• Korean Journal of Pharmacognosy
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• v.36 no.1 s.140
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• pp.56-59
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• 2005

Urease plays an important role in the urea metabolism and the effect of urease activity on human and environment is enormous. For instance, urease acts as a virulence factor of the urinary and gastrointestinal tracts infections in human and animal, being involved in kidney stone formation, catheter encrusatation, pyelonephritis, ammonia encephalopathy, hepatic coma, and urinary tract infections. Widespread urease activity in soil induces a plant damage due to ammonia toxicity and pH increase. Therefore, urease activity regulation through urease inhibitors would lead to an enhanced efficiency of urea nitrogen uptake in plants and to the improved therapeutic strategies for ureolytic bacterial infections. To search for new inhibitory compounds on urease activity from herbs, MeOH extracts of herbs were screened. Among of them, the MeOH extracts of Areca catechu exhibited an excellent inhibitory effect on urease activity. Two compounds were isolated from the ethyl acetate fraction by the activity guided fractionation. Their chemical structures were identified as (+)-catechin(compound I) and allantoin(compound II) by spectroscopic evidence, respectively. Compound I showed a stronger inhibitory effect on urease activity than compound II.

• KSBB Journal
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• v.23 no.3
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• pp.239-244
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• 2008

For physiological function of aloe concentrate by ultrafiltration (UF) process, jack bean urease inhibitory activity and bentonite flocculating activity of UF aloe concentrate was investigated and compared with fresh aloe gel. Urease inhibitory activity of UF aloe concentrate ranged from 87 to 90% in 1 mL sample. Also, urease inhibitory activity of UF aloe concentrate increased about 10% by heat treatment showing the heat stability. From Lineweaver-Burk plot for UF aloe concentrate, urease inhibition pattern indicated general non-competitive inhibition. From flocculation test of UF aloe concentrate about 1% (w/v) bentonite suspension, maximum flocclulating activity of 97% was obtained at 0.5 mL addition of UF aloe concentrate/ 5 ml bentonite suspension. However, flocculating activity of 81% was obtained at 1 mL addition of UF aloe concentrate/ 5 mL bentonite suspension, which was typical flocculating behavior of polymers with re-dispersion at overdose area. FT-IR spectra of UF aloe concentrate showed the characteristic patterns of $\beta$-binding polysaccharide and less deacetylation indicating higher level of bioactive polysaccharide content.

• Archives of Pharmacal Research
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• v.9 no.3
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• pp.163-167
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• 1986

Twenty six urea analogues, most of which have already been approved for human use, were tested for their antiurease activity in vitro. Cell-free extracts obtained from a clinical isolate of Proteus mirabilis was used as the source of enzyme. Acetohydroxamic acid which is a proven potent urease inhibitor but not approved for human use was again shown to be the most active compound among the tested. Phenacemide, cycloserine, and deferoxamine were demonstrated to be moderate inhibitors. Oxtetracycline, trimethoprim, and cefamandole revealed a demonstrable antiruease activity, but only at very high concentrations. The antiurease activity of cycloserine, trimethoprim, and cefamandole was pH dependent-only active at acidic pH. The inhibitory activity of acetohydroxamic acid however was independent of change in pH. The inhibitory activity of acetohydroxamic acid however was independent of change in pH. Hydrogen ion concentration plays an important role in urease activity and acidification (pH 5. 5) alone eliminates approximately 65% of the enzymic activity. Adjustment of pH therefore appears to be an important adjunct in reducing unrease activity and should always be studied to maximize the effcacy of antiurease compounds under investigation.

