RESUMEN

Aim: To evaluate the effect of a new Fe-cyclam complex on pathogenic bacterial species, including multidrug-resistant clinical specimens. Materials & methods: The complex [Fe(cyclam)ox]PF6 (D2) was tested in cytotoxicity and MIC tests. Clinical and reference strains of Gram-negative and Gram-positive bacteria were used. Considering Staphylococcus aureus strains, the profile of antimicrobial susceptibility and time-kill kinetics for D2 was performed. An in silico analysis for D2 was also performed. Results: D2 showed broad bacterial activity, mainly against specimens of Cutibacterium acnes, S. aureus, Pseudomonas aeruginosa and Acinetobacter baumannii. Low cytotoxicity in human cells was demonstrated. Conclusion: The tested compound proved to be a promising agent against resistant bacterial infections.

Asunto(s)

Acinetobacter baumannii , Antibacterianos , Humanos , Antibacterianos/farmacología , Antibacterianos/uso terapéutico , Staphylococcus aureus , Brasil , Farmacorresistencia Bacteriana Múltiple , Bacterias , Pruebas de Sensibilidad Microbiana , Pseudomonas aeruginosa

RESUMEN

OBJECTIVES: To evaluate the ability of the aqueous extract of Mitracarpus frigidus (MFAq) to inhibit lipid body formation and inflammatory mediator production in macrophages stimulated with lipopolysaccharide (LPS) and interferon gamma (IFN-γ). METHODS: MFAq was chemically characterized by ultrafast liquid chromatography/quadruple time-of-flight tandem mass spectrometry. The macrophages obtained from mice were incubated with MFAq. Cell viability and membrane integrity were evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide and propidium iodide assays, respectively. Moreover, NO, reactive oxygen species (ROS), transforming growth factor beta (TGF-ß), prostaglandin E2 (PGE2) levels and lipid bodies (LBs) were examined in macrophages that were stimulated with LPS and IFN-γ and treated with MFAq. Finally, molecular docking analysis was conducted to investigate the interaction of MFAq with the cyclooxygenase 2 (COX-2) enzyme. KEY FINDINGS: Chlorogenic acid, clarinoside, harounoside, rutin, kaempferol-3O-rutinoside and 2-azaanthraquinone were identified in MFAq. MFAq significantly inhibited NO, ROS and LBs, and did not affect the membrane integrity of macrophages. MFAq-treated cells showed significantly lower levels of TGF-ß and PGE2. Molecular docking demonstrated that the compounds found in MFAq are able to inhibit COX-2 by binding to important residues in the catalytic site. CONCLUSIONS: MFAq interferes with lipid metabolism in stimulated macrophages, leading to the reduction of important inflammatory mediators. Furthermore, MFAq can directly inhibit the COX-2 enzyme or inhibit its expression owing to its ability to reduce NO production.

Asunto(s)

Dinoprostona , Lipopolisacáridos , Animales , Ratones , Ciclooxigenasa 2/metabolismo , Dinoprostona/metabolismo , Especies Reactivas de Oxígeno/metabolismo , Lipopolisacáridos/farmacología , Metabolismo de los Lípidos , Simulación del Acoplamiento Molecular , Interferón gamma/metabolismo , Factor de Crecimiento Transformador beta/metabolismo

RESUMEN

In recent years, natural products with biological activities have been increasingly researched. The elucidation of phytoconstituents is necessary for the development of drugs as a natural alternative for the treatment of various diseases. The work aimed to evaluate in vitro and in silico bioactivities of hexane (CCHE) and methanol (CCME) fractions of ethanolic extract from Centrosema coriaceum Benth (Fabaceae) leaves and elucidate their phytoconstituents. CCHE and CCME showed antifungal activity for Candida glabrata (MIC of 1000 µg/mL) with fungistatic effect and action in cell envelope by sorbitol and ergosterol assays. CCHE and CCME presented promising antioxidant activity against the DPPH radical with IC50 of 13.61±0.50 and 6.31±0.40 µg/mL, respectively, and relative antioxidant activity (RAA%) of 45.77±3.61/ 28.53±2.25 % for CCHE and 82.18±2.25/51.99±3.23 % for CCME when compared to rutin and quercetin, respectively. Moreover, these fractions demonstrated promising results for the inhibition of lipid peroxidation by ß-carotene/linoleic acid assay. For anti-inflammatory and cytotoxicity activities, CCHE and CCME significantly inhibited the production of nitric oxide and TNF-α, without toxicity on murine intraperitoneal macrophages, respectively. Esters, alkanes, steroids, tocopherols, and terpenes were identified in CCHE by GC/MS. Flavonoids, phenolic acids, and disaccharides were detected in CCME by UFLC-QTOF-MS and FACE. Furthermore, rutin was purified from CCME. In silico predictions evidenced that compounds present in both fractions have high affinity to the fungal membrane besides antioxidant and anti-inflammatory activities. Based on these observations, CCHE and CCME have a noteworthy potential for the design of novel antifungal and anti-inflammatory agents that should be explored in future studies.

