Demonstrating the involvement of an active efflux mechanism in the intestinal absorption of chlorogenic acid and quinic acid using a Caco-2 bidirectional permeability assay

2021 ◽  
Author(s):  
Olivier Mortelé ◽  
Jennifer Jörissen ◽  
Irina Spacova ◽  
Sarah Lebeer ◽  
Alexander L. N. van Nuijs ◽  
...  
Keyword(s):  
Chlorogenic Acid ◽  
Intestinal Absorption ◽  
Quinic Acid ◽  
Active Efflux ◽  
Efflux Mechanism ◽  
Permeability Assay

The intestinal absorption of chlorogenic acid and quinic acid was investigated using an in vitro bidirectional Caco-2 permeability assay and LC-MS/MS.

scholarly journals Front cover: In Vitro Gut Metabolism of [U-13 C]-Quinic Acid, The Other Hydrolysis Product of Chlorogenic Acid

2018 ◽  
Vol 62 (22) ◽  
pp. 1870094
Author(s):  
Martine Naranjo Pinta ◽  
Ivan Montoliu ◽  
Anna-Marja Aura ◽  
Tuulikki Seppänen-Laakso ◽  
Denis Barron ◽  
...  
Keyword(s):  
Chlorogenic Acid ◽  
Hydrolysis Product ◽  
Quinic Acid ◽  
The Other ◽  
Front Cover ◽  
Gut Metabolism

Caffeic and chlorogenic acids inhibit key enzymes linked to type 2 diabetes (in vitro): a comparative study

2015 ◽  
Vol 26 (2) ◽  
Author(s):  
Ganiyu Oboh ◽  
Odunayo M. Agunloye ◽  
Stephen A. Adefegha ◽  
Ayodele J. Akinyemi ◽  
Adedayo O. Ademiluyi
Keyword(s):  
Type 2 Diabetes ◽  
Chlorogenic Acid ◽  
Caffeic Acid ◽  
Phenolic Acids ◽  
Quinic Acid ◽  
Inhibitory Effect ◽  
Dependent Manner ◽  
Key Enzymes

AbstractChlorogenic acid is a major phenolic compound that forms a substantial part of plant foods and is an ester of caffeic acid and quinic acid. However, the effect of the structures of both chlorogenic and caffeic acids on their antioxidant and antidiabetic potentials have not been fully understood. Thus, this study sought to investigate and compare the interaction of caffeic acid and chlorogenic acid with α-amylase and α-glucosidase (key enzymes linked to type 2 diabetes) activities in vitro.The inhibitory effect of the phenolic acids on α-amylase and α-glucosidase activities was evaluated. Thereafter, their antioxidant activities as typified by their 1,1-diphenyl-2 picrylhydrazyl radical scavenging ability and ferric reducing antioxidant properties were determined.The results revealed that both phenolic acids inhibited α-amylase and α-glucosidase activities in a dose-dependent manner (2–8 μg/mL). However, caffeic acid had a significantly (p<0.05) higher inhibitory effect on α-amylase [ICThe esterification of caffeic acid with quinic acid, producing chlorogenic acid, reduces their ability to inhibit α-amylase and α-glucosidase activities. Thus, the inhibition of α-amylase and α-glucosidase activities by the phenolic acids could be part of the possible mechanism by which the phenolic acids exert their antidiabetic effects.

In Vitro Gut Metabolism of [U-13C]-Quinic Acid, The Other Hydrolysis Product of Chlorogenic Acid

2018 ◽  
Vol 62 (22) ◽  
pp. 1800396 ◽  
Author(s):  
Martine Naranjo Pinta ◽  
Ivan Montoliu ◽  
Anna-Marja Aura ◽  
Tuulikki Seppänen-Laakso ◽  
Denis Barron ◽  
...  
Keyword(s):  
Chlorogenic Acid ◽  
Hydrolysis Product ◽  
Quinic Acid ◽  
The Other ◽  
Gut Metabolism

Anti-hepatitis B virus activity of chlorogenic acid, quinic acid and caffeic acid in vivo and in vitro

2009 ◽  
Vol 83 (2) ◽  
pp. 186-190 ◽  
Author(s):  
Gui-Feng Wang ◽  
Li-Ping Shi ◽  
Yu-Dan Ren ◽  
Qun-Fang Liu ◽  
Hou-Fu Liu ◽  
...  
Keyword(s):  
Hepatitis B Virus ◽  
Hepatitis B ◽  
Chlorogenic Acid ◽  
Caffeic Acid ◽  
Quinic Acid ◽  
Virus Activity ◽  
B Virus

scholarly journals Role of Acid pH and Deficient Efflux of Pyrazinoic Acid in Unique Susceptibility of Mycobacterium tuberculosis to Pyrazinamide

