<i>In Vitro</i> Evaluation of Selected Benzimidazole Derivatives as an Antioxidant and Xanthine Oxidase Inhibitors

Nile, Shivraj Hariram; Kumar, Brajesh; Park, Se W.

doi:10.1111/cbdd.12141

Cited by 62 publications

(49 citation statements)

References 42 publications

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“…All other phenolic compounds showed potent inhibitory activity within the range 5.5-7.2% as compared to allopurinol (7.5%) IC 50 in lM (Table 2). Phenolics are also effective inhibitors of several enzymes including XO, cyclooxygenase, and lipoxygenase (23,34). Flavonoids and phenolics are wellknown antioxidants and attract a tremendous amount of interest among researchers as possible therapeutic agents for diseases mediated by free radicals.…”

Section: Xanthine Oxidase Inhibitionmentioning

confidence: 99%

Antioxidant, α‐Glucosidase and Xanthine Oxidase Inhibitory Activity of Bioactive Compounds From Maize (Zea mays L.)

Nile

Park

2013

Chem Biol Drug Des

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Chemical investigations into maize (Zea mays L.) kernels yielded phenolic compounds, which were structurally established using chromatographic and spectroscopic methods. The isolated phenolic compounds from maize kernel were examined in vitro for their antioxidant abilities by DPPH (2,2-diphenyl-1-picryl hydrazine) radical, OH radical scavenging activity, and reducing ability, along with α-glucosidase and xanthine oxidase (XO) inhibition. The isolated maize phenolics revealed significant xanthine oxidase and α-glucosidase inhibitory activity to that of allopurinol and acarbose in vitro and in vivo, respectively. The kinetics study with xanthine oxidase revealed competitive type of inhibition by isolated maize vanillic acid (M2), ferulic acid (M5), 3'-methoxyhirsutrin (M7), and peonidin-3-glucoside (M10) as compared to control allopurinol. Overall, with few exceptions, all the phenolic compounds from maize kernel revealed significant biological activities with all parameters examined. Also, the phenolic compounds from maize were found to be more reactive toward DPPH radical and had considerable reducing ability and OH radical scavenging activity. These findings suggest that maize kernel phenolic compounds can be considered as potential antioxidant, α-glucosidase, and XO inhibitory agents those might be further explored for the design of lead antioxidant, antidiabetic and antigout drug candidates using in vivo trials.

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Section: Xanthine Oxidase Inhibitionmentioning

confidence: 99%

Antioxidant, α‐Glucosidase and Xanthine Oxidase Inhibitory Activity of Bioactive Compounds From Maize (Zea mays L.)

Nile

Park

2013

Chem Biol Drug Des

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“…Onion flavonoids and phenolics are well-known antioxidants and attract a tremendous amount of interest among researchers as possible therapeutic agents for diseases mediated by free radicals. Phenolics are also effective inhibitors of several enzymes including XO, cyclooxygenase, and lipooxigenase (Hoorn et al 2002; Nile et al 2013). Thus, the phenolic constituents may play an essential role in the inhibition of XO.…”

Section: Xanthine Oxidase Inhibitionmentioning

confidence: 99%

Total phenolics, antioxidant and xanthine oxidase inhibitory activity of three colored onions (Allium cepaL.)

Nile¹,

Park²

2013

Frontiers in Life Science

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Methanolic extracts from bulbs of three onion (Allium cepa L.) varieties: red (Pusa Red), white (Pusa White Round), and yellow (Arka Pitamber) and the CHCl 3 , Et 2 O, EtOAc, and n-BuOH fractions obtained from those extracts were investigated for their total phenolics and antioxidant activity. The antioxidant activity measurements, expressed as total antioxidant status (TAS), were 5.2-50.18, 2.2-35.6 and 3.5-42.2 mg ml −1 for red, white and yellow onion bulb extracts, respectively, as compared to trolox (IC 50 , 40.2 mg ml −1 ). The total phenolic content of the samples was 62-186, 56-156 and 68-165 mg GAE ml −1 for red, white and yellow onion bulb extracts, respectively, with all solvents. There was a positive correlation between the total phenolic content and antioxidant activity for MeOH extracts and EtOAc fractions (R 2 = 0.96, 0.8 respectively). Of the selected colored onion bulbs the red onion (IC 50 = 14.2 μg ml −1 ) revealed more potent xanthine oxidase inhibitory activity to those of yellow (IC 50 = 15.5 μg ml −1 ) and white onion (IC 50 = 17.0 μg ml −1 ) in vitro and as compared to control allopurinol (IC 50 = 10.5 μg ml −1 ). The kinetic study by xanthine oxidase revealed that the white and yellow onion extracts were non-competitive inhibitors, as K m values were constant, while V max consequently decreased with increased inhibitor concentration. In the red onion extract there was an increase in K m values while V max remained constant at all extract concentrations, thus confirming a competitive type of inhibition by the Lineweaver-Burk equation. These findings suggest that these onion varieties can be considered as potential sources of antioxidants and XO inhibitory agents.

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“…[34–36] It is also possible that our benzimidazole derivatives could potentially reduce ROS levels. A series of compounds were designed and tested to determine their potential use in AD treatment.…”

Section: Resultsmentioning

confidence: 99%

Identification of human presequence protease (hPreP) agonists for the treatment of Alzheimer's disease

Vangavaragu

Valasani

Gan

et al. 2014

European Journal of Medicinal Chemistry

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Amyloid-β (Aβ), a neurotoxic peptide, is linked to the onset of Alzheimer’s disease (AD). Increased Aβ content within neuronal cell mitochondria is a pathological feature in both human and mouse models with AD. This accumulation of Aβ within the mitochondrial landscape perpetuates increased free radical production and activation of the apoptotic pathway. Human Presequence Protease (hPreP) is responsible for the degradation of mitochondrial amyloid-β peptide in human neuronal cells, and is thus an attractive target to increase the proteolysis of Aβ. Therefore, it offers a potential target for Alzheimer’s drug design, by identifying potential activators of hPreP. We applied structure-based drug design, combined with experimental methodologies to investigate the ability of various compounds to enhance hPreP proteolytic activity. Compounds 3c & 4c enhanced hPreP-mediated proteolysis of Aβ (1–42), pF1β (2–54) and fluorogenic-substrate V. These results suggest that activation of hPreP by small benzimidazole derivatives provide a promising avenue for AD treatment.

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In Vitro Evaluation of Selected Benzimidazole Derivatives as an Antioxidant and Xanthine Oxidase Inhibitors

Cited by 62 publications

References 42 publications

Antioxidant, α‐Glucosidase and Xanthine Oxidase Inhibitory Activity of Bioactive Compounds From Maize (Zea mays L.)

Antioxidant, α‐Glucosidase and Xanthine Oxidase Inhibitory Activity of Bioactive Compounds From Maize (Zea mays L.)

Total phenolics, antioxidant and xanthine oxidase inhibitory activity of three colored onions (Allium cepaL.)

Identification of human presequence protease (hPreP) agonists for the treatment of Alzheimer's disease

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