• Title/Summary/Keyword: Sucrase inhibitory activity

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Antidiabetic Activity of an Ayurvedic Formulation Chaturmukha Rasa: A Mechanism Based Study

  • Sharma, Akansha;Tiwari, Raj K;Sharma, Vikas;Pandey, Ravindra K;Shukla, Shiv Shnakar
    • Journal of Pharmacopuncture
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    • v.22 no.2
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    • pp.115-121
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    • 2019
  • Objectives: The objective of this study was to evaluate antidiabetic activity of Chaturmukha rasa based on streptozotocin induced diabetes model, alpha amylase inhibitory activity, alpha Glucosidase inhibitory activity and inhibition of sucrase. Methods: Chaturmukha rasa was prepared as per Ayurvedic formulary. Antidiabetic activity was measured in experimentally streptozotocin induced rats. The dose was taken as 45 mg/kg, i.p. The antidiabetic activity of Chaturmukha rasa was compared Triphala Kwatha, a marketed formulation. Further In vitro $\acute{\alpha}$- Amylase Inhibitory Assay, In vitro salivary amylase Inhibitory Assay, In vitro ${\alpha}-Glucosidase$ Inhibitory Assay and In vitro Sucrase Inhibitory Assay was performed with respect to Chaturmukha rasa. The IC50 value was calculated for all the above activity. Results: Streptozotocin with Acarbose showed significant decrease in blood glucose level whereas streptozotocin with Triphala kwatha showed more decrease in blood glucose level than Streptozotocin with Acarbose. The combination of Streptozotocin + Triphala kwatha + Chaturmukha rasa showed a significant decrease in blood glucose level on 21st day. In vitro $\acute{\alpha}$- Amylase Inhibitory Assay the Chaturmukha rasa showed IC50 value $495.94{\mu}l$ when compared with Acarbose $427.33{\mu}l$, respectively. In the ${\alpha}-Glucosidase$ Inhibitory Assay Chaturmukha rasa showed IC50 value $70.93{\mu}l$ when compared with Acarbose $102.28{\mu}l$, respectively. In vitro Sucrase Inhibitory Assay Chaturmukha rasa showed IC50 value $415.4{\mu}l$ when compared with Acarbose $371.43{\mu}l$, respectively. Conclusion: This study supports that Chaturmukha rasa may inhibit diabetes by inhibition of salivary amylase or alpha Glucosidase or sucrase. This may be the mechanism by which Chaturmukha rasa inhibits diabetes. Further this study supports the usage of Chaturmukha rasa for the management of diabetes.

In vitro $\alpha$-Glucosidase Inhibitory Potential and Antioxidant Activity of Selected Lamiaceae Species Inhabited in Korean Penninsula

  • Kim, Dong-Soo;Kwon, Hyun Jeong;Jang, Hae-Dong;Kwon, Young-In
    • Food Science and Biotechnology
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    • v.18 no.1
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    • pp.239-244
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    • 2009
  • In the current study, inhibitory activity of 8 selected Korean edible plants of Lamiaceae family against $\alpha$-glucosidases, prepared from rat small intestine acetone powder was evaluated. Total flavonoids and oxygen radical absorbance capacity (ORAC) were also investigated. Methyl alcohol extracts of Scutellaria indica (SI) had the highest $\alpha$-glucosidase inhibitory activity relevant for potentially managing hyperglycemia, followed by Clinopodium gracile (CG) and Thymus quinquecostatus (TQ). These 3 species also showed significant antioxidant activity in ORAC system. The $\alpha$-glucosidase inhibitory activity of the extracts was compared to selected phenolics. Among the standard phenolics tested quercetin which was major flavonoid in the extracts had the highest $\alpha$-glucosidase inhibitory activity. CG, TQ, and SI which had high quercetin content and ORAC values also exhibited significant sucrase inhibitory activity. Results suggested that selected 3 Korean Lamiaceae species have the potential development of effective dietary strategy for postprandial hyperglycemia and oxidative stress-linked diabetes complications.

Characterization of an $\alpha$-Glucosidase Inhibitor Produced by Streptomyces sp. CK-4416

  • Chun, Hyoung-Sik;Chang, Heung-Bae;Kwon, Young-In;Yang, Han-Chul
    • Journal of Microbiology and Biotechnology
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    • v.11 no.3
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    • pp.389-393
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    • 2001
  • An $\alpha$-glucosidase inhibitor, CK-4416, was identified from the culture broth of Streptomyces sp. CK-4416. CK-4416, which had some specificity against intestinal disaccharidases, especially sucrase and matlase activities, was purified by adsorption and cationic ion exchange chromatographies. The molecular formula was determined to be $C_{37}H_{63}NO_{30}$ (MW 1001.31) by FAB-MS and NMR analyses. In vitro studies found CK-4416 to show a potent inhibitory activity against sucrase and maltase, but it had low inhibition against $\alpha$-amylase.

