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1.
Neurochem Int ; 175: 105706, 2024 May.
Artículo en Inglés | MEDLINE | ID: mdl-38423391

RESUMEN

Alcohol use disorder (AUD) is characterized by a set of behavioral, cognitive, nutritional, and physiological phenomena derived from the uncontrolled use of alcoholic beverages. There are cases in which AUD is associated with anxiety disorder, and when untreated, it requires careful pharmacotherapy. Blue Calm® (BC) is a food supplement indicated to aid restorative sleep, which has traces of medicinal plant extracts, as well as myo-inositol, magnesium bisglycinate, taurine, and L-tryptophan as its main chemical constituents. In this context, this study aimed to evaluate the potential of the BC in the treatment alcohol withdrawal-induced anxiety in adult zebrafish (aZF). Initially, BC was submitted to antioxidant activity against 2,2-diphenyl-1-picrylhydrazyl radical. Subsequently, the aZF (n = 6/group) were treated with BC (0.1 or 1 or 10 mg/mL; 20 µL; p.o.), and the sedative effect and acute toxicity (96 h) were evaluated. Then, the anxiolytic-like effect and the possible GABAergic mechanism were analyzed through the Light & Dark Test. Finally, BC action was evaluated for treating alcohol withdrawal-induced anxiety in aZF. Molecular docking was performed to evaluate the interaction of the major chemical constituents of BC with the GABAA receptor. BC showed antioxidant potential, a sedative effect, was not toxic, and all doses of BC had an anxiolytic-like effect and showed potential for the treatment of alcohol withdrawal-induced anxiety in aZF. In addition to the anxiolytic action, the main chemical constituents of BC were confirmed in the molecular docking, thus suggesting that BC is an anxiolytic that modulates the GABAergic system and has pharmacological potential for the treatment of alcohol withdrawal-induced anxiety.


Asunto(s)
Alcoholismo , Ansiolíticos , Síndrome de Abstinencia a Sustancias , Animales , Pez Cebra/fisiología , Ansiolíticos/farmacología , Ansiolíticos/uso terapéutico , Ansiedad/inducido químicamente , Ansiedad/tratamiento farmacológico , Ansiedad/psicología , Alcoholismo/tratamiento farmacológico , Simulación del Acoplamiento Molecular , Síndrome de Abstinencia a Sustancias/tratamiento farmacológico , Receptores de GABA-A , Antioxidantes/farmacología , Antioxidantes/uso terapéutico , Trastornos de Ansiedad/tratamiento farmacológico , Suplementos Dietéticos , Hipnóticos y Sedantes
2.
J Ethnopharmacol ; 321: 117506, 2024 Mar 01.
Artículo en Inglés | MEDLINE | ID: mdl-38012976

RESUMEN

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.


Asunto(s)
Apocynaceae , Candidiasis , Enfermedades Transmisibles , Antifúngicos/farmacología , Antifúngicos/química , Candida , Fluconazol/farmacología , Virulencia , Cromatografía Liquida , Apocynaceae/química , Corteza de la Planta/química , Antocianinas/farmacología , Extractos Vegetales/farmacología , Extractos Vegetales/química , Espectrometría de Masas en Tándem , Candida albicans , Fitoquímicos/análisis , Pruebas de Sensibilidad Microbiana
3.
Molecules ; 28(15)2023 Jul 26.
Artículo en Inglés | MEDLINE | ID: mdl-37570622

