Journal of Pharmacy Research

Print ISSN: 0974-6943
To explore novel and effective drugs for the treatment of Alzheimers disease(AD), a series of inhibitors of acetylcholineterase (AChE) were designed based on the Structure-based generation of a novel series of AchE inhibitors were carried out with crystal structure of acetylcholine esterase complexed with choline (PDB: 2HA3) obtained from protein data. Among synthesized inhibitor 7(a-e) exhibited good potency in enzyme inhibitory potency AChE: IC= 55 ± 0.53M, 73 ± 0.37M, and 51 ± 0.37M, 73 ± 0.40M, 48±0.75M, 7b and 7C also showed moderate to good activity in acetylcholinesterase assay in vitro using different sources of acetylcholinesterase studied (rat brain, human serum and electrical eel).
Aim Novel heterocycle 3-cyano 6,9-dimethyl 4-imino 2-methylthio 4H pyrimido [2,1-b] [1,3] benzothiazole 3 has been prepared by using 2-amino 4,7-dimethtyl benzothiazole 1 and bis-methylthio methylene malononitrile 2. Method Compound 3 prepared from 2-amino 4,7-dimethyl benzothiazole 1 was refluxed with bis-methylthio methylene malononitrile 2 in presence of anhydrous potassium carbonate and N,N-dimethyl formamide as solvent. Compound 3 possesses replaceable methylthio functionality at 2-postion, which was replaced by using selected different nucleophiles like phenols/aryl amines/heteryl amines and compounds containing active methylene group to afford 2-substituted derivatives 4–7 of compound 3. Results Heterocyclic compounds containing benzothiazoles fused with pyrimidines, pyrazoles reported to possess activity against the different types of cancers. Compound 3 and it's selected derivatives 4–7 were screened for their in-vitro anticancer activity towards 60 Human cancer cell lines at National Cancer Institute, Maryland USA. Many compounds exhibited remarkable activity against 60 human cell lines. Conclusion The compounds 3, 4-a, 4-d, 5-a, 6-a, 6-b exhibited maximum in-vitro anticancer activity against different cancers lines.
Background/aimDerivatives of thiazolidinones have attracted interest in recent years because it exhibits broad spectrum of biological activities like anticonvulsant, analgesic, anti-inflammatory. Thus we report the facile synthesis, characterization and biological evaluation of novel 1-[2 (substituted phenyl)-4-oxothiazolidin-3-yl]-3-(6-fluro-7-chloro 1,3-benzothiazol-2-yl)-ureas derivatives.Method The synthesis of novel potential anthelmintic agents of 1-[2 (substituted phenyl)-4-oxothiazolidin-3-yl]-3-(6-fluro-7-chloro 1,3-benzothiazol-2-yl)-ureas (TH16–TH20) were achieved by reaction with 2, 3, 4 (trisubstituted benzaldehyde) – N-(6-fluro-7-chloro-1,3-benzothiazol-2-yl) semicarbazon (V) with DMF, thioglycolic acid and zinc chloride. The products have been characterized by 1H NMR, mass spectrometry and elemental analysis.ResultAll the synthesized compounds show good to moderate anthelmintic activity against Perituma posthuma. The best results were achieved with molecules that had methyl and methoxy group at C-3 and C-2 position of phenyl ring, i.e., TH18 and TH20.Conclusion The results of novel 1-[2 (substituted phenyl)-4-oxothiazolidin-3-yl]-3-(6-fluro-7-chloro 1,3-benzothiazol-2-yl)-ureas derivatives exhibits anthelmintic activity against stander drug Albendazole. The modification of the heterocyclic ring of the parent compound offers a promising prospect and active analogues are expected to be found.
Background and aimThe current need for the discovery and development of new lead compounds exhibiting optimal antitumor potency as well as anti-inflammatory activity. Due to biological activity of significant number of compounds containing condensed pyrimidine ring system and our interest in MCRs reactions, we wish to report the synthesis of 4H-pyrimido[2,1-b][1,3]benzothiazole-3-carboxylate.MethodA novel one pot multi-component reaction of substituted benzaldehyde, ethyl cyanoacetate, 2-amino benzothiazole to give pyrimido[2,1-b][1,3]benzothiazole-3-carboxylate was described. The operational simplicity, environmental friendly conditions, regioselective formation of target product and high yield in significantly very short reaction time were major benefits.Result and discussionStructural assignments based on spectroscopic data (FT-IR, 1H NMR, mass spectra). Compounds evaluated for in vitro on panel of 60 different human tumor cell lines derived from nine neoplastic cancer types at NCI, and for the in vitro anti-inflammatory activity. Compound ethyl(4R)-2-amino-6,9-dimethyl-4-[4-(dimethylamino)phenyl]-4H-pyrimido[2,1-b][1,3]benzothiazole-3-carboxylate (4i) was found to possess good antiproliferative activity and compound ethyl(4R)-2-amino-6-chloro-4-(3,4,5-trimethoxyphenyl)-4H-pyrimido[2,1-b][1,3]benzothiazole-3-carboxylate (4g) was found to posses potent anti-inflammatory activity and compounds 4a, 4b, 4h also found to be significant anti-inflammatory activity.Conclusion The obtained results prove the necessity for further investigations to clarify the features underlying the antitumor potential of tested compounds and had potential to design lead for anti-inflammatory activity.
A series of N,5-disubstituted-1,3-thiazolidine-2,4-dione analogues (3a–h, 4a–h) were prepared by knoevenagel condensation of various aromatic aldehydes with N-substituted-1,3-thiazolidine-2,4-diones in toluene. The structures of the synthesized compounds were established based on the IR, 1H NMR, Mass and elemental analysis data. Drug likeness of the synthesized molecules were evaluated using online Molinspiration web JME Editor and OSIRIS Property Explorer and were found to obey rule of thumb.
Background/objectives Cerebral I/R injury is mainly characterized by oxidant production, complement activation, leukocyte–endothelial cell adhesion, platelet–leukocyte aggregation, increased microvascular permeability and decreased endothelium-dependent relaxation. I/R injury can lead to multiorgan dysfunction or death. In recent years, pyrimidines have received much attention of researchers because of their vasodilator, anti-inflammatory and antioxidant properties. Studies on cerebroprotective mechanism of pyrimidine derivatives on cerebral I/R injury are limited. Hence it is worthwhile to study the role of pyrimidines as cerebroprotective agents and evaluated for their possible inherent underlying mechanisms. Methods Experimental cerebral infarction was produced by bilateral common carotid artery occlusion (global cerebral ischemia) for 30 min followed by 4 h reperfusion in Wistar rats. The oxidative and anti-inflammatory biomarkers were estimated and percentage infarction was determined. Results and conclusions A dose dependent cerebroprotective action of pyrimidines (AUCP1 and AUCP2) in terms of limiting the infarct size was observed in the present in vivo model of cerebral I/R in Wistar rats. The antioxidant role of pyrimidines (AUCP1 and AUCP2) in cerebroprotection was confirmed by measuring SOD, CAT, MDA, levels. MDA levels were decreased; SOD and CAT levels were increased by treatment with pyrimidines (AUCP1 and AUCP2). The cerebroprotective actions of pyrimidines (AUCP1 and AUCP2) are partially attributed to their anti-inflammatory effects against I/R injury in rats as evidenced by significant reduction in pro-inflammatory markers MPO, TNF-α and significant increase in anti-inflammatory marker IL-10. Pyrimidines (AUCP1 and AUCP2) evaluated in the present investigation has offered significant cerebroprotection against ischemia-reperfusion induced cerebral infarction in rats.
