ABSTRACT
La isoforma AMPKß2 (proteína quinasa activada por AMP) favorece la homeostasis glucémica a través de un mecanismo independiente de insulina. Muchos "importagogos" de glucosa como SC4 actúan como activadores de AMPK, pero su consumo prolongado se asocia a efectos indeseables. Objetivo: en este trabajo se utilizó el acoplamiento molecular para analizar la posible interacción entre sapogeninas y AMPK. Métodos: se ha procedido a la preparación de los blancos proteicos, preparación de los ligandos y el acoplamiento molecular. Resultados: los resultados mostraron que ocho sapogeninas presentes en Chenopodium quinoa interactúan en el mismo sitio de unión que SC4 correspondiente al sitio ADaM de AMPK. Estas interacciones puntuaron valores de ΔG que oscilan entre -6,2 y -7,7 kcal/mol, siendo el ácido serjánico la sapogenina con el ΔG más bajo. La adición de grupos hidrofílicos como -OH y -COOH en la estructura química del ácido serjánico mejoró su afinidad de unión a la isoforma AMPKß2 abriendo la posibilidad de generar fármacos semi-sintéticos a partir de compuestos naturales con mayor actividad biológica y mejor especificidad.
The AMPKP2 (AMP-activated protein kinase) isoform promotes glycemic homeostasis through an insulin-independent mechanism. Many glucose "importers" such as SC4 act as AMPK activators, but their prolonged consumption is associated with undesirable effects. Objetive: in this work, molecular docking was used to analyze the possible interaction between sapogenins and AMPK. Methods: the preparation of the protein blanks, preparation of the ligands and molecular coupling have been carried out. Results: the results showed that eight sapogenins present in Chenopodium quinoa interact at the same binding site as SC4 corresponding to the ADaM site of AMPK. These interactions scored ΔG values ranging from -6.2 to -7.7 kcal/mol, with Serjanic acid being the sapogenin with the lowest ΔG. The addition of hydrophilic groups such as -OH and -COOH in the chemical structure of Serjanic acid improved its binding affinity to the AMPKß2 isoform opening the possibility of generating semi-synthetic drugs from natural compounds with higher biological activity and better specificity.
ABSTRACT
Objective: To establish a macroporous resin enrichment process for total triterpene sapogenins from Pfaffia glomerata,and evaluate the free radical scavenging activity of the total triterpene sapogenins. Methods: The transfer rate of triterpene sapogenins was used as the index. Static adsorption-desorption method was used to select the best macroporous resin,dynamic adsorption-desorption method was used to determine the enrichment process parame- ters,and orthogonal test was used to optimize the enrichment process. The 1,1- diphenyl- 2- trinitrophenylhydrazine (DPPH)and hydroxyl free radical scavenging tests were used to evaluate the free radical scavenging capacity of the triter- pene sapogenins. Results: The AB-8 type macroporous resin had the best enrichment effect on the triterpene sapoge-nins. The conditions for the optimum enrichment process were as follows:the concentration of triterpene sapogenins in the sample solution for resin column chromatography was 3.5 mg/ml,the ratio of diameter to height for the bed of resin column was 1:7,the amount of the raw herbs subjected to the resin column was 0.11 g/ml(herbs/resin),the flow rate for subjecting sample solution to resin column was 1 BV/h,the eluent was 95% aqueous ethanol,the eluting flow rate was 2BV/h,and the eluent volume for elution was 7 BV. After optimization,total triterpene sapogenins reached 65% in the samples prepared by the optimized process,and the transfer rate of total triterpene sapogenins reached 80.23% in the pre- paring process. The total triterpene sapogenin sample could scavenge the DPPH and hydroxyl free radicals,and the scav- enging rate for the DPPH and hydroxyl radicals reached 82.42% and 73.43% at the 1.0 mg/ml,respectively. Conclusion: The AB- 8 macroporous resin can be used for the enrichment and purification of triterpene sapogenins from P. glomerata. The optimized enrichment process was stable and feasible,and the obtained triterpene sapogenins showed a good free radical scavenging activity.
ABSTRACT
Objective To study the effects of dammarane sapogenins ( DS-1226 ) on sleep interruption-induced learning and memory impairment in mice.Methods 130 SPF healthy 5 -6-week old male ICR mice were randomly divided into control, model, DS-1226 low dose, DS-1226 medium dose and DS-1226 high dose groups.The behavioral alterations in open field (OF), Morris water maze (MWM) and step-through (ST) tests were detected at 15 days after rotating drum-induced sleep interruption ( SI) .Results The total distance, movement speed, total duration of movement were increased in OF test ( P<0.05, vs.the model group) after treatment.The latency of place navigation was increased from day 5 in the MWM test after 15 d sleep interruption, and the number of crossing in the target quadrant and the percent distance in target quadrant were decreased after 15 d sleep interruption ( P <0.05, vs.the control group), while the latency of place navigation was decreased, and the percent distance in target quadrant and percent time in target quadrant after high dose DS-1226 oral administration ( P<0.05, vs.the model group) were increased.Error times, distance in dark chamber, time in dark chamber and immobility time in dark chamber were increased in training of step through test ( P<0.05, vs.the control group);while these indexes were decreased after DS-1226 oral administration ( P<0.05, vs.the model group) .But there was no significant difference in the step through testing course.Conclusions The results show that orally administrated DS-1226 can ameliorate SI-induced learning and memory impairment, and there is a significant dosage-effect relationship.
ABSTRACT
Las plantas del género Solanum, dentro del que se encuentra el "lulo de perro" (Solanum marginatum), especie considerada una maleza, contienen saponinas, las cuales tienen propiedades de emulsionar la grasa, similares al jabón. Esta característica fue aprovechada para evaluar el poder sanitizante del extracto alcohólico del fruto, en calidad de limpiador biodegradable, de gran utilidad en la industria. El potencial sanitizante del limpiador preparado se evaluó según el procedimiento descrito por Carrascal, Páez y Burbano (1998), y se encontró como condiciones óptimas de efectividad antimicrobial: una concentración del 10% y un tiempo de contacto de 6 minutos sobre microorganismos bacilos gram negativos, que presentan un máximo de inhibición de 99,58%. Al comparar la efectividad del producto obtenido contra la de dos conocidos sanitizantes comerciales (Mat-98® y Germigel®), se encontró una respuesta similar. Por hidrólisis del crudo de saponina se liberaron las sapogeninas presentes, los cristales obtenidos se analizaron por espectroscopía infrarroja y se les determinó el punto de fusión, coincidiendo los resultados con la Hecogenina.
Plants of the genus Solanum, within which the "Lulo perro" (Solanum marginatum) is found and is considered as a weed species, contain saponins which have fat emulsifying properties similar to soap. This feature was used to evaluate the sanitizing power of the alcoholic extract of the fruit as a biodegradable cleaner which is very useful for industrial purposes. The sanitizing potential of the cleaner preparation was assessed using the procedure described by Carrascal, Páez y Burbano (1998), and it was found to have optimum antimicrobial effectiveness conditions: a 10% concentration and a 6 minute contact time over gram negative bacilli microorganisms which represent a maximum inhibition of 99 58%. When comparing the effectiveness of the product against two well-known commercial sanitizers. (Mat-98® and Germigel®), a similar response was found. Using crude hydrolysis of saponin, present sapogenins were released, the crystals obtained were analyzed using infrared spectroscopy, and melting point was determined. These results coincided with the Hecogenin.