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Withaferin A

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https://www.readbyqxmd.com/read/29194609/using-the-connectivity-map-to-discover-compounds-influencing-human-osteoblast-differentiation
#1
A M Brum, J van de Peppel, L Nguyen, A Aliev, M Schreuders-Koedam, T V Gajadien, C S van der Leije, A van Kerkwijk, M Eijken, J P T M van Leeuwen, B C J van der Eerden
Osteoporosis is a common skeletal disorder characterized by low bone mass leading to increased bone fragility and fracture susceptibility. Identification of factors influencing osteoblast differentiation and bone formation is very important. Previously, we identified parbendazole to be a novel compound that stimulates osteogenic differentiation of human mesenchymal stromal cells (hMSCs), using gene expression profiling and bioinformatic analyses, including the Connectivity Map (CMap), as an in-silico approach...
December 1, 2017: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/29165314/towards-natural-mimetics-of-metformin-and-rapamycin
#2
Alexander Aliper, Leslie Jellen, Franco Cortese, Artem Artemov, Darla Karpinsky-Semper, Alexey Moskalev, Andrew G Swick, Alex Zhavoronkov
Aging is now at the forefront of major challenges faced globally, creating an immediate need for safe, widescale interventions to reduce the burden of chronic disease and extend human healthspan. Metformin and rapamycin are two FDA-approved mTOR inhibitors proposed for this purpose, exhibiting significant anti-cancer and anti-aging properties beyond their current clinical applications. However, each faces issues with approval for off-label, prophylactic use due to adverse effects. Here, we initiate an effort to identify nutraceuticals-safer, naturally-occurring compounds-that mimic the anti-aging effects of metformin and rapamycin without adverse effects...
November 15, 2017: Aging
https://www.readbyqxmd.com/read/29157955/development-of-a-goat-model-for-evaluation-of-withaferin-a-cervical-implants-for-the-treatment-of-cervical-intraepithelial-neoplasia
#3
Leslie C Sherwood, Farrukh Aqil, Manicka V Vadhanam, Jeyaprakash Jeyabalan, Radha Munagala, David Hoetker, Sanjay Srivastava, Inder P Singh, Scott Cambron, Martin O'Toole, Wendy Spencer, Lynn P Parker, Ramesh C Gupta
Cervical cancer is caused by human papillomavirus (HPV). The disease develops over many years through a series of precancerous lesions. Cervical cancer can be prevented by HPV-vaccination, screening and treatment of precancer before development of cervical cancer. The treatment of high-grade cervical dysplasia (CIN(2+)) has traditionally been by cervical conization. Surgical procedures are associated with increased risk of undesirable side effects including bleeding, infection, scarring (stenosis), infertility and complications in later pregnancies...
November 17, 2017: Experimental and Molecular Pathology
https://www.readbyqxmd.com/read/29149589/bond-with-me-if-you-can-natural-product-covalent-ligand-and-reactivity-based-probe-compete-for-cysteine-in-pp2a-complex
#4
Douglas S Johnson, Jaimeen D Majmudar
In this issue of Cell Chemical Biology, Grossman et al. (2017) disclose a chemoproteomics-enabled strategy to identify the cysteine-reactive target(s) of the anti-cancer natural product withaferin A and then screen a cysteine-reactive fragment library to discover a covalent ligand for the same target.
November 16, 2017: Cell Chemical Biology
https://www.readbyqxmd.com/read/29142430/topical-delivery-of-withania-somnifera-crude-extracts-in-niosomes-and-solid-lipid-nanoparticles
#5
Tawona N Chinembiri, Minja Gerber, Lissinda H du Plessis, Jan L du Preez, Josias H Hamman, Jeanetta du Plessis
Background: Withania somnifera is a medicinal plant native to India and is known to have anticancer properties. It has been investigated for its anti-melanoma properties, and since melanoma presents on the skin, it is prudent to probe the use of W. somnifera in topical formulations. To enhance topical drug delivery and to allow for controlled release, the use of niosomes and solid lipid nanoparticles (SLNs) as delivery vesicles were explored. Objective: The objective of this study is to determine the stability and topical delivery of W...