1999 ◽  
Vol 181 (7) ◽  
pp. 2044-2049 ◽  
Author(s):  
Ying Zhang ◽  
Angelo Scorpio ◽  
Hiroshi Nikaido ◽  
Zhonghe Sun
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Efflux Pump ◽  
Acidic Ph ◽  
Active Efflux ◽  
Highly Active ◽  
Efflux Mechanism ◽  
Pyrazinoic Acid

ABSTRACT Pyrazinamide (PZA) is an important antituberculosis drug. Unlike most antibacterial agents, PZA, despite its remarkable in vivo activity, has no activity against Mycobacterium tuberculosis in vitro except at an acidic pH. M. tuberculosis is uniquely susceptible to PZA, but other mycobacteria as well as nonmycobacteria are intrinsically resistant. The role of acidic pH in PZA action and the basis for the unique PZA susceptibility of M. tuberculosisare unknown. We found that in M. tuberculosis, acidic pH enhanced the intracellular accumulation of pyrazinoic acid (POA), the active derivative of PZA, after conversion of PZA by pyrazinamidase. In contrast, at neutral or alkaline pH, POA was mainly found outside M. tuberculosis cells. PZA-resistantM. tuberculosis complex organisms did not convert PZA into POA. Unlike M. tuberculosis, intrinsically PZA-resistant M. smegmatis converted PZA into POA, but it did not accumulate POA even at an acidic pH, due to a very active POA efflux mechanism. We propose that a deficient POA efflux mechanism underlies the unique susceptibility of M. tuberculosisto PZA and that the natural PZA resistance of M. smegmatis is due to a highly active efflux pump. These findings may have implications with regard to the design of new antimycobacterial drugs.

Characterization and In Vitro Evaluation of Intestinal Absorption of Liposomes Encapsulating Zanamivir

2011 ◽  
Vol 8 (4) ◽  
pp. 392-397 ◽  
Author(s):  
Boontarika Boonyapiwat ◽  
Narong Sarisuta ◽  
Sarinnate Kunastitchai
Keyword(s):  
Intestinal Absorption ◽  
In Vitro Evaluation

Alpha-lactalbumin Effect on Myo-inositol Intestinal Absorption: In vivo and In vitro

2018 ◽  
Vol 15 (9) ◽  
pp. 1305-1311 ◽  
Author(s):  
Giovanni Monastra ◽  
Yula Sambuy ◽  
Simonetta Ferruzza ◽  
Daniela Ferrari ◽  
Giulia Ranaldi
Keyword(s):  
Intestinal Absorption ◽  
Intestinal Absorption In Vivo ◽  
Alpha Lactalbumin

In Silico Assessment of ADME Properties: Advances in Caco-2 Cell Monolayer Permeability Modeling

2019 ◽  
Vol 18 (26) ◽  
pp. 2209-2229 ◽  
Author(s):  
Hai Pham-The ◽  
Miguel Á. Cabrera-Pérez ◽  
Nguyen-Hai Nam ◽  
Juan A. Castillo-Garit ◽  
Bakhtiyor Rasulev ◽  
...  
Keyword(s):  
Intestinal Absorption ◽  
In Silico ◽  
Review Paper ◽  
Cell Monolayer ◽  
Cell Permeability ◽  
Drug Substances ◽  
Wide Range ◽  
Modeling Techniques

One of the main goals of in silico Caco-2 cell permeability models is to identify those drug substances with high intestinal absorption in human (HIA). For more than a decade, several in silico Caco-2 models have been made, applying a wide range of modeling techniques; nevertheless, their capacity for intestinal absorption extrapolation is still doubtful. There are three main problems related to the modest capacity of obtained models, including the existence of inter- and/or intra-laboratory variability of recollected data, the influence of the metabolism mechanism, and the inconsistent in vitro-in vivo correlation (IVIVC) of Caco-2 cell permeability. This review paper intends to sum up the recent advances and limitations of current modeling approaches, and revealed some possible solutions to improve the applicability of in silico Caco-2 permeability models for absorption property profiling, taking into account the above-mentioned issues.

Sign in / Sign up

Export Citation Format

Share Document