• Title/Summary/Keyword: Adenosine $A_1$-receptor

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Anti-Obesity Effects of Menthae Herba Hydrosol on High-Fat Diet Induced Obese Mice (고지방 식이로 유도된 비만 생쥐에서 박하 Hydrosol의 항비만 효과)

  • Soo-Min Choi;So-Young Kim;Young-Jun Kim;Chang-Hoon Woo;Mi-Ryeo Kim;Hee-Duk An
    • Journal of Korean Medicine Rehabilitation
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    • v.33 no.3
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    • pp.33-46
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    • 2023
  • Objectives We investigated anti-obesity effects of Menthae Herba hydrosol in obese mice. Methods Animals were divided into four groups, and treatments were performed for 7 weeks. After the treatment, serum lipid profiles, weight and pathological morphology in liver, kidney, adipose tissue were measured. Also, hepatic protein and gene expression levels of lipid metabolism-related factors were analyzed. Results Body weight was decreased in P3% group. In P1% (group fed high-fat diet and 1% Menthae Herba hydrosol) and P3% (group fed high-fat diet and 3% Menthae Herba hydrosol) group, weight of white adipose tissue, serum levels of triglyceride and blood urea nitrogen were decreased, and weight of muscle was increased. Also, liver, kidney and epididymal adipocyte size were reduced in P1% and P3% group. Adenosine monophosphate-activated protein kinase was increased and sterol regulatory element binding protein-1c (SREBP-1c) was decreased in P3% group. mPeroxisome proliferator-activator receptor-γ, mMonocyte chemotactic protein-1 were decreased in P1% and P3% group. In P3% group, mSREBP-1c was decreased and mCarnitine palmitoyl transferase-1 was increased. And mUncoupling protein 1 in brown adipose tissue was increased. Conclusions These results suggest that Menthae Herba hydrosol has a worthy effect on anti-obesity.

Therapeutic effect of Ferula assa-foetida oleo-gum resin in rats with letrozole-induced polycystic ovary syndrome

  • Amir Shieh;Seyyed Majid Bagheri;Maryam Yadegari;Davoud Javidmehr;Zeinab Farhadi
    • Clinical and Experimental Reproductive Medicine
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    • v.49 no.4
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    • pp.239-247
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    • 2022
  • Objective: Asafoetida is a gum derived from Ferula assa-foetida, which is used in traditional Iranian medicine to treat some reproductive system disorders. The effects of asafoetida on ovarian tissue, expression of certain genes associated with polycystic ovary syndrome (PCOS), and levels of liver, kidney, and blood cell factors after treatment in a rat model were investigated. Methods: Thirty rats were divided into five groups: normal, polycystic, and treatment with three doses of asafoetida (12.5, 25, and 50 mg/kg for 3 weeks after PCOS induction). PCOS was induced by letrozole at a dose of 1 mg/kg administered orally for 3 weeks. Blood samples were taken, and the ovaries were removed and prepared for histomorphometric examination. Liver and kidney parameters were measured. The mRNA expression levels of luteinizing hormone receptor, CYP11A1, adenosine monophosphate-activated protein kinase, adiponectin, and adiponectin receptors 1 and 2 were also measured by real-time polymerase chain reaction. Results: The levels of liver, kidney, and blood parameters did not significantly differ between the treatment groups and the control group. At doses of 25 and 50 mg/kg, ovarian histopathology, especially the thicknesses of the theca and granulosa layers, was significantly improved relative to the PCOS group. The expression of target genes also improved in the 25 and 50 mg/kg treatment groups. Conclusion: Asafoetida can be used to treat PCOS as a complementary approach to conventional therapies. Asafoetida appears to act by regulating and activating metabolic and ovarian cycle enzymes.

Anti-Oxidative and Anti-Obesity Activities of Tetrapanax papyriferus and Siegesbeckia pubescens Extracts and their Synergistic Anti-Obesity Effects (통초.희렴 추출물의 항산화.항비만 활성 및 혼합물의 항비만 시너지 효과)