Asunto(s)

Antifúngicos , Antioxidantes , Ratones , Animales , Antifúngicos/farmacología , Antifúngicos/química , Antioxidantes/química , Extractos Vegetales/química , Rutina , Antiinflamatorios/farmacología , Antiinflamatorios/química

RESUMEN

ETNOPHARMACOLOGICAL RELEVANCE: Annona muricata L. (soursop) is traditionally used in the treatment of inflammatory diseases, cancer, and infections caused by fungi. The therapeutic activity explored by its medicinal use is generally associated with its phytoconstituents, such as acetogenins and alkaloids. However, its potential antifungal bioactivity as well as its mechanism of action remains to be established. AIM OF THE STUDY: To evaluate the antifungal activity of the ethanolic extract of A. muricata leaves against multidrug-resistant Candida albicans (ATCC® 10231). MATERIAL AND METHODS: Phytoconstituents were detected by UFLC-QTOF-MS. The minimum inhibitory concentration was determined, followed by the determination of the minimum fungicidal concentration. For planktonic cells, the growth curve and cell density were evaluated. Studies to understand the mechanism of action on the cell envelope involved crystal violet permeability, membrane extravasation, sorbitol protection, exogenous ergosterol binding assay, metabolic activity, and cell viability. Furthermore, mitochondrial membrane potential was assessed. RESULTS: Our analyses demonstrated a significant inhibitory effect of A. muricata, with the ability to reduce fungal growth by 58% and cell density by 65%. The extract affected both the fungal plasma membrane and cell wall integrity, with significant reduction of the cell viability. Depolarization of the fungal mitochondrial membrane was observed after treatment with A. muricata. Rutin, xi-anomuricine, kaempferol-3O-rutinoside, nornuciferine, xylopine, atherosperminine, caffeic acid, asimilobine, s-norcorydine, loliolide, annohexocin, annomuricin, annopentocin, and sucrose were identified as extract bioactive components. CONCLUSIONS: Our findings show that the A. muricata extract is a source of chemical diversity, which acts as a potential antifungal agent with promising application to the therapy of infections caused by C. albicans.

Asunto(s)

Annona , Annona/química , Candida albicans , Antifúngicos/farmacología , Antifúngicos/uso terapéutico , Extractos Vegetales/uso terapéutico , Pared Celular , Membrana Celular , Verduras

RESUMEN

OBJECTIVES: This study aimed to evaluate the potential of aqueous extract from Mitracarpus frigidus aerial parts (MFAq) in the treatment of inflammation and oxidative stress, as well as to characterize its chemical constituents. METHODS: Total phenolic and flavonoid contents were determined, and phytoconstituents were detected by ultra-fast liquid chromatography/quadrupole-time-of-flight tandem mass spectrometry (UFLC-QTOF-MS). The antioxidant activity was evaluated by DPPH, TAC and ß-carotene/linoleic acid assays. In-vitro anti-inflammatory activity, cell viability and cell cycle were performed in J774A.1 cell line. In-vivo anti-inflammatory activity was investigated by two ear oedema assays (croton oil and phenol). KEY FINDINGS: Chlorogenic acid, clarinoside, quercetin-hexosylpentoside, rutin, kaempferol-3-O-rutinoside, kaempferol-rhamnosylhexoside, quercetin-pentosylrhamnosylhexoside, harounoside, 2-azaanthraquinone and sucrose were identified by UFLC-QTOF-MS. MFAq showed antioxidant activity, which was positively correlated to the content of phenolic compounds. MFAq significantly inhibited the production of nitric oxide, did not decrease viability in MTT assay (all concentrations) and showed no changes in membrane permeability and cell cycle of J774A.1 cell line. Furthermore, MFAq showed a reduction in ear oedema in all tested doses. CONCLUSION: MFAq was effective in some antioxidant and inflammatory parameters, in the experimental conditions that were used in the study. This is the first report of chemical composition and bioactivities from this extract.

