iosr-JPBS   Volume-5 ~ Issue-4

Abstract: Free radical oxidative injury has been linked to myocardial infarction. This study has been taken to analyse the extent of oxidative injury and the antioxidant defensive mechanism by estimating Malonaldehyde and defensive markers such as serum Ceruloplasmin,serum Catalase antioxidant defence by S. Uric Acid and S. Ceruloplasmin. On 5th day of MI, oxidative and serum Uric acid at 6-12 hrs of onset of myocardial infarction and 5 days after thrombolytic therapy.Out of total 100 cases,50 age matched Control cases and 50 cases of known Myocardial infarction(with ECG report) are taken.Serum Malonaldehyde is estimated by thiobarbituric acid method.Serum Ceruloplasmin by O-diansidine method,serum Uric acid by uricase kit method.Serum Catalase activity by Spectrophotometric assay of complex of Molybdate and Hydrogen peroxide. Routine Blood sugar,blood urea,Serum creatinine,Haemoglobin %,HIV,HBs Ag also done .The data is statistically analysed and the mean,SD values are calculated. Student 't' test and 'p' values are also calculated.Statistically significant increase in Malonaldehyde, Uric acid,Ceruloplasmin in MI cases compared to controls with 'p' values <0.000 is seen.Significant decrease in serum Catalase in cases compared to patients with 'p' value <0.000 is seen.There is a significant decrease in serum Uric acid,Malonaldehyde,Ceruloplasmin and increase in serum Catalase after 5 days of Thrombolytic therapy.The area under table of the ROC curves of different parameter is compared.In present study there is significant increase in serum Malonaldehyde, Uric acid,Ceruloplasmin levels in MI cases compared to controls. Malonaldehyde is the best markers to indicate Oxidative Stress In MI.

Key Words: Ceruloplasmin , Malonaldehyde , MI-Myocardial infarction, Reactive oxygen species and Uric acid

Abstract:In this paper, we explore the use of statistical learning approaches to predict drug-target like proteins from their primary sequences in order to facilitate the rapid discovery of new potential therapeutic targets from the large quantity of sequences in human genome. It was found that the Support Vector Machine (SVM) algorithm with a fine-tuned Gaussian kernel was able to make reasonably accurate prediction, which showed its potential to be used in the genome scale rapid drug target discovery, as a novel in silico approach supplementary to the conventional experimental approaches.

Keyword: SVM, Therapeutic, PCA, ICA

Abstract: Hypertension is a heterogenous disorder in which patients can be stratified by pathophysiology characteristics that have a direct bearing, on the efficacy of specifically targeted antihypertensive medications, on the detection of potentially curable forms of hypertension and on the risk of cardiovascular complications.The study is done to compare the effect of antihypertensive treatment with Enalapril and Atenolol on oxidative stress and insulin resistance in patients with essential hypertension .Plasma Malonaldehyde(MDA), reduced Glutathione and Catalase were estimated to measure oxidative stress and fasting plasma Insulin to measure Insulin resistance....

Keywords – Atenolol,,Catalase,Enalapril,Insulin resistance,Malonaldehyde,oxidative stress

Abstract: This study investigates the in vitro interactions of lisinopril with metformin which is important for the possible formulation of polypills comprising both drugs. The study was conducted using the USP apparatus II paddle method. The media used were buffer pH 1.2, 4.5, and 6.8 to simulate gastrointestinal tract pH. Lisinopril tablets (10 mg) were run in the presence of 500 mg metformin tablets and the degree of interaction was established after analyzing the dissolution samples with validated High Performance Liquid Chromatographic methods. The results indicated a statistically significant difference in the effect of lisinopril on the dissolution profile of metformin at pH 1.2, 4.5, and 6.8, with a decrease in the percentage of metformin released (p = 0.0052; p = 0.0037; and p = 0.0155, respectively). The effect of metformin on the dissolution profile of lisinopril was only statistically significant at pH 1.2 and 6.8 with an increase in the percentage of lisinopril released (p = 0.0062; p =0.0036, respectively), and no statistically significant difference at pH 4.5 (p = 0.7174). Thus, the co-administration of metformin with lisinopril could alter the bioavailability of both drugs. More studies may be conducted in vivo to further ascertain the level of interactions using animal or human model.

