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1.
Biomedicines ; 11(9)2023 Sep 14.
Article in English | MEDLINE | ID: mdl-37760978

ABSTRACT

Hyperuricemia, the metabolic alteration that leads to gout or gouty arthritis, is increasing worldwide. Glycoconjugated triazole-phthalimides show potent anti-inflammatory activity. The aim of this study was to evaluate the anti-hyperuricemia effect of glycoconjugated triazole-phthalimides. To develop hyperuricemia, groups of mice received orally potassium oxonate (250 mg/kg) for 7 days, and F2, F3 and F4 glycoconjugated triazole-phthalimides (20 mg/kg), allopurinol (300 mg/kg), and 1% carboxymethylcellulose; indomethacin (2 and 4 mg/kg) was the positive control for anti-arthritic effect. Genotoxic and mutagenic effects were evaluated by the comet and micronucleus assays, respectively. The hemolytic action of the compounds was evaluated. Phthalimides F2, F3 and F4 significantly reduced the levels of serum uric acid, creatinine and urea in hyperuricemic animals. In addition, the compounds were efficient in reducing protein denaturation in a dose-dependent manner. In an interesting way, the histopathological analysis of kidneys from groups treated with F2, F3 and F4 showed a glomerular architecture, with the Bowman's capsule and renal tubules having a normal appearance and without inflammatory changes. Also, F2 and F4 showed a small increase in micronuclei, indicating a low mutagenic effect, whilst by comet assay only, we could infer that F4 affected the frequency and damage index, thus indicating a very small genotoxic action. Similarly, the phthalimides showed a low degree of erythrocyte hemolysis (<3%). Our data demonstrate that the new glycoconjugate triazole-phthalimides have potential to treat hyperuricemia and its secondary complications, such as gouty arthritis, with a low to non-significant rate of erythrocytes hemolysis, genotoxicity and mutagenicity making these molecules strong candidates as pharmaceutical agents for treatment requiring uric-acid-lowering therapy.

2.
J Ethnopharmacol ; 303: 115964, 2023 Mar 01.
Article in English | MEDLINE | ID: mdl-36436717

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Medicinal plants belonging to the genus Mimosa, such as Mimosa tenuiflora, M. caesalpinifolia, and M. verrucosa are known for their popular use for asthma, bronchitis and fever. Ethnopharmacological studies report that Mimosa acutistipula is used to treat alopecia and pharyngitis, conditions that can be related to oxidative stress, inflammatory processes and painful limitations. However, there is no studies on its efficacy and mechanism of action. AIM OF THE STUDY: To elucidate the antioxidant, anti-inflammatory, analgesic and antipyretic activity of M. acutistipula leaves. MATERIALS AND METHODS: Phytochemical profile of M. acutistipula extracts was evaluated by several reaction-specific methods. Secondary metabolites such as tannins, phenols and flavonoids were quantified with colorimetric assays. In vitro antioxidant potential was evaluated using DPPH and ABTS + as free radical scavenging tests, FRAP and phosphomolybdenum as oxide-reduction assays, and anti-hemolytic for lipid peroxidation evaluation. In vivo anti-inflammatory evaluation was performed by paw edema, and peritonitis induced by carrageenan. Analgesic effect and its possible mechanisms were determined by acetic acid-induced abdominal writhing and the formalin test. Antipyretic activity was evaluated by yeast-induced fever. RESULTS: Cyclohexane, chloroform, ethyl acetate and methanol extracts of leaves had presence of tannins, flavonoids, phenol, alkaloids, terpenes (except methanolic extract), and saponins (only for methanolic and chloroformic extracts). In phenols, flavonoids and tannins quantification, methanolic and ethyl acetate extract had higher amounts of this phytocompounds. Ethyl acetate extract, due to its more expressive quantity of phenols and flavonoids, was chosen for carrying out the in vivo tests. Due to the relationship between oxidative stress and inflammation, antioxidant tests were performed, showing that ethyl acetate extract had a high total antioxidant activity (70.18%), moderate activity in DPPH radical scavenging, and a moderate ABTS + radical inhibition (33.61%), and FRAP assay (112.32 µg Fe2+/g). M. acutistipula showed anti-inflammatory activity, with 54.43% of reduction in paw edema (50 mg/kg) when compared to the vehicle. In peritonitis test, a reduction in the concentration of NO could be seen, which is highly involved in the anti-inflammatory activity and is responsible for the increase in permeability. In the analgesic evaluation, most significant results in writhing test were seen at 100 mg/kg, with a 34.7% reduction of writhing. A dual mechanism of action was confirmed with the formalin test, both neurogenic and inflammatory pain were reduced, with a mechanism via opioid route. In the antipyretic test, results were significantly decreased at all concentrations tested. CONCLUSION: M. acutistipula leaves ethyl acetate extract showed expressive concentrations of phenolic compounds and antioxidant activity. It also exhibited anti-inflammatory and analgesic activity, besides its antipyretic effect. Thus, these results provide information regarding its popular use and might help future therapeutics involving this specimen.