RESUMEN

The use of medicinal plants to treat inflammatory conditions and painful processes has attracted the attention of scientists and health professionals due to the evidence that natural products can promote significant therapeutic benefits associated with fewer adverse effects compared to conventional anti-inflammatory drugs. The genus Plectranthus is composed of various plants with pharmacological potential, which are used to treat various diseases in traditional communities worldwide. The present study systematically reviewed Plectranthus species with anti-inflammatory and analgesic potential. To this end, a systematic review was conducted following the Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) protocol. The search was conducted on the following databases: PubMed, ScienceDirect, SciVerse Scopus, and Web of Science. Different combinations of search terms were used to ensure more excellent article coverage. After the selection, a total of 45 articles were included in this review. This study identified twelve Plectranthus species indicated for the treatment of different inflammatory conditions, such as wounds, fever, bronchitis, abscess, asthma, hepatitis, labyrinthitis, tonsillitis, and uterine inflammation. The indications for pain conditions included headache, sore throat, heartburn, menstrual cramp, colic, toothache, stomachache, migraine, chest pain, abdominal pain, local pain, labor pain, and recurring pain. Among the listed species, ten plants were found to be used according to traditional knowledge, although only four of them have been experimentally studied. When assessing the methodological quality of preclinical in vivo assays, most items presented a risk of bias. The SR results revealed the existence of different Plectranthus species used to treat inflammation and pain. The results of this systematic review indicate that Plectranthus species have the potential to be used in the treatment of diseases with an inflammatory component, as well as in the management of pain. However, given the risk of biases, the experimental analysis of these species through preclinical testing is crucial for their safe and effective use.


Asunto(s)
Fitoterapia , Plectranthus , Femenino , Embarazo , Humanos , Etnofarmacología , Dolor Abdominal , Analgésicos/farmacología , Analgésicos/uso terapéutico , Antiinflamatorios/farmacología , Antiinflamatorios/uso terapéutico , Inflamación , Fitoquímicos
4.
Biomed Pharmacother ; 166: 115249, 2023 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-37597323

RESUMEN

Edema is one of the obvious indicators of inflammation and a crucial factor to take into account when assessing a substance's capacity to reduce inflammation. We aimed to evaluate the antiedematogenic and anti-inflammatory profile of the hydroethanolic barks extract of Ximenia americana (HEXA). The possible antiedematogenic and anti-inflammatory effect of EHXA (50, 100 mg/kg and 250 mg/kg v.o) was evaluated using the paw edema induced by carrageenan, zymosan, dextran, CFA and by different agents inflammatory (serotonin, histamine, arachidonic acid and PGE2), and pleurisy model induced by carrageenan and its action on IL-1ß and TNF-α levels was also evaluated. HEXA demonstrated a significant antiedematogenic effect at concentrations of 50, 100 and 250 mg/kg on paw edema induced by carrageenan, zymosan and dextran. However, the concentration of 50 mg/kg as standard, demonstrating the effect in the subchronic model, induced CFA with inhibition of 59.06 %. In models of histamine-induced paw edema, HEXA showed inhibition of - 30 min: 40.49 %, 60 min: 44.70 % and 90 min: 48.98 %; serotonin inhibition - 30 min: 57.09 %, 60 min: 66.04 % and 90 min: 61.79 %; arachidonic acid inhibition - 15 min: 36.54 %, 30 min: 51.10 %, 45 min: 50.32 % and 60 min: 76.17 %; and PGE2 inhibition - 15 min: 67.78 %, 30 min: 62.30 %, 45 min: 54.25 % and 60 min: 47.92 %. HEXA significantly reduced (p < 0.01) leukocyte migration in the pleurisy model and reduced TNF-α and IL-1ß levels in pleural lavage (p < 0.0001). The results showed that HEXA has the potential to have an antiedematogenic impact in both acute and chronic inflammation processes, with a putative mode of action including the suppression or regulation of inflammatory mediators.


Asunto(s)
Olacaceae , Pleuresia , Ácido Araquidónico , Carragenina , Dextranos , Histamina , Corteza de la Planta , Serotonina , Factor de Necrosis Tumoral alfa , Zimosan , Inflamación/inducido químicamente , Inflamación/tratamiento farmacológico , Antiinflamatorios/farmacología , Antiinflamatorios/uso terapéutico , Pleuresia/inducido químicamente , Pleuresia/tratamiento farmacológico , Dinoprostona , Modelos Teóricos , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico
5.
Curr Microbiol ; 80(8): 251, 2023 Jun 23.
Artículo en Inglés | MEDLINE | ID: mdl-37351656

