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天然产物中的萜烯酯:细胞毒活性的合成与评价

Terpene Esters from Natural Products: Synthesis and Evaluation of Cytotoxic Activity.

作者信息

Victor Mauricio M, David Jorge M, Sakukuma Maria C K, Costa-Lotufo Letícia V, Moura Andrea F, Araújo Ana J

机构信息

Instituto de Química, Universidade Federal da Bahia, Depto de Química Orgânica, Rua Barão do Jeremoabo, s/n, Campus de Ondina, Ondina, 40170-115 Salvador, BA, Brazil.

Instituto Nacional de Ciência e Tecnologia/INCT de Energia e Ambiente,Universidade Federal da Bahia/UFBA, Rua Barão de Geremoabo, 147, Campus de Ondina, 40170-290 Salvador, BA, Brazil.

出版信息

An Acad Bras Cienc. 2017 Jul-Sep;89(3):1369-1379. doi: 10.1590/0001-3765201720160780. Epub 2017 Aug 14.

DOI:10.1590/0001-3765201720160780
PMID:28813102
Abstract

Natural steroids and triterpenes such as b-sitosterol, stigmasterol, lupeol, ursolic and betulinic acids were transformed into its hexanoic and oleic esters, to evaluate the influence of chemical modification towards the cytotoxic activities against tumor cells. The derivatives were evaluated against five tumor cell lines [OVCAR-8 (ovarian carcinoma); SF-295 (glioblastoma); HCT-116 (colon adenocarcinoma); HL-60 (leukemia); and PC-3 (prostate carcinoma)] and the results showed only betulinic acid hexyl ester exhibits cytotoxic potential activity.

摘要

天然甾体和三萜类化合物,如β-谷甾醇、豆甾醇、羽扇豆醇、熊果酸和桦木酸,被转化为它们的己酸酯和油酸酯,以评估化学修饰对肿瘤细胞细胞毒性活性的影响。对这些衍生物针对五种肿瘤细胞系[OVCAR-8(卵巢癌);SF-295(胶质母细胞瘤);HCT-116(结肠腺癌);HL-60(白血病);和PC-3(前列腺癌)]进行了评估,结果表明只有桦木酸己酯表现出细胞毒性活性。

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