Subject(s)
Antipyretics , Mimosa , Peritonitis , Antioxidants/pharmacology , Antioxidants/therapeutic use , Antioxidants/chemistry , Antipyretics/pharmacology , Antipyretics/therapeutic use , Plant Extracts/pharmacology , Plant Extracts/therapeutic use , Plant Extracts/chemistry , Analgesics/pharmacology , Analgesics/therapeutic use , Analgesics/chemistry , Anti-Inflammatory Agents/pharmacology , Anti-Inflammatory Agents/therapeutic use , Anti-Inflammatory Agents/chemistry , Pain/drug therapy , Pain/chemically induced , Tannins , Flavonoids/pharmacology , Methanol/chemistry , Phenols/therapeutic use , Peritonitis/drug therapy , Edema/chemically induced , Edema/drug therapy
3.
Ultrasound Med Biol ; 48(12): 2417-2429, 2022 12.
Article in English | MEDLINE | ID: mdl-36115728

ABSTRACT

Therapeutic ultrasound (TUS) is the ultrasound modality widely used in physical therapy for the treatment of acute and chronic injuries of various biological tissues. Its thermal and mechanical effects modify the permeability of the plasma membrane, the flow of ions and molecules and cell signaling and, in this way, promote the cascade of physiological events that culminate in the repair of injuries. This article is a review of the biochemical and physiological effects of TUS with parameters commonly used by physical therapists. Integrins can translate the mechanical signal of the TUS into a cellular biochemical signal for protein synthesis and modification of the active site of enzymes, so cell function and metabolism are modified. TUS also alters the permeability of the plasma membrane, allowing the influx of ions and molecules that modulate the cellular electrochemical signaling pathways. With biochemical and electrochemical signals tampered with, the cellular response to damage is then modified or enhanced. Greater release of pro-inflammatory factors, cytokines and growth factors, increased blood flow and activation of protein kinases also seem to be involved in the therapeutic response of TUS. Although a vast number of publications describe the mechanisms by which TUS can interact with the biological system, little is known about the metabolic possibilities of TUS because of the lack of standardization in its application.


Subject(s)
Integrins , Physical Therapy Modalities , Ultrasonography , Protein Kinases , Cytokines
4.
J Ethnopharmacol ; 287: 114958, 2022 Apr 06.
Article in English | MEDLINE | ID: mdl-34965459

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Indigofera suffruticosa has reports of its popular use for analgesy in several cultures. Besides that, all parts of this plant are used for some medicinal outcome. The leaves are used in teas, decoctions, juices and included in baths for treating fever and inflammatory processes. AIM OF THE STUDY: To evaluate the anti-inflammatory activity mechanisms of I. suffruticosa leave aqueous extract (IsAE). MATERIALS AND METHODS: Phytochemical screening of IsAE was performed by thin layer chromatography. Total flavonoid content was determined and expressed by milligram of quercetin equivalent per gram of extract (mgEQ/g). 50% of the lethal dose that kills animals (LD50) was determined by acute toxicity in mice. Anti-inflammatory activity was evaluated through carrageenan-induced paw edema, peritonitis, and protein denaturation inhibition. Anti-nociceptive potential was evaluated by acetic acid-induced writhing and formalin tests. Antipyretic activity was assessed by yeast-induced fever. RESULTS: Phytochemical analysis revealed the presence of flavonoids and acid gallic in a quantity of 33.9 mg QE/g. Acute toxicity evaluation resulted in a LD50 of 3807.88 mg/kg. For carrageenan-induced paw edema test, IsAE in both doses (20 and 100 mg/kg) reduced the edema in 83.93%. IsAE reduced nitric oxide (NO) production and leucocytes migration to peritonitis inflammation site and at a concentration of 0.5 mg/mL showed also inhibition of protein denaturation similar to indomethacin in the same concentration. IsAE inhibited in 72.60% the number of contortions in writhing test. In formalin test, IsAE was also efficient, but showed results only in the second phase. In addition, the concentration of 100 mg/kg reduced fever significantly. CONCLUSIONS: IsAE proved to be anti-inflammatory, acting in different parts of the inflammation process, confirming its popular use.


