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Silibinin

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https://www.readbyqxmd.com/read/28527127/evaluation-of-heparg-cells-for-the-assessment-of-indirect-drug-induced-hepatotoxicity-using-inh-as-a-model-substance
#1
Anika Mann, Thomas Pelz, Knut Rennert, Alexander Mosig, Michael Decker, Amelie Lupp
HepaRG cells are widely used as an in vitro model to assess drug-induced hepatotoxicity. However, only few studies exist so far regarding their suitability to detect the effects of drugs requiring a preceding activation via the cytochrome P450 (CYP) system. A prototypic substance is the anti-tuberculosis agent INH, which is metabolized into N-acetylhydrazine, which then triggers hepatotoxicity. Therefore, the aim of the present study was to test if this effect can also be detected in HepaRG cells and if it can be counteracted by the known hepatoprotectant silibinin...
May 19, 2017: Human Cell
https://www.readbyqxmd.com/read/28509572/effect-of-silibinin-loaded-nano-niosomal-coated-with-trimethyl-chitosan-on-mirnas-expression-in-2d-and-3d-models-of-t47d-breast-cancer-cell-line
#2
Seyede Elmira Yazdi Rouholamini, Saeid Moghassemi, Zahra Maharat, Amirhossien Hakamivala, Susan Kashanian, Kobra Omidfar
Silibinin is a natural flavonoid with a strong antioxidant property and weak cytotoxic activity. It has demonstrated anti-tumoural activity against many types of malignancies; however, due to its hydrophobic structure, it has poor water solubility, bioavailability and permeability across intestinal epithelial cells. To improve the effect of silibinin, we have vehiculated silibinin by a highly stable niosomal nanostructure based on a Span 60/cholesterol (CH)/N-trimethyl chitosan (TMC) system in order to study its potential application for the delivery of silibinin in T47D cultured under three-dimensional (3D) and two-dimensional (2D) conditions...
May 16, 2017: Artificial Cells, Nanomedicine, and Biotechnology
https://www.readbyqxmd.com/read/28483599/therapeutic-effects-of-silibinin-on-lps-induced-acute-lung-injury-by-inhibiting-nlrp3-and-nf-%C3%AE%C2%BAb-signaling-pathways
#3
Lin Tian, Weimin Li, Tan Wang
Silibinin, a natural product extracted from Silybum marianum (milk thistle), has been reported to have anti-inflammatory effect. The aim of this study was to explore the therapeutic effects and potential mechanisms of silibinin on lipopolysaccharide (LPS)-stimulated inflammatory responses in acute lung injury (ALI). Male BALB/c mice were conditioned with silibinin 1 h after intranasal instillation of LPS. After 12 h, the myeloperoxidase (MPO) level in lung tissues, the wet/dry (W/D) ratio, inflammatory cytokines in the bronchoalveolar lavage fluid (BALF), and histopathological examination of lung were detected...
May 5, 2017: Microbial Pathogenesis
https://www.readbyqxmd.com/read/28478747/creation-of-a-virtual-antidotes-network-between-pharmacy-departments-of-catalan-hospitals
#4
Raquel Aguilar-Salmerón, Edurne Fernández de Gamarra-Martínez, Milagros García-Peláez, Antoni Broto-Sumalla, Lidia Martínez-Sánchez, Santiago Nogué-Xarau
Objetive: To design a virtual antidote network between hospitals that could help to locate on-line those hospitals that stocked those antidotes with the highest difficulty in terms of availability, and ensured that the medication was loaned in case of necessity. METHODS: The application was developed by four hospital pharmacists and two clinical toxicologists with the support of a Healthcare Informatics Consultant Company. RESULTS: The antidotes network in Catalonia, Spain, was launched in July 2015...
May 1, 2017: Farmacia Hospitalaria
https://www.readbyqxmd.com/read/28470323/differential-%C3%AE-amylase-%C3%AE-glucosidase-inhibitory-activities-of-plant-derived-phenolic-compounds-a-virtual-screening-perspective-for-the-treatment-of-obesity-and-diabetes
#5
Hassan Rasouli, Seyed Mohammad-Bagher Hosseini-Ghazvini, Hadi Adibi, Reza Khodarahmi
Recently, due to their biological properties, polyphenol-rich functional foods have been proposed to be unique supplementary and nutraceutical treatments for diabetes mellitus. Inhibition of α-amylase and α-glucosidase enzymes using natural products (especially polyphenols) is a novel oral policy to regulate carbohydrate metabolism and hyperglycemia. The present study aims to evaluate the α-amylase and α-glucosidase inhibitory activity of 26 polyphenols using molecular docking and virtual screening studies...