• Food Engineering Progress
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• v.13 no.4
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• pp.251-261
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• 2009

In vitro physiological functions such as jack bean (Canavalia ensiformis) urease inhibitory activity and retarding effect of glucose/bile acid of Aloe vera gel concentrated by the optimized DIS (Dewatering Impregnation & Soaking) process conditions were examined. Urease inhibitory activity of DIS aloes ranged from 84.6 to 94.4%, which was similar to or higher than 86.3% of fresh aloe. Also, urease inhibitory activity of DIS aloes was maintained at initial levels after heat treatment (90$^{\circ}C$, 10 min.) and drying treatment (freeze or hot air drying). Urease inhibition pattern from Lineweaver-Burk plot indicated general non-competitive inhibition, and inhibition constants ($K_{IE}$ and $K_{IES}$) of DIS aloes were 41-149 and 87-163 $\mu$L/mL, respectively. DIS(glucose) and DIS(polyethylene glycol) exhibited the highest retarding effect of glucose and bile acid. Their retarding effects were about 1.6 and 1.8 folds higher than that of fresh aloe after 0.5 and 1 hr of the dialysis, respectively. Conclusively, the above in vitro physiological functions of Aloe vera gel concentrated by DIS process suggested that aloe products treated with DIS would have the potential benefits for protection against Helicobacter pylori and reduction of blood glucose and cholesterol levels.

• Applied Biological Chemistry
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• v.46 no.2
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• pp.74-78
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• 2003

To determine the urease inhibitory activity of various heavy metal ions, a photometric cuvette assay for measuring ammonia production was developed. In this assay, the absorbance values at 630 m were linearly increased according to the ammonia concentrations up to 3.0 mg/l (r : 0.998). The urease inhibitions upon addition of a single species of heavy metal ions were in the decreasing order of Hg(II) > Pb(II) > Cu(II) > Cd(II) > Zn(II) ions. As expected, the urease inhibitions at a fixed concentration of a single species and at varying concentrations of other species occurred in the additive way. The above results show the applicability of the current method to the selective detection on Hg(II) ions as well as the screening of heavy metal ions possibly present at various samples.

• Korean Journal of Microbiology
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• v.37 no.2
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• pp.151-157
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• 2001

This study was conducted to select lactic acid bacteria which possess potential inhibitory effect on Helicobacter pylori, and to make feasibility test of fermented milk products using them. In order to select lactic acid bacteria specifically inhibiting the growth of H. pylori, antibacterial activity using paper disk method, adherence ability to Caco-2 cell inhibitory effect on urease activity of H. pylori, and milk fermentation feasibility were measured. Among 45 strains of lactic acid bacteria tested, 28 strains showed clear zone and Lactobacillus gasseri MK-03 showed the largest clear zone. Caco-2 cell adherence by lactic acid bacteria and inhibitory effect of them on H. pylori adherence were also evaluated. Of 28 strains tested, 18 strains appeared to be effective on adherence to Caco-2 cell, and especially Bifidobacterium longum MK-26 was found to be superior to others. When Bif. longum MK-26 and H. pylori were reacted with Caco-2 cell 2hrs before, adherence percentage of H. pylori decreased from 0.105% to 0.004%. To investigate inhibitory effect of lactic acid bacteria-derived supernatant on urease activity of H. pylori, pH-adjusted fermented supernatant(pH-4.4) was assessed by co-cultivation method. There of Lb. acidophilus MK-07-derived supernatant showed the most inhibitory effect on urease activity of H. pylori. Considering milk fermentation ability of selected 3 strains, they were comparably feasible to fermented milk products. Consequently, Lb. gasseri MK-03, Lb. acidophilus MK-07, and Bif. longum MK-26 were selected to specifically inhibit the growth of H. pylori, by antibacterial activity, inhibition of urease activity, and inhibition of Caco-2 cell adherence, respectively.

• Natural Product Sciences
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• v.23 no.1
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• pp.46-52
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• 2017

The aim of this study was to evaluate the anti-Helicobacter pylori activity of fractions and major aglycon compounds (baicalein, chrysin, oroxylin A, wogonin) of Scutellariae Radix. Minimum inhibitory concentration (MIC) measurement, DPPH radical-scavenging assay, DNA protection assay, and urease inhibition analysis were performed. The ethyl acetate (EtOAc) fraction showed the potent anti-Helicobacter activity, and therefore, compounds in the EtOAc fraction were subjected to further assay. The MICs of chrysin, oroxylin A, and wogonin against Helicobacter pylori 26695 were 6.25, 12.5 and $25{\mu}g/mL$, respectively. Baicalein exhibited the most effective DPPH radical-scavenging activity. DNA protection using Fenton reaction, chrysin, oroxylin A, and wogonin showed effective DNA protective effect. This result was also confirmed by quantitative real-time polymerase chain reaction (qRT-PCR). Regarding Jack bean urease (0.5 mg/mL, 50 unit/mg) inhibition, 20 mM ofbaicalein and chrysin inhibited urease activity by 88.2% and 72.5%, respectively.

