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Celastrol

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https://www.readbyqxmd.com/read/29453086/pegylated-polyaminoacid-capped-mesoporous-silica-nanoparticles-for-mitochondria-targeted-delivery-of-celastrol-in-solid-tumors
#1
Ju Yeon Choi, Biki Gupta, Thiruganesh Ramasamy, Jee-Heon Jeong, Sung Giu Jin, Han-Gon Choi, Chul Soon Yong, Jong Oh Kim
The major goal of cancer chemotherapy is to maximize the therapeutic efficacy of anticancer drugs, while minimizing their associated side effects. Celastrol (CST), which is extracted from the traditional Chinese medicinal plant Tripterygium wilfordii, has been reported to exhibit significant anticancer effects in various in vitro and in vivo cancer models. Nanoparticulate drug delivery systems could be employed to preserve and enhance the pharmacological effects of CST in cancer cells. Among these, mesoporous silica nanoparticles (MSNs) are one of the most promising drug delivery systems...
February 11, 2018: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/29446727/natural-terpenoids-against-female-breast-cancer-a-5-year-recent-research
#2
Sylvin Benjamin Ateba, Sadrine Tchoukouegno Ngeu, Marie Alfrede Mvondo, Job Tchoumtchoua, Charline Florence Awounfack, Liselotte Krenn, Dieudonne Njamen
BACKGROUND: The approval of Taxol® in 1993 marked the great entrance of terpenoids in the anti-cancer area and this drug is still highly important in the treatment of refractory ovarian, breast and other cancers. Over decades, other prominent natural terpenoids have become indispensable for the modern pharmacotherapy of breast cancer. However, given the rapid evolution of drug resistance, effective treatments for advanced breast cancers requiring cytotoxic chemotherapy represent a major unmet clinical need...
February 13, 2018: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29445341/celastrol-alleviates-airway-hyperresponsiveness-and-inhibits-th17-responses-in-obese-asthmatic-mice
#3
Zeyu Zeng, Xixi Lin, Rongying Zheng, Hui Zhang, Weixi Zhang
Severe airway hyperresponsiveness (AHR) is a clinical feature of asthma, which has been associated with obesity and has shown a poor response to standard asthma treatments such as glucocorticoids. Numerous studies have shown that Interleukin (IL)-17 producing CD4 + T cells (Th17 cells), which could be inhibited by celastrol, is essential in mediating steroid-resistant AHR. The following study investigates the impact of celastrol and its mechanism on the regulation of AHR in murine model of obesity and asthma...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29436996/herbal-products-for-common-auto-inflammatory-disorders-novel-approaches
#4
Fawzi Mahomoodally, Shanoo Suroowan
Common auto-inflammatory disorders (CAIDs) induce considerable suffering over the world. A panoply of synthetic medications areis available for theirits management. Nonetheless, available drug classes are limited by adverse effects, low systemic absorption, and high costs. In addition, no cure exists for most CAIDs. Interestingly, herbal products present a tremendous potential for development as anti-inflammatory agents. In this endeavor, major scientific databases; Google Scholar, Pubmed, ScienceDirect, and Scopus were explored to highlight novel therapeutic approaches using herbal products for CAIDs prophylaxis, management, treatment, and prevention of relapse...
February 12, 2018: Combinatorial Chemistry & High Throughput Screening
https://www.readbyqxmd.com/read/29434967/celastrol-suppresses-the-proliferation-of-lung-adenocarcinoma-cells-by-regulating-microrna-24-and-microrna-181b
#5
Yun-Fei Yan, Han-Han Zhang, Qing Lv, Yue-Mei Liu, You-Jie Li, Bao-Sheng Li, Ping-Yu Wang, Wen-Jing Shang, Zhen Yue, Shu-Yang Xie
Cumulative evidence has indicated that celastrol may suppress cancer growth; however, the underlying mechanism requires further investigation. In the present study, A549 cells were treated with various concentrations of celastrol. Lung cancer cell proliferation was evaluated using an MTT assay and observed under a microscope. Cell apoptosis was detected by Annexin V fluorescein isothiocyanate/propidium iodide double-labeled flow cytometry. The results demonstrated that celastrol suppressed proliferation and induced apoptosis in a dose-independent manner...
