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Novel Amphibian Bowman-Birk-Like Inhibitor with Antioxidant and Anticoagulant Effects Ameliorates Pancreatitis Symptoms in Mice.
Chai, Jinwei; Wu, Jiena; Li, Jinqiao; Liao, Hang; Lu, Wancheng; Guo, Ruiyin; Shao, Zuoyan; Jmel, Mohamed Amine; Martins, Larissa Almeida; Hackeng, Tilman; Ippel, Hans; Dijkgraaf, Ingrid; Kotsyfakis, Michail; Xu, Xueqing.
Afiliación
  • Chai J; Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, China.
  • Wu J; Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, China.
  • Li J; Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, China.
  • Liao H; Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, China.
  • Lu W; Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, China.
  • Guo R; Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, China.
  • Shao Z; Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, China.
  • Jmel MA; Institute of Parasitology, Biology Center of the Czech Academy of Sciences, Branisovska 31, Budweis (Ceske Budejovice) 37005, Czech Republic.
  • Martins LA; Institute of Parasitology, Biology Center of the Czech Academy of Sciences, Branisovska 31, Budweis (Ceske Budejovice) 37005, Czech Republic.
  • Hackeng T; Department of Biochemistry, Cardiovascular Research Institute Maastricht (CARIM), Maastricht University, 6229 ER Maastricht, The Netherlands.
  • Ippel H; Department of Biochemistry, Cardiovascular Research Institute Maastricht (CARIM), Maastricht University, 6229 ER Maastricht, The Netherlands.
  • Dijkgraaf I; Department of Biochemistry, Cardiovascular Research Institute Maastricht (CARIM), Maastricht University, 6229 ER Maastricht, The Netherlands.
  • Kotsyfakis M; Institute of Parasitology, Biology Center of the Czech Academy of Sciences, Branisovska 31, Budweis (Ceske Budejovice) 37005, Czech Republic.
  • Xu X; Institute of Molecular Biology and Biotechnology, Foundation for Research and Technology-Hellas, N. Plastira 100, 70013 Heracklion, Crete, Greece.
J Med Chem ; 66(17): 11869-11880, 2023 09 14.
Article en En | MEDLINE | ID: mdl-37610210
Acute pancreatitis (AP) is a serious inflammatory disorder and still lacks effective therapy globally. In this study, a novel Ranacyclin peptide, Ranacin, was identified from the skin of Pelophylax nigromaculatus frog. Ranacin adopted a compact ß-hairpin conformation with a disulfide bond (Cys5-Cys15). Ranacin was also demonstrated effectively to inhibit trypsin and have anticoagulant and antioxidant activities in vitro. Furthermore, the severity of pancreatitis was significantly alleviated in l-Arg-induced AP mice after treatment with Ranacin. In addition, structure-activity studies of Ranacin analogues confirmed that the sequences outside the trypsin inhibitory loop (TIL), especially at the C-terminal side, might be closely associated with the efficacy of its trypsin inhibitory activity. In conclusion, our data suggest that Ranacin can improve pancreatic injury in mice with severe AP through its multi-activity. Therefore, Ranacin is considered a potential drug candidate in AP therapy.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pancreatitis Tipo de estudio: Diagnostic_studies Límite: Animals Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2023 Tipo del documento: Article País de afiliación: China Pais de publicación: Estados Unidos
Texto completo
Añadir a Mi BVS
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pancreatitis Tipo de estudio: Diagnostic_studies Límite: Animals Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2023 Tipo del documento: Article País de afiliación: China Pais de publicación: Estados Unidos