October 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/29100399/oxidative-stress-induced-jnk-ap-1-signaling-is-a-major-pathway-involved-in-selective-apoptosis-of-myelodysplastic-syndrome-cells-by-withaferin-a
#6
Karine Z Oben, Sara S Alhakeem, Mary K McKenna, Jason A Brandon, Rajeswaran Mani, Sunil K Noothi, Liu Jinpeng, Shailaja Akunuru, Sanjit K Dhar, Inder P Singh, Ying Liang, Chi Wang, Ahmed Abdel-Latif, Harold F Stills, Daret K St Clair, Hartmut Geiger, Natarajan Muthusamy, Kaoru Tohyama, Ramesh C Gupta, Subbarao Bondada
Myelodysplastic syndromes (MDS) are a diverse group of malignant clonal hematopoietic stem cell disorders characterized by ineffective hematopoiesis, dysplastic cell morphology in one or more hematopoietic lineages, and a risk of progression to acute myeloid leukemia (AML). Approximately 50% of MDS patients respond to current FDA-approved drug therapies but a majority of responders relapse within 2-3 years. There is therefore a compelling need to identify potential new therapies for MDS treatment. We utilized the MDS-L cell line to investigate the anticancer potential and mechanisms of action of a plant-derived compound, Withaferin A (WFA), in MDS...
September 29, 2017: Oncotarget
https://www.readbyqxmd.com/read/29062040/regiospecific-synthesis-of-ring-a-fused-withaferin-a-isoxazoline-analogues-induction-of-premature-senescence-by-w-2b-in-proliferating-cancer-cells
#7
Faheem Rasool, Debasis Nayak, Archana Katoch, Mir Mohd Faheem, Syed Khalid Yousuf, Nazar Hussain, Chetan Belawal, N K Satti, Anindya Goswami, Debaraj Mukherjee
Induction of premature senescence represents a novel functional strategy to curb the uncontrolled proliferation of malignant cancer cells. This study unveils the regiospecific synthesis of novel isoxazoline derivatives condensed to ring A of medicinal plant product Withaferin-A. Intriguingly, the cis fused products with β-oriented hydrogen exhibited excellent cytotoxic activities against proliferating human breast cancer MCF7 and colorectal cancer HCT-116 cells. The most potent derivative W-2b triggered premature senescence along with increase in senescence-associated β-galactosidase activity, G2/M cell cycle arrest, and induction of senescence-specific marker p21(Waf1/Cip1) at its sub-toxic concentration...
October 23, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29043807/2-3-dihydro-3%C3%AE-methoxy-withaferin-a-protects-normal-cells-against-stress-molecular-evidence-of-its-potent-cytoprotective-activity
#8
Anupama Chaudhary, Rajkumar S Kalra, Chuang Huang, Jay Prakash, Sunil C Kaul, Renu Wadhwa
2,3-Dihydro-3β-methoxy withaferin-A (3βmWi-A) is a natural withanolide that is structurally close to withaferin-A (Wi-A), is cytotoxic to human cancer cells, and is a candidate anticancer natural compound. Using cell-based biochemical, molecular, and imaging assays, we report that Wi-A and 3βmWi-A possess contrasting activities. Whereas Wi-A caused oxidative stress to normal cells, 3βmWi-A was well tolerated at even 10-fold higher concentrations. Furthermore, it promoted survival and protected normal cells against oxidative, UV radiation, and chemical stresses...
October 27, 2017: Journal of Natural Products
https://www.readbyqxmd.com/read/29017913/the-use-of-natural-compounds-for-the-targeting-and-chemoprevention-of-ovarian-cancer
#9
Francesca Pistollato, Ruben Calderón Iglesias, Roberto Ruiz, Silvia Aparicio, Jorge Crespo, Luis Dzul Lopez, Francesca Giampieri, Maurizio Battino
Among gynaecological cancers, ovarian cancer represents the leading cause of death in women. Current treatment for ovarian cancer entails surgery followed by combined chemotherapy with platinum and taxane, which are associated, particularly cisplatin, with severe side effects. While this treatment approach appears to be initially effective in a high number of patients, nearly 70% of them suffer a relapse within a few months after initial treatment. Therefore, more effective and better-tolerated treatment options are clearly needed...
October 7, 2017: Cancer Letters
https://www.readbyqxmd.com/read/28936177/withaferin-a-induces-oxidative-stress-mediated-apoptosis-and-dna-damage-in-oral-cancer-cells
#10
Hsueh-Wei Chang, Ruei-Nian Li, Hui-Ru Wang, Jing-Ru Liu, Jen-Yang Tang, Hurng-Wern Huang, Yu-Hsuan Chan, Ching-Yu Yen
Withaferin A (WFA) is one of the most active steroidal lactones with reactive oxygen species (ROS) modulating effects against several types of cancer. ROS regulation involves selective killing. However, the anticancer and selective killing effects of WFA against oral cancer cells remain unclear. We evaluated whether the killing ability of WFA is selective, and we explored its mechanism against oral cancer cells. An MTS tetrazolium cell proliferation assay confirmed that WFA selectively killed two oral cancer cells (Ca9-22 and CAL 27) rather than normal oral cells (HGF-1)...
