RESUMEN
This study investigated anti-viral, antioxidant activity and anti-pyretic of crude extract from Artemisia afra, Artemisia absinthium and Pittiosporum viridflorum leaves. The crude extracts were prepared by maceration using aqueous, methanol and dichloromethane respectively. Antiviral studies were evaluated with influenza virus using Fluorescence based - Neuraminidase inhibitors. Antioxidant activities determined with DPPH, Nitric oxide, hydroxyl and super oxide anion radicals' Anti-pyretic activities were evaluated using rats with yeast induced pyrexia. Total phenol, flavonoids, and pro-anthocyanin contents of the plants samples were evaluated using standard protocols. The crude extracts exhibited neuraminidase inhibitory activity against the influenza virus at different thresholds. Artemisia absinthiumaqueous extract showed the best activity against A/Sydney/5/97. Whereas Artemisia afra methanol crude extract displayed highest antioxidant potential against the tested antioxidant parameters. All the crude extracts significantly reversed yeast induced pyrexia in rats, similar to paracetamol. Thus, they could serve as natural remedy for respiratory diseases such as Influenza.
Este estudio investigó la actividad antiviral, antioxidante y antipirética del extracto crudo de hojas de Artemisia afra, Artemisia absinthium y Pittiosporum viridflorum. Los extractos crudos se prepararon mediante maceración utilizando metanol acuoso y diclorometano respectivamente. Los estudios antivirales se evaluaron con el virus de la influenza utilizando inhibidores de neuraminidasa basados en fluorescencia. Actividades antioxidantes determinadas con DPPH, radicales aniónicos de óxido nítrico, hidroxilo y superóxido. Las actividades antipiréticas se evaluaron utilizando ratas con pirexia inducida por levaduras. El contenido total de fenol, flavonoides y proantocianina de las muestras de plantas se evaluó utilizando protocolos estándar. Los extractos crudos mostraron actividad inhibidora de neuraminidasa contra el virus de la influenza en diferentes umbrales. El extracto acuoso de Artemisia absinthium mostró la mejor actividad contra A/Sydney/5/97. Mientras que el extracto crudo de Artemisia aframetanol mostró el mayor potencial antioxidante contra los parámetros antioxidantes probados. Todos los extractos crudos revirtieron significativamente la pirexia inducida por levaduras en ratas, similar al paracetamol. Por tanto, podrían servir como remedio natural para enfermedades respiratorias como la Influenza.
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Plantas Medicinales , Extractos Vegetales/biosíntesis , Mezclas Complejas/biosíntesis , Antivirales , Sudáfrica , Antipiréticos , AntioxidantesRESUMEN
Reactive oxygen species are implicated in multiple pathological conditions including erectile dysfunction. This study evaluated the in vitro and in vivo antioxidant potential of the methanolic extracts of Inula glomerata and Salacia kraussii. The plant materials were pulverized and extracted with methanol. The phytochemical analysis, ability of the crude extracts to scavenge free radicals (ABTS, DPPH, NO.) in vitroas well as the total phenolic and flavonoid contents was investigated. In vivo, antioxidant potentials of the crude extracts (50/250 mg/kg body weight) were determined in an erectile dysfunction rat model. The phytochemical analysis revealed that both plants contain flavonoids, tannins, terpenoids, and alkaloids. The crude extracts at varying degree of efficiency, scavenged ABTS and DPPH radicals. The crude extracts at low concentrations (50 mg/kg b.w) significantly (p<0.05) diminished the level of malondialdehyde, augmented catalase activities and elevated glutathione levels. However, SOD activities were significantly boosted in a dose-dependent manner by the crude extracts. Therefore, I. glomerataand S. kraussiipossess antioxidant properties, hence, can serve as a therapeutic modality in the treatment of oxidative stress-induced erectile dysfunction.
Las especies reactivas de oxígeno están implicadas en múltiples condiciones patológicas, incluyendo la disfunción eréctil. Este estudio evaluó el potencial antioxidante in vitro e in vivo de extractos metanólicos de Inula glomeratay Salacia kraussii. Los materiales vegetales fueron pulverizados y extraídos con metanol. A estos extractos crudos se les llevó a cabo el análisis fitoquímico junto con el contenido total de fenólicos y flavonoides, así como se les investigó la capacidad in vitro para atrapar radicales (ABTS, DPPH, NO.). Los potenciales antioxidantes in vivo de los extractos crudos (50/250 mg/kg de peso corporal) se determinaron en un modelo en ratas con disfunción eréctil. El análisis fitoquímico reveló que ambas plantas contuvieron flavonoides, taninos, terpenoides y alcaloides. Los extractos crudos con un grado variable de eficiencia, atraparon a los radicales ABTS y DPPH. Los extractos crudos a bajas concentraciones (50 mg/kg p.c) significativamente (p<0.05) disminuyeron el nivel de malondialdehído, aumentaron las actividades de catalasa y elevaron los niveles de glutatión. Sin embargo, las actividades de SOD por los extractos crudos fueron significativamente dosis-dependientes. Así, los extractos de I. glomeratay S. kraussii mostraron propiedades antioxidantes, y por lo tanto, podrían servir como una alternativa terapéutica en el tratamiento de disfunción eréctil inducida por estrés oxidativo.
