Study On Synthesis And Activity Of CHC Photodynamic Response Compounds

Photodynamic therapy is a new type of cancer treatment method.It has no systemic toxicity and can be safely reused.Compared with traditional surgical treatment and radiochemical therapy,it has fewer side effects and has good application prospects.PDT mainly uses light to activate photosensitizers to produce reactive oxygen species and stimulate the body to produce anti-tumor immunity to treat cancer.The design and synthesis of photosensitizers is the focus of the PDT field.The current main problems of the second-generation photosensitizers are poor water solubility,the absorption wavelength affects the shallow penetration depth,the easy degradation under light,and the prone to photosensitization reaction.Chlorin is a representative of the second-generation photosensitizer.It has a clear structure and a high level of singlet oxygen quantum yield,which is a hot spot of current research.In this paper,pheophorbide a was prepared by extracting Spirulina platensis from Chenghai Lake in Yunnan Province,and further degraded and opened the ring to obtain Chenghaiporin.The X-ray single crystal diffraction of Cu ligand proves that the compound has the the same structure of Chlorin e6 from foreign sources.Designed to increase the maximum absorption wavelength by extending the chlorin macrocyclic conjugated system,and introducing amino acid groups to improve water solubility and biological activity.Six target compounds were obtained,and their structures were characterized by methods such as ~1H NMR and MS.The discovery of cisplatin has prompted the wide application of metal coordination compounds in drug modification and photosensitizer design.By introducing Pd to the CHC macrocyclic center,in order to improve its physical and chemical properties and PDT activity,three CHC centers were obtained for Pd coordination.The derivative of position.The Pd was characterized by 1H NMR,MS,XPS and other methods,and the valence state of Pd was analyzed.Absorption spectra,fluorescence spectra,photostability,cell uptake,active oxygen yield,phototoxicity and dark toxicity were measured for the synthesized series of compounds,and their photophysical properties and PDT activity were evaluated in vitro.After Pd coordination is introduced into the ring center,the stability of the compound is improved and the compound exhibits a low level of dark toxicity.Hep G2 cell detection of the compound’s PDT anti-tumor activity found that 13-MMA Pd CHCDME has high phototoxicity and is a promising photosensitizer.