International Journal of PharmTech Research

Print ISSN: 0974-4304
Antioxidant activity by DPPH methods of ethanolic extract, fractions from Calophyllum sclerophyllum Vesq stembark, and the chemical compound from the active fraction as antioxidant has been measured in this research. Extraction was done by maceration methods with ethanol 70% and then partition by n-hexane, ethyl acetate and n-buthanol. Then antioxidant activity assays of ethanolic extract and fractions by DPPH methods and using quercetin as positive control. The fraction that have antioxidant activity more over purified by colomn chromatography and recrystalization, and the pure compounds were elucidated by spectroscopic analysis and measured that antioxidant activity. The ethanolic extract have high antioxidant activity with IC50 5,96 ppm, and also ethyl acetate fraction and n-buthanol extract with IC50 3,03 and 3,89 ppm. The IC50 of quercetin value at 1,73 ppm. Two pure compounds have been isolated from ethyl acetate fraction, CSL 1 was chromanon acid (Isoapetalic acid) and CSL 2 was flavonoid (Astilbin), but only CSL 2 that showed activity as antioxidant, with IC50 7, 24 ppm. Those compounds not yet reported before from this species.
A new simple, rapid, sensitive, selective, and accurate method for the spectrophotometric determination of Chloramphenicol (CAP)in different pharmaceutical preparations. Chloramphenicol as active antibiotic is widely used in the treatment the diseases. The spectrophotometric method is based on the condensation reaction between CAP and 1,2 naphthoquinone-4-sulfonic(1,2 NQS) as reagent to formed an orange-red product after reducing nitro group in drug into amino group by used a concentrated HCl and zinc dust. Orange-red product was showed a maximum absorption at 489nm. Beers law was obeyed in the concentration range of 1-9µg.mL-1 with a molar absorptivity (1.86 * 10⁴),and sandell’s sensitivity (1.73* 10⁻²) µ, respectively. The analytical parameters were optimized as the following: It was found the time for completed reaction was (10 min) at temperature (70⁰C)in bicarbonate solution, and the best volumeof0.01 mol. L⁻¹ of 1,2 NQS solutionis1mL.Limit of detection (LOD), and limit of quantification (LOQ)are0.068 ppm, and 0.207 ppm, respectively, the recoveries range 98.52%-100.66%.The method was successfully applied to the analysis of the (CAP)in its pharmaceutical preparations(Eye drops,Ointments and Capsules). © 2016, International Journal of PharmTech Research. All rights reserved.
Scheme 2
Starting from 2-nitrophenylacetic acid, the synthesis of some pyrrolo[1,2-a]quinoline derivaives has been reduced to an experimentally simple three-step operation.
Alpha receptor play major role in the hypertension process and the inhibition of α1 receptor by alpha receptor blockers has been a common target of antihypertensive drug discovery. The present study deal with the synthesis of novel dihydropyrimidinone (DHPM) derivatives from the reaction of N-substituted piperazine and substituted dihydropyrimidinone was performed. To study SAR of dihydropyrimidinone derivatives we introduced electron releasing, electron withdrawing substitution on phenyl ring attached to piperazine scaffold and also the different linkers like SO2 and C=O between phenyl and piperazine ring were used. All compounds were found to be good to moderately good active. Compound 7g was most found to be most active from the result of pharmacological evaluation among the all the DHPM derivatives and it was merely same as active as standard drug prazosin. Structure activity relationships of these series of compounds showed that piperazine ring attached to DHPM instead of substituted aromatic amine were responsible for increasing binding affinity for α1A receptor. The SO2 bridge between phenyl ring and piperazine with electron releasing substituent increases α1A binding affinity. This work can be guidance for further development of DHPM moiety to get potent α1A receptor inhibitor antihypertensive agent.
The title compound 2-(4-(anthracen-9(10H)-ylideneamino)-4-(1,6-dihydro-1,2,4-triazin-5(2 H)-one)pyridine 6, molecular formula C29H43N5O, was obtained through a multi steps reactions using tricyclic ketone, anthrone, as starting material. All the newly synthesized compounds were characterized using spectroscopic methods such as FTIR, 1HNMR, 13CNMR and elemental analysis. All synthesized compounds were primary in vitro screened for their antibacterial activity against Gram-positive (Staphylococcus aureus ATCC 6538p, Staphylococcus epidermidis ATCC 12228 and Bacillus subtilis PTCC 1023) and Gram-negative (Escherichia coil ATCC 8739, Klebsiella pneumoniae ATCC 10031, and Pseudomonas aeruginosa ATCC 9027) bacteria by the drug diffusion method.
New series of 1,2,4-triazole based Schiff base (5a-5i) and 1,3,4-thiadiazole (6a-6g) derivatives were synthesized by utilizing 4-amino-5-(4-chloro-2-methylphenyl)-4H-1,2,4-triazole-3-thiol (4) as active intermediateand evaluated for invitro anti-hyperglycemic activity by α-glucosidase enzyme inhibition and invivo by streptozotocin (STZ) and nicotinamide induced T2DM rat model. The compounds 5a, 5c-g which showed potential DPPH radical scavenging activity with a level of inhibition ranging between 70% and 90% were considered for anti-hyperglycemic activity. The IC50 value, for the α-glucosidase inhibition capacity of the compounds 5a and 5c was 74.5μg and 113μg respectively. Blood glucose level of test compounds (5a, 5c-g) attenuated the progression of diabetes in a dose dependent manner following 14 days of treatment. The test compounds were given orally at 10mg/kg, 50mg/kg and 100mg/kg body weight of animals. The 14th day data with 10 mg/kg, compounds 5a and 5c showed significant decrease in plasma glucose concentration (92mg/dL and 109mg/dL respectively) and for the compounds 5a, 5c-g with 100mg/kg, the plasma glucose concentration was 94mg/dL to 111mg/dL.
