Physiological Study of Pungent Agents Extracted from Various Spices in Rat and Guinea Pig

在这项研究中，我们使用辣椒素、胡椒碱和二烯丙基二硫化物作为从香料中提取的刺激剂。为了阐明这些药物未知的直接或间接的生理作用，我们用大鼠和豚鼠的心脏和子宫进行了三种实验。研究1：辣椒素对大鼠和豚鼠离体心乳头肌的作用。辣椒素对大鼠乳头肌的收缩张力具有双重作用。也就是说，低浓度(0.1µM)使张力幅度增加，而高浓度(×10µM)使张力幅度降低。在β-受体阻滞剂心得安的存在下，低浓度时的张力增加从未发生过。在1赫兹的张力幅度中，辣椒素的有效浓度50%(EC_(50))约为10微米。所有浓度均以浓度依赖的方式降低大鼠乳头肌的张力。在1赫兹时，EC_&lt；50&gt；约为0.1微米，表现出较高的…大鼠对辣椒素更敏感。在同一动物中，我们研究了辣椒素对静息状态收缩(RSC)的影响，以了解其对细胞内钙储存的电生理作用，并将结果与咖啡因和兰尼定的作用进行了比较，因为RSC被认为主要依赖于从钙储存中释放的额外钙。因此，辣椒素对钙库没有直接影响。我们的数据表明，辣椒素引起的负性变力作用很大程度上是由于钙通道的阻断，我们以前已经报道过，使用分离的单个心室细胞(Jpn.J.Physiol.43[Suppl.2]：s155,1993)。研究2：辣椒素、胡椒碱和二烯丙基二硫化物对分离的大鼠子宫肌层的收缩作用的比较辣椒素、胡椒碱和二烯丙基二硫化物这三种药物都抑制了分离的大鼠子宫肌层自发收缩的幅度和频率。二烯丙基二硫化物抑制张力的效果最好，胡椒碱次之，辣椒素次之。S对二烯丙基二硫化物、胡椒碱和辣椒素的抑制幅度分别为20 mM、50 mM和0.1 mM。S对二烯丙基二硫化物和辣椒素的抑制频率分别为20 mM和0.1 mM。胡椒碱对频率无影响或影响很小。研究3：辣椒素、胡椒碱和二烯丙基二硫化物对糖尿病大鼠和非糖尿病大鼠呼吸和外周血流量的影响在嗅觉实验中，三种药物增加自发性糖尿病大鼠每分钟呼吸次数和腹部外周血流量，而对非糖尿病大鼠无或几乎没有影响。在味觉实验中，三种药物使非糖尿病大鼠的呼吸略有增加，但使糖尿病大鼠的呼吸减少。3种药物均能降低糖尿病大鼠的血流量，但对非糖尿病大鼠的血流量无影响。为了阐明这些实验事实，我们需要进一步的实验。较少

In this study we used capsaicin, piperine, and diallyl disulfide as pungent agents extracted from spices. We did next three kinds of experiments to clarify unknown direct or indirect physiological effects of these agents, using a whole body or isolated preparation of heart and uterus of rats and guinea pigs.Study 1 : Effects of capsaicin on isolated ventricular papillary muscle from rat and guinea pig. Capsaicin showed dual effects on the contractile tension of rat papillary muscle. That is, the low concentration (0.1muM) increased the amplitude of tension, but the high concentration (*10muM) decreased it. The increase in the tension at low concentration never happened in the presence of beta-blocker, propranolol. Effective concentration 50% (EC_<50>) of capsaicin in the amplitude of tension at 1Hz was around 10muM.On the other hand, all concentrations used decreased the tension of rat papillary muscle in a concentration-dependent manner. EC_<50> at 1Hz was around 0.1muM,showing a high … More sensitivity to capsaicin in rat. In the same animal, we investigated the effects of capsaicin on the rested-state contraction (RSC) to know its electrophysiological actions on intracellular Ca store, and compared the findings with effects of caffeine and ryanodine, because RSC is believed to be mostly dependent on extra Ca released from the Ca store. As a result, capsaicin had no direct effect on the Ca store. Our data suggest that capsaicin-induced negative inotropic action is largely due to a block of Ca channels, as we have reported previously, using isolated single ventricular cells (Jpn.J.Physiol.43 [Suppl.2] : s155,1993).Study 2 : Comparison of contractile effects between capsaicin, piperine and diallyl disulfide in isolated rat myometriumAll three agents, capsaicin, piperine and diallyl disulfide repressed the amplitude and frequency of spontaneous contraction of isolated rat myometrium. Diallyl disulfide was the most effective in inhibiting the amplitude of the tension, followed by piperine and capsaicin in that order. EC_<50> 's in inhibiting the amplitude were 20muM in diallyl disulfide, 50muM in piperine and 0.1mM in capsaicin. EC_<50> 's in inhibiting the frequency were 20muM in diallyl disulfide and 0.1mM in capsaicin. Piperine showed no or little effect on the frequency. It is suggested that these agents decrease the tension, via a block of Ca channels.Study 3 : Effects of capsaicin, piperine and diallyl disulfide on the respiration and periferal blood flow of diabetic and non-diabetic ratsIn olfactory experiments, three agents increased the number of respiration per minute and periferal blood flow in the abdomen of spontaneous diabetic rats, while they had no or little effect in non-diabetic ones. In taste experiments, three agents produced a little increase in the respiration of non-diabetic rats, but these produced a decrease in that of diabetics. The blood flow in diabetic rats was decreased by three agents, but that in non-diabetic rats was not effected. To elucidate these experimental facts, we need further experiments. Less