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Emily J Johnson, Christina S Won, Kathleen Köeck, Mary F Paine
Natural products, including botanical dietary supplements and exotic drinks, represent an ever-increasing share of the health care market. The parallel ever-increasing popularity of self-medicating with natural products increases the likelihood of co-consumption with conventional drugs, raising concerns for unwanted natural product-drug interactions. Assessing the drug interaction liability of natural products is challenging due to the complex and variable chemical composition inherent to these products, necessitating a streamlined preclinical testing approach to prioritize precipitant individual constituents for further investigation...
December 29, 2016: Biopharmaceutics & Drug Disposition
Jiawei Wan, Dong Li, Rong Song, Bakht Ramin Shah, Bin Li, Yan Li
Soy protein isolate (SPI) was selected to fabricate supersaturated self-emulsifying nanoemulsions, aiming to enhance physical stability and bioaccessibility of hydrophobic tangeretin. Dissolution studies demonstrated that tangeretin had the highest solubility in Tween 80, followed by oil phase solutions, and polymer solutions. Supersaturated tangeretin in oil phases easily formed crystals. That metastable zone was found to vary with its initial concentrations. After encapsulation by nanoemulsions, the addition of glycerol compressed the retention amount of tangeretin from 76% to 53%, but benefited the transparency...
April 15, 2017: Food Chemistry
Su-Hyeon Eun, Je-Te Woo, Dong-Hyun Kim
In the preliminary study, tangeretin (5,6,7,8,4'-pentamethoxy flavone), a major constituent of the pericarp of Citrus sp., inhibited TNF-α, IL-12, and IL-23 expression and nuclear factor kappa-B activation in lipopolysaccharide-stimulated dendritic cells; however, it did not affect IL-10 expression. Furthermore, tangeretin (5, 10, and 20 µM) suppressed the activation and translocation of nuclear factor kappa-B (p65) into the nuclei in vitro by inhibiting the binding of lipopolysaccharide on dendritic cells...
November 2, 2016: Planta Medica
Hany H Arab, Wafaa R Mohamed, Bassant M Barakat, El-Shaimaa A Arafa
BACKGROUND: Despite the efficacy of cisplatin as a chemotherapeutic agent against various cancers, its clinical utility is limited by serious adverse reactions including nephrotoxicity. AIM: The current study aims to investigate the protective potential of tangeretin, a citrus flavone with marked antioxidant actions, against cisplatin-induced renal injury in rats. METHODS: Tangeretin was administered at 50 and 100 mg/kg p.o. for 1 week starting one day before cisplatin (7...
October 25, 2016: Chemico-biological Interactions
Sen-Ling Feng, Zhong-Wen Yuan, Xiao-Jun Yao, Wen-Zhe Ma, Liang Liu, Zhong-Qiu Liu, Ying Xie
No abstract text is available yet for this article.
July 25, 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
Yuki Kuroda, Riko Ikeda, Toyomi Yamazaki, Keisuke Ito, Kazunari Uda, Keiji Wakabayashi, Tatsuo Watanabe
Tangeretin and nobiletin are polymethoxylated flavonoids in citrus peel. Both tangeretin and nobiletin are bitter; however, their bitterness has not been evaluated using human bitter taste receptors (hTAS2Rs). We screened 25 kinds of hTAS2Rs and found that hTAS2R14 and hTAS2R46 received both compounds.
October 2016: Bioscience, Biotechnology, and Biochemistry
Lian-Hua Zhao, Hong-Zheng Zhao, Xue Zhao, Wei-Jun Kong, Yi-Chen Hu, Shi-Hai Yang, Mei-Hua Yang
INTRODUCTION: Citri Reticulatae Pericarpium (CRP) is a commonly-used traditional Chinese medicine with flavonoids as the major bioactive components. Nevertheless, the contents of the flavonoids in CRP of different sources may significantly vary affecting their therapeutic effects. Thus, the setting up of a reliable and comprehensive quality assessment method for flavonoids in CRP is necessary. OBJECTIVE: To set up a rapid and sensitive ultra-fast liquid chromatography coupled with tandem mass spectrometry (UFLC-MS/MS) method for simultaneous quantification of seven bioactive flavonoids in CRP...
May 2016: Phytochemical Analysis: PCA
Clizia Guccione, Maria Camilla Bergonzi, Vieri Piazzini, Anna Rita Bilia
A chromatographic method for the qualitative and quantitative characterization of peels and preparations based on different species of Citrus was developed in order to obtain a complete profile of the constituents, including flavonoids and protoalkaloids. Commercial peels of sweet orange, lemon, mandarin, and grapefruit were analyzed. Seventeen constituents including flavanones, flavones, polymethoxyflavones, and protoalkaloids were identified by HPLC-PDA, HPLC-MS, and HPLC-MS/MS using a comparison of retention times and UV-Vis and MS spectra with reference standards and literature data...
