• 한국동물위생학회지
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• 제19권2호
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• pp.154-162
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• 1996

The effcets of adenosine 5'-triphosphate(ATP) were investigated on the uterine smooth muscle motility in the pig. The results were summarized as follows: 1. The effects of the porcine uterine smooth muscle and the contractile responses increased between the concentration of ATP $10^{-5}$ and $10^{-3}$ M with a dose-dependent manner. 2. The contractile response induced by ATP($10^{-4}$ M) was not blocked by pretreatment with cholinergic receptor blocker, atropine ($10^{-6}$ M) 3. The contractile response induced by ATP ($10^{-4}$ M) was not blocked by pretreatment with $\alpha$ -adrenergic receptor blocker, phentolamine(10$^{-6}$ M) and ${\beta}$-adrenergic blocker, propranolol ($10^{-6}$ M). 4. The contractile response induced by ATP($10^{-4}$ M) was not appeared in 4Ca^{++}$ -free medium. As the concentration of $Ca^{++}$ in $Ca^{++}$ -free medium was increased, the contractile response induced by ATP ($10^{-4}$ M) was enhenced but was completely inhibited by pretreatment with $Ca^{++}$ -channel blocker, papaverine($10^{-6}$ M) or verapamil($10^{-6}$ M). From these results, it was conclued that the effects of ATP were the contraction mediated by purinergic receptor in uterine smooth muscle of pig.

• 약학회지
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• 제43권5호
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• pp.659-664
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• 1999

To investigate the difference of contractile mechanism between KCI and phenylephrine-induced contraction, we observed effects of $Ca^{2+}$ antagonists and protein kinase inhibitors on aorta contraction of rats. Verapamil dose-dependently inhibited the contraction induced by KCI and phenylephrine, the inhibitory effect of verapamil was more potent in KCI-induced contraction than phenylephrine-induced contraction. Econazole and TMB-8 significantly inhibited CKI-induced contraction but did not inhibit phenylephrine-induced contraction. Staurosporine dose-dependently inhibited both KCI and phenylephrine-induced contraction. Genistein and calmodulin antagonists (W-7 and trifluoperazine) also inhibited both contraction in a dose dependent manner. However, the inhibitory effects of genistein and calmodulin antagonists were more potent in phenylephrine-induced contraction than KCI-induced contraction. These results suggest that involvements of $Ca^{2+}$ channel and protein kinase in rat aorta contraction were dependent on agonist causing aorta smooth muscle contraction.

• 대한한방내과학회지
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• 제12권2호
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• pp.74-88
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• 1991

In order to study the effects of Goosunsan known clinically for their effects of treatment for cough and asthmas the study was carried out to investigate the effect of Goosunsan extract on the contractile force of the isolated guinea pig's vaviovs kinds smooth muscles and elucidate its mechanism The result were obtained as follows: 1. The isolated trachea & ileum smooth muscles of guinea pig was suspended in the organ bath with oxygenated kreb's Henselsite bicarbonate buffer solution at $37^{\circ}C$, and the developed tension by the drug was recorded with Isometric transducer (nacro F-60). The resting tension was approximately 0.5g. 2. The isolated trachea & ileum smooth muscles of guinea pig was remakably relaxed by the administration of Goosunsan. 3. The contractile response of the trachea smooth muscle of the isolated guinea pig to histamine 10-4 M was remakably by Goosunsan extract. 4. The contractile response of the ileum smooth muscle of the isolated guinea pig to histamine 10-4 M was remakably by Goosunsan extract. 5. The contractile response of the trachea smooth muscle of the isolated guinea pig to acetylcholine 10-4 M was remakably by Goosunsan extract. 6. The contractile response of the ileum smooth muscle of the isolated guinea pig to acetylcholine 10-4 M was remakably by Goosunsan. 7. The contractile response of the trachea smooth muscle of the isolated guinea pig to 5-hydroxytryptamine 10-4 M was remakably by Goosunsan. 8. The contractile response of the ileum smooth muscle of the isolated guinea pig to 5-hydroxytryptamine 10-4 M was remakably by Goosunsan.

• Biomolecules & Therapeutics
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• 제9권1호
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• pp.51-54
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• 2001

Bufonis Venenum is a toad venom and its main components are bufadienolides, namely resibufogenin, bufalin and cinobufagin. The desensitizing effect of Bufonis Venenum is useful for the treatment of the premature ejaculation in Chinese medicine. But, minor components of Bufonis Venenum cause problems such as topical burring, pain, and erectile dysfunction. To clarify and eliminate the components responsible for these side effects, we prepared two extracts of Bufonis Venenum with either 70% ethanol or ethylacetate and tested their pharmacological effects. The extract of Bufonis Venenum with 70% ethanol produced pain response in rat hind paw, and exhibited contraction of rabbit corpus cavernosal muscle in vitro. On the other hand, the ethylacetate extract did not cause pain and smooth muscle contraction. The desensitizing effect of the ethylacetate extract was similar to that of the 70% ethanol extract. In conclusion, these results show that the extract of Bufonis Venenum with ethylacetate does not have the components causing side effects and deserve further study for therapeutic potential in premature ejaculation in men.