Asunto(s)
Animales , Ratas , Extractos Vegetales/farmacología , Extractos Vegetales/química , Inula/química , Salacia/química , Antioxidantes/farmacología , Antioxidantes/química , Ácidos Sulfónicos/metabolismo , Flavonoides/análisis , Especies Reactivas de Oxígeno , Ratas Sprague-Dawley , Estrés Oxidativo/efectos de los fármacos , Asteraceae/química , Celastraceae/química , Benzotiazoles/metabolismo , Compuestos Fenólicos/análisis , Fitoquímicos/análisis , Óxido Nítrico/metabolismoRESUMEN
BACKGROUND: Hyperglycemia-induced cardiovascular dysfunction has been linked to oxidative stress and accelerated apoptosis in the diabetic myocardium. While there is currently no treatment for diabetic cardiomyopathy (DCM), studies suggest that the combinational use of anti-hyperglycemic agents and triterpenes could be effective in alleviating DCM. HYPOTHESIS: To investigate the therapeutic effect of methyl-3ß-hydroxylanosta-9,24-dien-21-oate (RA3), in the absence or presence of the anti-diabetic drug, metformin (MET), against hyperglycemia-induced cardiac injury using an in vitro H9c2 cell model. METHODS: To mimic a hyperglycemic state, H9c2 cells were exposed to high glucose (HG, 33 mM) for 24 h. Thereafter, the cells were treated with RA3 (1 µM), MET (1 µM) and the combination of MET (1 µM) plus RA3 (1 µM) for 24 h, to assess the treatments therapeutic effect. RESULTS: Biochemical analysis revealed that RA3, with or without MET, improves glucose uptake via insulin-dependent (IRS-1/PI3K/Akt signaling) and independent (AMPK) pathways whilst ameliorating the activity of antioxidant enzymes in the H9c2 cells. Mechanistically, RA3 was able to alleviate HG-stimulated oxidative stress through the inhibition of reactive oxygen species (ROS) and lipid peroxidation as well as the reduced expression of the PKC/NF-кB cascade through decreased intracellular lipid content. Subsequently, RA3 was able to mitigate HG-induced apoptosis by decreasing the activity of caspase 3/7 and DNA fragmentation in the cardiomyoblasts. CONCLUSION: RA3, in the absence or presence of MET, demonstrated potent therapeutic properties against hyperglycemia-mediated cardiac damage and could be a suitable candidate in the prevention of DCM.
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Apoptosis/efectos de los fármacos , Metabolismo Energético , Hiperglucemia/patología , Lanosterol/análogos & derivados , Miocitos Cardíacos/efectos de los fármacos , Estrés Oxidativo/efectos de los fármacos , Animales , Antioxidantes/farmacología , Caspasas , Línea Celular , Cardiomiopatías Diabéticas , Glucosa/metabolismo , Insulina/metabolismo , Lanosterol/farmacología , Metformina/farmacología , Fosfatidilinositol 3-Quinasas/metabolismo , Ratas , Especies Reactivas de Oxígeno/metabolismo , Transducción de Señal/efectos de los fármacosRESUMEN
Aspalathin is a rooibos flavonoid with established blood glucose lowering properties, however, its efficacy to moderate complications associated with hepatic insulin resistance is unknown. To study such effects, C3A liver cells exposed to palmitate were used as a model of hepatic insulin resistance. These hepatocytes displayed impaired substrate metabolism, including reduced glucose transport and free fatty acid uptake. These defects included impaired insulin signaling, evident through reduced phosphatidylinositol-4,5-bisphosphate 3-kinase/ protein kinase B (PI3K/AKT) protein expression, and mitochondrial dysfunction, depicted by a lower mitochondrial respiration rate. Aspalathin was able to ameliorate these defects by correcting altered substrate metabolism, improving insulin signaling and mitochondrial bioenergetics. Activation of 5'-adenosine monophosphate-activated protein kinase (AMPK) may be a plausible mechanism by which aspalathin increases hepatic energy expenditure. Overall, these results encourage further studies assessing the potential use of aspalathin as a nutraceutical to improve hepatocellular energy expenditure, and reverse metabolic disease-associated complications.
Asunto(s)
Chalconas/farmacología , Metabolismo Energético/efectos de los fármacos , Mitocondrias/efectos de los fármacos , Proteínas Quinasas Activadas por AMP/metabolismo , Glucemia/metabolismo , Línea Celular , Chalconas/metabolismo , Glucosa/metabolismo , Hepatocitos/metabolismo , Humanos , Hipoglucemiantes/farmacología , Insulina/metabolismo , Resistencia a la Insulina/fisiología , Hígado/metabolismo , Mitocondrias/metabolismo , Modelos Biológicos , Palmitatos/metabolismo , Fosfatidilinositol 3-Quinasas/metabolismo , Proteínas Proto-Oncogénicas c-akt/metabolismo , Transducción de Señal/efectos de los fármacosRESUMEN
We previously demonstrated that an aspalathin-enriched green rooibos extract (GRE) reversed palmitate-induced insulin resistance in C2C12 skeletal muscle and 3T3-L1 fat cells by modulating key effectors of insulin signalling such as phosphatidylinositol-4,5-bisphosphate 3-kinase/protein kinase B (PI3K/AKT) and AMP-activated protein kinase (AMPK). However, the effect of GRE on hepatic insulin resistance is unknown. The effects of GRE on lipid-induced hepatic insulin resistance using palmitate-exposed C3A liver cells and obese insulin resistant (OBIR) rats were explored. GRE attenuated the palmitate-induced impairment of glucose and lipid metabolism in treated C3A cells and improved insulin sensitivity in OBIR rats. Mechanistically, GRE treatment significantly increased PI3K/AKT and AMPK phosphorylation while concurrently enhancing glucose transporter 2 expression. These findings were further supported by marked stimulation of genes involved in glucose metabolism, such as insulin receptor (Insr) and insulin receptor substrate 1 and 2 (Irs1 and Irs2), as well as those involved in lipid metabolism, including Forkhead box protein O1 (FOXO1) and carnitine palmitoyl transferase 1 (CPT1) following GRE treatment. GRE showed a strong potential to ameliorate hepatic insulin resistance by improving insulin sensitivity through the regulation of PI3K/AKT, FOXO1 and AMPK-mediated pathways.
