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Celastrol

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https://www.readbyqxmd.com/read/28522217/celastrol-inhibits-chondrosarcoma-proliferation-migration-and-invasion-through-suppression-cip2a-c-myc-signaling-pathway
#1
Jinhui Wu, Muchen Ding, Ningfang Mao, Yungang Wu, Chao Wang, Jiabin Yuan, Xiong Miao, Jingfeng Li, Zhicai Shi
Chondrosarcomas (CS) is the second most frequent tumors of cartilage origin. A small compound extracted from Thunder God Vine (Tripterygium wilfordii Hook. F.) called celastrol can directly bound CIP2A protein and effectively inhibit cell proliferation and induce apoptosis in several cancer cells. However, little knowledge is concern about the important role of CIP2A in CS patients and the therapeutic value of celastrol on CS. Our results showed that CIP2A and c-MYC were verified to be oncoproteins by detecting their mRNA and protein expression in 10 human CS tissues by qRT-PCR and Western blots...
April 14, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28509859/alcl%C3%A2-%C3%A2-6h%C3%A2-o-catalyzed-friedel-crafts-alkylation-of-indoles-by-the-para-quinone-methide-moiety-of-celastrol
#2
Yi Zhu, Ziwen Chen, Zhenfei Huang, Siwei Yan, Zhuoer Li, Hu Zhou, Xiaokun Zhang, Ying Su, Zhiping Zeng
A classical Friedel-Crafts alkylation of different indoles catalyzed by AlCl₃·6H₂O has been developed for a well-known important natural product, celastrol, resulting in a series of derivatives for further biological evaluation. The catalyst loading was reduced to 5 mol %, the reaction proceeds at ambient temperature and reaction time is only 3 h. The product yields range from 20% to 99%. A reaction mechanism is also proposed, based on our experiment results.
May 16, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28459364/cytotoxic-effect-of-celastrol-alone-or-in-combination-with-paclitaxel-on-anaplastic-thyroid-carcinoma-cells
#3
Si Hyoung Kim, Jun Goo Kang, Chul Sik Kim, Sung-Hee Ihm, Moon Gi Choi, Hyung Joon Yoo, Seong Jin Lee
The influence of celastrol alone or in combination with paclitaxel on survival of anaplastic thyroid carcinoma cells was investigated. In 8505C and SW1736 cells, after treatment of celastrol, cell viability decreased, and cytotoxic activity increased. The protein levels of heat shock protein (hsp) 90, hsp70, Bax, death receptor 5, cleaved caspase-3, cleaved poly (ADP-ribose) polymerase, phospho-extracellular signal-regulated kinase 1/2 (ERK1/2), and phospho-c-Jun N-terminal kinase (JNK) were elevated, and those of Bcl2, phospho-nuclear factor-kappaB (NF-κB), and total and phospho-Akt were reduced...
May 2017: Tumour Biology: the Journal of the International Society for Oncodevelopmental Biology and Medicine
https://www.readbyqxmd.com/read/28458159/celastrol-reduces-il-1%C3%AE-induced-matrix-catabolism-oxidative-stress-and-inflammation-in-human-nucleus-pulposus-cells-and-attenuates-rat-intervertebral-disc-degeneration-in-vivo
#4
Jian Chen, Jun Xuan, Yun-Tao Gu, Ke-Si Shi, Jun-Jun Xie, Jiao-Xiang Chen, Zeng-Ming Zheng, Yu Chen, Xi-Bang Chen, Yao-Sen Wu, Xiao-Lei Zhang, Xiang-Yang Wang
Celastrol has been reported to exert therapeutic potential on pro-inflammatory diseases including asthma, Crohn's disease, arthritis and neurodegenerative disorders via inhibiting NF-κB pathway. While the effect of celastrol on intervertebral disc degeneration (IDD), which is also a pro-inflammatory disease, remains unknown. In this study, we evaluated the effect of celastrol on IDD in IL-1β treated human nucleus pulposus cells in vitro as well as in puncture induced rat IDD model in vivo. Our results showed that celastrol reduced the expression of catabolic genes (MMP-3, 9, 13, ADAMTS-4, 5), oxidative stress factors (COX-2, iNOS) and pro-inflammatory factors (IL-6, TNF-a) induced by IL-1β in nucleus pulposus cells, also phosphorylation of IκBα and p65 were attenuated by celastrol, indicating NF-κB pathway was inhibited by celastrol in nucleus pulposus cells...
