The Study On Synthesis, Photocleavege And Biological Activities Of Light-Triggered Porphyrin Anticancer Prodrug

The anticancer drugs used by now mostly have the disadvantage that they can not be directionally transported to the cancer cells. They kill the cancer cells at the same time damnify the normal cells severely. Therefore, it is an important issue in medicine and pharmaceutics to develop new anticancer prodrugs which are more active and specific in killing cancer cells.1. Originality and innovationBy now, there is no porphyrin anticancer prodrug that can release the parent drug. In addition, although the light has been widely used in the prodrug design, there is no porphyrin carrier that can be transported selectively to cancer site in these prodrugs. In this work, according to the prodrug principle, we designed a new anticancer prodrug system which use porphyrin as the carrier and release the parent drug by UV light.This system is composed of three parts: porphyrin carrier, photoliable protecting groups, and the parent drug. For the sake of proving this concept quickly and availably, we designed and synthesized the anticancer prodrug model a. For studying the toxic origin and the anticancer mechanism of prodrug model a, we designed the control b, which was synthesized by linking the porphyrin and the nontoxic uracil.2. Research content(1) We have synthesized and characterized the porphyrin anticancer prodrug model a and its control b;(2) We have analyzed the photolytic product and rate of the anticancer prodrug model a. In addition, we have determined its value of photochemical quantum yield;(3) We have studied the biological activities of porphyrin anticancer prodrug model a.3. Research significanceThis porphyrin anticancer prodrug model a has the twofold orientation. On one hand, it is been selectively transported to the cancer sites. On the other hand, it can be released specially by 350 nm UV light. This porphyrin anticancer prodrug could improve the drugs'target and reduce its side effects. Therefore, the porphyrin anticancer prodrug system has a widely applicable prospect.