• 약학회지
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• 제58권5호
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• pp.337-342
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• 2014

The present study was undertaken to investigate the influence of diosgenin on vascular smooth muscle contractility and to determine the mechanism involved. We hypothesized that diosgenin, the primary ingredient of Dioscorea villosa, plays a role in vascular relaxation through inhibition of Rho-kinase in rat aortae. Denuded arterial rings from male Sprague-Dawley rats were used and isometric tensions were recorded using a computerized data acquisition system. Interestingly, diosgenin inhibited fluoride-induced contraction but didn't inhibit phorbol ester-induced contraction suggesting that additional pathways different from endothelial nitric oxide synthesis such as inhibition of Rho-kinase might be involved in the vasorelaxation. Furthermore, diosgenin didn't inhibit thromboxane $A_2$-induced increases in pERK1/2 levels suggesting the mechanism excluding inhibition of thromboxane $A_2$-induced increases in ERK1/2 phosphorylation. This study provides evidence that diosgenin induces vascular relaxation through inhibition of Rho-kinase in rat aortae.

• 생약학회지
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• 제14권2호
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• pp.51-59
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• 1983

Experimental studies were made with Melilotus officinalis extract which was extracted from flowers and leaves of Melilotus officinalis Dsr. (Leguminosae). In this paper, acute toxicity, analgesic action, prolongation of hypnosis time by induced pentobarbital-Nain mice, antiinflammatory effect in rats and effects on isolated intestines of mice and rats were studied, The result was as follows; 1. Very low toxicity in mice. 2. Analgesic action was recognized markedly in mice. 3. Prolongation of hypnosis time induced by pentobarbital-Na in mice was shown. 4. Relaxing action was shown on the isolated ileum in mice and antagonistic action was seen on $BaCl_2-induced$ contraction of the ileum that the relaxing effect of the intestinal smooth muscle was recognized. 5.Antiinflammatory effect was shown markedly in mice. 6.Hypotensive and vaso-dilating actions due to the vascular smooth muscle relaxation were noted in rabbits.

• 동의생리병리학회지
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• 제23권2호
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• pp.480-487
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• 2009

Atherosclerosis, slow progressing inflammatory lesion in arteries, is one of the major causes of cardiovascular diseases. As mortality due to cardiovascular disease keeps increasing in Korea, researches on pathological mechanism of atherosclerosis may be beneficial in fighting against cardiovascular diseases. It is known that migration and MMP-9 secretion of Vascular Smooth Muscle Cell(VSMC) play a significant part in pathogenesis of atherosclerosis, although detailed mechanism of entire process is not clarified. We investigated whether the seeds of Trichosanthes kirilowii maxim (TS), inhibit migration and MMP-9 production of HASMC(human aortic SMC), which were induced by TNF-${\alpha}$ treatment. Migration assay showed that TS inhibited the migration of HASMC induced by TNF-${\alpha}$, in dose dependent manner. Also by Zymography MMP-9 production of HASMC was found to be reduced by TS, both in time and in dose dependent manner. Western blotting results suggest TS suppress activity of MAPkinases.

• 생약학회지
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• 제15권4호
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• pp.188-193
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• 1984

It was previously indicated that 'Samulanshintang' had been examined for effects of the anticonvulsive, antipyretic, analgesic, sedative and antispasmodic actions. In order to investigate the effect on the cardiovascular system and anemic rabbits induced by phenlhydrazine HCl, pharmacological studies have been carried out with extract. The results of this investigation were summarized as follows: The relaxation of bronchial smooth muscle and antihistamine action were recognized. Antihypertensive and vasodilating actions due to vascular smooth muscle relaxation were noted in frogs and rabbits. 'Samulanshintang' lowered the rate of anemia induced by phenylhydrazine and rapidly recovered from the anemia state.

• 생약학회지
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• 제18권4호
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• pp.241-248
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• 1987

Woohwangchungsim-Won has been widely used for the treatment of appoplexy, hypertension, arteriosclerosis, insomnia and cerebrovascular accident, etc in oriental hospital and pharmacy. In order to investigate the efficacy of Woohwangchungsim-Won, the water extract of it were bioassayed for isolated ileum, blood vessels, blood pressure, heart and diuresis. The results of this studies were as follows; Spontaneous motilities of isolated ileum of mice were strongly suppressed, and contraction of isolated ileum of mice and guinea-pigs induced by acetylcholine chloride, barium chloride and histamine were inhibited. Vaso-dilating action due to vascular smooth muscle relaxation in frogs and rabbits, and hypotensive action in anesthetized rabbits were noted. Negative inotropic action on the isolated frog heart and diuretic effect in rabbits were shown.

