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Manjit Kaur, Raj K S Badhan
Clinical translation of BCRP inhibitors have failed due to neurotoxicity and novel approaches are required to identify suitable modulators of BCRP to enhance CNS drug delivery. In this study we examine 18 compounds, primarily phytochemicals, as potential novel modulators of AhR-mediated regulation of BCRP expression and function in immortalised and primary porcine brain microvascular endothelial cells as a mechanism to enhance CNS drug delivery. The majority of modulators possessed a cellular viability IC50 > 100µM in both cell systems...
October 19, 2016: Brain Research
Xiaoyu Zhuang, Bing Zhao, Shu Liu, Fengrui Song, Fengchao Cui, Zhiqiang Liu, Yunqi Li
Misfolding and aggregation of Cu, Zn superoxide dismutase (SOD1) is implicated in the etiology amyotrophic lateral sclerosis (ALS). The use of small molecules may stabilize the spatial structure of SOD1 dimer, thus preventing its dissociation and aggregation. In this study, "native" mass spectrometry (MS) was used to study the non-covalent interactions between SOD1 and flavonoid compounds. MS experiments were performed on a quadruple time-of-flight (Q-ToF) mass spectrometer with an electrospray ionization (ESI) source and T-wave ion mobility...
October 19, 2016: Analytical Chemistry
Xuan Zeng, Yang Bai, Wei Peng, Weiwei Su
BACKGROUND AND OBJECTIVES: Naringin, an active flavanone glycoside, has been widely considered as a prospective antitussive and expectorant. The present study aimed to elucidate the metabolic profile of naringin in the human body. METHODS: Four male and three female volunteers (20-30 years old and 18.8-21.7 kg/m(2) Body Mass Index) were orally administrated 320 mg naringin; their urine and feces were collected at different times and the corresponding metabolites were identified with a high resolution ultra-fast liquid chromatography-quadrupole-time-of-flight tandem mass spectrometry (UFLC-Q-TOF-MS/MS) system...
October 15, 2016: European Journal of Drug Metabolism and Pharmacokinetics
Po-Chun Chang, Yi-Chi Chao, Meng-Hsuan Hsiao, Hao-Syun Chou, Yi-Han Jheng, Xin-Hong Yu, Ning Lee, Connie Yang, Dean-Mo Liu
BACKGROUND: Developing a drug carrier with favorable handling characteristics that can respond to environmental changes following inflammation, such as pH changes, may be beneficial for treating periodontitis. This study aimed to investigate the preclinical feasibility of using naringin, a naturally derived polymethoxylated flavonoid compound with anti-inflammatory properties, to inhibit periodontitis induction via a thermo-gelling and pH-responsive injectable hydrogel. METHODS: The hydrogel was made of amphipathic carboxymethyl-hexanoyl chitosan (CHC), beta glycerol-phosphate (β-GP), and glycerol, and the thermo-gelling and pH-responsive characteristics of the hydrogel as well as the cell viability after treatment with the hydrogel containing naringin were evaluated in vitro...
October 14, 2016: Journal of Periodontology
Juanjuan Wang, Qingshui Shi, Chunyong Wu, Fang Feng
Zhi-Zi-Da-Huang decoction (ZZDHD) has been used for treatment of alcoholic liver disease in China for thousands of years. In order to reveal the dynamic biotransformation of the decoction in vivo, a high-throughout, sensitive and special method based on high performance liquid chromatography coupled with diode array detection and time-of-flight mass spectrometry (HPLC-DAD-TOF/MS) and high performance liquid chromatography coupled with triple quadrupole mass spectrometry (HPLC-QqQ/MS) was developed and validated...
October 4, 2016: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
Minchan Gil, Yun Kyu Kim, Sang Bum Hong, Kyung Jin Lee
Naringin, a flavanone glycoside extracted from various plants, has a wide range of pharmacological effects. In the present study, we investigated naringin's mechanism of action and its inhibitory effect on lipopolysaccharide-induced tumor necrosis factor-alpha and high-mobility group box 1 expression in macrophages, and on death in a cecal ligation and puncture induced mouse model of sepsis. Naringin increased heme oxygenase 1 expression in peritoneal macrophage cells through the activation of adenosine monophosphate-activated protein kinase, p38, and NF-E2-related factor 2...
2016: PloS One
Liu Xianchu, Professor Zheng Lan, Li Qiufang, Liu Yi, Ruan Xiangcheng, Hou Wenqi, Ding Yang
Previous research has demonstrated that lipopolysaccharide (LPS) can induce sepsis and lead to myocardial dysfunction. Naringin has various biological activities in LPS-induced sepsis. In this study, our aim was to investigate the effects of Naringin on LPS-induced cardiac injury and clarify its potential mechanism. We found that in vivo treatment with Naringin significantly ameliorated body weight loss, and attenuated cardiac histopathological changes after LPS challenge. Furthermore, Naringin inhibited LPS-induced increase of TNF-α, IL-1β and IL-6 activities to alleviate inflammatory response in heart...