Asunto(s)
Proteínas Quinasas Activadas por AMP/genética , Chalconas/farmacología , Hiperglucemia/tratamiento farmacológico , Hipoglucemiantes/farmacología , Resistencia a la Insulina , Fosfatidilinositol 3-Quinasas/genética , Proteínas Proto-Oncogénicas c-akt/genética , Células 3T3 , Proteínas Quinasas Activadas por AMP/metabolismo , Animales , Aspalathus/química , Carnitina O-Palmitoiltransferasa/genética , Carnitina O-Palmitoiltransferasa/metabolismo , Línea Celular , Chalconas/aislamiento & purificación , Dieta Alta en Grasa/efectos adversos , Azúcares de la Dieta/efectos adversos , Regulación de la Expresión Génica , Hepatocitos/citología , Hepatocitos/efectos de los fármacos , Hepatocitos/metabolismo , Hiperglucemia/etiología , Hiperglucemia/genética , Hiperglucemia/metabolismo , Hipoglucemiantes/aislamiento & purificación , Proteínas Sustrato del Receptor de Insulina/genética , Proteínas Sustrato del Receptor de Insulina/metabolismo , Masculino , Ratones , Fibras Musculares Esqueléticas/citología , Fibras Musculares Esqueléticas/efectos de los fármacos , Fibras Musculares Esqueléticas/metabolismo , Proteínas del Tejido Nervioso/genética , Proteínas del Tejido Nervioso/metabolismo , Ácido Palmítico/farmacología , Fosfatidilinositol 3-Quinasas/metabolismo , Fosforilación/efectos de los fármacos , Extractos Vegetales/química , Proteínas Proto-Oncogénicas c-akt/metabolismo , Ratas , Ratas Wistar , Receptor de Insulina/genética , Receptor de Insulina/metabolismo , Transducción de SeñalRESUMEN
The epidemic of cardiovascular diseases is a global phenomenon that is exaggerated by the growing prevalence of diabetes mellitus. Coronary artery disease and diabetic cardiomyopathy are the major cardiovascular complications responsible for exacerbated myocardial infarction in diabetic individuals. Increasing research has identified hyperglycemia and hyperlipidemia as key factors driving the augmentation of oxidative stress and a pro-inflammatory response that usually results in increased fibrosis and reduced cardiac efficiency. While current antidiabetic agents remain active in attenuating diabetes-associated complications, overtime, their efficacy proves limited in protecting the hearts of diabetic individuals. This has led to a considerable increase in the number of natural products that are screened for their antidiabetic and cardioprotective properties. These natural products may present essential ameliorative properties relevant to their use as a monotherapy or as an adjunct to current drug agents in combating diabetes and its associated cardiovascular complications. Recent findings have suggested that triterpenes isolated from Protorhus longifolia (Benrh.) Engl., a plant species endemic to Southern Africa, display strong antioxidant and antidiabetic properties that may potentially protect against diabetes-induced cardiovascular complications. Thus, in addition to discussing the pathophysiology associated with diabetes-induced cardiovascular injury, available evidence pertaining to the cardiovascular protective potential of lanosteryl triterpenes from Protorhus longifolia will be discussed.
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Anacardiaceae/química , Cardiotónicos/farmacología , Hipoglucemiantes/farmacología , Hipolipemiantes/farmacología , Lanosterol/análogos & derivados , Extractos Vegetales/farmacología , Animales , Cardiotónicos/uso terapéutico , Enfermedad de la Arteria Coronaria/etiología , Enfermedad de la Arteria Coronaria/metabolismo , Complicaciones de la Diabetes , Diabetes Mellitus/tratamiento farmacológico , Diabetes Mellitus/metabolismo , Cardiomiopatías Diabéticas/etiología , Cardiomiopatías Diabéticas/metabolismo , Modelos Animales de Enfermedad , Humanos , Hipoglucemiantes/uso terapéutico , Hipolipemiantes/uso terapéutico , Lanosterol/farmacología , Lanosterol/uso terapéutico , Fitoterapia/métodos , Extractos Vegetales/uso terapéutico , RatasRESUMEN
Accumulative evidence shows that chronic hyperglycaemia is a major factor implicated in the development of pancreatic ß-cell dysfunction in diabetic patients. Furthermore, most of these patients display impaired insulin signalling that is responsible for accelerated pancreatic ß-cell damage. Indeed, prominent pathways involved in glucose metabolism such as phosphatidylinositol 3-kinase/ protein kinase B (PI3-K/AKT) and 5' AMP-activated protein kinase (AMPK) are impaired in an insulin resistant state. The impairment of this pathway is associated with over production of reactive oxygen species and pro-inflammatory factors that supersede pancreatic ß-cell damage. Although several antidiabetic drugs can improve ß-cell function by modulating key regulators such as PI3-K/AKT and AMPK, evidence of their ß-cell regenerative and protective effect is scanty. As a result, there has been continued exploration of novel antidiabetic therapeutics with abundant antioxidant and antiinflammatory properties that are essential in protecting against ß-cell damage. Such therapies include triterpenes, which have displayed robust effects to improve glycaemic tolerance, insulin secretion, and pancreatic ß-cell function. This review summarises most relevant effects of various triterpenes on improving pancreatic ß-cell function in both in vitro and in vivo experimental models. A special focus falls on studies reporting on the ameliorative properties of these compounds against insulin resistance, oxidative stress and inflammation, the well-known factors involved in hyperglycaemia associated tissue damage.
