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Darrell Sawmiller, Ahsan Habib, Song Li, Donna Darlington, Huayan Hou, Jun Tian, R Douglas Shytle, Adam Smith, Brian Giunta, Takashi Mori, Jun Tan
Naturally-occurring bioactive flavonoids such as diosmin significantly reduces amyloid beta (Aβ) associated pathology in Alzheimer's disease (AD) mouse models. In the present study, oral administration of diosmin reduced cerebral Aβ oligomer levels, tau-hyperphosphorylation and cognitive impairment in the 3xTg-AD mouse model through glycogen synthase kinase-3 (GSK-3) and transient receptor potential canonical 6-related mechanisms. Diosmetin, one major bioactive metabolite of diosmin, increased inhibitory GSK-3β phosphorylation, while selectively reducing γ-secretase activity, Aβ generation, tau hyperphosphorylation and pro-inflammatory activation of microglia in vitro, without altering Notch processing...
October 15, 2016: Journal of Neuroimmunology
Marta Mendel, Magdalena Chłopecka, Natalia Dziekan, Wojciech Karlik
Citrus flavonoids are acknowledged for numerous pharmacological activities, including the myorelaxant effect on various smooth muscles. However, there is no data on their effect on jejunum contractility. Therefore, the aim of the study at hand was to evaluate the impact of hesperetin and diosmetin along with their glycosides on the motoric activity of intestine and to verify the possible mechanism of hesperetin-induced effect. The experiments were performed on rat isolated jejunum strips and were conducted under isometric conditions...
October 6, 2016: European Journal of Pharmacology
Satish Kumar Bedada, Praveen Kumar Boga
1. Carbamazepine (CBZ) is an antiepileptic drug with narrow therapeutic window and administration in humans receiving long-term therapy with diosmin (DSN) may occur, which leads to CYP3A4 mediated drug interactions. The purpose of the present study was to assess the influence of DSN on the metabolism and pharmacokinetics of CBZ in healthy volunteers. 2. An open-label, sequential, two period study was conducted in 12 healthy male volunteers. A single dose of DSN 500 mg was administered once daily for 10 days during treatment phase...
October 3, 2016: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
Azucena I Carballo-Villalobos, María-Eva González-Trujano, Francisco Pellicer, Francisco J López-Muñoz
Neuropathic pain is caused by a primary lesion, dysfunction, or transitory perturbation in the peripheral or central nervous system. In this study, we investigated the hesperidin antihyperalgesic effects alone or combined with diosmin in a model of neuropathic pain to corroborate a possible synergistic antinociceptive activity. Mechanical and thermal hyperalgesia were assessed in the aesthesiometer and plantar tests, respectively, after chronic constriction injury (CCI) model in rats receiving hesperidin (HS, 5 doses from 10 to 1000 mg/kg) alone or combined with diosmin (DS, 10 and 100 mg/kg) in comparison to gabapentin (31...
2016: BioMed Research International
M R Kuznetsov, S V Sapelkin, B V Boldin, S G Leont'ev, L A Neskhodimov
The authors analysed the results of examination and treatment of a total of 102 patients presenting with iliofemoral venous thrombosis. During treatment, ultrasonographic duplex scanning was used to determine the localization of the proximal margin of thrombotic masses, the time of appearing of the first signs of recanalization, its degree at various levels of the deep venous system, as well as alteration in velocity of the venous blood flow in the deep veins of the lower limbs. The dynamics of clinical symptoms was assessed by the visual analogue scale...
2016: Angiologii︠a︡ i Sosudistai︠a︡ Khirurgii︠a︡, Angiology and Vascular Surgery
Marcin Szymański, Daria Młynarek, Arkadiusz Szymański, Irena Matławska
Diosmin and hesperidin are natural flavonoid glycosides found in various plant materials, mainly in citrus fruits in different concentrations. Diosmin for pharmaceutical use is obtained mainly semi-synthetically from hesperidin. Hesperidin often accompanies diosmin as a natural impurity in different pharmaceutical formulations; therefore, a simple, fast and precise method for the simultaneous assay of diosmin and hesperidin in pharmaceutical formulations has been developed to control their contents. Chromatographic resolution was performed using a column with C-18 packing and the following mobile phase: methanol/water (45:55, v/v) with 0...
2016: Iranian Journal of Pharmaceutical Research: IJPR
Muthusamy Rajasekar, Kathiresan Suresh, Kathiresan Sivakumar
Diosmin is naturally found flavanoid in many citrus fruits known to have anti-inflammatory, antihyperglycemic, antioxidant and antimutagenic properties. Effects of Diosmin on IL-6/STAT-3 expression in hamster buccal pouch carcinogenesis remain unclear. Alterations in many genes encode crucial proteins, which regulate cell proliferation, differentiation and apoptosis have been implicated in oral cancer. In the present study, we investigated the effect of dietary Diosmin on IL-6/STAT-3 signaling in the 7,12-dimethylbenz[a]anthracene (DMBA)-induced hamster buccal pouch (HBP) carcinogenesis by examining the protein expression of IL-6/STAT-3 and its related genes...
