RESUMEN
Bioassay-guided isolation from Camellia sinensis (Theaceae) and Colchicum luteum (Liliaceae) utilizing an in vitro model of protease assay revealed colchicine (1) and caffeine (2) from chloroform fractions, respectively. Their structures were validated using spectral techniques. The purified compounds were further optimized with Gaussian software utilizing the B3LYP functional and 6-31G(d,p) basis set. The result files were utilized to determine several global reactivity characteristics to explain the diverse behavior of the compounds. Colchicine (1) showed a higher inhibition of protease activity (63.7 ± 0.5 %age with IC50 = 0.83 ± 0.07 mM), compared with caffeine (2) (39.2 ± 1.3 %age). In order to determine the type of inhibition, compound 1 was further studied, and, based on Lineweaver-Burk/Dixon plots and their secondary replots, it was depicted that compound 1 was a non-competitive inhibitor of this enzyme, with a Ki value of 0.690 ± 0.09 mM. To elucidate the theoretical features of protease inhibition, molecular docking studies were performed against serine protease (PDB #1S0Q), which demonstrated that compound 1 had a strong interaction with the different amino acid residues located on the active site of this understudied enzyme, with a high docking score of 16.2 kcal/mol.
Asunto(s)
Alcaloides , Camellia sinensis , Colchicum , Simulación del Acoplamiento Molecular , Colchicum/química , Camellia sinensis/química , Péptido Hidrolasas , Cafeína , Alcaloides/farmacología , Endopeptidasas , Colchicina , BioensayoRESUMEN
The antioxidant activity and the inhibitory potential of α-amylase of lyophilized hydroethanolic extracts of Conocarpus erectus leaves obtained by ultrasonication were determined. The most potent extract was subjected to ultra-high performance liquid chromatography system equipped with mass spectrometer for metabolite identification. The identified metabolites were docked in α-glucosidase to assess their binding mode. The results revealed that 60% ethanolic extract exhibited highest ferric reducing antioxidant power (4.08 ± 0.187 mg TE/g DE) and α-amylase inhibition (IC50 58.20 ± 1.25 µg/mL. The metabolites like ellagic acid, 3-O-methyl ellagic acid, ferujol, 5, 2 Ì-dihydroxy-6,7,8-trimethyl flavone and kaempferol glucoside were identified in the extract and subjected to molecular docking studies regarding α-amylase inhibition. The comparison of binding affinities revealed 3-O-methyl ellagic acid as most effective inhibitor of α-amylase with binding energy of -14.5911 kcal/mol comparable to that of acarbose (-15.7815 kcal/mol). The secondary metabolites identified in the study may be extended further for functional food development with antidiabetic properties.
Se determinó la actividad antioxidante y el potencial inhibidor de la α-amilasa de extractos hidroetanólicos liofilizados de hojas de Conocarpus erectus obtenidos por ultrasónicación. El extracto más potente se sometió a un sistema de cromatografía líquida de ultra alto rendimiento equipado con un espectrómetro de masas para la identificación de metabolitos. Los metabolitos identificados se acoplaron en α-glucosidasa para evaluar su modo de unión. Los resultados revelaron que el extracto etanólico al 60% exhibió el mayor poder antioxidante reductor férrico (4.08 ± 0.187 mg TE/g DE) e inhibición de la α-amilasa (IC50 58.20 ± 1.25 µg/mL. Los metabolitos como el ácido elágico, 3-O-metil elágico ácido, ferujol, 5, 2 Ì-dihidroxi-6,7,8-trimetil flavona y kaempferol glucósido se identificaron en el extracto y se sometieron a estudios de acoplamiento molecular con respecto a la inhibición de la α-amilasa. La comparación de las afinidades de unión reveló 3-O-metil El ácido elágico como inhibidor más eficaz de la α-amilasa con una energía de unión de -14,5911 kcal/mol comparable a la de la acarbosa (-15,7815 kcal/mol). Los metabolitos secundarios identificados en el estudio pueden ampliarse aún más para el desarrollo funcional de alimentos con propiedades antidiabéticas.