  • Park, Jung Ae;Jin, Kyong-Suk;Lee, Ji Young;Kwon, Hyun Ju;Kim, Byung Woo
    • Microbiology and Biotechnology Letters
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    • v.41 no.3
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    • pp.341-349
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    • 2013
  • In this study, the anti-oxidative and anti-obesity activities of two medicinal herb extracts, Tetrapanax papyriferus (TP) and Siegesbeckia pubescens (SP), were evaluated using DPPH radical scavenging activity assay, lipase enzyme inhibition assay, and the cell culture model system. Both methanol extracts of TP and SP showed DPPH radical scavenging activities dose-dependently, and the $IC_{50}$ of DPPH radical scavenging activities of the two medicinal herbs were 65.23 and 47.79 ${\mu}g/ml$, respectively. Furthermore, both extracts suppressed effectively lipase enzyme activity dose-dependently. Moreover, TP and SP extracts significantly suppressed adipocyte differentiation, lipid accumulation, triglyceride (TG) contents on 3T3-L1 preadipocytes in a dose-dependent manner without cytotoxicity. Their anti-obesity effect was modulated by cytidine-cytidine-adenosine-adenosine-thymidine (CCAAT)/enhancer binding proteins ${\alpha}$ ($C/EBP{\alpha}$), $C/EBP{\beta}$ and peroxisome proliferator-activated receptor ${\gamma}$ ($PPAR{\gamma}$) gene and protein expressions. Furthermore, TP and SP possessed a synergistic effect on anti-obesity activity. The identification of the active compounds that confer the anti-obesity activity of TP and SP might be needed.

Facilitation of Glucose Uptake by Lupeol through the Activation of the PI3K/AKT and AMPK Dependent Pathways in 3T3-L1 Adipocytes (3T3-L1 지방세포에서 PI3K/AKT 및 AMPK 경로의 활성화를 통한 루페올의 포도당 흡수촉진 효과)

  • Lee, Hyun-Ah;Han, Ji-Sook
    • Journal of Life Science
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    • v.32 no.2
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    • pp.86-93
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    • 2022
  • Lupeol is a type of pentacyclic triterpene and has been reported to have pharmacological activities against various diseases; however, the effect of lupeol on glucose absorption has not been elucidated yet. This study aimed to investigate the effect of lupeol on glucose uptake in 3T3-L1 adipocytes. Lupeol significantly facilitated glucose uptake by translocating glucose transporter type 4 (GLUT4) to the plasma membrane of the 3T3-L1 adipocytes, which was related to activation of the phosphoinositide 3-kinase (PI3K)/protein kinase B (AKT) and 5 'adenosine monophosphate-activated protein kinase (AMPK) pathways. In the PI3K/AKT pathway, lupeol stimulates the phosphorylation of insulin receptor substrate 1 (IRS-1), which activates PI3K. Its activation by lupeol promotes the phosphorylation of AKT, but not the atypical protein kinase C isoforms ζ and λ. Lupeol also promoted the phosphorylation of AMPK. The activation of AMPK increased the expressions of the plasma membrane GLUT4 and the intracellular glucose uptake. The increase in the glucose uptake by lupeol was suppressed by wortmannin (PI3K inhibitor) and compound C (AMPK inhibitor) in the 3T3-L1 adipocytes. The results indicate that lupeol can facilitate glucose uptake by increasing insulin sensitivity through the stimulation of the expression of plasma membrane glucose transporter type 4 via the PI3K/AKT and AMPK pathways in the 3T3-L1 adipocytes.

Effects of Non-Steroidal Anti-Inflammatory Drugs on the FMLP-Induced Migration of Neutrophil (비스테로이드성 항염증제가 FMLP에 의한 사람 중성구의 이동에 미치는 영향)

  • Kim, Woo-Mi;Kang, Koo-Il
    • The Korean Journal of Pharmacology
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    • v.30 no.1
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    • pp.137-143
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    • 1994
  • Enhancement or diminution of leukocyte migration to the specific site might be important factors for the development of inflammatory diseases. To investigate the effects of non-steroidal anti-inflammatory drugs (NSAIDs) on chemotaxis of neutrophil, we obtained neutrophils by Hypaque-Ficoll step gradient centrifugation and tested the effects of seven drugs on the n-formyl-leucyl-phenylalanine (FMLP)-induced migration of neutrophil using a 48-well micro chemotaxis assembly. Oxyphenbutazone, phenylbutazone, sulindac, zomepirac, and ibuprofen suppressed the migration of neutrophil at the therapeutic concentrations, however, indomethacin showed stimulation effect. IC50s for inhibition of neutrophil migration by these drugs are less than 100uM. When drugs were preincubated with FMLP, no inhibition on migration of neutrophil was observed. These results indicated that inhibitory effects of these drugs on migration of neutrophil might be related to the receptor sites of neutrophil rather than molecular inactivation of chemoattractant (FMLP). In conclusion, we suggested that the property of inhibition effects on neutrophil migration of several NSAIDs might be another mode of pharmacological action for anti-iflammatory effect, which showed significant effects at concentrations below therapeutic levels, in addition to cyclooxygenase inhibition.

