title: Synthesis of pheophorbide-a conjugates with anticancer drugs as potential cancer diagnostic and therapeutic agents.
abstract: Pheophorbide-a, a chlorine based photosensitizer known to be selectively accumulated in cancer cells, was conjugated with anticancer drugs, doxorubicin and paclitaxel in the purpose of selective cancer diagnosis and therapy. Pheophorbide-a was conjugated with anticancer drugs via directly and by the use of selective cleavage linkers in cancer cell. The fluorescence of pheophorbide-a and doxorubicin conjugate by excitation at 420 or 440 nm was greatly diminished possibly by the energy transfer mechanism between two fluorescent groups. However, upon treatment in cancer cells, the conjugate showed to be cleaved to restore each fluorescence of pheophorbide-a and doxorubicin after 48 h of incubation. Also, pheophorbide-a conjugates either with doxorubicin and paclitaxel inhibited the growth of various cancer cells more potently than pheophorbide-a, which displayed very weak inhibitory activity. The results indicated that the pheophorbide-a conjugates with anticancer drugs could be utilized for selective cancer therapy as well as for the fluorescence detection of cancer.
authors.affiliation: Graduate-Program of Medical System Engineering, Gwangju Institute of Science and Technology, Gwangju, Republic of Korea.
authors.forename: Hyun
authors.initials: H
authors.lastname: You
authors.forename: Hyo-Eun
authors.initials: HE
authors.lastname: Yoon
authors.forename: Jung-Hoon
authors.initials: JH
authors.lastname: Yoon
authors.forename: Hyojin
authors.initials: H
authors.lastname: Ko
authors.forename: Yong-Chul
authors.initials: YC
authors.lastname: Kim
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D002734:Chlorophyll / Q000031:analogs & derivatives* / Q000737:chemistry; D004305:Dose-Response Relationship, Drug; D004317:Doxorubicin / Q000737:chemistry / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D005453:Fluorescence; D005456:Fluorescent Dyes / Q000737:chemistry; D006367:HeLa Cells; D006801:Humans; D051379:Mice; D008809:Mice, Inbred C3H; D018613:Microscopy, Confocal; D008968:Molecular Conformation; D009369:Neoplasms / Q000175:diagnosis / Q000188:drug therapy*; D017239:Paclitaxel / Q000737:chemistry / Q000494:pharmacology*; D013050:Spectrometry, Fluorescence; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014018:Tissue Distribution; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D005456:Fluorescent Dyes; D002734:Chlorophyll; D004317:Doxorubicin; C032623:pheophorbide a; D017239:Paclitaxel