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Silibinin

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https://www.readbyqxmd.com/read/28192136/inhibition-of-glycation-and-aldose-reductase-activity-using-dietary-flavonoids-a-lens-organ-culture-studies
#1
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/28164196/preventive-effect-of-silibinin-in-combination-with-pu-erh-tea-extract-on-non-alcoholic-fatty-liver-disease-in-ob-ob-mice
#2
Wen-Yi Hu, Xiao-Hui Ma, Wang-Yi Zhou, Xin-Xin Li, Ting-Ting Sun, He Sun
There are presently no miracle drugs for non-alcoholic fatty liver disease (NAFLD). This study investigates the synergistic effect of Silibinin combined with Pu-erh tea extract (PTE) against NAFLD and explores the suggested mechanism of action. Ob/ob mice were fed a high fat diet along with the oral administration of Silibinin (86 mg per kg per day), PTE (250 mg per kg per day) or their combination for 6 weeks. Their lean littermates who were fed with standard chow diet were used as the control group. The blood biochemical index and histopathological evaluation were analyzed...
February 6, 2017: Food & Function
https://www.readbyqxmd.com/read/28128564/using-affinity-to-provide-long-term-delivery-of-antiangiogenic-drugs-in-cancer-therapy
#3
Edgardo Rivera-Delgado, Horst A von Recum
Antiangiogenic drugs encompass many of the different cancer drugs currently under clinical investigation. One of the drawbacks of antiangiogenic therapy, though, is that upon cessation of drug treatment tumors can recur with an accelerated growth rate. In this study we investigate the capacity of using affinity interactions between a polymer made from cyclodextrin and four antiangiogenic drugs, tranilast, SU5416, 2-methoxyestradiol, and silibinin, with the ultimate goal of creating delivery profiles on the order of antiangiogenic processes (needing weeks, rather than hours of delivery)...
February 9, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28124212/skin-delivery-of-egcg-and-silibinin-potential-of-peptide-dendrimers-for-enhanced-skin-permeation-and-deposition
#4
Pallavi Krishna Shetty, Jyothsna Manikkath, Karnaker Tupally, Ganesh Kokil, Aswathi R Hegde, Sushil Y Raut, Harendra S Parekh, Srinivas Mutalik
The aim of the present study was to evaluate the ability of the peptide dendrimers to facilitate transdermal delivery of antioxidants, silibinin, and epigallocatechin-3-gallate (EGCG). Drug-peptide dendrimer complexes were prepared and evaluated for their ability to permeate across the skin. The data revealed the ready formation of complexes between drug and peptide dendrimer in a molar ratio of 1:1. In vitro permeation studies using excised rat skin and drug-peptide dendrimer complexes showed highest values for cumulative drug permeation at the end of 12 h (Q12), with corresponding permeability coefficient (Kp) and enhancement ratio values also determined at this time point...
January 25, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28120452/silibinin-treatment-inhibits-the-growth-of-hedgehog-inhibitor-resistant-basal-cell-carcinoma-cells-via-targeting-egfr-mapk-akt-and-hedgehog-signaling
#5
Arpit Dheeraj, Cynthia M Rigby, Cindy L O'Bryant, Chapla Agarwal, Rana P Singh, Gagan Deep, Rajesh Agarwal
Basal cell carcinoma (BCC) is the most common skin malignancy. Deregulated hedgehog signaling plays a central role in BCC development; therefore hedgehog inhibitors have been approved to treat locally advanced or metastatic BCC. However, the development of resistance to hedgehog inhibitors is the major challenge in effective treatment of this disease. Herein, we evaluated the efficacy of a natural agent silibinin to overcome resistance with hedgehog inhibitors (Sant-1 and GDC-0449) in BCC cells. Silibinin (25-100 μM) treatment for 48 hrs strongly inhibited growth and induced death in ASZ001, Sant-1 resistant (ASZ001-Sant-1) and GDC-0449 resistant (ASZ001-GDC-0449) BCC cells...
January 25, 2017: Photochemistry and Photobiology
https://www.readbyqxmd.com/read/28119262/silibinin-induces-hepatic-stellate-cell-cycle-arrest-via-enhancing-p53-p27-and-inhibiting-akt-downstream-signaling-protein-expression
#6
Devaraj Ezhilarasan, Jonathan Evraerts, Brice Sid, Pedro Buc Calderon, Sivanesan Karthikeyan, Etienne Sokal, Mustapha Najimi
BACKGROUND: Proliferation of hepatic stellate cells (HSCs) plays a pivotal role in the progression of liver fibrosis consequent to chronic liver injury. Silibinin, a flavonoid compound, has been shown to possess anti-fibrogenic effects in animal models of liver fibrosis. This was attributed to an inhibition of cell proliferation of activated HSCs. The present study was to gain insight into the molecular pathways involved in silibinin anti-fibrogenic effect. METHODS: The study was conducted on LX-2 human stellate cells treated with three concentrations of silibinin (10, 50 and 100 μmol/L) for 24 and 96 hours...
