Inhibition activities of natural products on serine proteases

Jedinák, Andrej; Maliar, Tibor; Grančai, D; Nagy, Milan

doi:10.1002/ptr.1836

Cited by 54 publications

(38 citation statements)

References 9 publications

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“…Strategies to search for natural compounds based on ethno-botanical and chemo-taxonomical studies were described (Basso et al 2005). The present work followed also the previous study on inhibition activities of limited number of phenolic compounds toward serine proteases (Jedinák et al 2006).…”

Section: Resultsmentioning

confidence: 78%

Proteinase inhibition and antioxidant activity of selected forage crops

et al. 2010

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The hypothesis of the possible therapeutic potential of selected species of forage crops is discussed. Extracts from genotypes of Anthyllis sp., Astragalus sp., Coronilla sp., Lotus sp., Medicago sp., Melilotus sp., Onobrychis sp. and Trifolium sp. were prepared and tested for proteinase inhibition and antioxidant activities. We found that Trifolium pratense accession POLKIE99-3 expressed the highest relative trypsin inhibition activity (80.0%) compared to standards. The highest thrombin inhibition activity (81.4%) was detected in the Medicago sativa old cultivar Hodonínka, whereas the highest relative urokinase inhibition activity (62.5%) was expressed by the local population Nitranka. Relatively high antioxidant properties of Trifolium sp. accessions, Trifolium pratense genetic resources SVKZAH98-40, were of interest. Results of this study confirmed that there are significant differences in proteinase inhibition and antioxidant activity among important selected agricultural crops. The present paper may also be the starting point of the research aimed for development of new functional food and nutraceuticals, and/or of the research focused on new secondary metabolites with potential as bioactive compounds.Key words: trypsin; thrombin; urokinase; inhibition; antioxidant; activity; forage crops.Abbreviations: AOX, antioxidant activity; BBI, Bowman-Birk inhibitor; DMSO, dimethyl sulphoxide; Rel%BT, relative percentage value of activity to standardized black tea extract; Rel%Q, relative percentage value of activity to standard quercetin; SHE, sunflower oil hydrolysate ethanol; SITh, selectivity index of thrombin; SIU, selectivity index of urokinase; ThIA, thrombin inhibition activity; TrIA, trypsin inhibition activities; UIA, urokinase inhibition activity.

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Section: Resultsmentioning

confidence: 78%

Proteinase inhibition and antioxidant activity of selected forage crops

et al. 2010

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“…2,21,22 Moreover, quercetin has been shown to inhibit amylase release induced by agonists such as cholecystokinin, carbachol, phorbol ester tetra decanoylphorbol-13--acetate. [23][24][25] A recent study has shown that one hour after the last dose of cerulein administration, quercetin treatment attenuates the development of AP in mice. The aim of the present study was to evaluate the protective and therapeutic effects of quercetin on pancreatic injury in cerulein-induced acute pancreatitis in rats.…”

Section: Methodsmentioning

confidence: 99%

The effect of quercetin on cerulein-induced acute pancreatitis

Kahraman¹,

Vurmaz²,

Koca³

et al. 2017

Medical Express

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OBJECTIVE:The aim of this study was to evaluate the protective and therapeutic effects of quercetin on pancreatic injury in cerulein-induced acute pancreatitis. METHOD: Thirty-two rats were randomly divided into four groups, eight per group: (CT): untreated controls, (CER) treated with cerulein, 50 μg/kg body weight; (Q+CER) pre-treatment with quercetin, 100 mg/kg body weight, followed by cerulein, 50 μg/kg; (CER+Q) post-treatment, cerulein followed by quercetin, same doses. Cerulein was divided into four doses, given at 1-hour intervals by intraperitoneal injection. Quercetin was given either 1-hour before (in pre-treatment group) or 1-hour after (in post-treatment group) cerulein. Pancreatic malondialdehyde (MDA), carbonyl, myeloperoxidase (MPO), tumor necrosis factor-alpha (TNF-a), interleukin-6 (IL-6), reduced and oxidized glutathione (GSH and GSSG, respectively) were measured. Histology of the pancreas was studied. RESULTS: (1) MDA, carbonyl, MPO, TNF-a and IL-6 levels were significantly higher in CER vs CT rats. (2) MDA, carbonyl, MPO and TNF-α decreased significantly in pre-treated rats vs. CER. (3) MDA, MPO, TNF-α, IL-6 were significantly lower in post-treated rats vs. CER. (4) The reduced vs. oxidized glutathione ratio (GSH/GSSG) of was significantly lower CER vs. CT rats. (5) Pre-and post-treatment with quercetin significantly increased this ratio. (6) Pancreatic histology showed that quercetin had no significant effect on the histological image of the pancreas CONCLUSION: These results suggest that quercetin can attenuate the severity of cerulein-induced acute pancreatitis by acting as an antioxidant and anti-inflammatory agent and combating oxidative stress. Further studies are needed to clearly explain its utility on acute pancreatitis.

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“…var, major recorded in the Chinese Pharmacopoeia, 1) mainly contain hyperoside (HP), a ‰avonol glycoside, whose quality is controlled via determining HP using highperformance liquid chromatographic (HPLC) method. Thereby, many researches about HP appeared in literature, such as, the treatment of antidepressant, 2) cancer therapy, 3) strong inhibitor of HBsAg and HBeAg secretion in 2.2.15 cells and DHBV-DNA levels in the HBV-infected duck model, 4) possessing cytoprotective properties against oxidative stress by scavenging intracellular ROS and enhancing antioxidant enzyme activity, 5) protecting against the oxidative damage induced by TBHP, 6) and remarkable wound healing and anti-in‰ammatory. 7) Otherwise, many methods including capillary zone electrophoresis with electrochemical detection, 8) HPLC 9 11) and LC-MS/MS 12) have been reported for quantiˆcation of HP in various herbal medicines and biological ‰uids.…”

Section: Introductionmentioning

confidence: 99%

LC Determination and Pharmacokinetic Study of Hyperoside in Rat Plasma after Intravenous Administration

et al. 2010

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A simple and speciˆc high-performance liquid chromatographic (HPLC) method was developed for the pharmacokinetic study of hyperoside (HP, isolated from the leaves of Crataegus pinnatiˆda Bge. var. major ) in rats after intravenous administration. The plasma samples were deproteinized with methanol after addition of internal standard (I.S.), baicalin. HPLC analysis was performed on a Diamonsil C18 analytical column, using methanol-0.6％ aqueous phosphoric acid (45：55, v/v) as the mobile phase with UV detection at 340 nm. The calibration curve was linear over the range of 0.8921 59.7125 mg/ml in rat plasma. The average extraction recovery of HP was 99.33±0.86％, and the relative standard deviations (R.S.D.s) of the intra-and inter-day precisions were no more than 7.8 and 2.5％, respectively. The lower limit of quantiˆcation (LLOQ) was 0.8921 mg/ml. The validated method was successfully applied during a pharmacokinetic study in rats after intravenous administration of HP at diŠerent doses, and all the results indicated that the pharmacokinetics of HP in rats obeyed nonlinear processes.

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Inhibition activities of natural products on serine proteases

Cited by 54 publications

References 9 publications

Proteinase inhibition and antioxidant activity of selected forage crops

Proteinase inhibition and antioxidant activity of selected forage crops

The effect of quercetin on cerulein-induced acute pancreatitis

LC Determination and Pharmacokinetic Study of Hyperoside in Rat Plasma after Intravenous Administration

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