Dubertret L, Averbeck D, Zajdela F, Bisagni E, Moustacchi E, Touraine R, Latarjet R
Br J Dermatol. 1979 Oct;101(4):379-89. doi: 10.1111/j.1365-2133.1979.tb00015.x.
The carcinogenic risk of photochemotherapy (PUVA) with bi-functional furocoumarins such as 8-methoxypsoralen (8-MOP) which form cross-links in cellular DNA has initiated a search for active but less hazardous psoralens. A new compound, 3-carbethoxypsoralen (3-CPs), studied in the yeast Saccharomyces cerevisiae (eukaryote), has been shown to be very photoactive on DNA and to form only mono-additions to DNA. These lesions appear to be more easily repaired than the cross-links induced by 8-MOP. 3-CPs produces less nuclear genetic events such as nuclear mutations and mitotic crossovers, but more cytoplasmic 'petite' mutations (damage to mitochondrial DNA) than 8-MOP. In mice it was demonstrated that after local or intra-peritoneal administration, in contrast to 8-MOP, 3-CPs is non-toxic, non-erythematogenic, and non-carcinogenic. A study of ten psoriatic patients had shown that local applications of 3-CPs plus UV-A exhibit about the same therapeutic activity for the clearing of psoriatic lesions as local treatment with 8-MOP plus UV-A, but without any localized hyperpigmentation.
使用双功能补骨脂素（如8-甲氧基补骨脂素，8-MOP）进行光化学疗法（PUVA），因其会在细胞DNA中形成交联，具有致癌风险，这引发了人们对活性更高但危害较小的补骨脂素的探索。一种新化合物，3-乙氧羰基补骨脂素（3-CPs），在酿酒酵母（真核生物）中进行了研究，结果表明它对DNA具有很强的光活性，并且仅与DNA形成单加成。这些损伤似乎比8-MOP诱导的交联更容易修复。与8-MOP相比，3-CPs产生的核遗传事件（如核突变和有丝分裂交换）较少，但产生的细胞质“小菌落”突变（线粒体DNA损伤）更多。在小鼠中已证明，与8-MOP相比，局部或腹腔给药后，3-CPs无毒、无红斑形成且无致癌性。对10名银屑病患者的研究表明，局部应用3-CPs加紫外线A清除银屑病皮损的治疗活性与局部应用8-MOP加紫外线A相当，但不会出现任何局部色素沉着。
