In Vitro and In Vivo Inhibition of Intestinal Glucose Transport by Guava (Psidium Guajava) Extracts

Mol Nutr Food Res. 2018 Jun;62(11):e1701012. doi: 10.1002/mnfr.201701012. Epub 2018 May 17.

Abstract

Scope: Known pharmacological activities of guava (Psidium guajava) include modulation of blood glucose levels. However, mechanistic details remain unclear in many cases.

Methods and results: This study investigated the effects of different guava leaf and fruit extracts on intestinal glucose transport in vitro and on postprandial glucose levels in vivo. Substantial dose- and time-dependent glucose transport inhibition (up to 80%) was observed for both guava fruit and leaf extracts, at conceivable physiological concentrations in Caco-2 cells. Using sodium-containing (both glucose transporters, sodium-dependent glucose transporter 1 [SGLT1] and glucose transporter 2 [GLUT2], are active) and sodium-free (only GLUT2 is active) conditions, we show that inhibition of GLUT2 was greater than that of SGLT1. Inhibitory properties of guava extracts also remained stable after digestive juice treatment, indicating a good chemical stability of the active substances. Furthermore, we could unequivocally show that guava extracts significantly reduced blood glucose levels (≈fourfold reduction) in a time-dependent manner in vivo (C57BL/6N mice). Extracts were characterized with respect to their main putative bioactive compounds (polyphenols) using HPLC and LC-MS.

Conclusion: The data demonstrated that guava leaf and fruit extracts can potentially contribute to the regulation of blood glucose levels.

Keywords: GLUT2; SGLT1; guava extract; intestinal glucose transport; postprandial blood glucose.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Biological Transport / drug effects
  • Caco-2 Cells
  • Female
  • Fruit / chemistry
  • Glucose / metabolism*
  • Glucose / pharmacokinetics
  • Glucose Transporter Type 2 / genetics
  • Glucose Transporter Type 2 / metabolism
  • Glucose Transporter Type 5 / genetics
  • Glucose Transporter Type 5 / metabolism
  • Humans
  • Hypoglycemic Agents / pharmacology
  • Intestinal Mucosa / drug effects*
  • Intestinal Mucosa / metabolism
  • Mice, Inbred C57BL
  • Plant Extracts / analysis
  • Plant Extracts / chemistry
  • Plant Extracts / pharmacology*
  • Plant Leaves / chemistry
  • Polyphenols / analysis
  • Postprandial Period
  • Psidium / chemistry*
  • Sodium-Glucose Transporter 1 / genetics
  • Sodium-Glucose Transporter 1 / metabolism

Substances

  • Glucose Transporter Type 2
  • Glucose Transporter Type 5
  • Hypoglycemic Agents
  • Plant Extracts
  • Polyphenols
  • SLC2A2 protein, human
  • SLC2A5 protein, human
  • SLC5A1 protein, human
  • Sodium-Glucose Transporter 1
  • Glucose