Introduction Plants have been considered a promising source for discovering new compounds with pharmacological activities. The Fabaceae family comprises a large variety of species that produce substances with diverse therapeutic potential, including anti‐inflammatory activity. The limitations of current anti‐inflammatories generate the need to research new anti‐inflammatory structures with higher efficacy as well as develop methods for screening multiple samples, reliably and ethically, to assess such therapeutic properties. Objective Validate and apply a quantification method for prostaglandin E2 (PGE2) production from an ex vivo assay in human blood in order to screen anti‐inflammatory activity present in many Fabaceae species extracts. Methods Human blood was incubated with extracts from 47 Fabaceae species. After lipopolysaccharide (LPS)‐induced inflammation, PGE2 was quantified in the plasma by liquid chromatography with tandem mass spectrometry (LC–MS/MS). The extracts that presented PGE2 production inhibition were further assessed through in vivo assay and then chemically characterised through an analysis of ultra‐performance liquid chromatography electrospray ionisation quadrupole time‐of‐flight tandem mass spectrometry (UPLC‐ESI‐QTOF‐MS2) data. Results The new ex vivo anti‐inflammatory assay showed that five out of the 47 Fabaceae species inhibited PGE2 production. Results from an in vivo assay and the metabolic profile of the active extracts supported the anti‐inflammatory potential of four species. Conclusion The quantification method for PGE2 demonstrated fast, sensitive, precise, and accurate results. The new ex vivo anti‐inflammatory assay comprised a great, reliable, and ethical approach for the screening of a large number of samples before an in vivo bioassay. Additionally, the four active extracts in both ex vivo and in vivo assays may be useful for the development of more efficient anti‐inflammatory drugs.
There is some evidence in the literature of the photocyclization reaction of Tagitinin C (1) to Tagitinin F (2). Compound 2 has high pharmacological potential, but it is not easy to obtain, while compound 1 is easily obtained from a widespread plant, Tithonia diversifolia. Among different reaction conditions monitored, one was found that allowed the cyclization of 1 into 2 in <15 min in a photo‐dependent reaction. Scaling‐up the photocyclization of the pure compound 1 into 2 demonstrated 100% yield, and the isolation of 2 from a UV‐irradiated extract was eight‐fold higher than the quantity isolated from the non‐UV‐irradiated extract. We were also able to better understand the process of photoconversion and determine methods to isolate and quantify these compounds, which are known for their important antitumoral activities among other important pharmacological properties.
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