Activation of anti-oxidant of curcumin pyrazole derivatives through preservation of mitochondria function and Nrf2 signaling pathway

Liao, Liping; Shi, Jinguo; Jiang, Caibao; Zhang, Liantao; Feng, Lisi; Liu, Jiayong; Zhang, Jingxia

doi:10.1016/j.neuint.2019.01.026

Cited by 38 publications

(24 citation statements)

References 49 publications

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“…Additionally, 1-phenylisatin, a selective cannabinoid receptor type 2 (CB2R) agonist, has the same effects as those of TWK10-fermented soymilk extract in CCH-induced VaD rats [34]. Edaravone is a novel free radical scavenger that ameliorates neuronal damage and exerts neuroprotective effects in neurodegenerative diseases [35,36]. Edaravone markedly inhibits oxidative stress by elevating SOD activity and reducing MDA and ROS levels in the hippocampus of VaD rats.…”

Section: Promotion Of Free Radical Scavengingmentioning

confidence: 99%

Pharmacological Treatment of Vascular Dementia: A Molecular Mechanism Perspective

Kuang¹,

Zhou²,

Zhu³

et al. 2021

Aging and disease

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Section: Promotion Of Free Radical Scavengingmentioning

confidence: 99%

Pharmacological Treatment of Vascular Dementia: A Molecular Mechanism Perspective

Kuang¹,

Zhou²,

Zhu³

et al. 2021

Aging and disease

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“…This study hypothesized that incorporating a heterocyclic scaffold in the central part of curcumin's structural skeleton could stabilize the otherwise unsteady nature of curcumin which is usually credited to the β-diketone moiety (Liang 2009) (Liao 2019). Previous studies have also postulated that apart from contributing to the improved stability and bioavailability of the compound it could also lead to better antitumor and antiangiogenic activity (Jankun et al 2016).…”

Section: Cytotoxicity Evaluationmentioning

confidence: 99%

The inhibitory potency of isoxazole-curcumin analogue for the management of breast cancer: A comparative in vitro and molecular modeling investigation

Rodrigues

Hari

et al. 2021

Chem. Pap.

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Curcumin, a potent phytochemical derived from the spice element turmeric, has been identified as a herbal remedy decades ago and has displayed promise in the field of medicinal chemistry. However, multiple traits associated with curcumin, such as poor bioavailability and instability, limit its effectiveness to be accepted as a lead drug-like entity. Different reactive sites in its chemical structure have been identified to incorporate modifications as attempts to improving its efficacy. The diketo group present in the center of the structural scaffold has been touted as the group responsible for the instability of curcumin, and substituting it with a heterocyclic ring contributes to improved stability. In this study, four heterocyclic curcumin analogues, representing some broad groups of heterocyclic curcuminoids (isoxazole-, pyrazole-, N-phenyl pyrazole- and N-amido-pyrazole-based), have been synthesized by a simple one-pot synthesis and have been characterized by FTIR, 1H-NMR, 13C-NMR, DSC and LC–MS. To predict its potential anticancer efficacy, the compounds have been analyzed by computational studies via molecular docking for their regulatory role against three key proteins, namely GSK-3β—of which abnormal regulation and expression is associated with cancer; Bcl-2—an apoptosis regulator; and PR which is a key nuclear receptor involved in breast cancer development. One of the compounds, isoxazole-curcumin, has consistently indicated a better docking score than the other tested compounds as well as curcumin. Apart from docking, the compounds have also been profiled for their ADME properties as well as free energy binding calculations. Further, the in vitro cytotoxic evaluation of the analogues was carried out by SRB assay in breast cancer cell line (MCF7), out of which isoxazole-curcumin (IC50–3.97 µM) has displayed a sevenfold superior activity than curcumin (IC50–21.89 µM). In the collation of results, it can be suggested that isoxazole-curcumin behaves as a potential lead owing to its ability to be involved in a regulatory role with multiple significant cancer proteins and hence deserves further investigations in the development of small molecule-based anti-breast cancer agents. Graphic abstract

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“…It is reported that Nrf2 defends neurons against mitochondrial neurotoxic compounds, reduced GHS and imbalanced mitochondrial ROS production as well as improving the function and integrity of mitochondria. Besides, in many mitochondrial-related disorders especially NDs the function of Nrf2 is suppressed by several processes (98,59).…”

Section: The Roles Of Mitochondria In Ndsmentioning

confidence: 99%

“…For instance, curcumin pyrazole derivatives (e.g. C1-C6 and CNB-001) have significantly more protective properties on mitochondrial dysfunction and it related abnormalities by inhibiting the ΔΨm loss, attenuating intracellular ROS and enhancing nuclear translocation of Nrf2 (48,59).…”

Section: Curcumin Analogsmentioning

confidence: 99%

Effects of curcumin on mitochondria in neurodegenerative diseases

et al. 2019

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Activation of anti-oxidant of curcumin pyrazole derivatives through preservation of mitochondria function and Nrf2 signaling pathway

Cited by 38 publications

References 49 publications

Pharmacological Treatment of Vascular Dementia: A Molecular Mechanism Perspective

Pharmacological Treatment of Vascular Dementia: A Molecular Mechanism Perspective

The inhibitory potency of isoxazole-curcumin analogue for the management of breast cancer: A comparative in vitro and molecular modeling investigation

Effects of curcumin on mitochondria in neurodegenerative diseases

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