WordNet

limit, block, or decrease the action or function of; "inhibit the action of the enzyme"; "inhibit the rate of a chemical reaction"
control and refrain from showing; of emotions, desires, impulses, or behavior (同)bottle up, suppress
limit the range or extent of; "Contact between the young was inhibited by strict social customs"
first in order of importance; "the alpha male in the group of chimpanzees"; "the alpha star in a constellation is the brightest or main star"
the 1st letter of the Greek alphabet
the beginning of a series or sequence; "the Alpha and Omega, the first and the last, the beginning and the end"--Revelations
early testing stage of a software or hardware product; "alpha version"
a substance that retards or stops an activity
any high mountain

PrepTutorEJDIC

〈感情・欲望・行動・作用など〉‘を'抑制する / (…しないように)〈人〉‘を'抑制する,妨げる《+『名』+『from』+『名』(do『ing』)》
アルファ(ギリシア語アルファベットの第1字A,α;英語のA,aに相当) / アルファ星(星座の主星)
抑制する人(物) / 化学反応抑制剤
高山,高峰

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/05/30 10:28:53」(JST)

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Alpha-glucosidase inhibitors are oral anti-diabetic drugs used for diabetes mellitus type 2 that work by preventing the digestion of carbohydrates (such as starch and table sugar). Carbohydrates are normally converted into simple sugars (monosaccharides), which can be absorbed through the intestine. Hence, alpha-glucosidase inhibitors reduce the impact of carbohydrates on blood sugar.

Examples and differences [edit]

Examples of alpha-glucosidase inhibitors include:

Acarbose- Precose
Miglitol - Glyset
Voglibose

Even though the drugs have a similar mechanism of action, there are subtle differences between acarbose and miglitol. Acarbose is an oligosaccharide, whereas miglitol resembles a monosaccharide. Miglitol is fairly well absorbed by the body, as opposed to acarbose. Moreover, acarbose inhibits pancreatic alpha-amylase in addition to alpha-glucosidase.

Natural alpha glucosidase inhibitors [edit]

There are a large number of plants with Alpha-glucosidase inhibitor action.,^[1]^[2]

For example, research has shown the culinary mushroom Maitake (Grifola frondosa) has a hypoglycemic effect.^[3]^[4]^[5]^[6]^[7]^[8] The reason Maitake lowers blood sugar is because the mushroom naturally contains an alpha glucosidase inhibitor.[1] Another plant attracting a lot of attention is Salacia oblonga.^{[citation needed]}

Role in clinical use [edit]

Alpha-glucosidase inhibitors are used to establish greater glycemic control over hyperglycemia in diabetes mellitus type 2, particularly with regard to postprandial hyperglycemia. They may be used as monotherapy in conjunction with an appropriate diabetic diet and exercise, or they may be used in conjunction with other anti-diabetic drugs.

Alpha-glucosidase inhibitors may also be useful in patients with diabetes mellitus type 1; however, this use has not been officially approved by the Food and Drug Administration.

Mechanism of action [edit]

Alpha-glucosidase inhibitors are saccharides that act as competitive inhibitors of enzymes needed to digest carbohydrates: specifically alpha-glucosidase enzymes in the brush border of the small intestines. The membrane-bound intestinal alpha-glucosidases hydrolyze oligosaccharides, trisaccharides, and disaccharides to glucose and other monosaccharides in the small intestine.

Acarbose also blocks pancreatic alpha-amylase in addition to inhibiting membrane-bound alpha-glucosidases. Pancreatic alpha-amylase hydrolyzes complex starches to oligosaccharides in the lumen of the small intestine.

Inhibition of these enzyme systems reduces the rate of digestion of carbohydrates. Less glucose is absorbed because the carbohydrates are not broken down into glucose molecules. In diabetic patients, the short-term effect of these drugs therapies is to decrease current blood glucose levels: the long term effect is a small reduction in hemoglobin _A1c level.^[9]

Dosing [edit]

Since alpha-glucosidase inhibitors are competitive inhibitors of the digestive enzymes, they must be taken at the start of main meals to have maximal effect. Their effects on blood sugar levels following meals will depend on the amount of complex carbohydrates in the meal.

