Benzothiazole derivatives upregulate SIRT1 and relevant genes in high-fat fed C57BL/6J mice

Gu, Qing; Zhou, Penghui; Xu, Xiaoling; Fang, Weichun; Jia, Shaolong; Liu, Wei-Zhu; Su, Xu; Zhang, Jingshu; Wang, Hao; Yu, Peng; Hua, Erbing

doi:10.1007/s00044-014-1307-3

Cited by 4 publications

(4 citation statements)

References 21 publications

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“…N- (3-(benzo[d]thiazol-2-yl)phenyl)-3,4,5trimethoxybenzamide 62 (Figure 9) represents one of the few examples of synthetic compounds that are able to increase SIRT1 mRNA expression (mRNA SIRT1/β-actin greater than 1.5). Moreover, it improves plasma and hepatic lipid profiles and decreases blood glucose concentration, thus demonstrating potential anti-diabetic properties [108]. The (S)-enantiomer of synthetic tetrahydroisoquinoline alkaloid YS-51 63 (Figure 9) was found to be a potential therapeutic agent against the obesity-associated nonalcoholic fatty liver disease when tested in animals fed with high-fat diet that were supplemented with or without this compound.…”

Section: Compounds Increasing Sirt1 Expressionmentioning

confidence: 99%

Activators of Sirtuin-1 and their Involvement in Cardioprotection

Granchi

Minutolo

2018

CMC

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SIRT1 is a nicotinamide adenosine dinucleotide (NAD+)-dependent deacetylase, which removes acetyl groups from many target proteins, such as histone proteins, transcription factors and cofactors. SIRT1-catalyzed deacetylation of these factors modulates the activity of downstream proteins, thus influencing many biological processes. SIRT1 is involved in the regulation of metabolism, inflammation, and tumor growth. The activity of this enzyme is related to the beneficial health effects of calorie restriction, such as lifespan extension and, in particular, the activation of SIRT1 has a positive impact on the cardiovascular system. Therefore, SIRT1 is considered as an attractive drug target and modulation of SIRT1 may represents a new therapeutic strategy against cardiovascular diseases, as small molecules able to activate SIRT1 can be considered as cardioprotective agents. In this review, we summarize both natural or synthetic compounds developed as SIRT1 activators, with a focus on their promising therapeutic applications in cardiovascular pathologies.

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Section: Compounds Increasing Sirt1 Expressionmentioning

confidence: 99%

Activators of Sirtuin-1 and their Involvement in Cardioprotection

Granchi

Minutolo

2018

CMC

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“…SIRT-1 regulates glucose/lipid metabolism, since it deacetylates several proteins of the insulin signaling pathway, and its overexpression improves the sensitivity to insulin. Some SIRT-1 activators, such as JHJ1 , JHJ2 , and JHJ3 (derived from the structure of OAP) [ 82 ], have been reported to modulate the plasma lipid metabolism and blood glucose in high-fat fed mice by upregulating FoxO1, PPARγ, and PGC-1α genes [ 83 ], while another activator, named E6155 (identified by a high-throughput screening using the purified recombinant human SIRT-1 and HTRF SIRT-1 assay) by Liu and colleagues, improved blood glucose tolerance and insulin resistance in diabetic mice by activating LKB1/AMPK and IRS1/AKT pathways [ 84 ].…”

Section: Sirtuins As Targets In Different Pathologiesmentioning

confidence: 99%

Virtual Screening in the Identification of Sirtuins’ Activity Modulators

et al. 2022

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Sirtuins are NAD+-dependent deac(et)ylases with different subcellular localization. The sirtuins’ family is composed of seven members, named SIRT-1 to SIRT-7. Their substrates include histones and also an increasing number of different proteins. Sirtuins regulate a wide range of different processes, ranging from transcription to metabolism to genome stability. Thus, their dysregulation has been related to the pathogenesis of different diseases. In this review, we discussed the pharmacological approaches based on sirtuins’ modulators (both inhibitors and activators) that have been attempted in in vitro and/or in in vivo experimental settings, to highlight the therapeutic potential of targeting one/more specific sirtuin isoform(s) in cancer, neurodegenerative disorders and type 2 diabetes. Extensive research has already been performed to identify SIRT-1 and -2 modulators, while compounds targeting the other sirtuins have been less studied so far. Beside sections dedicated to each sirtuin, in the present review we also included sections dedicated to pan-sirtuins’ and to parasitic sirtuins’ modulators. A special focus is dedicated to the sirtuins’ modulators identified by the use of virtual screening.

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“…Hyperlipidemia is a dominant risk factor that contributes to the development and progression of atherosclerosis and subsequent cardiovascular disease, which is one of the most serious diseases for humans [1][2][3][4]. The BD has proved to improve the plasma and hepatic lipid profile and blood glucose through upregulating SIRT1, FOXO1, PPARγ and PGC-1α genes [5].…”

Section: Introductionmentioning

confidence: 99%

“…The experimental results would answer how BD could impact excretion of total sterols of fat-fed mice in view of relevant genetic regulations. (Fig 1) refer to the paper [5].…”

Section: Introductionmentioning

confidence: 99%

Benzothiazole Derivative Accelerates Excretion of Total Sterols in Long-Term High Fat Fed C57BL/6J Mice

Yu¹,

Jiang²,

Ao³

et al. 2016

Proceedings of the 2015 International Conference on Materials Chemistry and Environmental Protection (Meep-15)

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Benzothiazole derivative (BD): [N-(3-(benzothiazol-2-yl) phenyl)-1H-pyrazole-3-carboxamide] was tested for excretion of total sterols of high-fat diet fed C57BL/6J mice in view of lipid metabolism. The results showed that BD as supplementation of high-fat diet significantly improved the output of cholesterol in comparison to HF alone. Relevant mRNA expressions of HMG-CoA-R, SREBP-2, LDL-R, CYP7A1 and PPARα were significantly altered in liver. These results suggest that BD could promote the excretion of total sterols and play a beneficial role in lipids metabolism for a high-fat fed mice.

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Benzothiazole derivatives upregulate SIRT1 and relevant genes in high-fat fed C57BL/6J mice

Cited by 4 publications

References 21 publications

Activators of Sirtuin-1 and their Involvement in Cardioprotection

Activators of Sirtuin-1 and their Involvement in Cardioprotection

Virtual Screening in the Identification of Sirtuins’ Activity Modulators

Benzothiazole Derivative Accelerates Excretion of Total Sterols in Long-Term High Fat Fed C57BL/6J Mice

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