Pristimerin isolated from Salacia crassifolia (Mart. Ex. Schult.) G. Don. (Celastraceae) roots as a potential antibacterial agent against Staphylococcus aureus.

ETHNOPHARMACOLOGICAL RELEVANCE: Pristimerin is a triterpenoid considered the main component of Salacia crassifolia extracts. This terpene has shown promising antitumor, anti-inflammatory, and antimicrobial effects. Likewise, S. crassifolia has been used in traditional medicine to treat cancer and as an antimicrobial and anti-inflammatory agent. AIM OF THE STUDY: This study aimed to evaluate the antibacterial activity of the hexane extract of Salacia crassifolia roots (HER) and its isolate, pristimerin, against pathogenic bacteria. MATERIALS AND METHODS: First, we evaluated the spectrum of action of HER and pristimerin by the determination of the minimum inhibitory concentration (MIC) and the minimal bactericidal concentration (MBC). Subsequently, we analyzed the time-kill curve of these plant-derived compounds against Staphylococcus aureus. Then, we examined their mode of action by three different assays: the crystal violet methodology, the release of intracellular material, and transmission electron microscopy methods (TEM). Finally, we evaluated the effect of HER and pristimerin on the pre-formed biofilm of S. aureus by the crystal violet assay, the synergistic effect by the checkerboard method, the cytotoxicity against Vero cells, and the in silico activity using the online software PASS. RESULTS: HER and pristimerin presented a narrow spectrum of action against Gram-positive bacteria (MIC 0.195-25 µg/mL), and their primary mode of action is the alteration of membrane permeability of S. aureus. Our results show that the compounds disrupted the pre-formed biofilm of S. aureus in a dose-dependent manner. Furthermore, HER and pristimerin presented a significant synergic effect after the combination with well-known antibiotics, which was associated with the ability of these phytomedicines to change membrane permeability. Regarding the cytotoxic effect, the selective index (SI) of HER ranged from 0.37 to 11.86, and the SI of pristimerin varied from 0.24 to 30.87, according to the bacteria tested. CONCLUSIONS: Overall, HER and pristimerin showed a promising antibacterial effect in vitro through the alteration of membrane permeability of S. aureus.

Divergent cytokine response following maximum progressive swimming in hot water.

Exercise promotes transitory alterations in cytokine secretion, and these changes are affected by exercise duration and intensity. Considering that exercise responses also are affected by environmental factors, the goal of the present study was to investigate the effect of water temperature on the cytokine response to maximum swimming. Swiss mice performed a maximum progressive swimming exercise at 31 or 38°C, and plasma cytokine levels were evaluated immediately or 1, 6 or 24 h after exercise. The cytokine profile after swimming at 31°C was characterized by increased interleukin (IL)-6 and monocyte chemotactic protein-1 (MCP-1) levels, which peaked 1 h after exercise, suggesting an adequate inflammatory milieu to induce muscle regeneration. Transitory reductions in IL-10 and IL-12 levels also were observed after swimming at 31°C. The cytokine response to swimming was modified when the water temperature was increased to 38°C. Although exercise at 38°C also led to IL-6 secretion, the peak in IL-6 production occurred 6 h after exercise, and IL-6 levels were significantly lower than those observed after maximum swimming at 31°C (p = 0·030). Furthermore, MCP-1 levels were lower and tumour necrosis factor-α levels were higher immediately after swimming at 38°C, suggesting a dysregulated pro-inflammatory milieu. These alterations in the cytokine profile can be attributed in part to reduced exercise total work because exhaustion occurred sooner in mice swimming at 38°C than in those swimming at 31°C.