在 Dioscorea alata cv 中ACE 抑制活性的表征及其作为天然抗高血压提取物的含义
Keaton Logan1, Chukwuemeka Nwokocha2, Helen Asemota3
1Department of Basic Medical Sciences Biochemistry Section, Faculty of Medical Sciences, The University of the West Indies, Mona Campus, Kingston, Jamaica.
Journal of ethnopharmacology
|September 24, 2023
概括
牙买加Renta Yam (Dioscorea alata) 提取物通过抑制ACE并释放氧化,显示出强大的抗高血压活性. 这种天然来源为合成药物提供了有希望的替代品,其中2-Phenyl-1,3-oxazol-2-ine被确定为关键化合物.
科学领域:
- 药理学 药理学 是一个学科.
- 自然产品化学 自然产品化学
- 心血管研究研究心血管研究
背景情况:
- 亚姆 (Dioscorea sp.) 是一种植物. 提取物具有已知的药用特性,包括抗高血压作用.
- 负责的抗高血压生物活性的特定化合物仍然在很大程度上未被探索.
研究的目的:
- 为了识别牙买加兰塔 (Dioscorea alata) 中具有抗高血压特性的生物活性分数和化合物.
- 使用活动导向的化学信息分析来识别化合物.
主要方法:
- 顺序的固体-液体提取 (SLE) 和SPE-HPLC的 Dioscorea alata. 的分离.
- 气相色谱-质谱 (GC-MS) 用于化学成分分析.
- 试验室内氨酸转化酶 (ACE) 抑制试验和分子对接研究.
主要成果:
- 乙乙提取物 (DR2) 显示出显著的抗高血压活性 (ACE IC50 41.99 μg/mL).
- 鉴定出2--1,3-oxazol-2-ine (2PO) 是生物活性提取物中占主导地位的化合物.
- 2PO对ACE酶表现出强烈的结合亲和力,形成关键的键.
- 试验室试验显示了剂量依赖的ACE抑制,氧化 (NO) 释放刺激,并且在人类静脉内皮细胞 (HUVEC) 中没有毒性.
结论:
- 牙买加兰塔 (Dioscorea alata) 是天然抗高血压化合物的可行来源.
- 已识别的化合物,特别是2PO,显示出开发新型抗高血压疗法的潜力.
- 这种天然替代品可能有助于减轻与合成抗高血压剂相关的毒性.
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