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特定补骨脂素在银屑病中的安全性和治疗效果

Safety and therapeutic effectiveness of selected psoralens in psoriasis.

作者信息

Wolff K, Hönigsmann H

出版信息

Natl Cancer Inst Monogr. 1984 Dec;66:159-64.

PMID:6531023
Abstract

This review summarizes the most important facts regarding the clinical effectiveness of oral photochemotherapy for psoriasis with UV radiation at 320-400 nm (UVA) and selected furocoumarins. The most widely used compound is 8-methoxypsoralen (8-MOP); its effectiveness has been documented by many clinical trials. Oral 5-methoxypsoralen (5-MOP) has been evaluated as an alternative drug because it is less erythemogenic and thus reduces the danger of accidental over-exposure. It has been as effective as 8-MOP in clearing psoriasis, but the UVA doses required were considerably higher. Although oral 4,5',8-trimethylpsoralen does not clear psoriasis satisfactorily, excellent treatment results have been recorded when it was applied topically. The 3 drugs produce bifunctional adducts with DNA (cross-links), which may be of particular importance for mutagenesis and tumor formation. In an attempt to reduce possible oncogenic hazards, investigators are currently testing non-crosslinking furocoumarins for their therapeutic effectiveness. At present, these compounds are available for topical use only. 3-Carbethoxypsoralen has been reported to produce excellent treatment results by others but was ineffective in our clinical trials. Similarly disappointing was the application of 4,5'-dimethylangelicin and 5-methylangelicin. Although monofunctional compounds also inhibit cell proliferation in vitro, it appears that cross-linking is a prerequisite for the therapeutic success in psoriasis. The actual important of cross-links, however, remains to be clarified.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

本综述总结了关于口服光化学疗法治疗银屑病的最重要事实,该疗法采用320 - 400纳米的紫外线辐射(UVA)及选定的补骨脂素。最广泛使用的化合物是8 - 甲氧基补骨脂素(8 - MOP);许多临床试验已证明其有效性。口服5 - 甲氧基补骨脂素(5 - MOP)已被评估为替代药物,因为它引起红斑的作用较小,从而降低了意外过度暴露的风险。它在清除银屑病方面与8 - MOP一样有效,但所需的UVA剂量要高得多。虽然口服4,5',8 - 三甲基补骨脂素不能令人满意地清除银屑病,但局部应用时记录到了优异的治疗效果。这三种药物与DNA产生双功能加合物(交联),这可能对诱变和肿瘤形成尤为重要。为了降低可能的致癌风险,研究人员目前正在测试非交联补骨脂素的治疗效果。目前,这些化合物仅可用于局部使用。其他研究人员报告称3 - 乙氧羰基补骨脂素产生了优异的治疗效果,但在我们的临床试验中无效。4,5' - 二甲基白芷素和5 - 甲基白芷素的应用同样令人失望。虽然单功能化合物在体外也能抑制细胞增殖,但似乎交联是银屑病治疗成功的先决条件。然而,交联的实际重要性仍有待阐明。(摘要截短于250字)

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