Ascorbic acid-enhanced antiproliferative effect of flavonoids on squamous cell carcinoma in vitro

Kandaswami, Chithan; Perkins, Eddie; Soloniuk, Donald S.; Drzewiecki, G.; Middleton, Elliott

doi:10.1097/00001813-199302000-00012

Cited by 47 publications

(26 citation statements)

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“…Flavonoids constitute a group of interesting polyphenolic compounds with a wide distribution in fruits and vegetables (27,28) and have been shown to exert a wide range of beneficial effects on human health, including protection against cardiovascular diseases and different forms of cancers (18). In the past decade, some flavonoids have been implicated in the modulation of P-gp-type MDR in cancers and shown to inhibit a variety of ATP-binding proteins such as plasma membrane ATPase (24,44), cyclic AMP-dependent protein kinase (25), and protein kinase C (17).…”

mentioning

confidence: 99%

Flavonoid Dimers as Bivalent Modulators for Pentamidine and Sodium StiboglucanateResistance in Leishmania

Wong

Chan

Burkett

et al. 2007

Antimicrob Agents Chemother

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Drug resistance by overexpression of ATP-binding cassette (ABC) transporters is an impediment in the treatment of leishmaniasis. Flavonoids are known to reverse multidrug resistance (MDR) in Leishmania and mammalian cancers by inhibiting ABC transporters. Here, we found that synthetic flavonoid dimers with three (compound 9c) or four (compound 9d) ethylene glycol units exhibited a significantly higher reversing activity than other shorter or longer ethylene glycol-ligated dimers, with ϳ3-fold sensitization of pentamidine and sodium stibogluconate (SSG) resistance in Leishmania, respectively. This modulatory effect was dosage dependent and not observed in apigenin monomers with the linker, suggesting that the modulatory effect is due to its bivalent nature. The mechanism of reversal activity was due to increased intracellular accumulation of pentamidine and total antimony in Leishmania. Compared to other MDR modulators such as verapamil, reserpine, quinine, quinacrine, and quinidine, compounds 9c and 9d were the only agents that can reverse SSG resistance. In terms of reversing pentamidine resistance, 9c and 9d have activities comparable to those of reserpine and quinacrine. Modulators 9c and 9d exhibited reversal activity on pentamidine resistance among LeMDR1 ؊/؊ , LeMDR1 ؉/؉ , and LeMDR1-overexpressed mutants, suggesting that these modulators are specific to a non-LeMDR1 pentamidine transporter. The LeMDR1 copy number is inversely related to pentamidine resistance, suggesting that it might be involved in importing pentamidine into the mitochondria. In summary, bivalency could be a useful strategy for the development of more potent ABC transporter modulators and flavonoid dimers represent a promising reversal agent for overcoming pentamidine and SSG resistance in parasite Leishmania.

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confidence: 99%

Flavonoid Dimers as Bivalent Modulators for Pentamidine and Sodium StiboglucanateResistance in Leishmania

Wong

Chan

Burkett

et al. 2007

Antimicrob Agents Chemother

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“…At 20 µg/kg/d dose, chrysin was more active against sarcoma 180 than other concentrations tested. Some investigators have suggested that the growth inhibition activity of polymethoxylated flavonoids may, in part, be attributed due to their chemical stability [45] . At the concentration of 90 µg/ml, chrysin inhibited colony formation of Chinese hamster V79 cells more effectively than luteolin.…”

Section: Resultsmentioning

confidence: 99%

In vitro and in vivo Evaluation of Flavonoids from Heliotropium ellipticum Exudate for Antioxidant, Antineoplastic and Cytotoxic Activities II

Singh¹,

Sahu²,

Sharma³

2017

pharmaceutical-sciences

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“…[34][35][36] For the reason that, ascorbate is reported to have flavonoid protective 37,38) and flavonoid-enhancing activities. 39,40) But, Ghosal et al (1996), 41) have reported that the potent vitamin C like activity of P. emblica is due to the presence of low molecular weight hydrolysable tannins (emblicanin-A and emblicanin-B). Hence, it can be postulated that the enhanced antioxidant effect of KA than SA alone might be attributed to the synergistic effect of flavonoids, vitamin C and tannins present in KA.…”

Section: Discussionmentioning

confidence: 99%

Free Radical Quenching and Immunomodulatory Effect of a Modified Siddha Preparation, Kalpaamruthaa

Arulkumaran

Ramprasath

Shanthi

et al. 2007

JOURNAL OF HEALTH SCIENCE

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Kalpaamruthaa (KA), a modified indigenous Siddha formulation constitutes Semecarpus anacardium nut milk extract (SA), Phyllanthus emblica and honey. The present study attempt has been to investigate the antioxidant and immunomodulatory activities of KA. Antioxidant activity of KA was determined by using ferric thiocyanate and thiobarbituric acid methods. KA showed higher antioxidant activity when compared with vitamin E (α-tochoperol), a well-known antioxidant. Immunomodulatory activities on humoral and cellular immunity were studied by heamagglutination (HA) titre, delayed type hypersensitivity (DTH) and phagocytic index. KA was administered at the dosage level of 100, 150, 200, 250 and 300 mg/kg body weight. Also, KA enhanced the HA titre, phagocytic index and delayed type hypersensitivity in a dose dependent manner, which indicates that KA triggers both humoral and cell mediated immune responses to a greater extent. This improved antioxidant and immunomodulatory activities of KA might be due to the synergistic effect of flavonoids, vitamin C and hydrolysable tannins present in the drug. The current study shows that KA is effective at the dosage level of 200 mg/kg body weight were significantly induced immunomodulatory activity in a dose dependant manner.

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Ascorbic acid-enhanced antiproliferative effect of flavonoids on squamous cell carcinoma in vitro

Cited by 47 publications

References 0 publications

Flavonoid Dimers as Bivalent Modulators for Pentamidine and Sodium StiboglucanateResistance in Leishmania

Flavonoid Dimers as Bivalent Modulators for Pentamidine and Sodium StiboglucanateResistance in Leishmania

In vitro and in vivo Evaluation of Flavonoids from Heliotropium ellipticum Exudate for Antioxidant, Antineoplastic and Cytotoxic Activities II

Free Radical Quenching and Immunomodulatory Effect of a Modified Siddha Preparation, Kalpaamruthaa

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