Department of Pharmacology and Shanghai Key Laboratory of Bioactive Small Molecules, School of Basic Medical Sciences, State Key Laboratory of Medical Neurobiology, Institutes of Brain Science and Collaborative Innovation Center for Brain Science, Fudan University, Shanghai, China.
Key Laboratory of Medicinal Chemistry for Natural Resource (Yunnan University), Ministry of Education, Kunming, China.
J Sleep Res. 2017 Jun;26(3):386-393. doi: 10.1111/jsr.12518. Epub 2017 Mar 20.
Natural helicid (4-formylphenyl-O-β-d-allopyranoside), a main active constituent from seeds of the Chinese herb Helicia nilagirica, has been reported to exert a sedative, analgesic and hypnotic effect, and is used clinically to treat neurasthenic syndrome, vascular headaches and trigeminal neuralgia. In the current study, mechanical allodynia tests, electroencephalograms, electromyogram recordings and c-Fos expression in neuropathic pain-like model mice of partial sciatic nerve ligation were used to investigate the effect of helicid on neuropathic pain and co-morbid insomnia. Our results showed that helicid at a dose of 100, 200 or 400 mg kg could increase the mechanical threshold by 2.5-, 2.8- and 3.1-fold for 3 h after administration, respectively. Helicid at 200 and 400 mg kg given at 07:00 hours increased the amount of non-rapid eye movement sleep in a 3-h period by 1.27- and 1.35-fold in partial sciatic nerve ligated mice. However, helicid (400 mg kg ) given at 21:00 hours did not change the sleep pattern in normal mice. Immunohistochemical study showed that helicid (400 mg kg ) administration could reverse the increase of c-Fos expression in the neurons of the rostral anterior cingulate cortex and tuberomammillary nucleus, and the decrease of c-Fos expression in the ventrolateral preoptic area caused by partial sciatic nerve ligation. These results indicate that helicid is an effective agent for both neuropathic pain and sleep disturbances in partial sciatic nerve ligated mice.
天然 Helicid（4-甲酰基苯基-O-β-D-吡喃半乳糖苷）是中国草药 Helicia nilagirica 种子中的主要活性成分之一，具有镇静、镇痛和催眠作用，临床上用于治疗神经衰弱、血管性头痛和三叉神经痛。在本研究中，采用机械性痛觉过敏试验、脑电图、肌电图记录和 c-Fos 表达检测，研究 Helicid 对坐骨神经部分结扎模型小鼠神经病理性疼痛及其合并失眠的作用。结果表明，Helicid 在 100、200 和 400 mg·kg -1 剂量下，给药 3 h 后可分别使机械痛阈提高 2.5、2.8 和 3.1 倍。Helicid 在 200 和 400 mg·kg -1 剂量下，于 07:00 给药可使坐骨神经部分结扎小鼠 3 h 内非快速眼动睡眠时间分别增加 1.27 倍和 1.35 倍。然而，Helicid（400 mg·kg -1 ）于 21:00 给药并不改变正常小鼠的睡眠模式。免疫组化研究表明，Helicid（400 mg·kg -1 ）给药可逆转坐骨神经部分结扎引起的前扣带回皮质和结节乳头体神经元中 c-Fos 表达增加，以及腹外侧视前区 c-Fos 表达减少。这些结果表明，Helicid 是治疗坐骨神经部分结扎小鼠神经病理性疼痛和睡眠障碍的有效药物。
