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PubMed | Korea Institute of Science and Technology, International Ginseng and Herb Research Institute, Sangji University, Konkuk University and 2 more.
Type: Journal Article | Journal: Biomolecules & therapeutics | Year: 2016

Quercetin is a flavonoid usually found in fruits and vegetables. Aside from its antioxidative effects, quercetin, like other flavonoids, has a various neuropharmacological actions. Quercetin-3-O-rhamnoside (Rham1), quercetin-3-O-rutinoside (Rutin), and quercetin- 3-(2(G)-rhamnosylrutinoside (Rham2) are mono-, di-, and tri-glycosylated forms of quercetin, respectively. In a previous study, we showed that quercetin can enhance 7 nicotinic acetylcholine receptor (7 nAChR)-mediated ion currents. However, the role of the carbohydrates attached to quercetin in the regulation of 7 nAChR channel activity has not been determined. In the present study, we investigated the effects of quercetin glycosides on the acetylcholine induced peak inward current (IACh) in Xenopus oocytes expressing the 7 nAChR. IACh was measured with a two-electrode voltage clamp technique. In oocytes injected with 7 nAChR copy RNA, quercetin enhanced IACh, whereas quercetin glycosides inhibited IACh. Quercetin glycosides mediated an inhibition of IACh, which increased when they were pre-applied and the inhibitory effects were concentration dependent. The order of IACh inhibition by quercetin glycosides was RutinRham1>Rham2. Quercetin glycosides-mediated IACh enhancement was not affected by ACh concentration and appeared voltage-independent. Furthermore, quercetin-mediated IACh inhibition can be attenuated when quercetin is co-applied with Rham1 and Rutin, indicating that quercetin glycosides could interfere with quercetin-mediated 7 nAChR regulation and that the number of carbohydrates in the quercetin glycoside plays a key role in the interruption of quercetin action. These results show that quercetin and quercetin glycosides regulate the 7 nAChR in a differential manner.


Pyo M.K.,International Ginseng and Herb Research Institute | Choi S.-H.,Konkuk University | Shin T.-J.,Konkuk University | Hwang S.H.,Konkuk University | And 5 more authors.
Journal of Ginseng Research | Year: 2011

Ginseng has been used as a general tonic agent to invigorate the human body as an adaptogenic agent. In a previous report, we have shown that ginseng contains a novel glycolipoprotein called gintonin. The main function of gintonin is to transiently enhance intracellular free Ca2+ [Ca2+]i levels in animal cells. The previous method for gintonin isolation included multiple steps using organic solvents. In the present report, we developed a simple method for the preparation of crude gintonin from ginseng root as well as stem and leaf, which produced a higher yield of gintonin than the previous one. The yield of gintonin was 0.20%, 0.29%, and 0.81% from ginseng root, stem, and leaf, respectively. The apparent molecular weight of gintonin isolated from stem and leaf through sodium dodecyl sulfate polyacrylamide gel electrophoresis was almost same as that from root but the compositions of amino acids, carbohydrates or lipids differed slightly between them. We also examined the effects of crude gintonin from ginseng root, stem, and leaf on endogenous Ca2+-activated Cl- channel (CaCC) activity of Xenopus oocytes through mobilization of [Ca2+] i. We found that the order of potency for the activation of CaCC was ginseng root > stem > leaf. The ED50 was 1.4±1.4, 4.5±5.9, and 3.9±1.1 μg/mL for root, stem and leaf, respectively. In the present study, we demonstrated for the first time that in addition to ginseng root, ginseng stem and leaf also contain gintonin. Gintonin can be prepared from a simple method with higher yield of gintonin from ginseng root, stem, and leaf. Finally, these results demonstrate the possibility that ginseng stem and leaf could also be utilized for ginstonin preparation after a simple procedure, rather than being discarded. © The Korean Society of Ginseng.


