RESUMO

The aim of this study was to evaluate the cytotoxic potential of Aristolochia foetida Kunth. Stems and leaves of A. foetida Kunth (Aristolochiaceae) have never been investigated pharmacologically. Recent studies of species of the Aristolochiaceae family found significant cytotoxic activities. Hexane, dichloromethane, ethyl acetate and methanol extracts were analyzed by 1H NMR and GC-MS to know the metabolites in each extract. In GC-MS analysis, the main compounds were methyl hexadecanoate (3); hexadecanoic acid (4); 2-butoxyethyl dodecanoate (9); ethyl hexadecanoate (20); methyl octadeca-9,12,15-trienoate (28) and (9Z,12Z,15Z)-octadeca-9,12,15-trienoic acid (40). The results showed a significant reduction in cell viability of the MCF-7 (breast cancer) cell line caused by organic extracts in a dose-dependent manner. The cytotoxicity activity of the dichloromethane extract from the stems (DSE) showed IC50 values of 45.9 µg/mL and the dichloromethane extract of the leaves (DLE) showed IC50 values of 47.3 µg/mL. DSE and DLE had the highest cytotoxic potential in an in vitro study against the MCF-7 cell line and non-tumor cells obtained from the bovine mammary epithelial (bMECs). DSE and DLE induced a loss in mitochondrial membrane potential (ΔΨm) and can cause cell death by apoptosis through the intrinsic pathway in the MCF-7 cell line. DSE and DLE are cytotoxic in cancer cells and cause late apoptosis. Higher concentrations of DSE and DLE are required to induce a cytotoxic effect in healthy mammary epithelial cells. This is the first report of the dichloromethane extract of A. foetida Kunth that induces late apoptosis in MCF-7 cancer cells and may be a candidate for pharmacological study against breast cancer.

RESUMO

Aiming to investigate the antiplasmodial activity and the phytochemical composition of Xylopia sericea leaves, the essential oil and dichloromethane extract were analyzed by gas and liquid chromatography, respectively, both of them coupled to mass spectrometry, and were evaluated against the chloroquine-resistant Plasmodium falciparum strain (W2) and for cytotoxicity to HepG2 cells. Low growth inhibition of P. falciparum as well as low cytotoxicity to HepG2 cells were observed for the essential oil. The leaves dichloromethane extract showed moderate growth inhibition of P. falciparum and low cytotoxicity to HepG2 cells. Bioguided chromatographic fractionation of this extract led to fractions with increased antiplasmodial activity from which liriodenine (IC50 6.1 ± 0.1 µg/mL, CC50 > 1000.0 µg/mL, SI > 164), an aporphine alkaloid, and an acetogenin-rich fraction containing mainly isomers of annomontacin and 4-deoxy-annomontacin (IC50 22.7 ± 1.9 µg/mL, CC50 336.1 ± 15.5 µg/mL, SI = 15) might be highlighted for their antiplasmodial activity.

Assuntos

RESUMO

BACKGROUND: Microalgae are aquatic chlorophyll-containing organisms comprising unicellular microscopic forms, and their biomasses are potential sources of bioactive compounds, biofuels and food-based products. However, the neuroprotective effects of microalgal biomass have not been fully explored. In this study, biomass from two Chlorella species was characterized, and their antioxidant, anticholinesterase and anti-amyloidogenic activities were investigated. RESULTS: GC­MS analysis of the extracts revealed the presence of some phenols, sterols, steroids, fatty acids and terpenes. Ethanol extract of Chlorella sorokiniana (14.21 mg GAE/g) and dichloromethane extract of Chlorella minutissima (20.65 mg QE/g) had the highest total phenol and flavonoid contents, respectively. All the extracts scavenged 2,2-diphenyl-1-picrylhydrazyl, 2,2-azinobis (3-ethylbenzothiazoline-6-sulfonate) and hydroxyl radicals. The highest metal chelating activity of the extracts was observed in the ethanol extracts of C. minutissima (102.60 µg/mL) and C. sorokiniana (107.84 µg/mL). Furthermore, the cholinesterase inhibitory activities of the extracts showed that ethanol extract of C. sorokiniana (13.34 µg/mL) exhibited the highest acetylcholinesterase inhibitory activity, while dichloromethane extract of C. minutissima (11.78 µg/mL) showed the highest butyrylcholinesterase inhibitory activity. Incubation of the ß-amyloid protein increased the aggregation of amyloid fibrils after 96 h. However, ethanol extract of C. sorokiniana and C. minutissima inhibited further aggregation of Aß1­42 and caused disaggregation of matured protein fibrils compared to the control. This study reveals the modulatory effects of C. sorokiniana and C. minutissima extracts on some mediators of Alzheimer's disease and provides insights into their potential benefits as functional food, nutraceutics or therapeutic agent for the management of this neurodegenerative disease.

