Department of Pharmacy, Banasthali Vidyapith, Banasthali, India.
Department of Chemistry, Banasthali Vidyapith, Banasthali, India.
Fundam Clin Pharmacol. 2023 Dec;37(6):1153-1169. doi: 10.1111/fcp.12927. Epub 2023 Jun 24.
Tylophora indica (Burm. f.) Merr is a climbing perennial plant reported in Indian traditional system of medicine for its use in allergy and asthma. However, only few scientific studies have been performed in the past to validate its antiasthmatic potential.
The present study deals with investigation of airway smooth muscle relaxant and antiasthmatic potential of extract and subsequent fractions prepared from T. indica.
The most active fraction of T. indica leaves selected through bio-guided activity was subjected to liquid chromatography-mass spectrometry (LC-MS) analysis for chemical profiling. The binding affinity of identified compounds in fraction towards M and H receptors was determined by molecular docking study. F-2 (chloroform fraction prepared from methanolic extract of T. indica leaves) was examined for its smooth muscle relaxant properties using isolated trachea of guinea-pig. Further, F-2 was evaluated through in vivo studies employing ovalbumin-induced asthma model in guinea-pigs.
F-2 was found most effective in bioassay-guided fractionation. Characterization by LC-MS analysis revealed presence of five major bioactive compounds in F-2 that showed good docking interactions with M and H receptors. The ex vivo study demonstrated that F-2 could significantly relax tracheal rings via targeting multiple signalling pathways videlicet, namely, noncompetitive antagonism of the histamine and muscarinic receptors, β2-adrenergic stimulation and activation of soluble guanylyl cyclase. In in vivo studies, F-2 ameliorated airway hyperresponsiveness and decreased broncho alveolar lavage fluid (BALF) levels of inflammatory cytokines and immunoglobulin E (IgE).
These results confirm the traditional use of T. indica as an antiasthmatic agent which are evidenced through ex vivo, in silico and in vivo studies.
钩吻（Burm. f.） Merr 是一种攀援多年生植物，在印度传统医学中被用于治疗过敏和哮喘。然而，过去只有少数科学研究对其抗哮喘潜力进行了验证。
本研究旨在探讨钩吻叶提取物及其后续部分的气道平滑肌松弛和抗哮喘作用。
通过生物导向活性选择钩吻叶最活跃的部分，通过液质联用（LC-MS）分析进行化学分析。通过分子对接研究确定了该部分中鉴定化合物与 M 和 H 受体的结合亲和力。F-2（从钩吻叶甲醇提取物中制备的氯仿部分）用于研究其对豚鼠离体气管的平滑肌松弛作用。进一步，通过卵清蛋白诱导的豚鼠哮喘模型评估 F-2 的体内研究。
F-2 在生物测定指导的分离中被发现是最有效的。通过 LC-MS 分析进行的表征显示，F-2 中存在五种主要的生物活性化合物，这些化合物与 M 和 H 受体表现出良好的对接相互作用。离体研究表明，F-2 可以通过靶向多种信号通路（即竞争性拮抗组胺和毒蕈碱受体、β2-肾上腺素能刺激和激活可溶性鸟苷酸环化酶）显著松弛气管环。在体内研究中，F-2 改善了气道高反应性，并降低了支气管肺泡灌洗液（BALF）中炎症细胞因子和免疫球蛋白 E（IgE）的水平。
这些结果通过离体、计算和体内研究证实了传统上使用钩吻作为抗哮喘药物的用途。
