六磺丁基化c60对豚鼠胃环肌的影响

Shiang-Suo Huang, Lan Hui Chih, C. Lin, L. Chiang, T. Mashino, M. Mochizuki, K. Okuda, T. Hirota, M. Tsai, M. Tsai
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引用次数: 1

摘要

以豚鼠胃圆肌为实验对象,用药理学方法研究了富勒烯衍生物六磺丁基化(FC4S)对平滑肌收缩的影响。比较了单丙二酸C60 (MMA C60)对同种制剂的影响。这些化合物对大肠带绦虫、豚鼠门静脉和输精管的影响也进行了测试。而MMA C60没有引起胃环肌和大肠带绦虫的挛缩。FC4S和MMA C60均未引起豚鼠门静脉和输精管的收缩。哌唑嗪(0.5 μM)和心得安(0.5 μM)对FC4S引起的胃圆肌挛缩无明显影响。而阿托品(0.01、0.1和1 μM)、河豚毒素(0.1 μM)和低钙介质对FC4S诱导的胃圆肌挛缩有可逆的抑制作用。用不同毒蕈碱受体亚型拮抗剂检测FC4S对胃肌挛缩的影响。毒蕈碱M3受体拮抗剂4-DAMP (1 μM)和毒蕈碱M4受体拮抗剂tropicamide (1 μM)未改变FC4S引起的挛缩。毒蕈碱M1受体拮抗剂吡renzepine (0.1 μM)和毒蕈碱M2受体拮抗剂甲氧曲明(0.25 μM)可显著降低FC4S诱导的环状肌挛缩。阿托品(1 μM)或河豚毒素(0.1 μM)完全阻断FC4S诱导的胃圆肌挛缩。结论:FC4S引起胃圆肌挛缩。这可能是由于FC4S作用于胃肌中存在的胆碱能细胞,间接激活这些细胞中依赖河豚毒素的递质释放,进而激活肌肉中的毒蕈素M1、M2受体,引起收缩。
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EFFECTS OF HEXASULFOBUTYLATED C60 ON THE GASTRIC CIRCULAR MUSCLE OF GUINEA PIG
The effects of hexasulfobutylated (FC4S), the fullerene derivative on the contraction of smooth muscle were tested pharmacologically on the circular muscle of stomach of guinea pigs. The effects of monomalonic acid C60 (MMA C60) on the same preparations were compared. The effects of those compounds on the taenia coli, portal vein and vas deferens of guinea pigs were also tested. The FC4S did, while MMA C60 did not elicit contracture of the circular muscle of stomach and taenia coli. Both FC4S and MMA C60 did not elicit contraction on the portal vein and on the vas deferens of the guinea pig. Prazosin (0.5 μM) or propranolol (0.5 μM) did not alter the FC4S elicit contracture of the circular muscle of stomach. However, atropine (0.01, 0.1 and 1 μM), tetrodotoxin (0.1 μM) or low calcium medium decreased reversibly the FC4S elicited contracture of the circular muscle of stomach. The effect of FC4S on the contracture of the gastric muscles was also tested using various muscarinic receptor subtype antagonists. 4-DAMP (1 μM), muscarinic M3 receptor antagonist, and tropicamide (1 μM), muscarinic M4 receptor antagonist, did not alter the contracture elicited by FC4S. Pirenzepine (0.1 μM), muscarinic M1 receptor antagonist, and methoctramine (0.25 μM), muscarinic M2 receptor antagonist, significantly decreased the FC4S elicited contracture of the circular muscle. Atropine (1 μM) or tetrodotoxin (0.1 μM) completely blocked the FC4S elicited contracture of the circular muscle of stomach. It is concluded that FC4S elicited contracture of the circular muscle of stomach. The effect may be due to FC4S acts on the cholinergic cells existed in the gastric muscle and indirectly activating the tetrodotoxin dependent releasing of the transmitters from the cells, then, activating the muscarinice M1, M2 receptors in the muscle eliciting the contractures.
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