Flavonoids as Natural Inhibitors of Jack Bean Urease Enzyme

Author(s): Jalaluddin A. J. Awllia, Maryam AL-Ghamdi, Etimad Huwait, Sumaira Javaid, Atia-tul-Wahab, Saima Rasheed, M. Iqbal Choudhary

Journal Name: Letters in Drug Design & Discovery

Volume 13 , Issue 3 , 2016

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Abstract:

Enzyme urease plays an important role in several pathologies, such as urolithiasis, urinary catheter encrustation, hepatic encephalopathy, peptic ulcers, and gastric cancers. Its inhibition, therefore, has a major therapeutic significance. For this purpose, nine natural flavonoids 1-9 were evaluated for their urease inhibitory activity. Five of them (i.e. 1, 3, 7, 8, and 9) showed a urease inhibitory activity with IC50 values between 14.2 – 132.9 µM. Compounds 3, 8, and 9 showed a potent activity (IC50 =19.4 ± 1.39, 14.2 ± 0.30 and 17.7 ± 0.23 μM, respectively), in comparison to the standard urease inhibitor, acetohydroxamic acid (IC50 = 41.5 ± 1.50 µM). Furthermore, compounds 1, 7, and 9 exhibited a competitive mode of inhibition. Compounds 1, 3, 7, 8 and 9 were finally tested for cytotoxicity by using mouse fibroblast cell line (3T3 cell line) assay. Compounds 1, 3 and 7 were found non-cytotoxic, while compounds 8 and 9 showed some level of toxicity (IC50 = 18.75 ± 0.45 and 13.01 ± 0.70 µM, respectively). Present study identifies flavonoid 8 as a lead for further investigation towards designing novel urease inhibitors for the treatment of diseases associated with ureolytic bacteria.

Keywords: Flavonoids, peptic ulcer, urease inhibition, urolithiasis, mechanistic studies, cytotoxicity.

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Article Details

VOLUME: 13
ISSUE: 3
Year: 2016
Page: [243 - 249]
Pages: 7
DOI: 10.2174/1570180812666150914220050
Price: $65

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