February 2018: Oncology Letters
https://www.readbyqxmd.com/read/29429468/-research-advances-in-necrotizing-enterocolitis-in-neonates
#6
Xin Gan, Juan Li
Necrotizing enterocolitis (NEC) is a catastrophic disease caused by a variety of factors in neonates, especially preterm infants. Severe NEC has a high fatality rate, and most survivors may face short- and long-term adverse prognosis. Risk factors for NEC include preterm birth, non-breastfeeding, microbial abnormalities in the digestive tract, and ischemia-reperfusion injury. High-resolution abdominal ultrasound helps with the early diagnosis of NEC. The preventive measures for NEC include protecting the intestinal mucosa through nutritional intervention, interfering with intestinal injury signals, changing intestinal microflora, and performing early minimal enteral nutrition...
February 2018: Zhongguo Dang Dai Er Ke za Zhi, Chinese Journal of Contemporary Pediatrics
https://www.readbyqxmd.com/read/29421513/dihydro-%C3%AE-agarofurans-from-the-roots-of-the-australian-endemic-rainforest-tree-maytenus-bilocularis-act-as-leucine-transport-inhibitors
#7
Mario Wibowo, Qian Wang, Jeff Holst, Jonathan M White, Andreas Hofmann, Rohan A Davis
Phytochemical studies of the roots of the Australian plant, Maytenus bilocularis, resulted in the identification of six previously undescribed dihydro-β-agarofuran sesquiterpenoids, bilocularins D-I, along with three known natural products, namely 1α,2α,6β,15-tetraacetoxy-9β-benzoyloxydihydro-β-agarofuran, pristimerin, and celastrol. The structures of all compounds were characterized via analysis of 1D/2D NMR and MS data. The absolute configuration of bilocularin D was defined by X-ray crystallography analysis...
January 30, 2018: Phytochemistry
https://www.readbyqxmd.com/read/29398521/the-effect-of-celastrol-on-the-ocular-hypertension-induced-degeneration-of-retinal-ganglion-cells
#8
Lei Gu, Jacky M K Kwong, Daniel Yadegari, Fei Yu, Joseph Caprioli, Natik Piri
Celastrol, a quinine methide triterpene extracted from the perennial vine Tripterygium wilfordii, has been identified as a neuroprotective agent in various models of neurodegenerative disorders. We have reported earlier that systemic and intravitreal administration of celastrol stimulate the survival of retinal ganglion cells (RGCs) injured by optic nerve crush (ONC) and that mechanisms underlying celastrol׳s RGC protection may be associated with inhibition of TNF-alpha-mediated cell death. The present study evaluates the effect of celastrol on the survival of RGCs injured by ocular hypertension...
February 1, 2018: Neuroscience Letters
https://www.readbyqxmd.com/read/29394529/regulation-of-tgf-%C3%AE-smad-mediated-epithelial-mesenchymal-transition-by-celastrol-provides-protection-against-bleomycin-induced-pulmonary-fibrosis
#9
Thomas Divya, Bakthavatchalam Velavan, Ganapasam Sudhandiran
The respiratory disease pulmonary fibrosis (PF), which is characterized by scar formation throughout the lung, imposes a serious health burden. No effective drug without side effects has been proven to prevent this fatal lung disease. In this context, the present study was undertaken to elucidate the protective effect of celastrol, a quinine methide pentacyclic triterpenoid from a Chinese medicinal plant 'thunder God vine' against bleomycin (BLM)-induced PF. We also attempted to study how the cytokine transforming growth factor-β (TGF-β) stimulates fibrosis through the induction of epithelial-mesenchymal transition (EMT) and the role of celastrol in regulating EMT...
February 2, 2018: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/29394256/the-natural-anti-tumor-compound-celastrol-targets-a-myb-c-ebp%C3%AE-p300-transcriptional-module-implicated-in-myeloid-gene-expression
#10
Anna Coulibaly, Astrid Haas, Simone Steinmann, Anke Jakobs, Thomas J Schmidt, Karl-Heinz Klempnauer
Myb is a key regulator of hematopoietic progenitor cell proliferation and differentiation and has emerged as a potential target for the treatment of acute leukemia. Using a myeloid cell line with a stably integrated Myb-inducible reporter gene as a screening tool we have previously identified Celastrol, a natural compound with anti-tumor activity, as a potent Myb inhibitor that disrupts the interaction of Myb with the co-activator p300. We showed that Celastrol inhibits the proliferation of acute myeloid leukemia (AML) cells and prolongs the survival of mice in an in vivo model of AML, demonstrating that targeting Myb with a small-molecule inhibitor is feasible and might have potential as a therapeutic approach against AML...
