Hofmann A
Pharmacology. 1978;16 Suppl 1:1-11. doi: 10.1159/000136803.
A short survey of the history of ergot, of the original and, for a long time, only source of ergot alkaloids, is given. Once a dreaded poison, ergot has changed its role over the centuries to become a rich treasure house of valuable pharmaceuticals. In the Middle Ages it was the cause of epidemics of ergotism, which cost tens of thousands of people their lives. Ergot was first mentioned by the German physician Lonitzer in 1582 as a remedy used by midwives for quickening childbirth. The isolation of pharmacologically useful alkaloids started in 1906 with the discovery of ergotoxine and its adrenolytic activity by Barger, Carr and Dale. In 1918, Stoll isolated ergotamine, the first chemically pure ergot alkaloid, which found widespread therapeutic use in obstetrics and internal medicine. In 1935 the specific oxytocic principle of ergot, ergonovine, was discovered simultaneously in four separate laboratories. Since then, worldwide investigations on ergot alkaloids resulted in the elucidation of their structures and total syntheses and preparation of valuable therapeutics such as Methergine, Hydergine, Dihydergot, and others.
本文简要回顾了麦角的历史,麦角是麦角生物碱最初且长期以来唯一的来源。曾经令人恐惧的毒药,麦角在几个世纪里改变了它的角色,成为了宝贵药物的丰富宝库。在中世纪,它是麦角中毒流行病的起因,夺去了数万人的生命。1582年,德国医生洛尼策首次提及麦角,称其为助产士用于催生的药物。1906年,巴杰、卡尔和戴尔发现了麦角毒碱及其肾上腺素溶解活性,从此开始了对具有药理作用的生物碱的分离。1918年,斯托尔分离出麦角胺,这是第一种化学纯的麦角生物碱,在产科和内科得到了广泛的治疗应用。1935年,麦角的特异性催产成分麦角新碱在四个不同的实验室同时被发现。从那时起,全球范围内对麦角生物碱的研究导致了其结构的阐明、全合成以及如麦角新碱、氢化麦角碱、双氢麦角胺等宝贵治疗药物的制备。