CAJ | 학술논문

目的探讨海洋真菌Halorosellinia oceanicum323的两种代谢产物323-A和323-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323-A和323-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323-A和323-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5.51,5.56,5.62.此外,323-A和323-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期相收缩反应,但对通过细胞外钙离子内流所引起的第二时收缩无明显影响.结论232-A和323-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展前景.
목적탐토해양진균Halorosellinia oceanicum323적량충대사산물323-A화323-B대돈서리체회장수축적영향급기여Ca2+적관계.방법건립조알(Hist)、을선담감(ACh)、록화갑(KCl)치돈서회장수축적량효곡선,분별관찰323-A화323-B대수축적작용,병통과분석수시물대유ACh인기적량충수축성분적영향,대기작용궤제진행탐토.결과323-A화323-B균가제량의뢰성적억제Hist,ACh급KCl소인기적회장조수축,pD2′분별위5.13,4.97,5.36화5.51,5.56,5.62.차외,323-A화323-B대ACh유도적량충수축성분적영향여개길항제유랍파미(Ver)적작용상사,균가현저강저재외계무개리자존재시유세포내개석방소산생적제일시기상수축반응,단대통과세포외개리자내류소인기적제이시수축무명현영향.결론232-A화323-B균구유개길항작용,기작용궤제가능여Ver유사,제시이자재해방면적약이학활성구유심입연구적개치화잠재적개전전경.
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 Ca2+ , was significantly reduced by 323-A, 323-B, as well as Ver, whereas the subsequent sustained tonic contractions induced by adding Ca2+ 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.