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Silibinin

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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
#1
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
#2
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
#3
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
#4
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
#5
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
#6
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
#7
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
#8
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
#9
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
#10
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
#11
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
#12
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
#13
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
https://www.readbyqxmd.com/read/27822066/inhibitory-effects-of-silibinin-on-proliferation-and-lung-metastasis-of-human-high-metastasis-cell-line-of-salivary-gland-adenoid-cystic-carcinoma-via-autophagy-induction
#14
Canhua Jiang, Shufang Jin, Zhisheng Jiang, Jie Wang
OBJECTIVE: To investigate the possible mechanisms and effects of silibinin (SIL) on the proliferation and lung metastasis of human lung high metastasis cell line of salivary gland adenoid cystic carcinoma (ACC-M). METHODS: A methyl thiazolyl tetrazolium assay was performed to detect the inhibitory effects of SIL on the proliferation of ACC-M cells in vitro. Fluorescence microscopy and transmission electron microscopy were used to observe the autophagic process. Western blot was performed to detect the expression of microtube-related protein 1 light-chain 3 (LC3)...
2016: OncoTargets and Therapy
https://www.readbyqxmd.com/read/27753543/stat3-targeted-treatment-with-silibinin-overcomes-the-acquired-resistance-to-crizotinib-in-alk-rearranged-lung-cancer
#15
Elisabet Cuyàs, Almudena Pérez-Sánchez, Vicente Micol, Javier A Menendez, Joaquim Bosch-Barrera
The signal transducer and activator of transcription 3 (STAT3) has been suggested to play a prominent role in mediating non-small-cell lung cancer (NSCLC) resistance to some tyrosine kinase inhibitor (TKI)-mediated therapies. Using a model of anaplastic lymphoma kinase gene (ALK)-translocated NSCLC with acquired resistance to the ALK TKI crizotinib, but lacking amplifications or mutations in the kinase domain of ALK, we herein present evidence that STAT3 activation is a novel mechanism of crizotinib resistance that involves the upregulation of immune escape and epithelial to mesenchymal transition (EMT) signaling pathways...
December 16, 2016: Cell Cycle
https://www.readbyqxmd.com/read/27746612/silibinin-inhibits-proliferation-and-migration-of-human-hepatic-stellate-lx-2-cells
#16
Devaraj Ezhilarasan, Jonathan Evraerts, Sid Brice, Pedro Buc-Calderon, Sivanesan Karthikeyan, Etienne Sokal, Mustapha Najimi
BACKGROUND: Proliferation of hepatic stellate cells (HSCs) play pivotal role in the progression of hepatic fibrosis consequent to chronic liver injury. Silibinin (SBN), a flavonoid compound, has shown to possess cell cycle arresting potential against many actively proliferating cancers cell lines. The objective of this study was to evaluate the anti-proliferative and cell cycle arresting properties of SBN in rapidly proliferating human hepatic stellate LX-2 cell line. METHODS: LX-2 cells were fed with culture medium supplemented with different concentrations of SBN (10, 50 and 100 μM)...
September 2016: Journal of Clinical and Experimental Hepatology
https://www.readbyqxmd.com/read/27729375/role-of-p53-in-silibinin-mediated-inhibition-of-ultraviolet-b-radiation-induced-dna-damage-inflammation-and-skin-carcinogenesis
#17
Cynthia M Rigby, Srirupa Roy, Gagan Deep, Ruth Guillermo-Lagae, Anil K Jain, Deepanshi Dhar, David J Orlicky, Chapla Agarwal, Rajesh Agarwal
Non-melanoma skin cancers (NMSC) are a growing problem given that solar ultraviolet B (UVB) radiation exposure is increasing most likely due to depletion of the atmospheric ozone layer and lack of adequate sun protection. Better preventive methods are urgently required to reduce UV-caused photodamage and NMSC incidence. Earlier, we have reported that silibinin treatment activates p53 and reduces photodamage and NMSC, both in vitro and in vivo; but whether silibinin exerts its protective effects primarily through p53 remains unknown...
January 2017: Carcinogenesis
https://www.readbyqxmd.com/read/27695272/wound-healing-activity-of-silibinin-in-mice
#18
Rojalini Samanta, Ashok K Pattnaik, Kishanta K Pradhan, Beena K Mehta, Shakti P Pattanayak, Sugato Banerjee
BACKGROUND: Silibinin is a semi-purified fraction of silymarin contained in milk thistle (Silybum marianum Asteraceae). Primarily known for its hepatoprotective actions, silymarin may also stimulate epithelialization and reduce inflammation in excision wound. Previous studies show antioxidant, anti-inflammatory, and antimicrobial actions of silibinin. However, wound healing property of silibinin is not well studied. OBJECTIVE: This study investigates wound healing activity of silibinin topical formulation...
October 2016: Pharmacognosy Research
https://www.readbyqxmd.com/read/27685914/inhibitory-effects-of-silibinin-combined-with-doxorubicin-in-hepatocellular-carcinoma-an-in-vivo-study
#19
Wei-Guo Li, He-Qun Wang
PURPOSE: Hepatocellular carcinoma (HCC) is the one of the most common cancers and the third leading cause of cancer related mortality in the world. Unacceptable side effect and development of treatment resistance are the major concerns with the conventional chemotherapeutic agents. Combination therapy using phytotherapeutic agents is attracting the attention of investigators in view of the current needs. METHODS: In the present study we have evaluated the synergistic effect of silibinin, a nontoxic phytotherapeutic agent in combination with doxorubicin, in advanced HCC using HEPG2 cells and an orthotopic rat model of HCC...
July 2016: Journal of B.U.ON.: Official Journal of the Balkan Union of Oncology
https://www.readbyqxmd.com/read/27644625/preparation-characterization-and-cytotoxicity-of-silibinin-containing-nanoniosomes-in-t47d-human-breast-carcinoma-cells
#20
Boshra Amiri, Meysam Ebrahimi-Far, Zahra Saffari, Azim Akbarzadeh, Esmaeil Soleimani, Mohsen Chiani
BACKGROUND: Breast cancer is one of the most frequent cancer types within female populations. Silibinin is a chemotherapeutic agent active against cancer. Niosomes are biodegradable, biocompatible, safe and effective carriers for drug delivery. OBJECTIVE: To prepare nanoniosomal silibinin and evaluate its cytotoxicity in the T-47D breast cancer cell line. MATERIALS AND METHODS: Niosomes were prepared by reverse phase evaporation of a mixture of span 20, silibinin, PEG-2000 and cholesterol in chloroform and methanol solvent (1:2 v/v)...
2016: Asian Pacific Journal of Cancer Prevention: APJCP
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