海洋真菌Halorosellinia oceanicum 323的两种代谢产物对离体豚鼠回肠收缩的影响(英文)  

Effects of two metabolites of cultured marine fungus, Halorosellinia oceanicum 323, on the contraction of isolated guinea-pig ileum

作　　者：罗景慧[1] 杨迎暴[2] 林永成[3] 姜广策[3] 陈志良[1] 

机构地区：[1]南方医院药学部,广东广州510515 [2]第一军医大学药理教研室,广东广州510515 [3]中山大学化学与化工学院,广东广州510275

出　　处：《药学学报》2004年第8期586-590,共5页Acta Pharmaceutica Sinica

基　　金：NationalNaturalScienceFoundationofChina ( 2 9672 0 5 3and 2 0 0 72 0 5 8) ,NaturalScienceFoundationofGuangdongProvince ( 95 0 0 2 6and980 3 17) ,KeyProjectofNaturalScienceFoundationofGuangdongProvince ( 0 2 173 2 ),NationalHi tech 863Project ( 2 0 0 1AA6

摘　　要：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 。Aim To investigate the effects of 323-A and 323-B, two isomers extracted from the metabolites of cultured marine fungus, Halorosellinia oceanicum 323, on the contraction of isolated guinea pig ileum (GPI). Methods The GPI contractions were recorded with a two-channel-physiological recorder with tension transducers. Cumulative dose-response curves of contractions of isolated GPI induced by histamine (Hist), acetylcholine (ACh) and potassium chloride (KCl) were constructed, then the influences of 323-A and 323-B on each curve were observed. Furthermore, possible mechanisms underlying effects of the two compounds were explored by analyzing their influences on the biphasic contractile response to ACh, with comparison of a calcium antagonist, verapamil (Ver). Results The data indicated that both 323-A and 323-B inhibited the contractile actions of GPI triggered by Hist, ACh and KCl in a concentration-dependent manner, with pD2′ values of 5.13, 4.97, 5.36 and 5.51, 5.56, 5.62, respectively. The initial phase component of the ACh-elicited contractions, in the absence of external Ca 2+, was significantly reduced by 323-A, 323-B, as well as Ver, whereas the subsequent sustained tonic contractions induced by adding Ca 2+ to the bath solution were almost unaffected. Conclusion These results suggest that 323-A and 323-B have calcium antagonistic effects similar to that of Ver in mechanisms, and they might have potential to be developed as calcium antagonists.

关 键 词：海洋真菌 Halorosellinia oceanicum323 代谢产物 豚鼠 回肠收缩 离体回肠 钙离子 药理学 

分 类 号：R282.77[医药卫生—中药学]