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https://www.readbyqxmd.com/read/29210311/the-role-of-gut-microbiota-in-the-modulation-of-drug-action-a-focus-on-some-clinically-significant-issues
#1
Diego Currò
A healthy gut microbiota is necessary for the normal operation of several body functions, including gastrointestinal sensitivity and motility, lipid and glucid metabolism, immune surveillance, and host behavior. In addition, intestinal bacteria contribute to determining the pharmacological properties of several drugs by producing different drug metabolizing enzymes. Areas covered: Four enzymatic processes are discussed: prodrug activation; drug inactivation; drug deconjugation; and hydrolysis of natural glycosides with further metabolism of released aglycones...
December 6, 2017: Expert Review of Clinical Pharmacology
https://www.readbyqxmd.com/read/29187079/anti-inflammatory-antioxidant-and-anti-apoptotic-activity-of-diosmin-in-acetic-acid-induced-ulcerative-colitis
#2
A S Shalkami, Mia Hassan, A G Bakr
Ulcerative colitis (UC) is a chronic inflammatory disease affecting colon. The primary symptoms of UC are diarrhoea with blood and mucus and sometimes associated with pain. AIM: This study aimed to evaluate the effects of diosmin (DIO) on UC. METHODS: UC was induced in rats by rectal administration of acetic acid (AA). The degree of mucosal ulceration and damage was determined by evaluating the disease activity index (DAI) and colon damage index scores. Inflammation, oxidative stress and apoptotic responses were determined by measuring the levels of tumour necrosis factor-α (TNF-α), cyclooxygenase-2 (COX-II), malondialdehyde (MDA) and reduced glutathione (GSH) in addition to myeloperoxidase (MPO) activity and caspase-3 expression...
January 2018: Human & Experimental Toxicology
https://www.readbyqxmd.com/read/29134244/modulation-of-cyp3a-enzyme-activity-by-diosmin-and-its-consequence-on-carbamazepine-pharmacokinetics-in-rats
#3
Satish Kumar Bedada, Prasad Neerati
Diosmin is a widely used flavonoid for the treatment of varicose veins and hemorrhoids. Epileptic patients with hemorrhoids and varicose veins may use diosmin along with carbamazepine (CBZ) therapy, which leads to pharmacokinetic interaction between diosmin and CBZ. Therefore, the present study was performed to evaluate the effect of diosmin on the pharmacokinetics of CBZ in rats. Diosmin-mediated altered CYP3A enzyme activity in human and rat liver microsomes was examined using CYP3A dependent erythromycin N-demethylase assay...
November 14, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/29126754/effect-of-pulsed-therapeutic-ultrasound-and-diosmin-on-skeletal-muscle-oxidative-parameters
#4
Luis Fernando Sousa Filho, Paula P Menezes, Dayanne Valéria Soares Santana, Bruno S Lima, Shanmugan Saravanan, Grace Kelly M Almeida, José Evaldo R Menezes Filho, Marta M B Santos, Adriano Antunes A S Araújo, Evaleide Diniz de Oliveira
Cyclodextrins (CDs) have been widely used as a promising alternative in the formation of inclusion complexes with poorly soluble molecules. From this perspective, the present study aimed to study the inclusion complexes of diosmin in β-cyclodextrin, chemically quantify the diosmin-in-gel preparation and analyze the stability of the gels. Furthermore, we evaluated the effect of therapeutic pulsed ultrasound (TPU) in association with the gel-diosmin complex on the parameters of muscle damage and oxidative stress in rats...
November 7, 2017: Ultrasound in Medicine & Biology
https://www.readbyqxmd.com/read/29119110/a-randomized-controlled-trial-evaluating-the-effects-of-diosmin-in-the-treatment-of-radicular-pain
#5
Yinhe Wang, Xin Fang, Lei Ye, Yishan Li, Hongfei Shi, Yang Cao
Diosmin has been widely used to treat patients with vascular pain for its potent anti-inflammatory and analgesic effects. To evaluate the therapeutic effects of Diosmin in the treatment of radicular pain, we conducted an investigator-initiated, randomized, active-controlled noninferiority trial between January 1, 2009, and December 1, 2010. Diosmin (50 mg/kg/day) was orally administered to treat the radicular pain in 150 patients for one month. Another 150 patients with the same symptom were given 20% 250 ml mannitol (1 g/kg/day) for 7 days and dexamethasone (10 mg/day) for 3 days intravenously guttae...
