Novel peptide inhibitor of dipeptidyl peptidase IV (Tyr-Pro-D-Ala-NH2) with anti-inflammatory activity in the mouse models of colitis

Peptides ◽  
2018 ◽  
Vol 108 ◽  
pp. 34-45 ◽  
Author(s):  
M Salaga ◽  
A Binienda ◽  
P Draczkowski ◽  
P Kosson ◽  
R Kordek ◽  
...  
Molecules ◽  
2019 ◽  
Vol 24 (14) ◽  
pp. 2614 ◽  
Author(s):  
Nadia Hisamuddin ◽  
Wan Mastura Shaik Mossadeq ◽  
Mohd Roslan Sulaiman ◽  
Faridah Abas ◽  
Sze Wei Leong ◽  
...  

Curcumin, derived from the rhizome Curcuma longa, has been scientifically proven to possess anti-inflammatory activity but is of limited clinical and veterinary use owing to its low bioavailability and poor solubility. Hence, analogs of curcuminoids with improved biological properties have been synthesized to overcome these limitations. This study aims to provide the pharmacological basis for the use of 5-(3,4-dihydroxyphenyl)-3-hydroxy-1-(2-hydroxyphenyl)penta-2,4-dien-1-one (DHHPD), a synthetic curcuminoid analog, as an anti-edematogenic and anti-granuloma agent. The carrageenan-induced paw edema and the cotton pellet-induced granuloma assays were used to assess the anti-inflammatory activity of DHHPD in mice. The effects of DHHPD on the histaminergic, serotonergic, and bradykininergic systems were determined by the histamine-, serotonin-, and bradykinin-induced paw edema tests, respectively. DHHPD (0.1, 0.3, 1, and 3 mg/kg, intraperitoneal) evoked significant reductions (p < 0.05) in carrageenan-induced paw edema at different time intervals and granuloma formation (p < 0.0001) by 22.08, 32.57, 37.20, and 49.25%, respectively. Furthermore, DHHPD significantly reduced paw edema (p < 0.05) induced by histamine, serotonin, and bradykinin. The present study suggests that DHHPD exerts anti-edematogenic activity, possibly by inhibiting the synthesis or release of autacoid mediators of inflammation through the histaminergic, serotonergic, and bradykininergic systems. The anti-granuloma effect may be attributed to the suppression of transudative, exudative, and proliferative activities associated with inflammation.


1999 ◽  
Vol 126 (8) ◽  
pp. 1751-1760 ◽  
Author(s):  
Duncan Haworth ◽  
Amanda Rees ◽  
Peter J Alcock ◽  
Linda J Wood ◽  
Anand S Dutta ◽  
...  

2015 ◽  
Vol 29 (S1) ◽  
Author(s):  
Thiago Salles ◽  
Camila Zogbi ◽  
Thais Lima ◽  
Francisco Soriano ◽  
Adriana Girardi

2019 ◽  
Vol 2019 ◽  
pp. 1-14 ◽  
Author(s):  
Akash Ahuja ◽  
Deok Jeong ◽  
Mi-Yeon Kim ◽  
Jae Youl Cho

Trichosanthes tricuspidata Lour., also known as T. palmata Roxb, T. bracteata Lam., T. puber Blume, and Modecca bracteata, is a vine belonging to the Cucurbitaceae family (English name: redball snake gourd). Distributed in China, South and East Asia, and tropical Australia, it has been traditionally used as a medicinal plant for its antifever, laxative, anthelmintic properties and for migraine treatment. In this paper, we examined the effects of Trichosanthes tricuspidata Lour. ethanol extract (Tt-ME) in vitro and in vivo. To confirm the effects of Tt-ME on inflammatory responses, we conducted experimental analyses including level of nitric oxide (NO) production, RT-PCR, and immunoblotting and using a HCl/EtOH-induced gastritis animal model. Tt-ME attenuated the release of NO and decreased mRNA levels of inducible NO synthase (iNOS), TNF-α, and IL-6 in lipopolysaccharide- (LPS-) induced macrophages in a concentration-dependent manner. Tt-ME time-dependently suppressed nuclear translocation of nuclear factor kappa B (NF-κB) subunits p50 and p65, activator protein (AP-1) subunits c-Fos and c-Jun, and STAT3 transcriptional activity by inhibiting nuclear translocation of p50, p65, c-Fos, c-Jun, and STAT3. Tt-ME significantly downregulated NF-κB, MAPK, and JAK2 signaling by targeting Syk, Src, and IRAK1 protein kinases. Furthermore, matrix metalloproteinase-9 (MMP-9) expression and cell migration were observed to be downregulated by Tt-ME in LPS-activated macrophages. In vivo studies on Tt-ME also produced similar trends in Hcl/EtOH-induced gastritis mouse models by inhibiting proinflammatory cytokines and the inflammatory signaling pathway. Our results strongly suggest that Tt-ME exerted anti-inflammatory activity in LPS-stimulated macrophages and mouse models of acute inflammatory disease.


Planta Medica ◽  
2008 ◽  
Vol 74 (09) ◽  
Author(s):  
DA Uchil ◽  
SK Kamat ◽  
SS Menon ◽  
AM Scindia ◽  
GK Dang ◽  
...  

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