Motion sickness (MS) is the visceral discomfort caused due to contradicting visual and vestibular inputs to the brain leading to nausea and vomiting. Sensory conflict theory which proves histamine elevations as the primary reason for MS provides a path for an effective pharmaco-therapy. We aimed to evaluate the anti-MS effect of hesperidin (HSP) by modulating histamine and histamine receptor H1 (HRH1) expression. The inhibitory effect of HSP on histamine release was studied in KU812 cells treated with 10 µM calcium ionophore. The in vivo anti-MS effect of HSP was evaluated in Balb/c mice. Thirty six mice were divided into six groups namely, normal control (NC, no rotation), hesperidin at 80 mg/kg body weight control (HSP80, no rotation), motion sickness (MS, rotation induced), dimenhydrinate (Standard drug) at 20 mg/kg body weight + rotation (STD + MS), hesperidin at 40 mg/kg body weight + rotation (HSP40 + MS) and hesperidin at 80 mg/kg body weight + rotation (HSP80 + MS). Hypothalamus and brainstem samples were analysed for histamine levels and HRH1 expression by RT-PCR, Western blot and immunohistochemistry analysis. Calcium ionophore treated KU812 cells significantly increased histamine release when compared to control cells. Pre-treatment with HSP inhibited histamine, HRH1 mRNA and protein expression. Histamine, HRH1 mRNA and protein expression in hypothalamus and brainstem samples of MS group increased significantly when compared to the NC group. Pre-treatment with HSP significantly reduced histamine, HRH1 mRNA and protein expression. Thus, indicating that HSP has a potent anti- MS effect by decreasing the elevated levels of histamine, HRH1 mRNA and protein expression in hypothalamus and brainstem regions.

中文翻译：

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橙皮苷通过调节组胺和组胺H1受体表达来减轻晕动病。

运动病（MS）是内脏不适，是由于视觉和前庭对大脑的输入相矛盾而导致恶心和呕吐。证明组胺升高是MS的主要原因的感觉冲突理论为有效的药物治疗提供了途径。我们旨在通过调节组胺和组胺受体H1（HRH1）的表达来评估橙皮苷（HSP）的抗MS作用。在用10 µM钙离子载体处理的KU812细胞中研究了HSP对组胺释放的抑制作用。在Balb / c小鼠中评估了HSP的体内抗MS作用。将36只小鼠分为六组，分别为正常对照组（NC，不旋转），橙皮苷浓度为80 mg / kg体重的对照组（HSP80，不旋转），晕车病（MS，旋转诱发），苯海拉明（标准药物）每次20 mg / kg体重+旋转（STD + MS），橙皮苷在40 mg / kg体重+旋转（HSP40 + MS）和橙皮苷在80 mg / kg体重+旋转（HSP80 + MS ）。通过RT-PCR，Western印迹和免疫组化分析分析下丘脑和脑干样品的组胺水平和HRH1表达。与对照细胞相比，钙离子载体处理的KU812细胞显着增加了组胺释放。用HSP预处理可抑制组胺，HRH1 mRNA和蛋白表达。与NC组相比，MS组下丘脑和脑干样品中的组胺，HRH1 mRNA和蛋白表达显着增加。用HSP预处理可显着降低组胺，HRH1 mRNA和蛋白质表达。从而，