Asunto(s)
Extractos Vegetales/química , alfa-Amilasas/antagonistas & inhibidores , Myrtales/química , Antioxidantes/química , Benzopiranos/análisis , Técnicas In Vitro , Extractos Vegetales/farmacología , Hojas de la Planta/química , Simulación del Acoplamiento Molecular , Antioxidantes/farmacologíaRESUMEN
Search for safe antioxidants and novel nutraceuticals urged to evaluate the antioxidant, anti-acetylcholine esterase and anti-lipoxygenase activity of various leaf extracts of Conocarpus lancifolius. Extraction was optimized from freeze dried plant extracts quenched with liquid nitrogen using water, ethanol, methanol, hexane, ethyl acetate and chloroform. Maximum extract yield, total phenolic contents and total flavonoid contents were obtained in case of ethanolic extraction. The highest 2,2-diphenyl-1-picrylhydrazylradical scavenging in terms of IC50 value of 55.26 µg/mL was observed for ethanolic leaf extract. The acetylcholine esterase and lipoxygenase inhibitory activities (IC50) were also observed for ethanolic extract. These findings for ethanolic extract were statistically significant when compared with other extracts (ρ<0.05). The haemolytic % values indicated that all extracts were associated with very low or negligible toxicity. The epicatechin, isorhamnetin, rutin, scopoleptin, skimmianine, quercetin-3-O-α-rhamnoside, quercetin-3-O-ß-glucoside, cornoside, creatinine, choline, pyruvic acid, α-hydroxybutyric acid, phyllanthin and hypophyllanthin were identified as major functional metabolites in ethanolic leaf extract of C. lancifoliusby 1H-NMR. The identified metabolites were probably responsible for the pharmacological properties of C.lancifolius. The findings may be utilized as pharmacological leads for drug development and food fortification.
Se insta a la búsqueda de antioxidantes seguros y nuevos nutracéuticos para evaluar la actividad antioxidante, anti-acetilcolina esterasa y anti-lipoxigenasa de varios extractos de hojas de Conocarpus lancifolius. La extracción se optimizó a partir de extractos de plantas liofilizados enfriados con nitrógeno líquido usando agua, etanol, metanol, hexano, acetato de etilo y cloroformo. En el caso de extracción etanólica se obtuvo el rendimiento máximo de extracto, el contenido de fenoles totales y el contenido de flavonoides totales. La mayor eliminación de radicales 2,2-difenil-1-picrilhidrazilo en términos de valor de CI50 de 55,26 µg/mL se observó para el extracto de hoja etanólico. También se observaron las actividades inhibidoras de la acetilcolina esterasa y lipoxigenasa (CI50) para el extracto etanólico. Estos hallazgos para el extracto etanólico fueron estadísticamente significativos en comparación con otros extractos (ρ<0.05). Los valores del % hemolítico indicaron que todos los extractos estaban asociados con una toxicidad muy baja o insignificante. Se identificaron la epicatequina, isorhamnetina, rutina, escopoleptina, skimmianina, quercetina-3-O-α-ramnosido, quercetina-3-O-ß-glucósido, cornosido, creatinina, colina, ácido pirúvico, ácido α-hidroxibutírico, filantrina e hipofillantina. como metabolitos funcionales principales en el extracto etanólico de hojas de C. lancifoliuspor 1H-NMR. Los metabolitos identificados probablemente fueron responsables de las propiedades farmacológicas de C. lancifolius. Los hallazgos pueden utilizarse como pistas farmacológicas para el desarrollo de fármacos y la fortificación de alimentos.