1,3-Thiazolidin-4-one is a versatile lead molecule for designing potential bioactive agents. In the present study, pyridin-4-amine (1) on condensation with different aromatic aldehydes (2a-g) in presence of catalytic amount of concentrated hydrochloric acid in absolute ethanol yield N-[(Z)-(substitutedphenyl)methylidene]pyridin-4-amine (3a-g), which on cyclisation with 2-sulfanylpropanoic acid in dry 1,4-dioxane in presence of anhydrous zinc chloride afford the corresponding 2-(substitutedphenyl)-5-methyl-3-(pyridin-4-yl)-1,3-thiazolidin-4-ones (4a-g). The structure of the newly synthesized compounds (3a-g) and (4a-g) were confirmed by IR and 1H NMR spectral data. All the newly synthesized 1,3-thiazolidin-4-one analogues (4a-g) at various concentrations (10, 20, 50, 100 and 200 mcg/ml) have been evaluated for in vitro cytotoxicity against Dalton's ascites lymphoma (DAL) cancer cell line by trypan blue exclusion method. Compound 2-(2,4-dichlorophenyl)-5-methyl-3-(pyridin-4-yl)-1,3-thiazolidin-4-one (4b) and 2-(4-bromophenyl)-5-methyl-3-(pyridin-4-yl)-1,3-thiazolidin-4-one (4g) inhibited 100% and 78% DAL tumor cells at 100 mcg/ml and 100% and 89% at 200 mcg/ml concentration, whereas standard drug doxorubicin exhibit 100% DAL inhibition at a concentration of 100 mcg/ml. From the above study, compounds 4b and 4g which showed better results (> 50% inhibition) at lowest concentration were selected for in vitro testing of antiproliferative activity against L929 lung fibroblast cell line by using MTT 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay method. In the antiproliferative assay, compound 4b (IC 50 = 15.3 μg/ml) and compound 4g (IC 50 = 26.5 μg/ml) showed the highest cytotoxic activity against L929 cells.
A series of Carboxamide moiety with substituted 1,3,4-thiadiazole was designed and synthesized. These title compounds were prepared by condensation of benzoxazine with 2,5-disubstituted-1,3,4- thiadiazole. Structure elucidation of the synthesized compounds was done by spectral analysis. The anticonvulsant activity of the title compounds was evaluated by using PTZ model(60mg/kg) and carbamazepine taking as a reference standard (100 mg/kg). All synthesized compounds showed no sedation side effect as compared to reference standard (carbamazepine). The present study indicated that bromo substituted compounds MH-B 1T 2 (2- benzamido-5-bromo-N-(5-(2-chlorophenyl)-1,3,4-thiadiazol-2-yl)benzamide)showed significant protection against pentylenetetrazole induced convulsions which can be regarded as strong candidates for future investigations.
A series of 5-substituted-2-phenyl-1, 3, 4-thiadiazole were prepared by the reaction of different substituted benzoylisothiocyanate with 5-amino -2-phenyl -1, 3, 4-thiadiazole. The target molecules were characterized by CHNS analysis, IR, NMR and mass spectra. All these new compounds were screened for antibacterial and antifungal activity. Some of those compounds had promising antimicrobial activity.
In the present study a series of new 1,3,4-oxadiazole derivatives were synthesized. These newly synthesized compounds were characterized by NMR, mass spectral, IR spectral study and also by C, H, N analyses. All the newly synthesized compounds were screened for their antibacterial and antifungal studies. Antimicrobial studies revealed that compounds 6 showed significant antibacterial activity against Candida albicans. Compound 7 showed significant antifungal activity against Escherichia coli and Pseudomonas aeruginosa.
In the present study napthol was treated with ethylchloro acetate to get ethyl 2-(naphthalene- 2- yloxy)acetate (1), which on reaction with hydrazine hydrate gave 2(naphthalene- 2-yloxy)acetohydrazide (2).This on further reaction with potassium hydroxide and Carbon disulfide in methanol yielded 5- ((naphthalene-2-yloxy)methyl)-1,3,4-Oxadiazole-2(3H)- thione (3). The compound 3 was treated with formaldehyde and various secondary amines to form 5-((naphthalene-2-yloxy)methyl)-1,3,4-Oxadiazole-2(3H)- thione mannich bases (4a-4f).The structures of all the synthesized compounds were confirmed by spectral data (IR,H1NMR)and were tested for their antibacterial activity by agar cup plate method. The compound 4f showed relatively good antibacterial activity compared to standard used.
New 5-[1-(anthracen-9(10H)-ylideneamino)-2-(1H-imidazol-5-yl)ethyl]-1,3,4- thiadiazol-2-amine 3 has been synthesized from condensation reaction of N-anthracen-9(10H)-ylidenehistidine 2 with thiosemicarbazide in phosphorusoxy chloride. The prepared compounds were characterized by FTIR spectroscopy, electronic spectroscopy, 1HNMR and 13CNMR. Preliminary in vitro tests for fungicidal activity show that prepared compounds display good activity to Gibberela, Cercospora arachidicola, Physolospora piricola and Fusarium oxysporum.
6, 8 di substituted,2-ethyl, 1,3-benzoxazin-4(3H)-one (1-2). 3-amino, 6, 8-di substituted 2- ethyl quinazolin- 4-(3H)-one (3-4).3-amino chloro acetyl, 6,8-di substituted 2-ethyl-(3)quazolin-4(3H)-ones (5-6). 6,8-di substituted 2-ethyl, l3-[(7,11-di(2/4-substituted phenyl)-3-oxo-9-amino-imino-2,4-diazaspiro [quinazolin-4(3H)-one. (7-26) were prepared in present study. The newly synthesized compounds were screened for their anticonvulsant activity against electrically (MES) and chemically (PTZ, picrotoxin and bicuculline) induced seizures and compared with the standard drugs phenytoin sodium, Lamotrigine and Sodium valproate. The compound 23 was found to be most potent compound of this series.
