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Celastrol

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https://www.readbyqxmd.com/read/28782773/triptolide-and-celastrol-loaded-silk-fibroin-nanoparticles-show-synergistic-effect-against-human-pancreatic-cancer-cells
#1
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 7, 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
#2
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
#3
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
#4
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
#5
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
#6
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
#7
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...
June 16, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28679864/celastrol-ameliorates-inflammation-through-inhibition-of-nlrp3-inflammasome-activation
#8
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
https://www.readbyqxmd.com/read/28673005/celastrol-inhibits-migration-and-invasion-through-blocking-the-nf-%C3%AE%C2%BAb-pathway-in-ovarian-cancer-cells
#9
Zhongye Wang, Zhenyuan Zhai, Xiulan Du
Metastatic ovarian cancer is a major clinical challenge with poor prognosis and high mortality. Celastrol is a natural compound that has exhibits antiproliferative activity; however, its effects on metastasis-related phenotypes in ovarian cancer models are unclear. In the current study, the anti-invasive activities and associated signaling pathways of celastrol were determined in ovarian cancer cells. Cell proliferation was tested by MTT assay. Cell migration was detected by wound healing and Transwell assays, while cell invasion was detected by a Matrigel-coated Transwell method...
July 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28664158/celastrol-a-spectrum-of-treatment-opportunities-in-chronic-diseases
#10
REVIEW
Rita Cascão, João E Fonseca, Luis F Moita
The identification of new bioactive compounds derived from medicinal plants with significant therapeutic properties has attracted considerable interest in recent years. Such is the case of the Tripterygium wilfordii (TW), an herb used in Chinese medicine. Clinical trials performed so far using its root extracts have shown impressive therapeutic properties but also revealed substantial gastrointestinal side effects. The most promising bioactive compound obtained from TW is celastrol. During the last decade, an increasing number of studies were published highlighting the medicinal usefulness of celastrol in diverse clinical areas...
2017: Frontiers in Medicine
https://www.readbyqxmd.com/read/28621943/natural-products-discovered-in-a-high-throughput-screen-identified-as-inhibitors-of-rgs17-and-as-cytostatic-and-cytotoxic-agents-for-lung-and-prostate-cancer-cell-lines
#11
Christopher R Bodle, Duncan I Mackie, Michael P Hayes, Josephine H Schamp, Michael R Miller, Michael D Henry, Jonathan A Doorn, Jon C D Houtman, Michael A James, David L Roman
Regulator of G Protein Signaling (RGS) 17 is an overexpressed promoter of cancer survival in lung and prostate tumors, the knockdown of which results in decreased tumor cell proliferation in vitro. Identification of drug-like molecules inhibiting this protein could ameliorate the RGS17's pro-tumorigenic effect. Using high-throughput screening, a chemical library containing natural products was interrogated for inhibition of the RGS17-Gαo interaction. Initial hits were verified in control and counter screens...
July 28, 2017: Journal of Natural Products
https://www.readbyqxmd.com/read/28587825/synthesis-of-3-and-29-substituted-celastrol-derivatives-and-structure-activity-relationship-studies-of-their-cytotoxic-activities
#12
Wei-Guang Shan, Han-Guang Wang, Yan Chen, Rui Wu, Yan-Tao Wen, Li-Wen Zhang, You-Min Ying, Jian-Wei Wang, Zha-Jun Zhan
A series of 3-carbamate and 29-ester celastrol derivatives (compounds 1-26) were designed and synthesized. These analogues were evaluated for their cytotoxic activities against several cancer cell lines. Cytotoxicity data revealed that the properties of substituents and substitution position had important influence on cytotoxic activity. Modification of C-3 hydroxyl with size-limited groups did not reduce the activity obviously. The introduction of polarity group like piperazine could improve the solubility...
August 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28542649/evaluation-of-connectivity-map-discovered-celastrol-as-a-radiosensitizing-agent-in-a-murine-lung-carcinoma-model-feasibility-study-of-diffusion-weighted-magnetic-resonance-imaging
#13
Hong Young Jun, Tae-Hoon Kim, Jin Woo Choi, Young Hwan Lee, Kang Kyoo Lee, Kwon-Ha Yoon
This study was designed to identify potential radiosensitizing (RS) agents for combined radio- and chemotherapy in a murine model of human lung carcinoma, and to evaluate the in vivo effect of the RS agents using diffusion-weighted magnetic resonance imaging (DW-MRI). Radioresistance-associated genes in A549 and H460 cells were isolated on the basis of their gene expression profiles. Celastrol was selected as a candidate RS by using connectivity mapping, and its efficacy in lung cancer radiotherapy was tested...
2017: PloS One
https://www.readbyqxmd.com/read/28532223/preliminary-study-on-fabrication-characterization-and-synergistic-anti-lung-cancer-effects-of-self-assembled-micelles-of-covalently-conjugated-celastrol-polyethylene-glycol-ginsenoside-rh2
#14
Peng Li, XiaoYue Zhou, Ding Qu, Mengfei Guo, Chenyi Fan, Tong Zhou, Yang Ling
The aim of this study was to develop an amphipathic polyethylene glycol (PEG) derivative that was bi-terminally modified with celastrol and ginsenoside Rh2 (Celastrol-PEG-G Rh2). Such derivative was capable of forming novel, celastrol-loaded polymeric micelles (CG-M) for endo/lysosomal delivery and thereby synergistic treatment of lung cancer. Celastrol-PEG-G Rh2 with a yield of 55.6% was first synthesized and characterized. Its critical micellar concentration was 1 × 10(-5 )M, determined by pyrene entrapment method...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28522217/celastrol-inhibits-chondrosarcoma-proliferation-migration-and-invasion-through-suppression-cip2a-c-myc-signaling-pathway
#15
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...
May 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
#16
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
#17
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
#18
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...
July 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
#19
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...
June 5, 2017: Toxicology Letters
https://www.readbyqxmd.com/read/28397045/celastrol-protects-tgf-%C3%AE-1-induced-endothelial-mesenchymal-transition
#20
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
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