Asunto(s)

Rubiaceae , Antiinflamatorios/uso terapéutico , Antioxidantes/química , Edema/inducido químicamente , Edema/tratamiento farmacológico , Humanos , Fenoles/farmacología , Extractos Vegetales/química , Quercetina , Rubiaceae/química

RESUMEN

Centrosema coriaceum Benth belongs to Fabaceae family and have few studies of biological activity and chemical composition. Thus, the aims of this work were to determine chemical profile of the ethanolic extract of C. coriaceum leaves (CCE) by UFLC-QTOF-MS and to evaluate its in vitro biological potential. CCE showed MIC value of 1000 µg/mL against Candida glabrata (fungistatic effect) and high affinity in cell envelope by increasing cell permeability in nucleotide leakage, sorbitol and ergosterol assays. CCE showed antioxidant activity in all assays performed. For the anti-inflammatory and cytotoxicity activities, CCE, at all tested concentrations, significantly inhibited the production of nitric oxide and did not decrease J774A.1 cell viability below 70%. Finally, rutin, kaempferol-3O-rutinoside, caffeic acid, and sucrose were identified in CCE by UFLC-QTOF-MS. These results suggest, for the first time, that C. coriaceum has interesting antifungal, antioxidant, and anti-inflammatory activities.

Asunto(s)

Fabaceae , Antiinflamatorios/farmacología , Antioxidantes/farmacología , Extractos Vegetales/farmacología , Hojas de la Planta

RESUMEN

Spilanthol is a bioactive alkylamide from the native Amazon plant species, Acmella oleracea. However, antifungal activities of spilanthol and its application to the therapeutic treatment of candidiasis remain to be explored. This study sought to evaluate the in vitro and in vivo antifungal activity of spilanthol previously isolated from A. oleracea (spilanthol(AcO)) against Candida albicans ATCC® 10231™, a multidrug-resistant fungal strain. Microdilution methods were used to determine inhibitory and fungicidal concentrations of spilanthol(AcO). In planktonic cultures, the fungal growth kinetics, yeast cell metabolic activity, cell membrane permeability and cell wall integrity were investigated. The effect of spilanthol(AcO) on the proliferation and adhesion of fungal biofilms was evaluated by whole slide imaging and scanning electron microscopy. The biochemical composition of the biofilm matrix was also analyzed. In parallel, spilanthol(AcO) was tested in vivo in an experimental vulvovaginal candidiasis model. Our in vitro analyses in C. albicans planktonic cultures detected a significant inhibitory effect of spilanthol(AcO), which affects both yeast cell membrane and cell wall integrity, interfering with the fungus growth. C. albicans biofilm proliferation and adhesion, as well as, carbohydrates and DNA in biofilm matrix were reduced after spilanthol(AcO) treatment. Moreover, infected rats treated with spilanthol(AcO) showed consistent reduction of both fungal burden and inflammatory processes compared to the untreated animals. Altogether, our findings demonstrated that spilanthol(AcO) is an bioactive compound against planktonic and biofilm forms of a multidrug resistant C. albicans strain. Furthermore, spilanthol(AcO) can be potentially considered for therapeutical treatment of vulvovaginal candidiasis caused by C. albicans. LAY SUMMARY: This study sought to evaluate the antifungal activity of spilanthol against Candida albicans ATCC® 10 231™, a multidrug-resistant fungal strain. Our findings demonstrated that spilanthol(AcO) can be potentially considered for therapeutical treatment of vulvovaginal candidiasis caused by C. albicans.

Asunto(s)

Candidiasis Vulvovaginal , Enfermedades de los Roedores , Animales , Antifúngicos/farmacología , Antifúngicos/uso terapéutico , Biopelículas , Candida albicans , Candidiasis Vulvovaginal/tratamiento farmacológico , Candidiasis Vulvovaginal/veterinaria , Pruebas de Sensibilidad Microbiana/veterinaria , Alcamidas Poliinsaturadas/farmacología , Ratas , Enfermedades de los Roedores/tratamiento farmacológico

