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Celastrol

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https://www.readbyqxmd.com/read/29902110/celastrol-enhances-atoh1-expression-in-inner-ear-stem-cells-and-promotes-their-differentiation-into-functional-auditory-neuronal-like-cells
#1
Zhao Han, Yu-Yan Gu, Ning Cong, Rui Ma, Fang-Lu Chi
We aimed to investigate the beneficial effect of Celastrol on inner ear stem cells and potential therapeutic value for hearing loss. The inner ear stem cells were isolated and characterized from utricular sensory epithelium of adult mice. The stemness was evaluated by sphere formation assay. The relative expressions of Atoh1, MAP-2 and Myosin VI were measured by RT-PCR and immunoblotting. The up-regulation of MAP-2 was also analysed with immunofluorescence. The in vitro neuronal excitability was interrogated by calcium oscillation...
June 14, 2018: Organogenesis
https://www.readbyqxmd.com/read/29901111/dihydrocelastrol-exerts-potent-antitumor-activity-in-mantle-cell-lymphoma-cells-via-dual-inhibition-of-mtorc1-and-mtorc2
#2
Yongsheng Xie, Bo Li, Wenxuan Bu, Lu Gao, Yong Zhang, Xiucai Lan, Jun Hou, Zhijian Xu, Shuaikang Chang, Dandan Yu, Bingqian Xie, Yingcong Wang, Houcai Wang, Yiwen Zhang, Xiaosong Wu, Weiliang Zhu, Jumei Shi
Mantle cell lymphoma (MCL) is a distinct and highly aggressive subtype of B-cell non-Hodgkin lymphoma. Dihydrocelastrol (DHCE) is a dihydro-analog of celastrol, which is isolated from the traditional Chinese medicinal plant Tripterygium wilfordii. The present study aimed to investigate the effects of DHCE treatment on MCL cells, and to determine the mechanism underlying its potent antitumor activity in vitro and in vivo using the Cell Counting kit-8 assay, clonogenic assay, apoptosis assay, cell cycle analysis, immunofluorescence staining, western blotting and tumor xenograft models...
June 12, 2018: International Journal of Oncology
https://www.readbyqxmd.com/read/29882724/celastrol-as-a-pentacyclic-triterpenoid-with-chemopreventive-properties
#3
Priya Yadav, Vishal Jaswal, Ajay Sharma, Dharambir Kashyap, Hardeep S Tuli, Vivek K Garg, Shonkor K Das, R Srinivas
Celastrol is a highly investigated anticancer moiety. It is a pentacyclic triterpenoid, isolated several decades ago with promising role in chemoprevention. Celastrol has been found to target multiple proinflammatory, angiogenic and metastatic proteins. Inhibition of these targets results in significant reduction of cancer growth, survival and metastasis. This review summarizes the varied molecular targets of celastrol along with insight into the various recently published clinical, preclinical and industrial patents (2011-2017)...
June 8, 2018: Pharmaceutical Patent Analyst
https://www.readbyqxmd.com/read/29873512/proteostasis-as-a-therapeutic-target-in-glomerular-injury-associated-with-mutant-alpha-actinin-4
#4
Albert Yee, Joan Papillon, Julie Guillemette, Daniel R Kaufman, Chris R J Kennedy, Andrey V Cybulsky
Mutations in alpha-actinin-4 (actinin-4) result in hereditary focal segmental glomerulosclerosis (FSGS) in humans. Actinin-4 mutants induce podocyte injury due to dysregulation of the cytoskeleton and proteotoxicity. Injury may be associated with endoplasmic reticulum (ER) stress and polyubiquitination of proteins. We assessed if the chemical chaperone, 4-phenylbutyric acid (4-PBA) can ameliorate the proteotoxicity of an actinin-4 mutant. Actinin-4 K255E, which causes FSGS in humans (K256E in the mouse), showed enhanced ubiquitination, accelerated degradation, aggregate formation, and enhanced association with F-actin in glomerular epithelial cells (GECs)...
June 6, 2018: American Journal of Physiology. Renal Physiology
https://www.readbyqxmd.com/read/29793976/-nox2-cybb-deficiency-affects-zebrafish-retinotectal-connectivity
#5
Cory J Weaver, Aslihan Terzi, Haley Roeder, Theodore Gurol, Qing Deng, Yuk Fai Leung, Daniel M Suter
NADPH oxidases (Nox)-derived reactive oxygen species (ROS) have been linked to neuronal polarity, axonal outgrowth, cerebellar development, regeneration of sensory axons, and neuroplasticity. However, the specific roles individual Nox isoforms play during nervous system development in vivo remain unclear. To address this problem, we investigated the role of Nox activity in the development of retinotectal connections in zebrafish embryos. Zebrafish broadly express four nox genes ( nox1, nox2/cybb, nox5, and duox ) throughout the central nervous system during early development...
