title: Antitumor activity evaluation of meso-tetra (pyrrolidine substituted) pentylporphin-mediated photodynamic therapy in vitro and in vivo.
abstract: Photodynamic therapy is a minimally invasive and promising new method in cancer treatment and has attracted considerable attention in recent years. An ideal photosensitizer is a crucial element to photodynamic therapy. In the present paper, a novel porphyrin derivative, 5, 10, 15, 20-tetrakis (5-(pyrrolidin-1-yl) pentyl) porphin (TPPP) was synthesized. Its spectroscopic and physicochemical properties, therapeutic efficacy as a photosensitizer in photodynamic therapy for human bladder cancer in vitro and in vivo were investigated. TPPP had strong absorption at 648nm (ε=1.75×10(4)M(-1)cm(-1)), and two fluorescence emission peaks at 652nm and 718nm. PDT with TPPP showed low dark toxicity and high phototoxicity to human bladder cancer T24 cells in vitro. In bearing T24 tumor nude mice, the growth of tumor was significantly inhibited by combining use of 5mg/kg TPPP with 100J/cm(2) (650nm, 180mW/cm(2)) laser irradiation at 3h following injection of TPPP. The antitumor effect was also confirmed with histopathological assay. The histopathological study results revealed that PDT using TPPP and 100J/cm(2) (650nm, 180mW/cm(2)) laser irradiation induced tumor cells shrunken and necrotic. These results indicate that TPPP is useful as a new photosensitizer in PDT for cancer, and deserves further investigation.
authors: Department of Pharmaceutical Science & Technology, College of Chemistry and Biology, Donghua University, Shanghai 201620, China.
authors: Li-Jun
authors: LJ
authors: Zhang
authors: Shanghai Eastern Hepatobiliary Surgery Hospital, Shanghai 200433, China.
authors: Xiang-Hua
authors: XH
authors: Zhang
authors: Department of Pharmaceutical Science & Technology, College of Chemistry and Biology, Donghua University, Shanghai 201620, China.
authors: Ping-Yong
authors: PY
authors: Liao
authors: Shanghai Eastern Hepatobiliary Surgery Hospital, Shanghai 200433, China.
authors: Jing-Jian
authors: JJ
authors: Sun
authors: Department of Pharmaceutical Science & Technology, College of Chemistry and Biology, Donghua University, Shanghai 201620, China.
authors: Li
authors: L
authors: Wang
authors: Department of Pharmaceutical Science & Technology, College of Chemistry and Biology, Donghua University, Shanghai 201620, China.
authors: Yi-Jia
authors: YJ
authors: Yan
authors: Department of Pharmaceutical Science & Technology, College of Chemistry and Biology, Donghua University, Shanghai 201620, China. Electronic address: zlchen1967@qq.com.
authors: Zhi-Long
authors: ZL
authors: Chen
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects / Q000528:radiation effects; D001692:Biological Transport / Q000187:drug effects / Q000528:radiation effects; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects / Q000528:radiation effects; D003624:Darkness; D006801:Humans; D042541:Intracellular Space / Q000378:metabolism; D008297:Male; D051379:Mice; D010778:Photochemotherapy; D017319:Photosensitizing Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D011166:Porphyrins / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D011759:Pyrrolidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D026082:Singlet Oxygen / Q000378:metabolism; D023041:Xenograft Model Antitumor Assays
chemical_list: C000615697:5,10,15,20-tetrakis(5-(pyrrolidin-1-yl)pentyl)porphin; D000970:Antineoplastic Agents; D017319:Photosensitizing Agents; D011166:Porphyrins; D011759:Pyrrolidines; D026082:Singlet Oxygen
keywords: Human bladder cancer; Photodynamic therapy; Photosensitizer; Porphyrin; TPPP; Tumor