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Hippocampus-dependent cognitive enhancement induced by systemic gintonin administration

  • Kim, Sungmin;Kim, Min-Soo;Park, Kwanghoon;Kim, Hyeon-Joong;Jung, Seok-Won;Nah, Seung-Yeol;Han, Jung-Soo;Chung, ChiHye
    • Journal of Ginseng Research
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    • v.40 no.1
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    • pp.55-61
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    • 2016
  • Background: A number of neurological and neurodegenerative diseases share impaired cognition as a common symptom. Therefore, the development of clinically applicable therapies to enhance cognition has yielded significant interest. Previously, we have shown that activation of lysophosphatidic acid receptors (LPARs) via gintonin application potentiates synaptic transmission by the blockade of $K^+$ channels in the mature hippocampus. However, whether gintonin may exert any beneficial impact directly on cognition at the neural circuitry level and the behavioral level has not been investigated. Methods: In the current study, we took advantage of gintonin, a novel LPAR agonist, to investigate the effect of gintonin-mediated LPAR activation on cognitive performances. Hippocampus-dependent fear memory test, synaptic plasticity in the hippocampal brain slices, and quantitative analysis on synaptic plasticity-related proteins were used. Results: Daily oral administration of gintonin for 1 wk significantly improved fear memory retention in the contextual fear-conditioning test in mice.We also found that oral administration of gintonin for 1 wk increased the expression of learning and memory-related proteins such as phosphorylated cyclic adenosine monophosphate-response element binding (CREB) protein and brain-derived neurotrophic factor (BDNF). In addition, prolonged gintonin administration enhanced long-term potentiation in the hippocampus. Conclusion: Our observations suggest that the systemic gintonin administration could successfully improve contextual memory formation at the molecular and synaptic levels as well as the behavioral level. Therefore, oral administration of gintonin may serve as an effective noninvasive, nonsurgical method of enhancing cognitive functions.

The Changes of Cyclic AMP Content by Opiates in Chronic Haloperidol Treated Mouse Striatum (Haloperidol 장기 투여된 Mouse Striatum에서 cAMP양에 미치는 Opiates의 영향)

  • Kim, Soo-Kyung
    • The Korean Journal of Pharmacology
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    • v.30 no.1
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    • pp.11-18
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    • 1994
  • Cyclic adenosine 3'5'-monophosphate (cyclic AMP) has been frequently accepted as an intracellular messenger for receptor-mediated action of opioids. In this experiment, it was designed to determine the interaction of dopaminergic and opioidergic system in the mouse striatum in normal and chronic haloperidol treated groups. Haloperidol 750ug/kg I.P. for 10 days was performed for dopamine denervation. The morphine, DAGO, DPDPE, and U5O,488H inhibited the increase of haloperidol-induced cyclic AMP content in chronic haloperidol treated mouse striatum. The inhibition of DAGO and DPDPE showed significant increase compared to normal mouse striatum. Naloxone showed antagonistic effect on the morphine and U5O,488H in chronic haloperidol treated group, and showed antagonistic effect on morphine, DAGO, DPDPE, and U5O, 488H in normal mouse striatum. These findings support that there is a functional interrelationship of dopaminergic and opioidergic pathway in the striatum. This result provides an evidence that following destruction of striatal dopaminergic neuron, there are some changes of cAMP content on the ${\mu},\;{\gamma},\;and\;{\kappa}$ opioid receptor, but the ${\kappa}$ opioid receptor still has its function.

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Relationships between Single Nucleotide Polymorphism Markers and Meat Quality Traits of Duroc Breeding Stocks in Korea

  • Choi, J.S.;Jin, S.K.;Jeong, Y.H.;Jung, Y.C.;Jung, J.H.;Shim, K.S.;Choi, Y.I.
    • Asian-Australasian Journal of Animal Sciences
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    • v.29 no.9
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    • pp.1229-1238
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    • 2016
  • This study was conducted to determine the relationships of five intragenic single nucleotide polymorphism (SNP) markers (protein kinase adenosine monophosphate-activated ${\gamma}3$ subunit [PRKAG3], fatty acid synthase [FASN], calpastatin [CAST], high mobility group AT-hook 1 [HMGA1], and melanocortin-4 receptor [MC4R]) and meat quality traits of Duroc breeding stocks in Korea. A total of 200 purebred Duroc gilts from 8 sires and 40 dams at 4 pig breeding farms from 2010 to 2011 reaching market weight (110 kg) were slaughtered and their carcasses were chilled overnight. Longissimus dorsi muscles were removed from the carcass after 24 h of slaughter and used to determine pork properties including carcass weight, backfat thickness, moisture, intramuscular fat, $pH_{24h}$, shear force, redness, texture, and fatty acid composition. The PRKAG3, FASN, CAST, and MC4R gene SNPs were significantly associated with the meat quality traits (p<0.003). The meats of PRKAG3 (A 0.024/G 0.976) AA genotype had higher pH, redness and texture than those from PRKAG3 GG genotype. Meats of FASN (C 0.301/A 0.699) AA genotype had higher backfat thickness, texture, stearic acid, oleic acid and polyunsaturated fatty acid than FASN CC genotype. While the carcasses of CAST (A 0.373/G 0.627) AA genotype had thicker backfat, and lower shear force, palmitoleic acid and oleic acid content, they had higher stearic acid content than those from the CAST GG genotype. The MC4R (G 0.208/A 0.792) AA genotype were involved in increasing backfat thickness, carcass weight, moisture and saturated fatty acid content, and decreasing unsaturated fatty acid content in Duroc meat. These results indicated that the five SNP markers tested can be a help to select Duroc breed to improve carcass and meat quality properties in crossbred pigs.

