• Title/Summary/Keyword: ${\beta}3$-adrenergic receptor

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The Effects of Cholates on Smooth Muscle Strips and Cardiac Muscle (담즙산(膽汁酸)이 수종평골근(數種平滑筋) 및 심근표본(心筋標本)에 미치는 영향(影響))

  • Ro, J.Y.;Cho, T.S.;Hong, S.S.
    • The Korean Journal of Pharmacology
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    • v.16 no.1 s.26
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    • pp.41-50
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    • 1980
  • Chenodeoxycholic acid(CDCA) has been used as a gallstone dissolving agent since 1972. Recently, ursodeoxycholic acid(UDCA) has been reported to be effective in dissolving gallstones. Both bile acids increased bile flow. The increase in bile flow associated with an increase in cholesterol level in bile after CDCA or UDCA infusion was reported. In this study, using the smooth muscle strips of guinea pig and fowl, responses of the cholates were observed. In addition, the influence of adrenergic blocking agents on the response of the strips to cholates was investigated. Also the effects of cholates on cardiac function were examined by using isolated atria of rabbit and heart of anesthetized frog. The results are as follows: 1) All cholates, such as UDCA, CDCA, and CA produced a marked inhibitory effect on the motility in isolated duodenal strip of guinea pig and fowl, however, only UDCA showed the contraction in the isolated esophagus of fowl. These effects of cholates were blocked by propranolol. 2) In isolated guinea pig stomach strip and gall bladder, cholates exhibited a marked inhibitory effect on the motility and the effects due to UDCA and CA were blocked by phenoxybenzamine while CDCA was not affected. 3) The spontaneous and ouabain induced arrhythmia was partially abolished by cholates. However, concomitant administration of cholates with ouabain or epinephrine caused a marked prolongation in occurrence of atrial arrhythmia in comparison with ouabain or epinephrine alone in isolated rabbit atria. 4) In the heart of anesthetized frog, the epinephrine-induced arrhythmia was partially abolished by cholates. The combined treatment with cholates and ouabain or epinephrine produced a marked prolongation in occurrence of the arrhythmia in comparison with, ouabain or epinephrine alone. From the above results, it can be suggested that the effects of cholates on the smooth muscle of duodenum and esophagus are produced in response to adrenergic ${\beta}$-receptor and the effect or gall bladder and stomach is more likely due to the direct effect on the muscle. In addition, cholates exhibit a slight antiarrhythmic effect on heart, therefore, cholates can be classified as a nonselective antiarrhythmic drug, such as propranolol.

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Effect of Soumin Seonghyangjeongkisan Extract on Blood Pressure and Regional Cerebral Blood Flow in Rats (소음인(少陰人) 성향정기산(星香正氣散)이 백서(白鼠)의 혈압(血壓) 및 국소뇌혈류량(局所腦血流量)에 미치는 영향(影響))

  • Lee, Ki-ju;Kim, Kyung-yo
    • Journal of Sasang Constitutional Medicine
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    • v.12 no.1
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    • pp.228-239
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    • 2000
  • 1. Purpose : For many years, Soumin Seonghyangjeongkisan(少陰人 星香正氣散, SJ) has been used in Sasang(四象) constitutional medicine as a therapeutic agent for cerebral disease. The effects of SJ on the vascular system is not well-know. The purpose of this study is to make it clear the effects of SJ and composing drugs on blood pressure(BP) and regional cerebral blood flow(rCBF). 2. Method : We measured BP with Pressure Transducer, rCBF with Laser-Doppler flowmeter. Propranolo and methylene blue were used to determine the mechanisms of SJ effects. 3. Results and Conclusion : BP was not affected by SJ in rats, and rCBF was significantly increased by SJ in rats. rCBF was increased by Folium Perillae(蘇葉), Rhizoma Atractylodis(蒼朮), Pericarpium Arecae(大腹皮) and Rhizoma Arisaematic(南星), but decreased by Radix Saussurea(木香) in rats. The increase of rCBF is mediated by adrenergic ${\beta}-receptor$ and guanylyl cyclase which is enzyme producing cyclic GMP.