A simple and efficient procedure has been described for the synthesis of benzo[g]naphtho[b][1,8]naphthyrindes 3 by the condensation of 2-chloro-3-formylquinoline 1 with 1-naphthylamine 2 under microwave irradiation condition. The structures of the newly synthesized compounds were confirmed by analytical and spectral (IR, NMR, and Mass) data. All these compounds were evaluated for their in vitro growth-inhibitory activity against several microbes.
Lipases are hydrolases, an important group of biotechnologically relevant enzyme, which find immense application in industries like food, diary, pharmaceutical application. Commercial lipases are mostly produced from microbes in diverse habitats such as soil contaminated with oil, dairies, industrial wastes, oil seeds, decaying foods. Extensive studies on microbes have been made for their potential production of lipases. Of these important are: Achromobacter, Alcaligenes, Arthrobacter, Bacillus, Burkholderia, Chromobacterium, Pseudomonas including yeast and few endophytic fungi. Since, bacterial lipases are extracellular, unique in nature, it is essential to study the growth by varying the temperature, pH as well varying substrates such as carbon, nitrogen, lipid, solvent. Therefore, screening for an isolate having lipolytic activity was initiated toward the discovery of novel strain.
e (a) Growth pattern of Streptomyces fradiae strain MS02 on starch casein nitrate agar media. (b) Microscopic observation of isolate MS02 under the light microscope (10003). (c) SEM (scanning electron microscope) examination of the producer strain of MS02 showing its spore morphology feature and dimension of the microbe.
e Phylogenetic tree of MS02 (S. fradiae MTCC 11051) isolate based on maximum parsimony method using MEGA 4.0.2 e biologist-centric software.
e Antifungal activity of Streptomyces fradiae MS02 against the drug resistant fungal pathogens (a) Penicillium citrinum MTCC 1751 (b) Alternaria alternata MTCC 1362 (c) Candida albicans ATCC 10231 (d) Candida albicans MTCC 183 (e) Candida albicans MTCC 2512 (f) Trichophyton rubrum MTCC 296.  
Minimum inhibitory concentration of the active metabolite produced by the isolate Streptomyces fradiae MS02.
Background Isolation of naturally occurring Streptomyces sp. with an ability to produce metabolites having antimycotic property against the pathogenic fungus from unexplored area of Chhattisgarh.Methods Starch casein nitrate medium was used for isolation and screened for their antifungal activity by agar well diffusion method. Active isolate characterized based on the morphological, physiological and 16S rRNA sequencing. Optimization of extracellular antifungal metabolite production in terms of zone of inhibition (mm) using Candida albicans MTCC 183 as target organisms was performed and extracted with n-butanol. The minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC) of active metabolite was determined according to NCCLS.Results and discussionThe active isolate was identified as Streptomyces fradiae MTCC 11051, showed the best antifungal activity against yeasts and molds including dermatophytes which showed an inimitable and stable inhibitory activity in Starch casein nitrate broth. The maximum extracellular active metabolite production was achieved in the late log phase, which remained constant during the stationary phase. The MIC and MFC values of the culture supernatant were recorded between range 50 and 100 μg/ml.Conclusions The metabolite from S. fradiae was active against pathogenic fungus with a greater potency. These results confirmed the therapeutic potential of bioactive fermented products can be used in medicinal and pharmaceutical preparations for treating the fungal infections.
A simple, accurate ,precise, sensitive spectrofluorometric method was developed for estimation of 3-hydroxy androstane [16,17-C](6’methyl, 2’-1-hydroxy –isopropene-1-yl) 4,5,6 H pyran in ethanolic extract of Syzygium cumini seed. It showed strong intense yellow fluorescence having excitation and emission wavelength 366 and 435.65 nm. respectively. Linear relationship for the fluorescence intensity was obtained in the range 50-100 µg /mL. Limit of detection and limit of quantification was found to be 7.65 µg /mL and 23.20 µg /mL, respectively. The method was statistically validated and found suitable for estimation of 3-hydroxy androstane [16,17-C](6’methyl, 2’-1-hydroxy –isopropene-1-yl) 4,5,6 H pyran in a ethanol extract of plant Syzygium cumini.
The 2-(5-amino-1H-imidazol-4-yl)-2-iminoacetonitrile has been prepared from (Z)-N-(2-amino-1,2-dicyanovinyl)formamidine by treatment with barium hydroxide in ethanol. 2-(4-isopropylphenyl)-2,9-dihydro-1H-purine-6-carboxamide was obtained from 2-(5-amino-1H-imidazol-4-yl)-2-iminoacetonitrile in dry methanol. All compoundshave been fully characterized by spectroscopic data.
Background/aimsPyrimidines have a long and distinguished history extending from the days of their discovery as important constituents of nucleic acids to their current use in medicinal chemistry. As a part of project devoted to the development of pyrimidine analogs as antimicrobial agents we have focused our attention on synthesis of C5/C6 substituted pyrimidine derivatives, specifically C6 substituted pyrimidine analogs which have emerged as potent molecule in recent years.Methods2,4-Bis(substituted phenoxy)-6-(phenylthio)pyrimidines were prepared in five steps starting from barbituric acid. Initial reaction of barbituric acid (1) with POCl3 in presence of N,N-dimethylaniline under reflux furnished 2,4,6-trichloropyrimidine (2), which on hydrolysis with aq. NaOH under reflux yielded 6-chlorouracil (3). 6-Chlorourail on treatment with thiophenol in dry pyridine generated 6-phenylthiouracil (4), chlorination of 4 using excess POCl3 under reflux afforded the key synthon 2,4-dichloro-6-(phenylthio)pyrimidine (5). Aromatic nucleophillic substitution reaction of 5 with oxygen nucleophiles like sodium phenoxides provided the desired targeted compounds 6a–g in 62–86% yield. Structural assignments of the synthesized compounds were based on their IR, 1H NMR, mass and analytical data. The antimicrobial evaluation of newly synthesized compounds was carried out by cup–plate method.ResultsThe investigation of antimicrobial screening reveals that the compounds 5, 6b, 6c and 6f showed good activity against fungal strains comparable to the standard drug Flucanazole. Remaining compounds exhibited moderate activity against bacterial and fungal strains compared to standard drug.Conclusion We have developed a facile methodology which avoids the use of moisture sensitive reagents like organolithiums, diphenyl disulphide, etc. The C6 substituted pyrimidine analogs can be considered for further studies as potent antifungal agents.