Asunto(s)
Extractos Vegetales/farmacología , Combretaceae/química , Antioxidantes/farmacología , Fenoles/análisis , Flavonoides/análisis , Técnicas In Vitro , Extractos Vegetales/química , Inhibidores de la Colinesterasa/farmacología , Inhibidores de la Colinesterasa/química , Depuradores de Radicales Libres , Inhibidores de la Lipooxigenasa/farmacología , Inhibidores de la Lipooxigenasa/química , Etanol , Antioxidantes/químicaRESUMEN
The Tamarix dioica (T. dioica) is widely used medicinal plant to cure many chronic ailments. T. dioica is being used to manage diabetes mellitus in traditional medicinal system; however, very little scientific evidence is available on this plant in this context. The current study involves the fractionation of crude methanolic extract of T. dioica using n-hexane, ethyl acetate, chloroform, and n-butanol. The screening for antioxidant activity using 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay was carried out. The in vitro antidiabetic potential was assessed by measuring α-glucosidase inhibition. Total phenolic and flavonoid contents were also determined for each fraction. The metabolites were identified using highly sensitive and emerging 1H-NMR technique. The results revealed the ethyl acetate fraction as the most potent with DPPH scavenging activity of 84.44 ± 0.21% and α-glucosidase inhibition with IC50 value of 122.81 ± 2.05 µg/mL. The total phenolic and flavonoid content values of 205.45 ± 1.36 mg gallic acid equivalent per gram dried extract and 156.85 ± 1.33 mg quercetin equivalent per gram dried extract were obtained for ethyl acetate fraction. The bucketing of 1H-NMR spectra identified 22 metabolites including some pharmacologically important like tamarixetin, tamaridone, quercetin, rutin, apigenin, catechin, kaempferol, myricetin and isorhamnetin. Leucine, lysine, glutamic acid, aspartic acid, serine, and tyrosine were the major amino acids identified in ethyl acetate fraction. The molecular docking analysis provided significant information on the binding affinity among secondary metabolites and α-glucosidase. These metabolites were most probably responsible for the antioxidant activity and α-glucosidase inhibitory potential of ethyl acetate fraction. The study ascertained the ethnomedicinal use of T. dioica to manage diabetes mellitus and may be a helpful lead towards naturopathic mode for anti-hyperglycemia.
RESUMEN
The naturopathic treatment of obesity is a matter of keen interest to develop efficient natural pharmacological routes for disease management with low or negligible toxicity and side effects. For this purpose, optimized ultrasonicated hydroethanolic extracts of Taraxacum officinale were evaluated for antiobesity attributes. The 2,2-diphenyl-1-picrylhydrazyl method was adopted to evaluate antioxidant potential. Porcine pancreatic lipase inhibitory assay was conducted to assess the in vitro antiobesity property. Ultra-high performance chromatography equipped with a mass spectrometer was utilized to profile the secondary metabolites in the most potent extract. The 60% ethanolic extract exhibited highest extract yield (25.05 ± 0.07%), total phenolic contents (123.42 ± 0.007 mg GAE/g DE), total flavonoid contents (55.81 ± 0.004 RE/g DE), DPPH-radical-scavenging activity (IC50 = 81.05 ± 0.96 µg/mL) and pancreatic lipase inhibitory properties (IC50 = 146.49 ± 4.24 µg/mL). The targeted metabolite fingerprinting highlighted the presence of high-value secondary metabolites. Molecular-binding energies computed by docking tool revealed the possible contribution towards pancreatic lipase inhibitory properties of secondary metabolites including myricetin, isomangiferin, icariside B4, kaempferol and luteolin derivatives when compared to the standard drug orlistat. In vivo investigations revealed a positive impact on the lipid profile and obesity biomarkers of obese mice. The study presents Taraxacum officinale as a potent source of functional bioactive ingredients to impart new insights into the existing pool of knowledge of naturopathic approaches towards obesity management.
Asunto(s)
Fármacos Antiobesidad/farmacología , Metabolómica , Simulación del Acoplamiento Molecular , Obesidad/tratamiento farmacológico , Extractos Vegetales/farmacología , Taraxacum/química , Animales , Fármacos Antiobesidad/metabolismo , Fármacos Antiobesidad/uso terapéutico , Peso Corporal/efectos de los fármacos , Cromatografía Líquida de Alta Presión , Etanol/química , Lipasa/antagonistas & inhibidores , Lipasa/química , Lipasa/metabolismo , Ratones , Obesidad/metabolismo , Páncreas/enzimología , Extractos Vegetales/metabolismo , Extractos Vegetales/uso terapéutico , Conformación Proteica , Espectrometría de Masas en TándemRESUMEN
Butea monosperma is one of the extensively used plants in traditional system of medicines for many therapeutic purposes. In this study, the antioxidant activity, α-glucosidase and α-amylase inhibition properties of freeze drying assisted ultrasonicated leaf extracts (hydro-ethanolic) of B. monosperma have been investigated. The findings revealed that 60% ethanolic fraction exhibited high phenolic contents, total flavonoid contents, highest antioxidant activity, and promising α-glucosidase and α-amylase inhibitions. The UHPLC-QTOF-MS/MS analysis indicated the presence of notable metabolites of significant medicinal potential including apigenin, apigenin C-hexoside C-pentoside, apigenin C-hexoside C-hexoside, apigenin-6,8-di-C-pentoside and genistin etc., in B. monosperma leave extract. Docking studies were carried out to determine the possible role of each phytochemical present in leaf extract. Binding affinity data and interaction pattern of all the possible phytochemicals in leaf extract of B. monosperma revealed that they can inhibit α-amylase and α-glucosidase synergistically to prevent hyperglycemia.
