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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...
October 18, 2016: Cell Cycle
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
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 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 remain unknown...
October 11, 2016: Carcinogenesis
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
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
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
Dae Gyu Yun, Dong Gun Lee
Candida albicans is a common yeast that resides in the human body, but can occasionally cause systemic fungal infection, namely candidiasis. As this infection rate is gradually increasing, it is becoming a major problem to public health. Accordingly, we for the first time investigated the antifungal activity and mode of action of silibinin, a natural product extracted from Silybum marianum (milk thistle), against C. albicans. On treatment with 100μM silibinin, generation of reactive oxygen species (ROS) from mitochondria, which can cause yeast apoptosis via oxidative stress, was increased by 24...
September 14, 2016: International Journal of Biochemistry & Cell Biology
Mohammad Mahdi Ochi, Ghasem Amoabediny, Seyed Mahdi Rezayat, Azim Akbarzadeh, Bahman Ebrahimi
OBJECTIVE: This study aimed to evaluate a co-encapsulated pegylated nano-liposome system based on two herbal anti-tumor drugs, silibinin and glycyrrhizic acid, for delivery to a hepatocellular carcinoma (HCC) cell line (HepG2). MATERIALS AND METHODS: In this experimental study, co-encapsulated nano-liposomes by the thin layer film hydration method with HEPES buffer and sonication at 60% amplitude. Liposomes that co-encapsulated silibinin and glycyrrhizic acid were prepared with a specified molar ratio of dipalmitoylphosphatidylcholine (DPPC), cholesterol (CHOL), and methoxy-polyethylene glycol 2000 (PEG2000)-derived distearoyl phosphatidylethanolamine (mPEG2000-DSPE)...
July 2016: Cell Journal
Gagan Deep, Rahul Kumar, Dhanya K Nambiar, Anil K Jain, Anand M Ramteke, Natalie J Serkova, Chapla Agarwal, Rajesh Agarwal
Hypoxia is associated with aggressive phenotype and poor prognosis in prostate cancer (PCa) patients suggesting that PCa growth and progression could be controlled via targeting hypoxia-induced signaling and biological effects. Here, we analyzed silibinin (a natural flavonoid) efficacy to target cell growth, angiogenesis and metabolic changes in human PCa, LNCaP and 22Rv1 cells under hypoxic condition. Silibinin treatment inhibited the proliferation, clonogenicity and endothelial cells tube formation by hypoxic (1% O2 ) PCa cells...
August 17, 2016: Molecular Carcinogenesis
Olga M Palomino, Neire M Gouveia, Sonia Ramos, M Angeles Martín, Luis Goya
Silybum marianum Gaertn. (Milk thistle) has been used since ancient times for the relief of liver diseases characterized by intense oxidative stress such as inflammatory liver disease and cirrhosis. As oxidative stress by hyperglycemia is involved in micro- and macrovascular complications of type 2 diabetes, our aim was to assess the protective effect of milk thistle seed extract against oxidative stress induced by a high glucose concentration on endothelial cells (EA.hy926 cells). High-performance liquid chromatographic analysis shows flavonolignans silychristin and silibinin A and B as major components...
August 15, 2016: Planta Medica
Navaneethakrishnan Polachi, Guirong Bai, Tingyang Li, Yang Chu, Xiangyang Wang, Shuming Li, Ning Gu, Jiang Wu, Wei Li, Yanjun Zhang, Shuiping Zhou, He Sun, Changxiao Liu
Silibinin, a natural flavanone, derived from the milk thistle plant (Silybum marianum), was illustrated for several medicinal uses such as liver-protective, anti-oxidant, anti-cancer, anti-inflammation and many other. However, silibinin has poor absorbance and bioavailability due to low water solubility, thereby limiting its clinical applications and therapeutic efficiency. To overcome this problem, the combination of silibinin with phosphatidylcholine (PC) as a formulation was used to enhance the solubility and bioavailability...
November 10, 2016: European Journal of Medicinal Chemistry
Zhuo-Wei Shen, Meng-Yue Luo, Hai-Hong Hu, Hui Zhou, Hui-Di Jiang, Lu-Shan Yu, Su Zeng
NTCP is specifically expressed on the basolateral membrane of hepatocytes, participating in the enterohepatic circulation of bile salts, especially conjugated bile salts, to maintain bile salts homeostasis. In addition, recent studies have found that NTCP is a functional receptor of HBV and HDV. Therefore, it is important to study the interaction between drugs and NTCP and identify the inhibitors/substrates of NTCP. In the present study, a LLC-PK1 cell model stably expressing human NTCP was established, which was simple and suitable for high throughput screening, and utilized to screen and verify the potential inhibitors of NTCP from 102 herbal medicinal ingredients...
July 2016: Chinese Journal of Natural Medicines
Ramanathan Raghu, Sivanesan Karthikeyan
HIV/AIDS patients are more prone for opportunistic TB infections and they are administered the combined regimen of anti-retroviral drug zidovudine (AZT) and isoniazid (INH) for therapy. However, AZT+INH treatment has been documented to induce injury and remedial measures to prevent this adversity are not clearly defined. Silibinin (SBN) is a natural hepatoprotective principle isolated from medicinal plant Silybum marianum and is currently used for therapy of various liver diseases. This study investigate the hepatotoxic potentials of AZT alone, INH alone and AZT+INH treatments and the mitigating potentials of SBN against these drugs induced toxic insults of liver in rats...