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Mode of Action of Water Soluble β-Glucan from Oat (Avena sativa) on Calorie Restriction Effect In-Vitro and In-Vivo Animal Models (In-Vitro, In-Vivo 동물모델에서 귀리 유래 수용성 베타-글루칸의 칼로리 제한 효과 작용기전 규명)

  • Kang, Hanna;Kim, Se-Chan;Kang, Yong Soo;Kwon, Young-In
    • The Korean Journal of Food And Nutrition
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    • v.30 no.6
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    • pp.1222-1228
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    • 2017
  • In the current study, we investigated the inhibitory activity of water soluble ${\beta}-glucan$ from oat (Avena sativa) against various digestive enzymes such as ${\alpha}-glucosidase$, sucrase, maltase and glucoamylase. Inhibition of these enzymes involved in the absorption of disaccharide can significantly decrease the post-prandial increase of blood glucose level after a mixed carbohydrate diet. The ${\beta}-glucan$ had the highest documented rate of small intestinal sucrase inhibitory activity (2.83 mg/mL, $IC_{50}$) relevant for potentially managing post-prandial hyperglycemia. Furthermore, we evaluated the effects of ${\beta}-glucan$ on the level of post-prandial blood glucose in animal model. The post-prandial blood glucose levels were tested two hours after sucrose/starch administration, with and without ${\beta}-glucan$ (100, and 500 mg/kg-body weight). The maximum blood glucose levels (Cmax) of ${\beta}-glucan$ administration group were decreased by about 23% (from $219.06{\pm}27.82$ to $190.44{\pm}13.18$, p<0.05) and 10% (from $182.44{\pm}13.77$ to $165.64{\pm}10.59$, p<0.01) in starch and sucrose loading test, respectively, when compared to control in pharmacodynamics study. The ${\beta}-Glucan$ administration significantly lowered the mean, maximum, and minimum level of post-prandial blood glucose at 30 min after meal. In view of the foregoing, it is felt that our findings suggest that ${\beta}-glucan$ from oat serves to reduce post-prandial blood glucose rise secondary to slower absorption of glucose in the small intestine, via carbohydrate hydrolyzing enzymes inhibition.

Inhibitory Effects of Crude Drugs on $\alpha$-Glucosidase

  • Choi, Hyuck-Jai;Kim, Nam-Jae;Kim, Dong-Hyun
    • Archives of Pharmacal Research
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    • v.23 no.3
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    • pp.261-266
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    • 2000
  • The inhibitory activity of several crude drugs on $\alpha$-glucosidases, which are the key enzymes for carbohydrate digestion and the prevention of diabetic complications, was investigated. Several crude drugs including Terminaliae Fructus, Mori Cortex Radicis, Caesalpiniae Lignum and Cyrophora esculenta potently inhibited maltase and sucrase isolated from rat intestine, while Arecae Semen and Corni Fructus remarkably inhibited $\alpha$-amylase. Caesalpiniae Lignum and Gyrophora esculenta exhibited significant reductions of blood glucose elevation in mice loaded with maltose and sucrose.

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Antioxidant and Anti-hyperglycemic Effects of a Sanghwang Mushroom(Phellinus linteusau) Water Extract (상황버섯 열수추출물의 항산화 활성과 식후 혈당 상승 억제 효과)

  • Choi, Hwang-Yong;Ha, Kyoung-Soo;Jo, Sung-Hoon;Ka, Eun-Hye;Chang, Hung-Bae;Kwon, Young-In
    • The Korean Journal of Food And Nutrition
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    • v.25 no.2
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    • pp.239-245
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    • 2012
  • The inhibitory activities of a water extract of Sanghwang mushroom(Phellinus linteusau)(SWE) against ${\alpha}$-glucosidases were evaluated in this study. Inhibiting these enzymes involved in the absorption of disaccharides significantly decreases the postprandial increase in blood glucose level after a mixed carbohydrate diet. Oxygen radical absorbance capacity and 1,1-diphenyl-2-picryl hydrazyl scavenging activities of the SWE were evaluated to investigate the antioxidant activity of the SWE associated with complications of long-term diabetes. Furthermore, the postprandial blood glucose lowering effect of SWE was compared to a known type 2 diabetes drug($Acarbose^{(R)}$) in a Sprague-Dawley rat model. SWE significantly reduced the blood glucose increase after sucrose loading. These results suggest that SWE, which has high ${\alpha}$-glucosidase inhibitory activity and high antioxidant activities, has the potential to contribute to a useful dietary strategy for controlling postprandial hyperglycemia.