A series of new 4-thiazolidinones 5a-f were prepared by condensation of thioglycolic acid with Schiff bases 4a-f which in turns have been prepared by the action of amines on 2,6-dichloro-1-(N-substituted phenyl)-1,4- dihydropyridine-3,5-dicarbaldehydes 3. The structures of the newly synthesized compounds have been confirmed on the basis of elemental analysis and spectral studies. The newly synthesized title compounds have been screened for their in vitro antimicrobial activities. Some of the compounds exhibited encouraging results.
2H-1,4-pyridooxazin-3(4H)-one was synthesized by condensation of 2-amino-3-hydroxy-pyridine with chloroacetylchloride by using standard procedure. Esterification with ethylchloroacetate and further condensation with hydrazine hydrate produced hydrazide of 2H-1,4-pyridooxazin-3(4H)-one.Schiff base derivatives of 2H-1,4- pyridoxazin-3(4H)-one were synthesized by the acid catalyzed condensation 2-(3-oxo-2,3-dihydro-4H-1,4- pyridoxazin-4-yl)acetohydrazide with various benzaldehyde derivatives. Schiff base derivatives were characterized by FT-IR, 1H-NMR. All the synthesized compounds were subjected to antimicrobial screening by cup plate method and by estimating the minimum inhibitory concentration by adopting the two-fold serial dilution technique.
The reduction of ketones is one of the most important and practical reaction for producing non racemic alcohols, which are needed to synthesize industrially important chemicals such as pharmaceuticals, agrochemicals and natural products. Biocatalysis has turned out to be a highly competitive technology for asymmetric ketone reduction. In the present work, an attempt was made to identify a potential microorganism for the reduction of 3-[5-[(4-flurophenyl)-1,5, di-oxopentol]-yl] -4-(S) phenyl oxazolidin-2-one. Some of the fungi screened were Saccharomyces cerevisiae, Aspergillus niger(2 strains), Pichia farinosa, Candida vishwanathii, Rhizopus stolonifer and Penicillin species. The experimental results showed that S. cerevisiae, Aspergillus niger and C. viswanathii strains were able to bring about the conversion of selected ketone to alcohol. As Saccharomyces cerevisiae was found to be more effective in bringing about reduction, it was selected for further experiment. In order to improve the yield certain bioconversion parameters like pH of reaction medium, time of incubation, incubation temperature and biomass to substrate ratio were studied. The results showed that the bioreduction of the above mentioned substrate was maximum in pH 7.6 at 30°C when incubated for 48 h. The conversion increased with increase in biomass, however it reached saturation at the ratio of 300:1.
The hypolipidemic activity of Michelia champaca extract was studied on triton WR 1339 induced models of hyperlipidemia in rats. Hyperlipidemia in experimental rats evidenced by an enhancement in the levels of Cholesterol, Triglycerides, LDL,VLDL, HDL and Oxidative stress markers (MDA,GSH). Methanolic extract of flowers showed significant reduction in the level of serum cholesterol, triglycerides, LDL, VLDL,MDA,GSH and increase in HDL level which was similar to the standard drug atrovastatin. Preliminary phytochemical analysis revealed the presence of phytoconstituents such As Tannins, Saponins, Steroids, Terpenoids, Flavonoids, Carbohydrates, Anthroquinone, Polyphenol And Glycosides.
Simvastatin is a powerful lipid lowering agent that can decrease low density lipoprotein (LDL) level up to 50%. Simvastatin nanosuspension were prepared by high pressure homogenization method. The prepared formulation is evaluated for hypolipidemic activity in triton wr-1339 induced hyperlipidemic rats. The serum collected from different group of animals is evaluated by auto analyzer. The results shows that formulated nanosuspension have better efficacy compared to the unprocessed drug of simvastatin. Nanosuspension formulations has showed appropriate stability, formulation having drug content within the limits after 90 days.
A new, simple, sensitive, accurate and precise high-performance thin-layer chromatographic method for quantification of 3-hydroxy androstane [16,17-C](6′methyl, 2′-1-hydroxy -isopropene-1-yl) 4,5,6 H pyran, a marker compound in Syzygium cumini was developed and validated. This marker compound was isolated from the ethanol extract and identification was confirmed by using melting point and IR, NMR spectroscopy. An ethanol extract of the seed powder was chromatographed on silica gel 60F-254 plate with toluene : ethyl acetate (8.5:1.5 v/v) as mobile phase. Detection was performed by scanning in fluorescence mode at 366 nm. The method was validated for linearity, accuracy, recovery, precision, limit of detection, limit of quantification and specificity. The linear regression analysis data for the calibration plots for 3-hydroxy androstane [16,17-C](6′methyl, 2′-1-hydroxy -isopropene-1-yl) 4,5,6 H pyran showed good linear relationship with r 2 = 0.999, in the concentration range of 1000-5000 ng/spot. The limit of detection and limit of quantification were 131and 430 ng/spot, respectively. The amount of 3-hydroxy androstane [16,17-C](6′methyl, 2′-1-hydroxy -isopropene-1-yl) 4,5,6 H pyran found in seed powder extract was 7.38% . This method can be used as quality control method for checking the purity of Syzygium cumini seed powder, extract and its formulation.
