Beta-site amyloid precursor protein (APP) cleaving enzyme1 (BACE1) catalyzes the rate-limiting step of amyloid-β protein (Aβ) generation, and is considered as a prime target for Alzheimer's disease (AD). In search of a candidate for AD prevention, our efforts exploring the natural BACE1 inhibitor have led to the finding of nobiletin, tangeretin, and sinensetin-representative compounds of polyme...

Polymethoxyflavonoids (PMFs) are a family of the natural compounds that mainly compise nobiletin, tangeretin, heptamethoxyflavone (HMF), and tetramethoxyflavone (TMF) in citrus fruits. PMFs have shown various biological functions, including anti-oxidative effects. We previously showed that nobiletin, tangeretin, and HMF all inhibited interleukin (IL)-1-mediated osteoclast differentiation via th...

Nobiletin, a polymethoxy flavonoid (PMF), inhibits systemic bone resorption and maintains bone mass in estrogen-deficient ovariectomized mice. This study examined the anti-inflammatory effects of PMFs, nobiletin, and tangeretin on lipopolysaccharide (LPS)-induced bone resorption. Nobiletin and tangeretin suppressed LPS-induced osteoclast formation and bone resorption and suppressed the receptor...

The peels of citrus fruits (Pericarpium Citri Reticulatae, PCR) have long been used in traditional Chinese medicines (TCMs). Polymethoxylated flavonoids (PMFs) were found to be the main components present in PCR extracts, but their metabolism remains unclear which restrain the utilization of this TCM. In the present work, rat liver microsomes were immobilized on magnetic nanoparticles (LMMNPs) ...

Objective(s): Cisplatin is an effective antineoplastic agent; its clinical utility, however, is limited by a few salient toxic side effects like nephrotoxicity. This study aimed to determine the potential protective effects of tangeretin, a citrus-derived flavonoid, against renal tubular cell injury in cisplatin-induced renal toxicity of rats.Materials and Methods: Tangeretin was injected intra...

Abstract Citrus juice processing residues are mainly composed of peel, juice sack and seed. The peel, especially, consists of bioactive compounds such as flavones. Supercritical carbon dioxide (SC-CO2) extraction of flavonoid was carried out at a pressure of 30 MPa and temperature ranging from 80 to 160°C. Ratio of water and ethanol as a co-solvent was varied from 0 to 100%. Flavonoids such as ...

Flavonoids are widely occurring in our diet. In this study, the effects of nine flavonoids on acetaminophen (APAP) oxidation and related cytochrome P450 (P450) enzyme activities were investigated. With rat liver microsomes, APAP oxidation was stimulated 2- to 4-fold by 50 microM flavone or tangeretin and inhibited 65% by myricetin or quercetin. Only a slight inhibition of APAP oxidation was cau...

The presence in orange juice of compounds that specifically inhibit the P-glycoprotein (P-gp) drug efflux transporter, but not the cytochrome P450 (CYP) isozyme CYP3A4, was investigated. The uptake of [(3)H]vinblastine, a substrate of P-gp, by Caco-2 cells was measured. An ethyl acetate extract of orange juice did not affect the initial uptake rate of [(3)H]vinblastine but significantly increas...

Flavonoids are a group of polyphenolic compounds ubiquitous in many plants including fruits, vegetables, nuts, seeds, grains, tea and wine (Hollman & Katan, 1999). Flavonoids belong to two classes i) Flavanones and ii) Flavones. The most common flavanones are hesperetin from oranges and naringenin from grapefruit. The most common flavones, also known as polymethoxylated flavones, are tangeretin...

A study of relationships between the structure of flavones, flavanones, and chalcones and their capacity to induce increased 3,4-benzpyrene (BP) hydroxylase activity in the liver and lung of the rat has been carried out. Appropriate halogenation in creases inducing activity. In the compounds studied, hydroxylation reduces inducing capacity, but the corresponding methoxy compounds are active. Tw...