February 2017: Hepatobiliary & Pancreatic Diseases International: HBPD INT
https://www.readbyqxmd.com/read/28118130/development-of-a-terbium-sensitized-fluorescence-method-for-analysis-of-silibinin
#7
Saba Ershadi, Abolghasem Jouyban, Ommoleila Molavi, Ali Shayanfar
Silibinin is a natural flavonoid with potent anticancer properties, as shown in both in vitro and in vivo experiments.Various methods have been used for silibinin analysis. Terbium-sensitized fluorescence methods have been widely used for the determination of drugs in pharmaceutical preparations and biological samples in recent years. The present work is aimed at providing a simple analytical method for the quantitative determination of silibinin in aqueous solutions based on the formation of a fluorescent complex with terbium ion...
December 17, 2016: Journal of AOAC International
https://www.readbyqxmd.com/read/28078954/nanovesicle-delivery-to-the-liver-via-retinol-binding-protein-and-platelet-derived-growth-factor-receptors-how-targeting-ligands-affect-biodistribution
#8
Ching-Yun Hsu, Chun-Han Chen, Ibrahim A Aljuffali, You-Shan Dai, Jia-You Fang
AIM: Nanovesicles (NVs) conjugating ligands can deliver to the specific nidus. We designed a nanosystem targeting the injectable niosomes to liver for examining biodistribution. METHODOLOGY: Vitamin A and antiplatelet-derived growth factor receptor antibody were employed as the ligands to be taken by hepatic stellate cells. The biodistribution in rats was visualized by bioimaging. RESULTS: A significant liver accumulation was detected for antibody-embedded NVs at 2 h after dosing...
January 12, 2017: Nanomedicine
https://www.readbyqxmd.com/read/28078913/silibinin-loaded-magnetic-nanoparticles-inhibit-htert-gene-expression-and-proliferation-of-lung-cancer-cells
#9
Soumaye Amirsaadat, Younes Pilehvar-Soltanahmadi, Faraz Zarghami, Shahriar Alipour, Zohreh Ebrahimnezhad, Nosratollah Zarghami
Nanoparticle-based targeted drug delivery has the potential for rendering silibinin specifically at the favorite site using an external magnetic field. Also, it can circumvent the pitfalls of poor solubility. For this purpose, silibinin-loaded magnetic nanoparticles are fabricated, characterized and evaluated cytotoxicity and hTERT gene expression in A549 lung cancer cell line. silibinin-loaded PLGA-PEG-Fe3O4 had dose- and time-dependent cytotoxicity than pure silibinin. Additionally, hTERT expression is more efficiently reduced with increasing concentrations of nanosilibinin than pure silibinin...
January 12, 2017: Artificial Cells, Nanomedicine, and Biotechnology
https://www.readbyqxmd.com/read/28042859/a-novel-role-of-silibinin-as-a-putative-epigenetic-modulator-in-human-prostate-carcinoma
#10
Ioannis Anestopoulos, Aristeidis P Sfakianos, Rodrigo Franco, Katerina Chlichlia, Mihalis I Panayiotidis, David J Kroll, Aglaia Pappa
Silibinin, extracted from milk thistle (Silybum marianum L.), has exhibited considerable preclinical activity against prostate carcinoma. Its antitumor and chemopreventive activities have been associated with diverse effects on cell cycle, apoptosis, and receptor-dependent mitogenic signaling pathways. Here we hypothesized that silibinin's pleiotropic effects may reflect its interference with epigenetic mechanisms in human prostate cancer cells. More specifically, we have demonstrated that silibinin reduces gene expression levels of the Polycomb Repressive Complex 2 (PRC2) members Enhancer of Zeste Homolog 2 (EZH2), Suppressor of Zeste Homolog 12 (SUZ12), and Embryonic Ectoderm Development (EED) in DU145 and PC3 human prostate cancer cells, as evidenced by Real Time Polymerase Chain Reaction (RT-PCR)...
December 31, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28030611/silibinin-inhibits-platelet-derived-growth-factor-driven-cell-proliferation-via-downregulation-of-n-glycosylation-in-human-tenon-s-fibroblasts-in-a-proteasome-dependent-manner
#11
Yi-Hao Chen, Ching-Long Chen, Da-Wen Lu, Chang-Min Liang, Ming-Cheng Tai, Jiann-Torng Chen
The objective of this study was to evaluate the effects of silibinin on cell proliferation in platelet-derived growth factor (PDGF)-treated human Tenon's fibroblasts (HTFs). The effect of silibinin on cell proliferation in PDGF-treated HTFs was determined by examining the expression of proliferating cell nuclear antigen (PCNA) and performing WST-1 assays. Cell cycle progression was evaluated using flow cytometry. The related cyclins and cyclin-dependent kinases (CDKs) were also analyzed using western blot. A modified rat trabeculectomy model was established to evaluate the effect of silibinin on cell proliferation in vivo...