Urinary tract infections (UTIs) are one of the most widespread diseases in developing countries including Syria. The current study aims to evaluate the efficacy of the different methods: EMB agar, API 20E and polymerase chain reaction (PCR), in identifying a collection of Escherichia coli (E. coli) isolates that cause UTIs. In This study, were diagnosed isolates taken from samples of patients with UTIs. These isolates were obtained in the form of colonies identified as E coli by conventional methods on EMB agar. The colonies were identified using API 20E kit. Further confirmation was performed by PCR amplifying a target fragment of the E. coli 16S rRNA gene. Only 51 of the 75 isolates identified as E. coli using EMB agar indicated a positive results as E. coli after applying biochemical tests. Therefore, the error rate is 32%. After the application of PCR, we founded 65 isolates were E. coli which means the error rate is 13%. The PCR method showed good agreement with the conventional method (86.6%). We observed significantly the reduction of error rate when using PCR method comparing with biochemical method. This confirmed the inaccuracy of E. coli identification based on her formal characteristics and the biochemical testes only.
The present study elucidates that hexane extract of the sea urchin, Temnopleurus alexandri has an antibacterial activity. Of the gram-positive (Staphylococcus aureus ATCC 25923, Bacillus subtilis MTCC 441, Enterococcus faecalis ATCC 29212) and gram-negative (Escherichia coli ATCC 25922,Pseudomonas aeruginosa ATCC 27853, Klebsiella pneumoniae ATCC 15380,Proteus vulgaris MTCC 1771) bacteria tested, hexane extract showed antibacterial activity for all the bacteria tested except K.pneumoniae. Various concentrations of hexane extract (5,20,200,2000 and 5000ppm) were tested. Streptomycin and ampicillin were used as positive controls. Lowest (2.5ppm) MIC was noted for B. subtilis and P. aeruginosa. GC-MS analysis revealed the presence of Pentadecane, Heptadecane, Eicosane, Heneicosane, Docosane as major compounds in the extract. This study shows that hexane extract is a potent antibacterial agent and needs further purification for the specific compound, which is responsible for the said activity.
Preventive measures for spread of novel corona virus-COVID 19.
Demographic data analysis of students
Knowledge based questions regarding COVID-19
The rapid and extensive spread of the COVID-19 pandemic has become a major cause of concern in society. The aim of this study is to assess the Knowledge, awareness and perceptions of COVID-19 disease and related practices among students trough a questionnaire based survey. It has been seen that students are more active and comfortable online therefore an e-survey was conducted among COVID-19. Study outcomes with some interesting facts aboutstudent‟s knowledge, awareness and their perceptions for the same.
This 90 days vermicomposting work was conducted to evaluate the performance of epigeic earthworms E.andrei to alter and change four commonly dumped and littered solid wastes in Ethiopian cities and towns in to a high quality vermicompost. All wastes were mixed with cow dung in 3:1 ratio and treated with earthworm E.andrei in the following waste and worm mass proportion. 9kg of vegetable waste treated with 130gm of worms, 9kg of enset waste treated with 130gm of worms, 5kg of coffee husk treated with 70gm of worms, 8kg of khat waste treated with 115gm of worms. Results from all beddings treated by this species of earthworms showed that TKN increased b/n 50.3 - 56%, TK increased between 29.6 - 43.6 %, TP increased between 58.9% - 73.2%, Ca increased between 39.6 % - 61.5%, while TOC decreased between 35% - 38.4 % and the C:N ratio reduced between 60 - 68 %. The findings from this experiment generally indicated that vermicomposting could be one good option to improve solid waste management performance of Ethiopian cities and towns through the production of excellent biofertilizer for agronomic purpose.
Several novel ethyl (5-substitutedacetamido)-3-methylthio-1-phenyl-1H-pyrazole-4-carboxylate were synthesized and screened for their anti-inflammatory at the dose of 25mg/kg and analgesic activity at the dose of 50mg/kg. The compound 5a and 5f are prominent candidate which showed good anti-inflammatory activity among the series. The compound 5a, 5g and 5h showed 60% analgesic activity to that of standard aspirin by acetic acid induced writhing method.
3-methyl-1-phenyl-4-[(E)-2-{1H-pyrazolo [3,4-b] quinolin-3-yl} diazen-1-yl]-4,5-dihydro-1H-pyrazol-5-one derivative have been synthesized by the reaction between substituted phenyl pyrazolones and 3-amino -1 H-pyrazolo [3,4-b] quinoline. The novel compound structure has been established on the basis of their substituted phenyl pyrazolones derivatives. These compounds were tested for in vitro antifungal or antibacterial activity against Gram-Positive and Gram-Negative stain by standard method and synthesized compounds showed moderate to good antibacterial and antifungal activity with respect to standard drugs Ciprofloxacin and Flucanazole.
A new series of 3-[1H-benzimidazole-2-yl-amino]-2-phenyl-1, 3-thiazolidin-4-one (V) were synthesized by the reaction of a mixture of 2-(2-benzylidenehydrazinyl)-1H-benzimidazole IV and thioglycolic acid in DMF containing a pinch of anhydrous zinc chloride. The chemical structures of the synthesized compounds were confirmed by IR, mass spectral and C, H, N analysis techniques. The synthesized compounds were screened for depressant activity by the gross behavioral studies and the loco motor activity method. The synthesized compounds were significantly showed their CNS depressant activity that of standard.
Different 4, 5-substituted, 3-amino thiophene-2-Carbonitriles were prepared by using various ketones. From the 3-amino thiophene-2-carbonitriles different 4-amino thieno [2,3-d]pyrimidines were prepared and further these compounds were condensed with various aldehydes to afford Schiff's bases of Thieno[2,3-d]pyrimidines. The title compounds thus prepared were characterized by their physical (TLC, M.P) and spectral data (NMR, IR & Mass). Then the title compounds were screened for anti-microbial activity against different strains of microorganisms. Antibacterial activity was carried out by using both Gram positive and Gram negative bacterial strains, the anti fungal activity was carried against Candiada and Aspergillus species.
