• 통합자연과학논문집
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• 제10권1호
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• pp.7-13
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• 2017

Neuromedin U receptor 1 is a GPCR protein which binds with the neuropeptide, neuromedin. It is involved in the regulation of feeding and energy homeostasis and related with immune mediated inflammatory diseases like asthma. It plays an important role in maintaining the biological clock and in the regulation of smooth muscle contraction in the gastrointestinal and genitourinary tract. Analysing the structural features of the receptor is crucial in studying the pathophysiology of the diseases related to the receptor important. As the three dimensional structure of the protein is not available, in this study, we have performed the homology modelling of the receptor using 5 different templates. The models were subjected to model validation and two models were selected as optimal. These models could be helpful in analysing the structural features of neuromedin U receptor 1 and their role in disorders related to them.

• International Journal of Oral Biology
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• 제43권3호
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• pp.113-121
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• 2018

Taste is closely related to intake of food. Taste perception is also influenced by type of food ingested, and nutrition and health status. Bitter taste plays an important role in the survival of human and animals to avoid probable toxic and harmful substances. Vertebrate animals recognize bitter taste through type 2 taste receptors (T2Rs). Several T2Rs have been expressed extra-oral such as the gastrointestinal tract, respiratory tract, urogenital tract, brain and immune cells, and parts of their functions are being revealed. This review will discuss physiological roles of T2Rs in relation to innate immunity, secretion and smooth muscle contraction expressed in extra-oral cells and tissues, and we summarize relationships between polymorphisms in T2Rs and general or oral diseases. It is not a coincidence that animals pay much genetic costs for taste and smell during evolution.

• 사상체질의학회지
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• 제5권1호
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• pp.157-173
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• 1993

In order to investigate experimentally the clinical effects of Soeuminsohaphyangwon that was prescribed to cure the Wisunanrihanbyung of Soeum-In, the author experimented various activities of mixed extract from the Soeuminsohaphyangwon by the method prescribed in the experimental part. The results of the studies were summerized as follows : 1. Suppressive action was not shown on the convulsion induced by strychnine but significant effect was noted on the convulsion induced by picrotoxin and caffeine. 2. In acetic acid method experiment analgesic effect was noted. 3. A prolongation of anesthetic time by Pentobarbital sodium and antipyretic effect was observed. 4. Relaxing action was noted on the ileums of mice, also same effect was recognized on contraction of the ileums due to acetylcholine, barium chloride and histamine 2 HCl. 5. The expansion of blood vessels by relaxation of smooth muscle and fall of blood pressure were noted. According to the above results, effects based on oriental medical references were approximate to the actual experimental results.

• Biomolecules & Therapeutics
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• 제10권4호
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• pp.258-267
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• 2002

In this study the general pharmacological profiles of AS6 on the central nervous system, cardiovascular and the other organs were investigated. The dosages given were 0, 250, 500 and 1000 mg/kg and drugs were orally administered. The animals used for this study were mice, rats and guinea pigs. Significant increases (p<0.01) in the charcoal transport capacity were observed at the high dose of 1000 mg/kg and significant increases in retardation of pain threshold were observed in the test using acetic acid in all dosed animals. However, AS6 showed no noticeable effects on general behavior, motor coordination, spontaneous locomotor activity, hexobarbital-induced sleep time, body temperature, analgesic activity in the test using hot plate method and anticonvulsant activity. Furthermore no noticeable effects were observed in cardiovascular functions in the isolated rat heart, contraction and relaxation of the smooth muscle in the isolated guinea ileum, gastric secretion and renal function.

• Journal of Periodontal and Implant Science
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• 제26권4호
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• pp.1003-1012
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• 1996

The induction of a phenotype with preoperties may have clinical significance in the acceleration of the wound-healing process. Wound contraction involves a specialized cell known as the myofibroblast. The myofibroblasts can be identified by their intense staining of actin bundles with anti-actin antibody. Tissue-specific actin distribution is correlated with the contractile activity of the myofibroblasts and smooth muscle etc. This study was performed to determine the expression of actin filaments in the cytoplasm of cultured human gingival fibroblsts after GaAs laser(BIOSAER, Korea) irradiation. Human gingival fibroblasts were cultured from explants of normal interdental gingival tissue. The third-generation fibroblasts were used for immunohistochemical study. The cultured fibroblasts were exposed $0.53joule/cm^2$(lmW, 7 mimutes) of energy density, and then observed by immunohistochemical method using, rabbit anti0gelsolin, hen smooth muscle polyclonal antibody(Chemicon international inc.), and biotinylated goat anti-rabbit IgG(Vectastain) 24-, 36-, 48-hour after laser irradiation Following results were obtained ; 1. In nonirradiated cultures, round shaped active fibroblasts with abundant cytoplasm and prominet nucleoli were observed. 2. In 24- and 36-hour cultures after laser irradiation, spindle shaped cells with long process were observed. The intensity of stain was seen in cytoplasm of these modified fibroblasts. 3. In 48-hoour cultures after laser irradiation, stained spindle shape cell were not observed. The results suggest that the effect of the galium-arsenide laser treatment on cultured gingival fibroblasts is the rapid development of cytoplasmic actin filaments.