Side effects & precautions [edit]

Since alpha-glucosidase inhibitors prevent the degradation of complex carbohydrates into glucose, the carbohydrates will remain in the intestine. In the colon, bacteria will digest the complex carbohydrates, thereby causing gastrointestinal side effects such as flatulence and diarrhea. Since these effects are dose-related, it is generally advised to start with a low dose and gradually increase the dose to the desired amount. Pneumatosis cystoides intestinalis is another reported side effect. If a patient using an alpha-glucosidase inhibitor suffers from an episode of hypoglycemia, the patient should eat something containing monosaccharides, such as glucose tablets. Since the drug will prevent the digestion of polysaccharides (or non-monosaccharides), non-monosaccharide foods may not effectively reverse a hypoglycemic episode in a patient taking an alpha-glucosidase inhibitor.

References [edit]

^ Benalla W. Bellahcen S. Bnouham M. Current Diabetes Reviews. "Antidiabetic medicinal plants as a source of alpha glucosidase inhibitors. [Review]" Current Diabetes Reviews. 6(4):247-54, 2010 Jul 1.
^ Ji F. Xiao G. Dong L. Ma Z. Ni J. Zhongguo Zhong Yao Za Zhi/Zhongguo Zhongyao Zazhi "Development of alpha-glucosidase inhibitor from medicinal herbs. [Review]" (mostly in Chinese) China Journal of Chinese Materia Medica. 35(12):1633-40, 2010 Jun.
^ name="pmid11903406" Konno S, Tortorelis DG, Fullerton SA, Samadi AA, Hettiarachchi J, Tazaki H. (Dec 2001), "A possible hypoglycaemic effect of maitake mushroom on Type 2 diabetic patients.", Diabet Med. 18 (12): 1010, doi:10.1046/j.1464-5491.2001.00532-5.x, ISSN 0742-3071, PMID 11903406
^ Hong L, Xun M, Wutong W. (Apr 2007), "Anti-diabetic effect of an alpha-glucan from fruit body of maitake (Grifola frondosa) on KK-Ay mice.", J Pharm Pharmacol 59 (4): 575–82, doi:10.1211/jpp.59.4.0013, ISSN 0022-3573, PMID 17430642
^ Kubo K, Aoki H, Nanba H. (Aug 1994), "Anti-diabetic activity present in the fruit body of Grifola frondosa (Maitake). I.", Biol Pharm Bull. 17 (8): 1106–10, doi:10.1248/bpb.17.1106, ISSN 0918-6158, PMID 7820117
^ Lo HC, Hsu TH, Chen CY. (2008), "Submerged culture mycelium and broth of Grifola frondosa improve glycemic responses in diabetic rats.", Am J Chin Med. 36 (2): 265–85, doi:10.1142/S0192415X0800576X, ISSN 0192-415X, PMID 18457360
^ Manohar V, Talpur NA, Echard BW, Lieberman S, Preuss HG. (Jan 2002), "Effects of a water-soluble extract of maitake mushroom on circulating glucose/insulin concentrations in KK mice.", Diabetes Obes Metab. 4 (1): 43–8, doi:10.1046/j.1463-1326.2002.00180.x, ISSN 1462-8902, PMID 11874441
^ Horio H, Ohtsuru M. (Feb 2001), "Maitake (Grifola frondosa) improve glucose tolerance of experimental diabetic rats.", J Nutr Sci Vitaminol (Tokyo). 47 (1): 57–63, doi:10.3177/jnsv.47.57, ISSN 0301-4800, PMID 11349892
^ Samantha J. Venable; Diane S. Aschenbrenner, Drug Therapy In Nursing, Hagerstown, MD: Lippincott Williams & Wilkins, ISBN 0-7817-4839-9

