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与 (景天科)龙舌兰属植物皂苷的镇静和催眠活性相关的靶点和潜在机制。

Targets and underlying mechanisms related to the sedative and hypnotic activities of saponins from L. (crassulaceae).

机构信息

College of Food and Bioengineering, South China University of Technology, Guangzhou 510640, China.

The Second Clinical College of Guangzhou University of Chinese Medicine, Guangzhou 510120, China.

出版信息

Food Funct. 2021 Nov 1;12(21):10589-10601. doi: 10.1039/d1fo01178b.

DOI:10.1039/d1fo01178b
PMID:34585202
Abstract

L. (Crassulaceae) are popularly used as a natural supplement for the treatment of insomnia and anxiety. Here, saponin extracts from were investigated for their roles on relieving sleeplessness. The levels of neurotransmitters, hormones, and inflammation cytokines in plasma, and the expression of 5-hydroxytryptamine (5-HT), γ-aminobutyric acid (GABA), prostaglandin D2 (PGD2), interleukin-1β (IL-1β) and interleukin-6 (IL-6) in the hypothalamus and hippocampus were detected using ELISA, RT-PCR, and western blotting. First, the butanol fraction extracted from was collected as the total saponins (HJT-I), then a saponin-rich fraction (HJT-II) was obtained after the further purification of HJT-I. The saponin contents of HJT-I and HJT-II were 28.92% and 65.69%, respectively. Second, behavioral tests were performed and showed that both HJT-I and HJT-II could effectively reduce the duration of immobility in the tail suspension test, and shorten sleep latency and prolong the sleep duration time in the sodium barbital-induced sleeping test, with HJT-II better than HJT-I. Third, ELLISA results showed that the concentrations of GABA, 5-HT, norepinephrine (NA), PGD2, and IL-1β in plasma were significantly increased after HJT-I and HJT-II administration, while IL-6 was decreased. HJT-I and HJT-II also exhibited differential modulation of the receptors of 5-HT, GABA, PGD2, and IL-1β expression. In hypothalamus, HJT-II was more powerful than HJT-I in regulation of the GABARα2, GABARα3, and glutamic acid decarboxylase (GAD) 65/67 expression, as well as 5-HT and IL-1β. As for DPR and PGD2, HJT-II was more effective in the hippocampus. The efficacy of HJT-I was better than HJT-II at stimulating GABARα2, GAD 65/67, 5-HT, and IL-1β expression in the hippocampus. In conclusion, the potential sedative and hypnotic effects of HJT-I and HJT-II may possibly be related to the serotonergic, GABAergic, and immune systems, while the underlying mechanism of HJT-I and HJT-II differed from each other.

摘要

(景天科)被广泛用作治疗失眠和焦虑的天然补充剂。在这里,研究了从景天中提取的皂苷提取物在缓解失眠方面的作用。通过 ELISA、RT-PCR 和 Western blot 检测血浆中神经递质、激素和炎症细胞因子的水平,以及下丘脑和海马中 5-羟色胺(5-HT)、γ-氨基丁酸(GABA)、前列腺素 D2(PGD2)、白细胞介素-1β(IL-1β)和白细胞介素-6(IL-6)的表达。首先,从 中提取的正丁醇部分被收集为总皂苷(HJT-I),然后通过进一步纯化 HJT-I 获得富含皂苷的部分(HJT-II)。HJT-I 和 HJT-II 的皂苷含量分别为 28.92%和 65.69%。其次,进行行为测试表明,HJT-I 和 HJT-II 均可有效减少悬尾试验中不动时间的持续时间,并缩短戊巴比妥钠诱导睡眠试验中的睡眠潜伏期并延长睡眠时间,其中 HJT-II 优于 HJT-I。第三,ELISA 结果表明,HJT-I 和 HJT-II 给药后血浆中 GABA、5-HT、去甲肾上腺素(NA)、PGD2 和 IL-1β的浓度显着增加,而 IL-6 降低。HJT-I 和 HJT-II 还表现出对 5-HT、GABA、PGD2 和 IL-1β表达的受体的差异调节。在下丘脑,HJT-II 对 GABARα2、GABARα3 和谷氨酸脱羧酶(GAD)65/67 表达以及 5-HT 和 IL-1β的调节作用强于 HJT-I。至于 DPR 和 PGD2,HJT-II 在海马中的效果更好。在海马中,HJT-I 刺激 GABARα2、GAD 65/67、5-HT 和 IL-1β表达的功效优于 HJT-II。总之,HJT-I 和 HJT-II 的潜在镇静和催眠作用可能与 5-羟色胺能、GABA 能和免疫系统有关,而 HJT-I 和 HJT-II 的潜在机制彼此不同。

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