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Celastrol

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https://www.readbyqxmd.com/read/29040966/natural-product-celastrol-suppressed-macrophage-m1-polarization-against-inflammation-in-diet-induced-obese-mice-via-regulating-nrf2-ho-1-map-kinase-and-nf-%C3%AE%C2%BAb-pathways
#1
Dan Luo, Yumeng Guo, Yuanyuan Cheng, Jia Zhao, Yu Wang, Jianhui Rong
Macrophage polarization is implicated in the inflammation in obesity. The aim of the present study was to examine the anti-inflammatory activities of botanical triterpene celastrol against diet-induced obesity. We treated diet-induced obese C57BL/6N male mice with celastrol (5, 7.5 mg/kg/d) for 3 weeks, and investigated macrophage M1/M2 polarization in adipose and hepatic tissues. Celastrol reduced fat accumulation and ameliorated glucose tolerance and insulin sensitivity. Celastrol down-regulated the mRNA levels of macrophage M1 biomarkers (e...
October 16, 2017: Aging
https://www.readbyqxmd.com/read/29026082/targeted-delivery-of-celastrol-to-mesangial-cells-is-effective-against-mesangioproliferative-glomerulonephritis
#2
Ling Guo, Shi Luo, Zhengwu Du, Meiling Zhou, Peiwen Li, Yao Fu, Xun Sun, Yuan Huang, Zhirong Zhang
Mesangial cells-mediated glomerulonephritis is a frequent cause of end-stage renal disease. Here, we show that celastrol is effective in treating both reversible and irreversible mesangioproliferative glomerulonephritis in rat models, but find that its off-target distributions cause severe systemic toxicity. We thus target celastrol to mesangial cells using albumin nanoparticles. Celastrol-albumin nanoparticles crosses fenestrated endothelium and accumulates in mesangial cells, alleviating proteinuria, inflammation, glomerular hypercellularity, and excessive extracellular matrix deposition in rat anti-Thy1...
October 12, 2017: Nature Communications
https://www.readbyqxmd.com/read/29025894/nascent-rna-sequencing-reveals-a-dynamic-global-transcriptional-response-at-genes-and-enhancers-to-the-natural-medicinal-compound-celastrol
#3
Noah Dukler, Gregory T Booth, Yi-Fei Huang, Nathaniel Tippens, Colin T Waters, Charles G Danko, John T Lis, Adam Siepel
Most studies of responses to transcriptional stimuli measure changes in cellular mRNA concentrations. By sequencing nascent RNA instead, it is possible to detect changes in transcription in minutes rather than hours and thereby distinguish primary from secondary responses to regulatory signals. Here, we describe the use of PRO-seq to characterize the immediate transcriptional response in human cells to celastrol, a compound derived from traditional Chinese medicine that has potent anti-inflammatory, tumor-inhibitory, and obesity-controlling effects...
October 12, 2017: Genome Research
https://www.readbyqxmd.com/read/28994112/celastrol-attenuates-pain-and-cartilage-damage-via-sdf-1-cxcr4-signalling-pathway-in-osteoarthritis-rats
#4
Weifeng Wang, Chengzhi Ha, Tao Lin, Dawei Wang, Yuanhe Wang, Mingzhi Gong
OBJECTIVES: Celastrol has attracted wide interests for its anticancer and anti-inflammation properties, and studies have demonstrated that celastrol negatively modulates the stromal cell-derived factor-1 (SDF-1) and receptor C-X-C chemokine receptor type 4 (CXCR4) signalling. We aim in this study to investigate the effects of celastrol in osteoarthritis (OA) in vivo and explored the underlying molecular mechanisms. METHODS: We established a monoiodoacetate (MIA)-induced rat OA model and evaluated the joint pain and cartilage damage with or without celastrol treatments...
October 10, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28984147/celastrol-ameliorates-acetaminophen-induced-oxidative-stress-and-cytotoxicity-in-hepg2-cells
#5
A T Jannuzzi, M Kara, B Alpertunga
Acetaminophen (APAP) is the most commonly used analgesic and antipyretic drug in the world. However, hepatotoxicity caused by APAP overdose is the most frequent cause of acute liver failure worldwide and oxidative stress involved in the pathogenesis of APAP hepatotoxicity. Celastrol is a natural triterpenoid derived from Tripterygium wilfordii Hook F. that exhibits antioxidant, anti-inflammatory, and antitumor activities. In this study, we aimed to investigate the potential ameliorative effects of celastrol against APAP-induced cytotoxicity and oxidative stress...