Background Preparation of a new series of Michael adducts as an 1-(4-acetylphenyl)-3-aryloxypyrrolidine-2,5-dione derivates using cellulose sulfuric acid catalyst with objective of obtaining lead compounds for future development as anticonvulsants.Methods The inhibition by economically and efficiently synthesized targeted 1-(4-acetylphenyl)-3-aryloxypyrrolidine-2,5-diones 5a–n with γ-aminobutyric acid (GABA)-transaminase activity was studied with homogenized mice brain as described by Fowler & Qume followed by the fluorimetric analysis using Salvador & Albers method. All the compounds were characterized by physical, spectroscopic and elemental analysis.Results and discussionAmong the fourteen Michael adducts of 1-(4-acetylphenyl)-pyrrole-2,5-dione, 1-(4-acetylphenyl)-3-(4-Bromophenyloxy)-pyrrolidine-2,5-dione 5d and 1-(4-acetylphenyl)-3-(Salicyldehydoxy)-pyrrolidine-2,5-dione 5h showed more potent as in vitro barain GABA-transaminase activity with IC50 (100.5 ± 5.2 μM) and IC50 (160.4 ± 6.2 μM) respectively. This activity study was performed by using the fluorimetric analytical evaluation data compared with vigabatrin, a reference standard drug.Conclusion In conclusion, 1-(4-acetylphenyl)-3-(4-Bromophenyloxy)-pyrrolidine-2,5-dione 5d and 1-(4-acetylphenyl)-3-(Salicyldehydoxy)-pyrrolidine-2,5-dione 5h strongly fulfill where as 1-(4-acetylphenyl)-3-(2,4,6-Nitrophenyloxy)-pyrrolidine-2,5-dione 5l and 1-(4-acetylphenyl)-3-(2-Napthyloxy)-pyrrolidine-2,5-dione 5b significantly fulfill the criteria for mice brain GABA-T inhibitory agents.
Dendrimers are a new class of promising polymeric materials representing a novel class of polymers drastically different from that of traditional types of linear, cross linked and long branched polymers. The polyvalent nature of dendrimers is increasingly being recognized as means of overcoming intrinsically weak monovalent interactions and in generating a new class of drugs with totally improved and acceptable pharmacokinetic profiles for unique applications in health care. As the list of potential applications of this future polymer is increasing, especially more in the field of pharmaceuticals, the present review mainly emphasizes the diverse applications of dendrimers in pharmaceutical sector.
Comparison of various parameters for sustained release beads of Glipizide.
Glipizide is a second-generation sulfonylurea that can acutely lower the blood glucose level in humans and is typically prescribed to treat type II Diabetes [Non–Insulin Dependent Diabetes Mellitus]. Its short biological half-life [3.4±0.7 hours] necessitates that it be administered in two or three doses of 2.5 to 10 mg per day and the problem associated with gastrointestinal disturbances, attempts have been made to develop sustained release product. In the present investigation mucoadhesive beads of Glipizide were formulated employing sodium alginate, carbapol 974P and SCMC. The prepared formulations were evaluated for physical parameter, mucoadhesive properties, in vitro wash-off test and in vivo test by Folin-wv method. In-vitro drug release study was performed using USP XXI Basket apparatus and examined in simulated gastric fluid (Buffer pH 1.2 from 0 to 2 hours) and intestinal fluid (Buffer pH 7.4 from 2 to 8 hours). From Yates Algorithm it has been found that the carbapol 974P polymer is having more mucoadhesive property.
BackgroundDNA topoisomerases play important role in basic cellular biology. They have been identified as the molecular targets of a variety of pharmaceutical agents. DNA Gyrase, which is a type II topoisomerase, helps in the replication of double-stranded DNA. The drugs that target the DNA Gyrase are antibacterial drugs which interfere with the DNA rewind after replication, which consequently stops DNA and protein synthesis thus killing bacteria.Methods3,4-Heteroannelated quinolin-2-ones are docked with the DNA Gyrase of Staphylococcus aureus, using Genetic Optimization for Ligand Docking software. The docked poses of each ligand are analyzed and fitness Scores are calculated with Silver. Screening of antibacterial activity of title compounds is done by adopting disc diffusion method.Results & discussionThe binding interactions of a series of novel 3,4-disubstituted quinolin-2-ones, oxothieno quinolines, quino benzoxazepinones, quinobenzothiazepinones, triazolo thiadiazepino quinolinones, and quinobenzothiazinones with DNA Gyrase are determined and potential compounds are screened for antibacterial activity against Gram −ve and Gram +ve bacteria.Conclusion The results demonstrate that 1-ethyl-4-chloro-3-cyanoquinolin-2-one, 1-methyl-4-chloro-3-cyanoquinolin-2-one, and 3-amino-4,5-dihydro-5-ethyl-4-oxothieno[3, 2-c]quinolin-2-carboxylicacid revealed good fitness score with DNA Gyrase and exhibited promising antibacterial activity against S. aureus.
Novel 3,4,5-triarylisoxazole derivatives were synthesised by Suzuki reaction of 4-bromo-3, 5-diaryl isoxazoles with various boronic acid under microwave condition. The structures of the newly synthesised compounds are characterised by 1H NMR, 13C NMR, LC-MS and screened for their antifungal activity against Aspergillus flavus (NCIM No. 524), Fusarium oxysporum (NCIM No. 1072) and Candida albicans (NCIM No. 3102).
Background/aimPyrimidine is found as a core structure in a large variety of compounds that exhibit important biological activity. Specifically, 2,4,5,6-tetrasubstituted dihydropyrimidines have shown potent antimycobacterial activity. The use of combinatorial approaches toward the synthesis of drug-like scaffolds is a powerful tool in helping to speed up drug discovery. Recently, we have developed a laboratory made para toluenesulfonic acid (PTSA) as an efficient catalyst to generate 2,4,5,6-substituted dihydropyrimidine libraries using a one-pot multicomponent reaction.Methods Based on the activity of compound 7a, a series of novel 2,4,5,6-pyrimidine derivatives were synthesized by reacting N-(3,5-dichloro-2-ethoxy-6-fluoropyridin-4-yl)-3-oxobutanamide, urea or thiourea and appropriate aldehyde in the presence of catalytic amount of PTSA as an efficient catalyst using modifications at the 4th-position of the dihydropyrimidine moiety. Synthesized compounds analyzed by melting point, thin layer chromatography (TLC), IR, 1H NMR, mass spectra and in vitro antimycobacterial activity.ResultsAmong the synthesized compounds, compound N-(3,5-dichloro-2-ethoxy-6-fluoropyridin-4-yl)-4-(4-fluorophenyl)-6-methyl-2-oxo-1, 2, 3, 4-tetrahydropyrimidine-5-carboxamide (7j) was found to be the most potent against Mycobacterium tuberculosis CIP 103471 and M. tuberculosis H37Rv ATCC with minimum inhibitory concentration (MIC) 1.13 and 1.09 μg/ml respectively.ConclusionA series of novel Biginelli dihydropyrimidines of biological interest were synthesized and analyzed for their structures. Our present study makes it an interesting compound when compared to the current therapeutic agents and are considered the candidates to investigate further for the same.
