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New flavonoids with multiple bronchodilator activity pathways from Tephrosia purpurea L. (Pers.) growing in Saudi Arabia
Saudi Pharmaceutical Journal ( IF 4.1 ) Pub Date : 2024-02-15 , DOI: 10.1016/j.jsps.2024.101992
Maged S. Abdel-Kader , Abdulaziz S. Saeedan , Najeeb U. Rehman , Hayder M. Faqihi , Gamal A. Soliman

Total extract of () expressed potent bronchodilator effect in isolated Guinea pigs’ tracheal muscles. Fractionation of total extract ( using liquid–liquid technique followed by bronchodilator testing indicated that the activity was trapped to the chloroform (CHCl) soluble fraction. Phytochemical study of the CHCl fraction guided by bronchodilator activity led to the isolation of 7 active flavones of which compounds (Tephroapollin G), (Acetyltephroapollin C), (4′’-Dehydroxytephroapollin E), and (Tephroapollin F) were new. Structures were identified using relevant spectroscopic tools including optical rotations and CD data. Compounds , , and lanceolatin A () behaved like papaverine by inhibiting carbachol (CCh) as well as high potassium (K)-mediated contractions at equivalent concentrations with varied potencies whereas (-)-Tephroapollin G () selectively inhibited CCh-mediated contractions but was not found active against high K. -Tephroapollin F () and (-)-Pseudosemiglabrin () in contrast were significantly more potent to abolish CCh induced contraction when compared with high K similar to dicyclomine. Papaverine like dual phosphodiesterase enzyme Ca ion inhibitory activities of and were confirmed indirectly by the bolster of the isoprenaline curves against CCh to the left whereas Ca inhibitory effect of and – was confirmed by the rightward deflection of Ca concentration–response curves (CRCs) towards right with quashing of the maximum response in same fashion like verapamil. Moreover, compounds and at lower concentrations showed selective blockade of muscarinic receptor similar to atropine. Oral administration of the , CHCl and to guinea pigs significantly protected against bronchospasm induced by 0.2 % histamine aerosol .

中文翻译:

来自沙特阿拉伯生长的 Tephrosia purpurea L. (Pers.) 的具有多种支气管扩张活性途径的新类黄酮

()的总提取物在离体豚鼠的气管肌肉中表现出有效的支气管扩张作用。总提取物的分馏(使用液-液技术,然后进行支气管扩张剂测试表明活性被捕获到氯仿(CHCl)可溶性组分中。以支气管扩张剂活性为指导对 CHCl 组分进行植物化学研究,分离出 7 种活性黄酮,其中化合物(Tephroapollin G)、(Acetyltephroapollin C)、(4''-DeHydroxytephroapollin E) 和 (Tephroapollin F) 是新化合物。使用包括旋光度和 CD 数据在内的相关光谱工具鉴定了结构。化合物 、 和 lanceolatin A () 表现出与罂粟碱类似,通过抑制卡巴胆碱 (CCh) 以及不同效力的同等浓度的高钾 (K) 介导的收缩,而 (-)-Tephroapollin G () 选择性抑制 CCh 介导的收缩,但未发现对高钾有活性。 -相反,与双环胺类似的高 K 相比,Tephroapollin F () 和 (-)-Pseudosemiglabrin () 消除 CCh 诱导的收缩的效力明显更强。罂粟碱样双磷酸二酯酶 Ca 离子抑制活性通过对 CCh 向左的异丙肾上腺素曲线的支持间接证实,而 和 的 Ca 抑制作用通过 Ca 浓度-反应曲线 (CRC) 向右偏转间接证实以与维拉帕米相同的方式消除最大反应。此外,化合物在较低浓度下表现出与阿托品类似的毒蕈碱受体的选择性阻断。豚鼠口服 CHCl 和 CHCl 可以显着防止 0.2% 组胺气雾剂引起的支气管痉挛。
更新日期:2024-02-15
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