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Last update 23 Jan 2025

MGAM

Last update 23 Jan 2025

Basic Info

Synonyms

Alpha-1,4-glucosidase, alpha-glucosidase, maltase-glucoamylase

+ [4]

Introduction

Alpha-(1,4) exo-glucosidase involved in breakdown of dietary starch oligosaccharides in small intestine. Cleaves the non-reducing alpha-(1,4)-linked glucose residue in linear dextrins with retention of anomeric center stereochemistry (PubMed:12547908, PubMed:18356321, PubMed:27480812, PubMed:18036614, PubMed:22058037). Mainly hydrolyzes short length oligomaltoses having two to seven glucose residues (PubMed:12547908, PubMed:18356321, PubMed:27480812, PubMed:18036614, PubMed:22058037). Can cleave alpha-(1,2), alpha-(1,3) and alpha-(1,6) glycosidic linkages with lower efficiency, whereas beta glycosidic linkages are usually not hydrolyzed (PubMed:27480812).

Drugs associated with MGAM

Mitiglinide Calcium Hydrate/Voglibose

Target

MGAM x Potassium channel x VGKCs

Mechanism

MGAM inhibitors [+2]

Active Org.

Kissei Pharmaceutical Co., Ltd.

Originator Org.

Kissei Pharmaceutical Co., Ltd.

Active Indication

Diabetes Mellitus, Type 2

Inactive Indication-

Drug Highest PhaseApproved

First Approval Ctry. / Loc.

First Approval Date22 Apr 2011

Voglibose/Metformin Hydrochloride

Target

MGAM x PRKAB1

Mechanism

MGAM inhibitors [+1]

Active Org.

Athena Pharmaceutiques SAS

Originator Org.

Athena Pharmaceutiques SAS

Active Indication

Diabetes Mellitus, Type 2

Inactive Indication-

Drug Highest PhaseApproved

First Approval Ctry. / Loc.

First Approval Date01 Jan 2011

Acarbose

Target

Alpha-amylase x GANC x MGAM x α-glucosidase

Mechanism

Alpha-amylase inhibitors [+3]

Active Org.

Shanghai Shyndec Pharmaceutical Co., Ltd. [+2]

Originator Org.

Bayer AG

Active Indication

Diabetes Mellitus, Type 2 [+1]

Inactive Indication

Glucose Intolerance

Drug Highest PhaseApproved

First Approval Ctry. / Loc.

First Approval Date06 Sep 1995

239

Clinical Trials associated with MGAM

NCT05487859

/ Not yet recruitingPhase 2IIT

A Pilot Study of the Immunomodulatory Agent Acarbose in Combination With Standard Therapy in Metastatic Renal Cell Carcinoma (RCC)

The purpose of this study is to determine the safety and tolerability of acarbose in combination of immunotherapy based standard of care therapy in advanced renal cell carcinoma patients.

Start Date05 Oct 2025

Sponsor / Collaborator

The University of Alabama at Birmingham

CTR20243825

/ CompletedNot Applicable

伏格列波糖片人体生物等效性研究

[Translation] Study on the bioequivalence of voglibose tablets in healthy volunteers

本试验旨在研究单次空腹口服北京星昊医药股份有限公司生产的伏格列波糖片（0.2 mg）的药效学特征；以天津武田药品有限公司生产的伏格列波糖片（倍欣®，0.2 mg）为参比制剂，比较口服两制剂后血糖的△CSG,max、△AUEC0-2 h，评价两制剂的人体生物等效性。

[Translation]

This study aimed to study the pharmacodynamic characteristics of a single fasting oral administration of voglibose tablets (0.2 mg) produced by Beijing Xinghao Pharmaceutical Co., Ltd.; using voglibose tablets (Bexin®, 0.2 mg) produced by Tianjin Takeda Pharmaceutical Co., Ltd. as the reference preparation, to compare the △CSG,max and △AUEC0-2 h of blood glucose after oral administration of the two preparations, and to evaluate the bioequivalence of the two preparations in humans.

Start Date02 Nov 2024

Sponsor / Collaborator

Beijing Sunho Pharmaceutical Co., Ltd.

