• YAKHAK HOEJI
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• v.36 no.6
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• pp.518-528
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• 1992

To determine the optimal conformation of sulfonylureas, the correlation between conformation and hypoglycemic activity of the two sulfonylureas of tolbutamide and chlorpropamide as hypoglycemic agent was studied using an empirical potential function (ECEPP/2) and the hydration shell model in the unhydrated and hydrated states. The conformational energy was minimized from several starting conformations with possible torsion angles in each molecule. The conformational entropy change of each conformation was computed using a harmonic approximation. To understand the hydration effect on the conformation of the molecules in aqueous solution, the contribution of water-accessible volume of each group or atom in the lowest-free-energy conformation was calculated and compared each other. From comparison of the computed lowest-free-energy conformations of two sulfonylureas, it could be suggested that the hydration of sulfonylurea moiety is related to increase the hypoglycemic activity. From the calculation results, it was known that the conformational entropy is the major contribution to stabilize the low-free-energy conformations of two sulfonylureas in unhydrated state. Whereas, in hydrated state, the hydration free energy largely contributes to the total free energies of low-free-energy conformations of tolbutamide and conformational entropy contributes to stabilize the low-free-energy conformations of chlorpropamide. The torsion angles from phenyl ring to urea moiety of the low-free-energy conformations of the two sulfonylureas were shown the nearly regular trend. On the basis of these results, the conformation exhibiting the optimal hypoglycemic activity of sulfonylureas and the binding direction to pancreatic receptor site A could be predicted. Also, according to the side chain lengthening of urea moiety, tolbutamide showed various conformational change. Therefore, steric effect may be important factor in the interaction between sulfonylureas and the putative pancreatic receptor.

• Advances in Traditional Medicine
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• v.7 no.4
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• pp.418-425
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• 2007

The study was to evaluate the antihyperglycemic activity of Biophytum sensitivum (L.) DC in different extracts. Albino Wistar rats with alloxan hydrate induced diabetes were divided into 7 groups of 6 each. Both aqueous and methanolic extract of Biophytum sensitivum were prepared and given individually at different doses to different batches of rats (both normal and diabetic rats) after an overnight fast. Methanolic extract at the dose of 200 mg/kg body weight showed maximum blood glucose lowering effect in diabetic rats. The same dosages did not produce any hypoglycemic activity in normal rats. The antihyperglycemic activity of Biophytum sensitivum was compared with a standard drug Glibenclamide, an oral hypoglycemic agent. The above results suggest that maximum hypoglycemic effect was found only with a dose of up to 200 mg/kg b.w. of methanolic extract which is therefore the optimum dose for hypoglycemia and was used in all the experiments of the present study.

• Journal of Physiology & Pathology in Korean Medicine
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• v.23 no.1
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• pp.144-149
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• 2009

The purpose of this study was evaluated physiological activity of processed sulfur with Cordyceps militaris mycelium. Effect of blood glucose levels and lipid metabolism on streptozotocin-induced Diabetic Rats. To evaluate of hypoglycemic effects in vivo, we examined blood glucose levels, serum lipid profile and hepatotoxicity of streptozotocin (STZ) induced diabetic rats. Hypoglycemic effect of CM, CM+PSL and CM+PSH groups was significantly higher than DC groups. The activities of ALT, AST and ALP in CM+PSH group were lower than DC, PC groups. These results suggested that processed sulfur with Cordyceps militaris mycelium have activities of hypoglycemic effects.

• Proceedings of the Ginseng society Conference
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• 2006.05a
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• pp.69-70
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• 2006

Purpose: Panaxadiols are more potent than panaxatriols as far as insulin secretory activity is concerned. In this study, we examined insulin secretory activity and mechanism of compound K (CK), a major intestinal bacterial metabolite of ginsenosides. Method: Insulin secretory activity of CK was examined using pancreatic beta cells and in Oral Glucose Tolerance Test assay. In addition, insulin secretory mechanism was studied in terms of calcium dependent or independent pathways. Results: In vitro, CK enhanced the insulin secretion concentration-dependently when compared to glucose-stimulated control cells. Insulin secretory mechanism of CK seems to block ATP sensitive K channels, which was confirmed by diazoxide (K channel opener) but, insulin resistance ameliorating activity of CK can't be ruled out. In vivo, CK showed hypoglycemic effect in OGTT.