A new series of 5-[4-(substituted) benzylidene or benzyl] thiazolidine-2,4-dione have been synthesized using economical synthetic routes. The synthesized compounds 4a-4c, 7a-7c and 14a-14c were evaluated for their oral antihyperglycemic activity by fructose induced hyperglycemia in Wistar rats. From the results, compounds 7c and 14b have appreciable blood glucose-lowering effect compared to that of the reference drug, pioglitazone. Hypoglycemic activity of all compounds was compared with the results of their docking after removal of the co-crystallized ligand present in the 2PRG structure. Out of these compounds, compound 14b shows better interaction with amino acid residues of PPAR-γ and also shows better oral antihyperglycemic activity in this series.
In-order to emphasize the importance of sample rotation during irradiation in BI 2000, relative percentage dose profile measurements were carried out using FBX dosimeters placed in the central vertical plane of the irradiation volume, either using sample rotation facility or kept stationary. Results obtained were further intercompared with that of Fricke system under identical irradiation conditions. Difference between the maximum and minimum relative percentage dose as obtained for stationary and rotating conditions as measured by both the systems was found to be 32.0% and 27.5% respectively.
Objective-Giant Cell Tumors (GCT) in bone is a rare musculoskeletal tumor. The purpose of this study was to study the characteristics of patients with Giant Cell Tumors in RSUP. Haji Adam Malik for 2013- 2018. Materials and Methods-The type of research conducted is a retrospective descriptive research method. This research was conducted in RSUP. Adam Malik Haji Medan based on medical records of patients with Giant Cell Tumors during the period of January 2013 - December 2018. The collected medical and demographic data is tabulated and presented in the form of a frequency distribution chart or table and analyzed in full. Data analysis used in this study uses total sampling which is presented in the form of tables or diagrams.Results-During the period of the study taken from the medical record data of Medan Haji Adam Malik Hospital, 37 patients with Giant Cell Tumors were treated. Distribution of the number of sample subjects with diagnoses of giant cell tumors of male sex as many as 19 patients (51.3%) while female sex numbered 18 patients (48.6%). Based on the location of giant cell tumors obtained by distal radius of 3 patients (8.1%), femur as many as 9 patients (24.3%), fibula as many as 2 patients (5.4%), proximal tibia as many as 14 patients (37 , 9)%), then in categories other than long bones (digiti) as many as 5 patients (13.5%), patella as many as 2 patients (5.4%), and pedis as many as 2 patients (5.4%). Based on the actions taken, as many as 21 people (56.7%) carried out extensive excision, curettage + bone cement as many as 11 people (29.7%), amputation in 3 patients (8.1%), ORIF + bone grafts by 2 people (5.5%). In this study, of 37 patients with giant cell tumors with stage 1 no patients, stage 2 as many as 12 people (32.4%), stage 3 as many as 25 people (67.5%).Conclusion- Patients with tumor giant cells were found at productive age, there was not much difference in sex, the most campanacci stage was in stage 3, the most common sites were proximal to the tibia, the most extensive measures were also available, and metastases were not available to other organs.
Keloid is an abnormal scar that appears as an impact of the wound healing process. Trauma, skin tension, hormone, and genetics are the risk factors of keloid. This study was aimed to obtain the profile of keloid patients at Polyclinic of Dermatovenereology RSUP. Dr. M. Djamil Padang in the period 2014-2018. This was a retrospective descriptive study using data of medical records. The results showed that the incidence of keloid in the period 2014-2018 was 157 cases. Based on gender, females were the most (51.60%). The age group that had the highest in number was 15-24 years old (27.39%). Based on occupation, most were students (33 cases; 20,49%). The most common location of the lesion was on the chest, which accounted for 57 cases (36.31%). Seventy-six cases (48.41%) with interpretation big effect on patient life. Conclusion :Keloid was more common in females, age group 15-24 years old, and occupation as students. The most common location of the lesion was on the chest and a big effect on patient life.
Introduction : Spinal cord injury is a damaging situation related to severe disability and death after trauma.And the term spinal cord injury refers to damage of the spinal cord resulting from trauma. Spinal injuries treatment is still in debate for some cases, whether using conservative or surgical methods. Material and Methods : The study was a retrospective, unpaired observational analytic study with a crosssectional approach. It was conducted at Haji Adam Malik General Hospital, Medan from January 2016 to December 2018. Clinical outcome of patientswere calculated using SF 36, ODI, and VAS.Data would be tested using the Saphiro-Wilk test. We were using the significance level of 1% (0.01) and the relative significance level of 10% (0.1). Results : Clinical outcomes of patients with spinal cord injuries before posterior instrumentation rated using ODI and VAS were 75.93±6.75 and 4.75±0.98 respectively. Meanwhile, the scores were 10.75±3.29 (ODI) and 1.77±0.72 (VAS) post-operatively. Using SF-36, the scores were 72.9±16.5 (PF); 58±23.1 (PH); 63.1±21.8 (EP); 62.5±12 (ENE); 84.1±14.8 (EMO); 79.6±23.5 (SF); 62±125.3 (PAIN); 49.5±3.4 (GH); and 72±7.8 (HC) pre-operatively. After posterior instrumentation, the scores were 94.5±6.7 (PF); 100±0 (PH); 79.9±32.9 (EP); 88.6±13.7 (ENE); 92.3±1.7 (EMO); 100±0 (SF); 99.9±10.4 (PAIN); 89.3±14.9 (GH); and 92.4±9.7 (HC). Discussion : In this study, patients with thoracal, thoracolumbar and lumbar injuries who underwent surgery experienced significant improvements in quality of life. This is indicated by the significant difference in ODI, VAS, and SF-36 scores before and after surgery. The results of this study were consistent with other studies conducted by Hao et al, which showed that there was an improvement in the quality of life of patients after surgery. Conclusion : There are significant improvements in patient’s quality of life after posterior instrumentation of the spinal cord injury in thoracal, thoracolumbar, and lumbar regions based on the clinical outcomes.