July 2016: Planta Medica
Li-Li Ma, Da-Wei Wang, Xu-Dong Yu, Yan-Ling Zhou
Tangeretin (TANG), present in peel of citrus fruits, has been shown to various medicinal properties such as chemopreventive and neuroprotective. However, the chemopreventive effect of TANG on glioblastoma cells has not been examined. The present study was designed to explore the anticancer potential of TANG in glioblastoma cells and to investigate the related mechanism. Human glioblastoma U-87MG and LN-18 cells were treated with 45μM concentration of TANG and cell growth was measured by MTT assay. The cell cycle distribution and cell death were measured by flow cytometry...
July 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Erin E Mulvihill, Amy C Burke, Murray W Huff
Citrus flavonoids are polyphenolic compounds with significant biological properties. This review summarizes recent advances in understanding the ability of citrus flavonoids to modulate lipid metabolism, other metabolic parameters related to the metabolic syndrome, and atherosclerosis. Citrus flavonoids, including naringenin, hesperitin, nobiletin, and tangeretin, have emerged as potential therapeutics for the treatment of metabolic dysregulation. Epidemiological studies reveal an association between the intake of citrus flavonoid-containing foods and a decreased incidence of cardiovascular disease...
July 17, 2016: Annual Review of Nutrition
Antonietta Funaro, Xian Wu, Mingyue Song, Jinkai Zheng, Shanshan Guo, Kanyasiri Rakariyatham, Maria Teresa Rodriguez-Estrada, Hang Xiao
Dietary components in combination may act synergistically and produce enhanced biological activities. Herein, we investigated the anti-inflammatory effects of 2 flavonoids, that is luteolin (LUT) and tangeretin (TAN) in combination. Lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages were treated with noncytotoxic concentrations of LUT, TAN, and their combinations. The results showed that LUT/TAN in combination produced synergistic inhibitory effects on LPS-stimulated production of nitric oxide (NO). ELISA results demonstrated that LUT/TAN in combination caused stronger suppression on the LPS-induced overexpression of proinflammatory mediators, such as prostaglandin E2 (PGE2 ), interleukin (IL)-1β, and IL-6 than LUT or TAN alone...
May 2016: Journal of Food Science
Marina Russo, Francesca Rigano, Adriana Arigò, Danilo Sciarrone, Maria Luisa Calabrò, Sara Farnetti, Paola Dugo, Luigi Mondello
Polymethoxyflavones possess many biological properties, as lipid-lowering, hypoglycaemic, anti-inflammatory, antioxidant, and anticancer activities, therefore, they may be employed as nutraceuticals or therapeutic agents. The scarcity of pure polymethoxyflavones on the market as well as their low water solubility limited in vivo studies and the use of polymethoxyflavones as food or pharmaceutical supplements. Since mandarin peels are a rich source of polymethoxyflavones, tangeretin, nobiletin, sinensetin, tetra-O-methyl scutellarein, and heptamethoxyflavone were purified from a nonvolatile residue of a cold-pressed mandarin essential oil using a multidimensional preparative liquid chromatographic system coupled with a photodiode array detector and a single quadrupole mass spectrometer...
June 2016: Journal of Separation Science
Sen-Ling Feng, Zhong-Wen Yuan, Xiao-Jun Yao, Wen-Zhe Ma, Liang Liu, Zhong-Qiu Liu, Ying Xie
Multidrug resistance (MDR) and tumor metastasis are the main causes of chemotherapeutic treatment failure and mortality in cancer patients. In this study, at achievable nontoxic plasma concentrations, citrus flavonoid tangeretin has been shown to reverse ABCB1-mediated cancer resistance to a variety of chemotherapeutic agents effectively. Co-treatment of cells with tangeretin and paclitaxel activated apoptosis as well as arrested cell cycle at G2/M-phase. Tangeretin profoundly inhibited the ABCB1 transporter activity since it significantly increased the intracellular accumulation of doxorubicin, and flutax-2 in A2780/T cells and decreased the efflux of ABCB1 substrates in Caco2 cells without altering the expression of ABCB1...
August 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
Hany A Omar, Wafaa R Mohamed, Hany H Arab, El-Shaimaa A Arafa
Despite its broad applications, cisplatin affords considerable nephro- and hepatotoxicity through triggering inflammatory and oxidative stress cascades. The aim of the current investigation was to study the possible protective effects of tangeretin on cisplatin-induced hepatotoxicity. The impact of tangeretin on cisplatin-evoked hepatic dysfunction and histopathologic changes along with oxidative stress, inflammatory and apoptotic biomarkers were investigated compared to silymarin. Tangeretin pre-treatment significantly improved liver function tests (ALT and AST), inhibited cisplatin-induced lipid profile aberrations (total cholesterol and triglycerides) and diminished histopathologic structural damage in liver tissues...