Subject(s)
Anti-Inflammatory Agents/pharmacology , Indigofera/chemistry , Inflammation/drug therapy , Plant Extracts/pharmacology , Analgesics/isolation & purification , Analgesics/pharmacology , Animals , Anti-Inflammatory Agents/isolation & purification , Antipyretics/isolation & purification , Antipyretics/pharmacology , Fever/drug therapy , Indomethacin/pharmacology , Mice , Pain/drug therapy , Peritonitis/drug therapy , Phytochemicals/chemistry , Phytochemicals/pharmacology , Plant Extracts/chemistry , Plant Extracts/toxicity , Plant Leaves , Toxicity Tests, Acute
5.
J Biomol Struct Dyn ; 40(23): 13001-13016, 2022.
Article in English | MEDLINE | ID: mdl-34632943

ABSTRACT

Cutaneous Leishmaniasis (CL) is a neglected disease characterized by highest morbidity rates worldwide. The available treatment for CL has several limitations including serious side effects and resistance to the treatment. Herein we aimed to evaluate the activity of essential oil from the peel of Myrciaria floribunda fruits (MfEO) on Leishmania amazonensis. The cytotoxic potential of MfEO on host mammalian cells was evaluated by MTT. The in vitro leishmanicidal effects of MfEO were investigated on the promastigote and intracellular amastigote forms. The ultrastructural changes induced by MfEO were evaluated by Scanning Electron Microscopy (SEM). The molecular docking of the major compounds δ-Cadinene, γ-Cadinene, γ-Muurolene, α-Selinene, α-Muurolene and (E)-Caryophyllene onto the enzymes trypanothione reductase (TreR) and sterol 14-alpha demethylase (C14DM) were performed. Our results showed that MfEO presented moderate cytotoxicity for Vero cells and macrophages. The MfEO inhibited the growth of promastigote and the survival of intracellular amastigotes, in a dose- and time- dependent way. The MfEO presented high selectivity towards amastigote forms, being 44.1 times more toxic for this form than to macrophages. Molecular docking analysis showed that the major compounds of MfEO interact with Leishmania enzymes and that δ-Cadinene (δ-CAD) presented favorable affinity energy values over TreR and C14DM enzymes, when compared with the other major constituents. Molecular dynamics (MD) simulation studies revealed a stable binding of δ-CAD with lowest binding free energy values in MMGBSA assay. Our results suggested that δ-CAD may be a potent inhibitor of TreR and C14DM enzymes. Communicated by Ramaswamy H. Sarma.


Subject(s)
Antiprotozoal Agents , Leishmania , Oils, Volatile , Animals , Chlorocebus aethiops , Molecular Docking Simulation , Molecular Dynamics Simulation , Oils, Volatile/pharmacology , Oils, Volatile/chemistry , Fruit , Vero Cells , Antiprotozoal Agents/chemistry , Mammals
6.
J Biomol Struct Dyn ; 40(12): 5462-5480, 2022 08.
Article in English | MEDLINE | ID: mdl-33459182

ABSTRACT

In this work we aimed to perform an in silico predictive screening, docking and molecular dynamic study to identify 1,2,3-triazole-phthalimide derivatives as drug candidates against SARS-CoV-2. The in silico prediction of pharmacokinetic and toxicological properties of hundred one 1,2,3-triazole-phtalimide derivatives, obtained from SciFinder® library, were investigated. Compounds that did not show good gastrointestinal absorption, violated the Lipinski's rules, proved to be positive for the AMES test, and showed to be hepatotoxic or immunotoxic in our ADMET analysis, were filtered out of our study. The hit compounds were further subjected to molecular docking on SARS-CoV-2 target proteins. The ADMET analysis revealed that 43 derivatives violated the Lipinski's rules and 51 other compounds showed to be positive for the toxicity test. Seven 1,2,3-triazole-phthalimide derivatives (A7, A8, B05, E35, E38, E39, and E40) were selected for molecular docking and MFCC-ab initio analysis. The results of molecular docking pointed the derivative E40 as a promising compound interacting with multiple target proteins of SARS-CoV-2. The complex E40-Mpro was found to have minimum binding energy of -10.26 kcal/mol and a general energy balance, calculated by the quantum mechanical analysis, of -8.63 eV. MD simulation and MMGBSA calculations confirmed that the derivatives E38 and E40 have high binding energies of -63.47 ± 3 and -63.31 ± 7 kcal/mol against SARS-CoV-2 main protease. In addition, the derivative E40 exhibited excellent interaction values and inhibitory potential against SAR-Cov-2 main protease and viral nucleocapsid proteins, suggesting this derivative as a potent antiviral for the treatment and/or prophylaxis of COVID-19.Communicated by Ramaswamy H. Sarma.


Subject(s)
COVID-19 Drug Treatment , Humans , Molecular Docking Simulation , Molecular Dynamics Simulation , Phthalimides/pharmacology , Protease Inhibitors/chemistry , SARS-CoV-2 , Triazoles/pharmacology
7.
Food Chem ; 337: 127771, 2021 Feb 01.
Article in English | MEDLINE | ID: mdl-32777564

ABSTRACT

Faveleira (Cnidoscolus quercifolius) is an emerging Brazilian plant, with seeds rich in edible oil. This study investigates physicochemical properties, chemical composition, thermal and oxidative stability, in vitro and in vivo toxicity, antioxidant, antinociceptive and anti-inflammatory activities of faveleira seed oil. It was observed that the oil has low acidity, value of peroxide, chlorophyll, carotenoids, ß-carotene and high concentrations of unsaturated fatty acids. In addition to presenting thermal and oxidative stability and high total phenolic content, with vanillin, eugenol and quercetin were predominating. The oil showed no toxicity in vitro and in vivo, and presented antioxidant, anti-inflammatory and antinociceptive activities. These findings provide relevant and appropriate conditions for processing of faveleira seed oil as functional food.