Asunto(s)
Butea/química , Inhibidores de Glicósido Hidrolasas/química , Hipoglucemiantes/química , Fitoquímicos/química , Extractos Vegetales/química , Hojas de la Planta/química , Etanol/química , alfa-Amilasas/antagonistas & inhibidores , alfa-Amilasas/química , alfa-Glucosidasas/químicaRESUMEN
BACKGROUND: Diabetes mellitus type II (DMT-2) is a widely spread metabolic disorder both in developed and developing countries. The role of oxidative stress is well established in DMT-2 pathogenesis. The synthetic drugs for DMT-2 are associated with serious side complications. Antioxidant and α-glucosidase inhibitory actions of phytochemicals from various plant species are considered as an alternative to synthetic drugs for DMT-2 management. The present study aimed to evaluate the antioxidant activity, α-glucosidase inhibitory potential and phytochemical profiling of Hyophorbe lagenicaulis. METHODS: The total phenolic and flavonoid contents, in vitro antioxidant activity (α, α-diphenyl-ß-picrylhydrazyl (DPPH) free radical scavenging and phosphomolybdenum method) and α-glucosidase inhibition of ultrasonicated hydroethanolic H. lagenicaulis leaf extracts were determined spectrophotometrically. The results of DPPH assay and α-glucosidase inhibition were reported in terms of IC50 value. The phytochemical profiling was accomplished by UHPLC-Q-TOF/MS/MS technique. RESULTS AND DISCUSSION: Findings leaped 60% ethanolic extract as rich fraction regarding total phenolic and flavonoid contents. The 60% ethanolic fraction was a promising source of natural antioxidants and α-glucosidase inhibitory agents as indicated by anti-radical and enzyme inibitory activities. Kaempferol, rutin, hesperetin 5-O-glucoside, kaempferol-coumaroyl-glucoside, luteolin 3-glucoside, Isorhamnetin-3-O-rutinoside, trimethoxyflavone derivatives and citric acid were identified by UHPLC-Q-TOF-MS/MS. These compounds were believed to be responsible for the strong antioxidant and enzyme inhibitory activity of plant extracts. The extensive metabolite profiling of H. lagenicaulis was carried out the first time as never reported previously. The H. lagenicaulis might be an appropriate choice to manage diabetes mellitus in an alternate way. The findings may be further exploited extensively for toxicity evaluation to proceed with functional food development having antidiabetic attributes.
RESUMEN
The leaves of Cycas revoluta were explored for their antioxidant, α-glucosidase and α-amylase inhibitory properties to develop safe and diet based therapeutic treatment of diabetes. In optimized fractionation, 60% ethanol provided the highest extract yield of 19.35±0.05a%, TPC 95.70±1.60a mg GAE/g and TFC 55 .60 ± 1.20a mg Rutin/g extract. The antioxidant and anti α-glucosidase activities of 60% ethanolic extracts were also promising and statistically significant as compared with remaining plant extracts. Ultra-high-performance liquid chromatography-tandem mass spectrometry (UHPLC-Q-TOF-MS/MS) analysis of the leaf extract revealed the presence of three apigenin derivatives, kaempferol derivative, hexadecenoic acid and citric acid. The binding energy values of molecular docking studies supported the synergistic behavior of leaf extract to inhibit α-glucosidase activity. The leaves of Cycas revoluta were proved to be apigenin rich natural pool of metabolites of antidiabetic importance to improvise food functionalities.