2017: BioMed Research International
https://www.readbyqxmd.com/read/29100118/in%C3%A2-vitro-effects-of-diosmin-naringenin-quercetin-and-indole-3-carbinol-on-fish-hepatic-cyp1a1-in-the-presence-of-clotrimazole-and-dexamethasone
#6
Sidika Sakalli, Viktoriia Burkina, Nadezhda Pilipenko, Vladimir Zlabek, Galia Zamaratskaia
Phytochemicals are widely present in fruits, vegetables and other plants and have great health benefits owing to their antioxidant properties. They are naturally found in the aquatic environment as well as discharged from sewage treatment plants after their large consumption. Little is known about their impact on fish; particularly in light of their interactions with pharmaceuticals. Therefore, this study was designed to determine the effects of diosmin, naringenin, quercetin and idole-3-carbinol on CYP1A-dependent 7-ethoxyresorufin-O-deethylase (EROD) activity on rainbow trout hepatic microsomes in the presence of two pharmaceuticals: clotrimazole and dexamethasone...
October 23, 2017: Chemosphere
https://www.readbyqxmd.com/read/29091880/central-and-peripheral-anti-hyperalgesic-effects-of-diosmin-in-a-neuropathic-pain-model-in-rats
#7
Azucena Ibeth Carballo-Villalobos, María Eva González-Trujano, Francisco Pellicer, Noé Alvarado-Vásquez, Francisco Javier López-Muñoz
Flavonoids are natural compounds showing anti-hyperalgesic activity in models of pain. Diosmin is a compound poorly studied in the treatment of neuropathic pain. This study evaluates the anti-hyperalgesic actions of diosmin and possible mechanisms of action involved by using a neuropathic pain model in rats. Experimental neuropathic pain was induced by chronic constriction injury (CCI) in male Wistar rats, then aesthesiometric index and plantar tests were assessed to evaluate mechanical and thermal hyperalgesia, respectively, in order to explore the analgesic effects of acute and sub-chronic treatment with diosmin...
October 26, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29036797/effects-of-venotonic-drugs-on-the%C3%A2-microcirculation-comparison-between-ruscus-extract-and-micronized-diosmine1
#8
Fatima Zely Garcia de Almeida Cyrino, Daniela Signorelli Balthazar, Fernando Lencastre Sicuro, Eliete Bouskela
BACKGROUND: Chronic venous disease of the lower limbs is a common public health problem worldwide with negative impact on quality of life and results with drugs used to treat it are sparse, probably due to lack of good experimental models. OBJECTIVE: In this investigation we have tested the effects of two commonly used venotonic substances, Ruscus extract and micronized diosmine, on the microcirculation in vivo. METHODS: These substances were given orally, by gavage, during two weeks, twice daily and observations were made using the hamster cheek pouch preparation...
October 7, 2017: Clinical Hemorheology and Microcirculation
https://www.readbyqxmd.com/read/28988357/the-effects-of-diosmin-on-aflatoxin-induced-liver-and-kidney-damage
#9
Gökhan Eraslan, Zeynep Soyer Sarıca, Latife Çakır Bayram, Muhammet Yasin Tekeli, Murat Kanbur, Mürsel Karabacak
Aflatoxin is among the natural toxins that cause serious side effects on living things. Diosmin is also one of the compounds with broad pharmacological effects. In this study, the effects on the oxidant/antioxidant system of 50 mg/kg body weight/day dose of diosmin, aflatoxin (500 μg/kg body weight/day), and combined aflatoxin (500 μg/kg body weight/day) plus diosmin (50 mg/kg body weight/day) given to the stomach via catheter female adult Wistar Albino rats is examined. Forty rats were used in the experiment, and these animals were randomly allocated to four equal groups...
October 8, 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/28862211/diosmin-reduces-cell-viability-of-a431-skin-cancer-cells-through-apoptotic-induction
#10
Rajamanickam Buddhan, Shanmugam Manoharan
OBJECTIVES: Aim of the present study was to evaluate the in vitro cytotoxic potential of the diosmin in A431 skin cancer cells. MATERIALS AND METHODS: The cytotoxic (anti-cell proliferative) potential of diosmin in A431 cells was assessed using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay (cell viability), dual staining (apoptotic induction), dichloro-dihydro-fluorescein diacetate assay (reactive oxygen species [ROS] generation), DNA fragmentation study, Western blotting analysis (apoptotic markers expression) and flow cytometry (cell cycle arrest)...
