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https://www.readbyqxmd.com/read/28322965/inhibitory-effect-of-hesperetin-on-%C3%AE-glucosidase-molecular-dynamics-simulation-integrating-inhibition-kinetics
#1
Yan Gong, Xiu-Yuan Qin, Yuan-Yuan Zhai, Hao Hao, Jinhyuk Lee, Yong-Doo Park
The α-glucosidase inhibitor is of interest to researchers due to its association with type-2 diabetes treatment. Hesperetin is a flavonoid with natural antioxidant properties. This paper presents an evaluation on the effects of hesperetin on α-glucosidase via inhibitory kinetics using a Molecular Dynamics (MD) simulation integration method. Due to the antioxidant properties of hesperetin, it reversibly inhibits α-glucosidase in a slope-parabolic mixed-type manner (IC50=0.38±0.05mM; Kslope=0.23±0.01mM), accompanied by tertiary structural changes...
March 17, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28320087/the-renoprotective-activity-of-hesperetin-in-cisplatin-induced-nephrotoxicity-in-rats-molecular-and-biochemical-evidence
#2
Mukesh Kumar, Vicky Dahiya, Eshvendar Reddy Kasala, Lakshmi Narendra Bodduluru, Mangala Lahkar
Nephrotoxicity remain a major life-threatening complication in cancer patients on cisplatin chemotherapy. In this study, we investigated the protective effect and possible cellular mechanism of the hesperetin, a naturally-occurring bioflavonoid against cisplatin-induced renal injury in rats. Hesperetin was administered at a dose of 50mg/kg and 100mg/kg orally for 10days and cisplatin (7.5mg/kg, ip) was administered on the 5th day of experiment. Cisplatin induced nephrotoxicity was evidenced by alteration in the level of markers such as blood urea nitrogen, creatinine, serum albumin and severe histopathological changes in kidney...
March 14, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28284083/plasma-pharmacokinetics-and-bioavailability-of-verticillin-a-following-different-routes-of-administration-in-mice-using-liquid-chromatography-tandem-mass-spectrometry
#3
Jiang Wang, Xiaohua Zhu, Shamala Kolli, Hongyan Wang, Cedric J Pearce, Nicholas H Oberlies, Mitch A Phelps
Verticillin A is a natural product isolated from fungal cultures and has displayed potent antibiotic, antiviral, nematocidal, and anticancer properties in vitro. While in vivo studies have been limited due to sparse supply, the in vivo efficacy data that does exist demonstrates potent anti-tumor activity in murine cancer models. The current study aims to investigate the pharmacokinetics and bioavailability of verticillin A in mice to provide guidance for further efficacy assessment in mouse models. A sensitive and specific liquid chromatography-tandem mass spectrometry method was developed and validated for the quantification of verticillin A in mouse plasma...
March 1, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28262328/citrus-flavanones-mildly-interfere-with-pituitary-thyroid-axis-in-old-aged-male-rats
#4
Marko Miler, Ivana Jarić, Jasmina Živanović, Vladimir Ajdžanović, Nasta Tanić, Verica Milošević, Branka Šošić-Jurjević
Citrus flavanones naringenin (NAR) and hesperetin (HES) are potent antioxidants that may contribute to maintenance of health at old age by improving cardiovascular and metabolic status. However, they may also affect thyroid hormone economy. Keeping in mind impaired thyroid function at older age, in this study we tested wheather NAR or HES administration potentiate this decline. NAR or HES were administrated orally (15mg/kg) to male 24-month-old Wistar rats during 4 weeks. Control groups received vehicle, sunflower oil...
March 2, 2017: Acta Histochemica
https://www.readbyqxmd.com/read/28218440/physiologically-based-kinetic-modeling-of-hesperidin-metabolism-and-its-use-to-predict-in-vivo-effective-doses-in-humans
#5
Rungnapa Boonpawa, Albertus Spenkelink, Ans Punt, Ivonne M C M Rietjens
SCOPE: To develop a physiologically based kinetic (PBK) model that describes the absorption, distribution, metabolism, and excretion (ADME) of hesperidin in humans, enabling the translation of in vitro concentration-response curves to in vivo dose-response curves. METHODS AND RESULTS: The PBK model for hesperidin in humans was developed based on in vitro metabolic parameters. Hesperidin was predicted to mainly occur in the systemic circulation as different monoglucuronides...
