Dubertret L, Averbeck D, Bisagni E
C R Seances Acad Sci D. 1979 Mar 19;288(11):975-7.
The carcinogenic risk of the photochemotherapy (PUVA) with bifunctional furocoumarins such as 8-methoxypsoralen (8-MOP) forming cross-links in cellular DNA has initiated a search for active but less dangerous psoralens. The 3-carbethoxypsoralen (3-CPs), studied in the yeast Saccharomyces cerevisiae, has been very photoactive on DNA forming only monoadditions to DNA. In Mice it was demonstrated that after local or intra-peritoneal administration, 3-CPs is non toxic, non erythematogenic and non carcinogenic in contrast to 8-MOP. A limited study on ten psoriatic patients has shown that after local application 3-CPs exhibits about the same therapeutic activity as 8-MOP.
使用双功能呋喃香豆素(如8-甲氧基补骨脂素,8-MOP)进行光化学疗法(PUVA)会在细胞DNA中形成交联,其致癌风险促使人们寻找活性高但危险性较低的补骨脂素。在酿酒酵母中进行研究的3-乙氧羰基补骨脂素(3-CPs)对DNA具有很高的光活性,仅在DNA上形成单加成。在小鼠中已证明,与8-MOP相比,局部或腹腔注射3-CPs无毒、无红斑形成作用且无致癌性。对10名银屑病患者进行的有限研究表明,局部应用后3-CPs表现出与8-MOP大致相同的治疗活性。