Berberrubine chloride

Berberrubine chloride（CAS 号 15401-69-1）是Berberrubine（CAS号17388-19-1）的盐酸盐形式。Berberrubine是一种源自黄连等中药的天然异喹啉生物碱（小檗碱， Berberine（CAS号2086-83-1）主要代谢产物），核心生物学功能包括抗菌、抗炎、降糖、抗高尿酸血症、抗血栓形成及抑制结直肠癌、非小细胞肺癌（NSCLC）等肿瘤增殖，还能激活谷胱甘肽 S - 转移酶 Mu2（GSTM2）发挥肿瘤抑制作用；作用靶点及类型多样：抑制IMP 脱氢酶 2（IMPDH2，竞争性结合，对 IMPDH2 选择性高于 IMPDH1 15 倍以上）、硫氧还蛋白还原酶（TrxR，特异性靶向 Sec498 残基）、维生素 K 环氧化物还原酶（VKOR）及 γ- 谷氨酰羧化酶（GGCX），激活GSTM2（通过 SP1 转录因子激活及 DNA 去甲基化），抑制NF-κB 核转位、JAK2/STAT3 信号通路及尿酸转运体 URAT1/GLUT9，上调尿酸排泄转运体 OAT1/3/ABCG2，还可抑制拓扑异构酶 II 介导的 DNA 切割；关键活性数据：IMPDH2 抑制 IC₅₀ 2.37 μM、TrxR 抑制 IC₅₀ 5.0 μM，对白色念珠菌等真菌 MIC 值 1-16 μg/mL（13-(4 - 异丙基苄基) 衍生物活性最强）；常见用于治疗动物模型，包括 AOM/DSS 诱导结直肠癌模型、PO/HX 诱导高尿酸血症模型、角叉菜胶诱导血栓模型、DSS 诱导溃疡性结肠炎模型、NSCLC 异种移植模型。

常用应用与浓度：细胞培养中，SW620/LS174T 结直肠癌细胞 10-80 μM、A549 NSCLC 细胞 20-50 μM、ARPE-19 视网膜色素上皮细胞 0.2-25 μM、BFTC 905 膀胱癌细胞 50 μM；动物实验中，结直肠癌模型口服 25-50 mg/kg/d、高尿酸血症模型口服 6.25-25 mg/kg/d、血栓模型口服 50-100 mg/kg/d、结肠炎模型口服 100-200 mg/kg/d；临床无直接应用浓度；有效治疗浓度：细胞层面 10-80 μM 可抑制肿瘤细胞增殖、20 μM 联合顺铂可增强 NSCLC 化疗敏感性，动物层面 25-50 mg/kg/d 可显著抑制结直肠癌肿瘤生长、25 mg/kg/d 可降低高尿酸血症小鼠血清尿酸水平 75% 以上、100 mg/kg 口服可抑制血栓形成且不增加出血风险。

参考文献：

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