Keywords – Dissolution, Interactions, Lisinopril, Metformin, Polypills

Abstract: The aim of this study was to investigate the iron- and sulphur-oxidizing activities of thermophilic bacteria with reference to the possible use of such bacteria in the extraction of metals from mineral sulphides. The initial characterization of a range of isolates was based on growth studies with iron and sulphur substrates and on the comparison of whole cell. Three groups of bacteria were isolated and studied moderately thermophilic iron- and mineral sulphide-oxidizing bacteria, moderately thermophilic sulphur oxidizers and extremely thermophilic Sulfolobus-like organisms. Both moderately and extremely thermophilic acidophiles were isolated from hot spring and coal pile samples. The moderately thermophilic ironoxidizing bacteria and the extreme thermophiles which were examined were sub-divided into three and four sub-groups respectively, moderate thermophiles did not produce higher rates of ferric iron production than the mesophile T. ferrooxidans but iron oxidation was less sensitive to inhibition by chloride in a vessel containing a thermophile than in a vessel operating with the mesophile. Iron oxidation during autotrophic growth of moderately thermophilic acidophiles and the rapid dissolution of mineral sulphides during the autotrophic growth of both the moderate and the extreme thermophiles were demonstated, thus considerably increasing the potential industrial significance of these bacteria. The yield of soluble copper from a chalcopyrite concentrate was shown to increase with temperature from relatively low yields with the mesophile T. ferrooxidans, through moderate yields with the moderately thermophilic bacteria to almost complete mineral solubilization with the newly isolated Sulfolobus strains.

Keywords- thermophilic, heterotrophic, oxidizing, isolates, autotrophically, mixotrophic, chalcopyrite

Abstract: Sustained release gastroretentive dosage forms enable prolonged and continuous input of the drug to the upper parts of the gastrointestinal (GI) tract and improve the bioavailability of medications that are characterized by a narrow absorption window. A new strategy is proposed for the development of gastroretentive dosage forms for ofloxacin preferably once daily. The design of the delivery system was based on the sustained release formulation, with floating and swelling features in order to prolong the gastric retention time of the drug delivery systems. Different polymers, such as psyllium husk, HPMC K100M, crospovidone and its combinations were tried in order to get the desired sustained release profile over a period of 24 h. various formulations were evaluated for buoyancy lag time, duration of buoyancy, dimensional stability, drug content and in vitro drug release profile. It was found that dimensional stability of the formulation increases with the increasing psyllium husk concentration. It was also found that in vitro drug release rate increased with increasing amount of crospovidone due to the increased water uptake, and hence increased driving force for drug release. The optimized formulation was subjected to stability studies at different temperature and humidity conditions as per ICH guidelines.

Keywords: Ofloxacin; Sustained release; Psyllium husk; Gastroretentive

Abstract: A highly sensitive ultra-high performance liquid chromatography tandem mass spectrometry (UPLC–MS/MS) method was developed for the quantification of Almotriptan in human plasma.To the best of our knowledge; this is the sensitive method for the quantification of Almotriptan in human plasma. Matrix effects were strongly reduced and selectivity increased by using an efficient chromatographic separation on a sub-2μm column (Acquity UPLC HSS T3 1.8 μm, 2.1 × 50 mm) in 3 min with a gradient of ammonium formate 5mM and acetonitrile as mobile phase at a flow rate of 0.4 ml/min. Detection was made using a tandem quadrupole mass spectrometer operating in positive electrospray ionization mode, using multiple reaction monitoring. The procedure was fully validated according to the latest Food and Drug Administration guidelines. Very good results were obtained by using Naratriptan as internal standard, to compensate for the variability due to the extraction and ionization steps. The method was very sensitive with lower limits of quantification of 0.1 ng/ml for Almotriptan. The upper limit of quantification was 250 ng/ml. Accuracy (94.0–105.7%), Precision (1.0–6.7%), and internal standard-normalized matrix effects (95–102%) were in accordance with international recommendations. The method can be used for pharmacokinetic studies.

Keywords: Almotriptan, Human plasma, Multiple reaction monitoring, Quantification, Solid Phase Extraction, UPLC-MS/MS

Abstract: The antibacterial activity of ethanol, hot and cold water extracts of both fresh and dried leaves as well as the juice extracts of Moringa oleifera Lam. were obtained by standard disc diffusion methods against some human pathogenic bacteria; Staphylococcus aureus, Streptococcus faecalis, E. coli and Pseudomonas aeruginosa. The ethanol extracts of fresh leaves and dried leaves displayed a potential broad-spectrum activity against all the tested organisms, Staphylococcus aureus, Streptococcus spp, E. coli and Pseudomonas aeruginosa. Also, cold water extracts of fresh and dried leaves as well as hot water extracts of fresh and dried leaves inhibited the growth of the tested organisms with the exception of E. coli and Pseudomonas aeruginosa which were not inhibited by cold and hot water extract of fresh and dried leaves. The result of this study revealed that, the antibacterial activity of the extract could be enhanced if the components are purified. The plant therefore holds a promise as a potential source of new drugs for treating infections caused by these clinical pathogens.