February 20, 2017: Molecular Nutrition & Food Research
https://www.readbyqxmd.com/read/28202192/ordered-mesoporous-silica-functionalized-with-%C3%AE-cyclodextrin-derivative-for-stereoisomer-separation-of-flavanones-and-flavanone-glycosides-by-nano-liquid-chromatography-and-capillary-electrochromatography
#6
Mariana Silva, Damián Pérez-Quintanilla, Sonia Morante-Zarcero, Isabel Sierra, María Luisa Marina, Zeineb Aturki, Salvatore Fanali
In this paper a chiral stationary phase (CSP) was prepared by the immobilization of a β-CD derivative (3,5-dimethylphenylcarbamoylated β-CD) onto the surface of amino-functionalized spherical ordered mesoporous silica (denoted as SM) via a urea linkage using the Staudinger reaction. The CSP was packed into fused silica capillaries 100μm I.D. and evaluated by means of nano-liquid chromatography (nano-LC) and capillary electrochromatography (CEC) using model compounds for the enantio- and the diastereomeric separation...
February 9, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/28192136/inhibition-of-glycation-and-aldose-reductase-activity-using-dietary-flavonoids-a-lens-organ-culture-studies
#7
Kapil K Patil, Rajesh N Gacche
On the eve of increasing incidence of diabetes mellitus and related complications, the search for novel, safe and alternatives therapeutic approaches are evolving. In the present investigation, a panel of ten dietary flavonoids such as 4'-methoxyflavanone, formononetin, hesperetin, hesperidin, naringenin, naringin, rutin, diadzin, silibinin and silymarin was evaluated as possible inhibitors of sugar induced cataractogenesis using bovine lens organ culture studies. The effect of selected flavonoids was observed on glycation induced lens opacity, AGE fluorescence, carbonyl group formation (a biomarker of glycation), protein aggregation and aldose reductase (AR) inhibition...
February 10, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28111103/potentiation-of-the-anticoagulation-effect-of-warfarin-by-the-herbal-remedy-shu-jing-hwo-shiee-tang-in-rats-the-dosing-regimen-and-pharmacokinetic-interaction
#8
Yune-Fang Ueng, Chung-Kuang Lu, Sien-Hung Yang, Hong-Jaan Wang, Chiung-Chiao Huang
The herbal remedy Shu-Jing-Hwo-Shiee-Tang (SJHST) has been used in traditional Chinese medical care for the treatment of osteoarthritis. This study aims to examine the influence of SJHST on the oxidation and anticoagulation effect of warfarin in male rats. In three SJHST preparations (S1-S3), hesperidin, gentiopicrin, and paeoniflorin were identified as chemical marker ingredients. The inhibition of liver microsomal warfarin 7-hydroxylation (WOH) activity by 50% methanolic extracts of SJHST was potentiated by β-glucosidase pretreatment, but not by NADPH-fortified microsomal preincubation...
December 8, 2016: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28105859/structure-activity-relationship-of-flavanone-anti-degranulation-activity-of-7-o-substituted-hesperetin
#9
Toshiro Noshita, Akihiro Tai, Takuya Matsumoto, Kaori Miura, Kaoru Ikeda, Yoshitomo Hamada
A series of 7-O-substituted hesperetins was evaluated for degranulation-inhibiting activity in rat basophil leukaemia cells. 7-O-Methyl and 7-O-ethyl hesperetin exhibited potent anti-degranulation activity compared with the original hesperetin.
January 20, 2017: Natural Product Research
https://www.readbyqxmd.com/read/28103505/hesperetin-protects-against-h2o2-triggered-oxidative-damage-via-upregulation-of-the-keap1-nrf2-ho-1-signal-pathway-in-arpe-19-cells
#10
Chao Zhu, Yuchen Dong, Haile Liu, Hua Ren, Zhihua Cui
Age-related macular degeneration (AMD) is an irreversible vision loss disease that primarily results from oxidative stress that causes oxidative damage to the retinal pigment epithelial (RPE) cells. Hesperetin (Hesp) is a common flavanone glycoside compound that has been demonstrated to exhibit a variety of biological and pharmacological properties that include anti-inflammatory and antioxidant properties. The aim of this study is to explore the ability of Hesp to attenuate oxidative damage in hydrogen peroxide (H2O2)-stimulated ARPE-19 cells...
April 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28065188/flavanone-rich-citrus-beverages-counteract-the-transient-decline-in-postprandial-endothelial-function-in-humans-a-randomised-controlled-double-masked-cross-over-intervention-study
#11
Catarina Rendeiro, Honglin Dong, Caroline Saunders, Laura Harkness, Melvin Blaze, Yanpeng Hou, Ronald L Belanger, Giulia Corona, Julie A Lovegrove, Jeremy P E Spencer
Specific flavonoid-rich foods/beverages are reported to exert positive effects on vascular function; however, data relating to effects in the postprandial state are limited. The present study investigated the postprandial, time-dependent (0-7 h) impact of citrus flavanone intake on vascular function. An acute, randomised, controlled, double-masked, cross-over intervention study was conducted by including middle-aged healthy men (30-65 years, n 28) to assess the impact of flavanone intake (orange juice: 128·9 mg; flavanone-rich orange juice: 272·1 mg; homogenised whole orange: 452·8 mg; isoenergetic control: 0 mg flavanones) on postprandial (double meal delivering a total of 81 g of fat) endothelial function...