Although acne is usually recognized as an adolescent skin disorder, the prevalence of adults with acne is increasing. The clinical and epidemiological data of acne were evaluated with a view to establishing possible contributing etiological factors and observing whether clinical features differ from adolescent acne. Division of Dermatology and Venereology Outpatient Clinic Dr. M. Djamil hospital padang during January 2016 until December 2018.Retrospective study performed in Medical Cosmetic Division of Dermatology and Venereology Outpatient Clinic Dr. M. Djamil hospital padang during January 2016 until December 2018. Data was taken from medical records. Out of 224 patients included in the study 54.01% were women and 45.98 % were men. Majority of the patients had comedonal acne (45.53 %), whereas nodulocystic was the least common (13.39%). Most common predominant site of involvement was cheek (44.20 %), followed by chin (25.45 %), and mandibular area (14.58 %). Family history of acne was present in 57.70 %. Scarring was observed in a 39.2 %. Acne is predominant in women, with the most commonly involved of the cheeks, with the most common type was comedones type.
Objective- Psoas abscess one of rare manifestation of tuberculosis spondylitis. 5% of cases will develop psoas abscess and can increase the number of morbidity and mortality if the diagnosis and treatment were late. Material and Method-This is a cross sectional study to determine characteristics of psoas abscess in patient with tuberculosis spondylitis. The data is taken from patient’s medical record in Haji Adam Malik General Hospital from January 2016 to Desember 2018. The Population of this study is all the patients with tuberculosis spondylitis who come to Emergency Department or Outpatient Clinic. The collected data is tabulated and presented in the form of a frequency distribution diagram or table and analysed descriptively using total sampling. Results-The Subject for this study are 13 patients, within the proportion 5 patients are male (38.5%) and 8 patients are female (61.5%). The data show 5 patients have the ages < 18 years old (38.5%) and 8 patients have the ages > 18 years old (61.5%). All the patients get antituberculosis drugs as non operative treatment and 11 patients (84.6%) get an additional operative treatment for drainage the abscess. The site of psoas abscess in this study, 3 patients developed in thoracolumbal region (21.7%), 7 patients developed in lumbal region (53.8%) and 3 patients developed in lumbosacral region (21.7%). Conclusion- from this study we conclude that the incidence are happened in female more common than male, it usually affects young adult >18 years old and the common site of psoas abscess is lumbar region.
To evaluate fast dissolving tablets for Roflumilast employing with novel superdisintegrant using lepidium sativum mucilage by using 23 factorial design.The physical, chemical and micromeritic studies were evaluated for the prepared mucilage. To estabish fast dissolving tablets of Roflumilast with lepidium sativum mucilage ie a superdisinitegrant in different ratios by using direct compression method employing 23 factorial design. All the fast dissolving tablets were evaluated pre compression and post compression parameters like dissolution efficiency (DE%) percent of drug dissolved at 5 min (PD5). The Lepidium sativum mucilage was to be found fine,free flowing crystaline powder and excellent swelling nature in water. The FTIR and DSC studies were indicated to no interactions between roflumilast and Lepidium sativum mucilage. All the formulation batches shows good quality with regrad to drug content (98±0.092 to 100±0.026)hardness(3.4±0.43 to 3.6±0.64)friability (0.21±0.04 to 0.88±0.42). The optimized formulation batch shows less disintegrant time (52±0.24). The In– Vitro wetting time was less (i.e., 90s) in optimized formulation F2. The water absorption ratio of the formulated tablets was found to be in the range of (90.3±0.027 ). The cumulative drug dissolved in the optimized formulation F2 was found to be ( 99%) in 5 min. Lepidium sativum mucilage was found to be a super disintegrant which enhanced the dissolution efficiency when combined with Crospovidone, croscarmellose sodium, and hence it could be used in the formulation of fast dissolving tablets to provide immediate release of the contained drug within 5 min.
The purpose of this study was to asses the effects of fruit juice of Murraya koenigii (FJMK) on biochemical and physiological parameters in terms of repeated dose toxicity study in mice. Three doses 2.5, 5.0, and 10ml/kg were administered to a groups of 12 animals (six male and six female) daily for 28 days respectively. Animals receiving the vehicle (water) served as a control. The biochemical parameters like RBC, WBC, glucose, haemoglobin, cholesterol, creatinine, bilurubin, SGPT and SGOT were analyzed in all groups of animals respectively. While in physiological parameters like daily food consumption, weekly body weight, locomotor activity, grip strength, visual, auditory and organ weights were analysed respectively. Result of study showed that none of the animals from 2.5, 5.0 and 10ml/kg showed test material related changes in RBC,WBC, haemoglobin, creatinine, bilurubin, SGPT and SGOT parameter respectively. Similar results showed for some physiological parameter like visual, auditory, grip strength and locomotor activity. There were no other changes except the drastic and sudden weight loss, decrease in cholesterol and glucose of these animals. Animals from 5.0 and 10 ml/kg showed loss of subcutaneous fat during last two week of treatment. At the same dose level there decreases in total cholesterol and glucose level. The significant effect was observed with at dose of 10 ml/kg. There was increase in food consumption of animals at same dose level (5.0 and 10 ml/kg) compare to control and 2.5 ml/kg dose of animals. From results it conclude that administration of FJMK for 28 days decreases the body weight, subcutaneous fat and blood glucose level, as observed in medium and high dose group so it can be attributed to the intended use of fruit juice for antidiabetic and antiobesity dietary supplement.
