The Therapeutic Potential of Naringenin: A Review of Clinical Trials

Abstract

Naringenin is a flavonoid belonging to flavanones subclass. It is widely distributed in several Citrus fruits, bergamot, tomatoes and other fruits, being also found in its glycosides form (mainly naringin). Several biological activities have been ascribed to this phytochemical, among them antioxidant, antitumor, antiviral, antibacterial, anti-inflammatory, antiadipogenic and cardioprotective effects. Nonetheless, most of the data reported have been obtained from in vitro or in vivo studies. Although some clinical studies have also been performed, the main focus is on naringenin bioavailability and cardioprotective action. In addition, these studies were done in compromised patients (i.e., hypercholesterolemic and overweight), with a dosage ranging between 600 and 800 μM/day, whereas the effect on healthy volunteers is still debatable. In fact, naringenin ability to improve endothelial function has been well-established. Indeed, the currently available data are very promising, but further research on pharmacokinetic and pharmacodynamic aspects is encouraged to improve both available production and delivery methods and to achieve feasible naringenin-based clinical formulations.

Polyphenols: A concise overview on the chemistry, occurrence, and human health

“…The daily mean intake of naringenin has been estimated to be 58.1 mg (Ranka et al, ). Studies have been performed in hypercholesterolemic and overweight patients, with a dosage ranging between 600 and 800 μM/day (Salehi, Fokou, et al, ). Naringenin decreases low density lipoproteins and triglycerides, increases high density lipoproteins, and inhibits glucose uptake.…”

“…Naringenin, that is, the aglycone of naringin, is one of the best studied among the flavanones. It is mainly found in Citrus fruits, and a number of papers has highlighted its potential use in health conditions such as oxidative stress, inflammation, neurological disorders, and particularly cardiovascular/metabolic diseases (Salehi, Fokou, et al, 2019;Zeng, Jin, Zhang, Zhang, & Liang, 2018). The daily mean intake of naringenin has been estimated to be 58.1 mg (Ranka et al, 2008).…”

Dictyostelium discoideum as a pharmacological model system to study the mechanisms of medicinal drugs and natural products

“…PSENB,presenilin B protein;psrA,TPC1/2,TRPP2,transient receptor potential cation channel;PI3K,mTORC2, mechanistic target of rapamycin complex 2; RacGEF, Rho family GTPase guanine nucleotide exchange factor. benefits (Salehi et al, 2019). In D. discoideum, naringenin reduces cell growth, blocks cellular movement and causes cells to lose shape following acute (30 min) exposure (Waheed et al, 2014).…”

Plant‐derived glucose transport inhibitors with potential antitumor activity

“…(Rutaceae)], was found to decrease the 2‐DG uptake in differentiated 3 T3‐L1 cells, with IC 50 values of 61 μM and 71 μM under basal and insulin‐stimulated conditions, respectively (Claussnitzer, Skurk, Hauner, Daniel, & Rist, ). The potential antitumor activity of naringenin ( 9 ) has been discussed in a recent review article (Salehi et al, ). In an in vivo investigation, tumor metastasis was inhibited when 4‐week‐old female BALB/ c mice were inoculated with 4 T1 mouse breast cancer cells that were transduced with a TGF‐β1 generating 4 T1/TGF‐β1 cells and treated (orally) daily with 9 (200 mg/kg suspended in 1% carboxyl methyl cellulose) for 30 days (Zhang et al, ).…”