University, Chengdu 610041, PR China.

College of Pharmacy, Dalian Medical University, Dalian 116044, PR China.

出版信息

Steroids. 2021 Feb;166:108774. doi: 10.1016/j.steroids.2020.108774. Epub 2020 Dec 4.

DOI:10.1016/j.steroids.2020.108774
PMID:33285175
Abstract

Giosgenin is a naturally steroidal saponin exhibiting a variety of biological activities including antitumor ones. A series of novel diosgenyl quaternary ammonium derivatives were designed and synthesized to develop potential anti-tumor agents in our research. All novel derivatives were characterized by H NMR, C NMR and HR-MS, and evaluated for their in vitro anti-proliferative activities using MTT assay. The human cancer cell lines were A549 (Human lung cancer cell), H1975 (Human lung adenocarcinoma cell), A431 (Human skin squamous cell carcinoma), HCT-116 (Human colorectal adenocarcinoma cell), Aspc-1 (Human metastatic pancreatic cancer cell), Ramos (Human B lymphoma cell), HBE (Human bronchial epithelioid cell) and LO2 (Human normal hepatocyte).

摘要

吉奥辛苷元是一种具有多种生物活性的天然甾体皂苷,包括抗肿瘤活性。本研究设计并合成了一系列新型薯蓣皂苷季铵衍生物,以开发潜在的抗肿瘤药物。所有新的衍生物都通过 1H NMR、13C NMR 和 HR-MS 进行了表征,并通过 MTT 测定法评估了它们对体外增殖活性的抑制作用。人癌细胞株包括 A549(人肺癌细胞)、H1975(人肺腺癌细胞)、A431(人皮肤鳞状细胞癌)、HCT-116(人结直肠腺癌细胞)、Aspc-1(人转移性胰腺癌细胞)、Ramos(人 B 淋巴瘤细胞)、HBE(人支气管上皮样细胞)和 LO2(人正常肝细胞)。

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