PMID- 35015798
OWN - NLM
STAT- MEDLINE
DCOM- 20220308
LR  - 20220308
IS  - 2042-650X (Electronic)
IS  - 2042-6496 (Linking)
VI  - 13
IP  - 3
DP  - 2022 Feb 7
TI  - Inhibitory activity of flavonoids against human sucrase-isomaltase 
      (alpha-glucosidase) activity in a Caco-2/TC7 cellular model.
PG  - 1108-1118
LID - 10.1039/d1fo02995a [doi]
AB  - Type 2 diabetes (T2D) is the most common form of diabetes, and the number of 
      people with this metabolic disease is steadily increasing worldwide. Among the 
      available antidiabetic agents, alpha-glucosidase inhibitors are the most effective at 
      reducing postprandial hyperglycaemia (PPHG), one of the main characteristics of 
      T2D. However, most of the studies that have been performed have used the more 
      readily available rat intestinal preparations or yeast alpha-glucosidase as the 
      enzyme source, which despite being useful and cost effective, have a questionable 
      physiological value. The present study evaluates the inhibitory activity of a 
      selected group of flavonoids against human sucrase-isomaltase (SI), the 
      alpha-glucosidase found in Caco-2/TC7 cells. A microassay using the physiological 
      substrates sucrose and maltose, and a synthetic substrate, 
      p-nitrophenyl-alpha-D-glucopyranoside (pNPG) was performed. The most active flavonoid 
      was compound 4 (melanoxetin), presenting an IC(50) value similar using the two 
      natural substrates. In contrast, the tested flavonoids were not effective at 
      inhibiting SI, when pNPG was used as a substrate. Hydroxylation of flavonoids at 
      C-3 of the C ring, at C-3' and C-4' of the B ring, and at C-7 and C-8 of the A 
      ring were the features that improved the inhibitory activity of flavonoids 
      against human SI. These phenolic compounds deserve further exploration as 
      alternatives to the currently available alpha-glucosidase inhibitors. The present 
      study also demonstrates that the non-clinical in vitro studies conducted for the 
      evaluation of alpha-glucosidase activity should use the human source rather than 
      surrogate sources of alpha-glucosidase.
FAU - Proenca, Carina
AU  - Proenca C
AUID- ORCID: 0000-0003-0859-6526
AD  - LAQV, REQUIMTE, Laboratory of Applied Chemistry, Department of Chemical Sciences, 
      Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal. 
      egracas@ff.up.pt.
FAU - Rufino, Ana T
AU  - Rufino AT
AUID- ORCID: 0000-0002-8800-9020
AD  - LAQV, REQUIMTE, Laboratory of Applied Chemistry, Department of Chemical Sciences, 
      Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal. 
      egracas@ff.up.pt.
FAU - Ferreira de Oliveira, Jose Miguel P
AU  - Ferreira de Oliveira JMP
AUID- ORCID: 0000-0002-3883-0806
AD  - LAQV, REQUIMTE, Laboratory of Applied Chemistry, Department of Chemical Sciences, 
      Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal. 
      egracas@ff.up.pt.
FAU - Freitas, Marisa
AU  - Freitas M
AUID- ORCID: 0000-0001-9114-9967
AD  - LAQV, REQUIMTE, Laboratory of Applied Chemistry, Department of Chemical Sciences, 
      Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal. 
      egracas@ff.up.pt.
FAU - Fernandes, Pedro A
AU  - Fernandes PA
AUID- ORCID: 0000-0003-2748-4722
AD  - UCIBIO, REQUIMTE, Department of Chemistry and Biochemistry, Faculty of Sciences, 
      University of Porto, 4169-007 Porto, Portugal.
FAU - Silva, Artur M S
AU  - Silva AMS
AUID- ORCID: 0000-0003-2861-8286
AD  - QOPNA and LAQV, REQUIMTE, Department of Chemistry, University of Aveiro, 3810-193 
      Aveiro, Portugal.
FAU - Fernandes, Eduarda
AU  - Fernandes E
AUID- ORCID: 0000-0001-6424-0976
AD  - LAQV, REQUIMTE, Laboratory of Applied Chemistry, Department of Chemical Sciences, 
      Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal. 
      egracas@ff.up.pt.
LA  - eng
PT  - Journal Article
DEP - 20220207
PL  - England
TA  - Food Funct
JT  - Food & function
JID - 101549033
RN  - 0 (Flavonoids)
RN  - 0 (Hypoglycemic Agents)
RN  - 0 (Plant Extracts)
RN  - EC 3.2.1.20 (alpha-Glucosidases)
SB  - IM
MH  - Animals
MH  - Caco-2 Cells
MH  - Diabetes Mellitus, Type 2/*drug therapy
MH  - Disease Models, Animal
MH  - Flavonoids/*pharmacology
MH  - Humans
MH  - Hypoglycemic Agents/*pharmacology
MH  - Plant Extracts/*pharmacology
MH  - Rats
MH  - alpha-Glucosidases/*pharmacology
EDAT- 2022/01/12 06:00
MHDA- 2022/03/09 06:00
CRDT- 2022/01/11 17:38
PHST- 2022/01/12 06:00 [pubmed]
PHST- 2022/03/09 06:00 [medline]
PHST- 2022/01/11 17:38 [entrez]
AID - 10.1039/d1fo02995a [doi]
PST - epublish
SO  - Food Funct. 2022 Feb 7;13(3):1108-1118. doi: 10.1039/d1fo02995a.