著者

紺野 勝弘 Picolo Gisele Gutierrez Vanessa Brigatte Patricia Zambelli Vanessa Camargo Antonio C.M. Cury Yara

出版者

天然有機化合物討論会

雑誌

天然有機化合物討論会講演要旨集

巻号頁・発行日

no.50, pp.409-413, 2008-09-01

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Snakebite accidents by the South American rattlesnake Crotalus durissus terrificus account for 10% of those occurred in Brazil. It induces severe neurological symptoms, but does not induce pain or severe tissue destruction at the site of inoculation, which is in contrast to the most other snakebites. Due to these properties, the crude venom of this snake used to be employed for controlling pain, for example, of cancer. Recent studies using the crude venom experimentally demonstrated that this venom shows antinociceptive effect more potent than morphine. This effect is orally active and long-lasting for 3-5 days, and despite mediated by opioid receptors, it dose not develop peripheral tolerance nor induce physical dependence unlike morphine. These remarkable properties prompted us to purify and chemically characterize the substance responsible for the analgesic effect. Bioassay-guided fractionation led to the isolation of a novel peptide, designated crotalphine, with a sequence of 14 amino acid residues having a single disulfide bond. We report herein the isolation, sequence determination and synthesis of crotalphine. Pharmacological evaluation using synthetic peptide will also be reported.