2016: PloS One
https://www.readbyqxmd.com/read/28028386/in-vitro-drug-release-characteristic-and-cytotoxic-activity-of-silibinin-loaded-single-walled-carbon-nanotubes-functionalized-with-biocompatible-polymers
#12
Julia Meihua Tan, Govindarajan Karthivashan, Shafinaz Abd Gani, Sharida Fakurazi, Mohd Zobir Hussein
In this paper, we demonstrate the preparation of silibinin-loaded carbon nanotubes (SWSB) with surface coating agents via non-covalent approach as an effective drug delivery system. The resulting surface-coated SWSB nanocomposites are extensively characterized by Fourier transform infrared (FTIR) and Raman spectroscopies, ultraviolet-visible (UV-Vis) spectrometry and field emission scanning electron microscopy (FESEM). The FTIR and Raman studies show that an additional layer is formed by these coating agents in the prepared nanocomposites during the coating treatment and these results are confirmed by FESEM...
2016: Chemistry Central Journal
https://www.readbyqxmd.com/read/28027688/silibinin-sensitizes-chemo-resistant-breast-cancer-cells-to-chemotherapy
#13
Ommoleila Molavi, Farzaneh Narimani, Farshid Asiaee, Simin Sharifi, Vahideh Tarhriz, Ali Shayanfar, Mohammadsaied Hejazi, Raymond Lai
CONTEXT: Multiple drug resistance is the major obstacle to conventional chemotherapy. Silibinin, a nontoxic naturally occurring compound, has anticancer activity and can increase the cytotoxic effects of chemotherapy in various cancer models. OBJECTIVE: To evaluate the effects of silibinin on enhancing the sensitivity of chemo-resistant human breast cell lines to doxorubicin (DOX) and paclitaxel (PAC). MATERIALS AND METHODS: The cells were treated with silibinin (at 50 to 600 μM concentrations) and/or chemo drugs for 24 and 48 h, then cell viability and changes in oncogenic proteins were determined by MTT assay and Western blotting/RT-PCR, respectively...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/28006905/silychristin-skeletal-alterations-and-biological-activities
#14
David Biedermann, Martin Buchta, Veronika Holečková, David Sedlák, Kateřina Valentová, Josef Cvačka, Lucie Bednárová, Alena Křenková, Marek Kuzma, Ctibor Škuta, Žaneta Peikerová, Petr Bartůněk, Vladimír Křen
Silychristin is the second most abundant flavonolignan (after silybin) present in the fruits of Silybum marianum. A group of compounds containing silychristin (3) and its derivatives such as 2,3-dehydrosilychristin (4), 2,3-dehydroanhydrosilychristin (5), anhydrosilychristin (6), silyhermin (7), and isosilychristin (8) were studied. Physicochemical data of these compounds acquired at high resolution were compared. The absolute configuration of silyhermin (7) was proposed to be identical to silychristin A (3a) in ring D (10R,11S)...
December 23, 2016: Journal of Natural Products
https://www.readbyqxmd.com/read/28004303/silibinin-ameliorates-a%C3%AE-25-35-induced-memory-deficits-in-rats-by-modulating-autophagy-and-attenuating-neuroinflammation-as-well-as-oxidative-stress
#15
Xiaoyu Song, Biao Zhou, Lingyu Cui, Di Lei, Pingping Zhang, Guodong Yao, Mingyu Xia, Toshihiko Hayashi, Shunji Hattori, Yuko Ushiki-Kaku, Shin-Ichi Tashiro, Satoshi Onodera, Takashi Ikejima
Alzheimer's disease (AD) is a progressive, neurodegenerative disease. Accumulating evidence suggests that inflammatory response, oxidative stress and autophagy are involved in amyloid β (Aβ)-induced memory deficits. Silibinin (silybin), a flavonoid derived from the herb milk thistle, is well known for its hepatoprotective activities. In this study, we investigated the neuroprotective effect of silibinin on Aβ25-35-injected rats. Results demonstrated that silibinin significantly attenuated Aβ25-35-induced memory deficits in Morris water maze and novel object-recognition tests...