July 2017: Journal of Cancer Research and Therapeutics
https://www.readbyqxmd.com/read/28846859/diosmin-ameliorates-the-effects-of-oxidative-stress-in-lenses-of-streptozotocin-induced-type-1-diabetic-rats
#11
Weronika Wojnar, Ilona Kaczmarczyk-Sedlak, Maria Zych
BACKGROUND: Diabetic cataractogenesis is a complex process connected with hyperglycemia and oxidative stress. Free radicals induce many unfavorable changes in the activity of the antioxidative enzymes and may also lead to oxidative damage. Since diosmin, a plant-derived flavonoid, reveals antioxidative activity, the aim of the study was to investigate if this substance may counteract the oxidative stress in the lenses of diabetic rats. METHODS: The study was conducted on the male Wistar rats with streptozotocin-induced type 1 diabetes...
April 15, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28819818/diosmin-prevents-isoproterenol-induced-heart-mitochondrial-oxidative-stress-in-rats
#12
S Sharmila Queenthy, P Stanely Mainzen Prince, Babu John
Cardiac mitochondrial oxidative stress causes mitochondrial damage that plays an important role in the pathology of myocardial infarction. The preventive effects of diosmin on cardiac mitochondrial oxidative stress in isoproterenol-induced myocardial infarcted rats were evaluated. Rats were pretreated with diosmin (10 mg/kg body weight) daily for 10 days. Myocardial infarction was induced in rats by isoproterenol (100 mg/kg body weight) injection twice at an interval of 24 h (on 11th and 12th day). Isoproterenol-induced myocardial infarcted rats showed a significant increase in the levels of cardiac diagnostic markers, heart mitochondrial lipid peroxidation, calcium ion, and a significant decrease in the levels of heart mitochondrial glutathione peroxidase, reduced glutathione, glutathione-S-transferase, isocitrate, malate, α-ketoglutarate, and succinate dehydrogenases...
August 17, 2017: Cardiovascular Toxicology
https://www.readbyqxmd.com/read/28819543/diosmin-attenuates-methotrexate-induced-hepatic-renal-and-cardiac-injury-a-biochemical-and-histopathological-study-in-mice
#13
Mohamed M Abdel-Daim, Hesham A Khalifa, Abdelrahman Ibrahim Abushouk, Mohamed A Dkhil, Saleh A Al-Quraishy
The current study was designed to investigate the beneficial role of diosmin, a biologically active flavonoid, against methotrexate- (MTX-) induced hepatic, renal, and cardiac injuries in mice. Male Swiss albino mice received a single intraperitoneal injection of MTX (at 20 mg/kg, body weight) either alone or in combination with oral diosmin (at 50 or 100 mg/kg body weight, for 10 days). Serum was used to evaluate tissue injury markers, while hepatic, renal, and cardiac tissue samples were obtained for determination of antioxidant activity as well as histopathological examination...
2017: Oxidative Medicine and Cellular Longevity
https://www.readbyqxmd.com/read/28804235/management-of-varicose-veins-and-chronic-venous-insufficiency-in-a-comparative-registry-with-nine-venoactive-products-in-comparison-with-stockings
#14
G Belcaro, M Dugall, R Luzzi, M Corsi, A Ledda, A Ricci, L Pellegrini, M R Cesarone, M Hosoi, B M Errichi, U Cornelli, R Cotellese, G Agus, B Feragalli
The aim of this registry study was to compare products used to control symptoms of CVI. Endpoints of the study were microcirculation, effects on volume changes, and symptoms (analogue scale). Pycnogenol, venoruton, troxerutin, the complex diosmin-hesperidin, Antistax, Mirtoselect (bilberry), escin, and the combination Venoruton-Pycnogenol (VE-PY) were compared with compressions. No safety or tolerability problems were observed. At inclusion, measurements in the groups were comparable: 1,051 patients completed the registry...
September 2017: International Journal of Angiology: Official Publication of the International College of Angiology, Inc
https://www.readbyqxmd.com/read/28768146/diosmin-prevents-left-ventricular-hypertrophy-adenosine-triphosphatases-dysfunction-and-electrolyte-imbalance-in-experimentally-induced-myocardial-infarcted-rats
#15
Sharmila Queenthy Sabarimuthu, Stanely Mainzen Prince Ponnian, Babu John
Currently, there has been an increased interest globally to identify natural compounds that are pharmacologically potent and have low or no adverse effects for use in preventive medicine. Myocardial infarction is a vital pathological feature resulting in high levels of mortality and morbidity. Left ventricular hypertrophy (LVH), adenosine triphosphatases (ATPases) dysfunction and electrolyte imbalance play a vital role in the pathogenesis of myocardial infarction. This study aims to evaluate the preventive effects of diosmin on LVH, ATPases dysfunction and electrolyte imbalance in isoproterenol induced myocardial infarcted rats...