2017: Frontiers in Physiology
https://www.readbyqxmd.com/read/28923386/structure-based-design-synthesis-and-biological-evaluation-of-withaferin-a-analogues-as-potent-apoptotic-inducers
#11
Gabriel G Llanos, Liliana M Araujo, Ignacio A Jiménez, Laila M Moujir, Jaime Rodríguez, Carlos Jiménez, Isabel L Bazzocchi
Apoptosis inducers represent an attractive approach for the discovery and development of anticancer agents. Herein, we report on the development by molecular fine tuning of a withaferin A-based library of 63 compounds (2-64), 53 of them reported for the first time. Their antiproliferative evaluation on HeLa, A-549 and MCF-7 human tumor cell lines identified fifteen analogues displaying higher activity (IC50 values ranging 0.3-4.8 μM) than the lead (IC50 values ranging 1.3-10.1 μM) either in lag or log growth phases...
November 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28919038/covalent-ligand-discovery-against-druggable-hotspots-targeted-by-anti-cancer-natural-products
#12
Elizabeth A Grossman, Carl C Ward, Jessica N Spradlin, Leslie A Bateman, Tucker R Huffman, David K Miyamoto, Jordan I Kleinman, Daniel K Nomura
Many natural products that show therapeutic activities are often difficult to synthesize or isolate and have unknown targets, hindering their development as drugs. Identifying druggable hotspots targeted by covalently acting anti-cancer natural products can enable pharmacological interrogation of these sites with more synthetically tractable compounds. Here, we used chemoproteomic platforms to discover that the anti-cancer natural product withaferin A targets C377 on the regulatory subunit PPP2R1A of the tumor-suppressor protein phosphatase 2A (PP2A) complex leading to activation of PP2A activity, inactivation of AKT, and impaired breast cancer cell proliferation...
November 16, 2017: Cell Chemical Biology
https://www.readbyqxmd.com/read/28839383/withaferin-a-induces-apoptosis-in-osteosarcoma-u2os-cell-line-via-generation-of-ros-and-disruption-of-mitochondrial-membrane-potential
#13
Hui-Liang Zhang, Hong Zhang
BACKGROUND: Withaferin-A (WF-A) is a well-known dietary compound isolated from Withania sominifera. It has tremendous pharmacological potential and has been shown to exhibit antiproliferative activity against several types of cancerous cells. Currently, the main focus of anti-cancer therapeutic development is to identify apoptosis inducing drug-like molecules. Osteosarcoma is a rare type of osteocancer, affecting human. The present study therefore focused on the evaluation of antitumor potential of WF-A against several osteosarcoma cell lines...
July 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/28782635/withaferin-a-induced-impaired-autophagy-and-unfolded-protein-response-in-human-breast-cancer-cell-lines-mcf-7-and-mda-mb-231
#14
Kamalini Ghosh, Soumasree De, Srimoyee Mukherjee, Sayantani Das, Amar Nath Ghosh, Sumita Bandyopadhyay Sengupta
The autophagy-lysosome pathway and the ubiquitin-proteasome systems are the two major routes for eukaryotic intracellular protein clearance. Cancerous cells often display elevated protein synthesis and byproduct disposal, thus, inhibition of the protein degradation pathways became an emerging approach for cancer therapy. The present study revealed that withaferin-A (WA), the biologically active withanolide derived from Withania somnifera, initially induced formation of autophagosomes in human breast cancer cell-lines, MCF-7 and MDA-MB-231...
October 2017: Toxicology in Vitro: An International Journal Published in Association with BIBRA
https://www.readbyqxmd.com/read/28694686/molecular-docking-qsar-and-admet-studies-of-withanolide-analogs-against-breast-cancer
#15
Dharmendra K Yadav, Surendra Kumar, Saloni, Harpreet Singh, Mi-Hyun Kim, Praveen Sharma, Sanjeev Misra, Feroz Khan
Withanolides are a group of pharmacologically active compounds present in most prodigal amounts in roots and leaves of Withania somnifera (Indian ginseng), one of the most important medicinal plants of Indian traditional practice of medicine. Withanolides are steroidal lactones (highly oxygenated C-28 phytochemicals) and have been reported to exhibit immunomodulatory, anticancer and other activities. In the present study, a quantitative structure activity relationship (QSAR) model was developed by a forward stepwise multiple linear regression method to predict the activity of withanolide analogs against human breast cancer...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28693185/withaferin-a-inhibits-the-proliferation-of-gastric-cancer-cells-by-inducing-g2-m-cell-cycle-arrest-and-apoptosis
#16
Green Kim, Tae-Hyoun Kim, Eun-Ha Hwang, Kyu-Tae Chang, Jung Joo Hong, Jong-Hwan Park
Human gastric adenocarcinoma (AGS) is one of the most common types of malignant tumor and the third-leading cause of tumor-associated mortality worldwide. Withaferin A (WA), a steroidal lactone derived from Withania somnifera, exhibits antitumor activity in a variety of cancer models. However, to the best of our knowledge, the direct effect of WA on AGS cells has not previously been determined. The present study investigated the effects of WA on the proliferation and metastatic activity of AGS cells. WA exerted a dose-dependent cytotoxic effect on AGS cells...
