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Preclinical Evidence for the Pharmacological Actions of Naringin: a Review

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Preclinical Evidence for the Pharmacological Actions of Naringin: a Review Reviews 437 Preclinical Evidence for the Pharmacological Actions of Naringin: A Review Authors Saurabh Bharti, Neha Rani, Bhaskar Krishnamurthy, Dharamvir Singh Arya Affiliation Department of Pharmacology, All India Institute of Medical Sciences, New Delhi, India Key words Abstract BDNF: brain-derived neurotrophic factor l" naringin ! BMP: bone morphogenetic protein l" flavonoid Naringin, chemically 4′,5,7- trihydroxyflavanone- DMBA: 7,12-dimethylbenz[a]anthracene l" antioxidant 7-rhamnoglucoside, is a major flavanone glyco- DNFB: 2,4-dinitrofluorobenzene l" anti‑inflammatory side obtained from tomatoes, grapefruits, and DPP: dipeptidyl peptidase l" atherosclerosis l" diabetes mellitus many other citrus fruits. It has been experimen- DSS: dextran sodium sulphate l" neurological disorders tally documented to possess numerous biological EGF: epidermal growth factor l" cardiovascular disorders properties such as antioxidant, anti-inflamma- eNOS: endothelial nitric oxide synthase l" hepatoprotection tory, and antiapoptotic activities. In vitro and in ER: estrogen receptor l" nephroprotection vivo studies have further established the useful- ERK: extracellular signal-regulated kinase l" bone diseases ness of naringin in various preclinical models of FRAP: ferric reducing antioxidant power l" gastrointestinal diseases atherosclerosis, cardiovascular disorders, diabetes GSK: glycogen synthase kinase l" metabolic syndrome l" dentistry mellitus, neurodegenerative disorders, osteopo- hDuox2: human dual oxidase 2 l" cancer rosis, and rheumatological disorders. Apart from HMG‑CoA: hydroxymethylglutaryl-coenzyme A l" allergy this, naringin has also exerted chemopreventive HUVECs: human umbilical vascular endothelial l" drug interaction and anticancer attributes in various models of cells l" pharmacokinetics oral, breast, colon, liver, lung, and ovarian cancer. IC: inhibitory concentration This wide spectrum of biological expediency has ICAM-1: intercellular adhesion molecule 1 been documented to be a result of either the up- IFN: interferon regulation of various cell survival proteins or the IKK: IκB kinase inhibition of inflammatory processes, or a combi- IL: interleukin nation of both. Due to the scarcity of human stud- iNOS: inducible nitric oxide synthase ies on naringin, this review focuses on the various IRS-1: insulin receptor substrate-1 received August 12, 2013 established activities of naringin in in vitro and in JNK: c-Jun N-terminal kinase revised February 10, 2014 vivo preclinical models, and its potential thera- Kir: inward rectifying potassium channel accepted March 10, 2014 peutic applications using the available knowledge LPS: lipopolysaccharides This document was downloaded for personal use only. Unauthorized distribution is strictly prohibited. Bibliography in the literature. Additionally, it also encompasses MAPK: p38 mitogen-activated protein kinase DOI http://dx.doi.org/ the pharmacokinetic properties of naringin and MCP-1: monocyte chemotactic protein-1 10.1055/s-0034-1368351 its inhibition of CYP isoenzymes, and the subse- MDR: multidrug-resistance protein Published online Apil 7, 2014 quent drug interactions. Moreover, further clini- MIP-1α: macrophage inflammatory Planta Med 2014; 80: 437–451 cal research is evidently needed to provide signif- protein-1alpha © Georg Thieme Verlag KG Stuttgart · New York · icant insights into the mechanisms underlying MMP: matrix metalloproteinase ISSN 0032‑0943 the effects of naringin in humans. mTOR: mammalian target of rapamycin NF-κB: nuclear factor kappa-light-chain-en- Correspondence Dr. D. S. Arya, Professor hancer of activated B cells Department of Pharmacology Abbreviations NK: neurokinin All India Institute of Medical ! NNK: 4-(methylnitrosamino)-1-(3-pyridyl)- Sciences Ansari Nagar ABTS: 2,2-azinobis(3-ethylbenzothiazoline- 1-butanone New Delhi 110029 6-sulfonic acid) diammonium salt nNOS: neuronal nitric oxide synthase India Akt: protein kinase B Nrf2: nuclear factor-erythroid 2-related Phone: + 911126594266 Fax:+911126584121 AMPK: AMP-activated protein kinase factor-2 [email protected] AP: activator protein Bharti S et al. Preclinical Evidence for… Planta Med 2014; 80: 437–451 438 Reviews OATP: organic anion transporting polypeptide Sirt1: silent mating-type information regulation 2 PAF: platelet activating factor homolog-1 PARP: poly (ADP-ribose) polymerase sPLA2: secretory phospholipase A2 PGC1-α: peroxisome proliferator-activated receptor gamma STZ: streptozotocin coactivator SULT: sulfotransferases PGE2: prostaglandin E2 TBARS: thiobarbituric acid reactive substances PhIP: 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine TNF-α: tumor necrosis