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Silibinin

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https://www.readbyqxmd.com/read/28435252/polyphenol-nanoformulations-for-cancer-therapy-experimental-evidence-and-clinical-perspective
#1
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
#2
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
#3
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
#4
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
#5
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
#6
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
#7
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
#8
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...
March 5, 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
#9
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
#10
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
#11
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
#12
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
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
#13
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
#14
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
#15
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
#16
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 h 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
#17
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
#18
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
#19
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
#20
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
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