2018: PloS One
https://www.readbyqxmd.com/read/29382150/cloning-expression-analysis-and-functional-characterization-of-squalene-synthase-sqs-from-tripterygium-wilfordii
#11
Bin Zhang, Yan Liu, Mengmeng Chen, Juntao Feng, Zhiqing Ma, Xing Zhang, Chuanshu Zhu
Celastrol is an active triterpenoid compound derived from Tripterygium wilfordii which is well-known as a traditional Chinese medicinal plant. Squalene synthase has a vital role in condensing two molecules of farnesyl diphosphate to form squalene, a key precursor of triterpenoid biosynthesis. In the present study, T. wilfordii squalene synthase (TwSQS) was cloned followed by prokaryotic expression and functional verification. The open reading frame cDNA of TwSQS was 1242 bp encoding 413 amino acids. Bioinformatic and phylogenetic analysis showed that TwSQS had high homology with other plant SQSs...
January 29, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29355035/simultaneous-targeting-therapy-for-lung-metastasis-and-breast-tumor-by-blocking-the-nf-%C3%AE%C2%BAb-signaling-pathway-using-celastrol-loaded-micelles
#12
Yue Zhao, Yanan Tan, Tingting Meng, Xuan Liu, Yun Zhu, Yun Hong, Xiqin Yang, Hong Yuan, Xuan Huang, Fuqiang Hu
Metastasis is one of the major obstacles for successful therapy of breast tumor. To inhibit the metastasis and growth of breast tumor simultaneously, a Celastrol (Cela) loaded glucolipid-like conjugates (CSOSA/Cela) with αvβ3-ligand Tetraiodothyroacetic acid (TET) modification (TET-CSOSA/Cela) were established to block nuclear factor-kappa B (NF-κB) signaling pathway. The distribution of TET-CSOSA was remarkably increased in lung metastasis and primary tumor of 4T1 tumor-bearing mice by means of αvβ3 receptor-mediated interaction...
November 2018: Drug Delivery
https://www.readbyqxmd.com/read/29274099/effects-of-celastrol-on-tau-hyperphosphorylation-and-expression-of-hsf-1-and-hsp70-in-sh-sy5y-neuroblastoma-cells-induced-by-amyloid-%C3%AE-peptides
#13
Fanfan Cao, Ying Wang, Bin Peng, Xue Zhang, Denghai Zhang, Limin Xu
To observe the effects of celastrol on Tau hyperphosphorylation induced by amyloid-β peptides (Aβ) in SH-SY5Y neuroblastoma cells, the changes of Tau hyperphosphorylation and the expression of heat shock protein 90 (HSP90), HSP70 and heat shock factor 1 (HSF-1) in SH-SY5Y cells treated with Aβ1-42 and celastrol were measured. Tau hyperphosphorylation and HSP90 expression induced by Aβ1-42 was also measured by western blotting after HSP70 or HSF-1 knockdown by siRNA. The interaction between HSP70 and Tau or HSP70 and carboxyl terminus of HSP70 interacting protein (CHIP) was measured by Co-immunoprecipitiation...
December 22, 2017: Biotechnology and Applied Biochemistry
https://www.readbyqxmd.com/read/29231066/synthesis-and-characterisation-of-celastrol-derivatives-as-potential-anticancer-agents
#14
Hong-Jian Zhang, Guo-Rui Zhang, Hu-Ri Piao, Zhe-Shan Quan
In the present study, three series of novel celastrol derivatives were designed and synthesised by modifying the carboxylic acid at the 20th position with amino acid, amine, and triazole derivatives. All the synthesised compounds were screened for their anticancer activities using MTT assay against AGS, MGC-803, SGC-7901, HCT-116, A549, HeLa, BEL-7402, and HepG-2 cell lines. Most of the synthesised compounds exhibited potent antiproliferative effects. The most promising compound 3-Hydroxy-9β,13α-dimethyl-2-oxo-24,25,26-trinoroleana-1(10),3,5,7-tetraen-29-oic amide, N-(R)-methyl-3-(1H-indol-2-yl)propanoate (11) showed considerable high anticancer activity against AGS cell lines, with an IC50 value of 0...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/29202812/celastrol-improves-self-renewal-and-differentiation-of-human-tendon-derived-stem-cells-by-suppressing-smad7-through-hypoxia
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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