Flavonoids as prospective compounds for anti-cancer therapy

Ravishankar, Divyashree; Rajora, Amit Kumar; Greco, Francesca; Osborn, Helen M. I.

doi:10.1016/j.biocel.2013.10.004

Cited by 491 publications

(353 citation statements)

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“…The sample solution showed antiproliferative activity against Colo-205, T47D, and MCF7 and it significantly reduced the growth rate of cancer cells at a concentration of 50 µg/mL after 24 h treatment, however, the maximum effect was on Colo-205, as shown in Figure 5. The presence of various bioactive compounds like glycosides, flavonoids, phytosterols, and tannins (Shalabh et al, 2012) in the extract of T. natans and the polyphenols like trapain, euginin, and 1,2,3,6-tetra-O-galloyl-beta-D-glucopyranose (TGG) reported by Midori et al (2014) in the husk of T. natans may be responsible for anticancerous activities (Li et al, 2013;Ravishankar, Rajora, Greco, & Osborn, 2013). Yuan and Walsh (2006) reported dose-dependent inhibition against the proliferation of the human cervical epithelial adenocarcinoma HeLa cell line in the case of dulse and kelp extracts, which also have aquatic habitats as water chestnut.…”

Section: Antiproliferative Assaymentioning

confidence: 99%

DNA scission inhibition, antioxidant, and antiproliferative activities of water chestnut (Trapa natans) extracted in different solvents

Gani

Rasool

Shah

et al. 2015

CyTA - Journal of Food

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This investigation deals with the study of polyphenolic, antioxidant, and antiproliferative activities of water chestnut extracted in different solvents. The antioxidant activities of the extract in different solvents were the maximum in methanol, followed by ethanol and aqueous solution and were found to be 39.8%, 34.1% and 32.6% from DPPH assay, and 45.64%, 35.08% and 30.52% from lipid peroxidation assay, respectively, whereas the reducing power inhibition assay showed the maximum antioxidant potential in the aqueous extract of the sample, followed by methanolic and ethanolic extracts. The polyphenolic content of the water chestnut was found to be more in methanol than in aqueous and ethanolic extracts. The water chestnut extract also showed the antiproliferative potential when tested against the human colon cancer cell line (Colo-205), human ductal breast epithelial tumor cell line (T47D), and human breast adenocarcinoma cell line (MCF7). It also showed some protection from DNA damage induced by hydroxyl radicals in calf thymus DNA.Keywords: water chestnut; DNA scission inhibition; antioxidant activity; antiproliferative activity Esta investigación trata de un estudio sobre la actividad antioxidante, polifenólica y antiproliferativa de la castaña de agua extraída en diferentes solventes. La actividad antioxidante del extracto en diferentes solventes fue máxima en metanol, seguida por etanol y acuoso, además de encontrarse que era de 39,8%; 34,1% y 32,6%; en el ensayo DPPH y 45%; 64%; 35,08% y 30,52% en el ensayo de peroxidación lipídica respectivamente, mientras que el ensayo de reducción del poder de inhibición mostró el máximo potencial antioxidante en el extracto acuoso de la muestra, seguido por los extractos de metanol y etanol. Se encontró que el contenido polifenólico de la castaña de agua era más presente en metanol que en los extractos acuosos y de etanol. El extracto de castaña de agua también mostró el potencial antiproliferativo cuando se analizadó frente a la línea de la célula humana de cáncer de colon (Colo-205), la línea de la célula humana de tumor ductal epitelial de pecho (T47D) y la línea de la célula humana del adenocarcinoma de pecho (MCF7). También mostró cierta protección del daño del ADN inducido por radicales hidroxilos en ADN de timo de ternera.Palabras clave: castaña de agua; escisión inhibitoria del ADN; actividad antioxidante; actividad antiproliferativa

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Section: Antiproliferative Assaymentioning

confidence: 99%

DNA scission inhibition, antioxidant, and antiproliferative activities of water chestnut (Trapa natans) extracted in different solvents

Gani

Rasool

Shah

et al. 2015

CyTA - Journal of Food

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“…Flavonoids are known to block the initiation, promotion, and progression of cancer by modulating various signaling pathways that have significant roles in cell proliferation, differentiation, apoptosis, angiogenesis, and metastasis [5]. Thus, flavonoids (both natural and synthetic analogs) are being investigated for their potentials in cancer therapy.…”

Section: Discussionmentioning

confidence: 99%

“…Of these phytochemicals, flavonoids widely distributed in plants have received increasing attention for their potential chemopreventive role, because they have been known to impair cancer cell growth by modulating various signaling pathways involved in different stages of cancer development as well as inducing apoptosis [5].…”

Section: Introductionmentioning

confidence: 99%

The pleiotropic effects of fisetin and hesperetin on human acute promyelocytic leukemia cells are mediated through apoptosis, cell cycle arrest, and alterations in signaling networks

Adan

Baran

2015

Tumor Biol.

