The muscarinic receptor family expressed in smooth muscle throughout the body is thought to be composed of five subtypes coupling to distinct signaling systems,respectively.The population in smooth muscle is composed ...The muscarinic receptor family expressed in smooth muscle throughout the body is thought to be composed of five subtypes coupling to distinct signaling systems,respectively.The population in smooth muscle is composed of mainly M 2 and M 3 subtypes in a 80% to 20% mixture. The muscarinic receptor, mainly M 3 receptor, play an important role in regulating gastrointestinal smooth muscle contraction. Selective muscarinic M 3 antagonist should have therapeutic utility in the treatment of gastrointestinal disease.展开更多
目的:吴茱萸碱是中药吴茱萸重要生物碱成分之一,其具有明显的抗炎作用,但具体机制不清。研究显示瞬时受体电位香草醛亚型1受体(Transient Receptor Potential Vanilloid Type 1 Channel,TRPV1)对炎症反应具有明显的抑制作用,而吴茱萸碱...目的:吴茱萸碱是中药吴茱萸重要生物碱成分之一,其具有明显的抗炎作用,但具体机制不清。研究显示瞬时受体电位香草醛亚型1受体(Transient Receptor Potential Vanilloid Type 1 Channel,TRPV1)对炎症反应具有明显的抑制作用,而吴茱萸碱可激活TRPV1受体。本研究以人单核细胞(THP-1)培养模型,探明吴茱萸碱对M2型巨噬细胞功能的影响及TRPV1受体参与该过程中的作用,从而阐明吴茱萸碱抑制炎症反应的分子生物机制。方法:在THP-1细胞培养模型上,观察吴茱萸碱对白介素-4(Interleukin-4,IL-4)诱导的M2型巨噬细胞功能的影响,以及特异性TRPV1受体拮抗剂Capsazepine(CAPZ)对该过程的影响,并分别利用ELISA、荧光定量PCR和western blot确定M2型巨噬细胞功能指标,其中包括TGF-β1的产生、Arginase-1和Mannose Receptor m RNA和蛋白的表达。结果:本研究发现吴茱萸碱明显抑制IL-4诱导的M2型巨噬细胞功能亚型,其主要表现为TGF-β1分泌产生下降(P<0.05),同时伴有Arginase-1和Mannose Receptor m RNA和蛋白表达的降低(P<0.05),以上结果可被特异性TRPV1受体拮抗剂CAPZ所阻断(P<0.05)。结论:本研究显示吴茱萸碱通过激活TRPV1受体抑制M2型巨噬细胞功能反应,从而实现其抑制炎症反应的作用。展开更多
The cycle of G-protein activation and deactivation is a key in the signaling pathway of GPCRs (G protein coupled receptors). GTPase-activating proteins (GAPs) regulate heterotrimeric G proteins by increasing the rates...The cycle of G-protein activation and deactivation is a key in the signaling pathway of GPCRs (G protein coupled receptors). GTPase-activating proteins (GAPs) regulate heterotrimeric G proteins by increasing the rates at which the (subunits hydrolyze bound GTP to GDP. RGSs (regulators of G protein signaling) is a novel family and, in most cases, implicated in accelerating the hydrolysis of GTP. The opioid receptors are all seven serpentine transmembrane receptors coupled with G proteins Gi, Go, even Gs. Adenylate cyclase (AC) is展开更多
文摘The muscarinic receptor family expressed in smooth muscle throughout the body is thought to be composed of five subtypes coupling to distinct signaling systems,respectively.The population in smooth muscle is composed of mainly M 2 and M 3 subtypes in a 80% to 20% mixture. The muscarinic receptor, mainly M 3 receptor, play an important role in regulating gastrointestinal smooth muscle contraction. Selective muscarinic M 3 antagonist should have therapeutic utility in the treatment of gastrointestinal disease.
文摘目的:吴茱萸碱是中药吴茱萸重要生物碱成分之一,其具有明显的抗炎作用,但具体机制不清。研究显示瞬时受体电位香草醛亚型1受体(Transient Receptor Potential Vanilloid Type 1 Channel,TRPV1)对炎症反应具有明显的抑制作用,而吴茱萸碱可激活TRPV1受体。本研究以人单核细胞(THP-1)培养模型,探明吴茱萸碱对M2型巨噬细胞功能的影响及TRPV1受体参与该过程中的作用,从而阐明吴茱萸碱抑制炎症反应的分子生物机制。方法:在THP-1细胞培养模型上,观察吴茱萸碱对白介素-4(Interleukin-4,IL-4)诱导的M2型巨噬细胞功能的影响,以及特异性TRPV1受体拮抗剂Capsazepine(CAPZ)对该过程的影响,并分别利用ELISA、荧光定量PCR和western blot确定M2型巨噬细胞功能指标,其中包括TGF-β1的产生、Arginase-1和Mannose Receptor m RNA和蛋白的表达。结果:本研究发现吴茱萸碱明显抑制IL-4诱导的M2型巨噬细胞功能亚型,其主要表现为TGF-β1分泌产生下降(P<0.05),同时伴有Arginase-1和Mannose Receptor m RNA和蛋白表达的降低(P<0.05),以上结果可被特异性TRPV1受体拮抗剂CAPZ所阻断(P<0.05)。结论:本研究显示吴茱萸碱通过激活TRPV1受体抑制M2型巨噬细胞功能反应,从而实现其抑制炎症反应的作用。
文摘The cycle of G-protein activation and deactivation is a key in the signaling pathway of GPCRs (G protein coupled receptors). GTPase-activating proteins (GAPs) regulate heterotrimeric G proteins by increasing the rates at which the (subunits hydrolyze bound GTP to GDP. RGSs (regulators of G protein signaling) is a novel family and, in most cases, implicated in accelerating the hydrolysis of GTP. The opioid receptors are all seven serpentine transmembrane receptors coupled with G proteins Gi, Go, even Gs. Adenylate cyclase (AC) is
