The Celastraceae family comprises about 96 genera and more than 1.350 species, occurring mainly in tropical and subtropical regions of the world. The species of this family stand out as important plant sources of triterpenes, both in terms of abundance and structural diversity. Triterpenoids found in Celastraceae species display mainly lupane, ursane, oleanane, and friedelane skeletons, exhibiting a wide range of biological activities such as antiviral, antimicrobial, analgesic, anti-inflammatory, and cytotoxic against various tumor cell lines. This review aimed to document all triterpenes isolated from different botanical parts of species of the Celastraceae family covering 2001 to 2021. Furthermore, a compilation of their ¹³C-NMR data was carried out to help characterize compounds in future investigations. A total of 504 pentacyclic triterpenes were compiled and distinguished as 29 aromatic, 50 dimers, 103 friedelanes, 89 lupanes, 102 oleananes, 22 quinonemethides, 88 ursanes and 21 classified as others.

Three new triterpenes, 3,4-seco-3,11β-epoxyfriedel-4(23)-en-3β-ol (1), friedelan- 3α,11β‑diol (2), 7β,26-epoxyfriedelan-3a,7a-diol (3), a mixture of two new triterpenes 3a-hydroxyfriedelan-29-yl palmitate (4) and 3α-hydroxyfriedelan-29-yl stearate (5) and eleven known compounds were obtained from the hexane extract of Maytenus quadrangulata leaves. The structures and the relative stereochemistry of the new triterpenes were established through 1D/2D nuclear magnetic resonance (NMR), high resolution mass spectrometry (HRMS), and Fourier transform infrared (FTIR) spectral data. The hexane extract and isolated compounds were submitted to the cytotoxicity assays against leukemia (THP-1 and K562), ovarian (TOV-21G) and breast cancer (MDA-MB-231) cell lines. Compounds 1, 2 and 11β-hydroxyfriedelan-3-one (15) displayed high cytotoxicity and selectivity against leukemic cells when compared to positive control cytarabine (for THP-1) and imatinib (for K562). Furthermore, compound 2 showed similar cytotoxicity and an enhanced selectivity towards ovarian and breast cells in comparison to positive control etoposide.

Antifungal resistance is considered a global health threat. However, enzymatic inactivation of antifungals, a common mechanism seen in antibacterial resistance, has not yet been described in fungi. From a One Health perspective, this study demonstrates that Cryptococcus deuterogattii and C. neoformans, the leading agents of cryptococcosis, enzymatically inactivate fluconazole. Agrochemicals induce the overexpression of genes that code for acetyltransferases, specifically GCN5 and NAT10. These enzymes catalyze the acetylation of fluconazole into O-acetyl-fluconazole. This metabolite is unable to properly bind to 14-α-demethylase, the azole target, abolishing the antifungal activity. GCN5 and NAT10 inhibitors constrained acetylation and restored fluconazole activity, highlighting their potential as therapeutic adjuvants. The same phenotype was observed in other fungal species, suggesting broader relevance. Furthermore, O-acetyl-fluconazole was also detected in cerebrospinal fluid from cryptococcal meningitis patients undergoing fluconazole treatment. These findings reveal a previously unrecognized antifungal resistance mechanism and suggest that environmental traits shape clinically relevant resistance through conserved enzymatic pathways.

Avaliação da atividade leishmanicida do látex de Symphonia globulifera / Evaluation of the leishmanicida activity of Symphonia globulifera latex