Aim: The present study was undertaken to investigate the antistress potential of isolated compound, Quercetin from Euphorbia hirta. Study Design: In the present study extracted leaves of Euphorbia hirta were subjected to isolation and purification of phytoconstituent as marker. The structure of isolated compound was characterized and elucidated with chemical and spectroscopic techniques such as Infra Red, Nuclear Mass Resonance and Mass spectroscopy experiments. The anti-stress activity of isolated compound i.e. Quercetin from Euphorbia hirta using elevated plus maze (EPM) model and forced swimming test (FST) respectively in swiss albino mice. Methodology: The hydroalcoholic extract of Euphorbia hirta was partioned successively with petroleum ether, ethyl ether and ethyl acetate using separating funnel. Ethyl acetate fractions were subjected to silica gel column chromatography for the isolation of Quercetin. The structure was elucidated by spectroscopic methods. Albino mice were treated with different doses of the isolated compound Quercetin (i.e.25, 50 and 100 mg/kg orally) and behavior was observed on the EPM and FST. Results: The crude hydroalcoholic extract of Euphorbia hirta was successively partitioned with various solvents. Chemical structure of Quercetin was elucidated by IR, NMR and MASS spectroscopy. Mice pretreated with Quercetin at the dose of 25, 50 and 100 mg/kg show significant improvement in the swimming time. On the other hand, after administering 25, 50 and 100 mg/kg Quercetin significantly increased the time spent in open arm and decreased the time spent in the closed arm compared to the control group The anti stress effect of the Quercetin was prominent at 100 mg/kg. The result of EPM model and FST revealed that isolated compound having antistress activity. Conclusion: This is the first report of antistress activity of Quercetin and isolation of Quercetin by column chromatography from hydroalcoholic exract. The results also revealed that Quercetin is a novel compound for the treatment of neurobiological disorder (stress). Recent investigation of traditional herbal remedy (Quercetin) in controlling and treating diseases tend to prefer natural rather than synthetic ones.
Aims: In a search for natural substances with potential for the treatment of typhoid fevers and urinary tract infections (UTI), extracts and compounds obtained from S. filicaulis and L. ovalifolia were tested for antibacterial activity. Study Design: Extraction, fractionation, isolation and identification of compounds, antibacterial evaluation. Place and Duration of Study: University of Buea and University of Dschang, Cameroon, between February 2012 and December 2013. Methodology: The most active extracts were fractionated by column and thin layer chromatographic (TLC) techniques, and tested for antibacterial activity, using agar diffusion and broth dilution methods. The structures of pure compounds obtained were elucidated by NMR spectroscopy, physical data and by comparing these values with published data. Results: Methylene chloride extract of S. filicaulis was the most active (diameters of 12-15 mm). Methylene chloride (12-16 mm) and methanol (13-16 mm) extracts of L. ovalifolia were active against all isolates. MIC values ranged from 0.08 - 1.25 mg/ml for the fractions of S. filicaulis and 0.16 - 1.25 mg/mL for L. ovalifoliafractions. Streptococcus sp was the most sensitive microbial agent (MIC = 0.08 mg/mL) for fraction IS of S. filicaulis. Staphylococcus aureus and Streptococcus sp recorded the lowest MIC for fraction ML of L. ovalifolia. Two compounds isolated from S. filicaulis were identified as β-stigmasterol (1) and hexadecanoic acid (2) while one from L. ovalifolia was identified as β-sitosterol (3). These three compounds and two other secondary metabolites not yet identified (GL2 and GL3) showed antibacterial activity. The in vitro activity of β-stigmasterol against Klebsiella pneumoniae and Salmonella Typhimurium is reported herein for the first time. Conclusion: These plants may contain lead molecules for the formulation of drugs useful for the management of UTI and typhoid fevers caused by resistant pathogens.