April 27, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28435131/repression-of-acetaminophen-induced-hepatotoxicity-by-a-combination-of-celastrol-and-brilliant-blue-g
#5
Heba A Abdelaziz, Mohamed E Shaker, Mohamed F Hamed, Nariman M Gameil
The sterile inflammatory response is an eminent contributor to acetaminophen (APAP)-hepatotoxicity in humans. Recent advances unraveled an axial role of the NLRP3-inflammasome in APAP-post injury inflammation. Nevertheless, the role of signaling events preceded the NLRP3-inflammasome activation, like the transcription factor NF-κB and the purinergic receptor P2X7, is still unclear and needs further elucidation. Here, we investigated the pharmacological inhibition of these upstream signaling molecules by celastrol and brilliant blue G (BBG) (separately or simultaneously) in APAP-hepatotoxicity in mice...
April 21, 2017: Toxicology Letters
https://www.readbyqxmd.com/read/28397045/celastrol-protects-tgf-%C3%AE-1-induced-endothelial-mesenchymal-transition
#6
Fei Gong, Fang Zhao, Xue-Dong Gan
The endothelial-to-mesenchymal transition (EndMT) in endothelial cells contributes to the development of cardiac fibrosis, ultimately leading to cardiac remodeling. In this study, the effects and molecular mechanisms of celastrol (CEL) on transforming growth factor-β1 (TGF-β1)-induced EndMT in human umbilical vein endothelial (HUVEC-12) cells were investigated. The presented data demonstrated that CEL significantly blocked the morphology change of HUVEC-12 cells induced by TGF-β1 without cell cytotoxicity...
April 2017: Journal of Huazhong University of Science and Technology. Medical Sciences
https://www.readbyqxmd.com/read/28389259/autophagy-induction-by-celastrol-augments-protection-against-bleomycin-induced-experimental-pulmonary-fibrosis-in-rats-role-of-adaptor-protein-p62-sqstm1
#7
Thomas Divya, Anandasadagopan Sureshkumar, Ganapasam Sudhandiran
Pulmonary fibrosis (PF) is a chronic pulmonary disease of unknown cause with high mortality. Autophagy is an important homeostatic process that decides the fate of cells under stress conditions. This study is aimed to investigate whether impaired autophagic activity leads to fibrosis and pharmacological induction of autophagy provides protection against bleomycin (BLM)-induced PF. A single dose of BLM (3 U/kg body weight) was administered intratracheally to induce fibrosis in rats. Celastrol, a triterpenoid (5 mg/kg/body weight, intraperitoneally) was given in every 81 h for a period of 28 days...
April 4, 2017: Pulmonary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28388439/celastrol-induced-nur77-interaction-with-traf2-alleviates-inflammation-by-promoting-mitochondrial-ubiquitination-and-autophagy
#8
Mengjie Hu, Qiang Luo, Gulimiran Alitongbieke, Shuyi Chong, Chenting Xu, Lei Xie, Xiaohui Chen, Duo Zhang, Yuqi Zhou, Zhaokai Wang, Xiaohong Ye, Lijun Cai, Fang Zhang, Huibin Chen, Fuquan Jiang, Hui Fang, Shanjun Yang, Jie Liu, Maria T Diaz-Meco, Ying Su, Hu Zhou, Jorge Moscat, Xiangzhi Lin, Xiao-Kun Zhang
Mitochondria play an integral role in cell death, autophagy, immunity, and inflammation. We previously showed that Nur77, an orphan nuclear receptor, induces apoptosis by targeting mitochondria. Here, we report that celastrol, a potent anti-inflammatory pentacyclic triterpene, binds Nur77 to inhibit inflammation and induce autophagy in a Nur77-dependent manner. Celastrol promotes Nur77 translocation from the nucleus to mitochondria, where it interacts with tumor necrosis factor receptor-associated factor 2 (TRAF2), a scaffold protein and E3 ubiquitin ligase important for inflammatory signaling...
