Celastrol as a tool for the study of the biological events of metabolic diseases

Lan, Gongcai; Zhang, Jie; Ye, Wenbo; Yang, Fan; Li, Ang; He, Weiwei; Zhang, Weidong

doi:10.1007/s11426-018-9404-9

Cited by 11 publications

(7 citation statements)

References 71 publications

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“…The anti-cancer properties of celastrol, one of the most studied methylene quinones, have been attributed to apoptosis and autophagy induction, cell cycle arrest, and anti-metastatic and anti-angiogenic action [ 9 , 10 ]. Other works have evidenced the ability of celastrol in combating metabolic disorders such as obesity and type 2 diabetes [ 11 ]. Treatment with celastrol suppresses food intake, blocks reduction in energy consumption, and mediates weight loss by acting as a leptin sensitizer in mouse models [ 12 , 13 ].…”

Section: Introductionmentioning

confidence: 99%

Antimicrobial Activity and Mode of Action of Celastrol, a Nortriterpen Quinone Isolated from Natural Sources

Padilla-Montaño

Guerra

Moujir

2021

Foods

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Species of the Celastraceae family are traditionally consumed in different world regions for their stimulating properties. Celastrol, a triterpene methylene quinone isolated from plants of celastraceas, specifically activates satiety centers in the brain that play an important role in controlling body weight. In this work, the antimicrobial activity and mechanism of action of celastrol and a natural derivative, pristimerin, were investigated in Bacillus subtilis. Celastrol showed a higher antimicrobial activity compared with pristimerin, being active against Gram-positive bacteria with minimum inhibitory concentrations (MICs) that ranged between 0.16 and 2.5 µg/mL. Killing curves displayed a bactericidal effect that was dependent on the inoculum size. Monitoring of macromolecular synthesis in bacterial populations treated with these compounds revealed inhibition in the incorporation of all radiolabeled precursors, but not simultaneously. Celastrol at 3 µg/mL and pristimerin at 10 µg/mL affected DNA and RNA synthesis first, followed by protein synthesis, although the inhibitory action on the uptake of radiolabeled precursors was more dramatic with celastrol. This compound also caused cytoplasmic membrane disruption observed by potassium leakage and formation of mesosome-like structures. The inhibition of oxygen consumption of whole and disrupted cells after treatments with both quinones indicates damage in the cellular structure, suggesting the cytoplasmic membrane as a potential target. These findings indicate that celastrol could be considered as an interesting alternative to control outbreaks caused by spore-forming bacteria.

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Section: Introductionmentioning

confidence: 99%

Antimicrobial Activity and Mode of Action of Celastrol, a Nortriterpen Quinone Isolated from Natural Sources

Padilla-Montaño

Guerra

Moujir

2021

Foods

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“…33 Leptin, secreted mainly from adipocytes, communicates the satiety signal to the hypothalamus and regulates energy homeostasis. 34 Thus, loss of hypothalamic leptin signaling is usually sufficient to cause obesity. 34 In the past decade, the natural product celastrol was found to suppress food intake and substantially reduce body weight as a potent leptin sensitizer in animal models.…”

Section: Discussionmentioning

confidence: 99%

Cel-CS1K: A Celastrol–Chitosan Conjugate for Treating Diet-Induced Obesity

Zeng,

Tian,

Wang

et al. 2024

Chem. Res. Toxicol.

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Celastrol (Cel), extracted from Tripterygium wilfordii Hook, is a potential antiobesity drug, except for its adverse reactions in clinic. In the present study, we synthesized a promising celastrol–chitosan conjugate (Cel-CS1K) and evaluated its antiobesity effect and biological safety in diet-induced obese mice. Cel-CS1K showed higher drug loading (over 10 wt %), good solubility (18–19 mg/mL) in water, slower peak time (T max = 4 h), and clearance (T 1/2 = 8.97 h) in rats. Cel-CS1K effectively attenuated the cytotoxicity, celastrol-induced apoptosis, and fat accumulation of hepatocytes. Cel-CS1K reduced body weight and dietary amount same as the free Cel but with lower toxicity in blood, liver, and testis. Cel-CS1K improved the glucose homeostasis, HDL-C level, insulin sensitivity, and leptin sensitivity, while it significantly reduced the gene expression levels of LDL-C, TG, and TC in obese mice. Furthermore, the adipose-related gene expression levels provided evidence in support of a role for Cel-CS1K in losing weight by the multimode regulation. Overall, Cel-CS1K provides a translatable therapeutic strategy for the treatment of diet-induced obese humans.

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“…According to Schiavone et al, there are several clinical conditions such as Crohn’s disease, psoriasis, rheumatoid arthritis, diabetes, kidney disease, and transplantation with promising results of celastrol administration [ 115 ]. In vitro and in vivo animal studies suggested that celastrol has antidiabetic effects and improves diabetic nephropathy and whole-body insulin resistance, due to the inhibition of NF-κB in the hypothalamus [ 133 ]. In mice, celastrol showed obesity-controlling effects by inhibiting negative regulators of leptin [ 134 ], and reduced obesity-induced OS by increasing antioxidant enzymes and inhibiting NADH oxidase and ROS [ 135 ].…”

Section: Celastrolmentioning

confidence: 99%

Plant-Based Antioxidants for Prevention and Treatment of Neurodegenerative Diseases: Phytotherapeutic Potential of Laurus nobilis, Aronia melanocarpa, and Celastrol

et al. 2023

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With the progress of medicine, especially in the last century, life expectancy increased considerably. As a result, age-related diseases also increased, especially malignancies and degenerative diseases of the central nervous system. The incidence and prevalence of neurodegenerative diseases steadily increased over the years, but despite efforts to uncover the pathophysiological processes behind these conditions, they remain elusive. Among the many theories, oxidative stress was proposed to be involved in neurodegenerative processes and to play an important role in the morbidity and progression of various neurodegenerative disorders. Accordingly, a number of studies discovered the potential of natural plant constituents to have significant antioxidant activity. This review focused on several plant-based antioxidants that showed promising results in the prevention and treatment of neurodegenerative diseases. Laurus nobilis, Aronia melanocarpa, and celastrol, a chemical compound isolated from the root extracts of Tripterygium wilfordii and T. regelii, are all known to be rich in antioxidant polyphenols.

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Celastrol as a tool for the study of the biological events of metabolic diseases

Cited by 11 publications

References 71 publications

Antimicrobial Activity and Mode of Action of Celastrol, a Nortriterpen Quinone Isolated from Natural Sources

Antimicrobial Activity and Mode of Action of Celastrol, a Nortriterpen Quinone Isolated from Natural Sources

Cel-CS1K: A Celastrol–Chitosan Conjugate for Treating Diet-Induced Obesity

Plant-Based Antioxidants for Prevention and Treatment of Neurodegenerative Diseases: Phytotherapeutic Potential of Laurus nobilis, Aronia melanocarpa, and Celastrol

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