Asunto(s)
Hipoglucemiantes/uso terapéutico , Células Secretoras de Insulina/efectos de los fármacos , Triterpenos/uso terapéutico , Animales , Diabetes Mellitus/tratamiento farmacológico , Humanos , Resistencia a la Insulina , Estrés Oxidativo/efectos de los fármacosRESUMEN
BACKGROUND: Malaria continues to be a global burden as the efficacy of most commercial anti-malarial drugs has been compromised by the evolution of parasite resistance. With the urgent need created for the development of alternative and more efficient anti-malarial drugs, this study focused on the evaluation of anti-malarial agents of the Warburgia salutaris stem bark. METHODS: The stem bark was extracted with dichloromethane followed by silica gel column chromatography that led to the isolation of iso-mukaadial acetate, a drimanoid sesquiterpene. This compound was characterized by spectroscopic analysis (1H NMR, 13C NMR, IR and MS), and its structure was confirmed by X-ray crystallography. In vitro anti-plasmodial activity was investigated using a chloroquine sensitive NF54 Plasmodium falciparum strain. Cytotoxicity was measured using the MTT assay on HEK239 and HEPG2 cell lines. Chloroquine-sensitive Plasmodium berghei was used to infect Sprague-Dawley rats for in vivo studies. The W. salutaris crude extract and iso-mukaadial acetate were administered orally at 0.5; 1.5, 2.5 and 5 mg/kg, chloroquine was used as the reference drug. Determination of percentage parasitaemia, haematological parameters, and rat body weights was done throughout the experimental study period. RESULTS: The crude extract and iso-mukaadial acetate showed very good activity on the inhibition of parasite growth (IC50 0.01 ± 0.30 µg/ml) and (IC50 0.44 ± 0.10 µg/ml), respectively, with iso-mukaadial acetate having cytotoxicity activity of 36.7 ± 0.8 and 119.2 ± 8.8 (µg/ml) on HEK293 and HEPG2 cells, respectively. The crude extract and iso-mukaadial acetate reduced percentage parasitaemia in a dose-dependent manner in comparison to the control. There were no significant differences in the haematological parameters in all the experimental groups in comparison to control group. This study proves that W. salutaris contains components (including iso-mukaadial acetate) that exhibit anti-malarial activity. This study scientifically validates the use of this plant in folk medicine. CONCLUSIONS: This study proves that Warburgia salutaris contains components (including iso-mukaadial acetate) that exhibit anti-malarial activity and scientifically validates the use of this plant in folk medicine.
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Antimaláricos/farmacología , Magnoliopsida/química , Plasmodium berghei/efectos de los fármacos , Plasmodium falciparum/efectos de los fármacos , Sesquiterpenos/farmacología , Animales , Relación Dosis-Respuesta a Droga , Células HEK293 , Humanos , Masculino , Medicinas Tradicionales Africanas , Corteza de la Planta/química , Extractos Vegetales/aislamiento & purificación , Tallos de la Planta/química , Sesquiterpenos Policíclicos , Ratas , Ratas Sprague-DawleyRESUMEN
Type 2 diabetes remains one of the leading causes of death worldwide. Persistent hyperglycemia within a diabetic state is implicated in the generation of oxidative stress and aggravated inflammation that is responsible for accelerated modification of pancreatic beta cell structure. Here we investigated whether a lanosteryl triterpene, methyl-3ß-hydroxylanosta-9,24-dien-21-oate (RA-3), isolated from Protorhus longifolia can improve glucose tolerance and pancreatic beta cell ultrastructure by reducing oxidative stress and inflammation in high fat diet and streptozotocin-induced type 2 diabetes in rats. In addition to impaired glucose tolerance, the untreated diabetic rats showed increased fasting plasma glucose and C-peptide levels. These untreated diabetic rats further demonstrated raised cholesterol, interleukin-6 (IL-6), and lipid peroxidation levels as well as a destroyed beta cell ultrastructure. Treatment with RA-3 was as effective as metformin in improving glucose tolerance and antioxidant effect in the diabetic rats. Interestingly, RA-3 displayed a slightly more enhanced effect than metformin in reducing elevated IL-6 levels and in improving beta cell ultrastructure. Although the involved molecular mechanisms remain to be established, RA-3 demonstrates a strong potential to improve pancreatic beta cell ultrastructure by attenuating impaired glucose tolerance, reducing oxidative stress and inflammation.
