Chemical composition and antimicrobial activity of Cordiera myrciifolia leaves against pathogenic bacteria and fungi: Drug potentiation ability and inhibition of virulence.

Cordiera myrciifolia is an abundant species in Northeast Brazil that presents metabolites of biological/therapeutic interest. From this perspective, the present study aimed to investigate the chemical constituents and evaluate the in vitro antimicrobial activity of hexane (HECM) and ethanolic (EECM) extracts of C. myrciifolia leaves. The extracts were analyzed by chromatographic techniques (GC and UPLC) coupled with mass spectrometry. The antimicrobial activity of the extracts and the extracts combined with conventional drugs was evaluated by microdilution. The in vitro effect of the treatments on Candida's morphological transition was verified through cultivation in humid chambers. In HECM, 11 constituents including fatty acids, and triterpenes, including phytosterols, alkanes, tocols, and primary alcohols were identified. Triterpenes represented >40% of the identified constituents, with Lupeol being the most representative. In EECM, 13 constituents were identified, of which eight belonged to the class of flavonoids. High antibacterial activity of HECM was detected against Escherichia coli and Staphylococcus aureus, with Minimum Inhibitory Concentrations of 8 and 16 µg/mL, respectively. The combined activity was more effective when combined with Norfloxacin and Imipenem. In anti-Candida activity, the IC50 of the extracts ranged from 36.6 to 129.1 µg/mL. There was potentiating effect when associated with Fluconazole. Both extracts inhibited the filamentous growth of C. tropicalis at a concentration of 512 µg/mL. C. myrciifolia extracts prove to be candidates for the development of new therapeutic formulations to treat bacterial and fungal infections.

Chemical composition, antifungal, and anti-virulence action of the stem bark of Hancornia speciosa Gomes (Apocynaceae) against Candida spp.

ETHNOPHARMACOLOGICAL RELEVANCE: Hancornia speciosa Gomes is a fruit and medicinal species used for treating infectious diseases of the genitourinary system. However, its mechanism of action against microbes is still not fully understood. Infections in the genitourinary system caused by Candida spp. are associated with its fungal resistance and pathogenicity. New plant-derived compounds are an alternative to fight these Candida infections. AIM OF THE STUDY: The objective of this study was to evaluate the anti-Candida effects of extracts of the stem bark of H. speciosa. This research investigated the chemical composition of sulfuric ether (EEHS) and methanolic (MEHS) extracts, their drug-modifying action on fluconazole, and their anti-virulence action on the morphological transition of Candida species. MATERIALS AND METHODS: The extracts (EEHS and MEHS) of the stem bark of H. speciosa were chemically characterized via qualitative phytochemical screening and by liquid chromatography coupled with mass spectrometry (UPLC-MS-ESI-QTOF). The extracts were evaluated regarding their antifungal effects and fluconazole-modifying activity against Candida albicans, Candida krusei, and Candida tropicalis using the broth microdilution method. Additionally, the study evaluated the inhibition of fungal virulence in Candida species through morphological transition assays. RESULTS: The phytochemical screening revealed the presence of anthocyanidins, anthocyanins, aurones, catechins, chalcones, flavones, flavonols, flavanones, leucoanthocyanidins, tannins (condensed and pyrogallic), and xanthones in both extracts of the stem bark of H. speciosa. The UPLC-MS-ESI-QTOF analysis identified the same compounds in both extracts, predominating phenolic compounds. Some compounds were first time recorded in this species: gluconic acid, cinchonain IIb, cinchonain Ib isomer, and lariciresinol hexoside isomers. Most of the intrinsic antifungal activity was observed for the MEHS against C. krusei (IC50: 58.41 µg/mL). At subinhibitory concentrations (MC/8), the EEHS enhanced the action of fluconazole against all Candida strains. The MEHS exhibited greater efficacy than fluconazole inhibiting C. krusei growth. The EEHS completely inhibited hyphae appearance and reduced pseudohyphae formation in C. albicans. CONCLUSION: The stem bark of H. speciosa is a rich source of bioactive compounds, especially phenolic. Phenolic compounds can have important roles in fighting infectious diseases of the genitourinary system, such as candidiasis. The extracts of H. speciosa improved the action of the drug fluconazole against Candida species, inhibited hyphae appearance, and reduced pseudohyphae formation. The results of this study can support the development of new therapeutics against resistant strains of Candida.