December 2016: British Journal of Nutrition
https://www.readbyqxmd.com/read/28063664/hesperetin-etoposide-combinations-induce-cytotoxicity-in-u2os-cells-implications-on-therapeutic-developments-for-osteosarcoma
#12
Laura Coutinho, Helena Oliveira, Ana Rita Pacheco, Luis Almeida, Francisco Pimentel, Conceição Santos, José Miguel P Ferreira de Oliveira
Osteosarcoma chemotherapy has improved survival rates, however, chemoresistance and drug toxicity still limit therapy. Drug combinations may overcome these limitations by allowing fewer chemoresistant cells to survive. The aim of this study was to evaluate the cytotoxic potential of hesperetin to osteosarcoma and to analyze the cell cycle effects of combinations of hesperetin with chemotherapeutic agents. For this, the U2OS human osteosarcoma cell line was exposed to hesperetin or hesperetin combined with etoposide or doxorubicin in defined proportions...
February 2017: DNA Repair
https://www.readbyqxmd.com/read/28025998/in-vitro-screening-of-radioprotective-properties-in-the-novel-glucosylated-flavonoids
#13
Hao Yu, Jeremy S Haskins, Cathy Su, Allison Allum, Alexis H Haskins, Victoria A Salinas, Shigeaki Sunada, Taisuke Inoue, Yasushi Aizawa, Mitsuru Uesaka, Takamitsu A Kato
Novel glucosyl flavonoids are developed by the addition of glucose to naturally occurring flavonoids. Flavonoids are known antioxidants that possess radioprotective properties. In order to investigate the radioprotective properties of novel glucosyl flavonoids, in vitro DNA double-strand breaks (DSBs) analysis was carried out. In the present study, Quercetin, Naringenin, and Hesperetin groups of flavonoids included in the natural and novel glucosyl 13 flavonoids were investigated. Flavonoids were mixed with Lambda DNA, and subsequently exposed to gamma‑rays...
November 2016: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/27988309/naringenin-suppresses-edwardsiella-tarda-infection-in-gaks-cells-by-nana-sialidase-inhibition
#14
Sayaka Shinyoshi, Yuko Kamada, Koki Matsusaki, Petros Kingstone Chigwechokha, Supawan Tepparin, Kyosuke Araki, Masaharu Komatsu, Kazuhiro Shiozaki
Edwardsiella tarda (E. tarda) is a gram-negative bacterium, which causes Edwardsiellosis in aquaculture. Previous studies indicate that E. tarda NanA sialidase plays crucial roles in infection through the desialylation of glycoproteins in fish cells. On the other hand, 2-deoxy-2,3-dehydro-N-acetylneuraminic acid, classic sialidase inhibitor, negatively regulates E. tarda infection of goldfish scale GAKS cells. Here, to development the suppression model of E. tarda infection for aquaculture application, the possibility of NanA inhibitory activities in citrus phytochemicals was evaluated as citrus extracts have widely been used as a supplement in fish diets for the improvement of meat quality...
February 2017: Fish & Shellfish Immunology
https://www.readbyqxmd.com/read/27987794/bioflavonoid-hesperetin-overcome-bicalutamide-induced-toxicity-by-co-delivery-in-novel-snedds-formulations-optimization-in-vivo-evaluation-and-uptake-mechanism
#15
Abhishek Arya, Hafsa Ahmad, Sachin Tulsankar, Satish Agrawal, Naresh Mittapelly, Rajkumar Boda, Rabi S Bhatta, Kalyan Mitra, Anil K Dwivedi
In the present study, we designed Bicalutamide (BCT) and Hesperetin (HSP) co-loaded self nano-emulsifying drug delivery system (SNEDDS) to encounter the problem of BCT induced toxicity, low solubility, and bioavailability. Optimized BCT-HSP SNEDDS would produce an emulsion of globule size 30.84±1.24nm with a high encapsulation efficiency of BCT (91.29%) and HSP (88.19%), and showed rapid drug release. DPPH assay confirmed the retention of antioxidant potential of HSP in SNEDDS. DCFH-DA confirmed intense green fluorescence in HSP treated groups due to the generation of reactive oxygen species...