Subject(s)
Euphorbiaceae/metabolism , Plant Oils/chemistry , Analgesics/chemistry , Analgesics/pharmacology , Analgesics/therapeutic use , Animals , Antioxidants/chemistry , Brazil , Carotenoids/analysis , Cell Survival/drug effects , Chlorophyll/analysis , Euphorbiaceae/chemistry , Fatty Acids/analysis , Male , Mice , Pain/chemically induced , Pain/prevention & control , Phenols/analysis , Plant Oils/pharmacology , Plant Oils/therapeutic use , RAW 264.7 Cells , Seeds/chemistry , Seeds/metabolism
8.
J Ethnopharmacol ; 268: 113611, 2021 Mar 25.
Article in English | MEDLINE | ID: mdl-33242623

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Plinia cauliflora (Mart.) Kausel, known in Brazil as jabuticaba or jaboticaba has been used by Brazilian native populations for medicinal purposes, including those related to inflammatory conditions, such as asthma, diarrhea, disorders in female genitourinary tract, and tonsillitis. Inflammation has emerged as a main factor for the oxidative stress, hyperglycemia, and dyslipidemia present in chronic noncommunicable diseases (NCDs). Such disturbances have been a leading cause of death worldwide for decades, despite significant efforts in developing new therapies. Therefore, strengthening the relevance of ethnobotanic approaches, as P. cauliflora has the potential to become a natural, native, and traditional product to prevent and treat inflammation-associated diseases more effectively for more people. AIM OF THE STUDY: Evaluate anti-inflammatory, hypoglycemic, hypolipidemic, and analgesic properties of hydroethanolic extract of P. cauliflora epicarps (PcE). MATERIALS AND METHODS: Phytochemical compound from the PcE were identified through HPLC-DAD-ESI-MSn analysis. Antioxidant activity was determined by measuring 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging. The anti-inflammatory potential was investigated by carrageenan-induced paw edema and peritonitis in mice. Analgesic effect was assessed, in mice, though hot plate test and acetic acid-induced abdominal writhing. Antidiabetic and hypolipidemic potential were evaluated using alloxan-induced diabetic mice. RESULTS: Tannins, phenolic acids, and their derivatives were the predominant phytochemicals found. Overall, PcE showed different properties related to the treatment of clinical conditions associated with chronic diseases as a potent antioxidant activity, demonstrating a radical scavenging action similar to gallic acid. PcE oral administration also significantly reduced inflammation induced by paw edema and partially blocked leukocyte migration. Moreover, PcE produced peripheral and central analgesic effects, as evaluated in the writhing model and hot plate tests. Treatment with PcE significantly improved glucose levels and lipid markers in diabetic mice. CONCLUSIONS: P. cauliflora fruits are rich sources of secondary metabolites, mainly tannins and phenolic acids with high biological potential, which can effectively contribute to the approach of preventing and controlling chronic NCDs.


Subject(s)
Analgesics/therapeutic use , Anti-Inflammatory Agents/therapeutic use , Hypoglycemic Agents/therapeutic use , Hypolipidemic Agents/therapeutic use , Myrtaceae , Plant Extracts/therapeutic use , Analgesics/isolation & purification , Animals , Anti-Inflammatory Agents/isolation & purification , Brazil , Diabetes Mellitus, Experimental/drug therapy , Diabetes Mellitus, Experimental/metabolism , Dose-Response Relationship, Drug , Edema/drug therapy , Edema/metabolism , Female , Hypoglycemic Agents/isolation & purification , Hypolipidemic Agents/isolation & purification , Mice , Plant Extracts/isolation & purification , Random Allocation , Vitis
9.
Bioorg Chem ; 105: 104437, 2020 12.
Article in English | MEDLINE | ID: mdl-33339081