January 1, 2017: Human & Experimental Toxicology
https://www.readbyqxmd.com/read/28978034/celastrol-ameliorates-inflammation-through-inhibition-of-nlrp3-inflammasome-activation
#6
Xianjun Yu, Qun Zhao, Xixi Zhang, Haiwei Zhang, Yongbo Liu, Xiaoxia Wu, Ming Li, Xiaoming Li, Jingxuan Zhang, Xuzhi Ruan, Haibing Zhang
Celastrol exhibits potential anti-inflammatory activity in a variety of inflammatory diseases, but the mechanism remains poorly understood. Activation of NLRP3 inflammasome is involved in multiple inflammatory diseases. Here, we show that celastrol abolishes the NLRP3 inflammasome activation, inhibits subsequent caspase-1 activation and IL-1β secretion both in vitro and in vivo. Notably, interruption of ASC oligomerization and autophagy activation are involved in NLRP3 inflammasome inactivation by celastrol...
September 15, 2017: Oncotarget
https://www.readbyqxmd.com/read/28955491/effect-of-celastrol-on-bone-structure-and-mechanics-in-arthritic-rats
#7
Rita Cascão, Bruno Vidal, Mikko Arttu Jalmari Finnilä, Inês Pascoal Lopes, Rui Lourenço Teixeira, Simo Saarakkala, Luis Ferreira Moita, João Eurico Fonseca
OBJECTIVE: Rheumatoid arthritis (RA) is characterised by chronic inflammation leading to articular bone and cartilage damage. Despite recent progress in RA management, adverse effects, lack of efficacy and economic barriers to treatment access still limit therapeutic success. Therefore, safer and less expensive treatments that control inflammation and bone resorption are needed. We have previously shown that celastrol is a candidate for RA treatment. We have observed that it inhibits both interleukin (IL)-1β and tumor necrosis factor (TNF) in vitro, and that it has anti-inflammatory properties and ability to decrease synovial CD68+ macrophages in vivo...
2017: RMD Open
https://www.readbyqxmd.com/read/28944849/celastrol-alleviates-angiotensin-ii%C3%A2-mediated-vascular-smooth-muscle-cell-senescence-via-induction-of-autophagy
#8
Xian-Jie Xu, Wei-Bo Zhao, Shi-Bin Feng, Cheng Sun, Qiang Chen, Bing Ni, Hou-Yuan Hu
Reactive oxygen species (ROS) production has been implicated in the promotion of cellular senescence. Celastrol, a quinone methide triterpenoid isolated from the Celastraceae family, exerts antioxidant effects and enhances autophagy in various cell types. Since autophagy serves an important role in regulating ROS, it was hypothesized that the antioxidant effect of celastrol is via enhanced autophagy, thus inhibiting cell senescence. Therefore, the present study used a Senescence β‑Galactosidase Staining kit, western blot analysis and cell cycle analysis to investigate whether celastrol alleviates angiotensin (Ang) II‑induced cellular senescence by upregulating autophagy in vascular smooth muscle cells (VSMCs)...
September 20, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28935193/celastrol-inhibits-hepatitis-c-virus-replication-by-upregulating-heme-oxygenase-1-via-the-jnk-mapk-nrf2-pathway-in-human-hepatoma-cells
#9
Chin-Kai Tseng, Sung-Po Hsu, Chun-Kuang Lin, Yu-Hsuan Wu, Jin-Ching Lee, Kung-Chia Young
BACKGROUND AND PURPOSE: Celastrol, a quinone methide triterpene isolated from the root extracts of Tripterygium wilfordii, can greatly induce the gene expression activity of heme oxygenase-1 (HO-1) to achieve disease prevention and control. HO-1 induction was recently shown to result in anti-HCV activity by inducing type I interferon and inhibiting hepatitis C virus (HCV) NS3/4A protease activity. The aim of the present study is to evaluate the anti-HCV activity of celastrol and characterize its mechanism of inhibition...
September 19, 2017: Antiviral Research
https://www.readbyqxmd.com/read/28878153/high-throughput-study-of-the-effects-of-celastrol-on-activated-fibroblast-like-synoviocytes-from-patients-with-rheumatoid-arthritis
#10
Zhengyu Fang, Dongyi He, Bo Yu, Feng Liu, Jianping Zuo, Yuxia Li, Qi Lin, Xiaodong Zhou, Qingwen Wang
Celastrol, a natural triterpene, exhibits potential anti-inflammatory activity in a variety of inflammatory diseases. The present study aimed to investigate its biological effect on activated fibroblast-like synoviocytes (FLSs) from patients with rheumatoid arthritis (RA). The primary FLSs of the synovial tissues were obtained from synovial biopsies of patients with RA. The normal human FLS line (HFLS) was used as a control. After the RA-FLSs and HFLSs were treated with or without celastrol, various approaches, including the WST-1 assay, transwell assay, real-time PCR and ELISA analysis, were performed to estimate proliferation, invasion and expression of pro-inflammatory cytokines of the RA-FLSs...