Corrigendum to "Evaluation of freeze-dried phenolic extract from cashew apple by-product: Physical properties, in vitro gastric digestion and chemometric analysis of the powders" [Food Chemistry: Molecular Sciences 5 (2022) 100149].

[This corrects the article DOI: 10.1016/j.fochms.2022.100149.].

Metabolism Characterization and Chemical and Plasma Stability of Casearin B and Caseargrewiin F.

Oral preparations of Casearia sylvestris (guacatonga) are used as antacid, analgesic, anti-inflammatory, and antiulcerogenic medicines. The clerodane diterpenes casearin B and caseargrewiin F are major active compounds in vitro and in vivo. The oral bioavailability and metabolism of casearin B and caseargrewiin F were not previously investigated. We aimed to assess the stability of casearin B and caseargrewiin F in physiological conditions and their metabolism in human liver microsomes. The compounds were identified by UHPLC-QTOF-MS/MS and quantified by validated LC-MS methods. The stability of casearin B and caseargrewiin F in physiological conditions was assessed in vitro. Both diterpenes showed a fast degradation (p < 0.05) in simulated gastric fluid. Their metabolism was not mediated by cytochrome P-450 enzymes, but the depletion was inhibited by the esterase inhibitor NaF. Both diterpenes and their dialdehydes showed a octanol/water partition coefficient in the range of 3.6 to 4.0, suggesting high permeability. Metabolism kinetic data were fitted to the Michaelis-Menten profile with KM values of 61.4 and 66.4 µM and Vmax values of 327 and 648 nmol/min/mg of protein for casearin B and caseargrewiin F, respectively. Metabolism parameters in human liver microsomes were extrapolated to predict human hepatic clearance, and suggest that caseargrewiin F and casearin B have a high hepatic extraction ratio. In conclusion, our data suggest that caseargrewiin F and casearin B present low oral bioavailability due to extensive gastric degradation and high hepatic extraction.

UPLC-QTOF-MS/MS-based metabolomic approach and gastroprotective effect of two chemotypes of Egletes viscosa (L.) less. against ethanol-induced gastric ulcer in mice.