Background An indigenous marine Streptomyces coeruleorubidus BTSS-301 has been isolated from marine sediment sample near Visakhapatnam coast at a depth of 30 m. It exhibited broad spectrum of antimicrobial activity. However, for maximum production of a specific bioactive compound from indigenous isolates medium formulation is an essential step.Methods Optimization experiments for various carbon and nitrogen sources and cultural parameters were performed by shake flask culture method. The active compound in culture filtrate was extracted into ethyl acetate and then purified by silica gel column chromatography. The purified active compound was characterized by spectroscopy studies. The minimum inhibitory concentration was determined by broth dilution method.Results & discussionOptimization studies revealed that the highest antibiotic production was obtained when glucose at 10.0 g/l and NH4NO3 at 2.5 g/l were used as carbon and nitrogen sources respectively. Cultural parameters revealed that 96 h of incubation at 30 °C at 180 rpm with pH 7.2 of the production medium exhibited maximum yield. The purified active compound is identified as N-ethyl-2-(2-(3-hydroxybutyl) phenoxy) acetamide.Conclusion The antimicrobial compound from S. coeruleorubidus BTSS-301 could be a candidate in the generation of new antimicrobial agents from marine Streptomyces.
Purpose. The objective of the study was to develop the gastroretentive dosage forms of Quetiapine Fumarate using the combination of two hydrophilic polymers, sodium alginate and sodium carboxymethyl cellulose. Sodium alginate is rapidly hydrating polymer while sodium CMC is gelling polymer. METHODS. Initial preliminary developmental trials conducted to develop the composition for suitability of gastroretentive formulation. The selected composition was optimized by using 32 full factorial design of amount of sodium alginate and sodium CMC at three levels. The optimized formulation was studies for floating lag time, release kinetics, and swelling and erosion study. RESULTS. As it is desired to control the release of QF up to at least 14-16 hrs in the stomach and restrict its initial burst effect (because of its high acid solubility), parameters like floating lag time (Flag < 10 min.), time to release 50% drug (t50 < 6hrs) and time to release 90% drug (t90% < 16 hrs) are achieved by optimization of polymer combination for QF gastroretentive formulation. CONCLUSION. It has been proved that this can be used as platform technology for development of gastroretentive dosage forms for the drugs having pH dependent solubility. The combination of the sodium alginate and sodium carboxymethyl cellulose in the ratio of 17 :13 in presence of granulating agent, Eudragit L 30D 55 (3%) and gas generating agent,, sodium bicarbonate (10%) is suitable to achieve the desired release profile.
Aim To study the key pharmacophore requirements for heparanase inhibition and design of new molecules. Method Three dimensional quantitative structure activity relationship (3D QSAR) methodologies namely Comparative Molecular Field Analysis (CoMFA) and Comparative Molecular Similarity Indices Analysis (CoMSIA) were applied, PLS analysis was performed and QSAR models were generated for a set of 43 bezoxazol-5-yl acetic acid derivatives and 1,3-bis[4-(1H-bezimidazol-2-yl)-phenyl urea reported as potent inhibitors of heparanase. Result QSAR model showed good internal and external statistical reliability that is evident from the qloo2, rncv2 and rpred2. CoMFA model provides a correlation of steric and electrostatic field with biological activities. CoMSIA model provides a correlation of steric, electrostatic, acceptor, donor and hydrophobic fields with biological activities. Conclusion The identified key features enabled us to design novel symmetrical 1,3-bis[4-(1H-bezimidazol-2-yl)-phenyl urea derivatives.
N-[3-methyl-4-phenylthiazol-2(3H)-ylidene]benzenamine derivatives (5a-e) have been obtained according to the Hantzsch condensation. Desired compounds were prepared in high yield by the reaction of 1-methyl-3-arylthiourea derivatives (3a–e) and 2-bromoacetophenone in dry ethanol in the presence of a buffer. All compounds have been fully characterized by spectroscopic data.
Background In spite of all recent advancements, the complete cure of gastric ulcer disease has awaited, to be explored. Earlier we reported the potent anti-secretary and anti-ulcer activities of ethanol extract and a fraction of Nigella sativa, seed (NS) in indomethacin-induced gastric ulcers-models. Therefore, anti-ulcer activity of purified fraction of NS (NS-EA 51) in different experimental gastric ulcer-models was evaluated in the present study.Methods Anti-ulcer activity of NS-EA 51 was evaluated in histamine plus pylorus ligation (PL) and hypothermia-restrained stress, rats (adult male albino; weighing 180–220 g). Changes in the gastric secretion volume, pH, acid-output, pepsin activity, mucus secretion and ulcer indices were observed in histamine plus PL rats. Effects on gastric mucus secretion and ulcer indices were also evaluated in the hypothermic-restrain stressed models.ResultsNS-EA 51 antagonized histaminic effects on gastric juice volume, pH, acid-output, lesion formation and pepsin activities. Fraction also inhibited gastric ulcer formation induced by hypothermic-restrained stress in this study. But it did not show any significant change in the gastric mucus secretion in above models. The anti-ulcer effects of NS-EA 51 found comparable to the Famotidine, a reference anti-ulcer agent.ConclusionNS-EA 51 fraction isolated from NS may prove an effective anti-ulcer tool.
A world health organization survey indicated that about 75-80% of the world’s populations rely on non-conventional medicine, mainly of herbal sources, in their primary healthcare. There has been an explosion of scientific information concerning plants, crude plant extracts and various substances from plants as medicinal agents during last 30-40 years. Although herbal medicine has existed since the dawn of time, our knowledge of how plants actually affect human physiology remains largely unexplored. Numbers of plants are claiming various medicinal uses and many researches are going on in this view. They are believed to be much safer and proved elixir in the treatment of various ailments. The genus Artemisia consists of about 500 species, occurring throughout the world. Among the different species of Artemisia, A. absinthium and A. asiatica have a vast range of biological activities including cytotoxic, antihepatotoxic, antibacterial, antifungal, antioxidant, antimalarial etc. Terpenoids, flavonoids, coumarins, caffeoylquinic acids, sterols and acetylenes constitute major classes of phytoconstituents of the genus Artemisia. The present review comprises the phytochemical, ethnopharmacological and pharmacological reports of A. absinthium and A. asiatica. The future scopes of these plants have been emphasized with a view to isolate bioactive moieties which could be used for multifarious biological activities.