RESUMEN

The high incidence of Candida albicans infections has raised concerns regarding side effects and drug resistance, compounded by a limited number of alternative drugs. Silver nanoparticles (AgNPs) have prominent antimicrobial activity, but effective administration remains a challenge. In this study, AgNPs were synthesized via a green chemistry approach, using glucose as a reducing agent, and incorporated into an agar matrix to form a film (AgFilm). The AgNPs and AgFilm were characterized by Ultraviolet-visible (UV-vis) spectroscopy, Fourier transform infrared (FTIR) spectroscopy, dynamic light scattering (DLS), powder X-ray diffraction (PXRD), scanning electron microscopy (SEM), and atomic force microscopic (AFM). The UV-Vis spectra of the AgNPs and AgFilm showed bands at 415 and 413 nm, respectively. The PXRD and UV-Vis data suggest that the growth of AgNPs was effectively inhibited in the AgFilm. The diameter of AgNPs dispersed in AgFilm was 76 ± 42 nm, and the thickness of the film and 35 ± 3 µm. The antifungal activity of AgFilm was evaluated against 20 strains of C. albicans, demonstrating high antifungal activity with an inhibition zone of 19 ± 2 mm. Therefore, AgFilm could be a promising option for the treatment of superficial C. albicans infections.


Asunto(s)
Antifúngicos , Nanopartículas del Metal , Antifúngicos/farmacología , Plata/farmacología , Nanopartículas del Metal/química , Microscopía Electrónica de Rastreo , Extractos Vegetales/química , Espectroscopía Infrarroja por Transformada de Fourier , Antibacterianos/farmacología
6.
Microb Pathog ; 180: 106147, 2023 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-37169312

RESUMEN

This study aimed to evaluate the antibiotic effects of the fixed oils of Acrocomia aculeata (FOAA) and Syagrus cearenses (FOSC) against the bacterial strains and the fungi strains of the genus Candida spp. The method of serial microdilution using different concentrations was used for measuring the individual biological activity of the fixed oils. The fixed oil of A. aculeata showed the presence of oleic acid (24.36%), while the oil of S. cearensis displayed the content of myristic acid (18.29%), compounds detected in high concentration. The combination FOAA + Norfloxacin, and FOSC + Norfloxacin showed antibacterial activity against E. coli and S. aureus strains, demonstrating possible synergism and potentiation of the antibiotic action against multidrug-resistant strains. The combination FOAA + Fluconazole displayed a significant effect against Candida albicans (IC50 = 15.54), C. krusei (IC50 = 78.58), and C. tropicalis (IC50 = 1588 µg/mL). Regarding FOSC + Fluconazole, it was also observed their combined effect against the strains of C. albicans (IC50 = 3385 µg/mL), C. krusei (IC50 = 26.67 µg/mL), and C. tropicalis (IC50 = 1164 µg/mL). The findings of this study showed a significant synergism for both fixed oils tested when combined with the antibiotic.


Asunto(s)
Antiinfecciosos , Arecaceae , Fluconazol/farmacología , Arecaceae/química , Norfloxacino/farmacología , Escherichia coli , Staphylococcus aureus , Antiinfecciosos/farmacología , Antiinfecciosos/química , Candida albicans , Aceites de Plantas/farmacología , Antibacterianos/farmacología , Candida tropicalis , Pruebas de Sensibilidad Microbiana , Antifúngicos/farmacología , Antifúngicos/química
7.
Curr Res Toxicol ; 4: 100103, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-36970244

RESUMEN

Medicinal plants have been used for many years by communities to treat illnesses. The need for scientific proof of these vegetable's curative effects is as necessary as the proof of the inexistence of toxicity related to the use of extracts with therapeutic potential. Annona squamosa L. (Annonaceae), popularly known as "pinha", "ata" or "fruta do conde", has been used in traditional medicine for its analgesic and antitumor activities. The toxic effects attributed to this plant have also been explored as a pesticide and an insecticide. The aim of the present study was to investigate the toxicity of the methanolic extract of A. squamosa seeds and pulp against human erythrocytes. Blood samples were treated with methanolic extract at different concentrations, osmotic fragility was determined using saline tension assays and morphological analyzes were performed using optical microscopy. The extracts were analyzed using high performance liquid chromatography with diode array detection (HPLC-DAD) for phenolic quantification. The seed's methanolic extract showed toxicity above 50% from a concentration of 100 µg/mL, while also presenting echinocytes in the morphological analysis. The pulp's methanolic extract did not show toxicity to red blood cells or morphological changes at the concentrations tested. HPLC-DAD analysis revealed the presence of caffeic acid in the seed extract and gallic acid in the pulp extract. The seed's methanolic extract is toxic and the pulp's methanolic extract showed no toxicity against human erythrocytes.

