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Salsabeel N El Gendy¹, Amira K Elmotayam¹, Reham Samir²

¹Department of Pharmacognosy, Faculty of Pharmacy, Cairo University, Kasr El-Ainy Street, Cairo, 11562, Egypt.

|April 2, 2025

概括

使用Bacillus subtilis生物转化氨酸产生了apigenin-7-O-pentoside (A7P),这是一个强大的抗癌剂. 这种增强代谢物对肺癌和结直肠癌细胞具有显著的细胞毒性活性,对正常细胞的影响最小.

科学领域:

微生物学微生物学
药理学药理学是指药理学的学科.
生物化学生物化学

背景情况:

黄类化合物,如氨酸,具有治疗性质,但可以通过生物可用性受到限制.
生物转化提供了一种修改自然化合物的方法,有可能提高其生物活性.
细菌 Bacillus subtilis是一种具有已知的代谢能力的细菌,具有良好的特征.

研究的目的:

为了使用Bacillus subtilisATCC 23,857.7生物转化奎尔.
为了识别和描述由此产生的代谢产物.
评估这些代谢物对癌症细胞系的细胞毒性潜力,并将其与母化合物进行比较.

主要方法:

通过 Bacillus subtilis 生物转化奎尔丁.
使用LC-ESI-TOF-MS/MS.进行代谢物阐明.
通过MTT测定对A549和Caco-2癌细胞系进行细胞毒性评估.
对PI3Kδ和Cathepsin B进行分子对接研究.

主要成果:

鉴定出阿皮基宁-7-O-pentoside (A7P) 是主要的代谢物.
生物转化产品对A549 (IC50 = 0.78 mg/ml) 和Caco-2 (IC50 = 0.32 mg/ml) 细胞表现出度依赖的细胞毒性.
原始奎尔丁和生物转化产品对正常的人类皮肤纤维细胞 (hFB) 无毒.
分子对接表明A7P对与癌症相关的标 (PI3Kδ,CatB) 的结合亲和力高于Quercetin.

结论:

由Bacillus subtilis进行的生物转化有效地产生了从Quercetin中生成的生物活性代谢物.
阿皮基宁-7-O-pentoside 显示出有前途的抗癌潜力,因为它对关键癌症标具有增强的结合亲和力.
细菌生物转化是一种可行的策略,可以提高黄类药物的治疗疗效.

关键词:

它具有抗癌活性.原素-7-O-pentoside是一种原素-7-O-pentoside.卡瑟普辛B是B的类型之一.停靠研究对接研究微生物生物转化在PI3Kδδ

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