葡萄糖醛酸
体内
DMBA公司
维甲酸
效力
化学
毒性
芬瑞替尼
内科学
结合
内分泌学
乳腺肿瘤
药理学
体外
代谢物
生物
医学
癌症
生物化学
癌变
维甲酸
乳腺癌
生物技术
数学分析
基因
数学
作者
Hussein Abou‐Issa,Curley Rw,Panigot Mj,Tanagho Sn,Sidhu Bs,Alshafie Ga
出处
期刊:PubMed
日期:1997-12-31
卷期号:17 (5A): 3335-9
被引量:5
摘要
The growth inhibitory effects of N-(4- Hydroxyphenyl) retinamide (4-HPR) and its glucuronide derivative, N-(4-Hydroxyphenyl) retinamide-O-glucuronide (4-HPROG) on established DMBA induced rat mammary tumors were compared. The results indicate that the glucuronide analog had a greater antitumor potency than equimolar concentration of the free retinoid. Tumor regression occurred in 75% of the rats fed 2 mmol/Kg diet of 4-HPROG. In a 6-week study, the maximum tolerated dietary dose (MTD) was found to be 3.5 mmol/Kg diet for 4-HPR and 5 mmol/Kg diet in the case of 4-HPROG. The higher potency and lower toxicity of the glucuronide suggests that this conjugate may have an in vivo chemotherapeutic advantage over the parent free retinoid.
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