8.
J Microbiol Immunol Infect ; 56(1): 150-162, 2023 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-35864068

RESUMEN

BACKGROUND: Trichomonas vaginalis, a parasitic flagellated protozoan, is one of the main non-viral sexually transmitted diseases worldwide. Treatment options for trichomoniasis are limited to nitroimidazole compounds. However, resistance to these drugs has been reported, which requires the development of new anti-Trichomonas agents that confer suitable efficacy and less toxicity. METHODS: In the present work, we assessed the effectiveness of the liposomal system containing essential oils of Bunium persicum and Trachyspermum ammi against T. vaginalis in vitro. The chemical composition of B. persicum and T. ammi were analyzed using gas chromatography-mass spectrometry (GC-MS). Liposomal vesicles were prepared with phosphatidylcholine) 70%) and cholesterol)30%) using the thin-film method. The essential oils of B. persicum and T. ammi were loaded into the liposomes using the inactive loading method. Liposomal vesicles were made for two plants separately. Their physicochemical features were tested using Zeta-Sizer, AFM and SEM. The anti-Trichomonas activity was determined after 12 and 24 h of parasite cultures in TYI-S-33 medium. RESULTS: After 12 and 24 h of administration, the IC50 of the B. persicum essential oil nano-liposomes induced 14.41 µg/mL and 45.19 µg/mL, respectively. The IC50 of T. ammi essential oil nano-liposomes induced 8.08 µg/mL and 25.81 µg/mL, respectively. CONCLUSIONS: These data suggested that nano-liposomes of the essential oils of B. persicum and T. ammi may be a promising alternative to current treatments for Trichomonas infection.


Asunto(s)
Ammi , Apiaceae , Aceites Volátiles , Humanos , Aceites Volátiles/farmacología , Aceites Volátiles/química , Apiaceae/química , Extractos Vegetales
9.
Fundam Clin Pharmacol ; 37(2): 316-323, 2023 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-36205463

RESUMEN

The problem of antibiotic resistance by bacteria threatens human health. Therefore, studies in this area seek alternatives to circumvent it. The study with coumarins and eugenol has already proven that these classes of compounds act against bacteria. In this same aspect, exposure to LED also shows a bactericidal effect. Seeking a possible enhancement of this effect, the present work studied coumarins derived from eugenol in association with LED to investigate the bactericidal effect. Four compounds were tested. For this, minimum inhibitory concentrations (MICs) and modulation with three antibiotics against Escherichia coli and Staphylococcus aureus bacteria were determined. To test the behavior of the activity against exposure to LED, the plates were exposed for 20 min to blue light, 415 nm and then incubated at 37°C for 24 h. For control, duplicates were made, and one of them did not undergo this exposure. C1 exhibited better activity against S. aureus, as synergism prevailed under the conditions tested. C3 and C4 were promising against E. coli as they showed synergism in association with the three antibiotics both with and without LED exposure. Thus, the compounds showed bactericidal activity, and LED was shown to enhance synergism.


Asunto(s)
Eugenol , Staphylococcus aureus , Humanos , Eugenol/farmacología , Escherichia coli , Antibacterianos/farmacología , Pruebas de Sensibilidad Microbiana , Cumarinas/farmacología
10.
Life Sci ; 309: 121044, 2022 Nov 15.
Artículo en Inglés | MEDLINE | ID: mdl-36208657

