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从L.根部分离得到的五环三萜的肌肉松弛和退热作用

Muscle relaxant and antipyretic effects of pentacyclic triterpenes isolated from the roots of L.

作者信息

Khan Ajmal, Kashtoh Hamdy, Rauf Abdur, Halim Sobia Ahsan, Aleem Awan A, Bahadar Haji, Shareef Huma, Mabood Fazal, Khalid Asaad, Baek Kwang-Hyun, Al-Harrasi Ahmed

机构信息

Natural and Medical Sciences Research Center, University of Nizwa, P.O. Box 33, Birkat Al Mauz, Nizwa 616, Sultanate of Oman.

Department of Biotechnology, Yeungnam University, Gyeongsan 38541, Gyeongbuk, Republic of Korea.

出版信息

Heliyon. 2024 Apr 30;10(9):e30547. doi: 10.1016/j.heliyon.2024.e30547. eCollection 2024 May 15.

Abstract

The present article describes the muscle relaxant and antipyretic effects of pentacyclic triterpenes, oleanolic acid (), ursolic acid () and betulinic acid () isolated from roots of in animal models. The muscle relaxant effects of isolated pentacyclic triterpenes were determined by chimney and inclined plane tests. In the chimney test, pretreatment of pentacyclic triterpenes evoked significant dose dependent influence on muscle coordination. When administered intraperitoneally (i.p.) to mice at 10 mg/kg for 90 min, , , and exhibited muscle relaxant effects of 66.72 %, 60.21 %, and 50.77 %, respectively. Similarly, , and (at 10 mg/kg) illustrated 65.74 %, 59.84 % and 51.40 % muscle relaxant effects in the inclined plane test. In the antipyretic test, significant amelioration was caused by pretreatment of all compounds in dose dependent manner. , and (at 5 mg/kg) showed 39.32 %, 34.32 % and 29.99 % anti-hyperthermic effects, respectively 4 h post-treatment, while at 10 mg/kg, , and exhibited 71.59 %, 60.99 % and 52.44 % impact, respectively. The muscle relaxant effect of benzodiazepines is well known for enhancement of GABA receptors. There may exist a similar mechanism for muscle relaxant effect of pentacyclic triterpenes. The predicted binding pattern of all the compounds reflects good affinity of compounds with GABA receptor and COX-2. These results indicate that the muscle relaxant and antipyretic activities of these molecules can be further improved by structural optimization.

摘要

本文描述了从[植物名称]根部分离出的五环三萜类化合物齐墩果酸()、熊果酸()和桦木酸()在动物模型中的肌肉松弛和退热作用。通过烟囱试验和倾斜平面试验测定分离出的五环三萜类化合物的肌肉松弛作用。在烟囱试验中,五环三萜类化合物的预处理对肌肉协调性产生了显著的剂量依赖性影响。当以10mg/kg的剂量腹腔注射(i.p.)给小鼠90分钟时,[化合物名称1]、[化合物名称2]和[化合物名称3]分别表现出66.72%、60.21%和50.77%的肌肉松弛作用。同样,[化合物名称1]、[化合物名称2]和[化合物名称3](10mg/kg)在倾斜平面试验中分别表现出65.74%、59.84%和51.40%的肌肉松弛作用。在退热试验中,所有化合物的预处理均以剂量依赖性方式引起显著改善。[化合物名称1]、[化合物名称2]和[化合物名称3](5mg/kg)在治疗后4小时分别表现出39.32%、34.32%和29.99%的抗高热作用,而在10mg/kg时,[化合物名称1]、[化合物名称2]和[化合物名称3]分别表现出71.59%、60.99%和52.44%的作用。苯二氮䓬类药物的肌肉松弛作用因增强GABA受体而闻名。五环三萜类化合物的肌肉松弛作用可能存在类似机制。所有化合物预测的结合模式反映了化合物与GABA受体和COX-2具有良好的亲和力。这些结果表明,通过结构优化可以进一步提高这些分子的肌肉松弛和退热活性。

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