2016: PloS One
Yvonne Hagenlocher, Katharina Feilhauer, Michael Schäffer, Stephan C Bischoff, Axel Lorentz
PURPOSE: Allergic diseases with mast cells (MC) as main effector cells show an increased prevalence. MC also play an essential role in other inflammatory conditions. Therapeutical use of anti-inflammatory nutraceuticals directly targeting MC activation could be of interest for afflicted patients. Nobiletin and tangeretin are citrus peel polymethoxyflavones, a group of citrus flavonoids, possessing anticancer, antimetastatic, and anti-inflammatory activities. Here, we analyzed the effects of nobiletin/tangeretin on LPS- and IgE-mediated stimulation of human intestinal mast cells (hiMC)...
March 28, 2016: European Journal of Nutrition
A Max Batenburg, Teun de Joode, Robin J Gouka
An obstacle in the application of many "health ingredients" is their alleged off-flavor. We used a combination of chemical, sensory, and biological analyses to identify the bitter components in citrus peel-derived polymethoxyflavone preparations, claimed to be functional in the lowering of cholesterol. Nobiletin (56-81%) and tangeretin (10-33%) were found to be the main bitter components. Using in vitro receptor assays, hTAS2R14 was shown to be the main bitter receptor involved in their perception, with EC50 values of 14 and 63 μM, respectively...
March 30, 2016: Journal of Agricultural and Food Chemistry
Yalan Jiang, Fang Huang, Fuhai Wu, Huiqin Wu, Xiaolan Huang, Xin Deng
A method for the determination of 16 functional components of ginkgo dietary supplement tea such as catechin, vitexin, puerarin, isoflavoues aglycone, silymarin, quercetin, luteolin, apigenin, naringenin, hesperitin dihydrochalcone, kaempferol, hesperitin, isorhamnetin, baicalein, nobiletin and tangeretin by high performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) was proposed. The conditions of chromatography and mass spectrometry were optimized. The 16 flavonoids were separated on a C18 chromatographic column with acetonitrile and water (additional 0...
October 2015: Se Pu, Chinese Journal of Chromatography
Yu Young Lee, Eun-Jung Lee, Jin-Sun Park, Se-Eun Jang, Dong-Hyun Kim, Hee-Sun Kim
Tangeretin, a flavonoid from citrus fruit peels, has been proven to play an important role in anti-inflammatory responses and neuroprotective effects in several disease models, but further study is necessary for elucidating the detailed mechanisms of these effects. In this study, we examined the anti-inflammatory effect of tangeretin in lipopolysaccharide (LPS)-stimulated microglia. We first observed that tangeretin inhibited LPS-induced production of nitric oxide, tumor necrosis factor alpha, interleukin (IL)-6, and IL-1β, as well as LPS-induced mRNA expression of inducible nitric oxide synthases and cytokines...
June 2016: Journal of Neuroimmune Pharmacology: the Official Journal of the Society on NeuroImmune Pharmacology
Yi Rong Li, Shiming Li, Chi-Tang Ho, Ya-Han Chang, Kok-Tong Tan, Ting-Wen Chung, Bing-Yen Wang, Yu-Kuo Chen, Chi-Chen Lin
Tangeretin, a major phytochemicals in tangerine peels--an important Chinese herb, has been found to have anti-carcinogenic properties. To improve bioavailability and increase potency of tangeretin, its derivative, 5-acetyloxy-6,7,8,4'-tetramethoxyflavone (5-AcTMF), has been synthesized and shown potent inhibition of proliferation activity against human breast and leukemia cancer cell lines. In this study, we have further investigated the anticancer effects of 5-AcTMF on CL1-5 non-small cell lung cancer cells (NSCLC) both in vitro and in vivo and demonstrated that 5-AcTMF effectively inhibited cancer cell proliferation, induced G2/M-phase arrest associated with cdc2 and CDC25c and increased in the apoptotic cells associated with caspase activation, down regulation of Bcl-2, XIAP and Survivn, inducing release of cytochrome c into the cytosol and disruption of mitochondrial membrane potential...
2016: Cancer Biology & Therapy
Jiao-Jiao Xu, Zhong Liu, Wei Tang, Guo-Cai Wang, Hau Yin Chung, Qiu-Ying Liu, Ling Zhuang, Man-Mei Li, Yao-Lan Li
Human respiratory syncytial virus (RSV) is a common pathogen that causes pneumonia and bronchiolitis in infants and young children. Our previous study showed that tangeretin from Citrus reticulate possessed potent in vitro anti-RSV effects comparable to that of ribavirin. Therefore, in this study, we investigated the in vivo anti-RSV activity of tangeretin in 3-week-old male BALB/c mice. A plaque reduction assay and fluorescence quantitative polymerase chain reaction (FQ-PCR) showed that tangeretin inhibited RSV replication in the lung of mice...
November 4, 2015: Journal of Agricultural and Food Chemistry
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