In this study, an investigate effect of moisture absorption by ranitidine and resinates used to improve stability of ranitidine hydrochloride tablets. Moisture absorption by ranitidine at three different level of relative humidity (RH) has been studied. Percentage of moisture absorption at 22% was low as compared to 57% and 75% RH. To eliminate deliquescent tendency of drug, weak cation-exchange resins Indion 204, Indion 264 and Indion 254 were used in formulation as complexing agent. The drug loading process was optimized with respect to drug: resin ratio and pH of loading solution. The complexes were evaluated for bulk density, angle of repose, stability and in-vitro drug release. Optimum drug loading was at pH of 4.0 in drug: resin ratio of 1:1. In-vitro drug release studies showed more than 90% drug release from the optimized formulation within 30 min. X-Ray diffraction studies revealed ranitidine hydrochloride to be present in amorphous form in resinates. Tablets were prepared containing Indion 204: drug complex using different diluents. Tablets containing resinates and commercial products were exposed to 75%RH to observe their effect on moisture absorption. The type of dosage form also influenced moisture absorption. Uncoated tablets absorbed maximum amount of moisture, capsule intermediate while coated tablets absorbed minimum. Formulated tablets containing microcrystalline cellulose absorbed minimum amount of moisture as compared to formulations containing lactose and mannitol. Tablets containing resinates exhibited similar dissolution profile with commercial tablets. Indion 204 was found to be better complexing agent for reducing the hygroscopicity and to design stable ranitidine hydrochloride tablets.
Alcoholism is a major social problem in all societies. One of the effective drugs used in the treatment of alcoholism isdisulfiram, which acts as an antabuse, by inhibiting the enzyme, aldehyde dehydrogenase, causing accumulation of acetaldehydewhich results in flushing, tachycardia, nausea, etc. The extent of the alcoholism may vary from person to person. Mostof the alcoholics may be associated with one or the other diseases. This makes the treatment more complicated for physicians.In this study an attempt was made to examine 82 patients from inpatient and outpatient departments of the two majoralcohol rehabilitation centers, Sacred Heart Hospital, Thoothukudi and Raja Hospital, Tirunelveli, India. The disulfiramalcoholreactions were analyzed by a ‘Challenge test’ approved by the hospital committees, which included 24 parameters.In addition, a survey was carried out to identify the socio-economical- background and habits of these patients. Resultsshowed that a predominant number of patients belonged to the rural area with high rate of illiteracy or only with primaryeducation (32.5 % and 55 % respectively). Male patients (98.78 %) outnumbered the females. A higher proportion ofpatients from semi-urban and rural areas were found to consume tobacco along with alcohol (66.67 % and 75 % respectively).The challenge test showed that hypertension, flushing of the face, reddening of the eyes and uneasiness were themajor reactions observed in an hour. Majority of the patients were found weak, sleepy and in a confused state after onehour. The challenge test helped to study disulfiram-alcohol reactions effectively. The study has provided an insight topromote an awareness on the impact of alcoholism to the public and counseling the patients, particularly those in the ruraland semi urban areas.
In our present study, we carried out the antibacterial activity of the plant A. Indicum (L.) Sweet, which is a cosmopolitian genus belonging to the family of Malvaceae. Different parts of this plant are in use to treat various ailments in ethnomedicine especially its leaves have been used for treating infections. We carried out the anti bacterial activity of the extracts prepared from the dried leaves of A. Indicum (L.) Sweet using agar-well diffusion method against both gram positive and gram negative microorganisms. Among all the extracts the ethanolic extract of the leaves showed significant (P<0.001) antibacterial activity comparable to the standard penicillin potassium and streptomycin sulphate againstselected gram positive and gram negative bacteria.
Rheumatoid arthritis is a major ailment among rheumatic disorders. A large number of herbal extracts are in vogue used for treatment of various types of rheumatic disorders. Abutilon indicum (Linn.) Sweet, an Indian herb was reported to have anti-inflammatory as well as analgesic activity, in-vitro as well as in-vivo. The present study deals with anti-arthritic activity in-vitro. Various in-vitro anti-arthritic pharmacological models were studied, such as, inhibition of protein denaturation, effect of membrane stabilization, and proteinase inhibitory action.Herbal extract (aq.) with two different concentrations (100mcg/ml and 250mcg/ml.) was used and results were compared with acetyl salicylic acid (250mcg/ml.). The herbal extract showed dose dependent activity which was found to be better than that of acetyl salicylic acid.
Background The purpose of this investigation was to explore high selective, sensitive, rapid, stable, reproducible extraction method in long run with broader linear range. At the same time, it could be expected that, this method would be efficient in analyzing large numbers of plasma samples obtained for pharmacokinetic, bioavailability or bioequivalence studies.MethodsA simple, sensitive, selective and rapid high-performance liquid chromatography coupled with tandem mass spectrometry was developed and validated for quantification of Acamprosate in human plasma. The chromatography was performed by using waters atlantis HILIC, (2.1 mm × 50 mm, 3.0 μm) column connected with guard column waters atlantis HILIC, (2.1 mm × 10 mm, 3.0 μm). Acamprosate-d12 calcium trihydrate used as an IS. The extraction of drug and internal standard were obtained by solid phase extraction. The linearity was proved with concentration range 1.00–250.00 ng/ml for Acamprosate in human plasma.Results and discussionThe LOQ was demonstrated at 1.00 ng/ml. The within-batch, between-batch precision was found to be 2.21–4.07% and 2.00–3.20%. The within-batch, between-batch accuracy was found to be 96.26–102.00% and 98.27–102.00% for Acamprosate. Drug and IS were eluted within 3.0 min.Conclusion The developed LC-MS/MS assay for Acamprosate is rapid, simple, sensitive, selective and suitable for routine measurement of sample analysis. The validated method was successfully applied in pharmacokinetic study of human plasma.
Hydrogel matrix tablets of Acarbose was formulated using hydroxypropyl methyl cellulose and guar gum with the aim tostudy of release kinetic and to attain a near zero order release. In-vitro dissolution studies were carried out using USP type2 dissolution test apparatus. The release of drug followed a typical Higuchian pattern. Matrix tablets formulated employinghydroxypropyl methyl cellulose and guar gum slow release of Acarbose over a period of 12 h and were found suitable formaintenance portion of oral controlled release tablets. Acarbose release from these tablets were diffusion controlled andfollowed zero order kinetics after a lag time of 1h.The most successful of the study, exhibited drug release pattern very closeto theoretical release profile. A decrease in release kinetics of the drug was observed on increasing polymer ratio.