April 6, 2017: Molecular Cell
https://www.readbyqxmd.com/read/28349980/celastrol-an-active-constituent-of-the-tcm-plant-tripterygium-wilfordii-hook-f-inhibits-prostate-cancer-bone-metastasis
#9
K Kuchta, Y Xiang, S Huang, Y Tang, X Peng, X Wang, Y Zhu, J Li, J Xu, Z Lin, T Pan
No abstract text is available yet for this article.
March 28, 2017: Prostate Cancer and Prostatic Diseases
https://www.readbyqxmd.com/read/28338993/dihydrocelastrol-inhibits-multiple-myeloma-cell-proliferation-and-promotes-apoptosis-through-erk1-2-and-il-6-stat3-pathways-in-vitro-and-in-vivo
#10
Liangning Hu, Huiqun Wu, Bo Li, Dongliang Song, Guang Yang, Gege Chen, Bingqian Xie, Zhijian Xu, Yong Zhang, Dandan Yu, Jun Hou, Wenqin Xiao, Xi Sun, Gaomei Chang, Yiwen Zhang, Lu Gao, Bojie Dai, Yi Tao, Jumei Shi, Weiliang Zhu
Multiple myeloma (MM) is the second most frequent malignant hematological disease. Dihydrocelastrol (DHCE) is synthesized by hydrogenated celastrol, a treterpene isolated from Chinese medicinal plant Tripterygium regelii. In this study, we first reported the anti-tumor activity of DHCE on MM cells. We found that DHCE could inhibit cell proliferation and promote apoptosis through caspase-dependent way in vitro. In addition, DHCE could inactivate the expression of interleukin (IL)-6 and downregulate the phosphorylation of extracellular regulated protein kinases (ERK1/2) and the signal transducer and activator of transcription 3 (STAT3) in MM...
May 1, 2017: Acta Biochimica et Biophysica Sinica
https://www.readbyqxmd.com/read/28247763/n-n-dimethyl-tertiary-amino-group-mediated-dual-pancreas-and-lung-targeting-therapy-against-acute-pancreatitis
#11
Shi Luo, Peiwen Li, Sha Li, Zhengwu Du, Xun Hu, Yao Fu, Zhirong Zhang
Acute pancreatitis (AP) is a sudden inflammation of the pancreas with high mortality rate worldwide. As a severe complication to AP, acute lung injury has been the major cause of death among patients with AP. Poor penetration across the blood pancreas barrier (BPB) and insufficient drug accumulation at the target site often result in poor therapeutic outcome. Our previous work successfully demonstrated a dual-specific targeting strategy to pancreas and lung using a phenolic propanediamine moiety. Inspired by this, a simplified ligand structure, N,N-dimethyl tertiary amino group, was covalently conjugated to celastrol (CLT) to afford tertiary amino conjugates via either an ester (CP) or an amide linkage (CTA)...
May 1, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28242743/advances-in-hypoxia-mediated-mechanisms-in-hepatocellular-carcinoma
#12
Xin Xin Xiong, Xin Yao Qiu, Dian Xing Hu, Xiao Qian Chen
Hepatocellular carcinoma (HCC) is the fifth most common and the third most deadly malignant tumor worldwide. Hypoxia and related oxidative stress are heavily involved in the process of HCC development and therapies. However, direct and accurate measuring oxygen concentration and evaluating hypoxic effects in HCC prove difficult. Moreover, the hypoxia-mediated mechanisms in HCC remain elusive. Here, we summarize recent major evidence of hypoxia in HCC lesions by measuring pO2, the clinical importance of hypoxic markers in HCC, and recent advances in hypoxia-related mechanisms and therapies in HCC...