RESUMEN

Candida tropicalis is one the most relevant biofilm-forming fungal species increasingly associated with invasive mucosal candidiasis worldwide. The amplified antifungal resistance supports the necessity for more effective and less toxic treatment, including the use of plant-derived natural products. Scopoletin, a natural coumarin, has shown antifungal properties against plant yeast pathogens. However, the antifungal activity of this coumarin against clinically relevant fungal species such as C. tropicalis remains to be established. Here, we investigated the potential antifungal properties and mechanisms of action of scopoletin against a multidrug-resistant C. tropicalis strain (ATCC 28707). First, scopoletin was isolated by high-performance liquid chromatography from Mitracarpus frigidus, a plant species (family Rubiaceae) distributed throughout South America. Next, scopoletin was tested on C. tropicalis cultivated for 48h in both planktonic and biofilm forms. Fungal planktonic growth inhibition was analyzed by evaluating minimal inhibitory concentration (MIC), time-kill kinetics and cell density whereas the mechanisms of action were investigated with nucleotide leakage, efflux pumps and sorbitol and ergosterol bioassays. Finally, the scopoletin ability to affect C. tropicalis biofilms was evaluated through spectrophotometric and whole slide imaging approaches. In all procedures, fluconazole was used as a positive control. MIC values for scopoletin and fluconazole were 50 and 250 µg/L respectively, thus demonstrating a fungistatic activity for scopoletin. Scopoletin induced a significant decrease of C. tropicalis growth curves and cell density (91.7% reduction) compared to the growth control. Its action was related to the fungal cell wall, affecting plasma membrane sterols. When associated with fluconazole, scopoletin led to inhibition of efflux pumps at the plasma membrane. Moreover, scopoletin not only inhibited the growth rate of preformed biofilms (68.2% inhibition at MIC value) but also significantly decreased the extent of biofilms growing on the surface of coverslips, preventing the formation of elongated fungal forms. Our data demonstrate, for the first time, that scopoletin act as an effective antifungal phytocompound against a multidrug-resistant strain of C. tropicalis with properties that affect both planktonic and biofilm forms of this pathogen. Thus, the present findings support additional studies for antifungal drug development based on plant isolated-scopoletin to treat candidiasis caused by C. tropicalis.

RESUMEN

Psychorubrin, a natural pyranonaphthoquinone found in different plants, has become an interesting compound in the search for new antimicrobial therapeutic agents. Here, we investigated the potential antagonistic activity of psychorubrin against planktonic and biofilm bacteria. First, psychorubrin was tested against several Gram-positive and Gram-negative bacteria strains by a broth microdilution susceptibility method. Second, bacterial killing assay, bacterial abundance, and membrane viability were evaluated. The nucleotide leakage assay was used to verify membrane destabilization while antibiofilm activities were analyzed by the effect on established biofilm, static biofilm formation, isolation of biofilm matrix assay and scanning electron microscopy. In parallel, the combinatorial effect of psychorubrin and chloramphenicol was evaluated by the checkerboard method. Psychorubrin was active against Gram-positive bacteria, showing rapid time-dependent kinetics of bacterial killing, amplified nucleotide leakage, and greater activity against the methicillin-resistant species (MRSA) Staphylococcus aureus 33591 and 33592 and Staphylococcus pyogenes 10096. Psychorubrin also interfered with the composition of the biofilm matrix by reducing the total content of carbohydrates and proteins. A synergic effect between psychorubrin and chloramphenicol was observed for S. aureus 33592 and S. pyogenes 10096 while an additive effect was detected for S. aureus 33591. Our findings demonstrate, for the first time, an antagonistic activity of psychorubrin against bacteria not only in their planktonic forms but also in biofilms, and identify bacterial membranes as primary targets for this compound. Based on these observations, psychorubrin has a good potential for the design of novel antimicrobial agents.

RESUMEN

Palicourea rigida Kunth is traditionally used for the treatment of skin diseases, kidney pains and ovarian inflammation. Based on these traditional uses, this study evaluated the topical anti-inflammatory activity of the ethanol extract from P. rigida leaves (EEPR) and identified bioactive compounds. Ear edema was induced in Swiss mice by the topical application of Croton oil, arachidonic acid, phenol and capsaicin. Histopathological analysis and myeloperoxidase and N-acetyl-ß-D-glucosaminidase activities were determined. EEPR was characterized by UHPLC-UV-MS HPLC and the isolated compound was identified through 1H and 13C nuclear magnetic resonance and mass fragmentation. Interaction profiles between quercetin 3-O-ß-D-glucoside and cyclooxygenase-1 and -2 were established by molecular docking. EEPR significantly inhibited ear edema induced by Croton oil (p < 0.001), arachidonic acid (p < 0.01), phenol (p < 0.001) and capsaicin (p < 0.01 or p < 0.001). Histopathological analysis showed a reduction of edema, inflammatory cell infiltration and vasodilation. Additionally, the myeloperoxidase and N-acetyl-ß-D-glucosaminidase activities were decreased (p < 0.001). From spectroscopic data, quercetin 3-O-ß-D-glucoside was the identified compound. This compound can to interact with cyclooxygenase-1 and -2 through van der Waals interactions and dipole-dipole and hydrogen bonding's, demonstrating inhibition of these enzymes. The results indicate that EEPR is a source of active compounds with topical anti-inflammatory activity, justifying the traditional use of P. rigida and showing that this species has a therapeutic potential to treat skin inflammatory processes.