Kim G.-S.,South Korean National Institute of Animal Science | Lee S.-E.,South Korean National Institute of Animal Science | Noh H.-J.,South Korean National Institute of Animal Science | Kwon H.,International Ginseng and Herb Research Institute | And 3 more authors.
Journal of Ginseng Research | Year: 2012

This study was conducted to evaluate the effects of natural bioactive products such as Manda enzyme (T1), Yangmyeongwon (T2), effective microorganisms (T3), and Kelpak (T4) on the growth and ginsenoside contents of Panax ginseng cultured in an aeroponic system using a two-layer vertical type of nutrient bath under natural light conditions. The growth of ginseng plants showed specifi c characteristics according to the positions in which they were cultured due to the difference of light transmittance and temperature in the upper and lower layers during aeroponic culture in a two-layer vertical type of system. The growth of the aerial part of the leaves and stems of ginseng plants cultured in the lower layer (4,000 to 6,000 lx, 23°C to 26°C) of the nutrient bath was observed to be superior to that of the ginseng plants cultured in the upper layer (12,000 to 15,000 lx, 25°C to 28°C). The leaf area was significantly larger in the treatment of T2 and T4 (46.70 cm 2) than with other treatments. Conversely, the values of the root weight and root diameter were higher in ginseng plants cultured in the upper layer of the nutrient bath. The root weight was significantly heavier in the treatment of T4 (6.46 g) and T3 (6.26 g) than with other treatments. The total ginsenoside content in the leaves and roots was highest in the ginseng plants cultured by the treatment of T1, at 16.20%, while the total ginsenoside content obtained by other treatments decreased in the order of T4, T5 (control), T2, and T3, at 13.21%, 12.30%, 14.84%, and 14.86%, respectively. The total ginsenoside content of the ginseng leaves was found to be significantly higher in the treatment of T1 in the lower layer of the nutrient bath, at 15.30%, while the content of the ginseng roots in the treatments of T3 and T4, at 1.27% and 1.23%, respectively, was significantly higher than in other treatments in the upper layer of the nutrient bath. © The Korean Society of Ginseng.


Lee I.,Korea Institute of Oriental Medicine | Kim J.,Korea Institute of Oriental Medicine | Kim Y.S.,Korea Institute of Oriental Medicine | Yoo N.H.,International Ginseng and Herb Research Institute | And 5 more authors.
Journal of Natural Products | Year: 2012

Six new cycloartane-type triterpenes (1-6), 24-methylenecycloartane- 3β,6β,7β-triol (1), 24-methylenecycloartane-3β,6β, 7β,16β-tetraol (2), 24-methylenecycloartane-3β,6β,16β- triol (3), 24-methylenecycloartane-3β,7β,16β-triol 3-O-β-d-xylopyranoside (4), 24-methylenecycloartane-3β,6β, 16β-triol 3-O-β-d-xylopyranoside (5), and 24-methylenecycloartane- 3β,6β,7β-triol 3-O-β-d-xylopyranoside (6), were isolated from the leaves of Homonoia riparia, together with one known compound, 24-methylenecycloartane-3β,6β,7β,16β-tetraol 3-O-β-d-xylopyranoside (7). The structures of the new triterpenes were established by spectroscopic studies and from chemical evidence, and the inhibitory effects of compounds 1 and 3-7 on VEGF-induced vascular permeability were examined in vivo in rats using the Miles assay. In addition, the inhibitory effect of 7 on VEGF-induced tube formation by HUVECs in vitro was investigated. © 2012 The American Chemical Society and American Society of Pharmacognosy.


PubMed | International Ginseng and Herb Research Institute, Jeonbuk National University Medical School and Wonkwang University
Type: Journal Article | Journal: Molecular medicine reports | Year: 2015

Euphorbia maculata (EM) is a traditionally used antidiarrheal, antibacterial, antifungal and antioxidant agent. However, the effects of EM on platelet activity remain to be elucidated. Therefore, the present study investigated the antiplatelet effect of various EM extract fractions on platelet aggregation in rats. The antiplatelet activity of the EM fractions on collagen or adenosine diphosphate (ADP)induced platelet aggregation was evaluated invitro and exvivo. ThromboxaneB2 (TXB2) formation, rattail bleeding time and coagulation time were also measured. Among the fractions, the chloroform fraction of EM (CFEM) significantly inhibited ADPinduced platelet aggregation invitro. Furthermore, oral administration of 50mg/kg CFEM to rats significantly reduced ADPinduced platelet aggregation without increasing the tail bleeding time or coagulation time. In addition, EM significantly inhibited the level of TXB2 formation in a dosedependent manner. These results suggest that CFEM exhibits antiplatelet activity, without causing bleeding, via the suppression of TXB2 formation. CFEM may be a type of food which has the potential for preventing cardiovascular disease.


