RESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Solanum sisymbriifolium Lam., is used in Paraguayan folk medicine claiming antihypertensive and diuretic properties. AIM OF THE STUDY: This study aimed to determine the influence of chronic oral administration of the crude root extract and saponins obtained from S. sisymbriifolium Lam., on the blood pressure of male and female rats with hypertension induced by L-NAME, and its consequences on diuresis, the body weight, blood glucose, and level of serum parameters of liver and kidney functionality. MATERIALS AND METHODS: Wistar rats were randomly divided into seven male, and seven female groups (8 animals each), which received as 6-week pretreatment, 0.9% saline solution (two groups; 0.1mL/10 g of b.w.), L-arginine (100.0 mg/kg/day), enalapril (15.0 mg/kg/day), crude extract (CESs 100.0 mg/kg/day), and saponin purified fraction (1.0, and 10.0 mg/kg/day), and treated with L-NAME (20 mg/kg/day/i.p.) twice, 1, and 6 h after pre-treatment. The animals' body weight, glycemia, and blood pressure were recorded weekly, while serum, hepatic, renal, and histological parameters were analyzed at the end of 6-week of treatment. RESULTS: A protective effect of CESs (100.0 mg/kg/day), and saponins (1.0, and 10.0 mg/kg/day) against hypertension induced by L-NAME was verified in the systolic, diastolic, and mean blood pressure values, which were significantly lower than the positive L-NAME-hypertensive control group (male and female) at the end of the 6-week treatment. Also, pretreatment with enalapril (15.0 mg/kg/day) induced an efficient protective activity, which validates the method used. Likewise, the volume of urine, creatinine, uric acid, urea, and electrolyte excretion was enhanced at the end of 6-week of treatment in concordance with the reduction in serum level of the same parameters, compatible with the improvement of the diuretic activity. The glycemia, body weight, heart rate, and functional hepato-renal parameters were not modified after a 6-week of treatment, in comparison to the control group, indicating relatively acceptable harmless properties of CESs and saponins. Interestingly, the HDL level in females was increased in contrast to male rats by chronic saponins treatment when compared with the negative control group. CONCLUSIONS: It can be concluded that either the increment in blood pressure (systolic, diastolic, and median) or cardiorenal remodeling effects in male and female rats submitted to L-NAME-induced hypertensive condition, were prevented and well-preserved without a significant variation during a period of 6-week of pretreatment with CESs and saponins pretreatments. Likewise, an important diuretic effect was revealed after this period of treatment.
Asunto(s)
Hipertensión , Saponinas , Solanum , Animales , Antihipertensivos , Presión Sanguínea , Peso Corporal , Diuréticos/farmacología , Enalapril , Femenino , Hipertensión/inducido químicamente , Hipertensión/tratamiento farmacológico , Masculino , NG-Nitroarginina Metil Éster/farmacología , Extractos Vegetales , Ratas , Ratas Wistar , Saponinas/farmacología , Saponinas/uso terapéuticoRESUMEN
Dengue is the most important arthropod-borne viral disease worldwide. Infection with any of the four dengue virus (DENV) serotypes can be asymptomatic or lead to disease with clinical symptoms ranging from undifferentiated and self-limiting fever to severe dengue disease, which can be fatal in some cases. Currently, no specific antiviral compound is available for treating DENV. The aim of this study was to identify compounds in plants from Paraguayan folk medicine with inhibitory effects against DENV. We found high virucidal activity (50% maximal effective concentration (EC50) value of 24.97 µg/mL) against DENV-2 in the ethanolic extract of the roots of Solanum sisymbriifolium Lam. (Solanaceae) without an evident cytotoxic effect on Vero E6 cells. Three saponins isolated from the root extract showed virucidal effects (EC50 values ranging from 24.9 to 35.1 µg/mL) against DENV-2. Additionally, the saponins showed inhibitory activity against yellow fever virus (EC50 values ranging from 126 to 302.6 µg/mL), the prototype virus of the Flavivirus genus, suggesting that they may also be effective against other members of this genus. Consequently, these saponins may be lead compounds for the development of antiviral agents.
