Abdel-Kader Maged S, Saeedan Abdulaziz S, Rehman Najeeb U, Faqihi Hayder M, Soliman Gamal A
Department of Pharmacognosy, College of Pharmacy, Prince Sattam bin Abdulaziz University, Al-Kharj 11942, Kingdom of Saudi Arabia.
Department of Pharmacognosy, College of Pharmacy, Alexandria University, Alexandria 21215, Egypt.
Saudi Pharm J. 2024 Apr;32(4):101992. doi: 10.1016/j.jsps.2024.101992. Epub 2024 Feb 15.
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 .
（）的总提取物在离体豚鼠气管平滑肌中表现出强大的支气管扩张作用。采用液 - 液技术对总提取物进行分级分离，随后进行支气管扩张测试，结果表明活性集中在氯仿（CHCl）可溶级分中。以支气管扩张活性为导向对氯仿级分进行植物化学研究，从中分离出7种活性黄酮，其中化合物（Tephroapollin G）、（乙酰基Tephroapollin C）、（4'' - 去羟基Tephroapollin E）和（Tephroapollin F）为新化合物。利用包括旋光度和圆二色性（CD）数据在内的相关光谱工具确定了其结构。化合物、、和披针叶黄素A（）在等效浓度下以不同效力抑制卡巴胆碱（CCh）以及高钾（K）介导的收缩，其作用类似于罂粟碱，而（ - ） - Tephroapollin G（）选择性抑制CCh介导的收缩，但对高钾无活性。相比之下， - Tephroapollin F（）和（ - ） - 假半光荚素（）在消除CCh诱导的收缩方面比高钾更有效，类似于双环胺。和的罂粟碱样双重磷酸二酯酶和钙离子抑制活性通过异丙肾上腺素曲线对CCh向左的增强间接得到证实，而和 - 的钙离子抑制作用通过钙离子浓度 - 反应曲线（CRC）向右的偏转以及最大反应的消除得以证实，其方式类似于维拉帕米。此外，化合物和在较低浓度下表现出类似于阿托品的对毒蕈碱受体的选择性阻断作用。对豚鼠口服、氯仿级分和可显著预防0.2％组胺气雾剂诱导的支气管痉挛。