ETHNOPHARMACOLOGICAL RELEVANCE: Egletes viscosa (L.) (macela) is a native wild herb that can be found in different states of northeastern Brazil. The infusions of its flower buds are traditionally used for the treatment of gastrointestinal disorders. E. viscosa possesses two chemotypes (named A and B), distinguishable by the composition of the essential oil from the flower buds. Although there are previous studies of the gastroprotective effect of the isolated constituents of E. viscosa, its infusions have not been investigated yet. AIM OF THE STUDY: The present study aimed to evaluate and compare the chemical composition and the gastroprotective effect of flower bud infusions of E. viscosa from chemotype A (EVCA) and chemotype B (EVCB). MATERIALS AND METHODS: Sixteen infusions were brewed with flower buds according to the traditional preparation mode and were analyzed through a UPLC-QTOF-MS/MS based metabolomic approach for determination of their metabolic fingerprints and quantification of bioactive compounds. Afterward, these data were analyzed by chemometric methods (OPLS-DA) for discrimination of the two chemotypes. Additionally, infusions of EVCA and EVCB (50, 100 and 200 mg/kg, p.o.) were evaluated on gastric ulcers induced by absolute ethanol (96%, 0.2 mL, p.o.) in mice. To elucidate the gastroprotective mechanisms, the effect of EVCA and EVCB on gastric acid secretion and gastric wall mucus was determined and the role of TRPV1 channels, prostaglandins, nitric oxide and KATP channels were assessed. Moreover, the oxidative stress-related parameters and the histological aspects of the stomach tissue were analyzed. RESULTS: The chemotypes can be discriminated from each other using UPLC-QTOF-MS/MS chemical fingerprints. Both chemotypes presented similar chemical compositions, consisting basically of caffeic acid derivatives, flavonoids and diterpenes. The quantification of bioactive compounds demonstrated that chemotype A possesses more ternatin, tanabalin and centipedic than chemotype B. EVCA and EVCB (50, 100 and 200 mg/kg, p.o.) significantly decreased the severity of ethanol-induced gastric lesions, as shown by a reduction in histological alterations and leucocyte infiltration in gastric tissue. The gastroprotective mechanism of both infusions involves an antioxidant effect, maintenance of gastric mucus and reduction gastric secretion. Stimulation of endogenous prostaglandins and nitric oxide release, activation of TRPV1 channels, and KATP channels are also involved in the gastroprotection of the infusions. CONCLUSION: The gastroprotective effect of EVCA and EVCB was equivalent and mediated through antioxidant and antisecretory actions, including the activation of TRPV1 receptors, stimulation of endogenous prostaglandins and nitric oxide, and opening of KATP channels. The presence of caffeic acid derivatives, flavonoids and diterpenes in both infusions is involved in mediating this protective effect. Our findings support the traditional use of infusions of E. viscosa for gastric disorders regardless of the chemotype.

Endophytic Fungus of Achyrocline satureioides: Molecular Identification, Chemical Characterization, and Cytotoxic Evaluation of its Metabolites in Human Melanoma cell line.

Endophytic fungi are important sources of anticancer compounds. An endophytic fungus was isolated from the medicinal plant Achyrocline satureioides, and molecularly identified as Biscogniauxia sp. (family Xylariaceae) based on partial nucleotide sequences of the internal transcribed spacer genomic region (GenBank Accession No. ON257911). The chemical characterization and cytotoxic properties of secondary metabolites produced by Biscogniauxia sp. were evaluated in a human melanoma cell line (A375). The fungus was grown in potato-dextrose liquid medium for 25 days, and the extracted compounds were subjected to solid-phase fractionation to obtain the purified FDCM fraction, for which the metabolites were elucidated via ultra-performance chromatography coupled to a mass spectrometer. In the present study, 17 secondary metabolites of Biscogniauxia sp., including nine polyketide derivatives, five terpenoids, and three isocoumarins, were putatively identified. This is the first study to report of the ability of Biscogniauxia sp. in the production of isocoumarin orthosporin; the terpenoids nigriterpene A and 10-xylariterpenoid; the polyketide derivatives daldinin C, 7'dechloro-5'-hydroxygriseofulvin, daldinone D, Sch-642305, curtachalasin A, cytochalasin E, epoxycytochalasins Z8, Z8 isomer, and Z17. Furthermore, this study has reported the biosynthesis of Sch-642305 by a Xylariaceae fungus for the first time. FDCM significantly reduced the viability and proliferation of human melanoma cells at half-maximal inhibitory concentrations ​​of 10.34 and 6.89 µg/mL, respectively, and induced late apoptosis/necrosis and cell cycle arrest in G2/M phase after 72 h of treatment. Given its ability to produce unique metabolites with promising cytotoxic effects, Biscogniauxia sp. of A. satureioides may be a reservoir of compounds with important therapeutic applications.

LC-MS Analysis and Antifungal Activity of Turnera subulata Sm.