STUDIES ON BIOLOGICALLY ACTIVE SUBSTANCES IN NON-SAPONIN FRACTION OF KOREAN RED GINSENG

  • Okuda Hiromichi;Zheng Yinan;Matsuura Yukinaga;Takaku Takeshi;Kameda Kenji
    • Proceedings of the Ginseng society Conference
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    • 1993.09a
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    • pp.110-112
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    • 1993
  • Acidic polysaccharide from Korean red ginseng was found to inhibit pancreatic lipase activity and cause reduction of plasma triglyceride level after oral administration of corn oil emulsion to rats. Thus acidic polysaccharide may reduce plasma triglyceride through its inhibitory action on pancreatic lipase and successive inhibition of intestinal absorption of fat due to reduction of lipolysis. In the course of this experiment, we found an unknown ninhydrin positive substance in Korean red ginseng. The unknown substance was identified to be arginyl-fructosyl glucose(Arg - Fru - Glc). Coment of this new compound was $5.37\%$ in Korean red ginseng powder. Sucrase and maltase activities in mucous layer of rat jejunum were found to be inhibited by Arg-Fru-Glc. Physiological significance of the new compound was discussed based on these experimental results.

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Inhibitory Effects of Mulberry Fruit on Intestinal Disaccharidase Activity and Hyperglycemia in Streptozotocin-Induced Diabetic Rats

  • Hong, Jung-Hee;Kim, Sang-Woon;Choi, Kyung-Ho;Choi, Sang-Won;Rhee, Soon-Jae
    • Nutritional Sciences
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    • v.7 no.4
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    • pp.201-207
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    • 2004
  • The current study examined the effects of freeze-dried mulberry fruit on disaccharidase activity in the small intestine and the lowering of blood glucose in streptozotocin (STZ)-induced diabetic rats. Sprague-Dawley male rats were randomly assigned to one normal and three streptozotocin (STZ)-induced diabetic groups. The diabetic groups were fed a mulberry fruit-free diet (DM-group), 0.3% mulberry fruit diet (DM-F group) or 0.6% mulberry fruit diet (DM-2F group). After they were fed the experimental diets for three weeks, diabetes was induced with an intraperitoneal injection of streptozotocin 50 mg/kg b.w before sacrificing 9 days later using the same experimental treatments. Analyses of anthocyanins, flavonoid and 1-deoxynojirimycin (DNJ) of lyophilized mulberry fruit were carried out and the major anthocyanins were rutin (142.5 mg), isoquercitrin (10.3 mg), quercetin (5.8 mg), morin (1.6 mg) dihydroquercetin (3.83 mg), cy-3-O-glucopyranoside (230.45 mg) and cy-3-O-rutinoside (131.5 mg) on the basis of 100 g dry weight. Total DNJ content was 2.39 mg/g dry weight of lyophilized mulberry fruit. Blood glucose level decreased in the diabetic mts fed the mulberry fruit supplement. The content of the liver glycogen increased in the diabetic mts fed the mulberry fruit supplement. Disaccharidase activity in the proximal part of the intestine, such as that of maltase, sucrase and lactase in the mulberry fruit supplementation groups, were lower than that of the DM group. These results suggest that mulberry fruit possess a suppressive effect on hyperglycemia, possibly by inhibiting the activity of disaccharidase in the small intestine of rats.

Coating rice with mulberry leaves rich in deoxynojirimycin ameliorates hyperglycemia and dyslipidemia in C57BL/KsJ db/db mice

  • Lee, Joomin;Lee, Hyun-Joo;Lee, Jae-Joon
    • Nutrition Research and Practice
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    • v.12 no.6
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    • pp.469-478
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    • 2018
  • BACKGROUND/OBJECTIVES: Mulberry leaf (ML) has been shown to have an inhibitory effect on ${\alpha}$-glucosidase, and suppresses postprandial hyperglycemia, which may be related to its deoxynojirimycin (DNJ) content. This study was conducted to investigate the hypoglycemic and dyslipidemic effects of rice coated with ML rich in DNJ in a type 2 diabetes mouse model. MATERIALS/METHODS: The mice were divided into four groups (n = 8 each): non-diabetic normal control (NC); diabetic control (DM-C), fed with 10% polished rice powder (DM-R); and fed with 10% polished rice powder coated with DNJ-rich ML (DM-DNJR). RESULTS: Supplementation with DNJR for six weeks decreased levels of fasting blood glucose, plasma insulin, triglyceride, total cholesterol, and blood glycosylated hemoglobin; conversely, levels of glucagon-like peptide-1 and high-density lipoprotein-cholesterol showed an increase in the same treatment. In addition, weights of mesenteric, epididymal, and total adipose tissues decreased with DNJR supplementation, when compared with diabetic control db/db mice, while maltase, lactase, and sucrase activity in the small intestine were inhibited. The anti-diabetic effects were marginally greater in the DM-DNJR group than in the DM-R group. CONCLUSIONS: These results suggest that rice coated with ML rich in DNJ can reduce hyperglycemia and hyperlipidemia in db/db mice, and may prove useful for individuals with diabetes.