ABSTRACT

Organic compounds obtained by click chemistry reactions have demonstrated a broad spectrum of biological activities being widely applied for the development of molecules against pathogens of medical and veterinary importance. Cutaneous leishmaniasis (CL), caused by intracellular protozoa parasite of genus Leishmania, comprises a complex of clinical manifestations that affect the skin and mucous membranes. The available drugs for the treatment are toxic and costly, with long periods of treatment, and the emergence of resistant strains has been reported. In this study we investigated the in vitro effects of a phthalimide-1,2,3-triazole derivative, the 4-Phenyl-1-[2-(phthalimido-2-yl)ethyl]-1H-1,2,3-triazole (PT4) obtained by click chemistry, on mammalian cells and on L. amazonensis and L. braziliensis, the causative agents of CL in Brazil. In silico ADMET evaluation of PT4 showed that this molecule has good pharmacokinetic properties with no violation of Lipinski's rules. The in vitro assays showed that PT4 was more selective for both Leishmania species than to mammalian cells. This compound also presented low cytotoxicity to mammalian cells with CC50 > 500 µM. Treatment of promastigote forms with different concentrations of PT4 resulted in ultrastructural alterations, such as plasma membrane wrinkling, shortening of cell body, increased cell volume and cell rupture. The molecular dynamic simulations showed that PT4 interacts with Lanosterol 14 α-demethylase from Leishmania, an essential enzyme of lipid synthesis pathway in this parasite. Our results demonstrated PT4 was effective against both species of Leishmania. PT4 caused a decrease of mitochondrial membrane potential and increased production of reactive oxygen species, which may lead to parasite death. Taken together, our results pointed PT4 as promissing therapeutic agent against CL.


Subject(s)
Antiprotozoal Agents/pharmacology , Leishmania/drug effects , Triazoles/pharmacology , Animals , Antiprotozoal Agents/chemical synthesis , Antiprotozoal Agents/chemistry , Cell Survival/drug effects , Cells, Cultured , Dose-Response Relationship, Drug , Macrophages/drug effects , Membrane Potential, Mitochondrial/drug effects , Mice , Mice, Inbred BALB C , Models, Molecular , Molecular Structure , Parasitic Sensitivity Tests , Reactive Oxygen Species/metabolism , Structure-Activity Relationship , Triazoles/chemical synthesis , Triazoles/chemistry
10.
Adv Pharmacol Pharm Sci ; 2020: 1258707, 2020.
Article in English | MEDLINE | ID: mdl-32399519

ABSTRACT

This work evaluated the antioxidant properties and in vivo antinociceptive and anti-inflammatory effects of extracts obtained from fruit peels of Myrciaria floribunda (H. West ex Willd.) O. Berg (Myrtaceae). This plant is popularly known in Brazil as Cambuí or camboim. Different extracts were submitted to comparative analysis to determine the content of selected phytochemical classes (levels of total phenols, flavonoids, and monomeric anthocyanins) and the in vitro antioxidant potentials. The extract with higher potential was selected for in vivo evaluation of its antinociceptive and anti-inflammatory action. Finally, the chemical characterization of this extract was performed by high-performance liquid chromatography (HPLC). MfAE (extract obtained using acetone as solvent) showed the higher levels of phenols (296 mg GAE/g) and anthocyanins contents (35.65 mg Cy-3-glcE/g) that were associated with higher antioxidant activity. MfAE also exhibited in vivo anti-inflammatory and analgesic propertiers. This fraction inhibited the inflammatory and neurogenic phases of pain, and this effect was reversed by naloxone (suggesting the involvement of opioidergic system). MfAE reduced the abdominal contortions induced by acetic acid. The HPLC analysis revealed the presence of gallic acid (and its derivatives) and ellagic acid. Taken together, these data support the use of M. floribunda fruit peels for development of functional foods and nutraceutics.

11.
Pharmaceuticals (Basel) ; 13(3)2020 Mar 16.
Article in English | MEDLINE | ID: mdl-32188166

ABSTRACT

The relevance of oxidative stress in the pathogenesis of several diseases (including inflammatory disorders) has traditionally led to the search for new sources of antioxidant compounds. In this work, we report the selection of fractions with high antioxidant action from B. tetraphylla (BT) leaf extracts. In vitro methods (DPPH and ABTS assays; determination of phenolic and flavonoid contents) were used to select products derived from B. tetraphylla with high antioxidant action. Then, the samples with the highest potentials were evaluated in a model of injury based on the inoculation of a lethal dose of heat-inactivated Escherichia coli in Tenebrio molitor larvae. Due to its higher antioxidant properties, the methanolic extract (BTME) was chosen to be fractionated using Sephadex LH-20 column-based chromatography. Two fractions from BTME (BTFC and BTFD) were the most active fractions. Pre-treatment with these fractions protected larvae of T. molitor from the stress induced by inoculation of heat-inactivated E. coli. Similarly, BTFC and BTFD increased the lifespan of larvae infected with a lethal dose of enteroaggregative E. coli 042. NMR data indicated the presence of aliphatic compounds (terpenes, fatty acids, carbohydrates) and aromatic compounds (phenolic compounds). These findings suggested that products derived from B. tetraphylla leaves are promising candidates for the development of antioxidant and anti-infective agents able to treat oxidative-related dysfunctions.