factor-alpha PPAR: peroxisome proliferator-activated receptors VCAM-1: vascular cell adhesion molecule-1 RANKL: receptor activator of nuclear factor kappa-B ligand VEGF: vascular endothelial growth factor RANTES: regulated on activation, normal T cell expressed and secreted Introduction common dietary constituent would invariably be present in a lot ! of the dietary products consumed by humans. Thus, a human Naringin was first discovered by De Vry in the flowers of grape- being would be exposed to naringin intake in some form or an- fruit trees growing in Java in 1857, but he did not publish his other. Literature is replete with various researches and reviews findings at that time [1]. Extensive research on this “novel com- that focus on the numerous potential therapeutic effects of narin- pound” was conducted in the years to come by De Vry and Hoff- gin. In fact, a wide spectrum of beneficial effects has been attrib- man, and, subsequently, Will [2]. The name naringin is probably uted to naringin including cardiovascular, hypolipidemic, antia- derived from the Sanskrit term “narangiʼ meaning “orange” [2]. It therosclerotic, antidiabetic, neuroprotective, hepatoprotective, is present in citrus and grape fruits, beans, cherries, cocoa, orega- and anticancer activities [14,15]. These articles highlight the fact no, and tomatoes [3–8]. It is present in grapefruit juice up to con- that naringin possesses the potential to be employed as a thera- centrations of 800 mg/L [9]. The chemical structure of naringin peutic agent in a large number and variety of human ailments. At was first elucidated in 1928 by Asahina and Inubuse [10] and is the same time, the occurrence of adverse reactions with allo- depicted in l" Fig. 1. Naringin is a flavanone glycoside composed pathic medications might encourage physicians to explore safer of naringenin, an aglycone and neohesperidose attached to the alternatives in complementary medicine, thus prompting the de- hydroxyl group at C-7 and tastes bitter due to its glucose moiety velopment of naringin and related flavonoids for therapeutic [11]. Nevertheless, it can be converted to 1,3-diphenylpropan-1- purposes. one, a compound 300–1800 times sweeter than sugar with a Moreover, the knowledge of pharmacokinetic properties and po- menthol-like refreshing sweet taste when treated with potassi- tential interactions of naringin with other drugs would assume um hydroxide or another strong base [12]. Depending up on the paramount importance, as it would provide guidance for the maturity of the fruit and the method of purification, naringin nat- measures that should be taken and precautions to be followed urally occurs as a mixture of chiral isomers that markedly vary in during consumption of naringin, which would also simulta- proportion [13]. neously apply to patients taking other medications and concom- Naringin typically exemplifies the term “phytopharmaceutical”, itantly consuming dietary constituents rich in naringin. Unfortu- which commonly refers to products obtained from plants that nately, information on these parameters of naringin are limited are found to be useful in human disorders. Naringin being a very and scattered in the literature. Hence, this review aims at sum- Fig. 1 Naringin and its metabolism in humans. This document was downloaded for personal use only. Unauthorized distribution is strictly prohibited. Bharti S et al. Preclinical Evidence for… Planta Med 2014; 80: 437–451 Reviews 439 marizing the experimental work performed to date on biological Distribution actions, mechanisms of action, pharmacokinetic data, and clini- Zou and colleagues have demonstrated that naringin and its me- cally relevant drug interactions of naringin. To the best of our tabolites, being highly lipophilic, are distributed to almost all the knowledge, this attempt is the first of its kind. body organs with the highest concentrations being observed in the stomach and the lowest in the brain due to reduced blood brain barrier permeability. Naringin is concentrated in the liver Search Methodology and bile by the processes of active transport [32,33]. ! Database searches using Google Scholar, Pubmed, and Science Di- Metabolism rect were conducted until 15th December 2013 to include up-to- Naringin undergoes extensive phase I and phase II metabolism in date documented information in the present review article. The the liver, as depicted in l" Fig. 1. Liu and colleagues have identi- search was limited to English language papers. For data mining, fied a total of 23 metabolites of naringin after oral administration the following MESH words were used in the databases men- to rats (42 mg/kg) and dogs (12.4 mg/kg). They identified 4-hy- tioned above: naringin allergies, naringin Alzheimerʼs, naringin droxyphenylpropionic acid (37% in dogs and 16% in rats) as a ma- anti-inflammatory, naringin antioxidant, naringin
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