UpToDate Contents

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1. 糖尿病の治療におけるα-グルコシダーゼ阻害剤およびリパーゼ阻害剤 alpha glucosidase inhibitors and lipase inhibitors for treatment of diabetes mellitus
2. 2型糖尿病の予防 prevention of type 2 diabetes mellitus
3. 2型糖尿病における持続性高血糖のマネージメント management of persistent hyperglycemia in type 2 diabetes mellitus
4. 糖尿病の治療における低血糖のマネージメント management of hypoglycemia during treatment of diabetes mellitus
5. 高齢患者における2型糖尿病の治療 treatment of type 2 diabetes mellitus in the older patient

English Journal

Inhibitory kinetics and mechanism of kaempferol on α-glucosidase.

Peng X1, Zhang G2, Liao Y1, Gong D3.
Food chemistry.Food Chem.2016 Jan 1;190:207-15. doi: 10.1016/j.foodchem.2015.05.088. Epub 2015 May 19.
α-Glucosidase is a therapeutic target for diabetes mellitus, and α-glucosidase inhibitors play a vital role in the treatments for the disease. As a kind of potentially safer α-glucosidase inhibitor, flavonoids have attached much attention currently. In this study, kaempferol was found to show a n
PMID 26212963

Electrochemical assay of α-glucosidase activity and the inhibitor screening in cell medium.

Zhang J1, Liu Y2, Wang X1, Chen Y1, Li G3.
Biosensors & bioelectronics.Biosens Bioelectron.2015 Dec 15;74:666-72. doi: 10.1016/j.bios.2015.07.023. Epub 2015 Jul 11.
An electrochemical method is established in this work for the assay of α-glucosidase activity and the inhibitor screening through one-step displacement reaction, which can be directly used in cell medium. The displacement reaction can be achieved via strong binding of 4-aminophenyl-α-d-glucopyrano
PMID 26201984

Enzymatic synthesis of 2-deoxyglucose-containing maltooligosaccharides for tracing the location of glucose absorption from starch digestion.

Lee BH1, Koh DW2, Territo PR3, Park CS4, Hamaker BR5, Yoo SH6.
Carbohydrate polymers.Carbohydr Polym.2015 Nov 5;132:41-9. doi: 10.1016/j.carbpol.2015.06.012. Epub 2015 Jun 12.
The ileal brake mechanism which induces a potentially beneficial slower gastric emptying rate and increased satiety is triggered by macronutrients including glucose from glycemic carbohydrates. For optimization of this diet-induced health benefit, there is the need for a way to determine the locatio
PMID 26256322

Japanese Journal

α-グルコシダーゼ阻害薬 (特集糖尿病治療薬update : 適正な血糖管理を目指して) -- (糖尿病治療薬の薬効と適応基準)

遅野井健
日本臨床 73(3), 390-394, 2015-03
NAID 40020366973

Miglitol protects against age-dependent weight gain in mice: A potential role of increased UCP1 content in brown adipose tissue [Rapid Communication]

, , ,
Endocrine Journal advpub(0), 2015
… Miglitol is an absorbable alpha-glucosidase inhibitor that is used to control post-prandial hyperglycemia. …
NAID 130005060867

症例 α-グルコシダーゼ阻害薬と低グリセミック・インデックス食品が低血糖発作の回避に有効であることが持続血糖モニター(CGM)を用いて確認できたインスリン自己免疫症候群の1例

堀川敬,水柿祐子,本多敏朗 [他]
KKR札幌医療センター医学雑誌 11(1), 66-68, 2014
NAID 40020270308

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リンク元	「α-グルコシダーゼ阻害薬」「αグルコシダーゼ阻害剤」「α-グルコシダーゼ阻害剤」
関連記事	「inhibit」「inhibitor」「alpha」