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Effect of Taeumin Chungsimyoinjatang Extract on Blood Pressure and Regional Cerebral Blood Flow in Rats (태음인(太陰人) 청심연자탕(淸心連子湯)이 백서(白鼠)의 혈압(血壓) 및 국소뇌혈류량(局所腦血流量)에 미치는 영향(影響))

  • Park, Jae-hyung;Kim, Kyung-yo
    • Journal of Sasang Constitutional Medicine
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    • v.12 no.1
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    • pp.216-227
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    • 2000
  • 1. Purpose For many years, Taeumin Chungsimyoinjatang(太陰人 淸心蓮子湯, CS) has been used in Sasang(四象) constitutional medicine as a therapeutic agent for cerebral disease. The effects of CS on the vascular system is not well-known. The purpose of this study is to make it clear the effects of SJ and composing drugs on blood pressure(BP) and regional cerebral blood flow(rCBF). 2. Method We measured BP with Pressure Transducer, rCBF with Laser-Doppler flowmeter. Propranolol and methylene blue were used to determine the mechanisms of CS effects. 3. Results and Conclusion BP was not affected by CS in rats, and rCBF was significantly increased by CS in rats. rCBF was increased by Nelumbinis Semen(蓮于肉), Ophiopogonis Radix(麥門冬), Asparagi Radix(天門冬), Polygalae Radix(遠志), Zizyphi Spinosae Semen(酸棗仁), Longnae Arillus(龍眼肉), Raphani Semen, Chrysanthemi Flos(甘菊) in rats. The increase of rCBF is mediated by adrenergic ${\beta}$- receptor and guanylyl cyclase which is enzyme producing cyclic GMP.

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Alterations of Heart Rate Variability upon β3-Adrenergic Receptor Polymorphism and Combined Capsaicin, Sesamin, and L-Carnitine in Humans (복합 캡사이신, 세사인, 그리고 카르니틴과 베타3 유전자 다형에 대한 심박수 변이성의 영향)

  • Shin, Ki-Ok;Kim, Hyun-Jun;Kang, Sung-Hwun
    • Journal of Life Science
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    • v.18 no.3
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    • pp.291-297
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    • 2008
  • We investigated whether 1) the combined capsaicin (75 mg), sesamin (30 mg), and L-carnitine (900 mg) (CCSC) ingestion enhances autonomic nervous system (ANS) activities including thermogenic sympathetic activity as energy metabolic modulator, 2) ${\beta}_3-AR$ polymorphism of each subject influences with ANS activity. Seven healthy males $(22.0{\pm}0.5\;yr)$ volunteered for this study. The cardiac autonomic nervous activities evaluated by means of heart rate variability of power spectral analysis were continuously measured during 5 min every 30 min for total 120 min resting condition with CCSC or placebo oral administration chosen at random. The results indicated that, there are not $Arp/Arg^{64}$ variants of the ${\beta}_3-AR$ genotypes in our subjects. There were not also significant differences in heart rate during rest between both trials. The difference of ANS activity did not reach the statistical significance between both trials. However, the significant improvement showed TOTAL power, HF component, and the indices of SNS and PNS activities before and at 30 min after CCSC ingestion (p<0.05, respectively). In conclusions, although each component of combined CCSC is associated with lipolysis and/or fat oxidation, the combined CCSC consumption is not influenced in stimulation of thermogenic sympathetic activity as modulator of energy metabolism. In rather, our results suggested that CCSC ingestion improves the balance of both SNS and PNS activities. Therefore, it will be considered many combined nutrient components for ergogenic and/or lipolysis effects as well as genetic variants affecting ANS activity in further studies.