May 23, 2018: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/29789558/celastrol-alleviates-renal-fibrosis-by-upregulating-cannabinoid-receptor-2-expression
#6
Ming Tang, Xu Cao, Kun Zhang, You Li, Quan-You Zheng, Gui-Qing Li, Qian-Hui He, Shu-Jing Li, Gui-Lian Xu, Ke-Qin Zhang
Renal fibrosis is the final manifestation of various chronic kidney diseases, and no effective therapy is available to prevent or reverse it. Celastrol, a triterpene that derived from traditional Chinese medicine, is a known potent anti-fibrotic agent. However, the underlying mechanisms of action of celastrol on renal fibrosis remain unknown. In this study, we found that celastrol treatment remarkably attenuated unilateral ureteral obstruction (UUO)-induced mouse renal fibrosis. This was evidenced by the significant reduction in tubular injury; collagen deposition; accumulation of fibronectin, collagen I, and α-smooth muscle actin; and the expression levels of pro-fibrotic factors Vim, Cola1, and TGF-β1 mRNA, as well as inflammatory responses...
May 22, 2018: Cell Death & Disease
https://www.readbyqxmd.com/read/29787994/bioavailability-of-wilforlide-a-in-mice-and-its-concentration-determination-using-an-hplc-apci-ms-ms-method
#7
Zhijun Wang, Steven Yeung, Shang Chen, Yasmin Moatazedi, Moses S S Chow
Wilforlide A (WA), an active compound in Tripterygium wilfordii Hook F (TW) which is a traditional Chinese medicine for treatment of autoimmune diseases, is a quality control marker for TW product. At present, the bioavailability/pharmacokinetics of WA is not known. Such information is not only essential to evaluate the relevance of WA as a quality control maker, but also important for future clinical efficacy studies. Therefore, a high-performance liquid chromatography-atmospheric pressure chemical ionization tandem mass spectrometric method (HPLC-APCI-MS/MS) was developed and applied to a bioavailability/pharmacokinetic study of WA...
May 16, 2018: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/29773987/celastrol-attenuates-the-invasion-and-migration-and-augments-the-anticancer-effects-of-bortezomib-in-a-xenograft-mouse-model-of-multiple-myeloma
#8
Muthu K Shanmugam, Kwang S Ahn, Jong H Lee, Radhamani Kannaiyan, Nurulhuda Mustafa, Kanjoormana A Manu, Kodappully S Siveen, Gautam Sethi, Wee J Chng, Alan P Kumar
Several lines of evidence have demonstrated that deregulated activation of NF-κB plays a pivotal role in the initiation and progression of a variety of cancers including multiple myeloma (MM). Therefore, novel molecules that can effectively suppress deregulated NF-κB upregulation can potentially reduce MM growth. In this study, the effect of celastrol (CSL) on patient derived CD138+ MM cell proliferation, apoptosis, cell invasion, and migration was investigated. In addition, we studied whether CSL can potentiate the apoptotic effect of bortezomib, a proteasome inhibitor in MM cells and in a xenograft mouse model...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29765532/chemopreventive-activity-of-celastrol-in-drug-resistant-human-colon-carcinoma-cell-cultures
#9
Helena Moreira, Anna Szyjka, Kazimierz Gąsiorowski
Celastrol (tripterine) a pentacyclic triterpenoid extracted from the roots of Tripterygium wilfordii Hook f., exhibits potent antioxidant and anti-inflammatory activity and also exerts important anti-cancer effects, as induction of apoptosis and lowering the level of drug resistance of several cancers. Increased level of cellular resistance to cytostatic drugs is typical for colorectal cancers, and largely determines the failure of chemotherapy for this tumor. The purpose of our research was to evaluate the chemopreventive effect of celastrol on cultures of colon cancer cells resistant to doxorubicin (LOVO/DX)...
April 20, 2018: Oncotarget
https://www.readbyqxmd.com/read/29750991/celastrol-attenuates-incision-induced-inflammation-and-pain-associated-with-inhibition-of-the-nf-%C3%AE%C2%BAb-signalling-pathway-via-sarm
#10
Xuhui Chen, Bo Zhang, Jiayan Li, Miaomiao Feng, Yue Zhang, Wenlong Yao, Chuanhan Zhang, Li Wan
AIM: This study aimed to investigate whether celastrol (CEL) could alleviate incision-induced pain and decipher its possible mechanism. MATERIALS AND METHODS: Sprague-Dawley rats were randomly divided into five groups: naïve, vehicle, CEL (5 μg/paw, 10 μg/paw and 20 μg/paw). CEL or vehicle was administered intraplantarly before plantar surgical incision. Histological examinations of skin tissues were performed after HE staining. Additionally, immunohistochemical staining, RT-PCR and western blot were performed to analyse macrophages, proinflammatory cytokines, SARM and NF-κB expression, respectively...