February 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/27904048/inhibitory-effect-of-hesperetin-and-naringenin-on-human-udp-glucuronosyltransferase-enzymes-implications-for-herb-drug-interactions
#16
Dan Liu, Jie Wu, Hongbo Xie, Mingyi Liu, Isaiah Takau, Hong Zhang, Yuqing Xiong, Chunhua Xia
Hesperetin (HET) and naringenin (NGR) are flavanones found in citrus (oranges and grapefruit) and Aurantii Fructus Immaturus. The present study aims to investigate the inhibition potential of HET and NGR derivatives towards one of the most important phase II drug-metabolizing enzymes-uridine diphosphate (UDP)-glucuronosyltransferases (UGTs). We used trifluoperazine as a probe substrate to test UGT1A4 activity, and recombinant UGT-catalyzed 4-methylumbelliferone glucuronidation was used as a probe reaction for other UGT isoforms...
2016: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/27812412/in-silico-study-on-anti-chikungunya-virus-activity-of-hesperetin
#17
Adrian Oo, Pouya Hassandarvish, Sek Peng Chin, Vannajan Sanghiran Lee, Sazaly Abu Bakar, Keivan Zandi
BACKGROUND: The re-emerging, Aedes spp. transmitted Chikungunya virus (CHIKV) has recently caused large outbreaks in a wide geographical distribution of the world including countries in Europe and America. Though fatalities associated with this self-remitting disease were rarely reported, quality of patients' lives have been severely diminished by polyarthralgia recurrence. Neither effective antiviral treatment nor vaccines are available for CHIKV. Our previous in vitro screening showed that hesperetin, a bioflavonoid exhibits inhibitory effect on the virus intracellular replication...
2016: PeerJ
https://www.readbyqxmd.com/read/27803291/neuroprotective-efficacy-of-hesperetin-against-cadmium-induced-oxidative-stress-in-the-brain-of-rats
#18
Kalist Shagirtha, Nazima Bashir, Selvaraj MiltonPrabu
The present study was designed to investigate the neuroprotective effect of hesperetin (Hp) against cadmium (Cd)-induced neurotoxicity in rats. Cadmium (3 mg/kg body weight (b.w.), subcutaneous) administration for 3 weeks demonstrated neurotoxicity in rats by the decreased activity of acetylcholinesterase in the brain. The oxidative stress markers (thiobarbituric acid reactive substances and protein carbonyls) were significantly increased with decreased enzymatic (superoxide dismutase, catalase, glutathione peroxidase, glutathione S-transferase) and non-enzymatic antioxidants (reduced glutathione, total sulphydryl groups and vitamin C)...
November 1, 2016: Toxicology and Industrial Health
https://www.readbyqxmd.com/read/27771138/hesperidin-interaction-to-collagen-detected-by-physico-chemical-techniques
#19
Noriko Hiraishi, Takahiro Maruno, Naoya Tochio, Ryohei Sono, Masayuki Otsuki, Tsutomu Takatsuka, Junji Tagami, Yuji Kobayashi
OBJECTIVE: Dentin collagen can be modified by some plant-derived flavonoids to improve properties of dentin organic matrix. Hesperidin (HPN), a hesperetin-7-O-rutinoside flavonoid, has a potential of dentin modification for being based on evidence that a treatment with HPN may resist collagenase degradation and arrest demineralization of human dentin. In this study, biophysical and molecular-level information on the interaction of HPN and collagen was investigated. METHODS: HPN is extracted from citrus fruits...
October 19, 2016: Dental Materials: Official Publication of the Academy of Dental Materials
https://www.readbyqxmd.com/read/27722779/catabolism-of-citrus-flavanones-by-the-probiotics-bifidobacterium-longum-and-lactobacillus-rhamnosus
#20
Gema Pereira-Caro, Begoña Fernández-Quirós, Iziar A Ludwig, Inmaculada Pradas, Alan Crozier, José Manuel Moreno-Rojas
PURPOSE: Orange juice (OJ) flavanones undergo limited absorption in the upper gastrointestinal tract and reach the colon where they are transformed by the microbiota prior to absorption. This study investigated the ability of two probiotic bacteria, Bifidobacterium longum R0175 and Lactobacillus rhamnosus subsp. Rhamnosus NCTC 10302 to catabolise OJ flavanones. METHODS: The bacteria were incubated with hesperetin-7-O-rutinoside, naringenin-7-O-rutinoside, hesperetin and naringenin, and the culture medium and intracellular cell extracts were collected at intervals over a 48 h of incubation period...
October 8, 2016: European Journal of Nutrition
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