February 27, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/28239352/celastrol-attenuates-multiple-sclerosis-and-optic-neuritis-in-an-experimental-autoimmune-encephalomyelitis-model
#13
Hongbin Yang, Chang Liu, Jie Jiang, Yuena Wang, Xiaoyu Zhang
This study was aimed to evaluate the effects of celastrol, a natural compound with multiple bioactivities, on multiple sclerosis and optic neuritis (ON) in rat experimental autoimmune encephalomyelitis (EAE). EAE was induced in Sprague Dawley rats using myelin basic protein, and the animals received daily intraperitoneal injections of celastrol or vehicle for 13 days. The EAE rats showed abnormal neurobehavior and inflammatory infiltration and demyelination in the spinal cord. Significantly upregulated mRNA expression of pro-inflammatory cytokines interferon-γ and interleukin-17 and downregulated anti-inflammatory cytokines interleukin-4 were found in the spinal cord of EAE rats...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28195223/celastrol-an-active-constituent-of-the-tcm-plant-tripterygium-wilfordii-hook-f-inhibits-prostate-cancer-bone-metastasis
#14
K Kuchta, Y Xiang, S Huang, Y Tang, X Peng, X Wang, Y Zhu, J Li, J Xu, Z Lin, T Pan
BACKGROUND: Treatment failure of prostate cancer (PCa) is often due to bone metastasis. Celastrol, an active constituent of Tripterygium wilfordii roots, has shown anti-tumor effects in previous studies in accordance with its indication in traditional Chinese medicine. METHODS: Using a PC-3 cell model, in vitro assays were performed to evaluate the effects of celastrol on proliferation, migration (wound healing assay), tissues invasion (Transwell-Matrigel penetration assay) and vascular endothelial growth factor (VEGF) secretion (enzyme-linked immunosorbent assay)...
June 2017: Prostate Cancer and Prostatic Diseases
https://www.readbyqxmd.com/read/28189063/the-nf-%C3%AE%C2%BAb-inhibitor-celastrol-attenuates-acute-hepatic-dysfunction-induced-by-cecal-ligation-and-puncture-in-rats
#15
Ghada S El-Tanbouly, Mohammed S El-Awady, Nermeen A Megahed, Hatem A Salem, Hassan A El-Kashef
Acute hepatic dysfunction associating sepsis is mediated mainly by toll-like receptor-4 (TLR-4)/nuclear factor kappa-B (NF-κB) inflammatory pathway. This study explores potential hepatoprotective effect of the NF-κB inhibitor celastrol in cecal ligation and puncture (CLP) model in rats. Protective effect of celastrol (1mg/kg, i.p., 1h before CLP) was illustrated after 24h by preventing CLP-induced hepatic histopathological changes and elevation in serum hepatic biomarkers [alanine aminotransferase (ALT), aspartate aminotransferase (AST), total bilirubin (TB) and gamma aminotransferase (γ-GT)] without affecting mortality...
March 2017: Environmental Toxicology and Pharmacology
https://www.readbyqxmd.com/read/28161417/celastrol-attenuates-mitochondrial-dysfunction-and-inflammation-in-palmitate-mediated-insulin-resistance-in-c3a-hepatocytes
#16
Mohamad Hafizi Abu Bakar, Mohamad Roji Sarmidi, Joo Shun Tan, Mohamad Norisham Mohamad Rosdi
Accumulating evidence indicates that mitochondrial dysfunction-induced inflammation is among the convergence points for the greatest hallmarks of hepatic insulin resistance. Celastrol, an anti-inflammatory compound from the root of Tripterygium Wilfordii has been reported to mitigate insulin resistance and inflammation in animal disease models. Nevertheless, the specific mechanistic actions of celastrol in modulating such improvements at the cellular level remain obscure. The present study sought to explore the mechanistic roles of celastrol upon insulin resistance induced by palmitate in C3A human hepatocytes...
