Metabolomics approaches have become fundamental strategies for the analysis of complex mixtures, guiding the isolation of target compounds by focusing on unpublished or promising pharmacological properties. The discovery of novel anti-inflammatory agents is important due to several limitations regarding their potency, efficacy, and adverse effects. Thus, novel anti-inflammatory candidates are essential, aiming to find agents with better mechanisms of action. In this context, extracts from Poincianella pluviosa var. peltophoroides demonstrated significant in vivo anti-inflammatory potential. Thus, metabolomics analysis based on UHPLC-UV-HRFTMS data was performed for the identification of biomarkers with anti-inflammatory properties. Metabolomics-guided chromatographic process led to the isolation of novel compounds 4‴-methoxycaesalpinioflavone and 7-methoxycaesalpinioflavone, as well as known derivatives rhuschalcone VI and caesalpinioflavone. Isolated compounds caused edema inhibition and neutrophil recruitment. Two of them showed better efficacy than reference drugs (indomethacin and dexamethasone). Results of in vivo experiments corroborated those obtained through metabolomics and statistical analyses guiding the isolation of substances of interest.
A series of novel benzophenone derivatives containing a thiazole heterocyclic nucleus were designed by molecular hybridization. Molecular docking studies have demonstrated the inhibitory potential of the designed compounds against cyclooxygenase (COX) isoenzymes. These compounds were synthesized, characterized, and evaluated for their anti-inflammatory properties by the croton oil-induced ear edema assay to examine their effect on both prostaglandin (PG) production and neutrophils recruitment. The thiazole derivatives displayed a potent effect in terms of reducing ear edema. The analysis suggested that the presence of 4-phenyl-2-hydrazinothiazole and the absence of C4′-OCH3 on the benzophenone derivative structure are strongly related to the inhibition of PG production. In addition, the derivatives 2e, 3a and 3c concomitantly inhibit PG production and neutrophil recruitment, which may be a mechanism of action better than of common NSAIDs due to their inability to inhibit the neutrophil recruitment. Thus, these compounds can be considered as potential lead compounds toward the development of new anti-inflammatory drugs with an innovating mechanism of action.
Chagas Disease (CD), caused by flagellate protozoan Trypanosoma cruzi, is a Neglected Tropical Diseases (NTD) that affect approximately seven million people worldwide with a restrict therapeutical arsenal. In the present study, the essential oils from 18 Myrtaceae species were extracted, chemically dereplicated, and evaluated in vitro against T. cruzi. From these, eight essential oils were considered promising (IC50<10 μg/mL and SI>10) against the protozoan: Eugenia florida, E. acutata, E. widgrenii, Calyptranthes brasilienses, C. widgreniana, Plinia cauliflora, Campomanesia xanthocarpa, and Psidium guajava. Multivariate data analysis pointed out (E)‐caryophyllene, α‐humulene, limonene, caryophyllene oxide, and α‐copaene playing an important role in the anti‐T. cruzi activity. The obtained results demonstrated the potential of essential oils of Myrtaceae species as valuable sources of bioactive compounds against T. cruzi.
Background:
Sclerotinia sclerotiorum is a phytopathogenic fungus from Sclerotinaceae’s family. This fungus parasitizes approximately 400 species of plants of great economic importance, such as soybean and beans. In this study, the anti-inflammatory properties of extracts, fractions, and isolated compound ergosterol peroxide were investigated. The hexane fraction and 1 inhibited croton-oil-induced ear edema. In addition, ergosterol peroxide also inhibited neutrophil recruitment in myeloperoxidase assay, demonstrating that ergosterol peroxide has anti-inflammatory activity inhibiting both COX and LOX pathway activity. Moreover, these results provide new knowledge regarding S. sclerotiorum as a source of extracts and bioactive compounds.
Objective::
The present study aims to investigate the phytochemical profile of Sclerotinia sclerotiorum and its in vivo anti-inflammatory activity.
Method:
The crude extract, fractions, and ergosterol peroxide of Sclerotinia sclerotiorum were evaluated by croton oil-induced ear edema quantification of MPO (myeloperoxidase enzyme).
Results:
The crude extract and hexane fraction exhibited edema inhibition of 50.5 and 70.6%, respectively. The ergosterol peroxide isolated from the hexane bioactive fractions, exhibited significant inhibition of ear edema, indicating inhibition of the COX pathway. In addition, ergosterol peroxide inhibited neutrophil recruitment.
Conclusion:
The extract and fractions exhibited anti-inflammatory potential. The isolated compound exhibited anti-inflammatory potential.
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