Asunto(s)
Anacardiaceae/química , Antioxidantes/farmacología , Diabetes Mellitus Tipo 2/tratamiento farmacológico , Hipoglucemiantes/farmacología , Células Secretoras de Insulina/efectos de los fármacos , Lanosterol/análogos & derivados , Triterpenos/química , Animales , Glucemia , Diabetes Mellitus Tipo 2/inducido químicamente , Diabetes Mellitus Tipo 2/patología , Dieta Alta en Grasa , Glucosa/metabolismo , Prueba de Tolerancia a la Glucosa , Hiperglucemia/tratamiento farmacológico , Inflamación/tratamiento farmacológico , Insulina/metabolismo , Células Secretoras de Insulina/ultraestructura , Interleucina-6/metabolismo , Lanosterol/química , Lanosterol/aislamiento & purificación , Lanosterol/metabolismo , Estrés Oxidativo/efectos de los fármacos , Extractos Vegetales/química , Ratas Sprague-Dawley , Estreptozocina , Triterpenos/aislamiento & purificación , Triterpenos/farmacologíaRESUMEN
BACKGROUND: Tuberculosis is counted amongst the most infectious and lethal illnesses worldwide and remains one of the major threats to human health. The aim of the current study was to isolate and characterize anti-mycobacterial compounds present in Curtisia dentata (Burm.f.) C.A.Sm , a medicinal plant reportedly used in the treatment of tuberculosis, stomach ailments and sexually transmitted infections. METHODS: The bioassay guided principle was followed to isolate the anti-mycobacterial compounds. The crude ethanol extracts of the leaves was partitioned with various solvents four compounds such as ß-sitosterol, betulinic acid, ursolic acid and lupeol were successfully isolated. The compounds and their derivatives were evaluated for anti-mycobacterial activity using Microplate Alamar Blue Assay (MABA) against Mycobacterium tuberculosis H37RV (ATCC 27294). Furthermore, the derivatives were investigated for their toxicity against HepG2 and HEK293 using the MTT assay. RESULTS: The methanol fraction had the lowest minimum inhibitory concentration (MIC) of 22.2 µg/ml against the selected Mycobacterium strain when compared to other fractions. Ursolic acid acetate (UAA) was the most active compound with MIC value of 3.4 µg/ml. The derivatives had varying degrees of toxicity, but were generally non-toxic to the selected cell lines. Derivatives also exhibited highest selectivity index and offers a higher safety margin. CONCLUSIONS: The derivatives had better antimicrobial activity and low cytotoxic effects compared to isolated compounds. These increased their selectivity. It appears that acetylation of both betulinic acid and ursolic acid increased their activity against the selected Mycobacterium species. The results obtained in this study gives a clear indication that Curtisia dentata may serve as major source of new alternative medicines that may be used to treat TB. Furthermore, there is a need to explore the activity of these tested plant against other pathogenic Mycobacterium species.
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Antibacterianos/química , Antibacterianos/farmacología , Magnoliopsida/química , Extractos Vegetales/química , Extractos Vegetales/farmacología , Antibacterianos/aislamiento & purificación , Supervivencia Celular/efectos de los fármacos , Células HEK293 , Humanos , Pruebas de Sensibilidad Microbiana , Mycobacterium tuberculosis/efectos de los fármacos , Extractos Vegetales/aislamiento & purificación , Hojas de la Planta/químicaRESUMEN
The traditional use of medicinal plants in the management of sexual dysfunctions has a long history. This study investigated testicular dysfunction ameliorative effect of the methanolic roots extracts of Maytenus procumbens and Ozoroa paniculosa in a butanol-induced testicular dysfunction rat model. The rats in respective experimental groups were orally administered with the extract at 50 and 250 mg/kg bw, daily for 28 days. The cytotoxicity of the extracts was evaluated against HEK293, MCF-7, and HT29 cell lines. The extracts exhibited moderate (LC50 30.3-330.2 µg/mL) to weak (LC50 200.8-438.4 µg/mL) cytotoxicity level on the cancer and normal cells, respectively. While relatively lower serum testosterone levels and total sperm count along with decreased numbers of spermatogonia were noted in the untreated group, all these parameters were improved in the groups treated with the extracts at 250 mg/kg. Improved histomorphological changes of the testes were also observed when compared to the untreated group. While the extracts (at 250 mg/kg) increased serum reduced glutathione content and decreased malondialdehyde content, a relatively higher serum creatinine level was also observed in the treated animals group. The results indicate that the two plant extracts have potential to ameliorate testicular dysfunction.
RESUMEN
CONTEXT: The current rapid increase in the incidence of cardiovascular events indicates a need for the discovery of more effective cardioprotective agents. OBJECTIVE: This study evaluated the cardioprotective potential of a lanosteryl triterpene from Protorhus longifolia (Benrh.) Engl. stem bark. MATERIALS AND METHODS: Spectroscopic data analysis was used to confirm the structure of methyl-3ß-hydroxylanosta-9, 24-dien-21-oate (RA-3). The cardioprotective effect of RA-3 in isoproterenol-induced myocardial injury in hyperlipidemic rats was investigated. Rats were divided into the normal diet (ND) fed and high fat diet (HFD) fed groups. The HFD rats were further subdivided into three groups. The experimental group was orally administered with RA-3 (100 mg/kg) for 15 days. The rats were then injected with isoproterenol (85 mg/kg) to induce myocardial injury. At the end of the experiment, hearts and blood tissues were collected and used for histology and biochemical assays, respectively. RESULTS: RA-3 exhibited a cardioprotective effect as it minimized myocardial injury in HFD rats. Few lesions of acute hyaline degeneration and reduced fat deposition were observed in the heart tissue of the triterpene pretreated rats. Lactate dehydrogenase (LDH) activity was decreased in the blood of the RA-3 pretreated rats (44.1 mU/mL) compared to the untreated group (64.8 mU/mL). Increased glutathione (GSH) content and catalase (CAT) activity along with lower levels of malondialdehyde (MDA) in the triterpene pretreated animals (120.8 nmol/µL) than in the non-treated HFD fed rats (143.6 nmol/µL) were also observed. DISCUSSION AND CONCLUSION: The cardioprotective effect exhibited by RA-3 indicates its potential use in the management of cardiovascular diseases (CVD) and related health problems.
