title: The gastrointestinal irritation of polygala saponins and its potential mechanism in vitro and in vivo.
abstract: Processing alters the pharmacological activity and reduces the gastrointestinal toxicity of the polygalae. To investigate the effect of processing, different glycosyl substituent products were tested. Hypnotic and subhypnotic doses of pentobarbital-induced sleep tests on mice were used to evaluate the sedative activity of polygala saponins with different glycosyl substituents; isolated gut motility experiment was employed to study excitatory effects of different polygala saponins; the gastrointestinal irritation effects of different polygala saponins were compared by measuring the levels of gastric PGE2 and intestinal TNF-α on mice. When compared with control, Onjisaponin B (OJB) and tenuifolin (TEN), but not senegenin (SNG), significantly increased the number of sleeping mice and prolonged the sleeping time (P < 0.05); 80, 40, and 20 mg/L of OJB and 80 mg/L of TEN, but not SNG, obviously changed the amplitude and frequency of isolated jejunum (P < 0.05); all the three compounds significantly decreased the level of gastric PGE2 but had no obvious influences on the reduction of intestinal TNF-α level. For sedative and hypnotic effects, OJB > TEN > SNG; for the protection form gastrointestinal irritation and damages, OJB > TEN > SNG. Therefore, in processing Polygala, glycosyl breaking may be related to the decline of pharmacological activity and gastrointestinal toxicity of polygala saponins.
authors.affiliation: Ministry of Education Key Laboratory of Traditional Chinese Medicine Resources and Compounds, Hubei College of Traditional Chinese Medicine, Wuhan, Hubei 430061, China.
authors.forename: Li
authors.initials: L
authors.lastname: Wen
authors.affiliation: Wuhan Institute of Biological Products Co., Ltd., Wuhan, Hubei 430207, China.
authors.forename: Nan
authors.initials: N
authors.lastname: Xia
authors.affiliation: Ministry of Education Key Laboratory of Traditional Chinese Medicine Resources and Compounds, Hubei College of Traditional Chinese Medicine, Wuhan, Hubei 430061, China.
authors.forename: PeiPei
authors.initials: P
authors.lastname: Tang
authors.affiliation: Ministry of Education Key Laboratory of Traditional Chinese Medicine Resources and Compounds, Hubei College of Traditional Chinese Medicine, Wuhan, Hubei 430061, China.
authors.forename: Yi
authors.initials: Y
authors.lastname: Hong
authors.affiliation: Ministry of Education Key Laboratory of Traditional Chinese Medicine Resources and Compounds, Hubei College of Traditional Chinese Medicine, Wuhan, Hubei 430061, China.
authors.forename: ZiZhen
authors.initials: Z
authors.lastname: Wang
authors.affiliation: Ministry of Education Key Laboratory of Traditional Chinese Medicine Resources and Compounds, Hubei College of Traditional Chinese Medicine, Wuhan, Hubei 430061, China.
authors.forename: YaJie
authors.initials: Y
authors.lastname: Liu
authors.affiliation: Ministry of Education Key Laboratory of Traditional Chinese Medicine Resources and Compounds, Hubei College of Traditional Chinese Medicine, Wuhan, Hubei 430061, China.
authors.forename: YanJu
authors.initials: Y
authors.lastname: Liu
authors.affiliation: Ministry of Education Key Laboratory of Traditional Chinese Medicine Resources and Compounds, Hubei College of Traditional Chinese Medicine, Wuhan, Hubei 430061, China.
authors.forename: JianJun
authors.initials: J
authors.lastname: Liu
authors.affiliation: Ministry of Education Key Laboratory of Traditional Chinese Medicine Resources and Compounds, Hubei College of Traditional Chinese Medicine, Wuhan, Hubei 430061, China.
authors.forename: XiangQiong
authors.initials: X
authors.lastname: Li
mesh_terms: D000818:Animals; D006801:Humans; D051379:Mice; D015232:Dinoprostone / Q000096:biosynthesis; D045786:Diterpenes, Kaurane / Q000008:administration & dosage; D041981:Gastrointestinal Tract / Q000187:drug effects / Q000503:physiopathology; D015870:Gene Expression / Q000187:drug effects; D031801:Polygala / Q000737:chemistry; D012503:Saponins / Q000008:administration & dosage / Q000737:chemistry; D014315:Triterpenes / Q000008:administration & dosage; D014409:Tumor Necrosis Factor-alpha / Q000096:biosynthesis
chemical_list: D015232:Dinoprostone; D045786:Diterpenes, Kaurane; C474233:onjisaponin B; D012503:Saponins; D014315:Triterpenes; D014409:Tumor Necrosis Factor-alpha; C407311:tenuifolic saponin