Assuntos

RESUMO

AIMS: This study aims to improve characteristics of Piper regnellii extract to make it applicable in formulations to treat dermatophytosis, also known as ringworm. METHODS AND RESULTS: Microparticles (MPs) were produced by spray drying with gelatin, alginate and chitosan as encapsulating agents; characterized by scanning electron microscopy, encapsulation efficiency, thermal analyses and X-ray diffraction; and tested against Trichophyton rubrum by broth microdilution. Produced MPs had a mean diameter less than 2 µm, an increase in stability and release of the extract and good results for encapsulation efficiency, being 85·6% to gelatin MP, 71·3% to chitosan MP and 60·6% to alginate. MPs preserved the antifungal activity of P. regnellii extract T. rubrum. CONCLUSION: Microencapsulation provided a significant improvement in the stability of the P. regnellii extract and better solubilization of chemical compounds, maintaining the antifungal effect against T. rubrum. SIGNIFICANCE AND IMPACT OF THE STUDY: These results are useful for developing a formulation to treat fungal infections caused by dermatophyte species.

Assuntos

RESUMO

ABSTRACT Many infections worldwide are associated with bacterial biofilms. The effects of isolated neolignans (conocarpan and eupomathenoid-5) and the dichloromethane extract of Piper regnellii (Miq.) C. DC., Piperaceae, were tested against isolates of methicillin-resistant Staphylococcus aureus and methicillin-sensitive S. aureus biofilms and S. aureus planktonic cells. The dichloromethane extract presented better results than isolated neolignans against all of the biofilms tested, with a minimum inhibitory concentration <400 µg/ml for preformed biofilms and minimal biofilm inhibitory concentration of 15.6 µg/ml for biofilm formation. The minimum inhibitory concentration to planktonic cells was <12.5 µg/ml. These results indicate a good effect of the dichloromethane extract against methicillin-resistant S. aureus and methicillin-sensitive S. aureus biofilms and efficient prophylaxis.

RESUMO

INTRODUCCIÓN: el alga roja Galaxaura rugosa (J. Ellis & Solander) J.V. Lamouroux (Galaxauraceae) es una de las especies más abundantes en la plataforma rocosa del arrecife coralino del archipiélago cubano, sin embargo, poco se conoce de sus propiedades farmacológicas. OBJETIVOS: evaluar la actividad antiinflamatoria y analgésica del extracto en diclorometano del alga roja G. rugosa, así como la composición fitoquímica de esta especie. MÉTODOS: las algas se colectaron en el litoral norte de La Habana. La caracterización fitoquímica del alga se realizó según el Método de Chabra. Para la preparación del extracto se sometió la muestra a extracción Soxhlet con diclorometano a 40 ºC. La actividad antiinflamatoria tópica se estudió en el modelo de edema de la oreja inducido por aceite de Croton en ratones machos OF-1, a las dosis de 10*10-3; 0,125; 0,25; 0,5; 1 y 2 mg/oreja. Se evaluó también la actividad analgésica del extracto en el modelo de contorsiones inducidas por ácido acético al 0,8 %, por vía intraperitoneal (i.p.), a las dosis de 3; 6; 12,5; 25 y 100 mg/kg. RESULTADOS: G. rugosa presentó en su composición fitoquímica compuestos grasos, lactónicos, triterpénicos y/o esteroidales y carbohidratos. El extracto en diclorometano de G. rugosa a partir de la dosis de 0,125 mg/oreja presenta una potente actividad antiinflamatoria (superior al 40 %). El extracto logró reducir las contorsiones en más de un 75 % a partir de la dosis de 6 mg/kg. CONCLUSIONES: los resultados presentados demuestran que el extracto en diclorometano del alga roja G. rugosaestá constituido por una mezcla de compuestos capaces de inhibir con una elevada eficacia farmacológica la respuesta inflamatoria aguda y el dolor inducido por agentes químicos.