12.
Nat Prod Res ; : 1-5, 2019 Apr 23.
Article in English | MEDLINE | ID: mdl-31014086

ABSTRACT

This work aimed to investigate the chemical composition, antimicrobial, antinociceptive, acute toxicity and antioxidant activity of the essential oil of Algrizea minor (EOAm). The essential oil presented as the major constituents ß-Pinene (56.99%), α-Pinene (16.57%), Germacrene D (4.67%), Bicyclogermacrene (4.66%), (E)-Caryophyllene (3.76%) and Limonene (1.71%). It was verified that the essential oil did not show acute toxicity in the maximum dose of 5,000 mg/kg. In the evaluation of the antinociceptive activity it was verified that the essential oil reduced in 65.84% the number of writhing in the mice, reducing the pain in 59.17%, and the mechanism of action in pain reduction was opioid, similar to morphine. The essential oil also presented significant antimicrobial against Gram positive and Gram-negative bacteria and fungi, and the antioxidant activity was relevant. Therefore, these results demonstrate the great potential for the future development of pharmaceutical products with the essential oil of Algrizea minor (EOAm).

13.
Data Brief ; 21: 1347-1351, 2018 Dec.
Article in English | MEDLINE | ID: mdl-30456256

ABSTRACT

This text presents complementary data corresponding to schistosomiasis mansoni׳s vector control and toxicity on Schistosoma mansoni cercariae using potassium usnate. This information support our research article "Potassium Usnate Toxicity Against Embryonic Stages of the Snail Biomphalaria glabrata and Schistosoma mansoni Cercariae" [1], and focuses on the analysis of the detailed data regarding the different concentrations of potassium usnate and their efficiency to B. glabrata mortality and non-viability and S. mansoni cercariae mortality etiologic agent of the disease.

14.
Open Microbiol J ; 11: 179-188, 2017.
Article in English | MEDLINE | ID: mdl-29151994

ABSTRACT

INTRODUCTION: In this study, we evaluated the antimicrobial potential of cultivable endophytic fungi associated with Hancornia speciosa Gomes stem bark. METHODS AND MATERIALS: Plant samples were collected in rainy (July 2010) and dry (January 2011) seasons. In total, 116 endophytic fungi strains were isolated from 90 fragments (64.4% frequency of colonization). Higher fungi frequency was observed in the rainy season (84.4%). The strains were grouped into 14 species; the most frequent were Phoma cava (13.8%), Colletotrichum gloeosporioides (12.1%), and Lasiodiplodia theobromae (11.2%). Fungal diversity was similar in both the seasons. Among the 116 strains, 39 (33.6%) showed antimicrobial activity in preliminary screening. The ten most active isolates were subjected to semi-solid fermentation using rice or corn as substrates. Methanolic extracts were obtained from each fermentation medium and the minimum inhibitory (MIC) and minimum microbicide concentrations (MMC) were determined. RESULTS: The best antimicrobial results (MIC < 100 µg/mL) were observed for fungi strains grown in rice medium: Aspergillus niger FHS061 against Proteus mirabilis (MIC = 19 µg/mL) and Staphylococcus aureus (MIC = 39 µg/mL). These strains also showed good results when cultivated in corn medium against P. mirabilis (MIC = 78 µg/mL). CONCLUSION: Thus, the stem bark of H. speciosa harbors diverse endophytic fungi with antimicrobial potential.

15.
Medicines (Basel) ; 4(2)2017 May 03.
Article in English | MEDLINE | ID: mdl-28930242

ABSTRACT

Background: The biotechnological potential of medicinal plants from Brazilian Caatinga and the Atlantic Forest has not been extensively studied. Thus, screening programs are important in prospecting for compounds for developing new drugs. The purpose of this study was to determine the chemical composition and to evaluate the anti-Candida activity of essential oils from leaves of Hymenaea courbaril var. courbaril, Myroxylon peruiferum, and Vismia guianensis. Methods: The oils were extracted through hydrodistillation and their chemical compositions were analyzed by gas chromatography coupled with mass spectrometry. Antifungal activity against C. albicans, C. tropicalis, C. parapsilosis, C. glabrata, and C. krusei was evaluated by determining the minimal inhibitory (MIC) and fungicidal (MFC) concentrations. Results: The major compounds of the oils were caryophyllene oxide and trans-caryophyllene for H. courbaril; spathulenol, α-pinene, and caryophyllene oxide for M. peruiferum; and caryophyllene oxide and humulene epoxide II for V. guianensis oil. The oils showed antifungal activity against all the strains tested, and the MIC values ranged between 0.625 and 1.25 µL/mL and MFC from 0.625 to 2.5 µL/mL. Conclusion: The essential oils from the species studied have the potential to be evaluated as clinical applications in the treatment of candidiasis.