RESUMEN

The present study attempted to scrutinize the protective effect of the methanolic extract of P. chaba stem bark against paracetamol-induced hepatotoxicity in Sprague-Dawley rats, along with the gas chromatography-mass spectrometry (GC-MS) analysis to identify phytochemicals, which were further docked in the catalytic site of CYP2E1 and the MD simulation for system that plays a major role in the bio-activation of toxic substances that produce reactive metabolites, leading to hepatotoxicity. P. chaba stem methanol extract (250 and 500 mg/kg) were treated orally with the negative control and the negative control silymarin (50 mg/kg) groups. Phytochemical profiling was conducted using GC-MS. In in-silico studies, PyRx software was used for docking analysis and the stability of the binding mode in the target active sites was evaluated through a set of standard MD-simulation protocols using the Charmm 27 force field and Swiss PARAM. Co-administration of P. chaba at both doses with APAP significantly reduced the APAP-augmented liver marker enzymes ALT, AST, ALP, and LDH, along with serum albumin, globulin, hepatic enzymes, histopathological architecture, lipid profiles, total protein, and total bilirubin, and elevated the levels of MDA. The GC-MS analysis indicated that P. chaba extract is enriched in fatty acid methyl esters (46.23 %) and alkaloids (10.91 %) and piperine is represented as a main phytochemical. Among all the identified phytochemicals, piperine (-8.0 kcal/mol) was found to be more interacting and stable with the binding site of CYP2E1. Therefore, all of our findings may conclude that the P. chaba stem extract and its main compound, piperine, are able to neutralize APAP-induced hepatic damage.


Asunto(s)
Alcaloides , Enfermedad Hepática Inducida por Sustancias y Drogas , Piper , Silimarina , Ratas , Animales , Acetaminofén/toxicidad , Ratas Sprague-Dawley , Citocromo P-450 CYP2E1 , Cromatografía de Gases y Espectrometría de Masas , Enfermedad Hepática Inducida por Sustancias y Drogas/patología , Metanol/farmacología , Corteza de la Planta , Extractos Vegetales/uso terapéutico , Hígado , Alcaloides/farmacología , Silimarina/farmacología , Bilirrubina , Lípidos/farmacología , Ácidos Grasos , Albúmina Sérica , Ésteres/farmacología
11.
Microb Pathog ; 173(Pt A): 105827, 2022 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-36243385

RESUMEN

Eugenol has already had its pharmacological properties elucidated in previous studies, including antibacterial and antifungal properties. Based on such information, this study aimed to evaluate the antibacterial and modulatory activity of coumarin compounds prepared from dihydroeugenol and to associate them with blue LED light for the same activity. For this study, five of the substances available: compound 1 (C1), 8-methoxy-2-oxo-6-propyl-2H-chromen-3-carboxylic acid, compound (C2), 3-(hydroxy(4-nitrophenyl)methyl)-8- methoxy-6-propyl-2H-chromen-2-one, compound 7 (C3), 8-hydroxy-3-(4-nitrobenzoyl)-6-propyl-2H-chromen-2-one, compound 8 (C4), 3-(4-aminobenzoyl)-8-methoxy-6-propyl-2H-chromen-2-one and Compound 9 (C5), 8-methoxy-3-(4-nitrobenzoyl)-6-propyl-2H-chromen-2-one 2-one. To determine the MIC, the broth microdilution technique was used. The products were evaluated for their potential to modulate the activity of antibiotics. Afterward, the plates were submitted to blue LED light for 20 min. When exposed to LED, C3 exhibited a decrease in MIC for SA ATCC and C5 for EC ATCC, with an average of 645.08 µg/mL for both cases. C2 and C4 exhibited synergism in a greater number of situations. However, C3 showed promising activity against S. aureus. C1 and C2 already acted better against E. coli, with the difference that C1 acted better against these bacteria when associated with LED. In general, the compounds studied here exhibited good antibacterial activity when associated with LED.