September 6, 2017: Genes
https://www.readbyqxmd.com/read/28865279/design-synthesis-and-biological-evaluation-of-novel-c-29-carbamate-celastrol-derivatives-as-potent-and-selective-cytotoxic-compounds
#11
Sandra A C Figueiredo, Jorge A R Salvador, Roldán Cortés, Marta Cascante
Celastrol and its derivatives have been reported for their potent anticancer activity. Among other celastrol analogues, novel carbamate derivatives were designed and synthesised, and their biological activity on the viability of human cancer cell lines was evaluated. Additionally, a preliminary structure-activity relationship study was conducted. Derivative 18 showed the highest activity on cancer cell viability, combined with the best selectivity between malignant cells and non-malignant fibroblasts. Preliminary mechanistic studies of its anti-tumour action indicated that compound 18 has an antiproliferative effect on SKOV-3 human ovarian cancer cells (IC50 = 0...
October 20, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28864208/a-new-mechanism-of-inhibition-of-il-1%C3%AE-secretion-by-celastrol-through-the-nlrp3-inflammasome-pathway
#12
Wenyu Xin, Qiaoyun Wang, Dan Zhang, Chaoyun Wang
The NLRP3 (NOD-like receptor protein 3) inflammasome is a caspase-1-containing multiprotein complex that controls the release of IL-1β and has been associated with the development of inflammatory diseases. Celastrol, a pharmacologically active ingredient extracted from Tripterygium wilfordii Hook, has anti-inflammatory activities based on its inhibition of IL-1β secretion. The purpose of the present study was to investigate the possible modulation of NLRP3 inflammasome-mediated IL-1β and IL-18 release from macrophages by celastrol...
November 5, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28782773/triptolide-and-celastrol-loaded-silk-fibroin-nanoparticles-show-synergistic-effect-against-human-pancreatic-cancer-cells
#13
Baoyue Ding, Md Arif Wahid, Zhijun Wang, Chen Xie, Arvind Thakkar, Sunil Prabhu, Jeffrey Wang
Pancreatic cancer is a lethal disease with a dreadful 5-year survival rate of only 5%. In spite of several treatment options, the prognosis still remains extremely poor. Therefore, novel therapy strategies with combinations of drugs are urgently required to combat this fatal disease. Triptolide (TPL) and celastrol (CL), two main compounds in traditional Chinese medicine isolated from Thunder God Vine, have a broad range of bioactivities including anticancer activity. Silk fibroin (SF), a naturally occurring protein with several unique properties, is an ideal carrier material...
August 17, 2017: Nanoscale
https://www.readbyqxmd.com/read/28757108/celastrol-synergizes-with-oral-nifedipine-to-attenuate-hypertension-in-preeclampsia-a-randomized-placebo-controlled-and-double-blinded-trial
#14
Sha Xiao, Ming Zhang, Yuan Liang, Deling Wang
Preeclampsia, a disease mainly manifesting as serious hypertension during pregnancy, affects expectant mothers around the globe. Celastrol, a naturally existing triterpenoid, is known to exhibit beneficial effects attenuating cardiovascular symptoms including hypertension. We here assessed the treatment outcome against preeclampsia with a combined use of celastrol and nifedipine. A total of 626 patients with preeclampsia were enrolled, screened, and assigned by random to groups receiving either nifedipine + placebo or nifedipine + celastrol orally...
July 20, 2017: Journal of the American Society of Hypertension: JASH
https://www.readbyqxmd.com/read/28754470/oleanane-ursane-and-quinone-methide-friedelane-type-triterpenoid-derivatives-recent-advances-in-cancer-treatment
#15
REVIEW
Jorge A R Salvador, Ana S Leal, Ana S Valdeira, Bruno M F Gonçalves, Daniela P S Alho, Sandra A C Figueiredo, Samuel M Silvestre, Vanessa I S Mendes
Natural pentacyclic triterpenoids (PTs) have been often reported to exhibit a wide range of biological activities. Among them, the anticancer and anti-inflammatory activities are the most studied. Over the last two decades, the number of publications reporting the anticancer effects of PTs has risen exponentially, reflecting the increasing interest in these natural products for the development of new antineoplastic drugs. Among of the most investigated PTs regarding their anticancer properties are oleanane-, ursane and friedelane-types, including oleanolic, glycyrrhetinic, ursolic and asiatic acids, and celastrol, among others...