May 8, 2018: Life Sciences
https://www.readbyqxmd.com/read/29725253/anti-biofilm-and-anti-virulence-efficacy-of-celastrol-against-stenotrophomonas-maltophilia
#11
Hye-Rim Kim, Dongsup Lee, Yong-Bin Eom
Stenotrophomonas maltophilia is a multi-drug resistant opportunistic pathogen that causes nosocomial infections in immunocompromised patients. This pathogen is difficult to treat owing to its intrinsic multidrug resistance and ability to form antimicrobial-tolerant biofilms. In the present study, we aimed to assess the potential use of celastrol as a novel anti-biofilm and/or anti-virulence agent against S. maltophilia . Results showed that celastrol at its sub-inhibitory doses decreased biofilm formation and disrupt the established biofilms produced by S...
2018: International Journal of Medical Sciences
https://www.readbyqxmd.com/read/29694830/celastrol-attenuates-symptoms-of-preeclampsia-in-rats-by-inhibiting-matrix-metalloproteinase-9
#12
Sha Xiao, Ming Zhang, Zhenzhen He, Deling Wang
Preeclampsia is reported in pregnant women around the world and often causes maternal/fetal mortality and morbidity. In the current study, we assessed the efficacy of celastrol on a rat preeclampsia model induced by Nω -nitro-L-arginine methyl ester hydrochloride (L-NAME). Pregnant rats were administered L-NAME to establish preeclampsia. A total of 48 animals were randomly assigned into 4 groups (n=12 each): control, control plus celastrol treatment (control+celastrol), preeclampsia, and preeclampsia plus celastrol...
April 22, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29667734/celastrol-reverses-palmitic-acid-pa-caused-tlr4-md2-activation-dependent-insulin-resistance-via-disrupting-md2-related-cellular-binding-to-pa
#13
Xue Zhang, Ying Wang, Hui-Ya Ge, Yi-Jun Gu, Fan-Fan Cao, Chun-Xin Yang, Georges Uzan, Bin Peng, Deng-Hai Zhang
Elevated plasma statured fatty acids (FFAs) cause TLR4/MD2 activation-dependent inflammation and insulin tolerance, which account for the occurrence and development of obesity. It has been confirmed that statured palmitic acid (PA) (the most abundant FFA) could bind MD2 to cause cellular inflammation. The natural compound celastrol could improve obesity, which is suggested via inhibiting inflammation, yet the detailed mechanism for celastrol is still unclear. As celastrol is reported to directly target MD2, we thought disrupting the binding between FFAs and MD2 might be one of the ways for celastrol to inhibit FFAs-caused inflammation and insulin resistance...
April 18, 2018: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/29651912/effects-of-diclofenac-on-the-pharmacokinetics-of-celastrol-in-rats-and-its-transport
#14
Zengfu Wang, Dali Chen, Zhongwei Wang
CONTEXT: Diclofenac and celastrol are always used together for the treatment of rheumatoid arthritis; the herb-drug interaction potential between diclofenac and celastrol is still unknown. OBJECTIVE: This study investigates the effects of diclofenac on the pharmacokinetics of celastrol in rats. MATERIALS AND METHODS: Twelve male Sprague-Dawley rats were divided into two groups and received celastrol (1 mg/kg) or both celastrol (1 mg/kg) and diclofenac (10 mg/kg) by oral gavage, and blood samples were collected via the oculi chorioideae vein and determined using the LC-MS method developed in this study...
December 2018: Pharmaceutical Biology
https://www.readbyqxmd.com/read/29644847/preparation-of-microkernel-based-mesoporous-sio-2-cdte-sio-2-sio-2-fluorescent-nanoparticles-for-imaging-screening-and-enrichment-of-heat-shock-protein-90-inhibitors-from-tripterygium-wilfordii
#15
Yue Hu, Zhao-Yi Miao, Xiao-Jing Zhang, Xiao-Tong Yang, Ying-Ying Tang, Sheng Yu, Chen-Xiao Shan, Hong-Mei Wen, Dong Zhu
The currently utilized ligand fishing for bioactive molecular screening from complex matrixes cannot perform imaging screening. Here, we developed a new solid-phase ligand fishing coupled with an in situ imaging protocol for the specific enrichment and identification of heat shock protein 90 (Hsp 90) inhibitors from Tripterygium wilfordii, utilizing a multiple-layer and microkernel-based mesoporous nanostructure composed of a protective silica coating CdTe quantum dot (QD) core and a mesoporous silica shell, i...
