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Celastrol

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https://www.readbyqxmd.com/read/27920521/celastrol-nanomicelles-attenuate-cytokine-secretion-in-macrophages-and-inhibit-macrophage-induced-corneal-neovascularization-in-rats
#1
Zhanrong Li, Jingguo Li, Lei Zhu, Ying Zhang, Junjie Zhang, Lin Yao, Dan Liang, Liya Wang
The aim of the present study was to investigate the inhibitory effects of celastrol-loaded nanomicelles (CNMs) on activated macrophage-induced corneal neovascularization (CNV) in rats and cytokine secretion in macrophages. Using an angiogenesis assay in vitro, we detected the effects of CNMs on human umbilical vein endothelial cell (HUVEC) migration and invasion. In addition, the expression levels of cytokines secreted from hypoxia-induced macrophages were assessed through cytokine array analysis. The expression of hypoxia-inducible factors-1α (HIF-1α), nuclear factor-kappa B p65 (NF-κB p65), phospho-nuclear factor-kappa B p65 (phospho-NF-κB p65), p38 mitogen-activated protein kinase (p38 MAPK), phospho-p38 MAPK, extracellular signal-regulated kinase 1/2 (ERK1/2), and phospho-ERK1/2 was analyzed by western blotting...
2016: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/27919190/investigation-of-the-influence-of-glycyrrhizin-on-the-pharmacokinetics-of-celastrol-in-rats-using-lc-ms-and-its-potential-mechanism
#2
Guangkui Yan, Hanhua Zhang, Wei Wang, Yuan Li, Chenghuang Mao, Mingqiao Fang, Xianhong Yi, Jingdong Zhang
1. The aim of this study was to investigate the effects of glycyrrhizin on the pharmacokinetics of celastrol in rats. 2. Twelve male Sprague-Dawley rats were randomly assigned to two groups: control group and test group. Test group was pretreated with glycyrrhizin at a dose of 100 mg/kg/day for 10 days, and then the two groups were orally administered with celastrol at a dose of 1 mg/kg. The concentration of celastrol was determined using a sensitive and reliable LC-MS method. 3. The results showed that glycyrrhizin could significantly decrease the plasma concentration (from 64...
December 5, 2016: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/27910878/lipids-celastrol-protects-against-fatty-liver-through-sirt1
#3
Charlotte Ridler
No abstract text is available yet for this article.
December 2, 2016: Nature Reviews. Endocrinology
https://www.readbyqxmd.com/read/27900015/celastrol-negatively-regulates-cell-invasion-and-migration-ability-of-human-osteosarcoma-via-downregulation-of-the-pi3k-akt-nf-%C3%AE%C2%BAb-signaling-pathway-in-vitro
#4
Xiaolong Yu, Qiang Wang, Xin Zhou, Changlin Fu, Ming Cheng, Runsheng Guo, Hucheng Liu, Bin Zhang, Min Dai
Osteosarcoma (OS) is a primary malignant tumor of the bone, with a tendency to metastasize early. Despite the advances in treatment options, more than 30% of patients develop distant metastases, and the prognosis of these patients with metastases is extremely poor. Celastrol has been demonstrated to manifest multiple pharmacological activities, including induction of apoptosis in numerous types of cancer cell lines. Our previous studies have also suggested that Celastrol is capable of inducing apoptosis of human osteosarcoma cells via the mitochondrial-dependent pathway...
November 2016: Oncology Letters
https://www.readbyqxmd.com/read/27891586/celastrol-attenuates-cadmium-induced-neuronal-apoptosis-via-inhibiting-ca-2-camkii-dependent-akt-mtor-pathway
#5
Ruijie Zhang, Yu Zhu, Xiaoqing Dong, Beibei Liu, Nana Zhang, Xiaoxue Wang, Lei Liu, Chong Xu, Shile Huang, Long Chen
Cadmium (Cd), an environmental and industrial pollutant, affects the nervous system and consequential neurodegenerative disorders. Recently we have shown that celastrol prevents Cd-induced neuronal cell death partially by suppressing Akt/mTOR pathway. However, the underlying mechanism remains to be elucidated. Here we show that celastrol attenuated Cd-elevated intracellular free calcium ([Ca(2+) ]i ) level and apoptosis in neuronal cells. Celastrol prevented Cd-induced neuronal apoptosis by inhibiting Akt-mediated mTOR pathway, as inhibition of Akt with Akt inhibitor X or ectopic expression of dominant negative Akt reinforced celastrol's prevention of Cd-induced phosphorylation of S6K1/4E-BP1 and cell apoptosis...