Asunto(s)
Antioxidantes/farmacología , Cycas/metabolismo , Inhibidores de Glicósido Hidrolasas/farmacología , Extractos Vegetales/farmacología , Hojas de la Planta/metabolismo , Antioxidantes/química , Apigenina/análisis , Cromatografía Líquida de Alta Presión , Cycas/química , Evaluación Preclínica de Medicamentos , Etanol , Inhibidores de Glicósido Hidrolasas/química , Simulación del Acoplamiento Molecular , Extractos Vegetales/química , Plantas Medicinales/química , Plantas Medicinales/metabolismo , Espectrometría de Masas en Tándem , alfa-Amilasas/antagonistas & inhibidoresRESUMEN
Current work was performed to evaluate antioxidant activity, α-glucosidase inhibition, phytochemical profiling and in vivo hypoglycemic activity of freeze dried, ultrasonicated Hyophorbe indica leaf extracts. The highest total phenolic contents of 208.77±2.11 mg GAE/g DE and total flavonoid contents of 173.90±2.30 mg Rutin/g DE were obtained in 60% ethanol extract. The 60% ethanol extract exhibited maximum DPPH radical scavenging with IC50 value of 35.35±0.189µg/mL and total antioxidant power of 330.26±3.13 (ASE/g PE), respectively. The highest α-glucosidase inhibition (IC50 36.52 ± 0.08µg/mL) was also observed for 60% ethanol extract. The 60% ethanol extract at dose of 450 mg/kg body weight reduced blood glucose level of alloxan induced diabetic mice by 51.41% which was quite comparable with metformin (56.67%). Twelve compounds namely citric acid, procyanidin B3, epicatechin, procyanidin B2, catechin, catechin derivative, procyanidin B1, apigenin-c-hexocide-c-hexocide, kaempferol, kaempferol derivative, quinic acid derivative and gallic acid have been identified by using UHPLC-Q-TOF-MS/MS in 60% ethanol extract.
Asunto(s)
Antioxidantes/metabolismo , Arecaceae , Diabetes Mellitus Experimental/tratamiento farmacológico , Hipoglucemiantes/metabolismo , Metaboloma/fisiología , Extractos Vegetales/metabolismo , Animales , Antioxidantes/aislamiento & purificación , Antioxidantes/uso terapéutico , Diabetes Mellitus Experimental/sangre , Hipoglucemiantes/aislamiento & purificación , Hipoglucemiantes/uso terapéutico , Ratones , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/uso terapéutico , Hojas de la Planta/metabolismoRESUMEN
Synthetic drugs have widely been helpful in management of diabetes mellitus type 2. However, side effects associated with synthetic drugs serve as an impetus to explore plants as alternate mode of treatment. The hydroethanolic leaf extracts of Conocarpus erectus were evaluated for phenolic contents, flavonoid distribution, antioxidant activity and antidiabetic potential. The maximum extract yield, total phenolic and flavonoid contents were exposed by 60% ethanolic extract. The Antioxidant and anti α-glucosidase tendency of 60% ethanolic extract was the most promising and complemented by in-vivo antihyperglycemic impact on mice. The findings were substantial regarding suppression of blood glucose levels in alloxan induced diabetic mice establishing the Conocarpus erectus as proficient pool of nutraceuticals for diabetes mellitus type 2 management.
Asunto(s)
Combretaceae/química , Diabetes Mellitus Experimental/tratamiento farmacológico , Hipoglucemiantes/uso terapéutico , Fitoterapia/métodos , Animales , Antioxidantes/farmacología , Glucemia/efectos de los fármacos , Diabetes Mellitus Experimental/inducido químicamente , Flavonoides/análisis , Inhibidores de Glicósido Hidrolasas/farmacología , Masculino , Ratones , Fenoles/análisis , Extractos Vegetales/química , Extractos Vegetales/uso terapéutico , Hojas de la Planta/químicaRESUMEN
Background: Morinda citrifolia L. is widely used as a folk medicinal food plant to manage a panoply of diseases, though no concrete reports on its potential anti-obesity activity. This study aimed to evaluate the potential of M. citrifolia leaf extracts (MLE60) in the prevention of weight gain in vivo and establish its phytochemical profile. Design: Male Sprague-Dawley rats were divided into groups based on a normal diet (ND) or high fat diet (HFD), with or without MLE60 supplementation (150 and 350 mg/kg body weight) and assessed for any reduction in weight gain. Plasma leptin, insulin, adiponectin, and ghrelin of all groups were determined. 1H NMR and LCMS methods were employed for phytochemical profiling of MLE60. Results: The supplementation of MLE60 did not affect food intake indicating that appetite suppression might not be the main anti-obesity mechanism involved. In the treated groups, MLE60 prevented weight gain, most likely through an inhibition of pancreatic and lipoprotein activity with a positive influence on the lipid profiles and a reduction in LDL levels . MLE60 also attenuated visceral fat deposition in treated subjects with improvement in the plasma levels of obesity-linked factors . 1Spectral analysis showed the presence of several bioactive compounds with rutin being more predominant. Conclusion: MLE60 shows promise as an anti-obesity agents and warrants further research.