• Journal of the Korean Society of Food Science and Nutrition
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• v.33 no.5
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• pp.769-777
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• 2004

A Helicobacter pylori urease inhibitor from Rubus coreanus Miquel has been isolated and partially characterized for aiming to Prevent H. pylori growth and decrease harmful accumulation of ammonia in human gastric mucosa. We screened urease inhibitory activities in 519 extracts library prepared by solvent extraction from 173 kinds of edible plants, medicinal herbs, herbs and seaweeds using a colorimetric urease assay system. As results of primary and secondary screening, 70% acetone extract of Rubus coreanus Miquel was selected as potent candidate, showing about 24% inhibitory activity. The acetone extract was sequentially partitioned into RCE/RCWI and RCB/RCW2 layers with ethyl acetate and butanol. The major active component in RCW2, water layer from butanol fractionation was revealed to be peptidic or proteinous substance by inhibitory activity determination after pronase digestion and periodate oxidation. RCW2-IIIc a was isolated by sequential column chromatography on DEAE-Toyopearl 650C, Butrl-Toyopearl 650M and Sephadex LH-20. The isolated urease inhibitor RCW2-IIIc $\alpha$, was highly pure proteinous substance with molecular weight of 13kDa by high-performance gel permeation liquid chromatography. RCW2-IIIc$\alpha$ has about 5 times higher inhibitory activity than 70％ acetone extract, showing high stability against heat treatment and peptic digestion.

• Microbiology and Biotechnology Letters
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• v.45 no.3
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• pp.265-270
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• 2017

A key virulence factor for urinary tract pathogens is the enzyme urease, which catalyzes the hydrolysis of urea into ammonium ions and carbonic acid. Urease activity plays an important role in the pathogenesis of urinary tract infection. In this study, the inhibitory effect of zerumbone against six urease-producing bacteria (Klebsiella oxytoca, K. pneumoniae, Morganella morganii, Proteus mirabilis, P. vulgaris, and Staphylococcus saprophyticus) and their urease activities were evaluated. The results of the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) tests showed that zerumbone had antibacterial effect against these six urease-producing bacteria. The MIC and MBC of zerumbone ranged from 0.5 to 2 mM and 1 to 4 mM, respectively. In the urease inhibitory assay, zerumbone showed better urease inhibition ($56.28{\pm}2.45-37.83{\pm}3.47%$) than the standard urease inhibitor, acetohydroxamic acid ($40.46{\pm}1.94-22.99{\pm}3.53%$). However, zerumbone did not affect the levels of the urease subunit. These results clearly indicated that zerumbone has antibacterial potential against urease-producing bacteria and possesses excellent bacterial urease inhibition properties.

• Food Science and Biotechnology
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• v.15 no.3
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• pp.466-468
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• 2006

The antimicrobial effect of a novel flavonoid (7-O-butyl naringenin) on Helicobacter pylori ATCC 26695 and its inhibitory effects on the urease activity of the strain were evaluated by comparing with quercetin and naringenin. H. pylori was cultured with brain heart infusion supplemented with 5% horse serum at $37^{\circ}C$ under 10% $CO_2$ atmosphere and the inhibitory effects of flavonoids against the strain were detected using micro-plate methods. During 12 hr of incubation time, the optical densities of phenol red reduced (pink color) in the urea broth by producing ammonia were detected at 560 nm with a spectrophotometer. The results indicated that both quercetin and 7-O-butyl naringenin were effective against the growth of H. pylori. Moreover, inhibitory effect of 7-O-butyl naringenin on the growth of H. pylori was about two-fold higher than quercetin at the same concentration. With regard to H. pylori urease activity, 7-O-butyl naringenin had a greater inhibitory effect than did naringenin or quercetin at the same concentration.