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Mesut Ozdincer¹, Aslihan Dalmaz², Sefa Durmus³

¹Duzce University, Department of Composite - Materials, Graduate Education Institute, Duzce, 81620, Türkiye.

Anais da Academia Brasileira de Ciencias

|July 17, 2024

概括

新的西醇化合物显示出强大的抗微生物和抗癌潜力. 化合物6e对细菌和真菌表现出显著的活性,而其他衍生物则通过向VEGFR-2激酶来治疗胃肠道癌症.

科学领域:

药用化学医学化学
有机合成有机合成
药理学药理学是指药理学的学科.

背景情况:

索化合物是一种重要的双循环结构,具有多样化的生物应用.
这些化合物表现出广泛的活性,包括抗癌,抗微生物和抗炎作用.

研究的目的:

为了合成新的佐衍生物.
评估它们的抗微生物和抗癌性质.
通过计算对接来研究它们的作用机制.

主要方法:

合成本佐提亚醇化合物.
针对细菌和真菌菌株的抗微生物测定.
对胃肠道癌细胞系的抗增殖试验 (AGS,HCT116).
卡斯帕酶表达分析 (卡斯帕酶-3,8,9).
使用VEGFR-2激酶进行计算分子对接.

主要成果:

化合物6e对已测试的细菌和真菌菌株表现出优异的抗菌活性,特别是对金黄色葡萄球菌.
合成的本佐醇对胃肠道癌细胞表现出强烈的抗癌活性,对AGS细胞有显著影响.
化合物通过增加癌细胞系中的caspase-3,8和9表达来诱导亡.
对接研究表明,6a和6d化合物与VEGFR-2激酶具有强烈的结合亲和力.

结论:

合成的西醇衍生物具有显著的抗微生物和抗癌潜力.
化合物6e是一种高效的抗菌剂.
化合物6a和6d通过VEGFR-2激酶抑制显示为胃肠癌的治疗药物.

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