• Biomolecules & Therapeutics
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• 제10권1호
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• pp.19-24
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• 2002

The effects of a newly synthesized $H^+/K^+$ ATPase inhibitor,1-(2-methyl-4-methoxypheny)-4-[(3-hy-droxypropyl)amino] -6-methyl-2,3-dihydropyrrolo (3,2-c) quinoline (DBM-819) , on the central nervous system, isolated smooth muscle, cardiovascular and digestive systems and renal function were investigated in various experimental animals. Oral administration of DBM-819 had no effect on the central nervous system except body temperature of mice slightly decreased at doses of 15 and 50 mg／kg. DBM-819 produced a moderate analgesic effect in acetic acid-induced writhing test in mice at 50 mg／kg (p.o.). In conscious rats, DBM-819 (15 and 50 mg／kg, p.o.) showed a slight increase in blood pressure and a small decrease in heart rate. DBM-819 had an significant effect on agonist-induced contraction of guinea pig ileum at $1.5{\times}10^{-5}g/ml.$ No significant effect of DBM-819 (5 and 15 mg／kg, i.p) on urinary volume or urinary excretion of $Na^+,\;K^+$ and Cl- was observed in rats. DBM-819 had no significant effect on intestinal transport of a semisolid meal in mice at 15 and 50 mg／kg (p.o.). These findings suggest that DBM-819 exerts no significant pharmacological effects on the central nervous system and renal function at 15 mg／kg (p.o.), but produces some effects on the smooth muscle and circulatory system.

• Biomolecules & Therapeutics
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• 제26권2호
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• pp.139-145
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• 2018

The present study was undertaken to investigate the influence of hypothermia on endothelium-independent vascular smooth muscle contractility and to determine the mechanism underlying the relaxation. Denuded aortic rings from male rats were used and isometric contractions were recorded and combined with molecular experiments. Hypothermia significantly inhibited fluoride-, thromboxane $A_{2-}$, phenylephrine-, and phorbol ester-induced vascular contractions regardless of endothelial nitric oxide synthesis, suggesting that another pathway had a direct effect on vascular smooth muscle. Hypothermia significantly inhibited the fluoride-induced increase in pMYPT1 level and phorbol ester-induced increase in pERK1/2 level, suggesting inhibition of Rho-kinase and MEK activity and subsequent phosphorylation of MYPT1 and ERK1/2. These results suggest that the relaxing effect of moderate hypothermia on agonist-induced vascular contraction regardless of endothelial function involves inhibition of Rho-kinase and MEK activities.

• The Korean Journal of Physiology and Pharmacology
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• 제15권3호
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• pp.143-147
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• 2011

Defensins, cysteine-rich cationic polypeptides released from neutrophils, are known to have powerful antimicrobial properties. In this study, we sacrificed 30 rats to investigate the effects of ${\alpha}$-defensin 1 on detrusor muscle contractions in isolated rat bladder. From the experiments we found relaxing effects of ${\alpha}$-defensin 1 on the contractions induced by phenylephrine (PE) but not by bethanechol (BCh) in the detrusor smooth muscles. To determine the mechanisms of the effects of ${\alpha}$-defensin 1, the changes of effects on PE-induced contraction by ${\alpha}$-defensin 1 pretreatment were observed after pretreatment of Rho kinase inhibitor (Y-27632), protein kinase C (PKC) inhibitor (Calphostin C), potent activator of PKC (PDBu; phorbol 12,13-dibutyrate), and NF-${\kappa}B$ inhibitors (PDTC; pyrrolidinedithiocarbamate and sulfasalazine). The contractile responses of PE ($10^{-9}{\sim}10^{-4}$ M) were significantly decreased in some concentrations of ${\alpha}$-defensin 1 ($5{\times}10^{-9}$ and $5{\times}10^{-8}$ M). When strips were pretreated with NF-kB inhibitors (PDTC and sulfasalazine; $10^{-7}{\sim}10^{-6}$ M), the relaxing responses by ${\alpha}$-defensin 1 pretreatment were disappeared. The present study demonstrated that ${\alpha}$-defensin 1 has relaxing effects on the contractions of rat detrusor muscles, through NF-${\kappa}B$ pathway. Further studies in vivo are required to clarify whether ${\alpha}$-defensin 1 might be clinically related with bladder dysfunction by inflammation process.

