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[摘要]
还原型苦参碱类生物碱(包括苦参碱、槐定碱、槐果碱、拉马宁碱、槐胺碱、13α-羟基苦参碱等)具有中枢抑制和神经保护作用。其作用机制可能与以下作用密切相关:苦参碱类生物碱激活大麻素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,产生中枢抑制作用;还可能通过抗氧化以及抑制把关受体-4/核因子-κB(TLR4/NF-κB)通路和激活蛋白激酶A/cAMP反应元件结合蛋白(PKA/CREB)通路,抑制炎性因子表达,改善神经组织的微炎症状态,进而产生神经保护作用。
[Key word]
[Abstract]
Reduced matrine-type alkaloids including matrine, sophoridine, sophocarpine, lehmannine, sophoramine, and 13α-hydroxymatrine, which have central suppression and neuroprotective effect. Their active mechanisms may be closely related to the following actions:activating cannabine receptor-2 and up-regulating the expression of N-type voltage-gated calcium channels, improving synthesis and release of inhibitory neurotransmitters, γ-aminobutyric acid (GABA), and glycine, down-regulating the expression of GABA transporter 1 (GAT-1), increasing the concentration of GABA in synaptic cleft, and up-regulating the expression of GABAA receptor, thus strengthening GABAergic nerve function to exert central suppression effect. Reduced matrine-type alkaloids product neuroprotection by anti-oxygenating, inhibiting TLR4/NF-κB pathway, and activating PKA/CREB pathway to down-regulate the expressions of inflammatory cytokines, improve micro-inflammatory state on neuronal tissue, and then have the neuroprotective effect.
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