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Anacardiaceae , Cardiotónicos/farmacología , Lanosterol/farmacología , Extractos Vegetales/farmacología , Triterpenos/farmacología , Animales , Cardiotónicos/aislamiento & purificación , Dieta Alta en Grasa/efectos adversos , Corazón/efectos de los fármacos , Lanosterol/aislamiento & purificación , Miocardio/metabolismo , Miocardio/patología , Corteza de la Planta , Extractos Vegetales/aislamiento & purificación , Tallos de la Planta , Ratas , Ratas Sprague-Dawley , Triterpenos/aislamiento & purificaciónRESUMEN
Essential oils hydrodistilled from the rhizomes of Cyperus papyrus L. growing wild in two localities (KwaDlangezwa and Richards Bay) of uMhlathuze City, KwaZulu-Natal Province, South Africa has been studied. The major components of KwaDlangezwa oil were caryophyllene oxide (12.7 percent), cyperene (10.2 percent) and 1,8-cineole (8.4 percent). The oil of Richards Bay comprised mainly of caryophyllene oxide (24.4 percent), humulene epoxide II (13.2 percent), aristolene (9.1 percent) and aromadendrene epoxide II (7.3 percent). The antibacterial activity of the oils was assayed using agar-disc diffusion and broth-microdilution methods. The minimum inhibitory concentration (MIC) revealed that the oil samples inhibited the growth of Staphylococcus aureus (ATCC 3983 and ATCC 6538), with MIC of 1.25 and 0.31 mg/mL for each oil. Streptococcus faecalis (ATCC 29212; MIC of 1.25 and 0.6 mg/mL, respectively) and Escherichia coli (ATCC 4983; MIC of 1.25 mg/mL for both oils). Only the Richard Bay oil showed activity against Bacillus cereus and Bacillus pumilus with MIC of 1.25mg/mL, respectively.
Los aceites esenciales hidrodestilados de los rizomas de Cyperus papyrus L., que crecen en dos localidades (KwaDlangezwa y Bahía Richard) de la ciudad de uMhlathuze, la provincia KwaZulu-Natal, de Sudafrica han sido estudiados. Los mayores componentes del aceite de KwaDlangezwa fueron óxido de cariofileno (12,7 por ciento), cipereno (10,2 por ciento) y 1,8-cineol (8,4 por ciento). El aceite de la bahía de Richard consistió principalmente cariofileno (24,4 por ciento), epóxido II de humuleno (13,2 por ciento), aristoleno (9,1 por ciento) y epóxido II de aromandreno (7,3 por ciento). La actividad antibacterial de los aceites fueron ensayados utilizando la difusión en discos de agar y el método de microdilución en caldo. La concentración mínima inhibitoria (CMI) reveló que las muestras inhibieron el crecimiento de Staphylococcus aureus (ATCC 3983 y ATCC 6538), con una MIC de 1,25 y 0,31 mg/ml de cada aceite. Streptococcus faecalis (ATCC 29212; CMI de 1,25 y 0.6 mg/mL, respectivamente) y Escherichia coli (ATCC 4983; CMI de 1,25 mg/mL para ambos aceites). Solo el aceite de la bahía Richard mostró actividad contra Bacillus cereus y Bacillus pumilis con CMI de 1,25 mg/mL, respectivamente.
Asunto(s)
Antibacterianos/farmacología , Bacterias , Cyperus/química , Aceites Volátiles/química , Aceites Volátiles/farmacología , Antibacterianos/química , Cromatografía de Gases , Enterococcus faecalis , Escherichia coli , Pruebas de Sensibilidad Microbiana , Rizoma/química , Staphylococcus aureus , Sesquiterpenos/análisisRESUMEN
Control of postprandial hyperglycemia is crucial in the management of diabetes mellitus. Despite the use of the current hypoglycemic drugs, incidence of diabetes and related diseases continue to increase. This study aimed at evaluating the in vivo antihyperglycemic activity of methyl-3ß-hydroxylanosta-9,24-dien-21-oate (RA-3), a lanosteryl triterpene isolated, and characterized from Protorhus longifolia stem bark. Spectroscopic data analysis was used to establish and verify the structure of the triterpene. The antihyperglycemic activity of the triterpene was evaluated in an STZ-induced diabetes rat model. The experimental animals were orally administered with RA-3 (100 mg/kg body weight) daily for 14 days. An oral glucose tolerance test was also performed. The animals were euthanized and biochemical analysis of antioxidant status, some glycolytic enzymes and glycogen content were conducted on serum and liver samples, respectively. RA-3 exhibited hypoglycemic activity by reducing blood glucose levels by 37%. The triterpene also improved glucose tolerance in the diabetic rats. Relatively higher hepatic glycogen content, hexokinase and glucokinase activity with a decrease in glucose-6-phosphatase activity were observed in the triterpene-treated diabetic group when compared with the diabetic control group. The triterpene treatment further increased antioxidant status of the diabetic animals; increased activity of superoxide dismutase and catalase were observed along with a decrease in malondialdehyde content. The results indicate potential pharmaceutical effects of lanosteryl triterpene in the management of diabetes mellitus.
Asunto(s)
Anacardiaceae/química , Antihipertensivos , Diabetes Mellitus Experimental/tratamiento farmacológico , Hipertensión/tratamiento farmacológico , Lanosterol , Triterpenos , Animales , Antihipertensivos/química , Antihipertensivos/aislamiento & purificación , Antihipertensivos/farmacología , Femenino , Hipertensión/inducido químicamente , Lanosterol/química , Lanosterol/aislamiento & purificación , Lanosterol/farmacología , Masculino , Ratas , Ratas Sprague-Dawley , Triterpenos/química , Triterpenos/aislamiento & purificación , Triterpenos/farmacologíaRESUMEN
This paper reports on the compounds identified in the leaf and flower essential oils obtained by hydrodistillation of Plumeria alba L. (Apocynaceae) grown in Nigeria. The chemical analysis of the essential oils was achieved by means of gas chromatography (GC) and gas chromatography coupled with mass spectrometry (GC-MS). Linalool (13.2%), n-nonanal (9.6%), phenyl acetaldehyde (8.5%), neryl acetone (5.3%) and n-decanal (5.1%) were the main constituents of the leaf oil. On the other hand, the flower oil comprised mainly of limonene (9.1%), linalool (7.9%), α-cedrene (8.0%), caryophyllene oxide (7.9%) and (E, E)-α-farnesene (6.6%). This is the first report on the essential oil constituents of P. alba.
