Berberine-fluconazole microparticle-based combination therapy to treat candidiasis infections.

AIM: This study aims to incorporate alginate microparticles containing berberine and fluconazole into two different types of pharmaceutical formulations, to subsequently evaluate the antifungal activity against Candida albicans. METHODS AND RESULTS: Alginate microparticles containing BBR (berberine) and FLU (fluconazole) were produced by the spray-drying technique, characterized and incorporated in two pharmaceutical formulations, a vaginal cream and artificial saliva. Broth microdilution, checkerboard, time-kill curve, and scanning electron microscopy were carried out to determine the antifungal effects of BBR and FLU against C. albicans. The minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC) values of free BBR were 125 µg ml-1. Synergism between BBR and FLU was demonstrated by a fractional inhibitory concentration index (FICI) = 0.0762. The time-kill curve for the combination BBR + FLU showed a more pronounced decrease in fungal growth in comparison to free drugs, and an antibiofilm effect of BBR occurred in the formation and preformed biofilm. CONCLUSION: Alginate microparticles containing BBR and FLU were obtained and incorporated in a vaginal cream and artificial saliva. Both formulations showed good stability, antifungal effects, and organoleptic characteristics, which suggest that BBR-FLU microparticles in formulations have potential as antifungal therapy.

Study of chemical constituents, antioxidants and antimicrobial activities of Tamarindus indica L. seed.

The fruits of Tamarindus indica L. are consumed worldwide, with various parts of the plant being used for medicinal purposes. The residues (pericarp and seeds) generated during cellulose processing are of significant value as they contain bioactive compounds with diverse biological activities. The objective of this study was to evaluate the chemical constituents of the ethyl acetate fraction as possible substitutes for synthetic compounds with biological properties using ultra-high performance liquid chromatography coupled to high-resolution mass spectrometry (UHPLC-HRMS/MS) analysis and the evaluation of the antioxidant activity (ferric reducing antioxidant power [FRAP], 2,2'-azino-bis-3-ethylbenzthiazoline-6-sulphonic acid [ABTS], and 1-diphenyl-2-picrylhydrazyl [DPPH]), total phenolic compounds (TPC), and antimicrobial activity of the hydroalcoholic extract and tamarind seed fractions were also performed. The chemical investigation of the acetate fraction using UHPLC-HRMS/MS resulted in the putative identification of 14 compounds, including flavonoids, (+)-catechin/(-)-epicatechin, procyanidin B2, procyanidin C2, isoquercetin, quercetin, luteolin, rutin, taxifolin, eriodictyol, kaempferide, hydroxybenzoic acid, protocathecuic acid, and protocathecuic acid methyl and ethyl esters derivatives. The crude hydroalcoholic extract exhibited the best results in terms of TPC: 883.87 gallic acid equivalent (GAE; mg/g) and antioxidant activity: FRAP: 183.29 GAE (mg/g), ABTS: 39.67%, and DPPH: 91.08%. The extract exhibited excellent antibacterial activity against gram-positive bacteria, specifically Staphylococcus aureus minimum inhibitory concentration (MIC)/minimum bactericidal concentration (MBC; 62.5/125 g/mL) and Bacillus cereus MIC/MBC (125/250 g/mL), and gram-negative bacteria, specifically Aeromonas hydrophila MIC/MBC (125/250 µg/mL) and Pseudomonas aeruginosa MIC/MBC (250/500 g/mL). Morphological damage to cells was observed using flow cytometry and scanning electron microscopy. Tamarind seeds contain unique bioactive compounds that should be explored for their use as novel food preservatives. PRACTICAL APPLICATION: Original data were obtained regarding the Tamarindus indica L. seed extract and the ethyl acetate and hexane fractions. This research aimed to investigate the potential of these for food preservation and as alternatives to additives and synthetic compounds added to cattle feed. This paper reports novel findings regarding the chemical composition of the extract and its antioxidant activity, along with its antimicrobial activity against bacteria (gram-positive: Staphylococcus aureus, Bacillus cereus, and gram-negative: Salmonella enterica serovar Enteritidis, Escherichia coli, Pseudomonas aeruginosa, and Aeromonas hydrophila) and yeasts (Candida albicans and Saccharomyces cerevisiae).

The chemistry of Vernonanthura nudiflora (Less.) H. Rob. flowers and its antimicrobial activities.

Twenty-one known specialised metabolites were isolated from the flowers of Vernonanthura nudiflora (Less.) H. Rob., the structures of the compounds were established based on 1 D and 2 D NMR spectroscopic experiments. Others 28 compounds were putatively identified using the dereplication technique by UHPLC-HRMS/MS. Twenty-three of the compounds are being reported for the first time in this species. The mixture of sesquiterpene lactones piptocarphins A and B (17 + 18), and the flavone velutin (14) were tested against several microorganisms and showed promising activity against Mycobacterium tuberculosis with MIC of 15.6 µg/mL and 31.2 µg/mL, respectively. Furthermore, 17 + 18 showed greater cytotoxicity against VERO cells (IC50 = 7.0 ± 1.73) compared to compound 14 (IC50 85.0 ± 10.6 µg/mL). These findings reveal the feasibility of using the UHPLC-ESI-HRMS/MS-based dereplication strategy in complex fractions to identify specialised metabolites, moreover to V. nudiflora flowers being a source of compounds with antimycobacterial potential.

Chemical Characterization and Phytotoxic Effects of the Aerial Parts of Ruzigrass (Urochloa ruziziensis).

Studies of the phytotoxic effects between plants can be a crucial tool in the discovery of innovative compounds with herbicide potential. In this sense, we can highlight ruzigrass (Urochloa ruziziensis), which is traditionally used in the crop rotation system in order to reduce weed emergence. The aim of this work was to characterize the secondary metabolites of ruzigrass and to evaluate its phytotoxic effects. In total, eight compounds were isolated: friedelin, oleanolic acid, α-amyrin, 1-dehydrodiosgenone, sitosterol and stigmasterol glycosides, tricin and p-coumaric acid. Phytotoxic effects of the crude methanolic extract and fractions of ruzigrass were assessed using germination rate, initial seedling growth, and biomass of Bidens pilosa, Euphorbia heterophylla and Ipomoea grandifolia. Chemometric analysis discriminated the weed species into three groups, and B. pilosa was the most affected by fractions of ruzigrass. The phytotoxic activities of 1-dehydrodiosgenone, tricin, and p-coumaric acid are also reported, and p-coumaric acid and 1-dehydrodiosgenone were active against B. pilosa.

Curvulin and spirostaphylotrichins R and U from extracts produced by two endophytic Bipolaris sp. associated to aquatic macrophytes with antileishmanial activity.

In the present study, biological activity and chemical composition of two crude extracts of endophytic fungal strains of Bipolaris genera isolated from two species of aquatic macrophytes: Eichhornia azurea (Kunth) and Eichhornia crassipes (Mart.) were investigated. The nuclear magnetic resonance and mass spectrometry data provided the identification of three main compounds: curvulin (1), spirostaphylotrichin R (2) and U (3). The fragmentation mechanism of the precursor ions towards collision induced dissociation (CID) tandem mass spectrometry experiment (MS/MS) is also proposed. Furthermore, biological screening of the crude extracts displayed antileishmanial activity with IC50 values ranging from 70-84.2 µg.mL-1.