Research Progress in the Modification of Quercetin Leading to Anticancer Agents

Massi, Alessandro; Bortolini, Olga; Ragno, Daniele; Bernardi, Tatiana; Sacchetti, Gianni; Tacchini, Massimo; Risi, Carmela De

doi:10.3390/molecules22081270

Cited by 189 publications

(126 citation statements)

References 85 publications

(128 reference statements)

Supporting

Mentioning

120

Contrasting

Unclassified

Order By: Relevance

“…Habtemariam et al [53] found that eriodictyol with 3 ,4 -OH showed the strongest protective effect on L-929 cells from tumor necrosis factor (TNF)-induced cell death, while hesperidin (with 3'-OH but without 4'-OH) had no protective effect. It indicated that the flavones with 3',4'-OH had strong antioxidant activity, like dihydroquercetin and quercetin (compounds 1 and 3) [54][55][56][57]. Dihydroquercetin (compound 1) as well-known antioxidants protect DNA from oxidative damage and against oxidative stress by stimulating the expression of HO-1 and NQO1 through the Nrf2-dependent antioxidant pathway [58].…”

Section: The Structural Features and The Antioxidant And Anti-prolifementioning

confidence: 99%

Antioxidant and Anti-Proliferative Properties of Hagenia abyssinica Roots and Their Potentially Active Components

et al. 2020

View full text Add to dashboard Cite

Hagenia abyssinica (Bruce) J. F. Gmel. is a multipurpose dioecious tree that has been used to treat various ailments, for example, the flowers of H. abyssinica have been widely used as a tea to treat intestinal parasites by local residents and the roots of H. abyssinica could also be used for anticancer purposes. Antioxidant activity could be one of the most important pathways to suppress cancer and there is hardly any information available on the specific chemical components corresponding to the bioactivities of H. abyssinica to date. The present study intended to screen and evaluate the antioxidant and anti-proliferative properties of five different fractions from H. abyssinica along with their corresponding total flavonoid and phenolic contents and then further identify those compounds with the most potent antioxidant and anti-proliferative activities using high performance liquid chromatography (HPLC) coupled to mass spectrometry (MS) and nuclear magnetic resonance (NMR). The total flavonoid and phenolic content assays showed that the ethyl acetate (EA) fraction of H. abyssinica had higher flavonoid and phenolic levels than the other four fractions. Furthermore, the 2,2-diphenyl-1-picrylhydrazyl (DPPH) superoxide radical scavenging abilities, total antioxidant capacity (TAC) assay with 2,2′-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid (ABTS), and ferric-reducing antioxidant power (FRAP) were measured to evaluate the antioxidant activities of the five fractions and some pure compounds isolated from the EA fraction, which displayed higher antioxidant properties than that of the other fractions. Caffeic acid from the EA fraction showed even stronger DPPH scavenging ability (IC50 7.858 ± 0.31 µg/mL) than that of Vc (IC50 8.27 ± 0.11 µg/mL) as the positive control. The anti-proliferative properties of four fractions and the ethanol extract were evaluated by the 3-(4,5)-dimethylthiahiazo (-z-y1)-3,5-di-phenytetrazoliumromide (MTT) assay and the EA fraction exhibited higher anti-proliferative activities against three cancer cell lines than that of the other fractions. Additionally, the compounds with good antioxidant activity from the EA fraction of H. abyssinica were screened and identified using LC-MS and NMR and were also found to possess good anti-proliferative activity. In the MTT assay, the quercetin showed the strongest dose-dependent anti-proliferative activities to colon cancer cells (HT-29) and liver cancer cells (HepG2) among all of the compounds isolated. This study provided valuable information on the synergistic antioxidant and anti-proliferative properties of H. abyssinica.

show abstract

Section: The Structural Features and The Antioxidant And Anti-prolifementioning

confidence: 99%

Antioxidant and Anti-Proliferative Properties of Hagenia abyssinica Roots and Their Potentially Active Components

et al. 2020

View full text Add to dashboard Cite

show abstract

“…Quercetin (3,5,7,3′,4′‐pentahydroxyflavone) is a polyphenolic flavonol molecule present in many fruits and vegetables such as onions, apples, berries, peanuts, soybeans, potatoes, broccoli, grapes, citrus fruits, and tea . Several reports highlighted the potential of quercetin against behavioral deficits in different animal models …”

Section: Quercetinmentioning

confidence: 99%

Cholinesterase targeting by polyphenols: A therapeutic approach for the treatment of Alzheimer’s disease