CTR20242708

/ CompletedNot Applicable

伏格列波糖片在健康受试者中的生物等效性研究

[Translation] Bioequivalence study of voglibose tablets in healthy subjects

主要目的：采用随机、开放、单剂量、两制剂、两序列、四周期、完全重复交叉给药设计比较上海现代制药股份有限公司生产的伏格列波糖片（规格：0.3mg）与Teva Takeda Yakuhin Ltd.持证的伏格列波糖片（商品名：倍欣®，规格：0.3mg）的药效动力学参数，评价受试制剂与参比制剂在空腹条件下的人体生物等效性。次要目的：观察受试制剂和参比制剂在健康受试者中的安全性。

[Translation]

Primary objective: To compare the pharmacodynamic parameters of voglibose tablets (specification: 0.3 mg) produced by Shanghai Modern Pharmaceutical Co., Ltd. and voglibose tablets (trade name: Beixin®, specification: 0.3 mg) certified by Teva Takeda Yakuhin Ltd. using a randomized, open, single-dose, two-preparation, two-sequence, four-period, completely repeated crossover design, and to evaluate the bioequivalence of the test preparation and the reference preparation under fasting conditions. Secondary objective: To observe the safety of the test preparation and the reference preparation in healthy subjects.

Start Date14 Oct 2024

Sponsor / Collaborator

Shanghai Shyndec Pharmaceutical Co., Ltd.

100 Clinical Results associated with MGAM

100 Translational Medicine associated with MGAM

0 Patents (Medical) associated with MGAM

557

Literatures (Medical) associated with MGAM

01 Mar 2025·Food Chemistry

Peptidomics and molecular dynamics on bioactive peptides produced and characterized from the fermented whey of “Panchali” sheep of West India

Article

Author: Patil, G B ; Sarkar, Preetam ; Gawai, Kunal ; Tiwary, Bipransh Kumar ; Mankad, Maunil ; Sakure, Amar A ; Basaiawmoit, Bethsheba ; Hati, Subrota ; Kondepudi, Kanthi Kiran ; Pipaliya, Rinkal ; Bishnoi, Mahendra ; Maurya, Ruchika

The study assessed the peptide production by using potent Lactiplantibacillus plantarum KGL3A (MG722814) culture to ferment the sheep milk for evaluation of α-glucosidase inhibition, ACE inhibition, α-amylase inhibition, & inhibiting lipase activities. The maximal ACE inhibitory, α-amylase, α-glucosidase, & lipase inhibiting actions were 71.69 %, 71.32 %, 67.14 %, and 64.15 %, respectively, at 37 °C after 48 h. Proteolytic activity was tested at various incubation times & inoculation rates to maximise the conditions for growth and the greatest action (9.38 mg/mL) was reported at 2.5 % rate of inoculation after incubation of 48 h. The anti-diabetic as well as ACE inhibitory properties of less than 3 kDa were maximum in contrast to >3 kDa, <10 kDa, and > 10 kDa cut-off fractions. Further, when LPS stimulation is applied to RAW 267.4 macrophage cells, the overabundance generation of IL-6, IL-1β, NO, and TNF-α is greatly reduced by using KGL3A to ferment sheep milk. 2D gel electrophoresis & SDS-PAGE were utilized in relation to protein purifications. Maximum numbers of sheep milk's fermented protein bands were present, about 10 to 124 kDa by SDS-PAGE, and 38 spots of protein were discovered using 2D gel chromatography. Ultra-filtered fractions water soluble extracts (WSEs) were employed in RP-HPLC to differentiate between various peptide fractions. The peptide sequences produced were matched using the databases of AHTPDB and BIOPEP to match hypertensive peptides & antidiabetic peptides, respectively. Furthermore, the discovered peptide sequences from the fermenting sheep milk was studied due to their penchant for binding against the active locations of human bile salt activated lipase (hBAL); human maltase-glucoamylase (hMGA); human pancreatic alpha-amylase (hPAM); & human angiotensin-converting enzyme (hACE) through molecular docking.

