Mou Ning, Duan Zhiguang, Ma Pei, Fu Rongzhan, Fan Daidi
Shaanxi Key Laboratory of Degradable Biomedical Materials, School of Chemical Engineering, Northwest University Taibai North Road 229 Xi'an 710069 China.
Shaanxi R&D Center of Biomaterials and Fermentation Engineering, School of Chemical Engineering, Northwest University Xi'an 710069 China.
RSC Adv. 2019 Jul 1;9(35):20483-20491. doi: 10.1039/c9ra01549c. eCollection 2019 Jun 25.
Ginsenosides, as major active components of ginseng, possess various pharmacological activities, including anti-tumor, anti-diabetic and hypotensive effects. However, the sedative and hypnotic effect of ginsenosides and the involved mechanism remain unclear. In the present study, the hypnotic effect of rare protopanaxadiol-type (PD) ginsenosides, consisting of Rg3, Rk1, Rg5, and protopanaxatriol-type (PT) ginsenosides, consisting of Rh1, Rk3, Rh4, was investigated and compared in rodent models through behavioral pharmacology methods. Both rare PD and PT ginsenosides decreased spontaneous locomotion activity in normal mice and reduced sleep latency, and extended sleep duration in pentobarbital-treated mice. Moreover, PD and PT ginsenosides attenuated the insomnia induced by caffeine in mice. These hypnotic effects of PD and PT ginsenosides were potentiated by 5-hydroxytryptophan (5-HTP), a precursor of serotonin, and inhibited by -chlorophenylalanine (PCPA), a 5-HT synthesis inhibitor. Flumazenil (FLU, a specific gamma aminobutyric acid (GABA) antagonist) also impaired the hypnotic effect of both PD and PT ginsenosides. The aforementioned results indicated that PD and PT ginsenosides exhibit sedative and hypnotic activity, and PT ginsenosides show higher activity than PD ginsenosides at high doses (96 mg kg). Furthermore, the bioactivity of these two types of ginsenosides might be mediated the serotonergic and GABAergic systems.
人参皂苷作为人参的主要活性成分，具有多种药理活性，包括抗肿瘤、抗糖尿病和降血压作用。然而，人参皂苷的镇静催眠作用及其作用机制尚不清楚。在本研究中，通过行为药理学方法在啮齿动物模型中研究并比较了由Rg3、Rk1、Rg5组成的稀有原人参二醇型（PD）人参皂苷和由Rh1、Rk3、Rh4组成的原人参三醇型（PT）人参皂苷的催眠作用。稀有PD和PT人参皂苷均降低正常小鼠的自发运动活性，缩短戊巴比妥处理小鼠的睡眠潜伏期并延长睡眠时间。此外，PD和PT人参皂苷减轻了咖啡因诱导的小鼠失眠。PD和PT人参皂苷的这些催眠作用被5-羟色氨酸（5-HTP，血清素的前体）增强，并被5-羟色氨酸合成抑制剂对氯苯丙氨酸（PCPA）抑制。氟马西尼（FLU，一种特异性γ-氨基丁酸（GABA）拮抗剂）也削弱了PD和PT人参皂苷的催眠作用。上述结果表明，PD和PT人参皂苷具有镇静催眠活性，并且PT人参皂苷在高剂量（96 mg/kg）时比PD人参皂苷表现出更高的活性。此外，这两种类型人参皂苷的生物活性可能由血清素能和GABA能系统介导。
