ANTIHYPERTENSIVE AGENTS FROM RANUNCULACEAE

毛茛科抗高血压药

• 批准号: 2217036
• 负责人: S WILLIAM PELLETIER
• 金额: $ 18.34万
• 依托单位: UNIVERSITY OF GEORGIA
• 依托单位国家: 美国
• 财政年份: 1993
• 资助国家: 美国
• 起止时间: 1993-01-01 至 1995-12-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/2217036
• 关键词: alkaloids; antihypertensive agents; autonomic ganglion; autonomic reflex; chemical structure; diterpenes; dogs; drug design /synthesis /production; drug screening /evaluation; medicinal plants; membrane channels; membrane potentials; neurons; plant extracts; postganglionic fiber; sympathetic ganglion; thin layer chromatography; toxicology; vagus nerve; voltage /patch clamp; voltage gated channel

Current understanding of the effectiveness of the drugs derived from plants belonging to Aconitum, Delphinium and Consolida species (Ranunculaceae) is incomplete and further investigations are desirable. Extracts of more than 50 species of plants of these genera are used for their analgesic, antirheumatic and cardiotonic properties in the Chinese and Indian systems of medicine. The objectives of this research proposal are: (1) To isolate and purify the alkaloids to be tested. (2) to modify structures of active alkaloids for enhancement of antihypertensive activity. (3) to study the mechanism of reflex reception action. (4) to study the actions of alkaloids on autonomic reflexes. Isolation of key alkaloids in adequate amounts will be undertaken so that a pharmacological investigation of these compounds can be pursued. The purified naturally-occurring alkaloids and their derivatives will be screened for CVS activities. Alkaloids that manifest promising hypotensive activity will be structurally modified to enhance maximal therapeutic effects and minimal toxicity.

目前对药物有效性的了解 乌头属、飞燕草属和Consolida属植物 （毛茛科）不完整，需要进一步研究。 这些属的 50 多种植物的提取物用于 它们在中国的镇痛、抗风湿和强心作用 和印度的医学体系。 本研究计划的目的是： (1) 分离和纯化 待测生物碱。 (2)活性生物碱结构修饰 用于增强抗高血压活性。 (3)研究机理 反射性接收动作。 (4)研究生物碱的作用 自主反射。 将分离足量的关键生物碱，以便 可以对这些化合物进行药理学研究。 这 纯化的天然生物碱及其衍生物将 筛选 CVS 活动。 有前景的生物碱 降血压活性将在结构上进行修改，以增强最大 治疗效果好，毒性极小。