December 22, 2016: Neurochemical Research
https://www.readbyqxmd.com/read/27910775/hepatoprotective-effects-and-mechanisms-of-action-of-triterpenoids-from-lingzhi-or-reishi-medicinal-mushroom-ganoderma-lucidum-agaricomycetes-on-%C3%AE-amanitin-induced-liver-injury-in-mice
#16
Huihui Wu, Shanshan Tang, Zhaoqin Huang, Qian Zhou, Ping Zhang, Zuohong Chen
Most fatal mushroom poisonings are caused by species of the genus Amanita; the amatoxins are responsible for acute liver failure and death in humans. Ganoderma lucidum is a well-known traditional medicinal mushroom that has been shown to have obvious hepatoprotective effects. This study evaluated the hepatoprotective effects of triterpenoids from G. lucidum on liver injury induced by a-amanitin (α-AMA) in mice and the mechanisms of action of these triterpenoids, including radical scavenging and antiapoptosis activities...
2016: International Journal of Medicinal Mushrooms
https://www.readbyqxmd.com/read/27909727/anti%C3%A2-proliferative-activity-of-epigallocatechin%C3%A2-3%C3%A2-gallate-and-silibinin-on-soft-tissue-sarcoma-cells
#17
Kamran Harati, Björn Behr, Christoph Wallner, Adrien Daigeler, Tobias Hirsch, Frank Jacobsen, Marcus Renner, Ali Harati, Marcus Lehnhardt, Mustafa Becerikli
Disseminated soft tissue sarcomas (STS) present a therapeutic dilemma. The first-line cytostatic doxorubicin demonstrates a response rate of 30% and is not suitable for elderly patients with underlying cardiac disease, due to its cardiotoxicity. Well‑tolerated alternative treatment options, particularly in palliative situations, are rare. Therefore, the present study assessed the anti‑proliferative effects of the natural compounds epigallocatechin-3-gallate (EGCG), silibinin and noscapine on STS cells. A total of eight different human STS cell lines were used in the study: Fibrosarcoma (HT1080), liposarcoma (SW872, T778 and MLS‑402), synovial sarcoma (SW982, SYO1 and 1273) and pleomorphic sarcoma (U2197)...
January 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/27871793/combining-in-silico-and-in-vitro-approaches-to-evaluate-the-acetylcholinesterase-inhibitory-profile-of-some-commercially-available-flavonoids-in-the-management-of-alzheimer-s-disease
#18
Asokkumar Kuppusamy, Madeswaran Arumugam, Sonia George
The current objective of the study is to identify inhibitory affinity potential of the certain commercially available flavonoids, against crystal structure of acetylcholinesterase (AChE) enzyme using in silico and in vitro studies. The inhibitory profiles of the compounds have been compared with standard AChE inhibitor donepezil. In the docking studies, conformational site analysis and docking parameters like binding energy, inhibition constant and intermolecular energy were determined using AutoDock 4.2. Docking studies conducted with diosmin, silibinin, scopoletin, taxifolin and tricetin exhibited tight binding forces prevailing with the enzyme than between donepezil...
February 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/27867187/crosstalk-of-ros-rns-and-autophagy-in-silibinin-induced-apoptosis-of-mcf-7-human-breast-cancer-cells-in-vitro
#19
Nan Zheng, Lu Liu, Wei-Wei Liu, Fei Li, Toshihiko Hayashi, Shin-Ichi Tashiro, Satoshi Onodera, Takashi Ikejima
Reactive oxygen species (ROS) and reactive nitrogen species (RNS) play important roles in regulating cell survival and death. Silibinin is a natural polyphenolic flavonoid isolated from milk thistle with anti-tumor activities, but it was found to induce cytoprotective ROS/RNS in human breast cancer MCF-7 cells. Furthermore, treatment with silibinin down-regulates ERα expression in MCF-7 cells, and inducing both autophagy and apoptosis. In this study we explored the relationship between ER-associated pathways and RNS/ROS in MCF-7 cells...
November 21, 2016: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/27825919/formulation-and-evaluation-of-targeted-nanoparticles-for-breast-cancer-theranostic-system
#20
Pegah Dadras, Fatemeh Atyabi, Shiva Irani, Leila Ma'mani, Alireza Foroumadi, Zahra Hadavand Mirzaie, Marzieh Ebrahimi, R Dinarvand
Theranostic polymeric NPs developed for both cancer diagnosis and cancer therapy. This multifunctional polymeric vehicle was prepared by a single emulsion evaporation method, using carboxyl-terminated PLGA. LHRH as a targeting moiety, was conjugated to the surface of polymeric carrier by applying polyethylene glycol. The results indicated that the diameter of NPs was ~185.4±4.6nm as defined by DLS. The entrapment efficacy of docetaxel, silibinin, and SPIONs was 84.6±4.1%, 80.6±2.7%, and 77.9±4.3%, respectively...
January 15, 2017: European Journal of Pharmaceutical Sciences
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