RESUMEN
BACKGROUND: Type 2 diabetes mellitus (T2DM) is a metabolic disorder characterized by continuous hyperglycemia associated with insulin resistance and /or reduced insulin secretion. There is an emerging trend regarding the use of medicinal plants for the treatment of diabetes mellitus. Melicope lunu-ankenda (ML) is one of the Melicope species belonging to the family Rutaceae. In traditional medicines, its leaves and flowers are known to exhibit prodigious health benefits. The present study aimed at investigating anti-diabetic effect of Melicope lunu-ankenda (ML) leaves extract. METHODS: In this study, anti-diabetic effect of ML extract is investigated in vivo to evaluate the biochemical changes, potential serum biomarkers and alterations in metabolic pathways pertaining to the treatment of HFD/STZ induced diabetic rats with ML extract using 1H NMR based metabolomics approach. Type 2 diabetic rats were treated with different doses (200 and 400 mg/kg BW) of Melicope lunu-ankenda leaf extract for 8 weeks, and serum samples were examined for clinical biochemistry. The metabolomics study of serum was also carried out using 1H NMR spectroscopy in combination with multivariate data analysis to explore differentiating serum metabolites and altered metabolic pathways. RESULTS: The ML leaf extract (400 mg/kg BW) treatment significantly increased insulin level and insulin sensitivity of obese diabetic rats, with concomitant decrease in glucose level and insulin resistance. Significant reduction in total triglyceride, cholesterol and low density lipoprotein was also observed after treatment. Interestingly, there was a significant increase in high density lipoprotein of the treated rats. A decrease in renal injury markers and activities of liver enzymes was also observed. Moreover, metabolomics studies clearly demonstrated that, ML extract significantly ameliorated the disturbance in glucose metabolism, tricarboxylic acid cycle, lipid metabolism, and amino acid metabolism. CONCLUSION: ML leaf extract exhibits potent antidiabetic properties, hence could be a useful and affordable alternative option for the management of T2DM.
Asunto(s)
Glucemia/metabolismo , Diabetes Mellitus Experimental/tratamiento farmacológico , Hipoglucemiantes/uso terapéutico , Resistencia a la Insulina , Lípidos/sangre , Fitoterapia , Rutaceae/química , Animales , HDL-Colesterol/sangre , Diabetes Mellitus Experimental/sangre , Diabetes Mellitus Experimental/etiología , Diabetes Mellitus Tipo 2/sangre , Diabetes Mellitus Tipo 2/tratamiento farmacológico , Diabetes Mellitus Tipo 2/etiología , Hipoglucemiantes/farmacología , Insulina/sangre , Riñón/efectos de los fármacos , Hígado/efectos de los fármacos , Hígado/enzimología , Masculino , Metabolómica , Obesidad/complicaciones , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Hojas de la Planta , Espectroscopía de Protones por Resonancia Magnética , Ratas Sprague-Dawley , Triglicéridos/sangreRESUMEN
BACKGROUND: Obesity is a major health concern both in developed and developing countries. The use of herbal medicines became the subject of interest for the management of obesity due to its natural origin, cost effectiveness and minimal side effects. The present study aimed at investigating anti-obesity potential of ethanolic extract from Cosmos caudatus Kunth leaf (EECCL). METHODS: In this study, the rats were randomly divided into six groups i.e., (1) Normal Diet (ND); (2) Normal Diet and 175 mg/kgBW of EECCL (ND + 175 mg/kgBW); (3) Normal Diet and 350 mg/kgBW of EECCL (ND + 350 mg/kgBW); (4) High Fat Diet (HFD); (5) High Fat Diet and 175 mg/kgBW of EECCL (HFD + 175 mg/kgBW); (6) High Fat Diet