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      Hypoglycemic Efficacy of Docking Selected Natural Compounds against α-Glucosidase and α-Amylase

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          Abstract

          The inhibition of α-glucosidase and α-amylase is a clinical strategy for the treatment of type II diabetes, and herbal medicines have been reported to credibly alleviate hyperglycemia. Our previous study has reported some constituents from plant or herbal sources targeted to α-glucosidase and α-amylase via molecular docking and enzymatic measurement, but the hypoglycemic potencies in cell system and mice have not been validated yet. This study was aimed to elucidate the hypoglycemic efficacy of docking selected compounds in cell assay and oral glucose and starch tolerance tests of mice. All test compounds showed the inhibition of α-glucosidase activity in Caco-2 cells. The decrease of blood sugar levels of test compounds in 30 min and 60 min of mice after OGTT and OSTT, respectively and the decreased glucose levels of test compounds were significantly varied in acarbose. Taken altogether, in vitro and in vivo experiments suggest that selected natural compounds (curcumin, antroquinonol, HCD, docosanol, tetracosanol, rutin, and actinodaphnine) via molecular docking were confirmed as potential candidates of α-glucosidase and α-amylase inhibitors for treating diabetes.

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          Acarbose for prevention of type 2 diabetes mellitus: the STOP-NIDDM randomised trial.

          Jean-Louis Chiasson, Robert G Josse, Ramon Gomis … (2002)
          The worldwide increase in type 2 diabetes mellitus is becoming a major health concern. We aimed to assess the effect of acarbose in preventing or delaying conversion of impaired glucose tolerance to type 2 diabetes. In a multicentre, placebo-controlled randomised trial, we randomly allocated patients with impaired glucose tolerance to 100 mg acarbose or placebo three times daily. The primary endpoint was development of diabetes on the basis of a yearly oral glucose tolerance test (OGTT). Analyses were by intention to treat. We randomly allocated 714 patients with impaired glucose tolerance to acarbose and 715 to placebo. We excluded 61 (4%) patients because they did not have impaired glucose tolerance or had no postrandomisation data. 211 (31%) of 682 patients in the acarbose group and 130 (19%) of 686 on placebo discontinued treatment early. 221 (32%) patients randomised to acarbose and 285 (42%) randomised to placebo developed diabetes (relative hazard 0.75 [95% CI 0.63-0.90]; p=0.0015). Furthermore, acarbose significantly increased reversion of impaired glucose tolerance to normal glucose tolerance (p<0.0001). At the end of the study, treatment with placebo for 3 months was associated with an increase in conversion of impaired glucose tolerance to diabetes. The most frequent side-effects to acarbose treatment were flatulence and diarrhoea. Acarbose could be used, either as an alternative or in addition to changes in lifestyle, to delay development of type 2 diabetes in patients with impaired glucose tolerance.
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            Hypoglycaemia in diabetes mellitus: epidemiology and clinical implications.

            Brian M. Frier (2014)
            Hypoglycaemia is a frequent adverse effect of treatment of diabetes mellitus with insulin and sulphonylureas. Fear of hypoglycaemia alters self-management of diabetes mellitus and prevents optimal glycaemic control. Mild (self-treated) and severe (requiring help) hypoglycaemia episodes are more common in type 1 diabetes mellitus but people with insulin-treated type 2 diabetes mellitus are also exposed to frequent hypoglycaemic events, many of which occur during sleep. Hypoglycaemia can disrupt many everyday activities such as driving, work performance and leisure pursuits. In addition to accidents and physical injury, the morbidity of hypoglycaemia involves the cardiovascular and central nervous systems. Whereas coma and seizures are well-recognized neurological sequelae of hypoglycaemia, much interest is currently focused on the potential for hypoglycaemia to cause dangerous and life-threatening cardiac complications, such as arrhythmias and myocardial ischaemia, and whether recurrent severe hypoglycaemia can cause permanent cognitive impairment or promote cognitive decline and accelerate the onset of dementia in middle-aged and elderly people with diabetes mellitus. Prevention of hypoglycaemia is an important part of diabetes mellitus management and strategies include patient education, glucose monitoring, appropriate adjustment of diet and medications in relation to everyday circumstances including physical exercise, and the application of new technologies such as real-time continuous glucose monitoring, modified insulin pumps and the artificial pancreas.
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              Effects of acarbose on cardiovascular and diabetes outcomes in patients with coronary heart disease and impaired glucose tolerance (ACE): a randomised, double-blind, placebo-controlled trial

              Yong Huo, Zhihui Lang, John J McMurray … (2017)
              Article 0 comments Cited 105 times – based on 0 reviews     Review now
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                Author and article information

                Journal
                Journal ID (nlm-ta): Molecules
                Journal ID (iso-abbrev): Molecules
                Journal ID (publisher-id): molecules
                Title: Molecules : A Journal of Synthetic Chemistry and Natural Product Chemistry
                Publisher: MDPI
                ISSN (Electronic): 1420-3049
                Publication date (Electronic): 05 September 2018
                Publication date Collection: September 2018
                Volume: 23
                Issue: 9
                Electronic Location Identifier: 2260
                Affiliations
                [1 ]Department of Life Science and Institute of Biotechnology, National Dong-Hwa University, Hualien 97401, Taiwan; mecurry@ 123456gmail.com (J.R.); 810613101@ 123456gms.ndhu.edu.tw (C-H.J.); d9813003@ 123456gms.ndhu.edu.tw (S-R.L.); 810413105@ 123456gms.ndhu.edu.tw (C-H.C.)
                [2 ]Neural Regeneration Laboratory, Neurological Institute, Taipei Veterans General Hospital, Taipei 11217, Taiwan; mjtsai2@ 123456vghtpe.gov.tw
                [3 ]Department of Biotechnology and Animal Science, National Ilan University, Ilan 26047, Taiwan; dnlee@ 123456niu.edu.tw
                [4 ]National Museum of Marine Biology and Aquarium, Pingtung 94450, Taiwan; pjsung@ 123456nmmba.gov.tw
                [5 ]Graduate Institute of Marine Biotechnology, National Dong Hwa University, Pingtung 94450, Taiwan
                [6 ]Department of Chemistry, National Dong Hwa University, Hualien 97401, Taiwan
                Author notes
                [* ]Correspondence: leong@ 123456gms.ndhu.edu.tw (M.K.L.); cfweng@ 123456gms.ndhu.edu.tw (C-F.W.); Tel.: +866-3-890-3609 (M.K.L.); +886-3-890-3637 (C-F.W.); Fax: +886-3-890-0162 (M.K.L.); +886-3-890-0163 (C-F.W.)
                [†]

                These authors contributed equally to this work.

                Author information
                https://orcid.org/0000-0002-4160-2361
                https://orcid.org/0000-0002-6644-9236
                https://orcid.org/0000-0002-6927-1517
                Article
                Publisher ID: molecules-23-02260
                DOI: 10.3390/molecules23092260
                PMC ID: 6225388
                PubMed ID: 30189596
                SO-VID: e06c88fe-a5d2-4912-b2cf-808629673993
                Copyright © © 2018 by the authors.
                License:

                Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license ( http://creativecommons.org/licenses/by/4.0/).

                History
                Date received : 07 August 2018
                Date accepted : 03 September 2018
                Categories
                Subject: Article

                Keywords: natural compound,α-glucosidase,α-amylase
                Data availability:
                Keywords: natural compound, α-glucosidase, α-amylase

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