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二氢卟吩-卟啉酯对小鼠肿瘤在体内和体外的定位及光致敏作用

Localization and photosensitization of murine tumors in vivo and in vitro by a chlorin-porphyrin ester.

作者信息

Kessel D

出版信息

Cancer Res. 1986 May;46(5):2248-51.

PMID:3697968
Abstract

Preparation of the tumor-localizing preparation called hematoporphyrin derivative involves a two-step reaction wherein hematoporphyrin is acetylated and the reaction product subjected to alkaline hydrolysis. We have proposed that the tumor-localizing fraction of this product is composed of hematoporphyrin units joined by ester linkages. Using an analogous synthetic procedure, we prepared some new sensitizers in which hematoporphyrin is esterified to chlorins (reduced porphyrins). Because of the differences in absorption spectra, the porphyrin-chlorin esters are 5-fold more potent photosensitizers than are the porphyrin-porphyrin esters, with light of wavelength greater than 600 nm.

摘要

名为血卟啉衍生物的肿瘤定位制剂的制备涉及两步反应,其中血卟啉被乙酰化,反应产物进行碱性水解。我们已经提出,该产物的肿瘤定位部分由通过酯键连接的血卟啉单元组成。使用类似的合成方法,我们制备了一些新的敏化剂,其中血卟啉被酯化为二氢卟吩(还原卟啉)。由于吸收光谱的差异,在波长大于600 nm的光照射下,卟啉-二氢卟吩酯作为光敏剂的效力比卟啉-卟啉酯高5倍。

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