• 한국생물물리학회:학술대회논문집
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• 한국생물물리학회 2002년도 제9회 학술 발표회 프로그램과 논문초록
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• pp.35-35
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• 2002

The large conductance $Ca^{2＋}$ -activated $K^{＋}$ channels ($BK_{Ca}$) in vascular smooth muscle have been considered to function as a negative feedback in pressure-induced vasoconstriction. In the present study, the function of cytoskeletons in the regulation of $BK_{Ca}$ and its stretch sensitivity was investigated. Using the inside-out patch clamp technique, we recorded single channel activities of $BK_{Ca}$ with 150 mM KCl in the bath solution (pCa=6.5).(omitted)itted)

• Journal of Chest Surgery
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• 제23권3호
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• pp.452-464
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• 1990

It is well known that extracellular Calcium plays a very important role in several steps of smooth muscle excitability and contractility, and there have been many concerns about factors influencing the distribution of extracellular Ca++ and the Ca++ flux through the cell membrane of the smooth muscle. Based on the assumption that Mg++ may also play an important role in the excitation and contraction processes of the smooth muscle by taking part in affecting Ca++ distribution and flux, many researches are being performed about the exact role of Mg++, especially in the vascular smooth muscle. But yet the effect of Mg++ in the smooth muscle activity is not clarified, and moreover the mechanism of Mg++ action is almost completely unknown. Present study attempted to clarify the effect of Mg++ on the excitability and contractility in the multiunit and unitary smooth muscle, and the mechanism concerned in it. The preparations used were the guinea-pig aortic strip as the experimental material of the multiunit smooth muscle and the rat uterine strip as the one of the unitary smooth muscle. The tissues were isolated from the sacrificed animal and were prepared for recording the isometric contraction. The effects of Mg++ and Ca++ were examined on the electrically driven or spontaneous contraction of the preparations. And the effects of these ions were also studied on the K+ or norepinephrine contracture. All experiments were performed in tris-buffered Tyrode solution which was aerated with 100% 02 and kept at 35oC. The results obtained were as follows: 1] Mg++ suppressed the phasic contraction induced by electrical field stimulation dose-dependently in the guinea-pig aortic strip, while the high concentration of Ca++ never recovered the decreased tension. These phenomena were not changed by the a - or b - adrenergic blocker. 2]Mg++ played the suppressing effect on the low concentration [20 and 40 mM] of K+-contracture in the aortic muscle, but the effect was not shown in the case of 100mM K+-contracture. 3] Mg++ also suppressed the contracture induced by norepinephrine in the aortic preparation. And the effect of Mg++ was most prominent in the contracture by the lowest [10 mM] concentration of norepinephrine. 4] In both the spontaneous and electrically driven contractions of the uterine strip, Mg++ decreased the amplitude of peak tension, and by the high concentration of Ca++ the amplitude of tension was recovered unlike the aortic muscle. 5] The frequency of the uterine spontaneous contraction increased as the [Ca++] / [Mg++] ratio increased up to 2, but the frequency decreased above this level. 6] Mg++ decreased the tension of the low[20 and 40mM] K+-contracture in the uterine smooth muscle, but the effect did not appear in the 100mM K+-contracture. From the above results, the following conclusion could be made. 1] Mg++ seems to suppress the contractility directly by acting on the smooth muscle itself, besides through the indirect action on the nerve terminal, in both the aortic and uterine smooth muscles. 2] The fact that the depressant effect of Mg++ on the K+-contracture is in inverse proportion to an increase of K+ concentration appears resulted from the extent of the opening state of the Ca++ channel. 3] Mg++ may play a depressant role on both the potential dependent and the receptor-operated Ca++ channels. 4] The relationship between the actions of Mg++ and Ca++ seems to be competitive in uterine muscle and non-competitive in aortic strip.