Asunto(s)
Apocynaceae/química , Flores/química , Aceites Volátiles/análisis , Hojas de la Planta/química , Monoterpenos Acíclicos , Ciclohexenos/análisis , Cromatografía de Gases y Espectrometría de Masas , Limoneno , Monoterpenos/análisis , Nigeria , Sesquiterpenos Policíclicos , Sesquiterpenos/análisis , Terpenos/análisisRESUMEN
Two lanostane triterpenes, 3ß-hydroxylanosta-9,24-dien-21-oic acid (1) and methyl-3ß-hydroxylanosta-9,24-dien-21-oate (2), were isolated from the stem bark of Protorhus longifolia. Their structures were deduced on the basis of spectroscopic analysis (NMR, HRMS, IR). This study investigated the in vitro anti-adipogenic activity of the two triterpenes. Their inhibitory activity was evaluated on selected lipid digestive enzymes (pancreatic lipase and cholesterol esterase). The inhibitory activity of the compounds on hormone-sensitive lipase and their ability to bind bile acids were also evaluated. The effect of the compounds on glucose uptake in C2C12 muscle cells and 3T3-L1 adipocytes, and on triglyceride accumulation in 3T3-L1 adipocytes was investigated. The triterpenes effectively inhibited the activities of the enzymes with IC50 values ranging from 0.04 to 0.31 mg/mL. The compounds showed a high affinity for secondary bile acids. Both compounds stimulated glucose uptake in C2C12 muscle cells and 3T3-L1 adipocytes. Compound 1 significantly reduced triglyceride accumulation in mature differentiated 3T3-L1 adipocytes. It is apparent that these lanostane triterpenes enhance glucose uptake and suppress adipogenesis, which together with their inhibitory effects on lipid digestive enzymes suggests that they have antihyperlipidemic potential.
Asunto(s)
Anacardiaceae/química , Hipolipemiantes/química , Hipolipemiantes/farmacología , Lanosterol/análogos & derivados , Triterpenos/farmacología , Células 3T3-L1/efectos de los fármacos , Animales , Ácidos y Sales Biliares/metabolismo , Línea Celular , Relación Dosis-Respuesta a Droga , Evaluación Preclínica de Medicamentos/métodos , Inhibidores Enzimáticos/farmacología , Glucosa/metabolismo , Lanosterol/química , Lanosterol/farmacología , Metabolismo de los Lípidos/efectos de los fármacos , Masculino , Ratones , Estructura Molecular , Corteza de la Planta/química , Ratas Sprague-Dawley , Esterol Esterasa/antagonistas & inhibidores , Esterol Esterasa/metabolismo , Triterpenos/químicaRESUMEN
BACKGROUND: Hyperlipidemia, a metabolic disorder of lipids, is a well known risk factor of cardiovascular events and metabolic syndrome. In this study, the in vivo lipid-lowering activity of the triterpene (Methyl-3ß-hydroxylanosta-9,24-dien-21-oate), isolated from the stem bark of Protorhus longifolia, in high fat diet (HFD)-induced hyperlipidemic rats was investigated. METHODS: Structure of the isolated compound was established and confirmed based on spectral (NMR, HRMS, IR) data analysis. Rats were divided into two groups; normal group (fed the normal commercial rats' chow) and the HFD group. After 21 days of experimental period on their respective diets, the HFD rats were sub-divided into 4 groups of six rats per group. Two of the HFD groups were orally treated with the triterpene (100 and 200 mg/kg body weight) for 15 days. At the end of the experimental periods, the rats were sacrificed and blood samples were collected for biochemical assays. RESULTS: The results show that there were significant increases in total serum cholesterol (TC, 15.72 mmol/L) and low-density lipoprotein cholesterol (LDL-c, 7.41 mmol/L) with a reduction in high-density lipoprotein cholesterol (HDL-c, 14.75 mmol/L) in HFD-induced hyperlipidemic rats after 21 days. Oral administration of the triterpene (100 mg/kg.bw and 200 mg/kg.bw) for a period of 15 days resulted in significant lowering of the levels of TC (7.51 mmol/L) and LDL-c (4.46 mmol/L) with an increase in HDL-c (47.3 mmol/L) in HFD-induced hyperlipidemic rats. Significant decrease in atherogenic index and coronary risk index by the triterpene was observed in HFD-induced hyperlipidemic rats. CONCLUSIONS: The triterpene could effectively reduce or control the amount of serum cholesterol and LDL. It is apparent that the compound could contribute to new formulation with significant hypolipidemic effects.
