College of Pharmacy, Ningxia Medical University, Yinchuan, 750004, China.
Department of Pharmacy, General Hospital of Ningxia Medical University, Yinchuan, 750004, China.
J Ethnopharmacol. 2022 Mar 1;285:114861. doi: 10.1016/j.jep.2021.114861. Epub 2021 Nov 23.
Cynanchum komarovii Al. Iljinski is a ethnomedicinal herb and this ethno-medicine is used mainly to treat arthritis, toothache, reducing phlegm, relieving cough. Total alkaloids of Cynanchum komarovii Al. Iljinski (TACKI) is the main active compound of Cynanchum komarovii Al. Iljinski. Previous investigations have revealed that TACKI can significantly inhibit rat foot swelling caused by carrageenan; it has a significant inhibitory effect on granulation tissue proliferation. Pharmacology study showed that Cynanchum komarovii Al. Iljinski has analgesia, anti-inflammatory, antibacterial, anti-tumor, relieving cough and relieving asthma. However, there is no any investigation on the mechanism of analgesia and anti-inflammation.
To clarify the analgesic effect and material basis of Cynanchum komarovii Al. Iljinski, determine the analgesic effect of TACKI, and provide experimental data support for its traditional application in the treatment of various pains.
TACKI were prepared by the traditional acid extraction and alkaline precipitation method, and TACKI was analyzed through classic animal models of acute antinociceptive animal models and chronic antinociceptive. Evaluation of analgesic effects, and preliminary discussion of the mechanism of its analgesic effects were performed in this work.
Acute toxicity experiments showed that the LD of TACKI mice was 2960.88 mg/kg, and symptoms of poisoning appeared. Patholog of liver and kidney studies have shown that TACKI reduces eosinophils and increases basophils in kidney glomeruli. In the study of analgesic effects, TACKI had analgesic activity through the PWL, formalin test, and acetic acid writhing test. In the chronic inflammatory antinociceptive study, the latency of the withdrawal reflex in the TACKI group was prolonged, and the mechanical withdrawal reflex threshold was significantly increased. The protein expression of NMDA, GFAP and Iba-1 in rat brain tissue can be reduced significantly byTACKI. Meanwhile, the content of TNF-α and IL-6 in rat brain tissue is reduced.
TACKI has a significant analgesic activities. It may be related to inhibiting the activation of astrocytes and reducing the content of inflammatory mediators.
白首乌是一种民族药物草，主要用于治疗关节炎、牙痛、化痰、止咳。白首乌总生物碱（TACKI）是白首乌的主要活性化合物。先前的研究表明，TACKI 可显著抑制角叉菜胶引起的大鼠足肿胀；它对肉芽组织增生有显著的抑制作用。药理学研究表明，白首乌具有镇痛、抗炎、抗菌、抗肿瘤、止咳平喘等作用。然而，关于其镇痛和抗炎机制还没有任何研究。
阐明白首乌的镇痛作用及物质基础，确定 TACKI 的镇痛作用，为其传统应用于治疗各种疼痛提供实验数据支持。
采用传统的酸提取碱沉淀法制备 TACKI，通过经典的急性镇痛动物模型和慢性镇痛动物模型评价 TACKI 的镇痛作用，并对其镇痛作用机制进行初步探讨。
急性毒性实验表明，TACKI 对小鼠的 LD 为 2960.88mg/kg，出现中毒症状。肝、肾组织病理学研究表明，TACKI 可减少肾肾小球中的嗜酸性粒细胞，增加嗜碱性粒细胞。在镇痛作用研究中，TACKI 通过 PWL、福尔马林试验和醋酸扭体试验表现出镇痛活性。在慢性炎症性镇痛研究中，TACKI 组的退缩反射潜伏期延长，机械退缩反射阈值明显升高。TACKI 可显著降低大鼠脑组织中 NMDA、GFAP 和 Iba-1 的蛋白表达。同时，大鼠脑组织中 TNF-α 和 IL-6 的含量降低。
TACKI 具有显著的镇痛活性。它可能与抑制星形胶质细胞的激活和降低炎症介质的含量有关。
