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[Discovery of exogenous ligands for orphan receptor BRS-3 from Chinese herbs].
Qiu, Xin; Wu, Le-Hao; Yu, Yang; Jin, Yu; Wang, Ji-Xia; Wang, Chao-Ran; Zhang, Yan.
Afiliación
  • Qiu X; School of Pharmacy, Shanghai Jiao Tong University Shanghai 200240, China.
  • Wu LH; School of Pharmacy, Shanghai Jiao Tong University Shanghai 200240, China.
  • Yu Y; School of Pharmacy, Shanghai Jiao Tong University Shanghai 200240, China.
  • Jin Y; School of Pharmacy, East China University of Science and Technology Shanghai 200237, China.
  • Wang JX; Dalian Institute of Chemical Physics, Chinese Academy of Sciences Dalian 116023, China DICP-CMC Innovation Institute of Medicine Taizhou 225300, China.
  • Wang CR; Dalian Institute of Chemical Physics, Chinese Academy of Sciences Dalian 116023, China DICP-CMC Innovation Institute of Medicine Taizhou 225300, China.
  • Zhang Y; School of Pharmacy, Shanghai Jiao Tong University Shanghai 200240, China.
Zhongguo Zhong Yao Za Zhi ; 47(6): 1595-1602, 2022 Mar.
Article en Zh | MEDLINE | ID: mdl-35347958
Bombesin receptor subtype-3(BRS-3) is an orphan receptor in the bombesin receptor family. Its signal transduction mechanism and biological function have attracted much attention. Seeking the ligand for BRS-3 is of great significance for exploring its function. Considering the fact that the activation of BRS-3 receptor can induce the change in intracellular Ca~(2+) concentration, the fluo-rometric imaging plate reader(FLIPR) was utilized for ligand screening at the cellular level. Among more than 400 monomeric compounds isolated from Chinese herbs, yuanhunine from Corydalis Rhizoma and sophoraisoflavanone A and licoriphenone from Glycyrrhizae Radix et Rhizoma antagonized BRS-3 to varying degrees. It was confirmed in HEK293 cells expressing BRS-3 that yuanhunine, sophoraisoflavanone A, and licoriphenone inhibited the calcium current response after the activation of BRS-3 by [D-Phe~6,ß-Ala~(11),Phe~(13),Nle~(14)]bombesin-(6-14) in a dose-dependent manner with the IC_(50) values being 8.58, 4.10, and 2.04 µmol·L~(-1), respectively. Further study indicated that yuanhunine and sophoraisoflavanone A exhibited good selectivity for BRS-3. In this study, it was found for the first time that monomers derived from Chinese herbs had antagonistic activity against orphan receptor BRS-3, which has provided a tool for further study of BRS-3 and also the potential lead compounds for new drug discovery. At the same time, it provides reference for the research and development of innovative drugs based on the active ingredients of Chinese herbs.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Medicamentos Herbarios Chinos / Receptores de Bombesina Límite: Humans Idioma: Zh Revista: Zhongguo Zhong Yao Za Zhi Asunto de la revista: FARMACOLOGIA / TERAPIAS COMPLEMENTARES Año: 2022 Tipo del documento: Article País de afiliación: China Pais de publicación: China
Texto completo
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Imprimir
XML
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Medicamentos Herbarios Chinos / Receptores de Bombesina Límite: Humans Idioma: Zh Revista: Zhongguo Zhong Yao Za Zhi Asunto de la revista: FARMACOLOGIA / TERAPIAS COMPLEMENTARES Año: 2022 Tipo del documento: Article País de afiliación: China Pais de publicación: China