Department of Biology, The Chinese University of Hong Kong, Shatin, N.T., Hong Kong, PR China.
J Ethnopharmacol. 2010 Apr 21;128(3):679-84. doi: 10.1016/j.jep.2010.02.018. Epub 2010 Feb 26.
Stemona alkaloids with distinctly different chemical skeletons are recently reported as the active components in the antitussive herb Baibu derived from the root-tubers of Stemona tuberosa. This study aims to determine if alkaloids of this herb contribute equally to the antitussive functions, act on the same sites of cough reflex, and play any role in inducing central respiratory depressant effects.
Antitussive potency of four major alkaloids was evaluated on guinea pigs with citric acid aerosol to induce cough. The action sites of the alkaloids on cough reflex pathway were tested with electrical stimulation of the superior laryngeal nerve in guinea pigs. The central respiratory effects of croomine were also tested on guinea pigs.
Croomine, neotuberostemonine and stemoninine showed similar antitussive potency, while tuberostemonine showed much weaker antitussive potency. Neotuberostemonine, tuberostemonine and stemoninine acted on the peripheral cough reflex pathway, while croomine acted on the central part. Croomine also showed obvious central respiratory depressant effects.
The four major Stemona alkaloids in Stemona tuberosa do not contribute equally to antitussive potency in guinea pigs. Neotuberostemonine, tuberostemonine and stemoninine target on peripheral cough reflex pathway. Croomine acts on central sites in the cough reflex pathway and demonstrates central respiratory depressant effects, which can partly account for the adverse reactions reported for the herb.
具有明显不同化学骨架的百部生物碱最近被报道为来源于直立百部块根的止咳草药百部中的活性成分。本研究旨在确定该草药中的生物碱是否对等发挥止咳作用,作用于咳嗽反射的相同部位,以及是否在诱导中枢性呼吸抑制作用中发挥任何作用。
用柠檬酸气雾剂刺激豚鼠诱发咳嗽,评估四种主要生物碱的镇咳效力。用电刺激豚鼠的喉上神经测试生物碱对咳嗽反射途径的作用部位。还在豚鼠身上测试了克罗明的中枢呼吸作用。
克罗明、新百部碱和百部宁表现出相似的镇咳效力,而百部碱的镇咳效力则弱得多。新百部碱、百部碱和百部宁作用于外周咳嗽反射途径,而克罗明作用于中枢部分。克罗明还表现出明显的中枢性呼吸抑制作用。
直立百部中的四种主要百部生物碱对等发挥镇咳效力在豚鼠中并不相同。新百部碱、百部碱和百部宁作用于外周咳嗽反射途径。克罗明作用于咳嗽反射途径的中枢部位,并表现出中枢性呼吸抑制作用,这可以部分解释该草药报告的不良反应。