September 13, 2016: Environmental Toxicology and Pharmacology
Hongbo Shi, Honglin Shi, Feng Ren, Dexi Chen, Yu Chen, Zhongping Duan
A previous study has demonstrated that Ganshuang granule (GSG) plays an anti-fibrotic role partially by deactivation of hepatic stellate cells (HSCs). In HSCs activation, mammalian target of rapamycin (mTOR)-autophagy plays an important role. We attempted to investigate the role of mTOR-autophagy in anti-fibrotic effect of GSG. The cirrhotic mouse model was prepared to demonstrate the anti-fibrosis effect of GSG. High performance liquid chromatography (HPLC) analyses were used to identify the active component of GSG...
September 30, 2016: Journal of Cellular and Molecular Medicine
André Lucio Franceschini Sarria, Adriana Ferreira Lopes Vilela, Bárbara Mammana Frugeri, João Batista Fernandes, Rose Maria Carlos, Maria Fátima das Graças Fernandes da Silva, Quezia Bezerra Cass, Carmen Lúcia Cardoso
Metal chelates strongly influence the nature and magnitude of pharmacological activities in flavonoids. In recent years, studies have shown that a promising class of flavanone-metal ion complexes can act as selective cholinesterase inhibitors (ChEIs), which has led our group to synthesize a new series of flavanone derivatives (hesperidin, hesperetin, naringin, and naringenin) complexed to either copper (II) or zinc (II) and to evaluate their potential use as selective ChEIs. Most of the synthesized complexes exhibited greater inhibitory activity against acetylcholinesterase (AChE) than against butyrylcholinesterase (BChE)...
September 17, 2016: Journal of Inorganic Biochemistry
Min Young Kim, Sang Hoon Lee, Gwi Yeong Jang, Meishan Li, Youn Ri Lee, Junsoo Lee, Heon Sang Jeong
This study was performed to investigate changes in the phenolic acid and vitamin E profiles of germinated rough rice following high hydrostatic pressure treatment (HPT). Rough rice was germinated at 37°C for two days and subjected to 0.1, 10, 30, 50, and 100MPa pressures for 24h. The total phenolic acid content increased from 85.37μg/g at 0.1MPa to 183.52μg/g at 100MPa. The highest gallic acid (4.29μg/g), catechin (9.55μg/g), p-coumaric acid (8.36μg/g), ferulic acid (14.99μg/g), salicylic acid (14.88μg/g), naringin (6...
February 15, 2017: Food Chemistry
Cristina Zaragozá Arnaéz, Jorge Monserrat Sanz, Carolina Mantecón Ramiro, Lucinda Villaescusa Castillo, Francisco Zaragozá García, Melchor Álvarez de Mon Soto
Polyphenols are used as phlebotonic drugs, but their mechanism of action remains unknown. Since platelet activity and platelet-endothelial cell interactions are involved in the pathogenesis of cardiovascular disease, this work examines whether different flavonoid and coumarin drugs are able to inhibit platelet aggregation. This specific case of coumarins, the antiplatelet effect is not linked with a possible interaction over blood coagulation since this effect only dicoumarols have it. The antiplatelet capacity of polyphenols was assayed using peripheral blood platelets from healthy controls...
September 8, 2016: Vascular Pharmacology
José-Luis Giner, Ju Feng, David J Kiemle
The sugar subunits of natural glycosides can be conveniently determined by acid hydrolysis and (1)H NMR spectroscopy without isolation or derivatization. The chemical shifts, coupling constants, and integral ratios of the anomeric signals allow each monosaccharide to be identified and its molar ratio to other monosaccharides to be quantified. The NMR data for the anomeric signals of 28 monosaccharides and three disaccharides are reported. Application of the method is demonstrated with the flavonoid glycoside naringin (1), the aminoglycoside antibiotics kanamycin (2) and tobramycin (3), and the saponin digitonin (4)...
September 23, 2016: Journal of Natural Products
Jungha Park, Kyoung Hoon Jeong, Won-Ho Shin, Young-Seuk Bae, Un Ju Jung, Sang Ryong Kim
Granule cell dispersion (GCD) in the dentate gyrus (DG) of the hippocampus is a morphological alteration characteristic of temporal lobe epilepsy. Recently, we reported that treatment with naringin, a flavonoid found in grapefruit and citrus fruits, reduced spontaneous recurrent seizures by inhibiting kainic acid (KA)-induced GCD and neuronal cell death in mouse hippocampus, suggesting that naringin might have beneficial effects for preventing epileptic events in the adult brain. However, it is still unclear whether the beneficial effects of naringin treatment are mediated by the metabolism of naringin into naringenin in the KA-treated hippocampus...