2018

View full text Add to dashboard Cite

Alzheimer's disease (AD) is a progressive irreversible neurodegenerative disorder characterized by excessive deposition of β-amyloid (Aβ) oligomers, and neurofibrillary tangles (NFTs), comprising of hyperphosphorylated tau proteins. The cholinergic system has been suggested as the earliest and most affected molecular mechanism that describes AD pathophysiology. Moreover, cholinesterase inhibitors (ChEIs) are the potential class of drugs that can amplify cholinergic activity to improve cognition and global performance and reduce psychiatric and behavioral disturbances. Approximately, 60%-80% of all cases of dementia in the world are patients with AD. In view of the continuous rise of this disease especially in the aged population, there is a dire need to come up with a novel compound and/or mixture that could work against this devastating disease. In this regard, the best is to rely on natural compounds rather than synthetic ones, because natural compounds are easily available, cost-effective, and comparatively less toxic. To serve this purpose, lately, scientific community has started exploring the possibility of using different polyphenols either solitary or in combination that can serve as therapeutics against AD. In the current article, we have summarized the role of various polyphenols, namely quercetin, resveratrol, curcumin, gallocatechins, cinnamic acid, caffeine, and caffeic acid as an inhibitor of cholinesterase for the treatment of AD. We have also tried to uncover the mechanistic insight on the action of these polyphenols against AD pathogenicity.

show abstract

“…In addition, many of these compounds have common targets, suggesting that different compounds may provide synergistic effects. Quercetin belongs to the avonol group of polyphenolic compounds, which functions as antibacterial, antiviral, anti-in ammatory, antioxidant, anticancer, anti-diabetic, immunomodulatory, etc [72]. The existing studies [73][74][75]have provided convincing evidence on the renoprotective effects of quercetin in both animal and cell models of DKD.…”

Section: Discussionmentioning

confidence: 99%

A Network Pharmacology-Based Strategy for Predicting Active Ingredients and Potential Targets of Shuilu Erxian Dan in Treating Diabetic Kidney Disease

Yue

2020

Preprint

View full text Add to dashboard Cite

Background and objective: Recent years, some Chinese scholars have applied Shuilu Erxian Dan (SED) to the treatment of treating diabetic kidney disease (DKD) and achieved well curative effect. However, these studies are mostly limited to clinical observation. This study aimed to explore the molecular mechanisms of SED in treating DKD. Methods The active components of SED were retrieved in TCMSP database and BATMAN-TCM database, and the herbal targets were obtained by drugbank database and SwissTargetPrediction platform. The gene expression data of DKD patients were downloaded from GEO database and analyzed to obtain DKD-related targets. The ingredient-target network and the PPI network were constructed by Cytoscape software. The clusterProfiler package of R software is used for bioinformatic analysis. Molecular docking was further applied to verify the interaction between compounds and targets by Autodock Vina software. Results 610 differential expressed genes of DKD patients were obtained, and 29 potential targets of SED against DKD were screened out (including PPTGS2, FABP3, HSD17B2, FABP1, HSD11B2, CYP27B1, JUN, UGT2B7, VCAM1, CA2, MAOA, MMP2, CXCR1, SLC22A6, EPHX2, SLC47A1, FOS, EGF, CCL2, COL3A1, GSTA1, GSTA2, HSPA1A, DAO, ALDH2, ALB, GPR18, FPR2, and LPL). All the active ingredients in SED can act on the DKD-related targets, among which quercetin, Ellagic acid, and kaempferol may be the key active compounds. SED may play a therapeutic role in DKD by regulating pathways including “Fluid shear stress and atherosclerosis”, “AGE − RAGE signaling pathway in diabetic complications” and “IL-17 signaling pathway”. Conclusion This study suggests that the mechanism of SED treating DKD is a complex network with multi-target and multi-pathway, which provides a reference for future experimental studies.

show abstract

Research Progress in the Modification of Quercetin Leading to Anticancer Agents

Cited by 189 publications

References 85 publications

Antioxidant and Anti-Proliferative Properties of Hagenia abyssinica Roots and Their Potentially Active Components

Antioxidant and Anti-Proliferative Properties of Hagenia abyssinica Roots and Their Potentially Active Components

Cholinesterase targeting by polyphenols: A therapeutic approach for the treatment of Alzheimer’s disease

A Network Pharmacology-Based Strategy for Predicting Active Ingredients and Potential Targets of Shuilu Erxian Dan in Treating Diabetic Kidney Disease

Contact Info

Product

Resources

About