Fungi of the Candida genus are responsible for invasive candidiasis, which affects people all over the world and has high mortality rates. This is due to their virulence factors, which give them great resistance and pathogenicity. In addition, the emergence of multidrug-resistant strains makes it difficult to treat these infections. In this way, natural products have emerged as an alternative to standard drugs, where plants known for their medicinal properties such as Turnera subulata become attractive to research. The present work aimed to analyze the ethanol extract of Turnera subulata leaves against standard strains of Candida albicans, Candida krusei and Candida tropicalis using broth microdilution techniques. The identification of the compounds in T. subulata leaves by LC-MS revealed the presence of a wide variety of substances such as carboxylic acids and terpenes, with flavonoids and fatty acids being more evident. The antifungal assays showed that the extract was not able to inhibit the growth of the tested strains at concentrations with a clinical relevance. However, at higher concentrations, it was able to inhibit the fungal dimorphism of C. albicans and C. tropicalis. It is possible that the T. subulata extract has potential as an inhibitor of fungal virulence factors without affecting the cell viability. Further research should be carried out in order to assess its inhibitory potential for other fungal virulence factors.

Phytochemical study of Lantana camara flowers, ecotoxicity, antioxidant, in vitro and in silico acetylcholinesterase: molecular docking, MD, and MM/GBSA calculations.

Lantana camara L. (Verbenaceae), commonly called lead cambará, has often been used in folk medicine as antiseptic, antispasmodic, against hemorrhages, flu, colds, and diarrheic. This plant is considered a weed and an ornamental and medicinal plant and is an essential source of natural organic compounds, mainly flavonoids. This work aims to investigate the chemical composition and evaluate the biological properties such as antioxidant and acetylcholinesterase of the constituents from L. camara flowers. In addition, the computational simulation was carried out with the constituents identified. The results showed that methanolic extract of the flowers of L. camara presents toxicity, antioxidant activity with 97.8% inhibition percentage in the concentration of 0.25 mg mL-1 against the DPPH radical, and acetylcholinesterase activity. The phytochemical study of extract from L. camara flowers resulted in LC-MS identification of 18 polyphenolic compounds, such as phenolic acid derivatives, phenylethanoid glycosides, and flavonoids. In the in silico study, flavonoid isoverbascoside showed affinity energy of -9.9 kcal.mol-1 with the AChE enzyme. Their phytochemical content, mainly the presence of flavonoids and phenolic compounds in L. camara extracts, may be related to the antioxidant and anticholinesterase potential observed.

Chemical characterization, cytotoxicity, antimicrobial and antioxidant potential of Justicia pectoralis Jacq and Croton jacobinensis Baill extracts

Abstract In this research, aqueous and ethanolic extracts from Justicia pectoralis Jacq and Croton Jacobinensis Baill were characterized. The UPLC-QTOF-MSE analysis was performed on the extracts identified, predominantly, flavonoids, tannins and acids. The extracts did not indicate toxicity in human epithelial cells. C. jacobinensis presented a concentration of phenolics 60.5% higher than J. pectoralis in all scenarios evaluated and, for both samples, the hydroalcoholic extract at 70% exhibited the best efficiency in the extraction (14501.3 and 32521.5 mg GAE 100 g-1 for J. pectoralis and C. jacobinensis, respectively). The antioxidant activity presented a positive correlation with the concentration of phenolics, being 1.186,1 and 1.507,9 µM of Trolox for J. pectoralis and C. jacobinensis at 70% of ethanol; however, it was not verified statistical difference between the ethanolic solutions (p < 0.05). The antimicrobial activity of J. pectoralis extracts was highlighted once was the most effective against gram-positive bacteria. The results suggest that both J. pectoralis and C. jacobinensis extracts present the potential to be applied as natural additives due to their antioxidant and antimicrobial activity and safety. Thus, it is suggesting the development of studies that could investigate the interaction of these plant extracts with food matrices is required

Evaluation of freeze-dried phenolic extract from cashew apple by-product: Physical properties, in vitro gastric digestion and chemometric analysis of the powders.

