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从曼陀罗(天使的号角)果实中分离得到的羽扇豆醇型三萜(曼陀罗醇)的胃肠动力、肌肉松弛、解热及急性毒性筛选

Gastrointestinal Motility, Muscle Relaxation, Antipyretic and Acute Toxicity Screening of Amyrin Type Triterpenoid (Daturaolone) Isolated From Linnaeus (Angel's Trumpet) Fruits.

作者信息

Bawazeer Saud, Rauf Abdur, Bawazeer Sami

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Umm Al-Qura University, Makkah, Saudi Arabia.

Department of Chemistry, University of Swabi, Swabi, Pakistan.

出版信息

Front Pharmacol. 2020 Sep 25;11:544794. doi: 10.3389/fphar.2020.544794. eCollection 2020.

Abstract

Linn is used traditionally for the treatment of various diseases including relaxation of smooth muscles, relief of fever, as well as gastrointestinal disorder. This study deals with the bio-guided isolation of an active, amyrin-type triterpenoid, namely 3-oxo-6--hydroxy--amyrin (daturaolone; ), from the chloroform fraction of L. (Angel's trumpet) fruits and its gastrointestinal motility, antipyretic, and muscle relaxation effects in animal models. The chemical structure of daturaolone () was elucidated by NMR spectroscopy and crystallography techniques. The chloroform fraction and daturaolone () were assessed for the GIT motility test. Data exhibited in charcoal meal GI transit test show that chloroform fraction and daturaolone () significantly reduce GIT motility and increased intestinal transit time, comparable to the standard (atropine), a muscarinic receptor blocking agent. Muscle relaxant potency of the extract and daturaolone () was assessed in various animal paradigms. In the inclined plane screening test, it produced a significant (P < 0.05) muscle relaxation potential in a dose-dependent manner after 30, 60, and 90 min. Likewise, the muscle relaxation potential of the extract and daturaolone () was strongly complemented by the chimney and traction test, representing a dominant effect after 60 min of sample administration. The chloroform fraction showed good antipyretic activity, and while daturaolone () exhibited significant activity at a higher dose, the maximum effect (84.64%) was at 20 mg/kg i.p. In acute toxicity screening test, the chloroform extract (100, 250, 500, and 1,000 mg/kg) and daturaolone () (5, 10, 20, and 50 mg/kg) were found safe. In conclusion, the chloroform extract and daturaolone () exhibited strong gastrointestinal motility, muscle relaxation, and antipyretic activity in different animal models and intestinally, was found safe at higher tested doses.

摘要

传统上,曼陀罗用于治疗多种疾病,包括平滑肌松弛、退热以及胃肠道紊乱。本研究涉及从曼陀罗果实的氯仿提取物中进行生物导向分离一种活性的羽扇豆醇型三萜类化合物,即3-氧代-6-羟基-羽扇豆醇(洋金花醇酮),并在动物模型中研究其对胃肠道蠕动、解热和肌肉松弛的作用。通过核磁共振光谱和晶体学技术阐明了洋金花醇酮的化学结构。对氯仿提取物和洋金花醇酮进行了胃肠道蠕动测试评估。在炭末胃肠转运试验中显示的数据表明,氯仿提取物和洋金花醇酮显著降低胃肠道蠕动并延长肠道转运时间,与标准品(阿托品)相当,阿托品是一种毒蕈碱受体阻断剂。在各种动物模型中评估了提取物和洋金花醇酮的肌肉松弛效力。在斜面筛选试验中,在30、60和90分钟后,它以剂量依赖的方式产生了显著的(P < 0.05)肌肉松弛作用。同样,烟囱试验和牵引试验有力地补充了提取物和洋金花醇酮的肌肉松弛作用,表明在给药60分钟后有显著效果。氯仿提取物显示出良好的解热活性,虽然洋金花醇酮在较高剂量时表现出显著活性,但最大效果(84.64%)出现在腹腔注射20 mg/kg时。在急性毒性筛选试验中,发现氯仿提取物(100、250、500和1000 mg/kg)和洋金花醇酮(5、10、20和50 mg/kg)是安全的。总之,氯仿提取物和洋金花醇酮在不同动物模型中表现出强大的胃肠道蠕动、肌肉松弛和解热活性,并且在较高测试剂量下在肠道方面被发现是安全的。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f42d/7546419/080a8c37ac57/fphar-11-544794-g001.jpg

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