Asunto(s)
Escherichia coli , Staphylococcus aureus , Antibacterianos/farmacología , Bacterias , Luz , Pruebas de Sensibilidad Microbiana
12.
Molecules ; 27(18)2022 Sep 12.
Artículo en Inglés | MEDLINE | ID: mdl-36144652

RESUMEN

The inappropriate use of synthetic antibiotics has become a global public health problem. Therefore, the study of new alternatives for the treatment of infectious diseases is relevant and natural bioactive products are on the rise. This study conducted a scientific prospection of bioactive natural products with promising applications in the chemical control of microorganisms. A systematic review of the most recent articles was performed according to the following three steps: (i) eligibility assessment, (ii) screening, and (iii) inclusion of articles and information extraction. There has been an increase in the number of scientific publications on bioactive natural products for microbial control in the CAPES and SciELO databases (2001-2021). Seventeen relevant articles were included, most of which focused on extracts. Ascorbic acid, chlorogenic acid, chrysin, and quercetin were the most cited compounds. Natural products were shown to be effective in inhibiting more than 30 microorganisms. A discussion was presented on the research trends.


Asunto(s)
Productos Biológicos , Antibacterianos/farmacología , Productos Biológicos/química , Productos Biológicos/farmacología , Ácido Clorogénico , Extractos Vegetales/química , Quercetina
13.
Artículo en Inglés | MEDLINE | ID: mdl-35620400

RESUMEN

Background: Diabetes is a metabolic disease linked to multiple comorbidities, such as low-grade inflammation. ß-pinene, a monoterpene commonly found in aromatic plants, is endowed with anti-inflammatory effect and this fact lead us to investigate the possible hypoglycemic, hypolipidemic and anti-inflammatory effects of the monoterpene in the alloxan-induced diabetes experimental model. Methods: Male Wistar rats (200-250 g) were treated orally with ß-pinene (25, 50, 100, and 200 mg/kg) or glibenclamide (5 mg/kg), for seven consecutive days. Diabetes was induced by alloxan (40 mg/kg) through the penile vein. On the seventh day of treatment, blood samples were collected for biochemical analysis. The anti-inflammatory effect of ß-pinene was evaluated using the carrageenan-induced paw edema model, followed by the carrageenan-induced peritonitis. Results: The treatment with ß-pinene decreased plasma glucose, triglyceride, VLDL, LDL, and HDL levels, when compared to those of the control group. In addition, the association ß-pinene 10 mg/kg + glibenclamide 2 mg/kg significantly decreased blood glucose, total cholesterol, and triglyceride level. Finally, oral treatment with ß-pinene reduced carrageenan-induced paw edema and leukocyte migration in the peritoneum. Taken together, our results indicate that ß-pinene shows hypoglycemic and hypolipemic effects, which may involve some common mechanisms of glibenclamide. Besides, the monoterpene presented an anti-inflammatory action in diabetic rats that needs further investigation in order to clarify such effect and its correlation with the alterations observed in plasma parameters of ß-pinene-treated diabetic rats.

14.
Molecules ; 27(9)2022 Apr 25.
Artículo en Inglés | MEDLINE | ID: mdl-35566105

RESUMEN

Cymbopogon winterianus, known as "citronella grass", is an important aromatic and medicinal tropical herbaceous plant. The essential oil of C. winterianus (EOCw) is popularly used to play an important role in improving human health due to its potential as a bioactive component. The present study aimed to identify the components of the essential oil of C. winterianus and verify its leishmanicidal and trypanocidal potential, as well as the cytotoxicity in mammalian cells, in vitro. The EOCw had geraniol (42.13%), citronellal (17.31%), and citronellol (16.91%) as major constituents. The essential oil only exhibited significant cytotoxicity in mammalian fibroblasts at concentrations greater than 250 µg/mL, while regarding antipromastigote and antiepimastigote activities, they presented values considered clinically relevant, since both had LC50 < 62.5 µg/mL. It can be concluded that this is a pioneer study on the potential of the essential oil of C. winterianus and its use against the parasites T. cruzi and L. brasiliensis, and its importance is also based on this fact. Additionally, according to the results, C. winterianus was effective in presenting values of clinical relevance and low toxicity and, therefore, an indicator of popular use.