Values of density(ρ), ultrasonic speed(u) and viscosity(η) have been determined for four amino acids (glycine, L-alanine, L-valine and L-leucine) in aqueous fructose solutions (0.05, 0.10, 0.15, 0.20) M at T = 298.15 K. Apparent molar volume (Vφ), partial molar volumes (V0φ) and transfer volumes (ΔVφ0) are evaluated using density data. Apparent molar compressibility (Kφ), partial molar compressibility (K0φ) and transfer compressibility (ΔK0φ) have been calculated using ultrasonic speed data. Viscosity B- coefficients of Jones-Dole equation, B- coefficients transfer (ΔB), free energy of activation per mole of solvent (Δμ10*) and solute (Δμ20*) are estimated using viscosity data. The linear correlations of Vφ0, ΔVφ0, Kφ0 ,ΔKφ0, B, ΔB, Δμ20* for a homologous series of amino acids have been used to calculate the contribution of charged end groups (NH3+, COO-), CH2 and other alkyl chain of the amino acids. Our study concludes the existence of strong solute solvent interaction in the studied systems. Furthermore, all the four amino acids behave as structure maker in aqueous fructose solutions. The thermodynamics of viscous flow has also been discussed.
Obesity has become major worldwide health problems. Serotonin (5-hydroxytryptamine; 5-HT) is a neurotransmitter that contributes to the regulation of many physiological processes and abnormalities of the serotonergic system have been implicated in the pathogenesis of obesity. 5-HT 2A receptor is belongs to G-protein coupled receptor (GPCR), expressed widely throughout the central nervous system (CNS). Hypothalamic 5-HT 2A receptors might have a role in the regulation of feeding and energy homeostasis. 5-HT 2A receptor gene expression was increased in association with obesity. 5-HT 2A receptor antagonism increases expression of adiponectin and decreases plasminogen activator inhibitor 1 (PAI-1) expression via the 5-HT 2A receptor signaling cascade. Recently, development of 5-HT 2A receptor antagonists as a novel therapeutic strategy for obesity and associated comorbidities has been the focus of much interest. Here, we describe the role of 5-HT 2A receptor in pathogenesis of obesity.
Coumarins, an old class of compounds, are naturally occurring benzopyrone derivatives. The titled compounds of N-[2-(2-substituted aryl/heteryl)-4-oxo-1,3-thiazolidin-3-yl]-2-oxo-2H-chromene-3-Carboxamide derivatives (IV-a-m) totally thirteen compounds were prepared from benzylidine derivative of coumarin -3- carbohydrazide (II) which were derived from 3-carbethoxy coumarin derivative by Knoevenagal condensation method. All the Newly synthesized coumarin substituted with thiazolidinones was evaluated for their anti inflammatory activity. Screening of all the synthesized coumarin derivatives by Hind paw oedema method using the standard drug used is Aspirin and test Compounds were give at a dose of 100 mg/kg (bw).
The kinetics of hydrolysis of Mono-4-methyl-2-nitroaniline phosphate has been carried out in buffer solution at 50°C in the pH range 0.00 to 7.46. The rate of reaction increases with increase in pH up to 4.17. The maximum value at pH 4.17 is due to hydrolysis via mononegative and neutral species. The neutral and monoanion have been found to be reactive. The experimental and theoretical rate values are in good agreement.The nature of molecularity of hydrolytic reaction has been decided on the basis of temperature and solvent effect. The monoester involves P-N bond fission, which is strengthened by comparative kinetic rate data.
docking complex of HMG CoA Reductase protein (PDB ID: 1DQ8) with 1I  
Hypercholesterolemia, or high cholesterol, occurs when there is too much cholesterol in the body. Cholesterol is a soft, waxy, fat-like substance that is a natural component of all the cells of the body. Molecular docking is used to predict the binding orientation of small molecule drug candidates to their protein targets in order to in turn predict the affinity and activity of the small molecule. Hence docking plays an important role in the rational design of drugs. The present study is deals with the molecular docking of derivatives of 2α-hydroxyursolic acid which is the active component of the plant Banaba leaves (Lagerstroemia speciosa L. Pers, Lythraceae) against HMG CoA reducatse involved in cholesterol biosynthesis using AutoDock software. The protein file of HMG CoA reductase [PDB ID: 1DQ8] was taken from the protein data bank. The lead moiety 2α-hydroxyursolic acid has shown best ligand binding energy -5.32kcal/mol. All the derivatives have shown best ligand binding energy between–2.82 kcal/mol to -12.52kcal/mol. Out of the nine derivatives 1I show best ligand binding energy as -12.52 kcal/mol.
The water insoluble anti-diabetic drug nateglinide may be slowly or incompletely dissolved in gastro intestinal tract. The rate of dissolution and bioavailability of the drug may be increased by using superdisintegrants in its immediate release tablets. In the present study the selection of proper superdisintegrants among sodium starch glycolate, cross povidone, starch 1500 and cross carmelose sodium (CCS) was carried out to develop immediate release tablets of nateglinide. The differential scanning calorimetry, isothermal stress testing and FT-IR studies were carried out for compatibility testing between drug and excipients used in tablets. A 32 full factorial design was used to investigate the joint influence of 2 independent variables: amount of selected superdisintegrants, CCS and hardness of the tablets. The results of multiple linear regression analysis revealed that the dependent variables; disintegration time and drug release at 0.5h values are strongly dependent on the selected independent variables. The sign of coefficient of polynomial equation signified that an increase in disintegration time on decreasing the hardness of the tablets. An increase in the value of drug release at time 30 min observed on increasing the concentration of CCS. A checkpoint batch was also prepared to prove the validity of the evolved mathematical model. Tablet (F-5) containing 4%w/w of CCS at 5 kg/cm2 met the required DT (as per USP limit) and DR0.5 (100%). The systematic formulation approach helped in understanding the effect of formulation processing variables. Stability studies of factorial batches indicated that no significant change in appearance of the tablets, disintegration time, and percentage drug release were observed.