• The Korean Journal of Physiology and Pharmacology
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• 제21권6호
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• pp.687-694
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• 2017

Plumbagin, a hydroxy 1,4-naphthoquinone compound from plant metabolites, exhibits anticancer, antibacterial, and antifungal activities via modulating various signaling molecules. However, its effects on vascular functions are rarely studied except in pulmonary and coronary arteries where NADPH oxidase (NOX) inhibition was suggested as a mechanism. Here we investigate the effects of plumbagin on the contractility of skeletal artery (deep femoral artery, DFA), mesenteric artery (MA) and renal artery (RA) in rats. Although plumbagin alone had no effect on the isometric tone of DFA, $1{\mu}M$ phenylephrine (PhE)-induced partial contraction was largely augmented by plumbagin (${\Delta}T_{Plum}$, 125% of 80 mM KCl-induced contraction at $1{\mu}M$). With relatively higher concentrations (>$5{\mu}M$), plumbagin induced a transient contraction followed by tonic relaxation of DFA. Similar biphasic augmentation of the PhE-induced contraction was observed in MA and RA. VAS2870 and GKT137831, specific NOX4 inhibitors, neither mimicked nor inhibited ${\Delta}T_{Plum}$ in DFA. Also, pretreatment with tiron or catalase did not affect ${\Delta}T_{Plum}$ of DFA. Under the inhibition of PhE-contraction with L-type $Ca^{2+}$ channel blocker (nifedipine, $1{\mu}M$), plumbagin still induced tonic contraction, suggesting $Ca^{2+}$-sensitization mechanism of smooth muscle. Although ${\Delta}T_{Plum}$ was consistently observed under pretreatment with Rho A-kinase inhibitor (Y27632, $1{\mu}M$), a PKC inhibitor (GF 109203X, $10{\mu}M$) largely suppressed ${\Delta}T_{Plum}$. Taken together, it is suggested that plumbagin facilitates the PKC activation in the presence of vasoactive agonists in skeletal arteries. The biphasic contractile effects on the systemic arteries should be considered in the pharmacological studies of plumbagin and 1,4-naphthoquinones.

• 대한약학회:학술대회논문집
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• 대한약학회 2001년도 Proceedings of the Pharmaceutical Society of Korea
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• pp.99.1-99.1
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• 2001

• Tuberculosis and Respiratory Diseases
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• 제38권1호
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• pp.8-15
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• 1991

It has been well known that the integrity of airway epithelium is important in development of bronchial hyperreactivity and bronchial asthma. But the mechanisms involved are still unclear. To evaluate that airway epithelium is able to modulate the contraction of guinea pig tracheal smooth muscle, we investigated the responsiveness of intact and epithelium-denuded tracheal strips to histamine and acetylcholine. And to evaluate whether cyclooxgenase products play a role in this modulatory mechanism, we also investigated the effect of indomethacin pretreatment on the tracheal responsiveness to histamine. Results were as follows: 1) In guinea pig tracheal smooth muscle the presence of airway epithelium significantly reduced the response to histamine. 2) In the presence of indomethacin dose-response curves and $EC_{50}$ values were similar between intact and epithelium-denuded tracheal strips, that is, indomethacin abolished the influence of epithelium on the contracion of tracheal smooth muscle. 3) The response of tracheal smooth muscle to acetylcholine was similar both in the presence and absence of epithelium. These results suggest that airway epithelium of guinea pig may generate an inhibitory signal to decrease the response of tracheal smooth muscle to histamine and cyclooxygenase products may contrbute to the modulation of airway epithelium on the contracion of tracheal smooth muscle.