Asunto(s)

Antiinflamatorios/farmacología , Edema/tratamiento farmacológico , Extractos Vegetales/farmacología , Rubiaceae/química , Administración Tópica , Animales , Antiinflamatorios/aislamiento & purificación , Cromatografía Líquida de Alta Presión/métodos , Modelos Animales de Enfermedad , Edema/patología , Inflamación/tratamiento farmacológico , Inflamación/patología , Masculino , Ratones , Simulación del Acoplamiento Molecular , Extractos Vegetales/química , Hojas de la Planta

RESUMEN

This study aimed to further investigate the cytotoxicity against tumor cell lines and several bacterial strains of Annona squamosa and its mode of action. Methanol extracts of A. squamosa leaves (ASL) and seeds (ASS) were used. ASL showed significant antibacterial activity against S. aureus, K. pneumoniae and E. faecalis with MIC values of 78, 78 and 39 µg/mL respectively. Moreover, ASL exhibited significant biofilm disruption, rapid time dependent kinetics of bacterial killing, increased membrane permeability and significantly reduced the cell numbers and viability. Regarding the cytotoxicity against tumor cell lines, ASS was more active against Jurkat and MCF-7 cells, with CI50 1.1 and 2.1 µg/mL, respectively. ASL showed promising activity against Jurkat and HL60, with CI50 4.2 and 6.4 µg/mL, respectively. Both extracts showed lower activity against VERO cells and reduced the clonogenic survival at higher concentrations (IC90) to MCF-7 and HCT-116 lineages. The alkaloids anonaine, asimilobine, corypalmine, liriodenine nornuciferine and reticuline were identified in extracts by UPLC-ESI-MS/MS analysis. This study reinforced that A. squamosa presents a remarkable phytomedicinal potential and revealed that its antimicrobial mechanism of action is related to bacterial membrane destabilization.

Asunto(s)

Annona/química , Antibacterianos/farmacología , Enterococcus faecalis/efectos de los fármacos , Klebsiella pneumoniae/efectos de los fármacos , Extractos Vegetales/farmacología , Staphylococcus aureus/efectos de los fármacos , Animales , Línea Celular Tumoral/efectos de los fármacos , Membrana Celular/efectos de los fármacos , Chlorocebus aethiops , Humanos , Pruebas de Sensibilidad Microbiana

RESUMEN

OBJECTIVES: The aims of this study were to investigate the chemical composition and the antioxidant activity and antibacterial activity of the essential oil of Xylopia sericea fruits (OXS). The fruits of this species are popularly used for medicinal purposes, and as a condiment in food preparation. METHODS: The chemical composition of OXS was analysed by GC/MS. 1,1-Diphenyl-2-picrylhydrazyl (DPPH) scavenging, ß-carotene/linoleic acid bleaching and phosphomolybdenum and thiobarbituric acid-reactive substance (TBARS) assays were used to evaluate the antioxidant activity. Antibacterial activity was assessed by minimal inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) against bacterial strains of interest to human health and food spoilage. KEY FINDINGS: Eighty-four compounds were identified. The sesquiterpenes spathulenol (16.42%), guaiol (13.93%) and germacrene D (8.11%) were the most abundant constituents. OXS presented a significant antioxidant activity and also a high bacteriostatic effect against Staphylococcus aureus, Enterobacter cloacae, Bacillus cereus and Klebsiella pneumoniae. CONCLUSIONS: Those results evidenced the potential of OXS to treat human bacterial infections and as an antimicrobial ingredient for food preservation.

Asunto(s)

Antibacterianos/farmacología , Antioxidantes/farmacología , Frutas/química , Aceites Volátiles/farmacología , Extractos Vegetales/farmacología , Aceites de Plantas/farmacología , Xylopia/química , Antibacterianos/química , Antioxidantes/química , Bacterias/efectos de los fármacos , Compuestos de Bifenilo/química , Compuestos de Bifenilo/farmacología , Brasil , Pruebas de Sensibilidad Microbiana/métodos , Aceites Volátiles/química , Picratos/química , Picratos/farmacología , Extractos Vegetales/química , Aceites de Plantas/química , Sesquiterpenos/química , Sesquiterpenos/farmacología , Sesquiterpenos de Germacrano/química , Sesquiterpenos de Germacrano/farmacología , Sesquiterpenos de Guayano

