title: Synthesis and antitumor activity evaluation of a novel porphyrin derivative for photodynamic therapy in vitro and in vivo.
abstract: A novel porphyrin derivative, 5, 10, 15, 20-tetrakis (5-morpholinopentyl)-21H, 23H-Porphin (MPP, 4) and its photophysical characteristics, therapeutic efficacy of photodynamic therapy (PDT) in vitro and in vivo, tumor selectivity, and clearance from normal tissues were investigated here. MPP has strong absorption at relatively long wavelength (λmax = 648 nm, molar absorption coefficient ε ∼ 17,200 M(-1)cm(-1)) and can emit strong fluorescence at 653 and 718 nm. When administered to the animal tumor models by tail vein injection, MPP was capable of accumulating in the tumor site, as examined in vivo with the fluorescence signal of MPP. By the combination of MPP and a 650-nm laser irradiation, the viability of T24 cells could decrease by 4.37 %, and inhibition rate of T24 tumor could increase up to 91.21 % compared with control group, demonstrating the potential of MPP as an effective photosensitizer in PDT for tumor treatment.
authors.affiliation: Department of Pharmaceutical Science & Technology, College of Chemistry and Biology, Donghua University, Shanghai, 201620, People's Republic of China.
authors.forename: Li-Jun
authors.initials: LJ
authors.lastname: Zhang
authors.affiliation: Ningbo Dongmi Pharmaceutical Co. Ltd, Ningbo, Zhejiang, 315800, China.
authors.forename: Yi-Jia
authors.initials: YJ
authors.lastname: Yan
authors.affiliation: Department of Pharmaceutical Science & Technology, College of Chemistry and Biology, Donghua University, Shanghai, 201620, People's Republic of China.
authors.forename: Ping-Yong
authors.initials: PY
authors.lastname: Liao
authors.affiliation: Division of organic chemistry and biochemistry, Rudjer Boskovic Institute, Zagreb, Croatia.
authors.forename: Davor
authors.initials: D
authors.lastname: Margetic
authors.affiliation: Department of Pharmaceutical Science & Technology, College of Chemistry and Biology, Donghua University, Shanghai, 201620, People's Republic of China.
authors.forename: Li
authors.initials: L
authors.lastname: Wang
authors.affiliation: Department of Pharmaceutical Science & Technology, College of Chemistry and Biology, Donghua University, Shanghai, 201620, People's Republic of China. zlchen1967@yahoo.com.
authors.forename: Zhi-Long
authors.initials: ZL
authors.lastname: Chen
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D006801:Humans; D008297:Male; D051379:Mice; D010778:Photochemotherapy; D011166:Porphyrins / Q000138:chemical synthesis* / Q000494:pharmacology*; D013057:Spectrum Analysis; D014018:Tissue Distribution; D047368:Tumor Burden / Q000187:drug effects; D023041:Xenograft Model Antitumor Assays
chemical_list: D000970:Antineoplastic Agents; D011166:Porphyrins
keywords: Antitumor; MPP; Photodynamic therapy; Photosensitizer; Porphyrin