Effects of Essential Oils Extracted from Cnidii Rhizoma on Differentiation and Adipogenesis in 3T3-L1 Adiopocytes (천궁(川芎)의 정유 추출물이 3T3-L1 세포의 분화 및 지방 생성에 미치는 영향)

  • Choi, Soo-Min;Kim, So-Young;Park, Na-Ri;Kim, Jung-Min;Yang, Doo-Hwa;Woo, Chang-Hoon;Kim, Mi-Ryeo;An, Hee-Duk
    • Journal of Korean Medicine Rehabilitation
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    • v.28 no.3
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    • pp.13-25
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    • 2018
  • Objectives We investigated anti-obesity effects of essential oils extracted from Cnidii Rhizoma (CR) in immature adipocytes to magnify it's clinical therapeutic usage. Methods Essential oil of CR was extracted with ethyl acetate or petroleum ether and through steam distillation, respectively. Oil red-O staining for monitoring its inhibition effect on adipogenesis and differentiation in murine 3T3-L1 adipocytes and 3-(4,5-methylthiazol-2-yl)-2,5-diphenyletetra zolium bromide (MTT) assay for cell safety were done. Also phospho-adenosine monophosphate (AMP)-activted protein kinase (P-AMPK), AMP-activated protein kinase, phospho-acetyl-CoA carboxylase (P-ACC), acetyl-CoA carboxylase, peroxisome proliferator-activated receptor-${\alpha}$ (PPAR-${\alpha}$), peroxisome proliferator-activated receptor-${\gamma}$ (PPAR-${\gamma}$) and CCAAT/enhancer binding protein ${\alpha}$ (C/EBP-${\alpha}$) expressions as obesity-related factors were measured by western blot analysis. Results Protein expressions of P-AMPK, P-ACC and PPAR-${\alpha}$ were increased in essential oils-treated adipocytes compared to those of control group, respectively. Furthermore, protein expressions of PPAR-${\gamma}$ and C/EBP-${\alpha}$ were decreased in essential oils-treated adipocytes compared to those of control group, respectively. Conclusions These results demonstrate that essential oils of CR inhibit adipogenesis and differentiation. Also they promote the oxidation of fatty acids in adipocytes. Thus, results suggest that essential oils of CR could be used as a valuable material for anti-obesity therapeutics via control of lipid metabolism.

Studies on Secretion of Catecholamines evoked by Panaxadiol in the Isolated Rabbit Adrenal Gland (파낙사디올의 가토적출부신의 카테콜아민 분비작용에 관한 연구)

  • Lim, Dong-Yoon;Park, Kyu-Baik;Kim, Kyu-Hyeong;Choi, Cheol-Hee;Bae, Jae-Woong;Kim, Moo-Won
    • The Korean Journal of Pharmacology
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    • v.24 no.1
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    • pp.31-42
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    • 1988
  • The effect of Panaxadiol(PD), which is an active component of Korean Ginseng Saponins, on the secretion of catecholamines (CA) from the rabbit adrenal gland and its mode of action were investigated in the present study. $PD(400{\mu}g)$ increased significantly the secretion of CA from the isolated perfused rabbit adrenal gland. PD-induced secretion of CA was reduced markedly by treatment of atropine, CA secretion induced by Ach or PD was potentiated significantly by physostigmine-treatment. Chlorisondamine did inhibit CA secretion of PD or Ach. Perfusion of $PD(400{\mu}g)$ for 30 min enhanced the secretory activity of CA by Ach. Ouabain weakened the secretory response induced by PD but rather enhanced the response by Ach. Adenosine-treatment resulted in marked enhancement of CA secretion by PD or Ach, Pefusion with $Ca^{2+}-free$ Krebs containing EGTA (5 mM) for about 30 min totally blocked secretory effect induced by Ach and also weakened that by PD. From the above experimental results, it is suggested that PD causes secretion of catecholamines from the rabbit adrenal gland by a calcium-dependent exocytotic mechanism. The secretory effect of PD is due to the stimulation of cholinergic muscarinic and nicotinic receptors present in the adrenal gland and partly to a direct action on the chromaffin cell itself.

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