Structure validation using Ramachandran Plot by Procheck.
Side chain parameters of Acetyl-CoA carboxylase plot statistics.
Results obtained from molecular docking studies.
Aim Acetyl-CoA carboxylase (ACC) is a biotin-dependent enzyme which plays a key role in fatty acid biosynthesis via production of melonyl-CoA as an essential substrate. It is involved in homeostasis of fatty acids inside the system using both up and down regulating mechanisms. Apart from this In silico analysis of its catalytic site and regulatory sites make it a potential target for herbicidal and insecticidal drug targeting. Currently the 3D structure of Acetyl-CoA carboxylase (ACC) from Jatropha curcas has not been solved in Protein Data Bank (PDB). Hence the aim of the present study is to build the 3D structure of Acetyl-CoA carboxylase (ACC) from J. curcas also to perform a virtual screening for the identification of the effective inhibitors using molecular docking studies. Methods Homology modeling has been used to determine the 3D structure of Acetyl-CoA carboxylase (ACC) from J. curcas. Structure validation and molecular docking studies has been carried out using Procheck and Molegro Virtual Docker respectively. Results Ramachandran Plot confirmed quality of modeled structures along with main chain and side chain parameters. Out of 309 residues in SPDBV model, 244 were in core region 19 residues were in additional allowed region, 2 residues were in generous allowed region and no residues were in disallowed region. Conclusion Energy minimization for SPDBV model thermodynamically proved accepted structure with energy of −12,063.024 kJ/mol. The model further can be subjected to pharmacodynamic and pharmacokinetic studies. Molecular docking studies identified few established herbicides which could be promising inhibitors of Acetyl-CoA carboxylase (ACC). Efforts to screen and identify ACC inhibitors using flexible molecular docking resulted in Pinoxaden from Phenylpyrazole class as the most effective inhibitor with rerank = −81.436 and RMSD = 0.31.
The aim of this study was to compare the disintegrants efficiency of the three superdisintegrants (Ac-Di-Sol, Polyplasdone XL and Explotab) and also to compare disintegrant properties and disintegrant efficiency of agar (AG) and gellan gum (GG) with treated agar (TAG) and treated gellan gum (TGG) by formulating metoclopramide HCl immediate release tablets by direct compression method. In the present investigation, we have attempted first time report on TGG as disintegrant. Disintegration efficiency of powder disintegrants compared by swelling & hydration capacity of disintegrants. While efficiency of disintegrants in tablets compared by various test like disintegration time, dissolution test, wetting time & maximal water uptake study of metoclopramide HCl immediate release tablets. The rapid disintegration observed for the TAG and TGG containing tablets due to high-porous structure of treated form of disintegrants which confirmed by photomicroscope study. Comparing three classes of superdisintegrants represented by Ac-Di-Sol, Polyplasdone XL and Explotab with AG, TAG, GG and TGG. The treated form of disintegrants (TAG, TGG) in which TAG was found to be more effective than TGG. The disintegration efficiency was found in following decreasing order Ac-Di-Sol, Explotab, Polyplasdone XL, TAG, TGG, AG and GG.
Background Nucleus accumbens (NAcc) is known to be involved in reward and addictive functions. In the present study we tested parameters of ingestive activity and alcohol intake following lesions of nucleus accumbens in order to establish the role of this nucleus unequivocally.Materials and methodsMale Wistar albino rats were divided into groups, and were subjected to Sham lesion and bilateral lesion of nucleus accumbens. The consumption of water, ethanol and food were recorded daily and their body weight was noted weekly, for one week before lesion and 3 weeks following lesion. In another set, two bottle free choice test was carried out between 10% alcohol and potable water, rest of the procedures were maintained same as for the other set.ResultsThe lesioned rats showed increase in intake of alcohol (p < 0.01). There was no significant change in food intake or body weight. In two bottle free choice test, the rats consumed increased volume of fluid. There was highly increased water intake (p < 0.001). There was no significant change in their alcohol intake. The increase in water intake was significantly more than the increase seen in the alcohol intake in the group provided only alcohol.Conclusions Bilateral lesions in nucleus accumbens did not change the alcohol intake in two bottle choice test. But they showed increased water intake in two bottle choice suggesting increased thirst. The alcohol intake increases only when there is no water provided, suggesting the pivotal role of this centre in ingestive behaviour.
Comparison of dissolution profile of different formulations
Aceclofenac a non-steroidal anti-inflammatory drug, used in posttraumatic pain and rheumatoid arthritis. Aceclofenac fast-dispersible tablethave been prepared by direct compression method using microcrystalline cellulose as a direct compressible vehicle. Croscarmellose sodium and polyplasdone xl-10 were used as a superdisintegrants for the formulation. The disintegration time and dissolution parameter (t50% andt80%) decreased with increasing the concentration of polyplasdone. Those tablets were evaluated for weight variation, hardness, disintegration time, friability and dissolution.
e Formula for primary coating.
e Formula for secondary coating.
e FT-IR spectra: aceclofenac (a), aceclofenac and HPMC E5 (b), aceclofenac and EC N50 (c). 
e Kinetic data of coated aceclofenac pellets at different graphical plots.
AimThe aim of the present study was to prepare sustained release pellets of aceclofenac using pelletization technique.Methods The sustained release was ensured by coating the pellets with ethyl cellulose N50 and hydroxy propyl methyl cellulose E5. The influence of rate retarding polymer, ethyl cellulose in combination with film forming agent, HPMC in different weight ratios on drug release kinetics was studied.ResultsThe in vitro dissolution studies of aceclofenac from the sustained release pellets were carried out in pH 6.8 phosphate buffer using USP type I apparatus. Statistically significant differences were found among the drug release profile from different formulations.Conclusion The kinetic study revealed that the release of drug from the optimized formulation was appeared to follow first order kinetics. The dissolution profile and in vitro release kinetics showed that aceclofenac pellets were promising for sustained delivery of the drug.
AimThe main aim of this study was to prepare and evaluate once daily sustained release tablets of aceclofenac by using polyethylene oxides (PEOs) of different molecular weights as matrix polymers.MethodA direct compression method was used to prepare PEO matrices. Type and the amount of PEO in the matrices were varied to optimize in vitro aceclofenac release profiles.ResultsFrom the in vitro release studies, it was found that the matrix tablets containing 28% of PEO (80% PEO WSR 303 and 20% of PEO WSR N60K) showed similar release profiles, as estimated by similarity factor (f2), to a marketed product, Hifenac SR.From the bioavailability study in human volunteers, it was found that there was no statistically significant difference in the pharmacokinetic parameters such as Tmax and Cmax between the optimized sustained release formulation containing 28% of PEO and Hifenac SR.Conclusion It can be concluded from this study, that the bioavailability of the sustained release formulation developed was similar to that of Hifenac SR and the hydrophilic PEO matrices are novel sustained release carriers for the delivery of aceclofenac.