November 27, 2016: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/27881165/comparative-analysis-of-four-terpenoids-in-root-and-cortex-of-tripterygium-wilfordii-radix-by-different-drying-methods
#6
Tuanjie Wang, Fei Shen, Shulan Su, Yongliang Bai, Sheng Guo, Hui Yan, Tao Ji, Yanyan Wang, Dawei Qian, Jin-Ao Duan
BACKGROUND: Tripterygium wilfordii Radix, a well-known traditional medicine in china which is used for treatment of inflammation, pain, tumor and immune regulation for centuries in china, accompany with the serious toxic side effects. This study was carried out for simultaneously analyzing the four main components (triptolide, triptophenolide, demethylzeylasteral and celastrol) in Tripterygium wilfordii Radix under different drying processes, which was important for reducing the toxicity and quality control of Tripterygium wilfordii Radix in future...
November 23, 2016: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/27864779/activity-of-novel-inhibitors-of-staphylococcus-aureus-biofilms
#7
Seung-Gyun Woo, So-Yeon Lee, So-Min Lee, Kyoung-Hee Lim, Eun-Ju Ha, Yong-Bin Eom
Staphylococcus aureus is one of the most important pathogens causing chronic biofilm infections. These are becoming more difficult to treat owing to drug resistance, particularly because S. aureus biofilms limit the efficacy of antimicrobial agents, leading to high morbidity and mortality. In the present study, we screened for inhibitors of S. aureus biofilm formation using a natural product library from the Korea Chemical Bank (KCB). Screening by crystal violet-based biomass staining assay identified hit compounds...
November 18, 2016: Folia Microbiologica
https://www.readbyqxmd.com/read/27847245/celastrol-inhibits-dengue-virus-replication-via-up-regulating-type-i-interferon-and-downstream-interferon-stimulated-responses
#8
Jung-Sheng Yu, Chin-Kai Tseng, Chun-Kuang Lin, Yao-Chin Hsu, Yu-Hsuan Wu, Ching-Liang Hsieh, Jin-Ching Lee
ETHNOPHARMACOLOGICAL RELEVANCE AND AIM OF THE STUDY: Tripterygium wilfordii (lei gong teng; Thunder of God Vine), a member of the Celastraceae family, is a medicinal plant used to treat a range of illnesses. Celastrol is a quinone methide triterpene and the most abundant bioactive constituent isolated from the root extracts of T. wilfordii. Previous studies have shown that celastrol exhibits antiviral activity against HIV and SARS-CoV. To date, no investigations of the anti-DENV activity of celastrol have been reported...
November 12, 2016: Antiviral Research
https://www.readbyqxmd.com/read/27823626/plant-derived-triterpene-celastrol-ameliorates-oxygen-glucose-deprivation-induced-disruption-of-endothelial-barrier-assembly-via-inducing-tight-junction-proteins
#9
Dan Luo, Jia Zhao, Jianhui Rong
BACKGROUND: The integrity and functions of blood-brain barrier (BBB) are regulated by the expression and organization of tight junction proteins. OBJECTIVE: The present study was designed to explore whether plant-derived triterpenoid celastrol could regulate tight junction integrity in murine brain endothelial bEnd3 cells. METHODS: We disrupted the tight junctions between endothelial bEnd3 cells by oxygen glucose deprivation (OGD). We investigated the effects of celastrol on the permeability of endothelial monolayers by measuring transepithelial electrical resistance (TEER)...
December 1, 2016: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/27821810/investigating-the-mechanism-of-hepatocellular-carcinoma-progression-by-constructing-genetic-and-epigenetic-networks-using-ngs-data-identification-and-big-database-mining-method
#10
Cheng-Wei Li, Ping-Yao Chang, Bor-Sen Chen
The mechanisms leading to the development and progression of hepatocellular carcinoma (HCC) are complicated and regulated genetically and epigenetically. The recent advancement in high-throughput sequencing has facilitated investigations into the role of genetic and epigenetic regulations in hepatocarcinogenesis. Therefore, we used systems biology and big database mining to construct genetic and epigenetic networks (GENs) using the information about mRNA, miRNA, and methylation profiles of HCC patients. Our approach involves analyzing gene regulatory networks (GRNs), protein-protein networks (PPINs), and epigenetic networks at different stages of hepatocarcinogenesis...