Effect of dietary supplementation with Spirulina on the expressions of AANAT, ADRB3, BTG2 and FASN genes in the subcutaneous adipose and Longissimus dorsi muscle tissues of purebred and crossbred Australian sheep

  • Kashani, Arash;Holman, Benjamin William Behrens;Nichols, Peter David;Malau-Aduli, Aduli Enoch Othniel
    • Journal of Animal Science and Technology
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    • v.57 no.3
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    • pp.8.1-8.8
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    • 2015
  • Background: The demand for healthy, lean and consistent meat products containing low saturated fatty acid content and high quality polyunsaturated fatty acids (PUFA), especially long-chain (${\geq}C_{20}$) omega-3 PUFA, has increased in recent times. Fat deposition is altered by both the genetic background and dietary supplements, and this study aimed to assess the effect of dietary Spirulina supplementation levels on the mRNA expression patterns of genes controlling lipid metabolism in the subcutaneous adipose tissue (SAT) and Longissimus dorsi (ld) muscle of Australian crossbred sheep. Methods: Twenty-four weaned lambs belonging to four breeds under the same management conditions were maintained on ryegrass pasture and fed three levels of Spirulina supplement (control, low and high). In terms of nutrient composition, Spirulina is a nutrient-rich supplement that contains all essential amino acids, vitamins and minerals. It also is a rich source of carotenoids and fatty acids, especially gamma-linolenic acid (GLA) that infer health benefits. After slaughter, subcutaneous adipose tissue (SAT) and ld samples were subjected to mRNA extraction and reverse transcription using quantitative polymerase chain reaction (RT-qPCR) to assess the mRNA expression levels of the Aralkylamine N-acetyltransferase (AANAT), Adrenergic beta-3 receptor (ADRB3), B-cell translocation gene 2 (BTG2) and Fatty acid synthase (FASN) genes, which are associated with lipid metabolism. Results: Both low and high Spirulina supplementation levels strongly up-regulated the transcription of all the selected genes in both SAT and ld tissues (mostly in the subcutaneous adipose), but sheep breed and sex did not influence the gene expression patterns in these tissues. Conclusions: The evidence indicates that high Spirulina supplementation level resulted in a decrease in intramuscular fat content in Australian purebred and crossbred sheep due to the enhanced production of melatonin in sheep muscle tissues and strong up-regulation of mRNA expression of BTG2 in SAT which negatively affected fat deposition. In contrast, low Spirulina supplementation level strongly up-regulated the ADRB3 and FASN genes responsible for fat production. These findings are consistent with the observed phenotypic data suggesting that low Spirulina supplementation level can increase lamb production, with higher long-chain PUFA content.

Inhibitory Effects of ${\gamma}$-Aminobutyric Acid on the Contractility of Isolated Rat Vas Deferens (흰쥐의 적출 정관 수축성에 대한 ${\gamma}$-Aminobutyric Acid의 억제작용)

  • Ahn, Ki-Young;Kwon, Oh-Cheol;Ha, Jeoung-Hee;Lee, Kwang-Youn;Kim, Won-Joon
    • Journal of Yeungnam Medical Science
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    • v.9 no.2
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    • pp.382-395
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    • 1992
  • GABA is an inhibitory neurotransmitter in central nervous system and produce sedative, antianxiety and muscle reaxing effects via $GABA_A$ receptor or $GABA_B$ receptor. Recently it is known that GABA is widely distributed throughout peripheral organs and may playa physiological role in certain organ. The vas deferens is innervated by species-difference. These study, therefore, was performed to investigate the mode and the mechanism of action of GABA on the norepiniphrine-, ATP- and electric stimulation-induced contraction of vas deferens of rat. Sprague-Dawley rats were sacrificed by cervical dislocation. The smooth muscle strips were isolated from the prostastic portion and were mounted in the isolated muscle bath. PSS in the bath was aerated with 95/5%-$O_2/CO_2$ at $33^{\circ}C$. Muscle tensions were measured by isometric tension transducer and were recorded by biological recording system. 1. GABA, muscimol, a $GAB_A$ agonist, and baclofen, a $GABA_B$ agonist inhibited the electric field stimulation(EFS, 0.2Hz, 1mSec, 80 V, monophasic square wave)-induced contraction with a rank order of potency of GABA greater than baclofen greater than muscimol. 2. The inhibitory effect of GABA was antagonized by delta aminovaleric acid(DAVA), a $GABA_B$ antagonist, but not by bicuculline, a $GABA_A$ mtagonist. 3. The inhibitory effect of baclofen was antagonized by DAVA, but the effect of muscimol was not antagonized by bicuculline. 4. Exogenous norepinephrine(NE) and ATP contracted muscle strip concentration dependently, but the effect of acetylcholine was negligible : and GABA did not affect the NE-and ATP-induced contractions. 5. GABA, baclofen and muscimol did not affect basal tone, and GABA did not affect the NE-and ATP-induced contractionsm 6. EFS-induced contraction was including 2 distinctable components. The first phasic component was inhibited by beta gamma-methylene ATP(mATP), a desensitizing agent of APT receptor and the second tonic component was reduced by pretreatment of reserpine(3 mg/Kg, IP). 7. GABA inhibited the EFS-induced contraction of reserpinized strips, but not the mATP-treated strips. These results suggest that in the prostatic portion of the rat vas deferens, adrenergic and purinergic neurotransmissions are exist, and GABA inhibits the release of ATP via presynaptic $GABA_B$ receptor on the excitatory neurons.

