Hoshi A, Ikekawa T, Ikeda Y, Shirakawa S, Iigo M
Gan. 1976 Apr;67(2):321-5.
The antitumor activity of berberine, berberrubine, and their derivatives against sarcoma-180 ascites was determined by the total packed cell volume method. Berbine and tetrahydroberberine derivatives had no antitumor activity, but berberrubine (9-demethylberberine) and the ester derivatives of berberrubine had a strong antitumor activity. ED90 of berberrubine, its acetate and benzoate, were 15, 23, and 44 mg/kg, respectively. The therapeutic indices (LD10/ED90 by the present method) of these compounds were as follows: Berberrubine hydrochloride, 6.7 approximately 9.4; 9-acetyl-9-demethylberberine (9-acetylberberrubine) chloride, 7.6 approximately 8.7; 9-benzoyl-9-demethylberberine (9-benzoylberberrubine) chloride, 3.4 approximately 4.9.
采用全血细胞容积法测定了黄连素、小檗红碱及其衍生物对肉瘤-180腹水的抗肿瘤活性。黄连素和四氢黄连素衍生物无抗肿瘤活性，但小檗红碱（9-去甲基黄连素）及其酯衍生物具有较强的抗肿瘤活性。小檗红碱及其醋酸酯和苯甲酸酯的半数有效剂量（ED90）分别为15、23和44mg/kg。这些化合物的治疗指数（本法测定的LD10/ED90）如下：盐酸小檗红碱，约6.7至9.4；9-乙酰基-9-去甲基黄连素（9-乙酰基小檗红碱）氯化物，约7.6至8.7；9-苯甲酰基-9-去甲基黄连素（9-苯甲酰基小檗红碱）氯化物，约3.4至4.9。