The aim of this study was to produce powders from the phenolic extract of the cashew by-product using maltodextrin and gum arabic as encapsulating agents to preserve these bioactive compounds and their antioxidative activity. Extraction was assisted by an ultrasound bath to increase the release of the bioactive compounds, resulting in the hydroalcoholic extract from cashew bagasse. The powders were physically and morphologically characterized, and their total phenolics, antioxidant activity and bioaccessibility were evaluated. All parameters were analyzed by chemometrics. In addition, UPLC-HRMS analysis was used to evaluate the phenolic profile of the extracts, revealing that the powders were able to protect some of the original compounds of the extract, such as catechin, the myricetin fraction and quercetin. The powders showed high total phenolic retention capacity, especially maltodextrin (2893.34 ± 20.18 mg GAE/100 g (DW)), which was the encapsulant that preserved the highest content of polyphenols and antioxidant activity after bioaccessibility in comparison to the unencapsulated extract. The powders showed low water activity (<0.2), low moisture (<8%), high solubility (>60 %) and low hygroscopicity (<4%). The SEM analysis showed that lyophilized extract samples resembled broken glass, which is characteristic of the lyophilization process, and in addition to a predominantly amorphous structure as demonstrated by the X-ray diffraction. The extraction and encapsulation of phenolic compounds from the cashew by-product through lyophilization and using maltodextrin and gum arabic as encapsulants enabled their preservation and potential use of these compounds by the nutraceutical or food industry, and can be used as food additive in order to enrich the content of compounds and the antioxidant activity of numerous products.

Untargeted metabolomic profile of recovered bioactive compounds by subcritical water extraction of acerola (Malpighia emarginata DC.) pomace.

The untargeted metabolomics approach was used to compare the chemical profiles of acerola (Malpighia emarginata DC.) pomace extracts. The effect of drying the raw material before subcritical water extraction (SWE) at different temperatures on the yield, phenolic content, and in vitro antioxidant activity was evaluated. The results were compared with those obtained via Soxhlet and the findings suggest that SWE saves time (15 min) and solvent for extracting valuable components as compared to Soxhlet (6 h). An increase in temperature significantly improved the extraction yield (23.9 to 33.4 %), phenolic content (119.1 to 362 mgGAEg-1), and antioxidant activity, and higher values were obtained with SWE as compared to Soxhlet. The most abundant compounds detected by UPLC-ESI-QTOF-MS were ascorbic acid, kaempferol, quercetin, and isorhamnetin. The investigation of different moisture contents in the SWE showed promising results for eliminating the drying operation, saving time and energy, and obtaining highly concentrated phenolic-rich by-products.

Anti-Candida Properties of Gossypium hirsutum L.: Enhancement of Fungal Growth, Biofilm Production and Antifungal Resistance.

(1) Background: Candida is a genus of yeasts with notable pathogenicity and significant ability to develop antimicrobial resistance. Gossypium hirsutum L., a medicinal plant that is traditionally used due to its antimicrobial properties, has demonstrated significant antifungal activity. Therefore, this study investigated the chemical composition and anti-Candida effects of aqueous (AELG) and hydroethanolic (HELG) extracts obtained from the leaves of this plant. (2) Methods: The extracts were chemically characterized by UPLC-QTOF-MS/MS, and their anti-Candida activities were investigated by analyzing cell viability, biofilm production, morphological transition, and enhancement of antifungal resistance. (3) Results: The UPLC-QTOF-MS/MS analysis revealed the presence of twenty-one compounds in both AELG and HELG, highlighting the predominance of flavonoids. The combination of the extracts with fluconazole significantly reduced its IC50 values against Candida albicans INCQS 40006, Candida tropicalis INCQS 40042, and C. tropicalis URM 4262 strains, indicating enhanced antifungal activity. About biofilm production, significant inhibition was observed only for the AELG-treated C. tropicalis URM 4262 strain in comparison with the untreated control. Accordingly, this extract showed more significant inhibitory effects on the morphological transition of the INCQS 40006 and URM 4387 strains of C. albicans (4) Conclusions: Gossypium hirsutum L. presents promising antifungal effects, that may be potentially linked to the combined activity of chemical constituents identified in its extracts.