May 1, 2018: Analytical Chemistry
https://www.readbyqxmd.com/read/29614269/celastrol-inhibits-cancer-metastasis-by-suppressing-m2-like-polarization-of-macrophages
#16
Yuening Yang, Shuyuan Cheng, Guikai Liang, Lou Honggang, Honghai Wu
In recent years, a large amount of clinical and experimental data has shown that M2-like polarized tumor-associated macrophages (TAMs) play an important role in cancer metastasis. Therefore, TAMs, especially M2-like TAMs is a promising target for anti-tumor metastasis therapy. Here, we found that celastrol dose-dependently suppressed IL-13 induced CD206 expression both in RAW264.7 and in primary macrophages. Consistently, celastrol also inhibited the expression of M2-like specific genes, including MRC1, Arg1, Fizz1, Mgl2 and CD11c...
March 31, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29593812/the-effect-of-celastrol-on-learning-and-memory-in-diabetic-rats-after-sevoflurane-inhalation
#17
Wei-Tao Liao, Xiao-Yu Xiao, Yinaxian Zhu, Shao-Peng Zhou
Introduction: The aim was to devise an animal model showing some of the neuropathological changes seen in senile dementia, and to investigate the effect of celastrol on cognition neuropathology in this model. Material and methods: Forty male Sprague Dawley rats weighing 300-350 g were randomly divided into 5 groups ( n = 8 each): control (Con); inhaled sevoflurane (Sev); diabetes mellitus (DM); diabetes mellitus + inhaled sevoflurane (DM/Sev); diabetes + inhaled sevoflurane + celastrol (Cel)...
March 2018: Archives of Medical Science: AMS
https://www.readbyqxmd.com/read/29553945/celastrol-inhibits-colorectal-cancer-cell-proliferation-and-migration-through-suppression-of-mmp3-and-mmp7-by-the-pi3k-akt-signaling-pathway
#18
Tang Bufu, Xu Di, Zhao Yilin, Liang Gege, Chen Xi, Wang Ling
Colorectal cancer (CRC) is one of the most frequent malignant tumors. Signaling by the PI3K/AKT pathway is crucial for CRC development and progression, including proliferation and migration. Celastrol has an anticancer effect, but its mechanism needs to be determined. Here, we showed that celastrol suppressed CRC cell proliferation and migration. Celastrol treatment also decreased the PI3K/AKT pathway components, and MMP3 and MMP7 expression levels. In addition, knockdown of AKT, not mTOR, inhibited MMP3 and MMP7 expression levels and AKT silencing promoted the celastrol-induced effects on CRC cell proliferation and migration...
July 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/29540209/celastrol-treatment-protects-against-acute-ischemic-stroke-induced-brain-injury-by-promoting-an-il-33-st2-axis-mediated-microglia-macrophage-m2-polarization
#19
Mei Jiang, Xinghui Liu, Denghai Zhang, Ying Wang, Xiaoxia Hu, Fengxia Xu, Mingming Jin, Fanfan Cao, Limin Xu
BACKGROUND: Acute ischemic stroke (AIS) is the most common type of cerebrovascular disease and is a leading cause of disability and death worldwide. Recently, a study suggested that transformation of microglia from the pro-inflammatory M1 state to the anti-inflammatory and tissue-reparative M2 phenotype may be an effective therapeutic strategy for ischemic stroke. Celastrol, a traditional oriental medicine, may have anti-inflammatory and neuroprotective effects. However, the underlying mechanisms remain unknown...
March 14, 2018: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/29534015/targeting-hodgkin-and-reed-sternberg-cells-with-an-inhibitor-of-heat-shock-protein-90-molecular-pathways-of-response-and-potential-mechanisms-of-resistance
#20
Priscilla Segges, Stephany Corrêa, Bárbara Du Rocher, Gabriela Vera-Lozada, Flavia Krsticevic, Debora Arce, Cinthya Sternberg, Eliana Abdelhay, Rocio Hassan
Classical Hodgkin lymphoma (cHL) cells overexpress heat-shock protein 90 (HSP90), an important intracellular signaling hub regulating cell survival, which is emerging as a promising therapeutic target. Here, we report the antitumor effect of celastrol, an anti-inflammatory compound and a recognized HSP90 inhibitor, in Hodgkin and Reed-Sternberg cell lines. Two disparate responses were recorded. In KM-H2 cells, celastrol inhibited cell proliferation, induced G0/G1 arrest, and triggered apoptosis through the activation of caspase-3/7...
March 13, 2018: International Journal of Molecular Sciences
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