来自L. Tephrosia purpurea的多个支气管扩展活性通路的新型黄类药物. (个人) (个人) 在沙特阿拉伯不断增长
Maged S Abdel-Kader1,2, Abdulaziz S Saeedan3, Najeeb U Rehman3
1Department of Pharmacognosy, College of Pharmacy, Prince Sattam bin Abdulaziz University, Al-Kharj 11942, Kingdom of Saudi Arabia.
铁紫全提取物 (TPTE) 和其成份显示出支气管扩展作用. 他们分离了7种活性黄,其中4种新化合物表现出类似于帕帕维林和类似于迪西克洛的抗支气管的活性.
科学领域:
- 药理学 药理学是指药理学的学科.
- 自然产品 化学 化学
- 呼吸系统医学 呼吸系统医学
背景情况:
- 紫色 (T. purpurea) 是一种具有潜在呼吸系统益处的药用植物.
- 了解其支气管扩展活性的特定化合物对于治疗开发至关重要.
研究的目的:
- 从T. purpurea中分离和描述具有支气管扩展性能的活性化合物.
- 研究这些孤立化合物的作用机制.
- 评估提取物和分离化合物的体内疗效,以防止诱导的支气管.
主要方法:
- 紫素全提取物 (TPTE) 的液体-液体分化.
- 使用几内亚猪气管肌肉制剂进行活体生物试验引导的活性化合物的分离.
- 使用光谱技术 (NMR,MS,光学旋转,CD) 阐明结构.
- 在体外测试以确定对卡巴霍尔 (CCh) 和高 (K+) 诱导的收缩的抑制作用.
- 在体内评估对海豚中抗胰岛素诱导的支气管的保护.
主要成果:
- TPTE的甲基部分表现出显著的活体支气管扩展活性.
- 他们分离了七种活性黄,包括四种新型化合物:epi-Tephroapollin G (1),Acetyltephroapollin C (3),4''-Dehydroxytephroapollin E (4) 和epi-Tephroapollin F (5).
- 化合物1,3,4和兰西欧拉丁A (6) 抑制了CCH和K+诱导的收缩,表明双化酶和Ca++抑制作用.
- 化合物5和7是CCH诱导的收缩的强有力的抑制剂,类似于dicyclomine.
- 化合物2,5和7表现出选择性肌肉蛋白受体阻塞.
- 口服TPTE,其粉碎片及其化合物7可在体内显著保护抗胰岛素诱导的支气管.
结论:
- 紫色含有强大的支气管扩展化合物,主要是黄.
- 隔离的化合物表现出多种作用机制,包括固酶抑制,Ca++通道阻塞和肌肉蛋白受体对抗作用.
- 这些发现支持T. purpurea用于呼吸系统疾病的传统用途,并强调其作为新型抗喘药物的来源的潜力.
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