Rational design of biodegradable sulphonamide candidates treating septicaemia by synergistic dual inhibition of COX-2/PGE2 axis and DHPS enzyme

El-Dershaby, Nada H; El-Hawash, Soad A.M.; Kassab, Shaymaa E.; Dabees, Hoda G; Moneim, Ahmed E. Abdel; Wahab, Ibrahim A Abdel; Abd‐Αlhaseeb, Mohammad M.; El-Miligy, Mostafa M.M.

doi:10.1080/14756366.2022.2086868

Cited by 6 publications

(3 citation statements)

References 73 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…In addition, indomethacin and diclofenac sodium were used as standard nonselective human COX inhibitors. The enzymatic assay was carried out according to a procedure in the literature [ 22 , 23 ] utilizing an ovine COX-1/human recombinant COX-2 assay kit (catalog no. 560131; Cayman Chemicals Inc., Ann Arbor, MI, USA).…”

Section: Resultsmentioning

confidence: 99%

See 1 more Smart Citation

Rational Design and Synthesis of New Selective COX-2 Inhibitors with In Vivo PGE2-Lowering Activity by Tethering Benzenesulfonamide and 1,2,3-Triazole Pharmacophores to Some NSAIDs

et al. 2022

View full text Add to dashboard Cite

New selective COX-2 inhibitors were designed and synthesized by tethering 1,2,3-triazole and benzenesulfonamide pharmacophores to some NSAIDs. Compounds 6b and 6j showed higher in vitro COX-2 selectivity and inhibitory activity (IC50 = 0.04 µM and S.I. = 329 and 312, respectively) than celecoxib (IC50 = 0.05 µM and S.I. = 294). Compound 6e revealed equipotent in vitro COX-2 inhibitory activity to celecoxib. Furthermore, 6b and 6j expressed more potent relief of carrageenan-induced paw edema thickness in mice than celecoxib, with ED50 values of 11.74 µmol/kg and 13.38 µmol/kg vs. 16.24 µmol/kg, respectively. Compounds 6b and 6j inhibited the production of PGE2 with a % inhibition of PGE2 production of 90.70% and 86.34%, respectively, exceeding celecoxib’s percentage (78.62%). Moreover, 6b and 6j demonstrated a gastric safety profile comparable to celecoxib. In conclusion, compounds 6b and 6j better achieved the target goal as more potent and selective COX-2 inhibitors than celecoxib in vitro and in vivo.

show abstract

Section: Resultsmentioning

confidence: 99%

“…In vitro human COX-1 and human COX-2 enzymatic inhibitory activity of the tested compounds as well as the reference drugs was carried out according to the previously mentioned procedures [ 22 , 23 ]; for details, see Page S15, Supplementary File .…”

Section: Methodsmentioning

confidence: 99%

Rational Design and Synthesis of New Selective COX-2 Inhibitors with In Vivo PGE2-Lowering Activity by Tethering Benzenesulfonamide and 1,2,3-Triazole Pharmacophores to Some NSAIDs

et al. 2022

View full text Add to dashboard Cite

show abstract

“…Several studies using rodent models show that some algal derived components like carrageenan can induce intestinal inflammation, and to significantly alter gastrointestinal tract microbiota composition (Benard et al 2010;Chassaing et al 2017). Some algal based constituents like carrageenan are widely used to induce the innate immune response in animal models of inflammation, and points to the possibility of immune modifying properties for some algal species or constituents (Wei et al 2016;El-Dershaby et al 2022;Yi et al 2022). Indeed, several studies have reported inflammatory responses of human colonic epithelial cells to carrageenan (Borthakur et al 2007;Bhattacharyya et al 2008;Choi et al 2012).…”

Section: Discussionmentioning

confidence: 99%

Edible algae allergenicity – a short report

2022

View full text Add to dashboard Cite

The use of seaweed and algal derived products in the food industry has grown rapidly in recent times. Major areas of expansion have been in Western countries where algae derived commodities are being utilised as edible foods or sources of high value ingredients. However, studies focused on potential allergenicity attributed to these food items, prevalence of allergenicity, and public health awareness are limited. Therefore, the current research summarises the existing literature focused on algal induced allergy in humans. Of the available literature, a total of 937 titles were identified, and 33 articles underwent subsequent full-text screening. Most research focused on prevalence and were derived from studies conducted in Europe (58%), North America and Canada (33%), and the remainder Australia and South Korea (9%). No studies addressed the need for public education or labelling of algal products. Our review reports that the available evidence identified points to algal derived products as being potential sources of allergens in the human food chain. Several components have been characterised that are shown to induce allergic responses in humans. Few studies have assessed the prevalence of algal allergenicity in the general population and as such further research is warranted given the increased usage of these products in the food industry.

show abstract

Thymoquinone counteracts oxidative and inflammatory machinery in carrageenan-induced murine paw edema model

Hijazy

Dahran

Althagafi

et al. 2022

Environ Sci Pollut Res

View full text Add to dashboard Cite

Thymoquinone (TQ) is an active constituent in Nigella sativa, and is extensively reported for its distinguished antioxidant, and anti-in ammatory bioactivities. Despite the local protective response of the acute in ammation, it contributes to the development of various disease conditions such as cell death, organ damage, or genesis of tumors. Hence, in this study, the effects of orally administered TQ (50 and 100 mg/kg) for 14 days against edema development, oxidative stress, and in ammation were investigated in paw edema induced by carrageenan in mice. Indomethacin (10 mg/kg) was used as a reference drug. The results revealed that TQ reduced the paw edema volume in a time-dependent manner, attenuated acetic acid-provoked writhing movements, and reduced xylene-triggered ear edema.Hematological ndings revealed marked normalization of altered counts of WBCs, and platelets. Furthermore, paw tissue levels of MDA and NO showed marked decreases together with increases Nrf2, GSH, SOD, CAT, GPx, and GR after TQ administration. Additionally, TQ decreased the levels of proin ammatory mediators, such as IL-1b, TNF-α, IL-6, MCP-1, CRP, MPO, and NF-κB in the in amed paw tissue. Moreover, appreciable decreases were recorded in COX-2 and its product (PGE-2) as well as the immune reaction of TNF-α in TQ-treated mice. Histopathological ndings further validated the potential antioedematous, anti-in ammatory power of TQ in in amed tissues. Conclusively, the obtained ndings encourage the potent application of TQ to subside the acute in ammatory events because of its striking antioxidant and anti-in ammatory properties in the in amed paw tissue.

show abstract

Rational design of biodegradable sulphonamide candidates treating septicaemia by synergistic dual inhibition of COX-2/PGE2 axis and DHPS enzyme

Cited by 6 publications

References 73 publications

Rational Design and Synthesis of New Selective COX-2 Inhibitors with In Vivo PGE2-Lowering Activity by Tethering Benzenesulfonamide and 1,2,3-Triazole Pharmacophores to Some NSAIDs

Rational Design and Synthesis of New Selective COX-2 Inhibitors with In Vivo PGE2-Lowering Activity by Tethering Benzenesulfonamide and 1,2,3-Triazole Pharmacophores to Some NSAIDs

Edible algae allergenicity – a short report

Thymoquinone counteracts oxidative and inflammatory machinery in carrageenan-induced murine paw edema model

Contact Info

Product

Resources

About