Lee K.H.,Hanyang University | Bae I.Y.,Far East University of South Korea | Park S.I.,Hanyang University | Park J.-D.,Hanyang University | And 2 more authors.
Journal of Ginseng Research | Year: 2015

Background: Ginsenoside Rg3 and arginine-fructose (Arg-Fru) are known as the hypotensive compounds of Panax ginseng; however, their efficacy on antihypertension has not been reported yet to our best knowledge. Thus, hypotensive components-enriched fraction of red ginseng (HCEF-RG) was prepared from fine root concentrate (FR) and their antihypertensive effects were investigated in spontaneously hypertensive rats (SHR). Methods: Male SHRs were divided into six groups: control (Wistar Kyoto, SHR); FR 500; FR 1,000; HCEF-RG 500; and HCEF-RG 1,000; samples (mg/kg body weight) were orally administered every day for 8 wk. Blood pressure was monitored at 1 wk, 2 wk, 3 wk, 4 wk, 6 wk, and 8 wk by tail cuff method. At 8 wk after samples administration, mice were killed for the measurement of renin activity (RA), angiotensin-I converting enzyme inhibition, angiotensin II, and nitric oxide (NO) levels in plasma. Results: HCEF-RG with four-fold more Rg3 and 24-fold more Arg-Fru contents was successfully prepared from reacted mixtures of FR and persimmon vinegar (12 times against FR, v/v) at 80°C for 18 h. Both FR 1,000 and HCEF-RG 1,000 showed lowered systolic blood pressure than SHR control group and HCEF-RG 1,000 group exhibited a significant decrease in diastolic blood pressure. RA was significantly lowered in all treated groups, while angiotensin II did not affect by FR and HCEF-RG treatment. However, angiotensin-I converting enzyme inhibition and NO in FR 1,000 and HCEF-RG 1,000 were significantly increased compared with SHR control group. Conclusion: HCEF-RG is more effective and useful for alleviating hypertension than FR, implying the health benefit of Rg3 and Arg-Fru. © 2015.


Nam K.Y.,Chungnam Agricultrue Meister College | Kim Y.S.,International Ginseng and Herb Research Institute | Shon M.Y.,International Ginseng and Herb Research Institute | Park J.D.,International Ginseng and Herb Research Institute
Korean Journal of Pharmacognosy | Year: 2015

We have conducted a comprehensive literature review regarding the chemical constituents and biological activities of Korean black ginseng(Panax ginseng C. A. Meyer), three to nine times-steamed and dried ginseng, which shows strong black color through Maillared browning reaction. It has been reported that some chemically deglycosylated and transformed saponins are obtained from black ginseng as artifacts produced during intensive steaming. They have been known to be ginsenosides Rg3, Rg4, Rg5, Rg6, Rh1, Rh2, Rh4, Rk1 and Rk3, quite different from those of red ginseng, among which ginsenosides Rg3, Rg5 and Rk1 are considered to be major components. And also, black ginseng has been recently found to demonstrate anticancer, recovery from learning and memory damages, hypontensive, antidiabetic, antiobesitic, tonic and antiatopic activities, together with antioxidative and exercise performance improving activities, exhibiting their effects to be a little bit stronger than those of red ginseng. These findings suggest that black ginsng might play an important role in the development of promising functional foods and drugs from the viewpoint of the chemical composition and biological activities of black ginseng with a distinction from those of white and red ginsengs. In this review, the authors will survey and evaluate further functions of black ginseng with a focus on its physicochemical properties and biological activities. © 2015, Korean Society of Pharmacognosy. All rights reserved.


Lee Y.M.,Korea Institute of Oriental Medicine | Kim J.,Korea Institute of Oriental Medicine | Kim C.-S.,Korea Institute of Oriental Medicine | Jo K.,Korea Institute of Oriental Medicine | And 3 more authors.
European Journal of Pharmacology | Year: 2015

