视黄基取代的苄基醚。视黄基3,4,5-三甲氧基苄基醚（RTMBE）对乳腺癌发生的抑制作用。

Retinyl substituted-benzyl ethers. Inhibition of mammary carcinogenesis by retinyl 3,4,5-trimethoxybenzyl ether (RTMBE).

作者信息

Shealy Y F, Frye J L, Hill D L, Sani B P, Rogers T S, Riordan J M, Krauth C A, Lin T H, Eto I, Grubbs C J

机构信息

Southern Research Institute, Birmingham, AL 35255, USA.

出版信息

Anticancer Drug Des. 1998 Apr;13(3):159-82.

PMID:9595031

Abstract

Recently, we reported that retinyl 2-propynyl ether (RPE) inhibits MNU-induced mammary cancer in rats and is less toxic than RME and retinyl acetate. The preparation and biological investigations of retinyl ethers have now been extended to retinyl substituted-benzyl ethers, some of which bind to cellular retinol-binding protein. In long-term (160-180 days) experiments, retinyl 3,4,5-trimethoxybenzyl ether (RTMBE) has been shown to be active against MNU-induced mammary cancer in Sprague-Dawley rats. In effectiveness, RTMBE is comparable, at least, to retinyl acetate; but, unlike retinyl acetate, RTMBE is comparatively non-toxic to rats and mice, is not converted enzymatically to retinol, and does not cause significant increases in retinyl palmitate concentrations in the liver. RTMBE reaches high concentrations in mammary tissue. Two of the four RTMBE congeners that were evaluated in 90 day studies were moderately effective in inhibiting mammary carcinogenesis.

摘要

最近，我们报道了视黄基2-丙炔基醚（RPE）可抑制N-甲基-N-亚硝基脲（MNU）诱导的大鼠乳腺癌，且其毒性低于视黄基甲酯（RME）和视黄基乙酸酯。视黄基醚的制备和生物学研究现已扩展到视黄基取代苄基醚，其中一些可与细胞视黄醇结合蛋白结合。在长期（160 - 180天）实验中，视黄基3,4,5-三甲氧基苄基醚（RTMBE）已被证明对MNU诱导的斯普拉格-道利大鼠乳腺癌具有活性。在有效性方面，RTMBE至少与视黄基乙酸酯相当；但是，与视黄基乙酸酯不同，RTMBE对大鼠和小鼠相对无毒，不会被酶转化为视黄醇，也不会导致肝脏中视黄基棕榈酸酯浓度显著增加。RTMBE在乳腺组织中达到高浓度。在90天研究中评估的四种RTMBE同系物中有两种在抑制乳腺癌发生方面具有中等效果。