Asunto(s)
Hipolipemiantes/farmacología , Lanosterol/análogos & derivados , Magnoliopsida/química , Extractos Vegetales/farmacología , Animales , Aterosclerosis/etiología , Aterosclerosis/prevención & control , Enfermedad Coronaria/etiología , Enfermedad Coronaria/prevención & control , Dieta Alta en Grasa/efectos adversos , Evaluación Preclínica de Medicamentos , Hiperlipidemias/tratamiento farmacológico , Hiperlipidemias/etiología , Hipolipemiantes/uso terapéutico , Lanosterol/farmacología , Lanosterol/uso terapéutico , Hígado/efectos de los fármacos , Hígado/enzimología , Hígado/patología , Tamaño de los Órganos/efectos de los fármacos , Corteza de la Planta/química , Extractos Vegetales/uso terapéutico , Tallos de la Planta/química , Ratas Sprague-Dawley , Factores de RiesgoRESUMEN
BACKGROUND: Listeriosis is a fatal disease caused by pathogenic Listeria bacteria and it is most prevalent in immune-compromised individuals. The increase in numbers of immune-compromised individuals against a background of Listeria antibiotic resistance, limits listeriosis treatment options. This therefore calls for research into substitute treatments, of which, medicinal plants derived compounds offer a viable alternative. METHODS: The broth microdilution assay was used to determine the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of three plant triterpenes namely 3ß-hydroxylanosta-9,24-dien-21-oic acid, methyl-3ß-hydroxylanosta-9,24-dien-21-oate and 3ß-acetylursolic acid, against Listeria monocytogenes, Listeria ivanovii and Listeria grayi species. The chequerboard method was used to assess the interactions between the triterpenes and conventional antibiotics: ampicillin, neomycin, gentamicin and penicillin G. The lactate dehydrogenase membrane damage method was used to assess the triterpenes' membrane damaging potentials against the Listeria bacteria. RESULTS: The triterpenes' MIC values were found to range from 0.185 to 1.67 mg/ml while, the MBC determination assay results revealed that the test triterpenes were bacteriostatic against the Listeria bacteria. The interactions involving 3ß-hydroxylanosta-9,24-dien-21-oic acid were mainly additive with ampicillin and synergistic with neomycin, gentamicin and penicillin G. The interactions involving methyl-3ß-hydroxylanosta-9,24-dien-21-oate were mainly antagonistic with ampicillin, indifferent with neomycin, ranging from synergistic to indifference with gentamicin and synergistic with penicillin G. The interactions involving 3ß-acetylursolic acid were mainly indifferent with ampicillin, synergistic with neomycin and gentamicin while ranging between synergistic and additive with penicillin G. The low levels of cytosolic lactate dehydrogenase released from the cells treated with 4× MIC concentration of the triterpenes in comparison to that of cells treated with 3% Triton X-100 proved that membrane damage was not the mode of action of the triterpenes. CONCLUSION: This study therefore shows the potential that these plant triterpenes have in listeriosis chemotherapy especially as shown by the favourable interactions they had with penicillin G, one of the antibiotics of choice in listeriosis treatment.
Asunto(s)
Antibacterianos/farmacología , Listeria/efectos de los fármacos , Extractos Vegetales/farmacología , Plantas Medicinales/química , Triterpenos/farmacología , Antibacterianos/aislamiento & purificación , Membrana Celular/efectos de los fármacos , Interacciones Farmacológicas , L-Lactato Deshidrogenasa/análisis , Pruebas de Sensibilidad Microbiana , Viabilidad Microbiana/efectos de los fármacos , Extractos Vegetales/aislamiento & purificación , Triterpenos/aislamiento & purificaciónRESUMEN
The chemical composition of essential oil obtained by hydrodistillation of the leaves of Pachira glabra Pasq., (PgEO) has been studied by Gas Chromatography (GC) and Gas Chromatography coupled with Mass Spectrometry (GC/MS). Thirty three constituents representing 98.4% of total contents were identified from the essential oil. The major constituents of oil were limonene (23.2%), ß-caryophyllene (14.5%), phtyol (8.5%) and ß-bisabolene (6.3%). The antimicrobial activity of the PgEO was evaluated against a panel of ten bacteria and three fungal strain using agar diffusion and broth microdilution methods. Results have shown that the PgEO exhibited moderate to strong antimicrobial activity against the tested microorganisms except Citrobacter youagae, Micrococcus spp. and Proteus spp. The activity zones of inhibition (ZI) and minimum inhibitory concentrations (MIC) ranged between 13.7 mm-24.0 mm and 0.3 mg/mL-2.5 mg/mL, respectively. The insecticidal activity of PgEO was assayed against the adult Sitophilus zeamais. The lethal concentrations (LC50 and LC90) of the PgEO showed it to be toxic against adult S. zeamais at 32.2 and 53.7 mg/mL, respectively. This is the first report on the chemical composition and in vitro biological activities of essential oil of P. glabra growing in Nigeria.
Asunto(s)
Antibacterianos , Bacterias/efectos de los fármacos , Bombacaceae/química , Insecticidas , Aceites Volátiles/química , Aceites Volátiles/farmacología , Animales , Cromatografía de Gases , Ciclohexenos/análisis , Farmacorresistencia Bacteriana , Cromatografía de Gases y Espectrometría de Masas , Limoneno , Sesquiterpenos Monocíclicos , Aceites Volátiles/aislamiento & purificación , Fitol/análisis , Hojas de la Planta , Sesquiterpenos Policíclicos , Sesquiterpenos/análisis , Terpenos/análisisRESUMEN
Mimusops caffra E. Mey. ex A.DC and Mimusops obtusifolia Lam (both members of the Sapotaceae family), and Hypoxis colchicifolia Bak (family Hypoxidaceae) are used by traditional healers in Zululand to manage malaria. Anti-plasmodial investigation of the crude extracts and some triterpenes isolated from the plants showed activity against a chloroquine sensitive (CQS) strain of Plasmodium falciparum (D10). Among the crude extracts the leaves of M. caffra exhibited the highest activity, with an IC50 of 2.14 µg/mL. The pentacyclic tritepenoid ursolic acid (1), isolated from the leaves of M. caffra was the most active compound (IC50 6.8 µg/mL) as compared to taraxerol (2) and sawamilletin (3) isolated from the stem bark of M. obtusifolia (IC50 > 100). Chemical modification of the ursolic acid (1) to 3ß-acetylursolic acid (4) greatly enhanced its anti-plasmodial activity. Compound 4 reduced parasitaemia against Plasmodium berghei by 94.01% in in vivo studies in mice. The cytotoxicity of 3ß-acetylursolic acid (IC50) to two human cell lines (HEK293 and HepG2) was 366.00 µg/mL and 566.09 µg/mL, respectively. The results validate the use of these plants in folk medicine.