Advanced glycation end products (AGEs) are involved in the development of diabetic complications such as diabetic retinopathy. 5′-methoxybiphenyl-3,4,3′-triol (referred to as K24) was isolated using bioactivity-guided fractionation of Osteomeles schwerinae C. K. Schneid. and identified as a potent AGE inhibitor. To identify the protective effect of K24 on disruption of the blood-retinal barrier, AGE-RSA was intravitreally injected into rat eyes. K24 had an inhibitory effect on AGE-RSA-induced retinal vascular leakage by suppressing the expression of vascular endothelial growth factor (VEGF) and decreasing the loss of occludin. In addition, we examined whether K24 has a preventive effect against retinal pathogenic angiogenesis in an oxygen-induced retinopathy (OIR) mouse model. K24 significantly reduced the retinal non-perfused area and neovascular tufts in the OIR mice. These data indicate that K24 could serve as an innovative pharmaceutical agent to prevent blood-retinal barrier breakage and retinal pathogenic angiogenesis through an anti-VEGF mechanism. © 2015 Elsevier B.V. All rights reserved.


PubMed | International Ginseng and Herb Research Institute and Wonkwang University
Type: | Journal: Journal of ethnopharmacology | Year: 2016

Ginseng (Panax ginseng C. A. Meyer, Araliaceae) has been used as a traditional medicine for thousands of years for the treatment of a wide variety of diseases, including diabetes. Processed ginseng named Black ginseng exhibits more potent biological activities than white and red ginseng. The aim of this study was to investigate the effects of black ginseng extract (GBG05-FF) on hyperglycemia and glucose tolerance in streptozotocin (STZ)-induced diabetic mice.Black ginseng was produced by a repeated steaming and drying process, subsequent extraction with 70% ethanol, filtration, and lyophilization. The effect of GBG05-FF on glucose uptake and related protein expression and phosphorylation were determined in C2C12 cells. Furthermore, we evaluated the anti-diabetic effects of GBG05-FF in STZ-induced diabetic mice.GBG05-FF significantly (p<0.05) increased glucose uptake in C2C12 myotubes via AMPK, Sirt1 and PI3-K pathway. In addition, GBG05-FF improved the fasting blood glucose levels and glucose tolerance in STZ-induced diabetic mice. GBG05-FF decreased blood parameters such as glycated hemoglobin, triglyceride and total cholesterol. Quantitative RT-PCR assay revealed that in the STZ-induced diabetic mice treated with GBG05-FF, the expression of hepatic genes involved in gluconeogenesis (phosphoenolpyruvate carboxykinase (PEPCK), glucose 6-phosphatase (G6Pase)), glycogenolysis (liver glycogen phosphorylase (LGP)) and glycogenesis (glycogen synthase (GS)) was suppressed, while the expression of the genes involved in glucose uptake (glucose transporter (GLUT) 1, GLUT4) and -oxidation (acyl-CoA oxidase (ACO), carnitine palmitoyl transferase 1a (CPT1a), mitochondrial medium chain acyl-CoA dehydrogenase (MCAD)) in muscle were increased. GBG05-FF delayed diabetes-associated muscle atrophy by activating mTOR. The major bioactive compounds including ginsenoside Rg1, Rg3(S), Rg3(R), Rg5, Rk1 and Rh4 were evaluated for glucose uptake effect in C2C12 myotubes; the data indicated that Rh4 significantly (p<0.05) increased glucose uptake.Collectively, the results suggested that GBG05-FF is a potentially useful agent for treatment of diabetes by increasing glucose uptake.


PubMed | International Ginseng and Herb Research Institute and Korea Institute of Oriental Medicine
Type: Journal Article | Journal: Molecular medicine reports | Year: 2015

In the pathophysiology of diabetic retinopathy (DR), advanced glycation end products (AGEs) and vascular endothelial growth factor (VEGF) are thought to have important roles. It is known that VEGF causes a breakdown of the bloodretinal barrier (BRB) and retinal neovascularization; however, how AGEs affect the retina has largely remained elusive. OSSC1EK19 is a novel phytochemical component of Osteomeles schwerinae. The objective of the present study was to evaluate the protective effects of OSSC1EK19 on retinal vascular injury in AGEmodified rat serum albumin (AGE-RSA)-induced retinopathy. AGE-RSA-injected rat eyes were used investigate the protective effects of OSSC1EK19 on BRB breakdown. Intravitreal injection of OSSC1E-K19 prevented AGE-RSA-induced BRB breakdown and decreased retinal VEGF expression in retinal vessels. In addition, OSSC1E-K19 inhibited the loss of occludin, a significant tight junction protein. These results supported the potential therapeutic utility of OSSC1E-K19 for retinal vascular permeability diseases.

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