Gastroprotective and antielastase effects of protein inhibitors from Erythrina velutina seeds in an experimental ulcer model

2017 ◽  
Vol 95 (2) ◽  
pp. 243-250 ◽  
Author(s):  
Vanessa Cristina Oliveira de Lima ◽  
Richele Janaína de Araújo Machado ◽  
Norberto Kássio Vieira Monteiro ◽  
Ibson Lucas de Lyra ◽  
Christina da Silva Camillo ◽  
...  

Trypsin and chymotrypsin inhibitors from Erythrina velutina seeds have been previously isolated by our group. In previous studies using a sepsis model, we demonstrated the antitumor and anti-inflammatory action of these compounds. This study aimed to evaluate the gastroprotective and antielastase effects of protein inhibitors from E. velutina seeds in an experimental stress-induced ulcer model. Two protein isolates from E. velutina seeds, with antitrypsin (PIAT) and antichymotrypsin (PIAQ) activities, were tested. Both protein isolates showed a high affinity and inhibitory effect against human neutrophil elastase, with 84% and 85% inhibition, respectively. Gastric ulcer was induced using ethanol (99%) in 6 groups of animals (female Wistar rats, n = 6). Before ulcer induction, these animals were treated for 5 days with one of the following: (1) PIAT (0.2 mg·kg−1), (2) PIAT (0.4 mg·kg−1), (3) PIAQ (0.035 mg·kg−1), (4) ranitidine hydrochloride (50 mg·kg−1), (5) saline solution (0.9%), or (6) no intervention (sham). Both PIAT and PIAQ protected gastric mucosa, preventing hemorrhagic lesions, edema, and mucus loss. No histologic toxic effects of PIAT or PIAQ were seen in liver and pancreatic cells. Our results show that protein isolates from E. velutina seeds have potential gastroprotective effects, placing these compounds as natural candidates for gastric ulcer prevention.

Author(s):  
Sirima Mahattanadul ◽  
Sonsawan Kongpuckdee ◽  
Ruedeekorn Wiwattanapatapee ◽  
Pimpimon Tansakul ◽  
Anupong Nitiruangjaras ◽  
...  

Background: Curcumin was found to accelerate gastric ulcer healing by a main mechanism through suppression of iNOS mediated inflammation. Although tetrahydrocurcumin (THC) is claimed as an active antioxidant principle of curcumin, its antiulcer activity has not been systematically examined. The utility of self- microemulsifying drug delivery systems (SMEDDS) for curcumin and THC formulations in liquid form was also found to increase the rate and extent of release of curcumin- and THC-SMEDDS. Nevertheless, the beneficial antiulcer efficacy of these nanoproducts has not yet been evaluated. Objective: This study aimed to evaluate and compare antiulcer efficacy of curcumin- and THC-SMEDDS through inhibition of the iNOS/NO system in rat model. Methods: Antiulcer efficacy was compared in terms of an ability to accelerate the healing of gastric ulcerincluding the inhibitory efficacy on inflammatory NO production in activated macrophages and iNOS mRNA expression at the ulcerated area. Results: THC was found to have less ulcer healing capacity than curcumin with a lack of significant inhibitory effect on the iNOS/NO system. SMEDDS used in the study significantly increased the inhibitory efficacy of THC on iNOS/NO production and iNOS mRNA expression into a comparable inhibitory potency to that of curcumin. An oral administration of curcumin- or THC-SMEDDS once a day was capable of exerting a comparable curative efficacy to a twice-daily oral administration of curcumin or THC. Conclusion: The SMEDDS used in the study could bring an enhancement of inhibitory efficacy on the iNOS/NO system of antiulcer drug, leading to a reduction of daily dosing and dosing frequency.


Planta Medica ◽  
2013 ◽  
Vol 79 (13) ◽  
Author(s):  
S Mahattanadul ◽  
S Nima ◽  
S Tewtrakul ◽  
P Tansakul

1996 ◽  
Vol 71 ◽  
pp. 202
Author(s):  
Kouichirou Wada ◽  
Yoshinori Kamisaki ◽  
Masayuki Kitano ◽  
Yosuke Kishimoto ◽  
Kentaro Nakamoto ◽  
...  

2021 ◽  
Author(s):  
Priscilla Maiselina Sriepindonnta ◽  
Fatimah Nur Fitriani ◽  
Savannah Quila Thirza ◽  
Made Dinda Pratiwi ◽  
Dwi Evan Prima Putra Noviardi ◽  
...  

2017 ◽  
Vol 12 (2) ◽  
pp. 11
Author(s):  
Zaman Hayat ◽  
Mueen Ahmad Chaudhry ◽  
. Alamgeer

<p class="Abstract">The aim of this study was to validate the traditional uses of ulcerene, a poly-herbal formulation in ethanol, aspirin and stress-induced gastric ulcer model of rat. The extent of gastric ulcer formation was studied, using ulcer score, ulcer index, percentage cure through gross examination and histopathological evaluation. A significant (p&lt;0.001) dose-dependent anti-ulcerant effect was observed in ulcerene (50 and 100 mg/kg)-treated group with highest effectiveness against ethanol-induced ulcer. The concentration-dependent spasmolytic effect was seen in spontaneously contracting, high K<sup>+</sup> (80 mM) and carbachol (1 µM)-induced jejunum contractions (10, 0.3 and 1 mg/mL), similar to dicyclomine (10, 1 and 3 µM), indicated non-specific spasmolytic mechanism behind the effect. By considering these results, ulcerene can be suggested for the treatment of peptic ulcer.</p>


2001 ◽  
Vol 53 (5) ◽  
pp. 409-411 ◽  
Author(s):  
K. Gharzouli ◽  
G.A. Balint ◽  
M. Galfi ◽  
A. Rimanoczy ◽  
A. Juhasz

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