May 4, 2017: Food & Function
https://www.readbyqxmd.com/read/28458011/chrysin-and-silibinin-sensitize-human-glioblastoma-cells-for-arsenic-trioxide
#6
Michael Gülden, Daniel Appel, Malin Syska, Stephanie Uecker, Franziska Wages, Hasso Seibert
Arsenic trioxide (ATO) is highly efficient in treating acute promyelocytic leukemia. Other malignancies, however, are often less sensitive. Searching for compounds sensitizing arsenic resistant tumours for ATO the plant polyphenols, chrysin and silibinin, and the ATP binding cassette (ABC) transporter inhibitor MK-571, respectively, were investigated in human glioblastoma A-172 cells. The sensitivity of A-172 cells to ATO was characterized by a median cytotoxic concentration of 6 μM ATO. Subcytotoxic concentrations of chrysin, silibinin and MK-571, respectively, remarkably increased the sensitivity of the cells to ATO by factors of 4-6...
April 27, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/28457856/the-effect-of-milk-thistle-silybum-marianum-and-its-main-flavonolignans-on-cyp2c8-enzyme-activity-in-human-liver-microsomes
#7
Ahmed A Albassam, Reginald F Frye, John S Markowitz
Milk thistle is a widely-consumed botanical used for an array of purported health benefits. The primary extract of milk thistle is termed silymarin, a complex mixture that contains a number of structurally-related flavonolignans, the flavonoid, taxifolin, and a number of other constituents. The major flavonolignans present in most extracts are silybin A, silybin B, isosilybin A and isosilybin B, silydianin, silychristin and isosilychristin. Silymarin itself has been reported to inhibit CYP2C8 activity in vitro, but the effect of the individual flavonolignans on this enzyme has not been studied...
June 1, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28440514/silibinin-downregulates-mmp2-expression-via-jak2-stat3-pathway-and-inhibits-the-migration-and-invasive-potential-in-mda-mb-231-cells
#8
Hyo Joo Byun, Pramod Darvin, Dong Young Kang, Nipin Sp, Youn Hee Joung, Jong Hwan Park, Sun Jin Kim, Young Mok Yang
Worldwide, breast cancer (BCa) is the most common cancer in women. Among its subtypes, triple-negative breast cancer (TNBC) is an aggressive form associated with diminished survival. TNBCs are characterized by their absence, or minimal expression, of the estrogen and progesterone receptors, as well as the human epidermal growth factor receptor 2 (i.e. ER-/-, PR-/-, Her2-/Low). Consequently, treatment for this subtype of BCa remains problematic. Silibinin, a derivative of the flavonoid silymarin, is reported to have anticancer activities against hepatic and non-small cell lung cancers...
April 19, 2017: Oncology Reports
https://www.readbyqxmd.com/read/28435252/polyphenol-nanoformulations-for-cancer-therapy-experimental-evidence-and-clinical-perspective
#9
REVIEW
Yasamin Davatgaran-Taghipour, Salar Masoomzadeh, Mohammad Hosein Farzaei, Roodabeh Bahramsoltani, Zahra Karimi-Soureh, Roja Rahimi, Mohammad Abdollahi
Cancer is defined as the abnormal cell growth that can cause life-threatening malignancies with high financial costs for patients as well as the health care system. Natural polyphenols have long been used for the prevention and treatment of several disorders due to their antioxidant, anti-inflammatory, cytotoxic, antineoplastic, and immunomodulatory effects discussed in the literature; thus, these phytochemicals are potentially able to act as chemopreventive and chemotherapeutic agents in different types of cancer...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28418711/silibinin-improves-tnf-%C3%AE-and-m30-expression-and-histological-parameters-in-rat-kidneys-after-hepatic-ischemia-reperfusion
#10
Georgios Kyriakopoulos, Alexandra K Tsaroucha, Georgia Valsami, Maria Lambropoulou, Nikolaos Kostomitsopoulos, Eirini Christodoulou, Zacharias Kakazanis, Constantinos Anagnostopoulos, Christos Tsalikidis, Constantinos E Simopoulos
BACKGROUND: Remote kidney damage is a sequel of hepatic ischemia-reperfusion (I/R) injury. Silibinin is the main ingredient of the milk thistle plant seed extract with known antioxidant and hepatoprotective activity. Our study investigates the nephroprotective potential of intravenously administered silibinin, as a lyophilized SLB-hydoxypropyl-beta-cyclodextrin product, in hepatic I/R injury. MATERIAL AND METHODS: 63 Wistar rats were divided into three groups: Sham (virtual intervention); Control (45 min ischemia and reperfusion); and Silibinin (200 μL intravenous silibinin administration after 45 min of ischemia)...
