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Celastrol

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https://www.readbyqxmd.com/read/29202812/celastrol-improves-self-renewal-and-differentiation-of-human-tendon-derived-stem-cells-by-suppressing-smad7-through-hypoxia
#1
Tianyi Wu, Shenghe Liu, Gen Wen, Jia Xu, Yaling Yu, Yimin Chai
BACKGROUND: We aimed to evaluate the potential enhancing effect of celastrol on the stemness of human tendon-derived stem cells (hTSCs) in vitro and the underlying molecular mechanisms. METHODS: The capability of hTSC self-renewal was assessed by cell proliferation and colony formation as determined with the CCK-8 kit. Adipogenesis, chondrogenesis, and osteogenesis were determined by Oil Red O, Alcian Blue, and Alizarin Red staining, respectively. The relative mRNA levels of Sox9, PPARγ, Runx2, Smad7, and HIF1α were determined by real-time polymerase chain reaction (PCR)...
December 4, 2017: Stem Cell Research & Therapy
https://www.readbyqxmd.com/read/29190976/celastrol-induces-apoptosis-in-hepatocellular-carcinoma-cells-via-targeting-er-stress-upr
#2
Bo Ren, Hui Liu, Hang Gao, Shutong Liu, Zehui Zhang, Andrew M Fribley, Michael U Callaghan, Zhixiang Xu, Qinghua Zeng, Yulin Li
Hepatocellular carcinoma (HCC) is one of the most serious and deadly diseases worldwide with limited options for effective treatment. Biomarker-based active compound targeting therapy may shed some light on novel drugs for HCC. The endoplasmic reticulum (ER) stress and unfolded protein response (UPR) play important roles in the regulation of cell fate and have become novel signaling targets for the development of anticancer drugs. Celastrol, a triterpene from traditional Chinese medicine, has been reported to possess anti-tumor effects on various cancers...
November 3, 2017: Oncotarget
https://www.readbyqxmd.com/read/29179596/celastrol-attenuates-impairments-associated-with-lipopolysaccharide-induced-acute-respiratory-distress-syndrome-ards-in-rats
#3
Yongjun Wei, Yu Wang
Celastrol, a constituent from a traditional Chinese medicinal herb belonging to the family Celastraceae, has been shown to impart anti-inflammatory properties, in part, by inhibiting NF-κB activity and related induction of pro-inflammatory cytokine formation/release. The present study investigated the effects of celastrol in an animal model of acute respiratory distress syndrome (ARDS) induced by intratracheal administration of lipopolysaccharides (LPSs). Celastrol pre-treatment groups received celastrol by intraperitoneal injection on seven consecutive days before LPS treatment...
December 2017: Journal of Immunotoxicology
https://www.readbyqxmd.com/read/29128845/mitochondrial-alkaline-ph-responsive-drug-release-mediated-by-celastrol-loaded-glycolipid-like-micelles-for-cancer-therapy
#4
Yanan Tan, Yun Zhu, Yue Zhao, Lijuan Wen, Tingting Meng, Xuan Liu, Xiqin Yang, Suhuan Dai, Hong Yuan, Fuqiang Hu
Mitochondria, crucial regulators of inducing tumor cells apoptosis, can be treated as the prime target for tumor therapy. The selective and responsive release of proapoptotic therapeutics into mitochondria may notably improve antitumor efficiency. Herein, (4-Carboxybutyl) triphenylphosphonium bromide (CTPP), a lipophilic cation, was conjugated with glucolipid-like conjugates (CSOSA) to produce mitochondria-targeted conjugates (CTPP-CSOSA). Loading with weakly acidic drug Celastrol (Cela), CTPP-CSOSA/Cela micelles could selectively respond to mitochondrial alkaline pH (pH 8...
July 31, 2017: Biomaterials
https://www.readbyqxmd.com/read/29102699/self-assembled-phospholipid-based-phytosomal-nanocarriers-as-promising-platforms-for-improving-oral-bioavailability-of-the-anticancer-celastrol
#5
May S Freag, Wedad M Saleh, Ossama Y Abdallah
Celastrol (CST) is a promising natural drug of herbal origin that gained a great interest in the recent years by virtue of its wide variety of pharmacological actions. Nowadays, CST is extensively studied as a natural anticancer surrogate with a potential activity against various types of cancers. However, CST suffers from many limitations that handicapped its clinical utility such as limited aqueous solubility and poor gastrointestinal absorption which resulted into its low oral bioavailability. This work spotlights, for the first time, development of self-assembled phytosomal nanocarriers (CST-PHY) for improving CST solubility and oral bioavailability...
November 2, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29090408/knockdown-of-heat-shock-proteins-hspa6-hsp70b-and-hspa1a-hsp70-1-sensitizes-differentiated-human-neuronal-cells-to-cellular-stress
#6
Catherine A S Deane, Ian R Brown
Heat shock proteins are involved in cellular repair and protective mechanisms that counter characteristic features of neurodegenerative diseases such as protein misfolding and aggregation. The HSPA (Hsp70) multigene family includes the widely studied HSPA1A (Hsp70-1) and the little studied HSPA6 (Hsp70B') which is present in the human genome and not in mouse and rat. The effect of knockdown of HSPA6 and HSPA1A expression was examined in relation to the ability of differentiated human SH-SY5Y neuronal cells to tolerate thermal stress...
October 31, 2017: Neurochemical Research
https://www.readbyqxmd.com/read/29069290/potent-suppression-of-both-spontaneous-and-carcinogen-induced-colitis-associated-colorectal-cancer-in-mice-by-dietary-celastrol-supplementation
#7
Emily C Barker, Byung-Gyu Kim, Ji Hee Yoon, Gregory P Tochtrop, John J Letterio, Sung Hee Choi
Celastrol is an anti-inflammatory natural triterpenoid, isolated from the herb Tripterygium wilfordii or thunder god vine. Here we define mechanisms mediating anti-inflammatory activity of celastrol and demonstrate efficacy of a dietary celastrol supplement for chemoprevention of inflammation-driven carcinogenesis in mice. Dietary celastrol (31.25 ppm in rodent diet from 8 weeks to 25 weeks of age) is well tolerated and protects against LPS-induced acute inflammation in C57BL/6 mice, potently suppressing LPS-induction of inducible nitric oxide synthase (iNOS), cyclooxygenase (COX)-2, Interleukin (IL)-6, and IL-1β...
October 21, 2017: Carcinogenesis
https://www.readbyqxmd.com/read/29048668/celastrol-downregulates-e2f1-to-induce-growth-inhibitory-effects-in-hepatocellular-carcinoma-hepg2-cells
#8
Liang Ma, Lei Peng, Sheng Fang, Bangguo He, Zi Liu
Celastrol, a natural compound extracted from Tripterygium wilfordii, is known to exhibit potential anticancer activities in various types of tumor cells. E2F1 is reported to be overexpressed in several types of human tumors and its inactivation may be a valuable novel potential therapeutic strategy for cancer treatment. However, the molecular mechanism underlying the pro-apoptotic effects of celastrol on hepatocellular carcinoma (HCC) cells remains unclear, and E2F1-targeted compounds have been rarely identified...
September 19, 2017: Oncology Reports
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
#9
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
#10
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
#11
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...
November 2017: Genome Research
https://www.readbyqxmd.com/read/28994112/celastrol-attenuates-pain-and-cartilage-damage-via-sdf-1-cxcr4-signalling-pathway-in-osteoarthritis-rats
#12
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
#13
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
#14
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
#15
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
#16
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)...
November 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
#17
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
#18
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
#19
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
#20
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
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