Background/Objectives The main aim of the present work was to study the effect of various polymers like polyvinyl pyrrolidine (PVP) (k-30), polyvinyl alcohol (PVA), hydroxy propyl methyl cellulose (HPMC) and polyethylene glycol-4000 (PEG-4000) on dissolution enhancement of poorly water-soluble drug, aceclofenac from the prepared microcrystals.Methods Aceclofenac microcrystals were prepared using anti-solvent precipitation technique.ResultsThe prepared microcrystals were investigated for their particle size, solubility, drug content, flow properties, drug–excipient interactions, in-vitro dissolution studies. Microcrystals prepared using polymers showed improvement in the dissolution profile when compared to that of the pure aceclofenac. Dissolution enhancement was attributed to the decrease in the crystal size of the drug which is due to the preferential adsorption of the polymer on to the crystal surface.Conclusions The microcrystals prepared using PVP (k-30) showed better dissolution rates when compared with that of other polymers.
Aceclofenac, a non-steroidal anti-inflammatory drug is used for rheumatoid arthritis, osteoarthritis and ankylosingspondylitis. Aceclofenac, fast melting tablets have been prepared by direct compression method after incorporatingsuperdisintegrants such as L-Hydroxy Propyl Cellulose, Polyplasdone XL and Explotab in different (8%, 16% and 24%)concentrations. All the formulation were evaluated for the influence of disintegrants and their concentrations on the characteristicsof fast melting tablets mainly in terms of disintegration time and dissolution rate. Tablets containing Polyplasdone XL athigh concentration showed better disintegration character (26 seconds) along with rapid release (98% in 2 minutes). Noappreciable differences are seen in other formulations. The concentration of the superdisintegrants had also an effect ondisintegration time and in-vitro dissolution. There seems to be a trend towards use of higher level of disintegrants producingfaster disintegration and faster dissolution. The resulting tablets were also evaluated for its hardness, thickness, wetting timeand water absorption ratio. It is concluded that fast melting aceclofenac tablets could be prepared by direct compressionusing superdisintegrants
Wound healing activity of ethanolic (50% v/v) bark extract and the leaf of Pterospermum acerifolium were evaluated by using both excision and incision wound models in rats. The studies significant wound healing model reveals significant would healing activity of the extract and the leaves that is compariable with providines iodine. In the incision model, the tensile strength of the extract treated group is found to be higher than the later treated gourp of animals on 12th post wounding day. The results of the present study justify the would healing properties of the bark as suggestd by locality.
Antioxidant activity of ethanolic extract of Petrospermum acerifolium barks was studied for it free radical scavenging property in different in vitro models as 1, 1- Diphenyl – 2 picryl hydrazyl, nitric oxide, superoxide and hydroxyl radical model. The extract shows significant dose dependent free radical scavenging property in all model. The extract showed the presence of high phenolic content suggesting the plant to exhibit antioxidant activity.
Effect of Pterospermum acerifolium extract on Aspirin induced gastric ulceration (values a*re expressed as mean + S.E.; n = 6) (Dose of Pterospermum acerifolium extract (T 1 – 150 mg/kg and T 2 = 300 mg/kg) = standard drug omeprazole = S = 10 mg/kg  
The role of ethanolic fraction of Pterospermum acerifolium bark extract on different experimental ulcer models in rats was investigated.The extract demonstrated significant antiulcer activity against aspirin, indomethacin & ethanol induced ulcerations, significant inhibition of gastric secretary volume, and total acidity in pylorus ligated rats were observed to occur with the extract.
Tinospora cordifolia (Willd.) Miers ex Hook. F., and Tinospora sinensis (Lour.) Merrill, are herbaceous vines found all over India and are well known herbal medicines. Since, ancient time T. cordifolia, T. sinensis and Neem-giloe (T. cordifolia growing on Azadirachta indica A. Juss.) individually have been used in the ayurvedic medicine system in the form of Guduchi satwa to treat liver disorders. In the present studies, hepatoprotective potential of satwa prepared from three Tinospora species against hepatotoxicity induced by repeated dosing of acetaminophen was assessed. Repeated acetaminophen dosing produced elevations in the level of liver marker enzymes and changes in the lipid profile status of the animals. T. cordifolia had a specific action on maintaining lipid profile with improvements in the levels of total cholesterol, HDL and LDL. T. sinensis exhibited a positive effect on SGPT and ALP activities apart from improvements in VLDL and triglyceride levels. Neem guduchi had specific beneficial effect on SGOT and bilirubin levels. The differential hepatoprotective effect of these three different satwa was also evident from liver histology. T. cordifolia exhibited normalization of periportal hepatocytes while T. sinensis showed prominent hepato-regenerative activity with increase in the normal hepatocytes in the treatment group. The Neem guduchi treated group showed strikingly normal liver histology without any anatomically detectable anomalies. The results reveal that these satwa have their actions at different physiological targets and hence exhibit differential hepatoprotective activity. Due to this differential hepatoprotective activity these three satwa may be used in combination as a liver tonic. It is also required that the effect of these satwa on the acute acetaminophen hepatotoxicity should be assessed.
Madhuca longifolia is a folklore medicinal plant that is commonly used for the treatment of snakebite as antidote in Southern part of Tamilnadu, India. Stem bark is used to cure hydrocele, wounds in stomach (ulcer), scabies and rheumatism. Acetaminophen (APAP) is commonly used as an analgesic and an antipyretic agent that, in high doses, produces liver and kidney necrosis in mammals. The aim of the present study is to investigate the nephro, hepatoprotective and antioxidant activities of the ethanol extract of Madhuca longifolia (EEML) in two dose levels of 500 mg/kg & 750 mg/kg B/W on APAP induced toxicity in rats.Biochemical studies show that there is an increase in the levels of serum urea, hemoglobin (Hb), total leukocyte count, creatinine, packed cell volume, DLC, mean corpuscular volume and raised body weight along with reduced levels of neutrophils, mean corpuscular Hb content, mean corpuscular hematocrit, granulocytes, uric acid, and platelet concentrations.These values are retrieved significantly by the treatment with extracts at two different doses. The antioxidant studies reveal that the levels of renal superoxide dismutase, catalase, reduced glutathione and glutathione peroxidase in the APAP treated animals are increased significantly along with decreased MDA content in EEML treated groups. Apart from these, histopathological changes also reveal the protective nature of the Madhuca longifolia extract against APAP induced necrotic damage of hepato and renal tissues. In conclusion, these data suggest that the EEML can prevent both renal and liver damage from APAP induced toxicity in rats and it is likely mediated through its antioxidant activities.