Evidence for antioxidant and anti-inflammatory potential of mango (Mangifera indica L.) in naproxen-induced gastric lesions in rat.

This study investigated the anti-inflammatory and antioxidant effects of hydroalcoholic extracts of mango peel and pulp on oxidative damage in a naproxen-induced gastric injury rat model. The extracts were assessed for antioxidant activity (ABTS and FRAP methods), and the phenolic profile was investigated with UPLC-QToF-MSE . Gastric damage was evaluated in vivo by assessing the membrane lipid peroxidation (malondialdehyde (MDA) content), myeloperoxidase (MPO) enzyme activity, and glutathione (GSH) content. Mango peel and pulp contained high contents of bioactive compounds, particularly phenolics (69.50-5.287.70 mg gallic acid equivalents/100 g), carotenoids (651.30-665.50 µg/100 g), and vitamin C (21.59-108.19 mg/100 g). UPLC-QToF-MSE analysis identified 17 phenol compounds, including gallotannins, glycosylated flavonoids, and xanthone. The hydroalcoholic extracts of mango peel and pulp (LPe and LPu, respectively) significantly reduced the MPO activity and MDA content. In addition to preventing naproxen-induced GSH decline, LPe (30 mg/kg) and LPu (10 mg/kg) restored its content to normal levels. LPe and LPu neutralized the oxidizing agents triggered by naproxen and reduced the severity of gastric lesions owing to their antioxidant properties.

UPLC-MS-ESI-QTOF Analysis and Antifungal Activity of Aqueous Extracts of Spondias tuberosa.

This study aimed to identify the chemical composition of the Spondias tuberosa aqueous leaf and root extracts (EALST and EARST) and to evaluate their effect, comparatively, against opportunistic pathogenic fungi. Ultra-Performance Liquid Chromatography Coupled to a Quadrupole/Time of Flight System (UPLC-MS-ESI-QTOF) was employed for chemical analysis. Candida albicans and C. tropicalis standard strains and clinical isolates were used (CA INCQS 40006, CT INCQS 40042, CA URM 5974, and CT URM 4262). The 50% Inhibitory Concentration for the fungal population (IC50) was determined for both the intrinsic action of the extracts and the extract/fluconazole (FCZ) associations. The determination of the Minimum Fungicidal Concentration (MFC) and the verification of effects over fungal morphological transitions were performed by subculture in Petri dishes and humid chambers, respectively, both based on micro-dilution. UPLC-MS-ESI-QTOF analysis revealed the presence of phenolic and flavonoid compounds. The association of the extracts with fluconazole, resulted in IC50 values from 2.62 µg/mL to 308.96 µg/mL. The MFC of the extracts was ≥16,384 µg/mL for all tested strains, while fluconazole obtained an MFC of 8192 µg/mL against C. albicans strains. A reduction in MFC against CA URM 5974 (EALST: 2048 µg/mL and EARST: 1024 µg/mL) occurred in the extract/fluconazole association.

Antioxidant Activity of Stryphnodendron rotundifolium Mart. Stem Bark Fraction in an Iron Overload Model.

