Background. Dalbergia species has wide range of secondary metabolites and is traditionally used in treatment of painful micturition, swelling, and leprosy and as blood tonic. The study evaluates membrane stabilizing, anticoagulant, analgesic, cytotoxic, subacute anti-inflammatory, and depression potentials of D. candenatensis leaves metabolites. Methods. Membrane stabilizing activity was evaluated by hypotonic induced hemolysis assay, whereas anticoagulant activity is done through extrinsic pathway by measuring prothrombin time. Analgesic action, cytotoxic effect, and subacute anti-inflammatory activity were determined by acetic acid induced writhing model, brine shrimp lethality bioassay, and formaldehyde induced model, respectively. Depression activity was measured by the Open Field, Hole Cross, Hole Board, and thiopentone induced sleeping time measuring methods. Results. D. candenatensis contains phenolic, flavonoid, and tannin, quantified as 416.25 mg, 330.00 mg, and 432.22 mg Gallic Acid Equivalent/100 g of dry extract, respectively. Extract showed maximum inhibition of writhe, hemolysis, and edema, approximate to 57.14%, 36.62%, and 34.1%, respectively. LC50 value for nauplii was 151.499 μg/ml. Mean prothrombin time was approximate to 31.0 ± 2.31 seconds at 1.0 mg/ml. Extract showed depression activity, and maximum sleeping time was noted to be about 141 minutes. Conclusion. D. candenatensis leaves show dose dependent membrane stabilizing, anticoagulant, depression, analgesic, moderate cytotoxic, and subacute anti-inflammatory activities.
This study was designed to identify some bioactive phytochemicals from ethanolic extract of roots of Litsea polyantha and to evaluate some of its pharmacological activities. Phytochemical tests indicated the presence of reducing sugar, combined reducing sugar, tannins, flavonoids, alkaloids, terpenoids, and phenol. In the antioxidant assay using 2-diphenyl-1-picryl-hydrazyl (DPPH) free radical scavenging method, the IC50 value was found to be 82.31 μg/mL. Total content of phenolic compounds, flavonoid, and tannin was found to be 152.69 mg GAE/gm, 85.60 mg QE/gm, and 77.22 mg GAE/gm of dry extract, respectively. In disc diffusion antibacterial assay, the extract exhibited highest zone of inhibition up to 12.25 mm against Escherichia coli at the concentration of 500 μg/disc. For brine shrimp lethality bioassay, the extract exhibited LC50 56.082 μg/mL. In in vivo antihyperglycemic activity test by oral glucose tolerance test using Swiss Albino mice at the oral dose of 250 and 500 mg/kg, the extract showed statistically significant antihyperglycemic effect. Finally, in vivo, the extract exhibited the dose dependent CNS depressant effects by reducing the locomotors of Swiss Albino mice which was confirmed through three different neuropharmacological activity tests such as open field, hole cross, and hole board test.
Background: The root-bark of the medicinally important plant Zanthoxylum budrunga (ZBRB) brooks a variety of uses in ethnobotanical and ethnomedicinal practice in Bangladesh and thus demands biological investigation to reveal its therapeutic potentiality. So, the present study was perpetrated to explore antioxidant, analgesic, antidiarrhoeal, and a cytotoxic activity of ethanolic root-bark extract of Zanthoxylum budrunga and was also to quantify the major bioactive polyphenolic constituents by HPLC analysis. Methods: Total phenolic content was measured spectrophotometrically by using Folin Chiocalteu's reagent while in vitro antioxidant activity was determined by means of 2, 2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging assay and reducing power assay. HPLC analysis was performed to identify and quantify the major bioactive polyphenolic constituents present in the extract. Acetic acid induced writhing test and hot-plate test were conducted to evaluate the analgesic activity of the crude extract. On the other hand, in vivo antidiarrheal potentiality was investigated by using experimentally castor oil induced diarrhoea in mice and brine shrimp lethality bio-assay was implemented to check the cytotoxic potentiality of the crude extract. Results: Zanthoxylum budrunga showed DPPH scavenging activity (IC 50 54.27 μg/mL), while the total phenolic content was 647.91 mg GAE/100 g of extract. ZBRB also showed concentration dependent ferric reducing power activity. At the doses of 250 and 500 mg/kg, ZBRB exhibited statistically significant (P < 0.001) inhibition of writhing in test mice (64.58 and 77.78%, respectively). In hot-plate test, ZBRB, at the above dose levels, significantly (P < 0.001) prolonged pain threshold with response time of 5.80 and 6.81 s, respectively. In castor oil induced diarrhoeal episode in mice, ZBRB exhibited 66.56% and 83.39% inhibition of defecation at the doses of 250 and 500 mg/kg, respectively (P < 0.001). The LC 50 (Median lethal concentration) value of ZBRB in brine shrimp lethality bioassay was found to be 21. 84 μg/mL. In the HPLC analysis, (+)-catechin, caffeic acid and quercetin were detected with the concentration of 17. 94 mg/100, 3.72 mg/100 and 11.95 mg/100 g of ethanolic extract of ZBRB, respectively. Conclusion: The results rationalize the uses of the plant in traditional medicine for diarrhoeal as well as pain management. Catechin, caffeic acid, and other phenolics constituents might have some function in the observed activity.