16.
Article in English | MEDLINE | ID: mdl-28367220

ABSTRACT

Lectins are proteins extensively used in biomedical applications with property to recognize carbohydrates through carbohydrate-binding sites, which identify glycans attached to cell surfaces, glycoconjugates, or free sugars, detecting abnormal cells and biomarkers related to diseases. These lectin abilities promoted interesting results in experimental treatments of immunological diseases, wounds, and cancer. Lectins obtained from virus, microorganisms, algae, animals, and plants were reported as modulators and tool markers in vivo and in vitro; these molecules also play a role in the induction of mitosis and immune responses, contributing for resolution of infections and inflammations. Lectins revealed healing effect through induction of reepithelialization and cicatrization of wounds. Some lectins have been efficient agents against virus, fungi, bacteria, and helminths at low concentrations. Lectin-mediated bioadhesion has been an interesting characteristic for development of drug delivery systems. Lectin histochemistry and lectin-based biosensors are useful to detect transformed tissues and biomarkers related to disease occurrence; antitumor lectins reported are promising for cancer therapy. Here, we address lectins from distinct sources with some biological effect and biotechnological potential in the diagnosis and therapeutic of diseases, highlighting many advances in this growing field.

17.
Blood Coagul Fibrinolysis ; 27(2): 210-2, 2016 Mar.
Article in English | MEDLINE | ID: mdl-26397884

ABSTRACT

Portal vein thrombosis is considered a vaso-occlusive process that can appear during the course of hepatosplenic Schistosoma mansoni, but may result from impaired portal blood flow or be associated with acquired or inherited thrombophilic factors. Here, we report the case of a 67-year-old woman who developed thrombocytopenia as a result of hypersplenism. Following the diagnosis of hepatosplenic schistosomiasis, portal vein thrombosis was detected by ultrasound examination, while haematological tests revealed low levels of protein C (43.3%) and high levels of factor VIII (183.1%). The pathogenesis of portal vein thrombosis remains unclear in some patients with S. mansoni. We recommend, therefore, that early clinical and haemostatic investigations are done to evaluate risk of portal vein thrombosis and hence avoid further complications.


Subject(s)
Protein C Deficiency/diagnosis , Schistosomiasis/diagnosis , Splenomegaly/diagnosis , Thrombocytopenia/diagnosis , Venous Thrombosis/diagnosis , Aged , Animals , Factor VIII/metabolism , Female , Gene Expression , Hemostasis , Humans , Liver/metabolism , Liver/parasitology , Liver/pathology , Portal Vein/metabolism , Portal Vein/parasitology , Portal Vein/pathology , Protein C/metabolism , Protein C Deficiency/blood , Protein C Deficiency/complications , Protein C Deficiency/parasitology , Schistosoma mansoni/pathogenicity , Schistosoma mansoni/physiology , Schistosomiasis/blood , Schistosomiasis/complications , Schistosomiasis/parasitology , Spleen/metabolism , Spleen/parasitology , Spleen/pathology , Splenomegaly/blood , Splenomegaly/complications , Splenomegaly/parasitology , Thrombocytopenia/blood , Thrombocytopenia/complications , Thrombocytopenia/parasitology , Venous Thrombosis/blood , Venous Thrombosis/complications , Venous Thrombosis/parasitology
18.
Rev. paul. pediatr ; 33(3): 318-325, jul.-set. 2015. tab, ilus
Article in Portuguese | LILACS | ID: lil-761154

ABSTRACT

Objetivo:Determinar a prevalência de excesso de peso e analisar o consumo alimentar de risco e proteção para doenças cardiovasculares em adolescentes escolares da cidade de Vitória de Santo Antão, Pernambuco, Brasil.Métodos:Estudo transversal com adolescentes de ambos os sexos entre 10 e 19 anos, matriculados em 39 escolas públicas e privadas de Vitória de Santo Antão (PE). Foram obtidas variáveis sociodemográficas, antropométricas e do estilo de vida. O consumo alimentar foi avaliado por meio de questionário de frequência alimentar e posteriormente convertido em escores de padrão de consumo mensal. Obtiveram-se a distribuição de consumo para um grupo de alimentos associados ao risco de desenvolvimento de doenças cardiovasculares (Grupo Risco) e um grupo de alimentos protetores (Grupo Proteção). O nível de significância usado na decisão dos testes estatísticos foi de 5%.Resultados:A amostra foi constituída por 2.866 escolares; 54,2% do sexo feminino, com idade mediana de 14 anos (Intervalo Interquartílico = 12-16). A análise dos escores de consumo alimentar mostrou maior dispersão no grupo de alimentos protetores (51,1%) e maiores medianas de consumo de alimentos de risco nos adolescentes com mães de escolaridade >9 anos (p<0,001).Conclusões:O excesso de peso foi frequente nos adolescentes estudados. Os escores de consumo alimentar do grupo risco revelaram associação apenas com a escolaridade materna e evidenciaram a necessidade de maior conhecimento de educação nutricional as famílias, independentemente das condições socioeconômicas.