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Effects of Octreotide on the Contractility of Isolated Rat Vas Deferens (흰쥐 정관의 수축성에 미치는 Octreotide의 영향)

  • Jang, Sun-Ae;Kwon, Oh-Cheol;Ha, Jeoung-Hee;Lee, Kwang-Youn;Kim, Won-Joon
    • Journal of Yeungnam Medical Science
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    • v.10 no.1
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    • pp.144-156
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    • 1993
  • This study was performed to investigate the effect of octreotide on the contractility of rat vas deferens. The smooth muscle strips isolated from the prostatic portion were myographied in isolated organ bath, Electric field stimulation (monophasic square wave, duration: 1 mSec, voltage : 50 V, frequency : 5 Hz or 30 Hz, train: 10 Sec) produced reproducible contraction. The contraction was composed of two component, first phasic component (FPC) and second tonic component (STC). These contractions were abolished by tetrodotoxin ($1{\mu}M$). Octreotide inhibited the field stimulation induced contractions both FPC and STC concentration-dependently. The FPC was decreased by a desentization of purinergic receptor by pretreatment of mATP, and the STC was decreased by pretreatment of reserpine(3 mg/kg, IP) 24 hours before experiments. Octreotide reduced the field stimulation induced contraction in the presence of mATP and of reserpinized muscle strips. The inhibitory effect of octreotide was more potent at 5 Hz than at 30 Hz. Octreotide did not affect basal ton and exogenous norepinephrine- or ATP-induced contraction. These results suggest that octreotide inhibit the contractility of the isolated rat vas deferens by inhibition of the release of neurotransmitters, both ATP and norepinephrine from adrenergic nerve terminal.

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Obesity Regulation through Gut Microbiota Modulation and Adipose Tissue Browning (장내 미생물의 조절과 지방세포의 갈색지방화를 통한 비만 조절 연구)

  • Cho, Yejin;Shamim, Rahman Md.;Kim, Yong-Sik
    • Journal of Life Science
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    • v.29 no.8
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    • pp.922-940
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    • 2019
  • Obesity, represented by abnormal fat accumulation due to an imbalance between energy intake and expenditure, is a major public health issue worldwide, leading to multiple noncommunicable diseases, including atherosclerosis, hypertension, type 2 diabetes, and cancer. Diverse solutions have been proposed to combat obesity. Attention has focused on two types of adipose tissues as a promising therapeutic target in obesity: traditional brown and beige or brite. Unlike energy-storing white adipose (endocrine) tissue, traditional brown adipose tissue and beige adipose tissue have energy-dissipating thermogenic properties. Both types of tissue are present in adult humans and inducible through external stimuli, such as cold exposure, ${\beta}3$-adrenergic receptor agonists, and phytochemicals. Among these stimuli, microbiota present in the human intestinal tract participate in multiple metabolic activities. Modulation of gut microbiota may offer a potent and possibly curative strategy against various metabolic diseases. Numerous studies have focused on the effects of established antiobesity treatments on the gut microenvironment or brown-adipose-tissue activation. In this review, we focus mainly on stimuli known to alleviate obesity, weight gain, and metabolic diseases, in addition to known and possible inter-relations between gut microbiota modulation and similar interventions and adipose tissue browning. The findings may pave the way toward new strategies against obesity.