November 4, 2016: Oncotarget
https://www.readbyqxmd.com/read/27819370/competitive-profiling-of-celastrol-targets-in-human-cervical-cancer-hela-cells-via-quantitative-chemical-proteomics
#11
Yiqing Zhou, Weichao Li, Mingli Wang, Xixi Zhang, Haibing Zhang, Xiaofeng Tong, Youli Xiao
Celastrol, isolated from the traditional Chinese medicinal herb Tripterygium wilfordii Hook. f. (Thunder God's Vine), has been used to treat cancer, chronic inflammatory, autoimmune and other human diseases. However, to date, the protein targets and the mechanism of action of celastrol have remained elusive. In this study, we find that celastrol can react with protein thiols in a unique covalent and reversible manner, while protein denaturing disrupts the interaction. Through a competitive chemoproteomics approach utilizing a cysteine-targeting activity-based probe, we report the proteome-wide quantitative profiling of cellular targets of celastrol in human cervical cancer HeLa cells...
November 7, 2016: Molecular BioSystems
https://www.readbyqxmd.com/read/27774648/phytoconstituents-as-pharmacotherapeutics-in-rheumatoid-arthritis-challenges-and-scope-of-nano-submicromedicine-in-its-effective-delivery
#12
REVIEW
Mahfoozur Rahman, Sarwar Beg, Amita Verma, Fahad A Al Abbasi, Firoz Anwar, Sumant Saini, Sohail Akhter, Vikas Kumar
OBJECTIVES: The present review explores the therapeutic application of herbals in rheumatoid arthritis (RA) therapy, and how nano/submicromedicine can be fit in the scope of its therapeutic delivery in RA has been addressed. KEY FINDINGS: Incorporation of bioactive such as polyphenols, thymoquinone, resveratrol, hesperidin, curcumin, celastrol and gambogic acid in a dose-dependent manner showed quite high efficacy for the treatment of RA. It can be attributed to their targeting ability against various inflammatory mediators including nitric oxide (NO), cytokines, chemokines, adhesion molecules, NF-kβ, lipoxygenase (LOXs) and arachidonic acid (AA)...
October 24, 2016: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/27768597/celastrol-increases-osteosarcoma-cell-lysis-by-%C3%AE-%C3%AE-t-cells-through-up-regulation-of-death-receptors
#13
Zhaoxu Li, Junzhe Zhang, Jicun Tang, Ruiying Wang
γδ T cells has been shown to exhibit profound antitumor effects in a broad range of tumor entities, including OS. However, resistance to γδ T cells is a serious problem in the management of OS. This study investigates the impact of celastrol on the expression of death receptors 4/5 (DR4/5) on OS cell lines (HOS, U2OS) and cancer cell lysis by γδ T cells. The results showed that celastrol increased transcription of DR4/5 in HOS and U2OS, leading to increased cell surface, and total DR4/5 protein expression...
October 19, 2016: Oncotarget
https://www.readbyqxmd.com/read/27765370/resveratrol-piperine-and-apigenin-differ-in-their-nadph-oxidase-inhibitory-and-reactive-oxygen-species-scavenging-properties
#14
Scott Whitehouse, Pei-Lin Chen, Anna L Greenshields, Mat Nightingale, David W Hoskin, Karen Bedard
BACKGROUND: Many plant-derived chemicals have been studied for their potential benefits in ailments including inflammation, cancer, neurodegeneration, and cardiovascular disease. The health benefits of phytochemicals are often attributed to the targeting of reactive oxygen species (ROS). However, it is not always clear whether these agents act directly as antioxidants to remove ROS, or whether they act indirectly by blocking ROS production by enzymes such as NADPH oxidase (NOX) enzymes, or by influencing the expression of cellular pro- and anti- oxidants...
November 15, 2016: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/27764525/celastrol-prevents-cadmium-induced-neuronal-cell-death-by-blocking-mitochondrial-ros-inactivation-of-ampk-and-activation-of-mtor-pathway
#15
Ruijie Zhang, Nana Zhang, Hai Zhang, Chunxiao Liu, Xiaoqing Dong, Xiaoxue Wang, Yu Zhu, Chong Xu, Lei Liu, Sijun Yang, Shile Huang, Long Chen
BACKGROUND AND PURPOSE: Increasing evidence has suggested cadmium (Cd), as an inducer of reactive oxygen species (ROS), is a potential pathogenic factor in human neurodegenerative diseases. Thus, it is important to find effective interventions for Cd-induced oxidative stress in the central nervous system. The purpose of this study was to determine whether and how celastrol, a plant-derived triterpene, could mitigate Cd-induced ROS and cell death in neuronal cells. EXPERIMENTAL APPROACH: PC12, SH-SY5Y cells and primary murine neurons were chosen as a model to study celastrol neuroprotection against Cd-poisoning...