Aims: To isolate and investigate the antibacterial potency of novel compound obtained from methanolic extract of Curcuma longa rhizome. Place and Duration of Study: Bio-inorganic and Materials Chemistry Research laboratory, MMAM Campus (Tribhuvan university), Biratnagar, Nepal. The experimental work was done between March 2014 and August 2014. Methodology: The crude methanolic extract was prepared by digesting powdered Curcuma longa rhizome in distilled methanol and chromatographic technique like TLC and column chromatography were applied to isolate the new compound. The structural determination with proposed molecular structure was ascertained by different spectral techniques like IR, 1H NMR and TOF-MS studies and correct stereochemistry was assured by molecular modeling programmed software. The antibacterial potency of the compound was checked by Kirby Bauer paper disc diffusion method, using Mueller-Hinton's nutrient agar media. Results: The spectral studies revealed the presence of a novel compound, structurally different than curcumin, a major constituent of Curcuma longa. Elemental analysis (CHN) suggested it a Sulphur containing supramolecule with molecular formula C69H78N4O9S. Crystalinity of the compound was checked by X-ray powder diffraction studies, which reveal the crystalline nature of compound and data confirmed orthorhombic crystal system with Pmmm space group. Antibacterial screening for the compound suggested better antibacterial potency against K. pneumoniae and S. aureus bacteria. Conclusion: A novel compound has been isolated from Curcuma longa rhizome. Antibacterial assay suggested improved activity against selected pathogens relative to control drugs, Gentamicin.
Bioadhesive buccal delivery system is one of substitute to the oral route of drug administration; particularly drugs that are undergoing first pass effect. The rationale of this study was to develop a mucoadhesive buccal patch system containing drug venlafaxine with different ratios of polymeric systems like hydroxypropyl methyl cellulose E15, hydroxypropyl cellulose, methyl cellulose and sodium carboxymethyl cellulose by the solvent casting technique using propylene glycol as plasticizer. The physicochemical compatibility of the drug and the polymers were studied by FTIR and studies suggested absence of any incompatibility. Formulated buccal films were physically evaluated for thickness, weight variation, drug content, folding endurance, surface pH, swelling index, bioadhesive strength, in vitro residence time and in vitro drug release. All prepared formulations indicated good physical stability. Ex vivo permeation studies of optimized formulation was performed by using Franz diffusion cells. The release profile of venlafaxine followed zero-order and first-order kinetics in different formulations. However, the release of the drug from optimized formulation A12 (R2 = 0.9913 for Higuchi) was governed by diffusion mechanism and showed highest bioadhesive strength and in vitro residence time.
Aim: This research was aimed at evaluating the use of Grewia mollis Juss. (Tiliaceae) stem bark gum as a compression coating-agent in a formulation intended to deliver ibuprofen to the colon. Place and Duration of Study: Department of Pharmaceutics and Pharmaceutical Microbiology, Department of Pharmacology and Therapeutics (both in Ahmadu Bello University Zaria) and National Agency for Food and Drug Administration and Control (NAFDAC), Kaduna Laboratory between October 2012 and March 2014. Methods: Ibuprofen core tablets were prepared by the direct compression method and four different compression-coated formulations were produced using powdered and granulated Grewia gum (GG) or hydroxypropyl methyl cellulose (HPMC). The compression-coated tablets were also evaluated for tablet parameters; the in vitro drug release studies were carried out in different simulated gastro-intestinal fluids. An in vivo study was conducted in New Zealand rabbits using the optimized compression-coated tablet and compared with a conventional ibuprofen tablets. The pharmacokinetic parameters were estimated from concentration of ibuprofen in the rabbit plasma using the high performance liquid chromatograph (HPLC). Results: The tablets that were compression-coated with powdered GG showed better ability to offer barrier to drug release and to deliver the drug to the colon than those coated with granulated polymers. The tablets coated with powdered GG coated exhibited greater propensity to deliver ibuprofen to the colon than the other coated tablets. A lower Cmax, longer t1/2 of 8.66 h, longer MRT (7.43 h) and shorter ke (0.08 h-1) revealed that ibuprofen remained in the system for a longer period after oral administration of F2 than when MKT was administered. A high correlation coefficient (0.926) was obtained from the in vitro drug release studies and in vivo studies from F2 indicating that a good relationship was established between both studies. Conclusion: The results of this study have been able to establish that Grewia mollis stem bark gum can be used to effectively deliver ibuprofen to the colon.