Stryphnodendron rotundifolium Mart., popularly known as "barbatimão", is a plant species traditionally used by topical and oral routes for the treatment of infectious and inflammatory diseases. Considering the well-described antioxidant properties of this species, this study investigated the protective effects of its keto-aqueous extract using an in vitro model of iron overload. Phenolic compounds were quantified and identified by Ultra-Performance Liquid Chromatography coupled with quadrupole Time-Of-Flight Electrospray Ionization Mass Spectrometry (UPLC-ESI-qTOF-MS/MS) in positive and negative ions mode analysis. Antioxidant activity was analyzed following the iron-chelating-reducing capacity and deoxyribose degradation (2-DR) protection methods. The analysis identified condensed tannins (54.8 mg catechin/g dry fraction (DF), polyphenols (25 mg gallic acid/g DF), and hydrolyzable tannins (28.8 mg tannic acid/g DF). Among the constituents, prodelphinidin, procyanidin, and prorobinetinidine were isolated and identified. The extract significantly protected 2-DR degradation induced by Fe2+ (72% protection) or •OH (43% protection). The ortho-phenanthroline test revealed Fe2+-chelating and Fe3+-reducing activities of 93% and 84%, respectively. A preliminary toxicological analysis using Artemia salina revealed mortality below 10%, at a concentration of 0.25 mg/mL, indicating low toxicity under the present experimental conditions. In conclusion, the findings of the present study indicate that Stryphnodendron rotundifolium is a source of antioxidant compounds with the potential to be used in drug development in the context of iron overload disorders, which remains to be further investigated in vivo.

Chemical Constituents and Biological Activities of Croton heliotropiifolius Kunth.

Croton heliotropiifolius Kunth (Euphorbiaceae), whose occurrence has already been registered in the most varied Brazilian biomes, is commonly found in the Chapada do Araripe, Ceará. The species is traditionally used to treat fungal, parasitic, and degenerative diseases. This study investigated the chemical composition and pharmacological potential (antioxidant, antifungal, antiparasitic, and cytotoxic) of an aqueous extract obtained from the roots of C. heliotropiifolius. Following a qualitative phytochemical screening, the chemical constituents were identified by ultra-efficiency liquid chromatography coupled witha quadrupole/time-of-flight system (UPLC-QTOF). The antioxidant potential was verified by thin-layer chromatography (TLC). The direct and combined antifungal activity of the extract against opportunistic Candida strains was investigated using the microdilution method. The minimal fungicidal concentration (MFC) was determined by subculture, while the modulation of the morphological transition (fungal virulence) was evaluated by light microscopy. The in vitro antiparasitic activity was analyzed using epimastigotes of Trypanosoma cruzi and promastigotes of Leishmania braziliensis and Leishmania infantum, while cytotoxicity was determined in cultures of mouse fibroblasts. The phytochemical analysis identified the presence of acids, terpenes, flavonoids, lignans, and alkaloids. Among these constituents, the presence of polar and non-polar phenolic compounds with known antioxidant action was highlighted. While the extract showed clinically ineffective antifungal effects, it could enhance the effectiveness of fluconazole, in addition to inhibiting the morphological transition associated with increased virulence in Candida strains. Although the extract showed low cytotoxicity against fibroblasts, it also had weak antiparasitic effects. In conclusion, Croton heliotropiifolius is a source of natural products with antifungal and antioxidant potential.

Chemical profile of colorful bean (Phaseolus vulgaris L) flours: Changes influenced by the cooking method.

This study aimed to determine how the cooking methods change the phenolics and saponins profiles, oligosaccharides, antinutrients and antioxidant properties of flours from colorful beans. The autoclave cooking consisted of: 6 h soaking and 5 min cooking (C5); and 20 min cooking without soaking (C20). Both cooking methods significantly promote changes on the chemical compounds studied, and the intensity of these variations were affected by the cultivars. Most of flours of C5 beans presented a lower loss of anthocyanins (3.9-70.0%), DPPH (11.7-87.2%), ABTS (0.0-82.7%), and tannins (0.0-90.0%) compared with C20. The cooked flours of Artico and Realce showed some similarities among chemical compounds, as well as the lowest concentration of tannins (0.0 mg‧g-1), antioxidant activity (0.40 µmol Trolox‧g-1), and higher amounts of oligosaccharides and acetylcholine. Most of cooked flours presented a reduction in phenolics and soyasaponins αg and ßg, and an increase in soyasaponins Ba and I and oligosaccharides (mainly C20 flours).

UPLC-MS-QTOF analysis and antifungal activity of Cumaru (Amburana cearensis).

