氧化槐定碱和氧化槐果碱的中枢抑制和神经保护作用  

Research advance on Central Suppression and Neuroprotection of Oxysophoridine and Oxysophocarpine

作　　者：张明发[1] 沈雅琴[1] ZHANG Ming-fa;SHEN Ya-qin Shanghai Me(you Pharmaceutical Co.,Ltd,Shanghai 201204 China)

机构地区：[1]上海美优制药有限公司,上海201204

出　　处：《抗感染药学》2018年第9期1473-1476,共4页Anti-infection Pharmacy

摘　　要：氧化槐定碱和氧化槐果碱具有中枢抑制和神经保护作用,其作用机制可能具有氧化苦参碱激活大麻素2型受体和上调电压门控钙离子N型通道表达,促进抑制性神经递质(γ-氨基丁酸、甘氨酸)合成和释放,下调γ-氨基丁酸转运体-1表达,使突触间隙γ-氨基丁酸浓度升高以及上调γ-氨基丁酸-A受体表达,从而增强γ-氨基丁酸能神经功能。γ-氨基丁酸能神经功能的增强可抑制兴奋性神经递质谷氨酸过度表达并下调天冬氨酸(NMDA)受体和蛋白激酶C-γ表达,使NMDA受体磷酸化减弱,降低NMDA受体对谷氨酸的兴奋性,从而下调电压门控钙离子L型通道的表达,抑制钙离子内流,阻滞钙/钙调素依赖性蛋白激酶Ⅱ/cAMP反应元件结合蛋白(CaMKⅡ/CREB)通路,抑制炎症反应,产生中枢抑制和神经保护作用。综述氧化槐定碱和氧化槐果碱的中枢抑制和神经保护作用文献,并对其研究进展做了分析。Oxysophoridine and oxysophocarpine have central suppression and neuroprotective effect. The active mechanisnl of oxysophoridine and oxysophocarpine is to activate cannabine receptor-2 and up-regulate the expression of N-type voltage-gated calcium channels, improving synthesis and release of inhibitory neurotransmitters, γ-aminobu- tyric acid （GABA） and glycine, down-regulating the expression of GABA transporter 1 （GAT-1）, increasing the con- centration of GABA in synaptic cleft, and up-regulating the expression of GABAA receptor, thus strengthening GAP,- Acrgic nerve function. Enhancement of GBABergic nerve function can inhibit the expression of excitatory neurotrans- mitter, glutamic acid, N-methyI-D-aspartate （NMDA） receptor, and protein kinase C-γ, to decrease the excitation of NMDA recepto,＂ to glutamate, thus down-regulating the expression.of L-type voltage-gated calcium channels, and in- hibiting Ca^2＋ influent, as well as blocking CaMK Ⅱ/CREB pathway to inhibit inflammation and product central suppres- sion and neuroprotection. The literatures of the central inhibition and neuroprotection of sophoridine and sophoridine were reviewed and their research progresses were analyzed.

关 键 词：氧化槐定碱 氧化槐果碱 中枢抑制 神经保护 作用机制 

分 类 号：R286.6[医药卫生—中药学]