• The Korean Journal of Physiology and Pharmacology
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• 제21권6호
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• pp.609-616
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• 2017

Ardipusilloside-I is a natural triterpenoid saponin, which was isolated from Ardisia pusilla A. DC. The aim of the study was to evaluate the stimulation of ardipusilloside-I on gastrointestinal motility in vitro and in vivo. The experiment of smooth muscle contraction directly monitored the contractions of the isolated jejunal segment (IJS) in different contractile states, and the effects of ardipusilloside-I on myosin were measured in the presence of $Ca^{2+}$-calmodulin using the activities of 20 kDa myosin light chain ($MLC_{20}$) phosphorylation and myosin $Mg^{2+}$-ATPase. The effects of ardipusilloside-I on gastro emptying and intestinal transit in constipation-predominant rats were observed, and the MLCK expression in jejuna of constipated rats was determined by western blot. The results showed that, ardipusilloside-I increased the contractility of IJS in a dose-dependent manner and reversed the low contractile state (LCS) of IJS induced by low $Ca^{2+}$, adrenaline, and atropine respectively. There were synergistic effects on contractivity of IJS between ardipusilloside-I and ACh, high $Ca^{2+}$, and histamine, respectively. Ardipusilloside-I could stimulate the phosphorylation of $MLC_{20}$ and $Mg^{2+}$-ATPase activities of $Ca^{2+}$- dependent phosphorylated myosin. Ardipusilloside-I also stimulated the gastric emptying and intestinal transit in normal and constipated rats in vivo, respectively, and increased the MLCK expression in the jejuna of constipation-predominant rats. Briefly, the findings demonstrated that ardipusilloside-I could effectively excite gastrointestinal motility in vitro and in vivo.

• Journal of Yeungnam Medical Science
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• 제10권1호
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• pp.144-156
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• 1993

Octreotide는 somatostatin 동족체로서 8개의 aminoacid로 구성된 합성 polypeptide이다. 이는 외분비선과 내분비선, 특히 위의 분비기능과 췌장분비 기능을 억제하는 작용이 강하며 somatostatin에 비하여 체내 반감기가 길고 장기에 대한 선택성이 높기 때문에 소화성 궤양에 의해 유발되는 출혈, 급성췌장염, 그리고 소화기관의 분비선에 나타나는 종양의 치료에 대한 적용이 시도되고 있다. 저자등은 somatostatin이 말초 교감신경에 존재하며, 신경전달인자 또는 신경조정인자로서 작용할것이라는 보고와 임상적용시 혈압과 심박동수를 감소시킨다는 보고에 흥미를 가지고 그 유도체인 octreotide가 말초 교감신경에 미치는 작용을 관찰하기 위하여 다음과 같은 실험을 하였다. 흰쥐 (Sprague-Dawley)의 전립선 부위 정관 절편을 적출 근편 실험조에 현수하여 등척성 장력을 측정하였다. 흰쥐 적출정관은 전기장 자극(duration : 1 mSec, voltage: 50 V, frequency: 5 Hz or 30 Hz, train: 10 Sec)에 대하여 first phasic component (FPC)와 second tonic component (STC)로 구성된 수축 반응을 나타내었으며, 이러한 수축반응은 tetrodotoxin($10^{-6}M$) 전처치로 소실되었다. Octreotide는 전기장 자극에 의해 유발되는 수축 반응을 FPC, STC 모두 농도의존적으로 억제하였다. 그리고 24 시간 전에 reserpine(1 mg/kg, IP)을 전처치하여 norepinephrine을 고갈시킨 흰쥐에서 적출한 정관 절편과 beta-gamma-methylene ATP를 전처치하여 퓨린성 수용체를 탈감작시킴으로써 ATP의 작용을 배재한 정관절편의 전기장 유발 수축을 공히 억제하였다. 이러한 octreotide의 모든 수축 억제 작용들은 5 Hz의 전기장 자극을 가하였을 때, 30 Hz의 전기장 자극을 가하였을 때 보다 더 강하게 나타났다. 그러나 octreotide는 정관 절편의 기본장력에는 영향을 미치지 않았으며, 외부에서 첨가한 norepinephrine과 ATP에 의해 유발되는 수축반응에는 영향을 미치지 않았다. 이상의 결과로 미루어 보아 octreotide는 흰쥐적출 정관의 교감신경성 신경원으로부터 ATP와 norepinephrine의 유리를 억제함으로써 그 수축성을 억제하는 것으로 사료된다.