April 18, 2017: Journal of Investigative Surgery: the Official Journal of the Academy of Surgical Research
https://www.readbyqxmd.com/read/28401485/silymarin-and-its-active-component-silibinin-act-as-novel-therapeutic-alternatives-for-salivary-gland-cancer-by-targeting-the-erk1-2-bim-signaling-cascade
#11
Eun-Sun Choi, Sejun Oh, Boonsil Jang, Hyun-Ju Yu, Ji-Ae Shin, Nam-Pyo Cho, In-Hyoung Yang, Dong-Hoon Won, Hye-Jeong Kwon, Seong Doo Hong, Sung-Dae Cho
PURPOSE: Approximately 20% of all salivary gland cancer patients who are treated with current treatment modalities will ultimately develop metastases. Its most common form, mucoepidermoid carcinoma (MEC) is a highly aggressive tumor with an overall 5-year survival rate of ~30%. Until now, several chemotherapeutic drugs have been tested for the treatment of salivary gland tumors, but the results have been disappointing and the drugs often cause unwanted side effects. Therefore, several recent studies have focused on the potential of alternative and/or complementary therapeutic options, including the use of silymarin...
April 11, 2017: Cellular Oncology (Dordrecht)
https://www.readbyqxmd.com/read/28391184/thioredoxin-1-modulates-apoptosis-induced-by-bioactive-compounds-in-prostate-cancer-cells
#12
Aida Rodriguez-Garcia, David Hevia, Juan C Mayo, Pedro Gonzalez-Menendez, Lucia Coppo, Jun Lu, Arne Holmgren, Rosa M Sainz
Accumulating evidence suggests that natural bioactive compounds, alone or in combination with traditional chemotherapeutic agents, could be used as potential therapies to fight cancer. In this study, we employed four natural bioactive compounds (curcumin, resveratrol, melatonin, and silibinin) and studied their role in redox control and ability to promote apoptosis in androgen sensitive and insensitive prostate cancer cells. Here is shown that curcumin and resveratrol promote ROS production and induce apoptosis in LNCaP and PC-3...
March 31, 2017: Redox Biology
https://www.readbyqxmd.com/read/28376126/silibinin-treatment-prevents-endotoxin-induced-uveitis-in-rats-in-vivo-and-in-vitro
#13
Ching-Long Chen, Jiann-Torng Chen, Chang-Min Liang, Ming-Cheng Tai, Da-Wen Lu, Yi-Hao Chen
Uveitis, an intraocular inflammatory disease, occurs mostly in young people and can result in the loss of socioeconomic capabilities. Silibinin has been shown to exert anti-inflammatory effects in human retinal pigment epithelial (RPE) cells. The present study investigated the anti-inflammatory effect of silibinin pretreatment on endotoxin-induced uveitis (EIU) in rats and the mechanisms by which it exerts these effects. Uveitis was induced via injection of lipopolysaccharides (LPS) into Lewis rats. Twenty-four hours after the LPS injection, histological examination showed that silibinin decreased inflammatory cell infiltration in the anterior segment of the eyes of LPS-treated rats...
2017: PloS One
https://www.readbyqxmd.com/read/28365493/hydrogel-containing-silibinin-loaded-pomegranate-oil-based-nanocapsules-exhibits-anti-inflammatory-effects-on-skin-damage-uvb-radiation-induced-in-mice
#14
Marila Crivellaro Lay Marchiori, Cristina Rigon, Camila Camponogara, Sara Marchesan Oliveira, Letícia Cruz
The present study shows the development of a topical formulation (hydrogel) containing silibinin-loaded pomegranate oil based nanocapsules suspension and its evaluation as an alternative for the treatment of cutaneous UVB radiation-induced damages. For this, an animal model of skin injury induced by UVB radiation was employed. Gellan gum was used as gel forming agent by its direct addition to nanocapsules suspension. The hydrogels showed adequate pH values (5.6-5.9) and a silibinin content close to the theoretical value (1mg/g)...
