首页> 外国专利> HYDROPHILIC BERBERINE DERIVATIVE WITH R10 AND R11 CONNECTED AND APPLICATION THEREOF IN PREPARATION OF DRUGS

HYDROPHILIC BERBERINE DERIVATIVE WITH R10 AND R11 CONNECTED AND APPLICATION THEREOF IN PREPARATION OF DRUGS

机译:连接有R 10 和R 11 的亲水小碱衍生物及其在药物制备中的应用

摘要

Disclosed are an 8-dihalide methyl berberine quaternary ammonium compound shown in formulas (I) and (II), a synthetic method therefor, and an application thereof in preparation of drugs. The 8-dihalide methyl berberine quaternary ammonium compound is more hydrophilic than a substrate in the absence of conventional hydrophilic groups. The 8-dihalide methyl berberine quaternary ammonium compound has a remarkable anti-microbial activity, anti-inflammatory activity and anti-ulcerative colitis activity, can explicitly and significantly regulate target molecules, associated with tumor formation, in tumor cells of the colon cancer, liver cancer, lung cancer, breast cancer, osteosarcoma, and glioma, and has anti-tumor activity. The pharmacological action of the compound of the present invention is higher than that of a control drug. Moreover, the compound has the characteristics of nontoxicity or hypotoxicity, and can be used for preparing drugs for preventing, alleviating, and/or treating microbiological contamination, inflammation, ulcerative colitis, and tumors.
机译:公开了式(I)和(II)中所示的8-二卤化物甲基小ber碱季铵化合物,其合成方法及其在制备药物中的应用。在不存在常规亲水基的情况下,该8-二卤化物甲基小tern碱季铵化合物比底物更具亲水性。 8-二卤化物甲基小ber碱季铵盐化合物具有显着的抗微生物活性,抗炎活性和抗溃疡性结肠炎活性,可以在结肠癌,肝脏的肿瘤细胞中显着并显着调节与肿瘤形成相关的靶分子。癌症,肺癌,乳腺癌,骨肉瘤和神经胶质瘤,并具有抗肿瘤活性。本发明化合物的药理作用高于对照药物的药理作用。此外,该化合物具有无毒或低毒的特征,并且可以用于制备预防,减轻和/或治疗微生物污染,炎症,溃疡性结肠炎和肿瘤的药物。

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