March 15, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28129433/celastrol-ameliorates-cd-induced-neuronal-apoptosis-by-targeting-nox2-derived-ros-dependent-pp5-jnk-signaling-pathway
#17
Chong Xu, Xiaoxue Wang, Chenjian Gu, Hai Zhang, Ruijie Zhang, Xiaoqing Dong, Chunxiao Liu, Xiaoyu Hu, Xiang Ji, Shile Huang, Long Chen
Celastrol, a plant-derived triterpene, has neuroprotective benefit in the models of neurodegenerative disorders that are characterized by overproduction of reactive oxygen species (ROS). Recently, we have reported that cadmium (Cd) activates c-Jun N-terminal kinase (JNK) pathway leading to neuronal cell death by inducing ROS inactivation of protein phosphatase 5 (PP5), and celastrol prevents Cd-activated JNK pathway against neuronal apoptosis. Therefore, we hypothesized that celastrol could hinder Cd induction of ROS-dependent PP5-JNK signaling pathway from apoptosis in neuronal cells...
April 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/28128232/functional-characterization-of-nes-and-ges-responsible-for-the-biosynthesis-of-e-nerolidol-and-e-e-geranyllinalool-in-tripterygium-wilfordii
#18
Ping Su, Tianyuan Hu, Yujia Liu, Yuru Tong, Hongyu Guan, Yifeng Zhang, Jiawei Zhou, Luqi Huang, Wei Gao
Triptolide and celastrol, two principal bioactive compounds in Tripterygium wilfordii, are produced from geranylgeranyl diphosphate (GGPP) and farnesyl diphosphate ((E,E)-FPP) through terpenoid biosynthesis pathway. However, little is known about T. wilfordii terpene synthases which could competitively utilize GGPP and (E,E)-FPP as substrates, producing C15 and C20 tertiary alcohols. Here we firstly cloned the genes encoding nerolidol synthase (NES) and geranyllinalool synthases (GES1, GES2), which are responsible for the biosynthesis of (E)-nerolidol and (E,E)-geranyllinalool...
January 27, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28123944/celastrol-ameliorates-liver-metabolic-damage-caused-by-a-high-fat-diet-through-sirt1
#19
Yinliang Zhang, Chao Geng, Xiaoyan Liu, Meixia Li, Mingyue Gao, Xiaojun Liu, Fude Fang, Yongsheng Chang
OBJECTIVE: Celastrol was recently identified as a potential novel treatment for obesity. However, the effect of Celastrol on nonalcoholic fatty liver disease (NAFLD) remains elusive. The aim of this study is to evaluate the role of Celastrol in NAFLD. METHODS: Functional studies were performed using wild-type C57BL/6J (WT) mice and liver specific Sirt1-deficient (LKO) mice. The molecular mechanism was explored in primary mouse liver and primary hepatocytes. RESULTS: When WT mice receiving a high-fat diet (HFD) were treated with Celastrol, reductions in body weight, subcutaneous and visceral fat content, and liver lipid droplet formation were observed, along with reduced hepatic intracellular triglyceride and serum triglyceride, free fatty acid, and ALT concentrations...
January 2017: Molecular Metabolism
https://www.readbyqxmd.com/read/28119074/celastrol-attenuates-angiotensin-ii-mediated-human-umbilical-vein-endothelial-cells-damage-through-activation-of-nrf2-erk1-2-nox2-signal-pathway
#20
Miao Li, Xin Liu, Yongpeng He, Qingyin Zheng, Min Wang, Yu Wu, Yuanpeng Zhang, Chaoyun Wang
Angiotensin II (Ang II), as a crucial factor of endothelial dysfunction, participates in endothelial oxidative damage and inflammation, which is present in all cardiovascular disease (CVD). Celastrol, extracted from Trypterygiun wilfordii Hook F. ("Thunder of God Vine"), is a natural compound with antioxidant and anti-inflammatory activities. In this study, the protective effects of celastrol on human umbilical vein endothelial cell (HUVEC) injury induced by Ang II were observed and its mechanisms were elucidated...
February 15, 2017: European Journal of Pharmacology
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