October 19, 2016: Neuroreport
Yuri Oh, Hye-Won Lim, Yu-Hua Huang, Hee-Souk Kwon, Chang Duck Jin, Kyunghoon Kim, Chang-Jin Lim
Agastache rugosa Kuntze, known as a Korean mint, is an herbal medicine that has been used for the treatment of diverse kinds of symptoms in traditional medicine. This work was undertaken to assess the protective properties of A. rugosa leaves against UV-B-induced photoaging in HaCaT keratinocytes. They were evaluated via analyzing reactive oxygen species (ROS), promatrix metalloproteinase-2 (proMMP-2) and -9 (proMMP-9), total glutathione (GSH), total superoxide dismutase (SOD), cellular viability, flavonoid content and in vitro radical scavenging activity...
October 2016: Journal of Photochemistry and Photobiology. B, Biology
Rui Chen, Qiao-Ling Qi, Meng-Ting Wang, Qi-Yan Li
CONTEXT: Naringin is a natural flavanone glycoside that is found in the Chinese herbal medicines and citrus fruits. Studies have demonstrated that naringin possesses numerous biological and pharmacological properties, but few reviews of these studies have been performed. OBJECTIVE: The present review gathers the fragmented information available in the literature describing the extraction of naringin, its pharmacology and its controlled release formulations. Current research progress and the therapeutic potential of naringin are also discussed...
August 26, 2016: Pharmaceutical Biology
Sajjad Molavi Pordanjani, Seyed Jalal Hosseinimehr
It is well documented that ionizing radiation (IR) activates the transcription factor (NF-κB) which is a trigger for resistance cancer cells to treatment. It is involved in activation of pro-survival signaling pathways and resulting in cancer development and progression. In unstimulated condition, NF-κB is sequestered in cytoplasm but after the cell exposure to IR, proteasomal degradation of IκB flowing phosphorylation via IKK, leads to aberrantly NF-κB activation and nuclear translocation. Therefore, interruption in IκB degradation, proteasome action, IKK phosphorylation and NF-κB nuclear translocation provide robust strategies for inhibiting adverse effect of IR induced NF-κB...
August 24, 2016: Current Medicinal Chemistry
Ratana Banjerdpongchai, Benjawan Wudtiwai, Patompong Khawon
Naringin, a bioflavonoid found in Citrus seeds, inhibits proliferation of cancer cells. The objectives of this study were to investigate the mode and mechanism(s) of hepatocellular carcinoma HepG2 cell death induced by naringin. The cytotoxicity of naringin towards HepG2 cells proved dosedependent, measured by MTT assay. Naringintreated HepG2 cells underwent apoptosis also in a concentration related manner, determined by annexin Vfluorescein isothiocyanate (FITC) and propidium iodide (PI) employing flow cytometry...
2016: Asian Pacific Journal of Cancer Prevention: APJCP
Yunping Zhu, Huiyong Jia, Menglu Xi, Liya Xu, Shaoming Wu, Xiuting Li
An intracellular naringinase from Bacillus amyloliquefaciens 11568 isolated from soil was purified, identified, and characterized. The sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE) analysis of the purified enzyme gave a single protein band corresponding to a molecular mass of 32kDa. The optimum pH and temperature for naringinase and its α-l-rhamnosidase and β-d-glucosidase activities were pH 7.5 and 45°C, respectively. The enzymes were stable below 45°C between pH 3.5 and 8.5. The Km and the Vmax of the isolated naringinase were 0...
January 1, 2017: Food Chemistry
Andrea Hubeny, Markus Keiser, Stefan Oswald, Gabriele Jedlitschky, Heyo K Kroemer, Werner Siegmund, Markus Grube
Important antimalarial drugs, including quinolines, act against blood schizonts by interfering with hemoglobin metabolism. To reach their site of action, these compounds have to cross the plasma membrane of red blood cells (RBCs). Organic cation transporters (OCTs) and organic anion transporting polypeptides (OATPs) are important uptake transporters and interesting candidates for local drug transport. We therefore studied their interaction with antimalarial compounds (quinine, chloroquine, mefloquine, pyrimethamine, artemisinin, and artesunate) and characterized the expression of OATP1A2 and OATP2B1 in RBCs...
October 2016: Drug Metabolism and Disposition: the Biological Fate of Chemicals
Sanelisiwe Nzuza, Duduzile E Ndwandwe, Peter M O Owira
INTRODUCTION: The protective effects of grapefruit-derived naringin against HIV-1 Protease Inhibitors (PIs)-associated oxidative damage to pancreatic β-cells and apoptosis were investigated in RIN-5F cells in culture. METHODS: Cells in culture medium were challenged with 11-25 mM glucose with or without nelfinavir (1-10 μM), saquinavir (1-10 μM) and atazanavir (5-20 μM), respectively for 24 h to determine insulin secretion. The cells were further treated with nelfinavir (10 μM), saquinavir (10 μM), atazanavir (20 μM) with and without naringin or glibenclamide (10 μM) for 24 h to determine insulin secretion, lipid peroxidation, Superoxide Dismutase (SOD) activity, glutathione (GSH) levels, ATP production and caspase-3 and-9 activities, respectively...
December 5, 2016: Molecular and Cellular Endocrinology
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