and 350 mg/kgBW of EECCL (HFD + 350 mg/kgBW). The anti-obesity potential was evaluated through analyses of changes in body weight, visceral fat weight, and blood biochemicals including total cholesterol, triglycerides, high-density lipoprotein cholesterol (HDL-c), low-density lipoprotein cholesterol (LDL-c), leptin, insulin, adiponectin, ghrelin and fecal fat content. In addition, metabolite profiling of EECCL was carried out using NMR spectroscopy. RESULTS: Rats receiving EECCL together with HFD showed significant (p < 0.05) reduction in body weight gain compared to rats receiving HFD only. At the end of study, the body weight gain of EECCL treated rats was not significantly (p > 0.05) different with those of ND rats. Other related obesity biomarkers including plasma lipid profiles, insulin, leptin, ghrelin and adiponectin levels also showed significant improvement (p < 0.05). Administration of EECCL caused significant (p < 0.05) increase in fecal fat excretion, which validates the hypothesis of lipase inhibition, an anti-obesity mechanism similar to standard drug of Orlistat. The 1H-NMR spectra of EECCL ascertained the presence of catechin, quercetin, rutin, kaempherol and chlorogenic acid in the extract. CONCLUSION: Conclusively, EECCL showed anti-obesity properties by inhibition of intestinal lipid absorption and modulation of adipocytes markers.
Asunto(s)
Fármacos Antiobesidad/farmacología , Asteraceae/química , Extractos Vegetales/farmacología , Animales , Fármacos Antiobesidad/aislamiento & purificación , Peso Corporal , Dieta Alta en Grasa , Ingestión de Alimentos , Malasia , Masculino , Ratas , Ratas Sprague-DawleyRESUMEN
Diabetes mellitus is normally characterized by chronic hyperglycemia associated with disturbances in the fat, carbohydrate, and protein metabolism. There is an increasing trend of using natural products instead of synthetic agents as alternative therapy for disorders due to their fewer side effects. In this study, antidiabetic and antioxidant activities of different Melicope lunu-ankenda (ML) ethanolic extracts were evaluated using inhibition of α-glucosidase and 2,2-diphenyl-l-picrylhydrazyl (DPPH) radicals scavenging activity, respectively; whereas, proton nuclear magnetic resonance ((1) H NMR) and ultra-high performance liquid chromatography-tandem mass spectrometric (UHPLC-MS/MS) techniques were used for metabolite profiling of ML leaf extracts at different concentrations of ethanol and water. Sixty percent of ethanolic ML extract showed highest inhibitory effect against α-glucosidase enzyme (IC50 of 37 µg/mL) and DPPH scavenging activity (IC50 of 48 µg/mL). Antidiabetic effect of ML extracts was also evaluated in vivo and it was found that the high doses (400 mg/Kg BW) of ML extract exhibited high suppression in fasting blood glucose level by 62.75%. The metabolites responsible for variation among ML samples with variable ethanolic levels have been evaluated successfully using (1) H-NMR-based metabolomics. The principal component analysis (PCA) and partial least squares(PLS) analysis scores depicted clear and distinct separations into 4 clusters representing the 4 ethanolic concentrations by PC1 and PC2, with an eigenvalue of 69.9%. Various (1) H-NMR chemical shifts related to the metabolites responsible for sample difference were also ascribed. The main bioactive compounds identified attributing toward the separation included: isorhamnetin, skimmianine, scopoletin, and melicarpinone. Hence, ML may be used as promising medicinal plant for the development of new functional foods, new generation antidiabetic drugs, as a single entity phytomedicine or in combinational therapy.