July 14, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28730769/downregulation-and-subcellular-distribution-of-her2-involved-in-mda-mb-453-breast-cancer-cell-apoptosis-induced-by-lapatinib-celastrol-combination
#16
Yan-Yan Yan, Hong Bi, Wei Zhang, Qing Wen, Hong Liu, Jin-Xia Li, Hui-Zhi Zhang, Yan-Xia Zhang, Jia-Shan Li
PURPOSE: To investigate the effect and related molecular mechanisms of lapatinib/celastrol combination or single-agent treatment in HER2/neu-overexpressing MDA-MB-453 breast cancer cells. METHODS: The effects of treatment with lapatinib, celastrol or their combination on cell growth were determined using MTT assay. Drug synergy was determined using the combination index (CI) methods derived from Chou-Talalay equations using CalcuSyn software. Apoptotic morphology was observed by fluorescence microscope with Hoechst 33258 staining...
May 2017: Journal of B.U.ON.: Official Journal of the Balkan Union of Oncology
https://www.readbyqxmd.com/read/28715871/improvement-of-mitochondrial-function-by-celastrol-in-palmitate-treated-c2c12-myotubes-via-activation-of-pi3k-akt-signaling-pathway
#17
Mohamad Hafizi Abu Bakar, Joo Shun Tan
Compelling evidences posited that high level of saturated fatty acid gives rise to mitochondrial dysfunction and inflammation in the development of insulin resistance in skeletal muscle. Celastrol is a pentacyclic triterpenoid derived from the root extracts of Tripterygium wilfordii that possesses potent anti-inflammatory properties in a number of animal models with metabolic diseases. However, the cellular mechanistic action of celastrol in alleviating obesity-induced insulin resistance in skeletal muscle remains largely unknown...
September 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28707601/potential-role-of-natural-compounds-as-anti-angiogenic-agents-in-cancer
#18
Muthu K Shanmugam, Sudha Warrier, Alan Prem Kumar, Gautam Sethi, Frank Arfuso
BACKGROUND: Neovascularization, also known as angiogenesis, is the process of capillary sprouting from pre-existing blood vessels. This physiological process is a hallmark event in normal embryonic development as blood vessels generally supply both oxygen and nutrients to the cells of the body. Any disruption in this process can lead to the development of various chronic diseases, including cancer. In cancer, aberrant angiogenesis plays a prominent role in maintaining sustained tumor growth to malignant phenotypes and promoting metastasis...
July 12, 2017: Current Vascular Pharmacology
https://www.readbyqxmd.com/read/28688281/novel-celastrol-derivatives-with-improved-selectivity-and-enhanced-antitumour-activity-design-synthesis-and-biological-evaluation
#19
Sandra A C Figueiredo, Jorge A R Salvador, Roldán Cortés, Marta Cascante
Celastrol is one of the most active antitumour compounds among the natural triterpenoids. It has been reported to be highly active against a wide variety of tumours and to affect multiple cellular pathways. A series of new celastrol derivatives, including compounds bearing a urea group, have been synthesised and analysed for their biological activity against human cancer cell lines. Several compounds presented a stronger growth inhibition effect than celastrol on the cell lines studied. Among them, compound 24 was the most promising derivative, as it exhibited both a remarkable antiproliferative activity and an improved selectivity in tumour versus non-tumour cells...
September 29, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28679864/celastrol-ameliorates-inflammation-through-inhibition-of-nlrp3-inflammasome-activation
#20
Xianjun Yu, Qun Zhao, Xixi Zhang, Haiwei Zhang, Yongbo Liu, Xiaoxia Wu, Ming Li, Xiaoming Li, Jingxuan Zhang, Xuzhi Ruan, Haibing Zhang
Celastrol exhibits potential anti-inflammatory activity in a variety of inflammatory diseases, but the mechanism remains poorly understood. Activation of NLRP3 inflammasome is involved in multiple inflammatory diseases. Here, we show that celastrol abolishes the NLRP3 inflammasome activation, inhibits subsequent caspase-1 activation and IL-1β secretion both in vitro and in vivo. Notably, interruption of ASC oligomerization and autophagy activation are involved in NLRP3 inflammasome inactivation by celastrol...
June 27, 2017: Oncotarget
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