Design, synthesis, and biological evaluation of curcumin analogues as multifunctional agents for the treatment of Alzheimer’s disease

Chen, Shangying; Chen, Yuan; Li, Yanping; Chen, Shuhan; Tan, Jia‐Heng; Ou, Tian‐Miao; Gu, Lian‐Quan; Huang, Zhi‐Shu

doi:10.1016/j.bmc.2011.07.033

Cited by 87 publications

(55 citation statements)

References 42 publications

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“…What more, some other pharmacological activity were also been found in those mono-carbonyl curcumin analogues. such as antioxidant [64][65][66], anti-inflammatory [67,68], anti-bacterial [69], anti-AD [70], with which the class of compounds will having good development prospects.…”

Section: Resultsmentioning

confidence: 99%

Synthesis and Anticancer Activity of Mono-Carbonyl Analogues of Curcumin

Yin¹,

Zheng²,

Yao³

et al. 2013

JCT

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Curcumin has been reported to possess multifunctional bioactivities with low toxicity. However, the clinical application of curcumin has been significantly limited by its instability and poor metabolic property. Up to now, multiple approaches are being sought to overcome these limitations to obtaining “super curcumin”, and many analogues of curcumin have been designed and synthesized. In all of those analogues, a series of mono-carbonyl curcumin analogues deleting the β-diketone draw our attention. Since the seven-carbon β-diketone linker in curcumin may be responsible for its instability, the series of mono-carbonyl curcumin analogues deleting the β-diketone may be potential prodrug with improved pharmacokinetic and pharmacodynamic properties. This review just focuses on these more stable mono-carbonyl analogues of curcumin, and shows the new class of active structure by introducing the synthesis and anticancer activity of them

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Section: Resultsmentioning

confidence: 99%

Synthesis and Anticancer Activity of Mono-Carbonyl Analogues of Curcumin

Yin¹,

Zheng²,

Yao³

et al. 2013

JCT

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“…An 8-to 16 Å-wide rigid linker must separate two aromatic portions, and a hydroxylic group on one or both aromatic portions respectively ensures or increases Ab affinity [193]. The symmetrical, constrained piperidine-bispiperazine curcumin derivative 6.13 [194] ( Figure 6.6) shows improved physicochemical properties, bioavailability, and stability. It is a more potent inhibitor of Ab aggregation, anti-oxidant, and metal-chelating agent than curcumin in cell-free assays [194].…”

Section: Interfering With (Neuro)toxic Tau Species In the Aggregationmentioning

confidence: 97%

“…It is a more potent inhibitor of Ab aggregation, anti-oxidant, and metal-chelating agent than curcumin in cell-free assays [194]. It acts on Ab peptides by disfavoring the conformational transition to aggregationprone b-sheets, hindering the formation of both Ab fibrils and oligomers in an Ab aggregation assay, and decreasing oxidative stress in SH-SY5Y cells [194].…”

Section: Interfering With (Neuro)toxic Tau Species In the Aggregationmentioning

confidence: 99%

Targeting Assembly and Disassembly of Protein Aggregates

Seneci

2015

Chemical Modulators of Protein Misfolding and Neurodegenerative Disease

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“…Moreover, it has been reported that curcumin has poor bioavailability and absorption, rapid metabolism, and systemic elimination, which contributes to a reduction in its redox-potency (Table 3). Recent studies suggest that curcumin derivatives may cross the blood-brain barrier potentially increasing the efficacy of these compounds in brain-specific diseases (15,71). These results suggest the translational potential of natural product SOD-inducers may be questionable and tissue-specific; however, for various disease types SODinducers and their derivatives potentially have broad applicability in disease prevention.…”

mentioning

confidence: 99%

Manganese Superoxide Dismutase in Cancer Prevention

Robbins

Zhao

2014

Antioxidants & Redox Signaling

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Significance: Cancer is the second leading cause of death in the United States. Considering the quality of life and treatment cost, the best way to fight against cancer is to prevent or suppress cancer development. Cancer is preventable as indicated by human papilloma virus (HPV) vaccination and tamoxifen/raloxifen treatment in breast cancer prevention. The activities of superoxide dismutases (SODs) are often lowered during early cancer development, making it a rational candidate for cancer prevention. Recent Advances: SOD liposome and mimetics have been shown to be effective in cancer prevention animal models. They've also passed safety tests during early phase clinical trials. Dietary supplement-based SOD cancer prevention provides another opportunity for antioxidant-based cancer prevention. New mechanistic studies have revealed that SOD inhibits not only oncogenic activity, but also subsequent metabolic shifts during early tumorigenesis. Critical Issues: Lack of sufficient animal model studies targeting specific cancers; and lack of clinical trials and support from pharmaceutical industries also hamper efforts in further advancing SOD-based cancer prevention. Future Directions: To educate and obtain support from our society that cancer is preventable. To combine SOD-based therapeutics with other cancer preventive agents to obtain synergistic effects. To formulate a dietary supplementation-based antioxidant approach for cancer prevention. Lastly, targeting specific populations who are prone to carcinogens, which can trigger oxidative stress as the mechanism of carcinogenesis. Antioxid. Redox Signal. 20, 1628-1645.

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Design, synthesis, and biological evaluation of curcumin analogues as multifunctional agents for the treatment of Alzheimer’s disease

Cited by 87 publications

References 42 publications

Synthesis and Anticancer Activity of Mono-Carbonyl Analogues of Curcumin

Synthesis and Anticancer Activity of Mono-Carbonyl Analogues of Curcumin

Targeting Assembly and Disassembly of Protein Aggregates

Manganese Superoxide Dismutase in Cancer Prevention

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