An in vitro pharmacological examination of venom from the soldierfish Gymnapistes marmoratus

被引:10
作者
Hopkins, BJ
Hodgson, WC
Sutherland, SK
机构
[1] MONASH UNIV,DEPT PHARMACOL,CLAYTON,VIC 3168,AUSTRALIA
[2] UNIV MELBOURNE,AUSTRALIAN VENOM RES UNIT,PARKVILLE,VIC 3052,AUSTRALIA
关键词
D O I
10.1016/S0041-0101(96)00213-9
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The aim of the present study was to commence a characterisation of some of the basic pharmacological properties of venom from the soldierfish (Gymnapistes marmoratus). Soldierfish venom was prepared by extraction into 10% glycerol and centrifugation to remove insoluble material. Protein content was determined and venom concentrations were expressed as mu g venom protein. Soldierfish venom (0.5-15 mu g/ml) produced concentration-dependent contractile responses in guinea-pig isolated ileum (GPI) and longitudinal smooth muscle (LSM) preparations. The muscarinic receptor antagonist atropine (10 nM) significantly inhibited responses of LSM to soldierfish Venom (2.5 mu g/ml). Responses to soldierfish venom (4-5 mu g/ml) in GPI were not significantly affected by the ganglion-blocking drug mecamylamine (10 mu M) or by incubation with blood cholinesterase, The cyclooxygenase inhibitor indomethacin (2 mu M) significantly inhibited responses to soldierfish venom (2.5 mu g/ml) in LSM. Neither the thromboxane A(2)/prostaglandin H-2 receptor antagonist GR32191B (1 mu M) nor the leukotriene receptor antagonist SB205312 (10 nM) significantly affected responses to soldierfish venom (5 mu g/ml) in GPI. Responses to soldierfish venom (2.5-5 mu g/ml) were not significantly inhibited by the histamine receptor antagonist mepyramine (0.5 mu M), the angiotensin-converting enzyme inhibitor captopril (2 mu M) or the neurokinin-1 receptor antagonist CP-99,994 (0.1 mu M) in LSM. The angiotensin AT, receptor antagonist EXP3174 (0.1 mu M) also failed to inhibit significantly the responses to soldierfish venom (5 mu g/ml) in GPI, A fluorometric assay for the detection of 5-hydroxytryptamine (5-HT) and related compounds indicated a level in soldierfish venom of 1.60 +/- 0.01 ng of 5-HT-like substance per mu g venom protein. Soldierfish venom (0.5-10 mu g/ml) produced concentration-dependent contractile responses in rat isolated stomach fundus strips, and these responses (2.5 mu g/ml) were significantly inhibited by the 5-HT1/5-HT2 receptor antagonist methysergide (0.1 mu M). These results suggest that soldierfish venom may stimulate the release of acetylcholine to act at muscarinic receptors on guinea-pig gastrointestinal smooth muscle, The venom also appears to be causing the release of cyclooxygenase products, such as prostaglandins, and contains 5-HT, or a 5-HT-like substance, that acts directly at 5-HT receptors. (C) 1997 Elsevier Science Ltd.
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收藏
页码:1101 / 1111
页数:11
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