RESUMEN

ABSTRACT This study aimed to further investigate the cytotoxicity against tumor cell lines and several bacterial strains of Annona squamosa and its mode of action. Methanol extracts of A. squamosa leaves (ASL) and seeds (ASS) were used. ASL showed significant antibacterial activity against S. aureus, K. pneumoniae and E. faecalis with MIC values of 78, 78 and 39 µg/mL respectively. Moreover, ASL exhibited significant biofilm disruption, rapid time dependent kinetics of bacterial killing, increased membrane permeability and significantly reduced the cell numbers and viability. Regarding the cytotoxicity against tumor cell lines, ASS was more active against Jurkat and MCF-7 cells, with CI50 1.1 and 2.1 µg/mL, respectively. ASL showed promising activity against Jurkat and HL60, with CI50 4.2 and 6.4 µg/mL, respectively. Both extracts showed lower activity against VERO cells and reduced the clonogenic survival at higher concentrations (IC90) to MCF-7 and HCT-116 lineages. The alkaloids anonaine, asimilobine, corypalmine, liriodenine nornuciferine and reticuline were identified in extracts by UPLC-ESI-MS/MS analysis. This study reinforced that A. squamosa presents a remarkable phytomedicinal potential and revealed that its antimicrobial mechanism of action is related to bacterial membrane destabilization.

Asunto(s)

Humanos , Animales , Staphylococcus aureus/efectos de los fármacos , Extractos Vegetales/farmacología , Enterococcus faecalis/efectos de los fármacos , Annona/química , Klebsiella pneumoniae/efectos de los fármacos , Antibacterianos/farmacología , Pruebas de Sensibilidad Microbiana , Membrana Celular/efectos de los fármacos , Chlorocebus aethiops , Línea Celular Tumoral/efectos de los fármacos

RESUMEN

Manihot multifida (L.) Crantz (Euphorbiaceae) is widely used in popular medicine for the treatment of infected wounds. This study evaluated the in vitro antioxidant and antimicrobial potential of this species against strains of Gram-positive and Gram-negative bacteria and fungi, known to cause infections in humans. The extracts showed minimal inhibitory concentration (MIC) varying from 39 to 2500 µg/mL for antimicrobial activity. The methanolic extract of fruits, aqueous and hexane extracts of leaves showed a very strong activity against Candida albicans (ATCC 18804) with MIC of 39 µg/mL. Furthermore, the methanolic extract of M. multifida leaves exhibited DPPH (1,1-diphenyl-2-picrylhydrazyl) scavenging potential with inhibitory concentration (IC50) values of 46.9 µg/mL, followed by hexane extract of leaves with IC50 values of 59.2 µg/mL. The cytotoxic activity against brine shrimp was stronger for the methanolic extract of leaves (lethal concentration - LC50 of 15.6 µg/mL). These results suggest that M. multifida has interesting antimicrobial and antioxidant activities. Moreover, these results corroborate the popular use of this specie in treating fungal infections since it demonstrates significant activity against C. albicans.

Asunto(s)

Antibacterianos/farmacología , Antifúngicos/farmacología , Antioxidantes/farmacología , Manihot/química , Extractos Vegetales/farmacología , Animales , Artemia/efectos de los fármacos , Candida albicans/efectos de los fármacos , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Pruebas de Sensibilidad Microbiana , Hojas de la Planta/química

RESUMEN

The anti-inflammatory and apoptotic activity of the essential oil of Syzygium cumini (L.) Skeels, Myrtaceae, leaves was investigated in vivo. The anti-inflammatory action and chronic granulomatous inflammation in BALB/c mice, intravenously infected with Mycobacterium bovis, BCG, (Bacillo Calmet Guerim), was judged by measuring and classifying the granulomas formed in the hepatic parenchyma. The degree of apoptosis in the inflammatory cells was also measured. A reduction in the granulomatous area and a change in the pattern of the granulomas were found. Anti-mycobacterial activity of the essential oil against M. bovis was detected in vitro by an interferometric method in liquid culture medium. The chemical constituents of the essential oil were determined by GC/MS. Higher yields of the essential oil of S. cumini leaves were obtained by extraction in a Clevenger apparatus when the fresh leaves were previously frozen as a pre-processing step. The essential oil obtained from this plant demonstrated a statistically significant and dramatic effect in the chosen model system.