Keywords: Antimicrobial, leaf juice, Moringa oleifera, Pathogenic bacteria.

Abstract: Dihydroartemisinin-piperaquine phosphate (P-ALAXIN®) is a fixed-dose artemisinin-based combination therapy (ACT). Despite the efficacy and tolerability of this drug, there are adverse effects associated with it. This study was designed to investigate potential toxicity of two different doses of the drug in rats.Thirty rats (Wistar strain) weighing 200±20g were completely randomised into three treatment groups; Group A (control), Group B (Therapeutic dose) and Group C (double therapeutic dose of P-ALAXIN®). Creatinine, Urea and Bilirubin levels were significantly (p<0.05) elevated in the plasma of the rats that received the two doses of P-ALAXIN ® by 67 and 117%; 33 and 67%; 85 and 119% respectively when compared to the control. Activities of plasma ALP, ALT, AST and GGT were also significantly (p<0.05) higher in the two treated group by 22 and 32%; 26and 36%; 18 and 34%; 43 and 91% respectively. Moreover, plasma Total cholesterol, HDL-cholesterol, LDL-cholesterol and triglycerides in the two treated groups were significantly increase (p<0.05) by 24 and 38%; 38 and 75%; 37 and 88% and 28 and 64% respectively. These were accompanied by a significant (p<0.05) increase in the MDA level by 33 and 45% respectively in the two treated groups. Furthermore, the two doses of P-ALAXIN® significantly (p<0.05) reduced hepatic ascorbic acid and GSH by 44 and 58% and 44 and 75% respectively, with a concomitant reduction in activities of hepatic GST. Similarly, there was a significant reduction in the activities of hepatic Catalase, and SOD. These data indicate that therapeutic and double therapeutic doses of P-ALAXIN® has adverse effects on both enzymic and non-enzymic antioxidant status and induces marked renal and liver damages and oxidative stress in rats.

Keywords: Dihydroartemisinin-piperaquine phosphate,Therapeutic and Double therapeutic doses,Oxidative stress Renal and Liver damage.

Abstract: The antimicrobial efficiency of Phyllanthus amarus Schum. and Thonn, medicinal plants (leaf extracts), was examined using ethanol and chloroform as solvents and tested against human pathogens ; Staphylococcus aureus, Escherichia coli, and Candida albican, using the agar well-diffusion method and minimum inhibitory concentration. The result of the phytochemical analysis of the plant showed that the plant contain, alkaloid, tannins, steroid, saponins, phlobatannin, terpenoids and cardiac glycoside while anthraquinone was absent. The plant showed significant activity against all pathogens, but the alcoholic extract of P. amarus showed the maximum zone of inhibition and minimum inhibitory concentration against all the microorganisms. The alcoholic extracts of these plants could be a possible source of obtaining new and effective herbal medicines to treat infections; hence, it justified the ethnic use of P. amarus against various infectious diseases.

Keywords: Antimicrobial, Phyllantus amarus, Phytochemical, Pathogenic bacteria, Zones of inhibition.

Abstract: The lips and associated structures, in different groups of fishes, are greatly modified in relation to the characteristic mode of feeding, food preference and the mode of life exhibited by the fish. The successful maintenance of fish populations in challenging environments requires responsive adjustments in their behaviour, morphology and physiology and these have been reflected by modifications at the level of their organ systems, organs and tissues. The lips are no exception to this. The importance of food in daily life of a fish is obvious, and is reflected in the form of the mouth, lips, jaw and so on. These structures present more diverse modifications than any other organ of the body. The functional aspects of the lips and associated structures in family Gobiidae, Cobitidae, Belontiidae and few species of Cyprinidae show considerable variation and exhibit unique morphological modifications associated with their lips and other structures around the mouth regarding information on the level of surface architecture as seen under SEM in relation to various food and feeding habits and ecological niches.