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Fisetin and hesperetin, flavonoids from various plants, have several pharmaceutical activities including antioxidative, anti-inflammatory, and anticancer effects. However, studies elucidating the role and the mechanism(s) of action of fisetin and hesperetin in acute promyelocytic leukemia are absent. In this study, we investigated the mechanism of the antiproliferative and apoptotic actions exerted by fisetin and hesperetin on human HL60 acute promyelocytic leukemia cells. The viability of HL60 cells was evaluated using the MTT assay, apoptosis by annexin V/propidium iodide (PI) staining and cell cycle distribution using flow cytometry, and changes in caspase-3 enzyme activity and mitochondrial transmembrane potential. Moreover, we performed wholegenome microarray gene expression analysis to reveal genes affected by fisetin and hesperetin that can be important for developing of future targeted therapy. Based on data obtained from microarray analysis, we also described biological networks modulated after fisetin and hesperetin treatment by KEGG and IPA analysis. Fisetin and hesperetin treatment showed a concentration-and time-dependent inhibition of proliferation and induced G2/M arrest for both agents and G0/G1 arrest for hesperetin at only the highest concentrations. There was a disruption of mitochondrial membrane potential together with increased caspase-3 activity. Furthermore, fisetin-and hesperetin-triggered apoptosis was confirmed by annexin V/PI analysis. The microarray gene profiling analysis revealed some important biological pathways including mitogen-activated protein kinases (MAPK) and inhibitor of DNA binding (ID) signaling pathways altered by fisetin and hesperetin treatment as well as gave a list of genes modulated ≥2-fold involved in cell proliferation, cell division, and apoptosis. Altogether, data suggested that fisetin and hesperetin have anticancer properties and deserve further investigation.

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“…As an anti-cancer agent, flavonoids block the cell cycle and induce apoptosis, disrupting cell division and growth [11]. A wide range of targets for other diseases has also been introduced herein.…”

Section: Resultsmentioning

confidence: 99%

“…The flavonoids block the cell cycle causing apoptosis and disrupts mitotic spindle formation, which is needed for cell division. Therefore, flavonoids make them promising not only for therapeutic drugs for many other illnesses but also make them promising lead compounds in anti-cancer research [11].…”

Section: The Relevance Of Flavonoids For Medicinal Chemistry and Drugmentioning

confidence: 99%

Structural Analysis of Flavonoid/Drug Target Complexes: Natural Products as Lead Compounds for Drug Development

Sosa¹,

Sosa²,

Phansalkar³

et al. 2017

Nat Prod Chem Res

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Plants produce pigments called flavonoids that are synthesized (de novo) primarily from the amino acid phenylalanine. Many natural products such as herb preparations for medicinal use contain flavonoids and so these diverse structural compounds have become potential lead compounds for a variety of illnesses ranging from specific cancers to gout. Recently, Biotechnology has been utilized through bioorganic engineering to manufacture flavonoid and modified flavonoids for medicinal applications. A growing number of protein-flavonoid complexes have been crystallized and their structures solved in the last decade. A summary of the protein-flavonoid complexes with medicinal relevance is presented herein. A detailed analysis of selected protein-flavonoid complexes is provided. The goal is to provide insights for modifications to known flavonoids that could be biomanufactured to generate more specific and efficient binding of flavonoids to protein targets with medicinal relevance.

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Flavonoids as prospective compounds for anti-cancer therapy

Cited by 491 publications

References 115 publications

DNA scission inhibition, antioxidant, and antiproliferative activities of water chestnut (Trapa natans) extracted in different solvents

DNA scission inhibition, antioxidant, and antiproliferative activities of water chestnut (Trapa natans) extracted in different solvents

The pleiotropic effects of fisetin and hesperetin on human acute promyelocytic leukemia cells are mediated through apoptosis, cell cycle arrest, and alterations in signaling networks

Structural Analysis of Flavonoid/Drug Target Complexes: Natural Products as Lead Compounds for Drug Development

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