• The Korean Journal of Physiology
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• 제28권2호
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• pp.159-167
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• 1994

The contraction of rabbit basilar artery was examined as a function of changes in the $Na^+$ electrochemical gradient in order to determine the contribution of $Na^+/Ca^{2+}$ exchange to the modulation of contractility. Ouabain $(10^{-5}\;M)$ or $K^+-free$ Tyrode solution caused an increase in tonic tension even in the presence of a $Ca^{2+}$ channel blocker $(10^{-6}\;M\;verapamil)$ and an ${\alpha}-receptor$ blocker $(10^{-5}\;M\;phentolamine)$. After treatment with ouabain $(10^{-5}\;M)$, contractions were augmented by reduction of external $Na^+$ concentration. The longer the treatment with ouabain $(10^{-5}\;M)$ was, the larger the amplitude of $Na^+-free$ contracture was. $Na^+-free$ contracture wag induced by either substitution of equimolar Tris for $Na^+$ or substitution of equimolar $Li^+\;for\;Na^+$. The competition between $Na^+\;and\;Ca^{2+}$ for the $Na^+/Ca^{2+}$ exchange carrier would exist, because it was observed that contractility was dependent on the $Na^+$ electrochemical gradient or the extracellular $Ca^{2+}$ concentration (2 mM, 4 mM). Ryanodine $(10^{-7}\;M)$, the blocker of intracellular $Ca^{2+}$ release from the sarcoplasmic reticulum, did not suppress the development of $Na^+-free$ contracture. The contractile response to norepinephrine $(10^{-6}\;M)$ was augmented by reducing the extracellular $Na^+$ concentration. The relaxation rate from caffeine-induced contraction was dependent on the extracellular $Na^+$ concentration (0 mM, 140 mM). From the above results, it could be suggested that $Na^+/Ca^{2+}$ exchange can move $Ca^{2+}$ either into or out of rabbit basilar arterial smooth muscle. $Ca^{2+}$ entry or extrusion is dependent upon the $Na^+$ electrochemical gradient. $Na^+/Ca^{2+}$ exchange plays a significant role in the regulation of contractility in rabbit basilar arterial smooth muscle.

• 대한한방내과학회지
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• 제28권4호
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• pp.797-807
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• 2007

Objectives : The purpose of this study was to investigate whether Mahwangyunpye-tang(MYT) significantly affects mucin secretion from airway epithelial cells. Methods : Confluent hamster tracheal surface epithelial (HTSE) cells were metabolically radiolabeled with 3H-glucosamine for 24 hrs and chased for 30 min in the presence of MYT to assess the effect of the agent on 3H-mucin secretion. Total elution profiles of control spent media and treatment sample through Sepharose CL-4B column were analyzed. Effect of MYT on contractility of isolated tracheal smooth muscle was investigated; also investigated was effect of the agent on MUC5AC gene expression in cultured NCI-H292 cells. Possible cytotoxicities of the agent were assessed both by measuring lactate dehydrogenase (LDH) release from HTSE cells and examining the rate of survival and proliferation of NCI-H292 cells. Results : MYT significantly increased mucin secretion from cultured HTSE cells, without significant cytotoxicity. MYT chiefly affected the 'mucin' secretion. MYT inhibited Acetylcholine-induced contraction of isolated tracheal smooth muscle. MYT did not significantly affect the expression levels of MUC 5AC gene in cultured NCI-H292 cells. Conclusions : Based on the above results, it is suggested that MYT increased mucin secretion from cultured HTSE cells without significant cytotoxicity and inhibited contraction of isolated tracheal smooth muscle.

• 대한한의학회지
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• 제17권2호
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• pp.296-302
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• 1996

Pericarpium Citri Nobilis Viride, a traditional herb medicine, has been used in Korea and China for many centuries as a treatment for respiratory disease. The purpose of the present study was to determine the effect of Pericarpium Citri Nobilis Viride on histamine-induced tracheal smooth muscle contraction in rats. Guinea pigs(500g , female) were killed by $CO_2$ exposure and a segment (8-10mm) of the thoracic trachea from each guinea pig was cut into equal segments and mounted 'in pairs' in a tissue bath. Contractile force was measured with force displacement transducers under 0.5g loading tension. The dose of histamine which evoked 50% of maximal response $(ED_{50})$ was obtained from cumulative dose response curves for histamine $(10^{-7}-10^{-4}M)$. Contractions evoked by histamine ($ED_{50}$) were inhibited significantly by Pericarpium Citri Nobilis Viride. The mean percent inhibition was 53.7% (P<0.05) after 1.5mg／ml Pericarpium Citri Nobilis Viride, and 87.7% (P<0.01) after 5.0mg／ml Pericarpium Citri Nobilis Viride. Propranolol $(10^{-7}M)$ slightly but significantly attenuated the inhibitory effects of Pericarpium Citri Nobilis Viride. Following treatment with propranolol the mean present inhibition caused by 1.5 and 5.0mg／ml Pericarpium Citri Nobilis Viride. Indomethacin and methylene blue $(10^{-7}M)$ did not significantly alter the inhibitory effect of Pericarpium Citri Nobilis Viride These results indicate that Pericarpium Citri Nobilis Viride can relax histamine-induced contraction of guinea pig tracheal smooth muscle, and that this inhibition involves in part symphathetic nerve system.