October 20, 2016: British Journal of Pharmacology
https://www.readbyqxmd.com/read/27673633/effects-of-celastrol-on-bv-2-microglial-cells-exposed-to-in-vitro-hypoxia
#16
V Rački, M Marcelić, J Mršić-Pelčić, N Kučić
No abstract text is available yet for this article.
October 6, 2016: Clinical Therapeutics
https://www.readbyqxmd.com/read/27671821/celastrol-and-its-role-in-controlling%C3%A2-chronic-diseases
#17
Shivaprasad H Venkatesha, Kamal D Moudgil
Celastrol, a triterpenoid derived from traditional Chinese medicinal plants, has anti-inflammatory, antioxidant, and anticancer activities. Celastrol has shown preventive/therapeutic effects in experimental models of several chronic diseases. These include, chronic inflammatory and autoimmune diseases (e.g., rheumatoid arthritis, multiple sclerosis, systemic lupus erythematosus, inflammatory bowel disease, and psoriasis), neurodegenerative disorders (e.g., Alzheimer's disease, Parkinson's disease, and Amyotrophic lateral sclerosis), atherosclerosis, obesity, Type 2 diabetes, and cancer...
2016: Advances in Experimental Medicine and Biology
https://www.readbyqxmd.com/read/27658784/the-ros-derived-mitochondrial-respirstion-not-from-nadph-oxidase-plays-key-role-in-celastrol-against-angiotensin-ii-mediated-hepg2-cell-proliferation
#18
Xin Liu, Rui-Wei Gao, Miao Li, Chun-Feng Si, Yong-Peng He, Min Wang, Ying Yang, Qing-Yin Zheng, Chao-Yun Wang
Angiotensin II (AngII) is an important factor that promotes the proliferation of cancer cells, whereas celastrol exhibits a significant antitumor activity in various cancer models. Whether celastrol can effectively suppress AngII mediated cell proliferation remains unknown. In this study, we studied the effect of celastrol on AngII-induced HepG2 cell proliferation and evaluated its underlying mechanism. The results revealed that AngII was able to significantly promote HepG2 cell proliferation via up-regulating AngII type 1 (AT1) receptor expression, improving mitochondrial respiratory function, enhancing nicotinamide adenine dinucleotide phosphate (NADPH) oxidase activity, increasing the levels of reactive oxygen species (ROS) and pro-inflammatory cytokines...
November 2016: Apoptosis: An International Journal on Programmed Cell Death
https://www.readbyqxmd.com/read/27647369/optimization-and-biological-evaluation-of-celastrol-derivatives-as-hsp90-cdc37-interaction-disruptors-with-improved-druglike-properties
#19
Fen Jiang, Hui-Jie Wang, Qi-Chao Bao, Lei Wang, Yu-Hui Jin, Qiong Zhang, Di Jiang, Qi-Dong You, Xiao-Li Xu
Heat shock protein 90 (Hsp90) as a molecular target for oncology therapeutics has attracted much attention in the last decade. The Hsp90 multichaperone complex has important roles in the growth and/or survival of cancer cells. Cdc37, as a cochaperone, associates kinase clients to Hsp90 and promotes the development of malignant tumors. Disrupting the Hsp90-Cdc37 interaction provides an alternative strategy to inhibit the function of Hsp90 for cancer therapy. Celastrol, as a natural product, can disrupt the Hsp90-Cdc37 interaction and induce degradation of kinase clients...
November 1, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27609747/targeting-cancer-stem-cells-and-signaling-pathways-by-phytochemicals-novel-approach-for-breast-cancer-therapy
#20
Prasad R Dandawate, Dharmalingam Subramaniam, Roy A Jensen, Shrikant Anant
Breast cancer is the most common form of cancer diagnosed in women worldwide and the second leading cause of cancer-related deaths in the USA. Despite the development of newer diagnostic methods, selective as well as targeted chemotherapies and their combinations, surgery, hormonal therapy, radiotherapy, breast cancer recurrence, metastasis and drug resistance are still the major problems for breast cancer. Emerging evidence suggest the existence of cancer stem cells (CSCs), a population of cells with the capacity to self-renew, differentiate and be capable of initiating and sustaining tumor growth...
October 2016: Seminars in Cancer Biology
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