01 Feb 2025·Physiology & Behavior

Plasma proteomic signature of chronic psychosocial stress in mice

Article

Author: O'Connor, Lewis A ; English, Jane A. ; O'Leary, Olivia F ; Scaife, Caitriona ; Golubeva, Anna V ; Golubeva, Anna V. ; Nolan, Yvonne M ; Donoso, Francisco ; O'Connor, Lewis A. ; Nolan, Yvonne M. ; English, Jane A ; Melo, Thieza G ; Melo, Thieza G. ; O'Leary, Olivia F.

Chronic stress significantly impacts both physical and mental wellbeing, increasing risk of cardiovascular disease, immune dysregulation, and psychiatric conditions such as depression and anxiety disorders. The plasma proteome is a valuable source of biomarkers of health and disease, but the limited number of studies exploring the potential of the plasma proteome as a biomarker for stress-related disorders underscores the importance of further investigation of the effects of chronic stress on the plasma proteome. The aim of this study was to examine the effect of a 5-week chronic psychosocial stress paradigm on the plasma proteome in mice and to determine if any affected proteins correlated with stress-induced changes in behaviour and physiology, and thus might represent biomarkers of negative impacts of chronic stress. Using LC-MS/MS proteomic analysis, 38 proteins in the mouse plasma proteome were identified to be affected by chronic psychosocial stress. Functional analysis revealed that these proteins clustered into biological functions including inflammatory response, regulation of the immune response, complement and coagulation cascades, lipid metabolic process, and high-density lipoprotein particles. Correlation analyses of the identified proteins with stress-induced behavioral or physiological changes stress revealed significant correlations between stress-induced anxiety-like behaviour and Phosphatidylinositol-glycan-specific phospholipase D, Complement C2, Epidermal growth factor receptor, Prosaposin, Actin-related protein 2/3 complex subunit 1B, Maltase-glucoamylase, Mannosyl-oligosaccharide 1,2-alpha-mannosidase IA and Fibrinogen-like protein 1. Chronic psychosocial stress blunted acute stress-induced corticosterone release, and this correlated with abundance of Pyrethroid hydrolase Ces2a; N-fatty-acyl-amino acid synthase/hydrolase Pm20d1, Mannosyl-oligosaccharide 1,2-alpha-mannosidase IA, Alpha-2-macroglobulin-P and L-selectin. Finally, stress-induced reductions in both brown and epididymal fat correlated with Phosphatidylinositol-glycan-specific phospholipase D, Complement C2, Epidermal growth factor receptor, Kininogen-1, Apolipoprotein M, Angiopoietin-related protein 3, Proprotein convertase subtilisin/kexin type 9, and Lipopolysaccharide-binding protein. These findings demonstrate that chronic psychosocial stress induces alterations in plasma proteins implicated in key biological processes and pathways related to stress response, immune function, and lipid metabolic regulation. Further investigation into these proteins may provide new avenues for identification of biomarkers or mediators of stress-induced pathology.

08 Jan 2025·Journal of Agricultural and Food Chemistry

Expression of Recombinant Human α-Glucosidase in HEK293 Cells

Article

Author: Qiao, Ying ; Odagaki, Yuki ; Ikeda, Yuki ; Takita, Teisuke ; Arikawa, Emi ; Nishimoto, So ; Debarbat, Anaïs ; Ito, Masaaki ; Kimura, Toshiyuki ; Yano, Haruna ; Yasukawa, Kiyoshi

In mammals, intestinal α-glucosidase exists as a maltase-glucoamylase complex (MGAM) and a sucrase-isomaltase complex (SI). In this study, we transiently expressed human MGAM and SI in human embryonic kidney 293 (HEK293) cells. At pH 6.0 and 37 °C, the MGAM-expressing HEK293 cells extract (MGE) exhibited maltase, glucoamylase, and isomaltase activities but not sucrase activity, whereas the SI-expressing HEK293 cells extract (SIE) exhibited sucrase, isomaltase, and maltase activities but not glucoamylase activity. The apparent K_m value of the MGE for maltose hydrolysis was 14-26% of that of the SIE for maltose, sucrose, and isomaltose hydrolysis. The respective apparent V_max values of the MGE and SIE for sucrose and isomaltose hydrolysis were 0% and 6% and 10% and 42% of those for maltose hydrolysis. These results indicated that the maltase activities of MGAM and SI were higher than those of sucrase and isomaltase.

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