Objective:The aim of the present study was to determine the prevalence of excess weight and analyze eating habits in relation to cardiovascular disease in adolescents from the city of Vitória de Santo Antão, state of Pernambuco, northeast Brazil.Methods:A cross-sectional study was carried out with male and female students (10-19 years old) enrolled at public and private schools in Vitória de Santo Antão. Sociodemographic, anthropometric and lifestyle variables were collected. Food consumption was evaluated using a Food Frequency Questionnaire and subsequently converted to monthly intake pattern scores, obtaining the intake distribution for a group of foods associated with the risk of developing cardiovascular disease and for a group of protective foods. The significance level for the statistical tests was set at 5.0%.Results:The sample consisted of 2866 students. The female gender accounted for 54.2% of the sample, and median age was 14 years (interquartile range: 12-16 years). The food intake scores showed greater dispersion in the group of protective foods (51.1%). Higher median scores for consumption of risk foods were found among adolescents whose mothers had more than 9 years of schooling (p<0.001).Conclusions:Excess weight was prevalent among the students analyzed. The consumption of risk foods was only associated with maternal schooling, which shows the need for nutritional interventions directed at families, regardless of socioeconomic status.


Subject(s)
Humans , Male , Female , Adolescent , Eating , Cardiovascular Diseases , Overweight/epidemiology
19.
PLoS One ; 10(8): e0135370, 2015.
Article in English | MEDLINE | ID: mdl-26267788

ABSTRACT

BACKGROUND: Schistosomiasis mansoni is a chronic liver disease, in which some patients (5-10%) progress to the most severe form, hepatosplenic schistosomiasis. This form is associated with portal hypertension and splenomegaly, and often episodes of gastrointestinal bleeding, even with liver function preserved. Splenectomy is a validated procedure to reduce portal hypertension following digestive bleeding. Here, we evaluate beneficial effects of splenectomy on blood coagulation factors and liver function tests in hepatosplenic schistosomiasis mansoni compared to non-operated patients. METHODOLOGY/PRINCIPAL FINDINGS: Forty-five patients who had undergone splenectomy surgery were assessed by laboratory analyses and ultrasound examination and compared to a non-operated group (n = 55). Blood samples were obtained for liver function tests, platelet count and prothrombin time. Coagulation factors (II, VII, VIII, IX and X), protein C and antithrombin IIa, plasminogen activator inhibitor-1 were measured by routine photometric, chromogenic or enzyme-linked immunosorbent assays, while hyperfibrinolysis was defined by plasminogen activator inhibitor-1 levels. Both groups had similar age, gender and pattern of periportal fibrosis. Splenectomized patients showed significant reductions in portal vein diameter, alkaline phosphatase and bilirubin levels compared to non-operated patients, while for coagulation factors there were significant improvement in prothrombin, partial thromboplastin times and higher levels of factor VII, VIII, IX, X, protein C and plasminogen activator inhibitor-1. CONCLUSION/SIGNIFICANCE: This study shows that the decrease of flow pressure in portal circulation after splenectomy restores the capacity of hepatocyte synthesis, especially on the factor VII and protein C levels, and these findings suggest that portal hypertension in patients with hepatosplenic schistosomiasis influences liver functioning and the blood coagulation status.


Subject(s)
Hemostasis , Liver/metabolism , Schistosomiasis mansoni/surgery , Splenectomy , Alkaline Phosphatase/blood , Bilirubin/blood , Female , Humans , Liver/diagnostic imaging , Liver/physiology , Male , Middle Aged , Plasminogen Activator Inhibitor 1/metabolism , Protein C/metabolism , Prothrombin/metabolism , Ultrasonography
20.
Front Microbiol ; 6: 350, 2015.
Article in English | MEDLINE | ID: mdl-25999918

ABSTRACT

Endophytic fungi were isolated from healthy leaves of Indigofera suffruticosa Miller, a medicinal plant found in Brazil which is used in folk medicine to treat various diseases. Among 65 endophytic fungi isolated, 18 fungi showed activity against at least one tested microorganism in preliminary screening, and the best results were obtained with Nigrospora sphaerica (URM-6060) and Pestalotiopsis maculans (URM-6061). After fermentation in liquid media and in semisolid media, only N. sphaerica demonstrated antibacterial activity (in Potato Dextrose Broth-PDB and in semisolid rice culture medium). In the next step, a methanolic extract from rice culture medium (NsME) and an ethyl acetate extract (NsEAE) from the supernatant of PDB were prepared and both exhibited antimicrobial activity against Gram-negative and Gram-positive bacteria. The best result was observed against Staphylococcus aureus, with minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values of 1.56 mg/mL and 6.25 mg/mL, respectively, for NsME and MIC and MBC values of 0.39 mg/mL and 3.12 mg/mL, respectively, for NsEAE. This study is the first report about the antimicrobial activity of endophytic fungi residing in I. suffruticosa leaves, in which the fungus N. sphaerica demonstrated the ability to produce bioactive agents with pharmaceutical potential, and may provide a new lead in the pursuit of new biological sources of drug candidates.

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