RESUMEN

In our previous work (Fabri et al. 2009), we showed that different extracts of Mitracarpus frigidus had significant antibacterial, antifungal and leishmanicidal activities. In order to increase our knowledge about this species, this work assesses the chemical composition and the in vitro biological activity of its essential oil. Thus, the essential oil obtained by hydrodistillation of the aerial parts of M. frigidus was analyzed by GC/MS. Among several compounds detected, 11 were identified, being linalool and eugenol acetate the major components. The essential oil exhibited a moderate antibacterial effect against Staphyloccocus aureus, Bacillus cereus, Pseudomonas aeruginosa and Enterobacter cloacae (MIC 250 µg/mL). On the other hand, it showed a strong antifungal effect against Cryptoccocus neoformans (MIC 8 µg/mL) and Candida albicans (MIC 63 µg/mL). Expressive activity against L. major and L. amazonensis promastigote forms with IC50 values of 47.2 and 89.7 µg/mL, respectively, were also observed. In addition, the antioxidant activity was investigated through DPPH radical-scavenging and showed a significative activity with IC50 of 38 µg/mL. The cytotoxicity against Artemia salina was moderate with LC(50) of 88 µg/mL. The results presented here are the first report on the chemical composition and biological properties of M. frigidus essential oil.

Asunto(s)

Antibacterianos/farmacología , Antifúngicos/farmacología , Antiprotozoarios/farmacología , Aceites Volátiles/farmacología , Rubiaceae/química , Animales , Antibacterianos/aislamiento & purificación , Antifúngicos/aislamiento & purificación , Antiprotozoarios/aislamiento & purificación , Candida albicans/efectos de los fármacos , Cryptococcus neoformans/efectos de los fármacos , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Leishmania/efectos de los fármacos , Pruebas de Sensibilidad Microbiana , Aceites Volátiles/química , Pruebas de Sensibilidad Parasitaria , Rubiaceae/clasificación

RESUMEN

The bioactivity guided fractionation of the dichloromethane extract of Mitracarpus frigidus afforded the pyranonaphthoquinone psychorubrin. This compound, hitherto unknown in the genus Mitracarpus, had its biological activity evaluated against one panel of bacteria and two fungi, three tumor cell lines (HL60, Jurkat and MCF-7) and four Leishmania species. Its identity was confirmed unambiguously by (1)H, (13)C, (1)H-COSY, IR and UV-Vis spectroscopy and mass spectrometry. Psychorubrin displayed a very promising antitumor with IC(50) of 4.5, 5.6 and 1.1 µM for HL60, Jurkat and MCF-7 cell lines, respectively. Antimicrobial activity, mainly against Cryptococcus neoformans (MIC of 87.3 µM) was observed. A pronounced antileishmanial potential was also verified with IC(50) varying from 1.7 to 2.7 µM for the Leishmania species tested. This is the first report of the presence of pyranonapthoquinones in the Mitracarpus genus, which may serve as a chemotaxonomical marker.

Asunto(s)

Antibacterianos/farmacología , Antineoplásicos Fitogénicos/farmacología , Antiprotozoarios/farmacología , Naftoquinonas/farmacología , Rubiaceae/química , Antibacterianos/aislamiento & purificación , Antineoplásicos Fitogénicos/aislamiento & purificación , Antiprotozoarios/aislamiento & purificación , Línea Celular Tumoral , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Humanos , Concentración 50 Inhibidora , Leishmania/efectos de los fármacos , Pruebas de Sensibilidad Microbiana , Naftoquinonas/aislamiento & purificación

RESUMEN

This paper compares two medicinal species of Kalanchoe, which are often used interchangeably by the population, regarding the distribution of anthocyanins under the influence of four luminosity levels for 6 months. For the morphoanatomical analysis, the 6th stem node of each plant was sectioned. Usual histochemical tests revealed the presence of anthocyanins by cross sections of the stems, petioles and leaf blades. The petioles and leaf blades were submitted to the extraction with acidified methanol, and the anthocyanins were quantified by spectrophotometric readings. At the macroscopic level, it was noticed for both species a higher presence of anthocyanins in stems and petioles of plants under full sunlight. The microscopy of K. brasiliensis stems evidenced the deposition of anthocyanins in the subjacent tissue to the epidermis and cortex, which increased with light intensity. In K. pinnata a subepidermal collenchyma was observed, which interfered in the visualization of anthocyanins. In petioles and leaf blades of K. brasiliensis the deposition of anthocyanins was peripheral, and in K. pinnata it was also throughout the cortex. The quantification of anthocyanins in petioles showed in 70% of light higher averages than in 25%, but in leaf blades there were no significant results. This study contributes to the pharmacognosy of Kalanchoe and it is sustained by the description of flavonoids as biological markers of the genus.