Asunto(s)
Antiinfecciosos , Cymbopogon , Aceites Volátiles , Plantas Medicinales , Animales , Antiparasitarios/farmacología , Cromatografía de Gases , Cymbopogon/química , Humanos , Mamíferos , Aceites Volátiles/química , Aceites Volátiles/farmacología
15.
Molecules ; 27(7)2022 Mar 27.
Artículo en Inglés | MEDLINE | ID: mdl-35408565

RESUMEN

Weeds are an important source of natural products; with promising biological activity. This study investigated the anti-kinetoplastida potential (in vitro) to evaluate the cytotoxicity (in vitro) and antioxidant capacity of the essential oil of Rhaphiodon echinus (EORe), which is an infesting plant species. The essential oil was analyzed by GC/MS. The antioxidant capacity was evaluated by reduction of the DPPH radical and Fe3+ ion. The clone Trypanosoma cruzi CL-B5 was used to search for anti-epimastigote activity. Antileishmanial activity was determined using promastigotes of Leishmania braziliensis (MHOM/CW/88/UA301). NCTC 929 fibroblasts were used for the cytotoxicity test. The results showed that the main constituent of the essential oil was γ-elemene. No relevant effect was observed concerning the ability to reduce the DPPH radical; only at the concentration of 480 µg/mL did the essential oil demonstrate a high reduction of Fe3+ power. The oil was active against L. brasiliensis promastigotes; but not against the epimastigote form of T. cruzi. Cytotoxicity for mammalian cells was low at the active concentration capable of killing more than 70% of promastigote forms. The results revealed that the essential oil of R. echinus showed activity against L. brasiliensis; positioning itself as a promising agent for antileishmanial therapies.


Asunto(s)
Antiprotozoarios , Enfermedad de Chagas , Lamiaceae , Leishmaniasis Mucocutánea , Aceites Volátiles , Trypanosoma cruzi , Animales , Antioxidantes/farmacología , Antiprotozoarios/farmacología , Enfermedad de Chagas/tratamiento farmacológico , Mamíferos , Aceites Volátiles/farmacología
16.
Biomed Pharmacother ; 150: 112938, 2022 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-35413602

RESUMEN

Osteoarthritis (OA) is a degenerative joint disease that occurs when there is a change in the mechanical and biological properties of the articular cartilage and the subchondral bone; The condition is more prevalent in women than in men. Pequi oil (PO), which is extracted from the fruits of the pequi tree (Caryocar coriaceum Wittm), is widely used in traditional medicine in the Brazilian northeast for the management of inflammation and joint pain. The aim of this study was to develop a pharmaceutical formulation containing Carbopol® hydrogel nanoencapsulated with pequi pulp fixed oil (PeONC) and evaluate its therapeutic effect on functionality and pain in women with knee osteoarthritis. The study was divided into two stages: Stage 1 - preparation and physico-chemical characterization of the pharmaceutical formulation containing PeONC, cell viability assays and skin irritability testing. Step 2 - A double-blind randomized clinical trial evaluating knee symptoms, quality of life, pressure pain, function, muscle strength and range of motion. The nanoformulation was in a gel form, with a particle size of 209.5 ± 1.06 nm, a pH of 6.23 ± 0.45, a zeta potential of - 23.1 ± 0.4 mV, a polydispersity index of 0.137 ± 0.52, and containing nanocapsules with a spherical shape a polymeric wall and an oily nucleus. The gel showed no cytotoxicity and was not irritating to human skin. The treatment with PeONC increased the strength of the knee flexor and extensor muscles and the total motion range of the knee. In addition, the treatment reduced knee instability, pain, swelling, and locking; There was also an improvement in some items of the SF-36 quality of life questionnaire such as in respect of functional capacity and social aspects. In conclusion, PeONC was found to be a stable, safe formulation with no toxicity in respect of topical use in humans. Additionally, the treatment produced an increase in muscle strength and functionality that was associated with reduced knee symptoms and improved quality of life. Our findings showed that in a group of women treated with PeONC mitigated the symptoms of knee osteoarthritis.


Asunto(s)
Ericales , Malpighiales , Osteoartritis de la Rodilla , Femenino , Humanos , Masculino , Osteoartritis de la Rodilla/tratamiento farmacológico , Dolor/tratamiento farmacológico , Aceites de Plantas/farmacología , Aceites de Plantas/uso terapéutico , Calidad de Vida
17.
Pharmaceutics ; 14(4)2022 Mar 24.
Artículo en Inglés | MEDLINE | ID: mdl-35456532

RESUMEN

(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.