August 18, 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Renato Riera Toledo, Maria Elisabeth Rennó de Castro Santos, Taylor Brandão Schnaider
BACKGROUND: Venous ulcers are common complications of chronic venous insufficiency that result in severe physical and mental suffering to patients. The oral administration of diosmin/hesperidin has been used as adjuvant therapy in the treatment of chronic venous insufficiency. The purpose of this study was to evaluate and compare the effect of pycnogenol and diosmin/hesperidin on the healing of venous ulcers. METHODS: This longitudinal, prospective, randomized clinical trial was conducted with 30 adult patients with venous ulcers from a vascular surgery outpatient clinic of a university hospital...
August 10, 2016: Annals of Vascular Surgery
Sahabuddin Ahmed, Nitin Mundhe, Manash Borgohain, Liakat Chowdhury, Mohit Kwatra, Nityanand Bolshette, Anwaruddin Ahmed, Mangala Lahkar
Hyperglycaemia-mediated oxidative stress plays an imperative role in the progression of diabetic nephropathy. NF-kB is an important transcription factor in eukaryotes which regulates a diverse array of cellular process, including inflammation, immunological response, apoptosis, growth and development. Increased expression of NF-kB plays a vital role in the pathogenesis of many inflammatory diseases including diabetic nephropathy. Hence, the present study was designed to explore the nephroprotective nature of diosmin by assessing the various biochemical parameters, markers of oxidative stress and proinflammatory cytokine levels in alloxan-induced diabetic Wistar rats...
October 2016: Inflammation
Luciana Naso, Valeria R Martínez, Luis Lezama, Clarisa Salado, María Valcarcel, Evelina G Ferrer, Patricia A M Williams
The natural antioxidant flavonoid diosmin, found in citric fruits, showed low antioxidant properties among other flavonoids due to its structural characteristics and low cytotoxicity against lung (A549) and breast (T47D, SKBR3 and MDAMB231) cancer cell lines. The anticancer behavior has been improved by the metal complex generated with the flavonoid and the oxidovanadium(IV) ion. This new complex, [VO(dios)(OH)3]Na5·6H2O (VOdios), has been synthesized and characterized both in solid and solution states. The interaction of the metal ion through the sugar moiety of diosmin precluded the improvement of the antioxidant effects...
September 15, 2016: Bioorganic & Medicinal Chemistry
Alejandro Gonzalez Ochoa
BACKGROUND: In the treatment of venous leg ulcers, vasoactive drugs such as diosmin hesperidin micronized purified flavonoids (DH), and recently sulodexide (SDX), have been used besides compression therapy and local measures. The purpose of this study is to investigate whether administering both drugs SDX and DH is better than DH alone in the treatment of venous ulcer. METHODS: In an open-label, observational, non-parallel trial, 70 patients with 90 venous ulcers were treated with multi-layer bandaging, local measures and DH, 37 patients (50 ulcers) also received SDX, 33 patients (40 ulcers) without SDX were the control group...
June 16, 2016: International Angiology: a Journal of the International Union of Angiology
Alfredo Aires, Eduardo Marrinhas, Rosa Carvalho, Carla Dias, Maria José Saavedra
Pterospartum tridentatum and Mentha pulegium are largely used in Portuguese folk medicine to treat several human disorders and inflammatory processes but without any consistent evidence for those beneficial pointed properties. Thus, the aim of the current work is to evaluate its benefits and phytochemicals related to those beneficial properties. A distinct polyphenol profile between P. tridentatum and M. pulegium was found. Taxifolin, myricetin, ginestin, ginestein, and ginestein derivatives, biochanin A-glucoside, and biochanin A were identified in P...
2016: BioMed Research International
Satish Kumar Bedada, Praveen Kumar Boga, Harish Kaushik Kotakonda
1. Diosmin (DSN) has been found to possess P-glycoprotein (P-gp) inhibition activity in vitro and in vivo in rats, which may have potential to cause P-gp-mediated interactions in humans. The purpose of the present study was to investigate the effect of DSN on pharmacokinetics of fexofenadine (FEX) in healthy human volunteers. 2. An open-label, two-period, sequential study was conducted in 12 healthy male volunteers. A single dose of FEX 120 mg was administered to volunteers during control and treatment phases...
May 6, 2016: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
Viktoriia Burkina, Vladimir Zlabek, Ruth Halsne, Erik Ropstad, Galia Zamaratskaia
Flavonoids are known to have effects on cytochrome P450 enzymatic activity. However, little effort has been made to examine species differences and the relevance of studies on mammalian and fish microsomes so that extrapolations can be made to humans. Therefore, the effects of several naturally occurring flavonoids on the activity of CYP3A-dependent 7-benzyloxy-4-trifluoromethylcoumarin O-debenzylase (BFCOD) were evaluated in human, pig, mouse, and juvenile rainbow trout sources of hepatic microsomes. Each was exposed to three concentrations (1, 10, and 100μM) of diosmin, naringin, and naringenin...