Key words: Cyprinidae, fishes, lip and morphology

Abstract: Cancer is a highly complex disease due to the disruption of tissue architecture. Thus, tissues, and not individual cells, are the proper level of observation for the study of carcinogenesis. Thus the shape and regularity of the epithelial connective tissue interface(ECTI),has classically been used to describe both physiological and pathological changes in the oral mucosa,including cancer. However, the description of ECTI has most often been subjective. The use of fractal geometry, has therefore been used to describe the irregularities of ECTI profiles taken from the oral mucosa both in normal and abnormal cases.Also the Pseudoepitheliomatous hyperplasia (PEH) of the covering epithelium mimics the squamous cell carcinoma invasion.PEH cells do not show marked atypia ,but the presence of pseudoinvasive pattern remains a diagnostic problem since several misdiagnosed cases have been reported. Similar diagnostic problems do occur sometimes between normal & dysplasia or dysplasia & squamous cell carcinoma. The aim of this study is to investigate the objective morphometric criteria to distinguish each entity separately ie. normal ,dysplasia ,pseudoepitheliomatous hyperplasia & squamous cell carcinoma .

Keywords: oral mucosa, squamous cell carcinoma, fractal analysis, complexity, tumor shape

Abstract: Allium Cepa has been used in folk medicine for treatment of tumors and to relieve dropsy (heart failure related edema). This present study was conducted to determine the effects of the aqueous extract of onion (Allium cepa) on Blood parameters in Wistar rats. Eighteen (18) rats (105 – 158 g) were randomly selected into 3 groups of 6 animal (n = 6) each, Group A served as the control received 1 ml of distilled water while Group B received 45 mg/kg body weight of onion juice and Group C received 20 mg/kg body weight of onion juice extracts for 21 days of experimental period. Animals were sacrificed by cervical dislocation 24 hours after the last administration and blood samples were collected via the retro-orbital route with the aid of a capillary tube, into an EDTA bottle for analysis. The result shows that the juice extracts at various doses significantly (p<0.05) increase the total white blood cell counts, Lymphocyte count, Neutrophils count, also there was a significant (p<0.05) increase in the red blood cell count in rats treated with onion juice. The packed cell volume of rats treated with onion extract were significantly (p<0.05) increased. There was no significant (p˃0.05) increase in the Platelet count, Monocytes count, Eosinophil count, Basophil count of the rats in all groups. Allium cepa affect the amount of circulating blood cells thus promoting health benefits.

Keywords: Allium cepa, adult wistar rat, Blood parameters, Aqueous extract.

Abstract: Cancer is the 2nd leading cause of death in humans. Proteine.g. tyrosine kinaseleads to cancer when become constitutively active due to mutation. So there is a need to develop tyrosine kinase inhibitors to avoid cancer.In the present study the problem of designing an anticancer drug with more efficacies was solved by using computer aided drug designing (CADD). Antioxidants were used as tyrosine kinase inhibitors. Molecular docking studies of antioxidants belonging from different classes were carried out with human target protein having pdbid:2HCK in order to find out the most active antioxidant drug having high inhibitory activity in cancer.Docking of 36 selected ligands, comprised of active drugs for cancer and compounds having anticancer activity, was done with the active site of protein 2HCK and a lead compound was recognized on the basis of hydrogen bonding, hydrophobic and ionic interactions. Three analogues of the lead compound were designed to enhance its activity against cancer. Analogues were docked with protein 2HCK and their interactions showed that they could possess good inhibitory activity against cancer with suitable drug-like properties as compared to other active drugs for cancer and therefore could be recommended for further studies.

Keywords: Antioxidants, Tyrosine Kinase inhibitors, lead compound, Cancer, Molecular docking

Abstract: Recently, there have been growing concerns over the reliance and safety of untested and unregulated plant remedies. Brideliaferruginea is one of the herbal plants commonly used, of which chronic toxicity studies are yet to be examined. Sub-chronic toxicological effects of methanolicbenth bark extract of brideliaferruginea on biochemical indices in rats were evaluated. Three groups of six animals each were used in this study. Group 1 (control)received no treatment. Group 2 and 3 (treated)received calculated doses of 250mg/kg and 500mg/kg of the extract orally for four weeks. All animals were sacrificedusingdiethylether anesthesia 24hours after the last dosing and blood samples taken. Periodic weights and packed cells volume(PCV) were measured, portions of the heart and brain were excised, homogenized and used for bioassays. From our results, we observedsignificant decrease (p<0.05) in PCV; superoxide dismutase in Heart and Brain; and brain catalase. No significant effect (p>0.05) was observed in heart and brain;reduced glutathione;catalase, also no effect was observed in lipid peroxidation of heart and brain. However, the two doses kept the weight constant for a period of four (4) weeks. Overall, thebark extract of brideliaferrugineamay affect antioxidant and blood status as well as keeping body weight constant. We suggest therefore thatdoses approaching or above 250mg/kg body weight should be avoided by individuals or in herbal preparations.

