Grapefruit component interacting with rat and human P450 CYP3A: possible involvement of non-flavonoid components in drug interaction

Biological & Pharmaceutical Bulletin
K FukudaY Yamazoe

Abstract

Active components in grapefruit juice, which modulate a cytochrome P450 (CYP3A) activity, were investigated. CYP3A-catalyzed 6beta-hydroxylation of testosterone in livers of rat and human was inhibited by the addition of an ethyl acetate-extract of grapefruit juice. Several components of grapefruit juice, including naringin, naringenin, limonin and obacunone, also showed inhibitory effects in human liver microsomes. However, the amounts of these components in grapefruit juice are too low to account for the inhibition by the ethyl acetate-extracts. Analyses with HPLC indicate the existence of inhibitory components in the extract, which are distinct from these known compounds and are specific to grapefruit juice. These results suggest that hydrophobic components other than flavonoids, probably coumarin derivatives, are responsible for the inhibitory effect of grapefruit juice.

Citations

Apr 12, 2000·British Journal of Clinical Pharmacology·C C LibersaM A Lhermitte
Nov 28, 2002·Pharmacology & Therapeutics·Bent H Havsteen
Feb 14, 1998·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·N MutoK Tanaka
Jan 25, 2011·Expert Opinion on Drug Metabolism & Toxicology·Michael J HanleyDavid J Greenblatt
May 9, 2002·Drug Metabolism Reviews·Slobodan Rendic
Sep 17, 2004·Biochemical and Biophysical Research Communications·Gilly Regev-ShoshaniZohar Kerem
Mar 17, 2005·Drug Metabolism and Pharmacokinetics·Hiroshi IwataTadashi Watabe
Oct 18, 2011·Toxicology in Vitro : an International Journal Published in Association with BIBRA·Yong-Long HanCheng Guo
May 4, 2001·JPEN. Journal of Parenteral and Enteral Nutrition·L N Chan
Jul 6, 2000·Japanese Journal of Pharmacology·L Q GuoY Yamazoe
Jan 1, 2008·Drug Metabolism and Drug Interactions·Kandhagatla RajnarayanaDevarakonda R Krishna
Aug 16, 2012·The Journal of Pharmacology and Experimental Therapeutics·Yi Zhu, Qing-Yu Zhang
Jul 31, 2001·Journal of Clinical Psychopharmacology·D J GreenblattR I Shader
Dec 13, 2019·The Journal of Pharmacy and Pharmacology·Keishi YamasakiHakaru Seo
Sep 3, 2003·Biological & Pharmaceutical Bulletin·Ken-Ichi FujitaKazuhiko Arimori
Jul 1, 2006·Journal of Natural Medicines·Shinzo HosoiAkiyo Sakushima
Oct 10, 1998·Journal of Chromatography. B, Biomedical Sciences and Applications·H W PengT H Tsai
Nov 7, 2020·International Journal of Molecular Sciences·Rahul PatelAmr ElShaer
Jun 22, 2000·Archives of Biochemistry and Biophysics·W TassaneeyakulY Yamazoe
Jun 6, 2000·Advanced Drug Delivery Reviews·X Li, W K Chan
Mar 20, 2004·Fitoterapia·Laura GiamperiDonata Ricci

❮ 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.