The aim of the present study was to develop a sustained release bio-adhesive matrix based Gliclazide tablet to match the in-vitro and ex-vivo experimental profile, and can be used to the treatment of Type II Diabetes Mellitus. It will be expected that single Gliclazide tablet reduce glycosylated hemoglobin and overcoming individual large fluctuation of oral bioavailability. Eleven types of tablets were formulated by wet granulation technique which contains 30 mg of Gliclazide and different concentrations of diverse bio-adhesive polymers which conforming to the USP/BP monograph. The prepared tablets were evaluated for their physicochemical parameters, bio-adhesive behavior and also in-vitro release pattern and ex-vivo residence time. Formulated F-6 tablet (300 mg) contains 30 mg Gliclazide, 90 mg Carbopol 974P NF, 155 mg Lactose, 15 mg Povidone, 5 mg Magnesium Stearate and 5 mg Talc. Carbopol based F-6 tablets showed highest significance adherence (164.1 gm) property and also exhibited greater than 300 minutes ex-vivo residence time. In-vitro release pattern of F-6 formulation was 44.74% (Mean Dissolution Time 52.86 hrs which was studied for 8 hours in phosphate buffer media at pH 7.4. Different kinetic models including zero order, first order, Higuchi and Korsmeyer pattern were applied to evaluate drug release behavior. Zero order and Korsmeyer pattern indicated most appropriate model for describing the release profile of F-6 formulation. The drug release mechanism was consequently found to be diffusion, swelling and erosion. The results point out that Carbopol 974P NF bio-adhesive matrix Gliclazide tablets have marked sustained release properties.
Background Merremia umbellata subsp. orientalis (Hallier f.), commonly known as Sapussunda in Bengali, is used in folk medicine for the treatment of different diseases such as helminthiasis, rheumatism, fever, wounds, burns, sores, management of pain due to cut etc. The present study was carried out to evaluate the antioxidant, analgesic and anthelmintic activities of ethanolic extract of stems of Merremia umbellate (ESMU). Methods Phytochemical investigation was carried by using standard chemical test as described in literatures. In vitro free radical scavenging activity of ethanolic extract was quantitatively estimated using DPPH (2,2-diphenyl-1-picrylhydrazyl) free radicals scavenging assay. Total phenolic and tannin content were spectrophotometrically determined by Folin Ciocalteu reagent whereas the flavonoid was determined by aluminum chloride colorimetric assay. Acetic acid induced writhing method and hot plate method, using Swiss albino mice, were used to investigate the analgesic effect of ESMU whereas in-vitro anthelmintic activity was evaluated against Haemonchus contortus (Nematode) of cattle. Results Phytochemical screening revealed that the ESMU contain reducing sugar, alkaloids, flavonoids, tannins, gums, steroid, xanthoproteins, glycosides and acidic compound. In DPPH free radical scavenging assay, the extract showed scavenging potential with IC50 value of 161.81 μg/mL. Total phenolics, tannin and flavonoid content of crude extract were found to be 87.4 mg GAE/gm, 68.2 mg GAE /gm and 64.27 mg QE/gm respectively. Significant (P < 0.001) analgesic effect was observed in acetic acid induced writhing method at both doses 250 and 500 mg/kg. Similar effect was found in hot plate method that measures antinociceptive effect in response to heat stimuli. The ESMU also exhibited significant (P < 0.001) anthelmintic activity in a concentration dependent manner. The paralysis time and time for death were recorded as 9.30, 8.62 and 7.65 min and 19.58, 18.82, and 16.43 min respectively at a concentration of 25, 50 and 100 mg/mL respectively. Conclusion Based on the results obtained in this study clearly strengthen the traditional uses of M. umbellate stems as antioxidant, antinociceptive and anthelmintic. Therefore, this result suggested that the stems of Merremia umbellata might be a potential source of useful bioactive compounds.
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