Asunto(s)
Virus del Dengue , Saponinas , Solanum , Antivirales/farmacología , Saponinas/farmacología , Replicación Viral , Virus de la Fiebre AmarillaRESUMEN
Dengue is the most important arthropod-borne viral disease worldwide. Infection with any of the four dengue virus (DENV) serotypes can be asymptomatic or lead to disease with clinical symptoms ranging from undifferentiated and self-limiting fever to severe dengue disease, which can be fatal in some cases. Currently, no specific antiviral compound is available for treating DENV. The aim of this study was to identify compounds in plants from Paraguayan folk medicine with inhibitory effects against DENV. We found high virucidal activity (50% maximal effective concentration (EC50) value of 24.97 µg/mL) against DENV-2 in the ethanolic extract of the roots of Solanum sisymbriifolium Lam. (Solanaceae) without an evident cytotoxic effect on Vero E6 cells. Three saponins isolated from the root extract showed virucidal effects (EC50 values ranging from 24.9 to 35.1 µg/mL) against DENV-2. Additionally, the saponins showed inhibitory activity against yellow fever virus (EC50 values ranging from 126 to 302.6 µg/mL), the prototype virus of the Flavivirus genus, suggesting that they may also be effective against other members of this genus. Consequently, these saponins may be lead compounds for the development of antiviral agents.
Asunto(s)
Saponinas/farmacología , Solanum , Virus del Dengue , Antivirales/farmacología , Replicación Viral , Virus de la Fiebre AmarillaRESUMEN
ABSTRACT The antibacterial activity of the alkaloid extract from the leaves of Croton bonplandianum Baill. and its main compounds, sparsiflorine and crotsparine, was tested against Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae and Pseudomonas aeruginosa by the resazurin microtitre-plate method. Pure compounds were identified by spectroscopic techniques, mainly 1D and 2D NMR. The alkaloid extract showed activity particularly against the S. aureus and P. aeruginosa. Regarding the pure compounds, the crotsparine was inactive against the microorganisms assayed, whereas the sparsiflorine indicated a moderate activity similar to the alkaloid extract. The Pseudomonas aeruginosa was the most sensitive of the tested microorganisms with MIC of 0.141 mg/mL. The results suggest that the activity of the extract may be credited mainly to the presence of the sparsiflorine. Although the activity of the sparsiflorine does not get close to the antimicrobial drugs in clinical use, it still could be a lead compound for the development of new antibacterial substances.
RESUMO A atividade antibacteriana do extrato alcaloidal das folhas de Croton bonplandianum Baill., além dos principais compostos isolados, esparsiflorina e crotsparina, foi testada contra Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae e Pseudomonas aeruginosa. Foi utilizado o método de microdiluição em placa empregando resazurina como indicador da viabilidade celular. Os compostos isolados foram identificados por técnicas espectroscópicas, principalmente RMN 1D e 2D. O extrato alcaloidal foi ativo principalmente contra S. aureus e P. aeruginosa. Crotsparina mostrou-se inativa contra todos os micro-organismos testados, enquanto esparsiflorina apresentou atividade moderada, a qual foi similar à do extrato bruto. Pseudomonas aeruginosa foi a mais sensível das bactérias testadas, com CIM de 0,141 mg/mL. Os resultados sugerem que a atividade do extrato pode ser devida em grande medida pela presença de esparsiflorina. Apesar de a CIM da esparsiflorina não ter se aproximado daquela apresentada pelos agentes antimicrobianos em uso clínico, tal composto ainda pode compor um protótipo interessante para o desenvolvimento de novas substâncias antibacterianas.
Asunto(s)
Euphorbiaceae/clasificación , Alcaloides/análisis , Antibacterianos/análisis , Extractos Vegetales , Fagos de Staphylococcus , Croton/clasificaciónRESUMEN
Isonuatigenin-3-O-beta-solatriose (1) was isolated from the roots of Solanum sisymbriifolium. Its structure was determined by spectroscopic methods.
Asunto(s)
Fitoterapia , Extractos Vegetales/química , Solanum , Humanos , Estructura Molecular , Raíces de Plantas , Saponinas/químicaRESUMEN
Two novel trimers, triscutins A and B (1 and 2), based on pristimerin triterpene units, were isolated and characterized from Maytenus scutioides. Their structures were determined on the basis of spectroscopic evidence, including 1H-13C heteronuclear correlation (HMQC), long-range correlation with inverse detection (HMBC), and ROESY NMR experiments; and their absolute configurations, by means of CD studies. Compounds 1 and 2 were assayed for antimicrobial and cytotoxic activities, and their possible biosynthetic route is proposed.