September 2016: Environmental Toxicology and Pharmacology
Komal Raina, Sushil Kumar, Deepanshi Dhar, Rajesh Agarwal
Globally, the risk of colorectal cancer (CRC) as well as the incidence of mortality associated with CRC is increasing. Thus, it is imperative that we look at alternative approaches involving intake of non-toxic natural dietary/non-dietary agents, for the prevention of CRC. The ultimate goal of this approach is to reduce the incidence of pre-neoplastic adenomatous polyps and prevent their progression to more advanced forms of CRC, and use these natural agents as a safe intervention strategy during the clinical course of this deadly malignancy...
November 20, 2016: Journal of Biomedical Research
Riccardo Bertin, Zheng Chen, Raffaella Marin, Maddalena Donati, Angela Feltrinelli, Monica Montopoli, Sabina Zambon, Enzo Manzato, Guglielmina Froldi
Studies indicate that oxidative modifications of endothelium and LDL play a preeminent role in atherogenesis; therefore, the preservation of the endothelial antioxidant capacity and the inhibition of LDL oxidation by use of plant-derived compounds are an appealing strategy against several vascular disorders. On this basis, baicalein, eupatorin, galangin, magnolol, myricetin, oleuropein, silibinin and bilobalide were studied against various oxidative conditions. The radical scavenging capacity was analysed using DPPH and ORAC assays...
August 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Ji-Won Park, Na-Rae Shin, In-Sik Shin, Ok-Kyoung Kwon, Joong-Sun Kim, Sei-Ryang Oh, Jae-Hong Kim, Kyung-Seop Ahn
Silibinin, the main ingredient of silymarin, has been used as a traditional drug for over 2000 years to treat a range of liver diseases. Recent studies have also demonstrated that silibinin possesses antiinflammatory and anticancer properties. In the study, we researched the efficacy of silibinin on the development of COPD using a cigarette smoke (CS)-induced and lipopolysaccharide (LPS)-induced COPD model mice and stimulation of NCI-H292 cells with CS condensate. Silibinin was administered to mice by oral gavage 1 h before CS exposure for 10 days...
July 29, 2016: Phytotherapy Research: PTR
Ching-Hsuan Liu, Chun-Ching Lin, Wen-Chan Hsu, Chueh-Yao Chung, Chih-Chan Lin, Alagie Jassey, Shun-Pang Chang, Chen-Jei Tai, Cheng-Jeng Tai, Justin Shields, Christopher D Richardson, Ming-Hong Yen, D Lorne J Tyrrell, Liang-Tzung Lin
OBJECTIVE: Silibinin is a flavonolignan that is well established for its robust antiviral activity against HCV infection and has undergone several clinical trials for the management of hepatitis C. Despite its potency, silibinin suffers from poor solubility and bioavailability, restricting its clinical use. To overcome this limitation, we developed highly bioavailable silibinin nanoparticles (SB-NPs) and evaluated their efficiency against HCV infection. DESIGN: SB-NPs were prepared using a nanoemulsification technique and were physicochemically characterised...
July 19, 2016: Gut
Qian Xu, Wei Liu, Xiaoling Liu, Weiwei Liu, Hongju Wang, Guodong Yao, Linghe Zang, Toshihiko Hayashi, Shin-Ichi Tashiro, Satoshi Onodera, Takashi Ikejima
Primary cilium is a cellular antenna, signalling as a sensory organelle. Numerous pathological manifestation is associated with change of its length. Although the interaction between autophagy and primary cilia has been suggested, the role of autophagy in primary cilia length is largely unknown. In this study the primary cilia were immunostained and observed by using confocal fluorescence microscopy, and we found that silibinin, a natural flavonoid, shortened the length of primary cilia, meanwhile it also induced autophagy in 3T3-L1 cells...
September 2016: Molecular and Cellular Biochemistry
Jasmine Sati, Biraja Prasad Mohanty, Mohan Lal Garg, Ashwani Koul
Silibinin, a major bioactive flavonolignan in Silybum marianum, has received considerable attention in view of its anticarcinogenic activity. The present study examines its anticancer potential against 7, 12-dimethylbenz(a)anthracene (DMBA) and 12-O-tetradecanoylphorbol-13-acetate (TPA) induced skin cancer. Male LACA mice were randomly segregated into 4 groups: Control, DMBA/TPA, Silibinin and Silibinin+DMBA/TPA. Tumors in DMBA/TPA and Silibinin+DMBA/TPA groups were histologically graded as squamous cell carcinoma...
2016: PloS One
Sang-Hun Kim, Kwang-Youn Kim, Sun-Nyoung Yu, Young-Kyo Seo, Sung-Sik Chun, Hak-Sun Yu, Soon-Cheol Ahn
BACKGROUND: Silibinin, a biologically active compound of milk thistle, has chemopreventive effects on cancer cell lines. Recently it was reported that silibinin inhibited tumor growth through activation of the apoptotic signaling pathway. Although various evidences showed multiple signaling pathways of silibinin in apoptosis, there were no reports to address the clear mechanism of ROS-mediated pathway in prostate cancer PC-3 cells. Several studies suggested that reactive oxygen species (ROS) play an important role in various signaling cascades, but the primary source of ROS was currently unclear...
2016: BMC Cancer
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