Asunto(s)
Antioxidantes/farmacología , Inhibidores de Glicósido Hidrolasas/farmacología , Hipoglucemiantes/farmacología , Extractos Vegetales/farmacología , Rutaceae/química , alfa-Glucosidasas/metabolismo , Animales , Antioxidantes/análisis , Compuestos de Bifenilo/metabolismo , Diabetes Mellitus/enzimología , Inhibidores de Glicósido Hidrolasas/análisis , Hipoglucemiantes/análisis , Masculino , Picratos/metabolismo , Extractos Vegetales/química , Hojas de la Planta/química , Ratas Sprague-Dawley , Espectrometría de Masas en Tándem , alfa-Glucosidasas/análisisRESUMEN
The current study was designed to check the antioxidant and enzyme inhibition potential of various extracts/ fractions of three selected plants. The aerial parts of Conocarpus erectus (Combretaceae), Ficus variegata (Moraceae) and Ficus maclellandii (Moraceae) were extracted with ethanol (95%) and the resulting crude extracts were partitioned with n-hexane, chloroform and n-butanol successively. Folin-Ciocalteu reagent was used to calculate the total phenolic contents, flavonoids contents were calculated with aluminum chloride while antioxidant and enzyme studies were carried out through standard protocols. All extracts/fractions contained reasonable amount of phenolic compounds ranging from 0.58-58.23 mg CE/g of DW and 0.43-30.56 mg GAE/g of DW. Total flavonoids were determined using rutin and quercetin standards, ranging from 2.65-18.2 mg rutin equivalent/g of dry weight and 0.92-5.41 mg quercetin equivalent/g of dry weight. Antioxidant studies such as DPPH inhibition FRAP and total antioxidant capacity (TAC) was checked. The crude ethanolic extract of C. erectus showed maximum antiradical scavenging power (90.43%; IC50=7 µg) and ferric reducing antioxidant power (16.5 µM eq.FeSO4.7H2O), respectively while leave extract of F. variegata (chloroform) was the most active (0.6577) in TAC among other extracts of the selected medicinal plants. Butanolic leave extract of C. erectus exhibited maximum enzyme inhibition activity (91.62% with IC50 40 µg/ml) while other extracts showed significant activity. It was observed from results that all extracts/fractions of under consideration plants, exhibited significant bioactivities especially ethanolic and butanolic fractions, which may be the richest source of such type of activities.
Asunto(s)
Antioxidantes/farmacología , Inhibidores de la Colinesterasa/farmacología , Combretaceae/química , Ficus/química , Extractos Vegetales/farmacología , Acetilcolinesterasa/metabolismo , Antioxidantes/aislamiento & purificación , Compuestos de Bifenilo/química , Inhibidores de la Colinesterasa/aislamiento & purificación , Relación Dosis-Respuesta a Droga , Compuestos Férricos/química , Proteínas Ligadas a GPI/antagonistas & inhibidores , Proteínas Ligadas a GPI/metabolismo , Humanos , Fitoterapia , Picratos/química , Componentes Aéreos de las Plantas , Extractos Vegetales/aislamiento & purificación , Plantas Medicinales , Solventes/químicaRESUMEN
Current study presents RSM based optimized production of biodiesel from palm oil using chemical and enzymatic transesterification. The emission behavior of biodiesel and its blends, namely, POB-5, POB-20, POB-40, POB-50, POB-80, and POB-100 was examined using diesel engine (equipped with tube well). Optimized palm oil fatty acid methyl esters (POFAMEs) yields were depicted to be 47.6 ± 1.5, 92.7 ± 2.5, and 95.4 ± 2.0% for chemical transesterification catalyzed by NaOH, KOH, and NaOCH3, respectively, whereas for enzymatic transesterification reactions catalyzed by NOVOZYME-435 and A. n. lipase optimized biodiesel yields were 94.2 ± 3.1 and 62.8 ± 2.4%, respectively. Distinct decrease in particulate matter (PM) and carbon monoxide (CO) levels was experienced in exhaust emissions from engine operating on biodiesel blends POB-5, POB-20, POB-40, POB-50, POB-80, and POB-100 comparative to conventional petroleum diesel. Percentage change in CO and PM emissions for different biodiesel blends ranged from -2.1 to -68.7% and -6.2 to -58.4%, respectively, relative to conventional diesel, whereas an irregular trend was observed for NOx emissions. Only POB-5 and POB-20 showed notable reductions, whereas all other blends (POB-40 to POB-100) showed slight increase in NOx emission levels from 2.6 to 5.5% comparative to petroleum diesel.