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目的 探讨海洋真菌Haloroselliniaoceanicum 32 3的两种代谢产物 32 3 A和 32 3 B对豚鼠离体回肠收缩的影响及其与Ca2 + 的关系。方法 建立组胺 (Hist)、乙酰胆碱 (ACh)、氯化钾 (KCl)致豚鼠回肠收缩的量效曲线 ,分别观察 32 3 A和 32 3 B对收缩的作用 ,并通过分析受试物对由ACh引起的两种收缩成分的影响 ,对其作用机制进行探讨。结果 32 3 A和 32 3 B均可剂量依赖性的抑制Hist,ACh及KCl所引起的回肠条收缩 ,pD2′分别为 5 13,4 97,5 36和 5 5 1,5 5 6 ,5 6 2。此外 ,32 3 A和 32 3 B对ACh诱导的两种收缩成分的影响与钙拮抗剂维拉帕米 (Ver)的作用相似 ,均可显著降低在外界无钙离子存在时由细胞内钙释放所产生的第一时相收缩反应 ,但对通过细胞外钙离子内流所引起的第二时相收缩无明显影响。结论 32 3 A和 32 3 B均具有钙拮抗作用 ,其作用机制可能与Ver类似 ,提示二者在该方面的药理学活性具有深入研究的价值和潜在的开发前景
Objective To investigate the effects of 32 3 A and 32 3 B, two marine metabolites of marine fungus Halorosellinia oceanicum 32 3, on contractile activity of guinea pig ileum and its relationship with Ca2 +. Methods A dose-response curve of ileum contraction induced by histamine (Hist), acetylcholine (ACh) and potassium chloride (KCl) was established. The effects of 32 3 A and 32 3 B on contractility were observed. ACh induced contraction of two components, its mechanism of action were discussed. Results Both 32 3 A and 32 3 B inhibited the ileal contraction induced by Hist, ACh and KCl in a dose-dependent manner with pD2 ’of 5 13,4 97,5 36 and 5 5 1,5 5 6 respectively 2. In addition, the effect of 32 3 A and 32 3 B on ACh-induced contractions was similar to that of the calcium antagonist verapamil (Ver), both of which were significantly decreased by intracellular calcium in the absence of calcium The contractile response to the first phase produced did not have a significant effect on the second phase contractions caused by the influx of extracellular calcium ions. Conclusions 32 3 A and 32 3 B all have calcium antagonism, and their mechanism may be similar to that of Ver, suggesting that their pharmacological activities in this area have in-depth research value and potential development prospects