The present study was undertaken to assess the potential of Tamarind seed polysaccharide (TSP) to act as a matrix former in sustained release matrix tablets of Glipizide. The polysaccharide was isolated and confirmed by phytochemical analysis. The drug and isolated polysaccharide was found to be compatible as confirmed by IR spectral studies and Differential Scanning Calorimetry. The TSP powder was evaluated for its micromeritic properties viz. Bulk density, Tapped density, Angle of repose, Hausner’s ratio, Carr’s index and the results indicated good flow properties. The isolated polysaccharide was also evaluated for various physicochemical properties such as solubility, swelling index, melting point and viscosity. The optimized sustained release dosage form of Glipizide with TSP was prepared and evaluated using Response Surface Methodology by employing a 32 full factorial design. Independent variables studied were concentration of TSP (X1) and type of diluents (Lactose, Starch and MCC) (X2). The dependent variables were percentage drug release at 4h (Q4), 8h (Q8) and swelling index (SI). The formulated tablets were found to have better uniformity of weight and the drug content with low SD values. The in vitro drug dissolution study was carried out using USP 22 apparatus II, paddle method and the release mechanisms were explored. The release data was incorporated into various mathematical models and the drug release mechanism of formulations was found to be non Fickian diffusion. Polynomial equations and response surface plots were generated for all dependent variables. It was observed that all the factors had significant contribution on all dependent variables. In vitro drug release study was compared with the commercial Glynase XL tablets using the similarity factor (f2). The dissolution study proved that dried Tamarind seed polysaccharide can be used as a matrix forming material for making once daily Sustained release matrix tablets of Glipizide.
The aim of the present work was to formulate nanoparticles for pioglitazone hydrochloride drug. Pioglitazone hydrochloride is a antidiabetic drug, and BCS Class - II drug having low solubility and high permeability. Nanoparticles were prepared by Solvent displacement method using 32 full factorial design. The concentration of Chitosan (X1) and Pluronic F68 (X2) were chosen as independent variables while percentage drug release at 12th hour, drug entrapment efficiency and particle size was taken as dependent variables. The dissolution profile of all nine factorial formulations was fitted to zero order, first order, Higuchi and Korsemayer Peppas models to ascertain the kinetic modeling of drug release. The prepared formulations were further evaluated for drug content, drug excipient interactions, surface morphology by SEM, Differential scaning calorimetry (DSC), Zetapotential. All independent variables were found to significantly influence the particle size and entrapment efficiency. The in- vitro drug release profile showed that the suitability of Chitosan loaded nanoparticles in sustaining pioglitazone release for prolonged time.
The present research concerns the formulation and evaluation of sustained release pellets filled capsule of opioid analgesic, Tramadol HCl. Development of sustained release dosage form is to maintain therapeutic blood levels of the drug for extended period of time. Sustained release formulation provides uniform concentration at absorption site, maintains plasma concentration within a therapeutic range, reduces the dosage frequency and minimizes the side effects (nausea) associated with drug by avoiding dose dumping effect. Oral sustained release pellet formulations of Tramadol HCl were prepared using extrusion-spheronization technique. Pellets provide specific advantages of smoother plasma concentration profile and gradual absorption than tablet. HPMC K100M and EC along with the coating of Eudragit RSPO were chosen to achieve the desired dissolution profile. Their concentrations were optimized using 32 full factorial design to achieve the aim of sustaining the drug release for 12 hours. The prepared pellets were studied for different flow properties and drug release studies.
In the present paper QSAR study has been attempted on the in vitro antimycobacterial activities of NBenzylsalicylamides and N-Benzylsalicylthioamides derivatives reported by Dolezal et al against Mycobacterium avium CNCTC My (330/88) using electrotopological state atom (E-state) parameter. The reported minimum inhibitory concentrations [MIC] of the compounds determined after 14 days of incubation. Different statistical tools used in this communication are stepwise regression analysis and partial least squares analysis (PLS). All the developed models indicate the importance of connecting moiety methylcarboxamido / methylthiocarboxamido group between two substituted phenyl groups. From the PLS models it has been observed that hydroxyl group is negatively contributed towards activity. The models also indicate the Positive contribution of amino group towards activity. Based on internal validation (Q 2), external validation (R 2pred) PLS analysis was found to be the best model (Q 2=0.699, R 2pred=0.832).
Comparative molecular field analysis and comparative molecular similarity indices analysis (CoMSIA) based on three dimensional quantitative structure-activity relationship (3D-QSAR) studies were conducted on a series (28 compounds) of indolealkanoic acid derivatives as potent diabetes mellitus inhibitors. The best prediction was obtained with a CoMFA standard model (q 2= 0.850, r 2= 0.983) and with CoMSIA combined steric, electrostatic, hydrophobic, hydrogen bond donor and acceptor fields (q 2= 0.856, r 2= 0.977). CoMFA and CoMSIA contour maps were then used to analyze the structural features of ligands to account for the activity in terms of positively contributing physiochemical properties such as steric, electrostatic, hydrophobic and hydrogen bond donor fields. The resulting contour maps produced by the best CoMFA and CoMSIA models were used to identify the structural features relevant to the biological activity in this series of analogs. The information obtained from CoMFA and CoMSIA 3-D contour maps can be used for the design of indolealkanoic acid derivatives as potent inhibitors of diabetes mellitus. The binding mode of the high active compound at the active site of Novel Benzothiazepine Inhibitor in Complex with human Aldose Reductase (PDB id: 3P2V) was explored using FlexX docking program and hydrogen-bonding interactions were observed between the inhibitor and the target.
Top-cited authors
Sundarapandian Vaidyanathan
  • Vel Tech - Technical University
Maheshgouda Basagouda Patil
  • SDVS Sangh, SAnkeshwar - 591313
Ravi Kumar
  • Independent Researcher
Cmm Madhusudhana
  • Computer Sciences Corp
Mahesh Paschapur