[關(guān)鍵詞]
[摘要]
還原型苦參堿類生物堿(包括苦參堿、槐定堿、槐果堿、拉馬寧堿、槐胺堿、13α-羥基苦參堿等)具有中樞抑制和神經(jīng)保護作用。其作用機制可能與以下作用密切相關(guān):苦參堿類生物堿激活大麻素2型受體和上調(diào)電壓門控鈣離子N型通道表達,促進抑制性神經(jīng)遞質(zhì)(γ-氨基丁酸、甘氨酸)合成和釋放,下調(diào)γ-氨基丁酸轉(zhuǎn)運體-1表達,使突觸間隙γ-氨基丁酸濃度升高以及上調(diào)γ-氨基丁酸-A受體表達,從而增強γ-氨基丁酸能神經(jīng)功能,產(chǎn)生中樞抑制作用;還可能通過抗氧化以及抑制把關(guān)受體-4/核因子-κB(TLR4/NF-κB)通路和激活蛋白激酶A/cAMP反應(yīng)元件結(jié)合蛋白(PKA/CREB)通路,抑制炎性因子表達,改善神經(jīng)組織的微炎癥狀態(tài),進而產(chǎn)生神經(jīng)保護作用。
[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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[基金項目]