Aims: To characterize the antioxidant properties of twelve selected medicinal plants commonly used in Jordan in traditional medicine. Methodology: The following in vitro antioxidant assays were used: total antioxidant capacity, DPPH free radical scavenging, ferric reducing, ferrous chelating, total phenols and flavonoids. Results: Considering the overall antioxidant activities (µg AA equivalent /mg extract), the studied plants were arranged in the following decreasing order of their extract strength: Pistacia palaestina Boiss. (232) > Arbutus andrachne L. (197) > Hypericum triquetrifolium Turra (186) > Zingiber officinale Roscoe (185) > Mentha spicata L. (184) > Rosmarinus officinalis L. (183) > Salvia triloba L.f. (154) > Verbena triphylla L’H’er. (117) > Origanum syriacum L. (109) > Teucrium polium L. (96) > Nigella sativa L. (80) > Ceratonia siliqua L. (69). When the antioxidant capacity of the dry weights (g AA equivalent /100g dry weight) of tested plants was calculated, the plants were arranged from the strongest to the weakest as follows: Pistacia palaestinaBoiss. (7.1%) > Arbutus andrachne L. (6.1%) > Hypericum triquetrifolium Turra (4.3%) > Salvia triloba L.f. (2.4%) > Rosmarinus officinalis L. (2.2%) > Ceratonia siliqua L. (1.9%) > Zingiber officinale Roscoe (1.4%) > Nigella sativa L. (1.1%) > Origanum syriacum L. (0.8%) > Mentha spicata L. (0.7%) > Teucrium polium L. (0.6%) > Verbena triphylla L’H’er. (0.5%). The antioxidant activities of studied plants were explained by their content of total phenols and flavonoids. Nigella sativa L. had the lowest antioxidant activity and the lowest total phenols and flavonoids, but the highest metal chelating activity. This plant however, could be used as a good source for new agents for iron chelating drugs. Conclusion: Medicinal plants commonly used in Jordan varied widely in their antioxidant and metal chelating abilities. Both abilities should be tested when characterizing the antioxidant properties of medicinal plants. The ability of the dry weight of plant should also be noted.
Aims: To evaluate the powder, compaction and tableting properties of co-processed silicified starch for direct compression formulation. Study Design: The study was designed to co-process cassava starch and colloidal silicon dioxide in a combination ratio of 98:2 using a simple physical method. Place and Duration of Study: Department of Pharmaceutics and Pharmaceutical Microbiology, Faculty of Pharmaceutical Sciences, Ahmadu Bello University, Zaria, between March 2013 and June 2013. Methodology: Co-processing of cassava starch and colloidal silicon dioxide was carried out using the method of co-fusion where a dispersion of cassava starch was prepared in distilled water (40% w/w) and mixed with colloidal silicon dioxide prior to thermal treatment at a temperature of 54±2ºC for 15 min in a water bath. The co-processed mixture was dehydrated with ethanol (99%) and tray dried in a Hot air oven at 40ºC for 2 h. It was then kept in an air-tight container for further studies. Powder properties were assessed by measuring the angle of repose, bulk and tapped densities, Carr’s index and Hausner’s ratio. Compaction studies were carried out on tablets compressed at a range of pressures on the Hydraulic Carver Press and analyzed using Heckel and Kawakita equations. Tablets were prepared using chloroquine phosphate as the drug of choice on a Single Stroke Tablet Press by direct compression and evaluated under uniformity of weight, thickness, crushing strength, friability, disintegration and dissolution tests. Results: The studies revealed an improvement in the functionality of the co-processed excipient with respect to flow, compression and tableting properties when compared to cassava starch. Conclusion: The silicification of cassava starch by co-processing was able to improve the powder and compaction properties of the excipient suitable for producing tablets by direct compression.