• Korean journal of food and cookery science
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• v.13 no.1
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• pp.23-29
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• 1997

The hypoglycemic effect of fractions of methanol extract of Cassia tora was investigated in diabetic rats. Sprague-Dawley male rats weighing 180∼230 g were divided into 6 groups. Diabetes was induced in the male rats by intravenous injection of streptozotocin at a dose of 45 mg/kg dissolved in citrate buffer (pH 4.5). The diabetic animals then had plasma glucose concentration of above 300 mg/㎗. Fractions of methanol extract of Cassia tora were administered orally into the diabetic rats for 14 days after streptozotocin injection. The food intake and body weight gain were monitored and plasma levels of glucose, triglyceride, free fatty acid, HDL-cholesterol, cholesterol and ALT activity were determined. Levels of glycogen, cholesterol and triglyceride in liver were analysed. Weights of liver and kidney were lighter in all the fraction-administered groups than streptozotocin-control group. Plasma glucose level was significantly decreased by the administration of butanol fraction at 14 days. Plasma triglyceride levels were lower in chloroform, butanol and H$_2$O fraction-administered groups compared to streptozotocin-control group. Plasma cholesterol and HDL-cholesterol levels were not significantly different in all groups. Administrations of each of the four fractions have decreased plasma free fatty acid level, ALT activity and liver triglyceride levels in the diabetic rats. Liver glycogen levels in chloroform, butanol and H$_2$O fraction-administered groups were higher than streptozotocin-control group. It is suggested from the results that butanol fraction of methanol extract of Cassia tora may contain the antihyperglycemic compounds.

• Journal of the Korean Chemical Society
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• v.56 no.2
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• pp.251-256
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• 2012

A novel series of benzothiazole derivatives were synthesized and assayed in vivo to investigate their hypoglycemic activity by streptozotocin-induced diebetic model in rat. These derivatives showed considerable biological efficacy when compared to glibenclamide, a potent and well known antidiabetic agent as a reference drug. All the compounds were effective, amongst them 3d showed more prominent activity at 100 mg/kg p.o. The experimental results are statistically significant at p<0.01 and p<0.05 level.

• Journal of Ginseng Research
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• v.17 no.2
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• pp.101-108
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• 1993

This study was made to understand a hypoglycemic action of the fat soluble fraction of Panax ginseng C.A. Meyer in streptozotocin induced diabetic rats by determining the activities of several enzymes related to carbohydrate and lipid metabolism as well as several blood component levels such as glucose and ketone bodies, and non-esterified fatty acids. Albino rats (Sprague Dawley, 170-200g, 3) were injected once with 70mg streptozotocinhg body weight intraperitoneally and fed with ordinary diet for 7 days, and then the fat soluble fraction (5 mg~20 mg/day/rat) was injected intraperitoneally once a day for three days to rats having high blood glucose level over 340 mg/100ml. After a final injection of the fat soluble fraction, rats u.ere starved for 16 hours followed by the analysis of blood serum and liver enzymes. It was found that increased levels of glucose, ketone bodies and free fatty acids in streptozotocin induced rats were decreased appreciably by administration of the fat soluble fraction. However, the amount of administered fat soluble fraction did not show any significantly different hypoglycemic action. Decreased activities of glucokinase, phosphofructokinase, pyruvate kinase, 6-phosphogluconate dehydrogenase and acetyl CoA carboxylase of the liver of streptozotocin induced diabetic rats were greatly modified suggesting that a hypoglycemic action of the fat soluble fraction was also appreciable as ginseng saponin fraction. We also compared a hypoglycemic action of the fat soluble fraction prepared from American ginseng and Chinese ginseng with that of Korean pain ginseng. 핀o significant difference of the hypoglycemic activity was observed between the above ginseng fat soluble fractions, suggesting that a study of the fat soluble fraction might be one of the most interesting subjects relating to diabetic hyperglycemia in the near future.

• Korean Journal of Plant Resources
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• v.19 no.6
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• pp.670-676
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• 2006

Tea polysaccharide had high antioxidant activity and it could be used to cure diabetes. Antioxidant activity of tea poly-saccharide (TPS) from three kinds of tea (green tea, oolong tea and black tea) were compared, the result indicated that oolong tea polysaccharide (OTPS) had the highest antioxidant activity. In order to explicate the mechanism of antioxidant and hypoglycemic activity, the streptozotocin (STZ)-induced diabetes mice model (DM) was established. The influence of OTPS on blood-glucose, content of MDA and NO, and activities of GSH-PX, SOD, NOS in serum, kidney and liver were investigated. The result showed that after four weeks injection of OTPS to DM mice, the blood-glucose of three treatment group reduced by 14.5%,21.5% and 33.3%, respectively, comparing to the model control. The reduction effect of OTPS increased with the rise of dose. The activity of SOD and GSH-PX elevated significantly, while the activity of NOS decreased. The content of MDA and NO reduced significantly. The above results imply that antioxidant activity was enhanced. Comparing to XKW treatment, the effect of a dose of 300mg/(kg. bw) OTPS was much better. The research showed that the OTPS had a significant effect on reducing blood glucose, and could enhance the antioxidant activity of DM mice.