INTRODUCTION: the red alga Galaxaura rugosa (J. Ellis & Solander) J.V. Lamouroux (Galaxauraceae) is one of the most abundant species on the rocky platform of the Cuban coral reef. However, little is known about its pharmacological properties. OBJECTIVES: evaluate the anti-inflammatory and analgesic activity of a dichloromethane extract from the red alga G. rugosa and determine the phytochemical composition of the species. METHODS: the algae were collected from the northern coast of Havana. Phytochemical characterization of the alga was performed using Chabra's method. The extract was obtained with a Soxhlet device with dichloromethane at 40 ºC. Topical anti-inflammatory activity was studied with the croton oil ear edema test model in male OF-1 mice at doses of 10*10-3, 0.125, 0.25, 0.5, 1 and 2 mg/ear. The analgesic activity of the extract was evaluated on a model of writhing induced by 0.8 % acetic acid administered intraperitoneally (i.p.) at doses of 3, 6, 12.5, 25 and 100 mg/kg. RESULTS: phytochemical analysis of G. rugosa revealed the presence of fatty, lactonic, triterpenic and/or steroidal compounds, as well as carbohydrates. The dichloromethane extract of G. rugosa at the dose of 0.125 mg/ear displayed a potent anti-inflammatory activity (above 40 %). The extract reduced writhing by more than 75 % with a dose of 6 mg/kg. CONCLUSIONS: results show that dichloromethane extract of the red alga G. rugosa is composed of a mixture of compounds capable of inhibiting the acute inflammatory response and the pain induced by chemical agents with a high pharmacological efficacy. composed of a mixture of compounds capable of inhibiting the acute inflammatory response and the pain induced by chemical agents with a high pharmacological efficacy.

Assuntos

RESUMO

Vasorelaxant effect of Hyptis fruticosa dichloromethane extract (HFDE) on isolated rings of rat mesenteric artery was evaluated in this study. In intact rings, HFDE (0.1-3000 µg/mL) induced concentration-dependent vasorelaxations (Emax = 119±14 percent; n = 6) of phenylephrine tonus that were not modified after endothelium removal (Emax = 116±6 percent; n = 6), after KCl 20 mM (Emax = 135±9 percent; n = 6) or in rings pre-contracted with KCl 80 mM (Emax = 125±4 percent; n = 6). In endothelium denuded rings, HFDE (300 or 1000 µg/mL) inhibited contractions induced by CaCl2 (maximal inhibition = 25±7 percent and 95±1 percent; respectively). Furthermore, HFDE promoted an additional vasorelaxation (15±3 percent; n = 7) after maximal response of 10 µM nifedipine (78±3 percent; n = 7). In conclusion, HFDE induces vasorelaxant effect through an endothelium-independent pathway, which appears to be due in major part to inhibition of the Ca2+ influx through voltage-operated Ca2+ channels.

O efeito vasorelaxante do extrato diclorometano de Hyptis fruticosa Salzm. ex Benth., Lamiaceae (HFDE), em anéis isolados de artéria mesentérica de ratos foi avaliado nesse estudo. Em anéis intactos, pré-contraídos com fenilefrina (10 µM), HFDE (0,1-3000 µg/mL) induziu vasorelaxamento de maneira dependente de concentração (Emax = 119±14 por cento; n = 6), o qual não foi afetado após remoção do endotélio (Emax = 116±6 por cento; n = 6), após KCl 20 mM (Emax = 135±9 por cento; n = 6) ou em anéis pré-contraídos com KCl 80 mM (Emax = 125±4 por cento; n = 6). Em anéis sem endotélio, HFDE (300 ou 1000 µg/mL) inibiu as contrações induzidas por CaCl2 (inibição máxima = 25±7 por cento e 95±1 por cento, respectivamente). Além disso, HFDE promoveu um vasorelaxamento adicional (15±3 por cento; n = 7) sobre o relaxamento máximo de 10 µM de nifedipina (78±3 por cento, n = 7). Em conclusão, HFDE induz efeito vasorelaxante através de uma via independente de endotélio, possivelmente devido à inibição do influxo de Ca2+ através de canais de Ca2+ operados por voltagem.