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Dopamine transporter inhibitory and antiparkinsonian effect of common flowering quince extract.

机译:多花木瓜提取物对多巴胺转运蛋白的抑制和抗帕金森病作用。

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Common flowering quince (FQ) is the fruit of Chaenomeles speciosa (Sweet) Nakai. FQ-containing cocktails have been applied to the treatment of neuralgia, migraine, and depression in traditional Chinese medicine. The present study assessed whether FQ is effective in dopamine transporter (DAT) regulation and antiparkinsonism by utilizing in vitro and in vivo assays, respectively. FQ at concentrations of 1-1000 mug/ml concentration-dependently inhibited dopamine uptake by Chinese hamster ovary (CHO) cells stably expressing DAT (D8 cells) and by synaptosomes. FQ had a slight inhibitory action on norepinephrine uptake by CHO cells expressing the norepinephrine transporter and no inhibitory effect on gamma-aminobutyric acid (GABA) uptake by CHO cells expressing GABA transporter-1 or serotonin uptake by the serotonin transporter. A viability assay showed that FQ mitigated 1-methyl-4-phenylpyridinium-induced toxicity in D8 cells. Furthermore, in behavioral studies, FQ alleviated rotational behavior in 6-hydroxydopamine-treated rats and improved deficits in endurance performance in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-treated mice. Furthermore, immunohistochemistry revealed that FQ markedly reduced the loss of tyrosine hydroxylase-positive neurons in the substantia nigra in MPTP-treated mice. In summary, FQ is a selective, potent DAT inhibitor and has antiparkinsonian-like effects that are mediated possibly by DAT suppression. FQ has the potential to be further developed for Parkinson's disease treatment.
机译:常见的开花木瓜(FQ)是木瓜木瓜的果实。含FQ的鸡尾酒已被用于中药的神经痛,偏头痛和抑郁症的治疗。本研究分别通过体外和体内试验评估FQ是否对多巴胺转运蛋白(DAT)调节和抗帕金森病有效。 FQ浓度为1-1000杯/毫升时,浓度依赖性地抑制稳定表达DAT的中国仓鼠卵巢(CHO)细胞(D8细胞)和突触小体摄取多巴胺。 FQ对表达去甲肾上腺素转运蛋白的CHO细胞对去甲肾上腺素的吸收有轻微的抑制作用,对表达GABA转运蛋白-1的CHO细胞或5-羟色胺转运蛋白对5-羟色胺的吸收没有抑制作用。生存力分析表明FQ减轻了D8细胞中1-甲基-4-苯基吡啶鎓诱导的毒性。此外,在行为研究中,FQ减轻了6-羟基多巴胺治疗的大鼠的旋转行为,并改善了1-甲基-4-苯基-1,2,3,6-四氢吡啶(MPTP)治疗的小鼠的耐力表现缺陷。此外,免疫组织化学显示,FQ显着减少了MPTP处理的小鼠黑质中酪氨酸羟化酶阳性神经元的丢失。总之,FQ是一种选择性的,有效的DAT抑制剂,具有抗帕金森病样的作用,可能是由DAT抑制介导的。 FQ有可能进一步开发用于帕金森氏病的治疗。

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