Asunto(s)
Antiinfecciosos/aislamiento & purificación , Antineoplásicos Fitogénicos/aislamiento & purificación , Plantas Medicinales/química , Triterpenos/aislamiento & purificación , Antibacterianos , Antiinfecciosos/farmacología , Antineoplásicos Fitogénicos/farmacología , Bacterias/efectos de los fármacos , Candida/efectos de los fármacos , Dicroismo Circular , Ensayos de Selección de Medicamentos Antitumorales , Células HeLa , Humanos , Espectroscopía de Resonancia Magnética , Pruebas de Sensibilidad Microbiana , América del Sur , Triterpenos/farmacología , Células Tumorales CultivadasRESUMEN
15alpha-Hydroxy-21-keto-pristimerine (1), a new nortriterpene quinone methide was isolated from the root bark of Maytenus catingarum along with other well-known related compounds, including pristimerine (2), tingenone, and 20alpha-hydroxy-tingenone. The structure of 1 was determined by means of 1H and 13C NMR spectroscopy, including homonuclear and heteronuclear correlations. Compound 1 showed antibiotic activity against Gram-positive bacteria.
Asunto(s)
Antibacterianos/aislamiento & purificación , Rosales/química , Antibacterianos/farmacología , Candida albicans/efectos de los fármacos , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Espectroscopía de Resonancia Magnética , Pruebas de Sensibilidad Microbiana , Noresteroides/aislamiento & purificación , Noresteroides/farmacología , Raíces de Plantas/química , Espectrofotometría Infrarroja , Espectrofotometría UltravioletaRESUMEN
By antimicrobial and cytotoxic-guided fractionation, a bioactive norquinone-methide triterpene, 15 alpha-hydroxypristimerin, was isolated from a South American medicinal plant, Maytenus scutioides. Its structure was determined on the basis of spectroscopic evidence. Successful chemical transformation of pristimerin to netzahualcoyene indicates that the 15-hydroxy compounds seems to be a possible percursor of 14(15)-ene-quinone-methide-triterpenoids in the biogenetic pathway.
Asunto(s)
Antibacterianos/aislamiento & purificación , Antineoplásicos Fitogénicos/aislamiento & purificación , Plantas Medicinales/química , Triterpenos/aislamiento & purificación , Antibacterianos/química , Antibacterianos/farmacología , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/farmacología , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Humanos , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Análisis Espectral , Triterpenos/química , Triterpenos/farmacología , Células Tumorales CultivadasRESUMEN
The new phenols 6-oxo-tingenol, 3-O-methyl-6-oxo-tingenol and 6-oxo-iguesterol were isolated from the root bark of Maytenus canariensis. Their structures were determined by 1H and 13C NMR spectroscopic studies, including HMQC, HMBC, DEPT and ROESY and chemical transformations. The synthesis of 6-oxo-tingenol was achieved from tingenone. These compounds exhibit antibiotic activity against Gram-positive bacteria.
Asunto(s)
Antibacterianos/aislamiento & purificación , Raíces de Plantas/química , Plantas Medicinales/química , Terpenos/aislamiento & purificación , Antibacterianos/química , Isótopos de Carbono , Espectroscopía de Resonancia Magnética , Espectrometría de Masas , Protones , Terpenos/químicaRESUMEN
Scutione (1), a new norquinonemethide triterpene with a netzahualcoyene type skeleton, has been isolated from the root bark of Maytenus scutioides (Celastraceae) by bioactivity-directed fractionation. The structure of 1 has been elucidated by means of 1H and 13C NMR spectroscopic studies, including 1H-13C heteronuclear correlation (HETCOR), a long-range correlation spectrum with inverse detection (HMBC) and ROESY experiments. Compound 1 showed antibiotic activity against Gram-positive bacteria and modest cytotoxic activity against HeLa, Hep-2 and Vero cell lines. Fluoride derivatives 2-4 were prepared and assayed for bioactivity, where 2 showed slight improvement of the cytotoxic potency.