November 5, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28738538/diosmin-improved-cognitive-deficit-and-amplified-brain-electrical-activity-in-the-rat-model-of-traumatic-brain-injury
#16
Mohammad Ali Mirshekar, Hamed Fanaei, Fereshteh Keikhaei, Fatemeh Sargolzaee Javan
OBJECTIVE: Traumatic brain injury (TBI) is one of the main causes of intellectual and cognitive disabilities in humans. Clinically, it is essential to limit the progress of cognitive impairment after TBI. It is reported that diosmin has a neuroprotective effect that can limit the progress of the impairment. The aim of this study was to evaluate the effects of diosmin on neurological score, memory, tumor necrosis factor-α (TNF-α) level and long-term potentiation in hippocampal dentate gyrus after the injury...
September 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28722093/-a-multicenter-randomized-controlled-trial-of-wheat-cellulose-particles-in-the-treatment-of-internal-hemorrhoids
#17
Yunhua Peng, Wei Yang, Yehuang Wang, Xiaohua Fan, Xueping Zheng, Juanjuan Gai
OBJECTIVE: To evaluate the efficacy and safety of wheat cellulose particles (testa triticum tricum purify, Fiberform) in the treatment of internal hemorrhoid. METHODS: A multicenter randomized controlled clinical trial was adopted. From October 2015 to July 2016, 60 patients with internal hemorrhoid were enrolled from three medical centers, including Department of Anorectum, Shuguang Hospital of Shanghai University of Traditional Chinese Medicine, Department of Anorectum, The Third Affiliated Hospital of Nanjing University of Chinese Medicine, Department of Anorectum, The Second Affiliated Hospital of Guangzhou University of Chinese Medicine...
July 25, 2017: Zhonghua Wei Chang Wai Ke za Zhi, Chinese Journal of Gastrointestinal Surgery
https://www.readbyqxmd.com/read/28665324/diosmin-a-citrus-nutrient-activates-imidazoline-receptors-to-alleviate-blood-glucose-and-lipids-in-type-1-like-diabetic-rats
#18
Chia-Chen Hsu, Mang Hung Lin, Juei-Tang Cheng, Ming Chang Wu
Diosmin is a nutrient that is widely contained in citrus and that has been indicated to improve glucose metabolism in diabetic disorders. Recently, we demonstrated that diosmin induces β-endorphin to lower hyperglycemia in diabetic rats. However, the mechanisms of diosmin in opioid secretion were unclear. Therefore, we focused on the secretion of opioids from isolated adrenal glands induced by diosmin. The changes in the released β-endorphin-like immunoreactivity (BER) were determined using ELISA. Diosmin increased the BER level in a dose-dependent manner, and this effect was markedly reduced in the absence of calcium ions...
June 30, 2017: Nutrients
https://www.readbyqxmd.com/read/28663085/spectroscopic-and-structural-studies-of-the-diosmin-monohydrate-and-anhydrous-diosmin
#19
Łukasz Szeleszczuk, Dariusz Maciej Pisklak, Monika Zielińska-Pisklak, Iwona Wawer
Diosmin, a flavone glycoside frequently used in therapy of various veins diseases in monohydrate form, exhibits poor solubility in water and low bioavailability. Due to the fact that the anhydrous forms of drugs generally have better bioavailability than the corresponding hydrates, the aim of this study was to analyze the conversion of diosmin monohydrate (DSNM) to anhydrous diosmin (DSNA) that occurs upon heating. The mechanism of this transformation was examined as well as advanced structural studies of each form were performed using 13C CP/MAS SSNMR, DSC, FT-IR and PXRD techniques...
June 27, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28627244/a-comparative-study-of-mentha-arvensis-l-and-mentha-haplocalyx-briq-by-hplc
#20
Bing Tian Zhao, Tae In Kim, Young Ho Kim, Jong Seong Kang, Byung Sun Min, Jong Keun Son, Mi Hee Woo
We have developed a new method to simultaneously determine five marker compounds in Menthae Herba via HPLC/PDA - including hesperidin (1), rosmarinic acid (2), diosmin (3), didymin (4) and buddleoside (5). The newly developed method was successfully used to analyse for two species (Mentha arvensis L. and Mentha haplocalyx Briq.) of Menthae Herba, and the satisfactory results were obtained from the validation of developed method. The pattern analysis could greatly discriminate between M. arvensis L. and M. haplocalyx Briq...
June 18, 2017: Natural Product Research
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