Objectives To evaluate the hepatoprotective activity of ethanolic extracts of Caralluma umbellata Haw. (ECU) against acetaminophen (APAP) induced hepatic damage in rats.Methods Hepatoprotective activity of ECU was evaluated in APAP induced hepatic damage in rat. Hepatic damage was assessed by an elevation of alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), cholesterol, and total bilirubin which were released in to the blood from damaged cells. Hepatic tissue antioxidant enzyme such as, superoxide dismutase (SOD), glutathione peroxidase (GPx), reduced glutathione (GSH) and Catalase (CAT) was also determined in APAP induced hepatic damage in rat.ResultPre-treatment of ECU, 1 h prior to APAP administration significantly protected the elevation of serum transaminases, ALP and cholesterol activities. Similarly the activity of total bilirubin was significantly (P < 0.05) decreased in ECU plus APAP treated group than the acetaminophen induced hepatotoxic group. Both pre-treatment of ECU and silymarin diets significantly inhibited the depletion of antioxidant enzymes SOD, GPx, GSH and CAT, compared to the group of APAP treated rats.Conclusion The results revealed that pre-treatment with ECU prevented both serum biochemical and tissue antioxidant evidence of hepatic damage induced by APAP and it could be used as natural potential ingredients for pharmaceutical industry.
Aim The objective of the present investigation was to formulate and evaluate microencapsulated Glibenclamide produced by the emulsion–solvent evaporation method. Methods Microparticles were prepared using cellulose acetate by emulsion solvent evaporation method and characterized for their micromeritic properties, encapsulation efficiency, particle size, drug loading, FTIR, DSC, SEM analysis. In vitro release studies were performed in phosphate buffer (pH 7.4). Stability studies were conducted as per ICH guidelines. Results The resulting microparticles obtained by solvent evaporation method were free flowing in nature. The mean particle size of microparticles ranges from 132.54 to 178.44 μm and encapsulation efficiency ranges from 89.96 to 98.48%. The infrared spectra and differential scanning calorimetry thermographs confirmed the stable character of Glibenclamide in the drug-loaded microparticles. Scanning electron microscopy revealed that the microparticles were spherical in nature. In vitro release studies revealed that the drug release was sustained up to 12 h. The release kinetics of Glibenclamide from optimized formulation followed zero-order and peppas mechanism. The mechanism of drug release from the microparticles was found to be non-Fickian type. Conclusion Cellulose Acetate microparticles containing Glibenclamide could be prepared successfully by using an emulsion solvent evaporation technique, which will not only sustain the release of drug but also manage complicacy of the diabetes in a better manner.
Objective: Assessment of Antioxidant activity of Cassia auriculata leaves by using In vitro model.Method:In the present study evaluation of ethyl acetate of extract Cassia auriculata leaves with the help of two In-vitro antioxidant models were carried out for Nitric-oxide scavenging Activity and DPPH method. IC50 value was calculated and compared with standard Ascorbic acid.Results:Ethyl acetate extract was found to be extremely effective in scavenging nitric-oxide (IC50 51.3ìg/ml). In inhibition of DPPH Radical Scavenging activity (IC50 96.6µg ìg/ml) Ethyl acetate extract showed different levels of antioxidant activities in tested models.
Background To isolate and characterize terpenoid and antibacterial activity of 95% ethanol extract from the leaves of Delonix regia.Methods95% ethanol crude extract was further partitioned with different solvents. The ethyl acetate soluble part was subjected to column chromatography and eluted with solvent mixtures of increasing polarity. The structure of isolated compound was identified on the basis of spectral analysis. i.e. FT-IR, 1H NMR, 13C NMR, EI/MS and ESI-MS/MS. Antibacterial activity of isolated terpenoid was against Gram positive, Gram negative bacterial strains observing the zone of inhibition. Antibacterial activity was done by well diffusion method at a concentration of 25 μg/25 μl, using ethanol as the control.ResultsCompound characterization using various spectroscopic techniques identified the final isolated compound as oleananoic acid acetate and it showed excellent antibacterial activity.Conclusions The present study we proved oleananoic acid acetate have medicinal property. This is the first report of the presence of terpenoid in the leaves of D. regia. The method of isolation is simple, cost effective and efficient.
In the present study, antioxidant potential of the methanol extract of the leaves and roots of Achyranthes aspera Linn. was evaluated by using 1, 1-diphenyl-2-picrylhydrazyl (DPPH) scavenging assay. The extract showed antioxidant activity in dose dependent manner. In DPPH scavenging assay the IC50 value of the leaves and root extracts were found to be 241.86ìg/ml and 129.91ìg/ml respectively, the IC50 value of the reference standard ascorbic acid was 7.81 ìg/ml. This study revealed that methanolic extract of root possesses potent anti-oxidant activity than methanolic extract of leaves.
Achyranthes aspera Linn (Amaranthaceae), commonly known as apamarga, is a commonly available plant in India. It is traditionally known as Latjira, and Prickly chaff. Different constituents are find in different part of the Achyranthes aspera (eg. Saponins A and B, amino acids, hentriacontane, hormones ecdysterone and Petrol extract of shoot 17-pentatriacontanol). Some alkaloids and fatty acids are also indicates. therefore its use in the treatment of different type of acute and chronic disease.whole plants of Achyranthes aspera have pharmacological activity. The claims were gathered by interviewing traditional healers, especially women.
The ethanolic extract of leaves of “ Achyranthus aspera linn”. was screened for antilithiatic activity in male albino wister rats and result were summarized based on ionic changes in urine. Lithiasis (stone formation) induced by oral administration of 0.75% ethylene glycolated water to adult albino Wister rats for 28 days . The ionic chemistry of urine was altered by ethylene glycol , which elevates the urinary concentration of ions .eg. calcium , oxalate , phosphate , thereby contributing renal stone formation . Supplementation with ethanolic extract of leaves of. “ Achyranthus aspera linn”. Significantly reduce the elevated urinary calcium and oxalate ion concentration in the urine, confirming the stone inhibitory effect . Also it elevates the urinary concentration of magnesium, which is considered as one of the inhibitor of crystallation . The high urine creatinine level observed in ethylene glycol treated rats was also reduced following treatment with extract . The increased deposition of stone forming constituents in the kidneys of calculogenic rats was also significantly lowered by curative and preventive treatment using ethanolic extract . The histopathological findings also showed signs of improvement after treatment with ethanolic extract . all the observations provided the basis for the conclusion that the ethanolic extract of leaves of “ Achyranthus aspera linn”. is endonned with antilithiatic activity.
Top-cited authors
Kameshwar Sharma Yadavilli
  • University of Delhi
Sonal Bhatnagar
Reeta Kumari
  • University of Delhi
Prashith Kekuda T.R
  • S.R.N.M.N College of Applied Sciences, Shimoga, Karnataka, India
Bhaskar Rao
  • VIT University