Inhibitory effect of a bitter melon extract on the P-glycoprotein activity in intestinal Caco-2 cells

British Journal of Pharmacology
Tomoko KonishiMakoto Shimizu

Abstract

Extracts of bitter melon, soybean, dokudami and welsh onion by 40% methanol increased the accumulation of rhodamine-123 by Caco-2 cells, suggesting that these extracts inhibited P-glycoprotein (P-gp). The extract of bitter melon was separated in a tC18 cartridge column and the eluate from 80% acetonitrile most markedly increased the [(3)H]-daunomycin accumulation by Caco-2 cells. The inhibitory compounds in the bitter melon fraction were isolated by HPLC with Pegasil C4 and Pegasil ODS columns. The HPLC fraction having the highest activity was analyzed by (1)H-NMR and FAB-MS, and the active compound was identified as 1-monopalmitin. The inhibitory activities of 1-monopalmitin and its related compounds suggested that the inhibition of P-gp activity was not dependent on the degree of unsaturation of fatty acid in the monoglyceride, but on the chain length. It was also suggested that the monoglyceride structure played an important role in the inhibition of P-gp activity. Monoglycerides could therefore alter the pharmacokinetics of drugs by inhibiting the P-gp-mediated efflux.

References

Oct 15, 1990·FEBS Letters·S Lee-HuangP L Huang
Nov 1, 1987·Proceedings of the National Academy of Sciences of the United States of America·F ThiebautM C Willingham
Sep 12, 1995·Proceedings of the National Academy of Sciences of the United States of America·S Lee-HuangH F Kung
Dec 1, 1996·Critical Reviews in Food Science and Nutrition·E Boyle, J B German
Apr 23, 1999·Pharmaceutical Research·R B KimG R Wilkinson
Dec 11, 1999·Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan·H Suzuki
Feb 16, 2000·European Journal of Cancer : Official Journal for European Organization for Research and Treatment of Cancer (EORTC) [and] European Association for Cancer Research (EACR)·C A PlouzekG C Yeh
Nov 22, 2001·Biochemical and Biophysical Research Communications·E J WangW W Johnson
Jan 30, 2002·Journal of Nutritional Science and Vitaminology·T MiuraI Suzuki
Sep 5, 2002·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Bhagwant D RegeJames E Polli
Mar 11, 2003·American Journal of Health-system Pharmacy : AJHP : Official Journal of the American Society of Health-System Pharmacists·Ethan BaschCatherine Ulbricht
May 23, 2003·Journal of Pharmaceutical Sciences·Katrijn BogmanJürgen Drewe
Nov 13, 2008·Cytotechnology·U A Germann, T C Chambers

❮ Previous
Next ❯

Citations

Mar 3, 2007·Nature Reviews. Drug Discovery·Christopher J H PorterWilliam N Charman
Feb 10, 2009·Bioscience, Biotechnology, and Biochemistry·Hitoshi InokuchiMakoto Shimizu
Feb 9, 2010·Bioscience, Biotechnology, and Biochemistry·Makoto Shimizu
Sep 3, 2013·Evidence-based Complementary and Alternative Medicine : ECAM·Haw-Wen ChenChong-Kuei Lii
Apr 9, 2014·Expert Opinion on Drug Metabolism & Toxicology·Parvin Zakeri-Milani, Hadi Valizadeh
Jun 24, 2009·Expert Opinion on Drug Metabolism & Toxicology·Wenxia ZhangLee Yong Lim
Nov 3, 2009·Phytomedicine : International Journal of Phytotherapy and Phytopharmacology·Chadarat AmpasavateNusara Piyapolrungroj
Jan 18, 2008·Advanced Drug Delivery Reviews·Joseph M CustodioLeslie Z Benet
May 10, 2011·Journal of Clinical Pharmacology·Werner SiegmundWilhelm Kirch
Jul 28, 2016·Seminars in Cancer Biology·Komal RainaRajesh Agarwal
Jan 7, 2006·Phytotherapy Research : PTR·Varaporn Buraphacheep JunyaprasertMikihisa Takano
Oct 17, 2020·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Camila Juliana DomínguezAldo Domingo Mottino
Oct 5, 2020·Food and Chemical Toxicology : an International Journal Published for the British Industrial Biological Research Association·Jack W StaplesErica L Woodahl
Mar 19, 2020·Cell Reports·Daniel RekerGiovanni Traverso
Jun 11, 2008·Journal of Agricultural and Food Chemistry·Hideo SatsuMakoto Shimizu

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.