July 2017: Oncology Letters
https://www.readbyqxmd.com/read/28688542/evaluation-of-apoptotic-activity-of-withania-coagulans-methanolic-extract-against-human-breast-cancer-and-vero-cell-lines
#17
Rumana Ahmad, Afreen Fatima, A N Srivastava, Mohsin Ali Khan
BACKGROUND: The genus Withania (Family: Solanaceae) holds an important position in Ayurveda, the Indian traditional system of medicine. Withania somnifera Dunal and Withania coagulans Dunal have been documented in folklore as panaceas for various ailments since time immemorial. W. coagulans (WC), commonly called as Indian cheese maker is used for fermenting milk for cheese production in various parts of India. OBJECTIVES: In the study, in vitro cytotoxicity of methanolic extract of dried fruits (berries) of WC was evaluated in a dose dependent manner using trypan blue dye exclusion method against human breast cancer cell line MDA-MB-231 and normal kidney epithelial cell line Vero in the range 20-200 μg/ml...
July 2017: Journal of Ayurveda and Integrative Medicine
https://www.readbyqxmd.com/read/28686599/flux-balance-analysis-predicts-warburg-like-effects-of-mouse-hepatocyte-deficient-in-mir-122a
#18
Hua-Qing Wu, Mei-Ling Cheng, Jin-Mei Lai, Hsuan-Hui Wu, Meng-Chun Chen, Wen-Huan Liu, Wu-Hsiung Wu, Peter Mu-Hsin Chang, Chi-Ying F Huang, Ann-Ping Tsou, Ming-Shi Shiao, Feng-Sheng Wang
The liver is a vital organ involving in various major metabolic functions in human body. MicroRNA-122 (miR-122) plays an important role in the regulation of liver metabolism, but its intrinsic physiological functions require further clarification. This study integrated the genome-scale metabolic model of hepatocytes and mouse experimental data with germline deletion of Mir122a (Mir122a-/-) to infer Warburg-like effects. Elevated expression of MiR-122a target genes in Mir122a-/-mice, especially those encoding for metabolic enzymes, was applied to analyze the flux distributions of the genome-scale metabolic model in normal and deficient states...
July 2017: PLoS Computational Biology
https://www.readbyqxmd.com/read/28681243/synergistic-inhibition-of-glioma-cell-proliferation-by-withaferin-a-and-tumor-treating-fields
#19
Edwin Chang, Christoph Pohling, Nooshin Beygui, Chirag B Patel, Jarrett Rosenberg, Dong Ho Ha, Sanjiv S Gambhir
Glioblastoma (GBM) is the most aggressive and lethal form of brain cancer. Standard therapies are non-specific and often of limited effectiveness; thus, efforts are underway to uncover novel, unorthodox therapies against GBM. In previous studies, we investigated Withaferin A, a steroidal lactone from Ayurvedic medicine that inhibits proliferation in cancers including GBM. Another novel approach, tumor treating fields (TTFields), is thought to disrupt mitotic spindle formation and stymie proliferation of actively dividing cells...
July 5, 2017: Journal of Neuro-oncology
https://www.readbyqxmd.com/read/28676732/proinflammatory-cytokines-il-6-and-tnf-%C3%AE-increased-telomerase-activity-through-nf-%C3%AE%C2%BAb-stat1-stat3-activation-and-withaferin-a-inhibited-the-signaling-in-colorectal-cancer-cells
#20
Seyung S Chung, Yong Wu, Quincy Okobi, Debbie Adekoya, Mohammad Atefi, Orette Clarke, Pranabananda Dutta, Jaydutt V Vadgama
There are increasing evidences of proinflammatory cytokine involvement in cancer development. Here, we found that two cytokines, IL-6 and TNF-α, activated colorectal cancer cells to be more invasive and stem-like. Combined treatment of IL-6 and TNF-α phosphorylated transcription factors STAT3 in a synergistic manner. STAT3, STAT1, and NF-κB physically interacted upon the cytokine stimulation. STAT3 was bound to the promoter region of human telomerase reverse transcriptase (hTERT). IL-6 and TNF-α stimulation further enhanced STAT3 binding affinity...
2017: Mediators of Inflammation
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