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Evaluation of bronchodialatory and antimicrobial activities of Otostegia fruticosa: A multi-mechanistic approach
Saudi Pharmaceutical Journal ( IF 3.0 ) Pub Date : 2020-01-31 , DOI: 10.1016/j.jsps.2020.01.007
Mohd Nazam Ansari , Najeeb Ur Rehman , Aman Karim , Tiegsti Bahta , Khalil Y. Abujheisha , Syed Rizwan Ahamad , Faisal Imam

Otostegia fruticosa, a plant belonging to the family Lamiaceae, is endemic to Ethiopia. In Ethiopian traditional medicine, O. fruticosa has been used for the treatment of several respiratory-related disorders. The present study was designed to evaluate the bronchodilatory and antimicrobial activities of O. fruticosa leaves crude extract (Of.Cr). Ex-vivo experiments were conducted on guinea-pig trachea provided with physiological oxygenated buffer solution using emkaBath setup. The crude extract was analyzed by gas chromatography-mass spectrometry. Of.Cr, showed the presence of terpenes, fragrance components, saponins, and higher fatty acids. Of.Cr when tested on contracted tracheal chains with carbamylcholine (CCh, 1 µM) and high K+ (80 mM) produced relaxation by showing higher potency against CCh with incomplete inhibition of high K+. Dicyclomine, used as a positive control, also showed selectively higher potency to inhibit CCh when compared with its effect against K+. In the anticholinergic curves, Of.Cr at 1 mg/mL deflected CCh-induced concentration–response curves (CRCs) competitively to the right like dicyclomine (0.03 µM) and atropine whereas a higher dose of Of.Cr (3 mg/mL) produced a non-parallel shift in the CCh curves like a higher dose of dicyclomine (0.1 µM). In the calcium channel inhibitory assay, Of.Cr at 3 & 5 mg/mL, deflected CRCs of Ca++ to the right like verapamil, used as positive control. Of.Cr, at concentrations (1–3 mg/mL) increases cAMP levels in isolated tracheal homogenates, similar to positive control phosphodiesterase inhibitor (papaverine). When tested for antibacterial activity against standard and clinical strains, Of.Cr was found more active (MIC 475 µg/ml) against S. aureus (NCTC 6571), while the maximum inhibition (MIC 625 µg/ml) was observed by the extract when tested against MRSA. These results determine the mechanistic pathways of the observed bronchodilatory effect of Otostegia fruticosa with a combination of anticholinergic and dual inhibition of phosphodiesterase and voltage-gated Ca++ channels.



中文翻译:

评估金耳麦草的支气管扩张和抗菌活性一种多机制方法

Otostegia fruticosa是唇形科的一种植物,是埃塞俄比亚特有的。在埃塞俄比亚的传统医学中,金黄色葡萄球菌已被用于治疗几种与呼吸有关的疾病。本研究的目的是评估的支气管扩张和抗菌活性O.紫穗槐叶粗提物(Of.Cr)。使用emkaBath装置在配有生理性含氧缓冲液的豚鼠气管上进行离体实验。通过气相色谱-质谱法分析粗提取物。Of.Cr表明存在萜烯,香料成分,皂苷和高级脂肪酸。用氨基甲酰胆碱(CCh,1 µM)和高K +对气管收缩链进行测试时的Of.Cr(80毫米)由显示用高介电常数的不完全抑制针对CCH更高的效力产生松弛+。与对K +的效果相比,用作阳性对照的双环胺也显示出更高的抑制CCh的能力。在抗胆碱能曲线中,浓度为1 mg / mL的Of.Cr与右旋二环胺(0.03 µM)和阿托品竞争性地偏向了CCh诱导的浓度-反应曲线(CRC),而较高剂量的Of.Cr(3 mg / mL)在CCh曲线中产生了非平行位移,如更高剂量的双环明(0.1 µM)。在钙通道抑制试验中,浓度为3和5 mg / mL的Of.Cr导致Ca ++的CRC偏转像维拉帕米一样向右,用作阳性对照。浓度为(1-3 mg / mL)的Of.Cr可增加分离的气管匀浆中的cAMP水平,类似于阳性对照磷酸二酯酶抑制剂(罂粟碱)。当测试对标准菌株和临床菌株的抗菌活性时,发现Of.Cr对金黄色葡萄球菌(NCTC 6571)的活性更高(MIC 475 µg / ml),而提取物观察到最大的抑制作用(MIC 625 µg / ml)。在针对MRSA进行测试时。这些结果确定了观察到的金盏花支气管扩张作用与抗胆碱能和磷酸二酯酶双重抑制以及电压门控的Ca ++通道的结合的机制途径。

更新日期:2020-01-31
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