RESUMEN

Polyherbal Formulations (PHF) were developed by combining fruit juices of Momordica charantia, Cucumis sativus, and Solanum lycopersicum in different ratios and optimized through Oral Glucose Tolerance Test (OGTT) model. PHF-C pretreated rats showed the highest reduction of Serum Glucose Levels (SGL) after 60 min of glucose administration. PHF-C was incorporated into spheroids using fresh juice (FJS) and lyophilized powder (LPS) of selected plants. In OGTT study, LPS showed a significant reduction of SGL. LPS was characterized as almost spherical, having disintegration time 8 min, adequate friability, and good flow properties. In STZ-induced diabetic rats on 7th, 14th, and 21st days, LPS was reduced SGL by 9.01%, 20.9%, 38.9% (250 mg/kg dose); 20.5%, 33.9%, and 50.7% (500 mg/kg dose), respectively. LPS showed a significant improvement in abnormal body weight, biochemical, and oxidative parameters in comparison to PHF-C and metformin. Novel formulation LPS (500 mg/kg) was found more effective (p < .05) in reversing STZ-induced hyperglycemia as compared to PHF-C (1,000 mg/kg) and at par with metformin (500 mg/kg). PRACTICAL APPLICATIONS: Fresh vegetable juice contains large quantities of vitamins and minerals. Cooking and processing of fruits may destroy their nutritional value. However, FJS also has some limitations, including seasonal specificity, patient compliance, less stability, loss of vitamins and fibers, abnormal sugar level, weak immunity, and difficult to carry by patients. Lyophilization is a well-known method to improve the physical state, shelf life, and stability of phytoconstituents. Poor absorption and less bioavailability also impede the acceptance of PHF. To overcome these limitations, a suitable novel drug delivery system is required which has high therapeutic efficacy and enhanced bioavailability. The patented spheroids of herbal extracts which are in use for the treatment of the number of diseases encouraged the present work. Spheroid protects the constituents of herbal drugs from gastric destruction and gut bacteria. The outcome of present research supports the concept of enhanced stability and bioavailability of phytoconstituents present in FJS.

Asunto(s)

Diabetes Mellitus Experimental , Metformina , Momordica charantia , Animales , Diabetes Mellitus Experimental/tratamiento farmacológico , Jugos de Frutas y Vegetales , Humanos , Hipoglucemiantes , Ratas

RESUMEN

OBJECTIVE: To isolate the neuroprotective component from Convolvulus pluricaulis Chois. (Convolvulaceae) which can be used as a lead molecule in the treatment of Huntington's disease (HD). METHODS: The methanolic extract of whole plant was fractionated into four fractions; chloroform, ethyl acetate, n-butanol, and aqueous fraction. The chloroform and ethyl acetate fractions were pooled on the basis of antioxidant activity and TLC profile and charged into silica gel column. Four subfractions were collected from column (FrA, FrB, FrC, and FrD) and further assessed for antioxidant potential by 2,2-diphenyl-1-picrylhydrazyl in vitro assay. 3-Nitropropionic acid (3-NP) was administered to Wister rats for induction of HD. Different fractions were administered for 14 days. Different behavioral alterations were assessed in between study period. Animals were euthanized immediately following the last behavioral session, and biochemical parameters were measured. RESULT AND DISCUSSION: Systemic administration of 3-NP showed marked motor deficits and oxidative damage in rats. Only FrB showed significant antioxidant activity and on further purification gave pure compound (scopoletin). Our study showed that FrB (20 mg/kg) pre-treatment significantly attenuated the loss in body weight, improved the locomotor activity, grip strength, and gait abnormalities. It also has attenuated the increased malondialdehyde and nitrite levels, and restored superoxide dismutase and reduced GSH enzyme activity in the striatum and cortex in 3-NP-treated groups. These results suggest that C. pluricaulis Chois. exhibits a neuroprotective effect by accelerating brain antioxidant defense mechanisms in 3-NP-treated rats.

Asunto(s)

Antioxidantes/farmacología , Convolvulus/química , Enfermedad de Huntington/tratamiento farmacológico , Fármacos Neuroprotectores/farmacología , Animales , Conducta Animal , Peso Corporal , Cuerpo Estriado/efectos de los fármacos , Cuerpo Estriado/metabolismo , Glutatión/metabolismo , Enfermedad de Huntington/inducido químicamente , Peroxidación de Lípido/efectos de los fármacos , Masculino , Malondialdehído/metabolismo , Síndromes de Neurotoxicidad/tratamiento farmacológico , Nitritos/metabolismo , Nitrocompuestos/efectos adversos , Propionatos/efectos adversos , Ratas , Ratas Wistar , Superóxido Dismutasa/metabolismo

RESUMEN

Multifactorial metabolic diseases, for instance diabetes develop several complications like hyperlipidemia, hepatic toxicity, immunodeficiency etc., Hence, instead of mono-drug therapy the management of the disease requires the combination of herbs. Marketed herbal drugs comprise of irrational combinations, which makes their quality control more difficult. Phytoconstituents, despite having excellent bioactivity in vitro demonstrate less or no in vivo actions due to their poor lipid solubility, resulting in high therapeutic dose regimen; phospholipids encapsulation can overcome this problem. Hence, present study was designed to develop a phospholipids encapsulated polyherbal anti-diabetic formulation. In the present study, polyherbal formulation comprises of lyophilized hydro-alcoholic (50% v/v) extracts of Momordica charantia, Trigonella foenum-graecum and Withania somnifera 2:2:1, respectively, named HA, optimized based on oral glucose tolerance test model in normal Wistar rats. The optimized formulation (HA) entrapped in the phosphatidylcholine and cholesterol (8:2) vesicle system is named HA lipids (HAL). The vesicles were characterized for shape, morphology, entrapment efficiency, polar-dispersity index and release profile in the gastric pH. The antidiabetic potential of HA, marketed polyherbal formulation (D-fit) and HAL was compared in streptozotocin-induced diabetic rat model of 21 days study. The parameters evaluated were behavioral changes, body weight, serum glucose level, lipid profile and oxidative stress. The antidiabetic potential of HA (1000 mg/kg) was at par with the D-fit (1000 mg/kg). However, the potential was enhanced by phospholipids encapsulation; as HAL (500 mg/kg) has shown more significant (P < 0.05) potential in comparison to HA (1000 mg/kg) and at par with metformin (500 mg/kg).

RESUMEN

BACKGROUND: Theobjective of the present study was to evaluate the anti-inflammatory activity of aqueous extract of Mirabilis jalapa Linn. (MJL)(Nyctaginaceae) leaves for scientific validation of the folklore claim of the plant. The leaves are used as traditional folk medicine in the south of Brazil to treat inflammatory and painful diseases. Cosmetic or dermo-pharmaceutical compositions containing MJL are claimed to be useful against inflammation and dry skin. METHODS: Aqueous extract of the leaves was prepared by cold maceration. RESULTS: The anti-inflammatory activity was evaluated using carrageenan and formalin-induced paw edema models in Wistar albino rats. The anti-inflammatory activity was found to be dose dependent in carrageenan-induced paw edema model. The aqueous extract has shown significant (P < 0.05) inhibition of paw oedema, 37.5% and 54.0% on 4 (th) hour at the doses of 200 and 400 mg/kg, respectively. Similar pattern of paw edema inhibition was seen in formalin-induced paw edema model. The maximum percentage inhibition in paw edema was 32.9% and 43.0% on 4 (th) day at the doses of 200 and 400 mg/kg, respectively. CONCLUSION: The results of present study demonstrate that aqueous extract of the leaves possess significant (P < 0.05) anti-inflammatory potential.