2015
DOI: 10.1021/acs.jnatprod.5b00156
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3,5-Diarylpyrazole Derivatives Obtained by Ammonolysis of the Total Flavonoids from Chrysanthemum indicum Extract Show Potential for the Treatment of Alzheimer’s Disease

Abstract: Four new 3,5-diarylpyrazole analogues (1-4) were isolated from an extract of the flowers of Chrysanthemun indicum using a combination of ammonolysis of the total flavonoid extract and an Aβ aggregation inhibitory activity guided purification procedure. All four compounds (1-4) showed moderate to potent activity against Aβ aggregation with EC50 values of 4.3, 15.8, 1.3, and 2.9 μM, respectively. Moreover, compound 3 showed low cytotoxicity and significant neuroprotective activity against Aβ-induced cytotoxicity… Show more

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Cited by 36 publications
(29 citation statements)
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“…47 . It is noteworthy to mention here that, 3,5-diarylpyrazole analogues become one Wu et al, 2015 of the best alternatives to bioactive compounds, as it exhibit several advantages like A² aggregation, neuroprotective activity which are useful in Alzheimer's disease treatment 48 54 . The supercritical-carbon dioxide fluid extract from Chrysanthemum indicum Wu et al, 2014 Linne plays a vital role against lipopolysaccharide-induced acute lung injury (ALI) in mice.…”
Section: Key Findings Referencementioning
confidence: 99%
“…47 . It is noteworthy to mention here that, 3,5-diarylpyrazole analogues become one Wu et al, 2015 of the best alternatives to bioactive compounds, as it exhibit several advantages like A² aggregation, neuroprotective activity which are useful in Alzheimer's disease treatment 48 54 . The supercritical-carbon dioxide fluid extract from Chrysanthemum indicum Wu et al, 2014 Linne plays a vital role against lipopolysaccharide-induced acute lung injury (ALI) in mice.…”
Section: Key Findings Referencementioning
confidence: 99%
“…) . A natural extract of the flowers of Chrysanthemum indicum was also diversified using this strategy, resulting in the generation of four new 3,5‐diarylpyrazole analogues ( 128 – 131 ) . All four compounds showed moderate to potent activity against amyloid‐ β ‐induced aggregation, indicating their potential for treating Alzheimer's disease …”
Section: Biological Synthetic and Semisynthetic Approachesmentioning
confidence: 99%
“…The subsequent isolation of each compound produced from such reactions affords a diverse natural‐product‐like library of new molecular scaffolds. There have also been some reports on similar methods that chemically convert natural extracts . However, we defined diversity‐enhanced extracts as natural extracts formed by multiple diversity‐generating reactions that not only convert functional groups, but also form new carbon–carbon bonds and modify the molecular scaffolds similarly to diversity‐oriented synthesis.…”
Section: Introductionmentioning
confidence: 99%
“…There have also been some reports on similar methodst hat chemically convert natural extracts. [6][7][8][9][10][11] However, we defined diversity-enhanced extracts as natural extracts formed by multiple diversity-generating reactions that not only convert functional groups, buta lso form new carbon-carbon bonds and modify the moleculars caffolds similarly to diversity-oriented synthesis.…”
Section: Introductionmentioning
confidence: 99%