• The Journal of Korean Physical Therapy
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• 제14권4호
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• pp.454-474
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• 2002

Vasoactive intestinal peptide (VIP) is a very potent dilatator and a nonadrenergic, noncholinergic (NANC) neurotransmitter or neuromodulator in the peripheral and the central nervous systems. The mechanisms of action of VIP were examined in aortic circular and in uterine longitudinal smooth muscle strips of the rat. The effects of sympathetic neurotransmitter were investigated in gastric and aortic circular muscle strips of the mouse and the rat. The effects of silver spike point, SSP, low frequency electrical stimulations of VIP, sympathetic neurotransmitter and $\beta$-endorphin were examined in plasma, serum and 24h urine from the healthy volunteer. In gastric smooth muscle strips from the mouse, adrenergic neurotransmitter norepinephrine was inhibitory effected, followed by caused phasic and tonic contraction to the, muscrine receptor agonist carbachol and acetylcholine, respectively. In urine from the healthy volunteer, both norepinephrine and epinephrine were significantly decreased in continue type and low frequency (3 Hz) of SSP electrical stimulations. The contractile responses to S-HT in uterine longitudinal smooth muscle strips of the rats were completely decreased by a VIP 1 $\mu$M. The contractile responses to PGF2$\alpha$ were not decreased by a VIP. In plasma and serum from the healthy volunteer, both VIP and $\beta$-endorphin were significantly increased in continue type and low frequency (3 Hz) of SSP electrical stimulations. Therefore, this study demonstrate that VIP has the capacity to relax vascular or gastric smooth muscles in part by stimulating the generation of NO, and silver spike point low frequency electrical stimulation has the capacity both to decrease sympathetic neurotransmitters and to increase VIP, $\beta$-endorphin.

• 대한한의학회지
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• 제21권2호
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• pp.60-67
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• 2000

Objectives : Radix Angelicae Gigantis(RAG) and Resina Ferulae(RF) have been used in oriental medicine or folk medicine to increase stamina. The aim of this study was the characterization of the mechanism of action of RAG and RF on smooth muscle and macrophages in rats to find new substances for the treatment of erectile dysfunction, cardiovascular diseases and immune dysfunction. Methods : We investigated the effects of the water extracts of RAG and RF on phenylephrine or KCl-contracted rat endothelium-denuded aorta, the production of NO in vascular smooth muscle cell (VSMC) and the production of NO and induction of iNOS in the $IFN-{\gamma}-primed$ RAW 264.7 cells. Results : The water extracts of the RAG and RF showed significant concentration-dependent relaxation effects on phenylephrine or KCl-contracted rat endothelium-denuded aorta. It also reduced the tension of the rat endothelium denuded aorta which was contracted in $Ca^{2+}-free$ media. On the other hand, it increased production of NO in VSMC which was stimulated with $IL-{\beta}$ or $IL-{\beta}$ plus $IFN-{\gamma}$. The water extracts of RAG and RF increased production of NO and induction of iNOS in the $IFN-{\gamma}-primed$ RAW 264.7 cells. Conclusions : According to the above results, the water extracts of RAG and RF relaxed the smooth muscle effectively and increased the production of NO in VSMC and macrophages. So, these herbs can be applied to erectile dysfunction, hypertension, angina pectoris, artherosclerosis and a defense defect for virus or microbe.

• 대한한의학회지
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• 제31권6호
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• pp.47-57
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• 2010

Objective: The present study investigated the effect of ethanol extract of Cynanchum wilfordii (ECW) on vascular relaxation and vascular inflammation in rat artery isolated from rats and anti-inflammatory activity in human aortic smooth muscle cells (HASMC). Methods: Vascular tone and guanosine 3',5'-cyclic monophosphate (cGMP) production were examined in rat artery isolated from Sprague Dawley rats, in the presence of ECW. HASMC were incubated with tumor necrosis factor-alpha (TNF-${\alpha}$) or Angiotensin II for 24 h. Matrix metalloproteinase (MMP)-2 and anti-oxidant activity of ECW was investigated by pretreatment with ECW in HASMC. Results: Cumulative treatment of ECW relaxed aortic smooth muscles of rats in a dose-dependent manner. ECW-induced vasorelaxation was significantly decreased by pretreatment of L-arginine methyl ester (L-NAME) or oxadiazolo-quinoxalinone (ODQ). Furthermore, ECW treatment of thoracic aorta significantly increased cGMP production. Incubation of ECW with ODQ or L-NAME markedly decreased ECW-induced cGMP production. ECW treatment dose-dependently suppressed TNF-${\alpha}$- or Angiotensin II-induced increase in matrix metalloproteinase-2 expression in HASMC. Also, ECW exhibited 2,2-diphenyl-1-picrylhydrazyl radical scavenging activity in vitro and reduced TNF-${\alpha}$-induced increase in reactive oxygen species production in a dose-dependent manner. Conclusions: Taken together, the results suggest that ECW exerts vascular relaxation via NO/cGMP signaling pathway and decreases MMP-2 expression via anti-oxidant activity.