This study was aimed at investigating the phytochemical constituents, antifungal properties and antibiotic-modifying activity of the aqueous crude extract and fractions of Amburana cearensis seeds (CEFAC). The CEFAC were chemically characterized by LC-MS/MS-QTOF. In addition, the antifungal activity was assayed by the microdilution method against strains of Candida albicans. The phytochemical profile of CEFAC exhibited phenolic compounds, organic acids, and polyphenols. The results of the assessment of antifungal activity reveled an IC50 ranging from 45.6 to 2048 µg/mL. Interestingly, when CEFAC was associated with Fluconazole, we evidenced a decreased IC50 (1.81-11.9 µg/mL), suggesting a synergism with antibiotic. It was possible to identify in the crude extract and fractions several phenolic compounds, organic acids, and some polyphenols in positive ionization mode. These results suggest that CEFAC may present compounds with the ability to interact and act synergistically with antimicrobial drugs, highlighting its potential as an alternative source for the development of new antimicrobial agents.

Garlic passion fruit (Passiflora tenuifila Killip): Assessment of eventual acute toxicity, anxiolytic, sedative, and anticonvulsant effects using in vivo assays.

Several Passiflora species are known for their sedative and anxiolytic properties. However, the functional properties of Passiflora tenuifila Killip are still unexplored. The objective of this work was to evaluate the phenolic composition and acute toxicity, anxiolytic, sedative, and anticonvulsant effects using in vivo assays. The whole fruit (peel, pulp, and seed) was lyophilized and used for all assays. LC-MS showed 19 phenolic compounds, tentatively identified as flavonoids and phenolic acids. Acute treatment with single doses of up to 2000 mg kg-1 in Wistar rats showed no signs of mortality or toxicity over 14 days. The assay of functional effects was performed with Swiss mice, four groups, received by gavage, doses of P. tenuifila (200 or 400 mg kg-1 body weight), water, and diazepam (as negative and positive control), and behavior tests were performed after 60 min of the treatments. The animals treated with P. tenuifila fruit showed a significant decrease in locomotor activity, indicating a sedative and anxiolytic activity. No significant changes were observed in the rotarod apparatus, suggesting that the P. tenuifila fruit did not cause muscle relaxation. The 400 mg kg-1 dose of P. tenuifila exerted a protective effect against pentylenetetrazole-induced seizures, decreasing the severity and not causing the death of the animals. In conclusion, P. tenuifila showed no acute toxicity and had a promising effect as an anxiolytic agent, hypnotic-sedative and anticonvulsant, which could be related to its composition of flavonoids and phenolic acids.

Use of the natural products from the leaves of the fruitfull tree Persea americana against Candida sp. biofilms using acrylic resin discs.

The search for natural substances such as plant extracts with antimicrobial properties has considerably increased, given that biofilms constitute a barrier against antifungal therapy, where these can be formed on any surface, such as acrylic resin prosthesis. The objective of this study was to identify the chemical composition of the Persea americana Mill. leaf ethanol extract (EEFPa) using the UPLC-QTOF-MS/MS technique, to verify its antifungal activity through a sensitivity test according to the conditions described in the documents in M27-A3 (CLSI, 2008) and M60 (CLSI, 2017), to induce biofilm formation in acrylic resin discs and quantify their formation using tetrazolium salt reduction (MTT), as well as to treat these with the extract and fluconazole. Ten of the twelve compounds present in the extract were identified. In the sensitivity test the lowest minimum inhibitory concentration observed was 512 µg/mL, while fluconazole concentrations ranged from 64 to 1 µg/mL. During biofilm induction, all the isolates were able to form biofilms within 48 h. During biofilm treatment, the extract was less effective at biofilm reduction than Fluconazole. The EEFPa showed significant antifungal activity against some of the strains in this study, however the extract showed lower effect when compared to fluconazole against the biofilm formation.