March 23, 2017: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/28321778/effects-of-mir-21-downregulation-and-silibinin-treatment-in-breast-cancer-cell-lines
#15
Zohreh Jahanafrooz, Nasrin Motamed, Behnaz Bakhshandeh
Silibinin is a natural polyphenol with high antioxidant and anticancer properties, which causes cell cycle arrest and apoptosis in most cancer cell types including breast cancer, but the in-line mechanisms, are still unknown. Silibinin significantly downregulated oncomiR miR-21 expression in breast cancer cells. Here the effect of anti-miR-21 on cell viability, apoptotic induction, cell cycle distribution, and the expression levels of downstream targets of miR-21 were investigated in MCF-7 and T47D cells. MiR-21 mimic transfection was also applied in silibinin treated samples to evaluate functional role of miR-21downregulation on silibinin effects...
March 20, 2017: Cytotechnology
https://www.readbyqxmd.com/read/28273632/the-protective-effects-of-silibinin-in-the-treatment-of-streptozotocin-induced-diabetic-osteoporosis-in-rats
#16
Te Wang, Leyi Cai, Yangyang Wang, Qingqing Wang, Di Lu, Hua Chen, Xiaozhou Ying
Diabetic osteoporosis (DO) is a complication of diabetes mellitus. Our previous study showed that silibinin can attenuate high glucose mediated human bone marrow stem cells dysfunction through antioxidant effect. However, no study has yet investigated the effect of silibinin in diabetic rats. Therefore, we assessed the effects of silibinin on bone characteristics in streptozotocin-induced diabetic rats. The aim of our study was to determine whether providing silibinin in the different supplementation could prevent bone loss in diabetic rats or not...
May 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28250272/the-binding-of-silibinin-the-main-constituent-of-silymarin-to-site-i-on-human-serum-albumin
#17
Keishi Yamasaki, Hiroki Sato, Saori Minagoshi, Karin Kyubun, Makoto Anraku, Shigeyuki Miyamura, Hiroshi Watanabe, Kazuaki Taguchi, Hakaru Seo, Toru Maruyama, Masaki Otagiri
Silibinin is the main constituent of silymarin, an extract from the seeds of milk thistle (Silybum marianum). Because silibinin has many pharmacological activities, extending its clinical use in the treatment of a wider variety of diseases would be desirable. In this study, we report on the binding of silibinin to plasma proteins, an issue that has not previously been extensively studied. The findings indicated that silibinin mainly binds to human serum albumin (HSA). Mutual displacement experiments using ligands that primarily bind to sites I and II clearly revealed that silibinin binds tightly and selectively to site I (subsites Ia and/or Ic) of HSA, which is located in subdomain IIA...
2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28229968/cytotoxic-and-toxicogenomic-effects-of-silibinin-in-bladder-cancer-cells-with-different-tp53-status
#18
Daiane Teixeira DE Oliveira, Andre Luiz Ventura Savio, Joao Paulo DE Castro Marcondes, Tatiane Martins Barros, Ludmila Correia Barbosa, Daisy Maria Favero Salvadori, Glenda Nicioli DA Silva
Silibinin is a natural phenol found in the seeds of the milk thistle plant. Recent data have shown its effectiveness for preventing/treating bladder tumours. Therefore, in this study we investigated the cytotoxic and toxicogenetic activity of silibinin in bladder cancer cells with different TP53 statuses. Two bladder urothelial carcinoma cell lines were used: RT4 (wild-type TP53 gene) and T24 (mutated TP53 gene). Cell proliferation, clonogenic survival, apoptosis rates, genotoxicity and relative expression profile of FRAP/mTOR, FGFR3, AKT2 and DNMT1 genes and of miR100 and miR203 were evaluated...
March 2017: Journal of Biosciences
https://www.readbyqxmd.com/read/28223550/nadh-autofluorescence-a-new-metabolic-biomarker-for-cancer-stem-cells-identification-of-vitamin-c-and-cape-as-natural-products-targeting-stemness
#19
Gloria Bonuccelli, Ernestina Marianna De Francesco, Rianne de Boer, Herbert B Tanowitz, Michael P Lisanti
Here, we assembled a broad molecular "tool-kit" to interrogate the role of metabolic heterogeneity in the propagation of cancer stem-like cells (CSCs). First, we subjected MCF7 cells to "metabolic fractionation" by flow cytometry, using fluorescent mitochondrial probes to detect PCG1α activity, as well ROS and hydrogen-peroxide (H2O2) production; NADH levels were also monitored by auto-fluorescence. Then, the various cell populations were functionally assessed for "stem cell activity", using the mammosphere assay (3D-spheroids)...
March 28, 2017: Oncotarget
https://www.readbyqxmd.com/read/28192136/inhibition-of-glycation-and-aldose-reductase-activity-using-dietary-flavonoids-a-lens-organ-culture-studies
#20
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...
May 2017: International Journal of Biological Macromolecules
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