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12 - O - 十四烷酰佛波醇 - 13 - 乙酸酯和芫花酯素对表皮鸟氨酸脱羧酶活性、异丙肾上腺素刺激的环磷酸腺苷水平以及体内小鼠皮肤肿瘤诱导的影响。

Effects of 12-O-tetradecanoylphorbol-13-acetate and mezerein on epidermal ornithine decarboxylase activity, isoproterenol-stimulated levels of cyclic adenosine 3':5'-monophosphate, and induction of mouse skin tumors in vivo.

作者信息

Mufson R A, Fischer S M, Verma A K, Gleason G L, Slaga T J, Boutwell R K

出版信息

Cancer Res. 1979 Dec;39(12):4791-5.

PMID:227591
Abstract

The tumor promoter 12-O-tetradecanoylphorbol-13-acetate and the antileukemic agent mezerein are diterpene esters of plant origin with certain structural similarities. Both compounds, when applied topically to mouse skin, were equipotent on a molar basis in inducing hyperplasia, inflammation, and ornithine decarboxylase activity, as well as in reducing cyclic adenosine 3':5'-monophosphate accumulation in response to beta-adrenergic stimulation. In contrast, mezerein was much less effective as a tumor promoter; the phorbol ester at 8.5 nmol/application yielded 78-fold more tumors than did 8.5 nmol mezerein per application to similarly initiated SENCAR mice. The superiority of the phorbol ester was nearly as great in CD-1 mice.

摘要

肿瘤促进剂12 - O - 十四烷酰佛波醇 - 13 - 乙酸酯和抗白血病药物狼毒素是具有一定结构相似性的植物源二萜酯。当将这两种化合物局部应用于小鼠皮肤时,在诱导增生、炎症和鸟氨酸脱羧酶活性方面,以及在减少β - 肾上腺素能刺激后环磷酸腺苷3':5'-单磷酸的积累方面,按摩尔计算它们的效力相当。相比之下,狼毒素作为肿瘤促进剂的效果要差得多;在对同样起始的SENCAR小鼠每次应用8.5 nmol佛波酯时产生的肿瘤数量比每次应用8.5 nmol狼毒素时多78倍。佛波酯在CD - 1小鼠中的优势也几乎同样显著。

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