Background: There is a correlation between tumor and inflammation. The activity of 13-[CH₂CO-Cys(Bzl)-OBzl]-berberine (13-Cys-BBR) slowing tumor growth is higher than that of BBR. Whether the anti-inflammation activity of 13-Cys-BBR is higher than that of BBR remains unknown. There is a correlation between thrombosis and inflammation. Whether 13-Cys-BBR is an inhibitor of thrombosis remains unknown.
Purpose: The object of this investigation is to compare the activities of 13-Cys-BBR inhibiting thrombosis and inflammation to those of BBR.
Methods: In vivo anti-thrombosis assay was performed on rat model of arterial and venous thrombosis. In vivo anti-inflammation assay was performed on mouse model of xylene induced ear edema.
Results: At oral dose of 66.7 nmol/kg, 13-Cys-BBR, but not BBR, inhibited the rats to form both venous thrombus and arterial thrombus. At oral dose of 2 μmol/kg, 13-Cys-BBR, but not BBR, inhibited the ears of the mice to occur edema.
Conclusion: The anti-venous thrombosis activity, anti-arterial thrombosis activity and anti-inflammation activity of 13-Cys-BBR were significantly higher than those of BBR. 13-Cys-BBR is a promising preclinical candidate.



中文翻译：

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开发 13-Cys-BBR 作为具有抗血栓和抗炎双重作用的药物。

背景：肿瘤和炎症之间存在相关性。13-[CH ₂ CO-Cys(Bzl)-OBzl]-小檗碱(13-Cys-BBR)减缓肿瘤生长的活性高于BBR。13-Cys-BBR 的抗炎活性是否高于 BBR 尚不清楚。血栓形成与炎症之间存在相关性。13-Cys-BBR 是否是血栓形成的抑制剂仍然未知。
目的：本研究的目的是比较 13-Cys-BBR 与 BBR 抑制血栓形成和炎症的活性。
方法：对大鼠动静脉血栓模型进行体内抗血栓试验。对二甲苯诱导的耳水肿小鼠模型进行体内抗炎试验。
结果：在 66.7 nmol/kg 的口服剂量下，13-Cys-BBR，但不是 BBR，抑制大鼠形成静脉血栓和动脉血栓。在2 μmol/kg的口服剂量下，13-Cys-BBR，而不是BBR，抑制了小鼠耳朵出现水肿。
结论： 13-Cys-BBR的抗静脉血栓活性、抗动脉血栓活性和抗炎活性均显着高于BBR。13-Cys-BBR 是一种很有前途的临床前候选药物。