• Journal of Ginseng Research
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• v.21 no.3
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• pp.174-186
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• 1997

In this study, rat hepatocytes known to have active carbohydrate metabolism were obtained by using the liver perfusion technique to examine the hypoglycemic action of red ginseng saponin components [ginsenoside (mixture, $Rb_1$, and $Rg_1$)] and incubated in two different media-one containing insulin and glucagon (control group), and the other containing glucagon only, The specific activities of some regulatory enzymes such as glucokinase, glucose 6-phosphate dehydrogenase, 6-phosphogluconate dehydrogenase, and glucose 6-phosphatase, in main pathways which were directly related to the glucose metabolism were compared between these two kinds of hepatocytes cultured in two different media. The effects of red ginseng saponin components [ginsenoside (mixture, $Rb_1$, and $Rg_1$)] under the concentration of $10^3$~$10^6$% on these enzymes In hepatocytes were also investigated, when they were added to these two media. The results were as follows. The specific activity of enzymes such as glucokinase, glucose 6-phosphate dehydrogenase, and 6-phosphogluconate dehydrogenase related to glucose-consuming pathways of insulin-deficient group was much less than control one, however, their decreased activity was recovered after the addition of ginseng components at all range of concentrations. The increased specific activity of these on - zymes was shown by the addition of ginseng components to the control group. On the other hand, the specific activity of glucose 6-phosphatase related to glucose-producing pathway of insulin-deficient group was much higher than control one, but their Increased activity was decreased after the addition of ginseng components at all range of concentrations. The same results were obtained after the addition of ginseng components to the control group. These results suggest that the red ginseng saponin components might better diabetic hyperglycemia by regulating the activity of enzymes related to glucose metabolism directly and/or Indirectly though more detailed studies were needed.

• Journal of Pharmacopuncture
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• v.25 no.3
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• pp.242-249
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• 2022

Objectives: The aim of this work is to evaluate the in vitro antioxidant, hypoglycemic, and antiobesity effects of Euphorbia resinifera extracts and investigate the phenolic constituents and the toxicity of these extracts. Methods: Phytochemical screening was performed to detect polyphenols and flavonoids. Antioxidant activity was evaluated by four methods (DPPH, ABTS, H₂O₂, and xanthine oxidase inhibition). The hypoglycemic effect was determined by the inhibition of α-amylase and α-glucosidase enzymes in vitro and via a starch tolerance study in normal rats. The antiobesity effect was estimated by in vitro inhibition of lipase. Results: Phytochemical screening revealed that the ethanolic extract was rich in polyphenols (99 ± 0.56 mg GEA/g extract) and tannins (55.22 ± 0.17 mg RE/g extract). Moreover, this extract showed higher antioxidant activity in different tests: the DPPH assay (IC₅₀ = 53.81 ± 1.83 ㎍/mL), ABTS assay (111.4 ± 2.64 mg TE/g extract), H₂O₂ (IC₅₀ = 98.15 ± 0.68 ㎍/mL), and xanthine oxidase (IC₅₀ = 10.26 ± 0.6 ㎍/mL). With respect to hypoglycemic effect, the aqueous and ethanolic extracts showed IC₅₀ values of 119.7 ± 2.15 ㎍/mL and 102 ± 3.63 ㎍/mL for α-amylase and 121.4 ± 1.88 and 56.6 ± 1.12 ㎍/mL for α-glucosidase, respectively, and the extracts lowered blood glucose levels in normal starch-loaded rats. Additionally, lipase inhibition was observed with aqueous (IC₅₀ = 25.3 ± 1.53 ㎍/mL) and ethanolic (IC₅₀ = 13.7 ± 3.03 ㎍/mL) extracts. Conclusion: These findings show the antioxidant, hypoglycemic, and hyperlipidemic effects of E. resinifera extracts, which should be investigated further to validate their medicinal uses and their pharmaceutical applications.