Screening The Anticancer Activity for New Schiff Bases of Natural Steroids

Q3 Chemistry Molekul Pub Date : 2023-11-20 DOI:10.20884/1.jm.2023.18.3.8859
Nawfal Abdul Samad Selman, Layla Jasim Abbas
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Abstract

The significance of cholesterol and ergosterol (provitamin d2) in biological systems has prompted interest in these compounds as pharmaceuticals. It has been reported on the effective straightforward synthesis of Schiff base modifications of cholesterol aldehyde and ergosterol aldehyde and their assessment as possible agents against cancer (esophagus natural cell lines and human cancer cells). Through a process called Steglish esterification, the initial cholesterol and ergosterol are converted into their respective aldehyde derivatives, by reacting with amines such as 2-amino 6-fluoro benzothiazole, carbohydrazide, and thiosemicarbazide, these aldehyde derivatives are transformed into the appropriate Schiff base derivatives, and then their anticancer activity is checked using the MTT (Microculture Tetrazolium Assay) assay method. For the purpose of analyzing their cytotoxic effects, these compounds were tested on cancerous (SK-GT-4, human esophageal adenocarcinoma) and normal (normal cell line, Rat Embryonic fibroblast (REF)) cell lines. The MTT assay results revealed that the compounds (a1, a2, c1, c2, compound 1) were more harmful to human esophageal cancer cell line than to healthy cell line other than compounds (t1, t2, compound 2, ergosterol and cholesterol alone). Overall, our research indicated that provitamin D2 (ergosterol), a1, a2, c2, t2, compound 1, had a growth-inhibiting effect on both cell lines compared to c1, t1, compound 2, and cholesterol alone.
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筛选天然类固醇的新型希夫碱的抗癌活性
胆固醇和麦角固醇(维生素 d2)在生物系统中的重要性促使人们对这些化合物作为药物产生了兴趣。有报告称,胆固醇醛和麦角固醇醛的希夫碱修饰物可直接有效合成,并可作为抗癌剂(食道天然细胞系和人类癌细胞)。通过一种称为 Steglish 酯化的过程,初始胆固醇和麦角甾醇被转化为各自的醛衍生物,通过与胺类物质如 2- 氨基 6-氟苯并噻唑、羧酰肼和硫代氨基甲酰肼反应,这些醛衍生物被转化为适当的希夫碱衍生物,然后使用 MTT(微培养四氮唑测定法)检测它们的抗癌活性。为了分析它们的细胞毒性作用,这些化合物分别在癌细胞(SK-GT-4,人食管腺癌)和正常细胞(正常细胞系,大鼠胚胎成纤维细胞(REF))上进行了测试。MTT 试验结果表明,与化合物(t1、t2、化合物 2、麦角甾醇和胆固醇)相比,化合物(a1、a2、c1、c2、化合物 1)对人食管癌细胞株的伤害大于对健康细胞株的伤害。总之,我们的研究表明,与 c1、t1、化合物 2 和单独的胆固醇相比,维生素 D2(麦角甾醇)、a1、a2、c2、t2 和化合物 1 对两种细胞株都有抑制生长的作用。
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来源期刊
Molekul
Molekul Chemistry-Chemistry (all)
CiteScore
1.30
自引率
0.00%
发文量
31
审稿时长
4 weeks
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