June 15, 2016: Biochemical Pharmacology
Maria José Martinez-Zapata, Robin W M Vernooij, Sonia Maria Uriona Tuma, Airton T Stein, Rosa M Moreno, Emilio Vargas, Dolors Capellà, Xavier Bonfill Cosp
BACKGROUND: Chronic venous insufficiency (CVI) is a common condition caused by valvular dysfunction with or without associated obstruction, usually in the lower limbs. It might result in considerable discomfort with symptoms such as pain, itchiness and tiredness in the legs. Patients with CVI may also experience swelling and ulcers. Phlebotonics are a class of drugs often used to treat CVI. This is an update of a review first published in 2005. OBJECTIVES: To assess the efficacy and safety of phlebotonics administered both orally and topically for treatment of signs and symptoms of lower extremity CVI...
2016: Cochrane Database of Systematic Reviews
C Yao, Y Xu, L Chen, H Jiang, C S Ki, J S Byun, W Bian
BACKGROUND: Effective treatment for breast cancer-related chronic lymphedema (bcrl) remains a clinical challenge. Acupuncture and moxibustion treatments have been shown to be beneficial and safe for treating bcrl. In the present randomized controlled trial, we compared the effectiveness of combined acupuncture and moxibustion ("warm acupuncture") with that of diosmin in bcrl. METHODS: Breast cancer patients who met the inclusion and exclusion criteria (n = 30) were randomized to experimental and control groups (15 per group)...
February 2016: Current Oncology
Kapil K Patil, Rohan J Meshram, Nagesh A Dhole, Rajesh N Gacche
Sugar induced cataractogenesis and visual impairment is more prominent ophthalmic problem in humans suffering from diabetes. Flavonoids have been identified as one of the therapeutically important class of phytochemicals possessing myriad of biological activities. Analyzing the anti-cataract effects of flavonoids from natural sources is an important aspect owing to their bioavailability in variety of dietary sources. In the present study a panel of ten dietary flavonoids like 3, 6-dihydroxy flavone, 3, 7-dihydroxy flavone, chrysin, 3-hydroxy-7-methoxy flavone, apigenin, genistein, baicalein, galangin, Biochanin-A, and diosmin were evaluated for their anti-cataract effects in sugar induced lens model studies...
March 1, 2016: Archives of Biochemistry and Biophysics
V Vinoth Prabhu, D Sathyamurthy, Anand Ramasamy, Saibal Das, Medepalli Anuradha, Sudhakar Pachiappan
Context There have not been any conclusive studies of the effects of diosmin, a modified flavanone glycoside obtained from Teucrium gnaphalodes L'Her (Lamiaceae), on urolithiasis. Objective To evaluate anti-urolithiatic effects of diosmin in ammonium chloride and ethylene glycol-induced renal stone in experimental animals. Materials and methods Thirty Sprague-Dawley were divided into five groups (n=6) receiving the following treatments, respectively, p.o. for 15 consecutive days: distilled water, 0.75% v/v ethylene glycol + 2% w/v ammonium chloride, 0...
September 2016: Pharmaceutical Biology
Fábio Dos Santos Schlottfeldt, Sheila Marques Fernandes, Daniel Malisani Martins, Priscilla Cordeiro, Cassiane Dezoti da Fonseca, Mirian Watanabe, Maria de Fatima Fernandes Vattimo
Objective To evaluate the effect of diosmin and hesperidin flavonoids in the prevention of amphotericin B nephrotoxicity, through an experimental model on rats. Method Adult, male Wistar rats were distributed into the following groups: saline; diosmin hesperidin (animals that received 50 mg/kg of diosmin hesperidin, drinking water, for ten days); amphotericin B (animals that received 15 mg/kg/day of amphotericin B through intraperitoneal treatment for five days); amphotericin B+diosmin hesperidin. Renal function, fractional excretion of sodium; potassium and magnesium and oxidative metabolites were evaluated...
February 2015: Revista da Escola de Enfermagem da U S P
Andreana Marino, Gokhan Zengin, Antonia Nostro, Giovanna Ginestra, Paola Dugo, Francesco Cacciola, Natalizia Miceli, Maria Fernanda Taviano, Angela Filocamo, Giuseppe Bisignano, Abdurrahman Aktumsek
The antimicrobial activity of acetone, methanol and aqueous extracts of Asphodeline anatolica E. Tuzlaci leaves was evaluated against American type culture collection, food and clinical isolates (Listeria monocytogenes and Staphylococcus aureus including methicillin-resistant strains-MRSA). Biofilm formation, toxicity and characterisation of the polyphenolic content were analysed. The acetone extract demonstrated a higher antibacterial activity against S. aureus including MRSA strains, L. monocytogenes and Pseudomonas aeruginosa than against other extracts...
January 4, 2016: Natural Product Research
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