18.
3 Biotech ; 12(3): 61, 2022 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-35186658

RESUMEN

Spondias mombin is used in the folk medicine for the treatment of diarrhea and dysentery, indicating that extracts obtained from this species may present pharmacological activities against pathogenic microorganisms. The purpose of this work was to investigate the chemical composition and evaluate the antimicrobial activity of extracts obtained from the leaves (aqueous) and bark (hydroethanolic) of S. mombin both as single treatments and in combination with conventional drugs. Following a qualitative chemical prospection, the extracts were analyzed by HPLC-DAD. The antimicrobial activities were evaluated by microdilution. The combined activity of drugs and extracts was verified by adding a subinhibitory concentration of the extract in the presence of variable drug concentrations. The Minimum Fungicidal Concentration (MFC) was determined by a subculture of the microdilution test, while the effect of the in vitro treatments on morphological transition was analyzed by subculture in moist chambers. While the qualitative analysis detected the presence of phenols and flavonoids, the HPLC analysis identified quercetin, caffeic acid, and catechin as major components in the leaf extract, whereas kaempferol and quercetin were found as major compounds in the bark extract. The extracts showed effective antibacterial activities only against the Gram-negative strains. With regard to the combined activity, the leaf extract potentiated the action of gentamicin and imipenem (against Staphylococcus aureus), while the bark extract potentiated the effect of norfloxacin (against S. aureus), imipenem (against Escherichia coli), and norfloxacin (against Pseudomonas aeruginosa). A more significant antifungal (fungistatic) effect was achieved with the bark extract (even though at high concentrations), which further enhanced the activity of fluconazole. The extracts also inhibited the emission of filaments by Candida albicans and Candida tropicalis. Together, these findings suggest that that the extract constituents may act by favoring the permeability of microbial cells to conventional drugs, as well as by affecting virulence mechanisms in Candida strains.

19.
Molecules ; 27(2)2022 Jan 14.
Artículo en Inglés | MEDLINE | ID: mdl-35056820

RESUMEN

Amburana cearensis (Allemão) ACSm. belongs to the Fabaceae family and occurs in the Brazilian semiarid, Argentina, Paraguay, Bolivia, and Peru. Numerous studies that portray its ethnobotany, use in popular medicine, chemical composition, and biological activities exist in the literature. This review aimed to provide an overview of the chemical composition, ethnopharmacology, and biological activities associated with A. cearensis and its isolated constituents. Information was collected from internet searches in the Scopus, Medline, PubMed, Google Scholar, and ScienceDirect databases were performed covering publications from 1997-2020. An ethnopharmacological literature analysis revealed that A. cearensis is used to treat a wide range of respiratory disorders in addition to intestinal, circulatory, and inflammatory problems. Coumarins, flavonoids, phenolic glycosides, phenolic acids, phenylpropanoid derivatives, and triterpenoids, among others, have been reported as active compounds, with High-Performance Liquid Chromatography (HPLC) being the main analytical technique used. The A. cearensis extracts and compounds presented several biological activities, including antimicrobial, antinociceptive, anti-inflammatory, antioxidant, neuroprotective, and myorelaxant activities, among others. This review provides a useful bibliography for future investigations and A. cearensis applications; however, future studies should focus on its toxic effects and the mechanisms of action of its extracts and isolated constituents to guide clinical applications.


Asunto(s)
Antiinfecciosos/farmacología , Antioxidantes/farmacología , Fabaceae/química , Glucósidos/farmacología , Fitoquímicos/farmacología , Extractos Vegetales/farmacología , Antiinflamatorios , Fitoterapia
20.
Molecules ; 28(1)2022 Dec 30.
Artículo en Inglés | MEDLINE | ID: mdl-36615503

RESUMEN

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.


Asunto(s)
Antifúngicos , Fluconazol , Antifúngicos/química , Fluconazol/farmacología , Cromatografía Liquida , Cromatografía Líquida de Alta Presión , Extractos Vegetales/química , Espectrometría de Masas en Tándem , Candida albicans , Candida tropicalis , Pruebas de Sensibilidad Microbiana
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