{"title":"山柑孕酮类化合物对大鼠离体子宫收缩素及其他催产素诱导的收缩作用。","authors":"J B Calixto, R L Brum, R A Yunes","doi":"10.1016/0306-3623(91)90579-u","DOIUrl":null,"url":null,"abstract":"<p><p>1. The effects of 5 pregnane compounds isolated from the rhizomes of Mandevilla illustris were examined against bradykinin (BK), Lysyl-bradykinin (L-BK), acetylcholine (ACh) and oxytocin (Ot)-induced contractions in the isolated uteri of the rat. 2. Compounds MI 15 and MI 18 (5-40 micrograms/ml) caused a parallel and concentration-dependent rightward displacement of BK and L-BK concentration-response curves. Compound MI 21 (2.5-10 micrograms/ml) also produced a concentration-dependent displacement to the right of the BK concentration-response curve, but reduced its maximal response. Schild analysis of these data were linear (r close to 1) and furnished the following PA2 values (as G/ml): 6.0, 5.1 and 5.9, respectively. However, the slopes were significantly higher than unity. Compounds MI 25 and MI 27 (10-40 micrograms/ml) caused little or even no effect against BK and ACh responses. 3. In addition, compounds MI 18 and MI 21 (10-40 micrograms/ml) also antagonized in a concentration-dependent manner L-BK concentration-response curves. Schild plot were linear (r close to 1) and yielded the nominal pA2 values (as G/ml) of 5.0 and 5.8, respectively, but the slopes were significantly different from one. 4. Like the results obtained previously with the crude extract from M. illustris, the purified compounds from the rhizome of this plant were not selective towards kinin action since at the same range concentrations they markedly interfered with both the sensitivities and the maximal responses caused by ACh and Ot in this preparation.</p>","PeriodicalId":12487,"journal":{"name":"General pharmacology","volume":"22 6","pages":"1071-5"},"PeriodicalIF":0.0000,"publicationDate":"1991-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0306-3623(91)90579-u","citationCount":"4","resultStr":"{\"title\":\"Action of pregnane compounds from Mandevilla illustris against contractions induced by kinins and other oxytocics in the rat isolated uterus.\",\"authors\":\"J B Calixto, R L Brum, R A Yunes\",\"doi\":\"10.1016/0306-3623(91)90579-u\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>1. The effects of 5 pregnane compounds isolated from the rhizomes of Mandevilla illustris were examined against bradykinin (BK), Lysyl-bradykinin (L-BK), acetylcholine (ACh) and oxytocin (Ot)-induced contractions in the isolated uteri of the rat. 2. Compounds MI 15 and MI 18 (5-40 micrograms/ml) caused a parallel and concentration-dependent rightward displacement of BK and L-BK concentration-response curves. Compound MI 21 (2.5-10 micrograms/ml) also produced a concentration-dependent displacement to the right of the BK concentration-response curve, but reduced its maximal response. Schild analysis of these data were linear (r close to 1) and furnished the following PA2 values (as G/ml): 6.0, 5.1 and 5.9, respectively. However, the slopes were significantly higher than unity. Compounds MI 25 and MI 27 (10-40 micrograms/ml) caused little or even no effect against BK and ACh responses. 3. In addition, compounds MI 18 and MI 21 (10-40 micrograms/ml) also antagonized in a concentration-dependent manner L-BK concentration-response curves. Schild plot were linear (r close to 1) and yielded the nominal pA2 values (as G/ml) of 5.0 and 5.8, respectively, but the slopes were significantly different from one. 4. Like the results obtained previously with the crude extract from M. illustris, the purified compounds from the rhizome of this plant were not selective towards kinin action since at the same range concentrations they markedly interfered with both the sensitivities and the maximal responses caused by ACh and Ot in this preparation.</p>\",\"PeriodicalId\":12487,\"journal\":{\"name\":\"General pharmacology\",\"volume\":\"22 6\",\"pages\":\"1071-5\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"1991-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.1016/0306-3623(91)90579-u\",\"citationCount\":\"4\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"General pharmacology\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.1016/0306-3623(91)90579-u\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"General pharmacology","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1016/0306-3623(91)90579-u","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 4
摘要
1. 研究了从山茱萸根茎中分离的5种孕烷类化合物对大鼠离体子宫缓激肽(BK)、赖氨酸-缓激肽(L-BK)、乙酰胆碱(ACh)和催产素(Ot)诱导的子宫收缩的抑制作用。2. 化合物mi15和mi18 (5 ~ 40 μ g /ml)引起BK和L-BK浓度-响应曲线平行且浓度相关的右位移。化合物MI 21 (2.5 ~ 10 μ g /ml)在BK浓度-反应曲线右侧也产生浓度依赖性位移,但降低了其最大反应。柴尔德分析这些数据是线性的(r接近1),并提供以下PA2值(以G/ml):分别为6.0,5.1和5.9。然而,坡度明显高于统一。化合物mi25和mi27(10 ~ 40微克/毫升)对BK和ACh的抑制作用很小,甚至没有作用。3.此外,化合物MI 18和MI 21 (10 ~ 40 μ g /ml)对L-BK的拮抗作用也呈浓度依赖性。席尔德图呈线性(r接近1),标称pA2值(以G/ml计)分别为5.0和5.8,但斜率与1有显著差异。4. 与之前从鸢尾草粗提物中获得的结果一样,从鸢尾草根茎中纯化的化合物对激肽的作用没有选择性,因为在相同的浓度范围内,它们明显干扰了该制剂中乙酰胆碱和乙酰胆碱引起的敏感性和最大反应。
Action of pregnane compounds from Mandevilla illustris against contractions induced by kinins and other oxytocics in the rat isolated uterus.
1. The effects of 5 pregnane compounds isolated from the rhizomes of Mandevilla illustris were examined against bradykinin (BK), Lysyl-bradykinin (L-BK), acetylcholine (ACh) and oxytocin (Ot)-induced contractions in the isolated uteri of the rat. 2. Compounds MI 15 and MI 18 (5-40 micrograms/ml) caused a parallel and concentration-dependent rightward displacement of BK and L-BK concentration-response curves. Compound MI 21 (2.5-10 micrograms/ml) also produced a concentration-dependent displacement to the right of the BK concentration-response curve, but reduced its maximal response. Schild analysis of these data were linear (r close to 1) and furnished the following PA2 values (as G/ml): 6.0, 5.1 and 5.9, respectively. However, the slopes were significantly higher than unity. Compounds MI 25 and MI 27 (10-40 micrograms/ml) caused little or even no effect against BK and ACh responses. 3. In addition, compounds MI 18 and MI 21 (10-40 micrograms/ml) also antagonized in a concentration-dependent manner L-BK concentration-response curves. Schild plot were linear (r close to 1) and yielded the nominal pA2 values (as G/ml) of 5.0 and 5.8, respectively, but the slopes were significantly different from one. 4. Like the results obtained previously with the crude extract from M. illustris, the purified compounds from the rhizome of this plant were not selective towards kinin action since at the same range concentrations they markedly interfered with both the sensitivities and the maximal responses caused by ACh and Ot in this preparation.