Asunto(s)

Antocianinas/análisis , Kalanchoe/química , Luz , Plantas Medicinales/química , Kalanchoe/anatomía & histología , Farmacognosia , Hojas de la Planta/anatomía & histología , Hojas de la Planta/química , Tallos de la Planta/anatomía & histología , Tallos de la Planta/química , Plantas Medicinales/anatomía & histología , Espectrofotometría

RESUMEN

This study compares the development of Kalanchoe brasiliensis and Kalanchoe pinnata, which are medicinal species known as "saião" and "folha da fortuna" that are used interchangeably by the population for medicinal purposes. The experiment consisted of 20 plots/species planted in plastic bags with homogeneous substrate in a randomized design, which grown under light levels (25%, 50%, 70%, full sunlight) at environment temperature, and a treatment under a plastic with greater temperature range than the external environment. It was obtained for K. pinnata a greater plant height, total length of sprouts, stems, production and dry matter content of leaves than that obtained for K. brasiliensis, which achieved higher averages only for the length of lateral branches. The species showed increases in height, which varied in inverse proportion to the light, and it was observed the influence of temperature in K. pinnata. The production and dry matter content of leaves were proportional to the luminosity; the same occurred in the thickness of leaves for K. brasiliensis. In the swelling index and Brix degree, K. brasiliensis showed higher averages than K. pinnata. In relation to the total content of flavonoids it was not observed significant differences for both species. The analyzed parameters showed the main differences in the agronomic development of the two species.

Asunto(s)

Flavonoides/análisis , Kalanchoe/crecimiento & desarrollo , Kalanchoe/anatomía & histología , Kalanchoe/química , Luz , Hojas de la Planta/química , Temperatura

RESUMEN

This study compares the development of Kalanchoe brasiliensis and Kalanchoe pinnata, which are medicinal species known as "saião" and "folha da fortuna" that are used interchangeably by the population for medicinal purposes. The experiment consisted of 20 plots/species planted in plastic bags with homogeneous substrate in a randomized design, which grown under light levels (25 percent, 50 percent, 70 percent, full sunlight) at environment temperature, and a treatment under a plastic with greater temperature range than the external environment. It was obtained for K. pinnata a greater plant height, total length of sprouts, stems, production and dry matter content of leaves than that obtained for K. brasiliensis, which achieved higher averages only for the length of lateral branches. The species showed increases in height, which varied in inverse proportion to the light, and it was observed the influence of temperature in K. pinnata. The production and dry matter content of leaves were proportional to the luminosity; the same occurred in the thickness of leaves for K. brasiliensis. In the swelling index and Brix degree, K. brasiliensis showed higher averages than K. pinnata. In relation to the total content of flavonoids it was not observed significant differences for both species. The analyzed parameters showed the main differences in the agronomic development of the two species.

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Este estudo compara o desenvolvimento de Kalanchoe brasiliensis e Kalanchoe pinnata, espécies medicinais conhecidas como "saião" e "folha da fortuna" que são utilizadas indiferenciadamente pela população para fins medicinais. O experimento consistiu em 20 parcelas/espécie plantadas em sacos plásticos com substrato homogêneo, em delineamento ao acaso, cultivadas sob níveis de luminosidade (25 por cento, 50 por cento, 70 por cento, luz plena) em temperatura ambiente, e um tratamento sob plástico com maior amplitude térmica que o meio externo. Obteve-se para K. pinnata maiores alturas de plantas, comprimentos totais de brotos, caules, produção e teor de matéria seca de folhas que para K. brasiliensis, que alcançou maiores médias apenas para comprimentos de ramos laterais. As espécies apresentaram aumento em altura que variou em proporção inversa à incidência luminosa, e observou-se a influência da temperatura em K. pinnata. A produção e teor de matéria seca de folhas foram proporcionais à luminosidade; o que também ocorreu na espessura foliar para K. brasiliensis. No índice de intumescência e grau Brix, K. brasiliensis apresentou maiores médias que K. pinnata. Em relação ao teor de flavonoides totais, não foram observadas diferenças significativas para ambas as espécies. Os parâmetros analisados apontaram as principais diferenças no desenvolvimento agronômico das duas espécies.

Asunto(s)

Flavonoides/análisis , Kalanchoe/crecimiento & desarrollo , Kalanchoe/anatomía & histología , Kalanchoe/química , Luz , Hojas de la Planta/química , Temperatura