Keywords: Herbal plants, Brideliaferrugineabenth bark, Antioxidants, PCV and Body weight.

Abstract: The last decades have witnessed an upsurge of neuropeptides research. These substances regulate or influence various functions in the body like appetite, water intake, learning and memory, adaptive responses to environmental stress, thermoregulation and fever, social behaviour, and sleep. Kisspeptin (formerly known as metastin) is a protein that is encoded by the KISS1 gene in the Anteroventral periventricular nucleus (AVPV) and Arcuate nucleus (ARC) nuclei of the hypothalamus which was originally discovered in 1996 by Lee and Welch while conducting oncology research at the Pennsylvania State University College of Medicine. It couple to G-protein receptor ligand for (GPR54) G-protein receptor 54 (Messager et al, 2005). It is found to play many important physiological roles which include: initiation of puberty, anti-oxidative effect, regulation of prolactin release, glucose homeostasis, role in nutrition status and fertility, role in pregnancy, increases sensitivity of chemoreceptors on type 2 carotid bodies, anti-metastatic effect, hot flushes in post-menopausal women. Kisspeptins are so named because the arginine–phenylalanine residues are present at the amino terminal "Arg-Phe-NH2"; all of the kisspeptin fragments have a C-terminal decapeptide that is critical for biological activity (Clements et al, 2001; Kotani et al, 2001).

Abstract: In this proposal synthesis of a very simple Schiff base from substituted benzoic acid and substituted aldehyde and formed complex with transition metal such as zirconium (IV). The chemical structure of the synthesized metal ligand complex were confirmed by IR and elemental analysis. This complex showed the antimicrobial and antifungal activity and examined against different gram +ve and –ve bacteria and fungal strains.

Keywords: Antimicrobial, Antifungal activity; substituted aldehyde, Schiff base.

Abstract: The growth pattern and nutritional status of under five children in Owo Local Government Area of Ondo State was assessed between May and November, 2009 to know if their growth were normal or constitute public health problem. A total of 600 randomly selected male and female under-five children were surveyed using anthropometry. 120 infants (0.5-12 months old) were randomly selected from 15 primary hath centres while 480 children (aged 13-60 months) were randomly selected from crèche and nursery schools. Anthropometric measurements of subjects such as weight, height and MVAC were obtained. Data were analyzed using EPI-Info 2000 nutritional software. Findings show that majority of the children's growth in height and weight slightly fall below CDC/NCHS growth curve at 50th percentile of reference population when compared. Overall mean weight, height and MUAC of the children were 10.6kg, 78.5cm and 16.3cm respectively. 17% and 43% of all the children were stunted and underweight, while 9% and 6% were severely stunted and underweight (z-score <-3 S.D). Chronic and severe or acute form of malnutrition affects child's mental capability; it erodes attention span and learning process. It is one of the highest causes of morbidity and mortality. Even stunting among the potential female mothers can bring about maternal morbidity and obstructed child labour, which becomes a recycle generational problem particularly through the female life course.

Keywords: children, Growth pattern, Nutritional status, Malnutrition.

Abstract: Pregnant women have been widely recognized as a vulnerable group from health point of view. They need more food than normal person for the proper nourishment of the growing fetus. The study was carried out among 150 pregnant women of whom 80 of them attended antenatal clinic in the general hospital while 70 used the traditional birth home for antenatal .A structured questionnaire was used for data collection. Dietary information was obtained using food frequency and 24-hour dietary recall. The result showed that 56.4% of the women consumed cereals more than and 10.0% took it once in a day, 37.2% admitted the consumption of legume once 5.1% consumed it twice in a day. The mean nutrient intake of the respondents showed that the intake of energy was 93% of the RDA, while protein was above the RDA (113%). However vitamin A, E, C and folic acid were 40%, 20%, 30% and40% of RDA respectively. Also, intake of calcium and iron was found to be 36%, and 50% respectively .The nutrient comparison of the respondents showed that women from the general hospital were able to meet up with their energy, protein, and zinc as it was found to be 99%, 122%, and 100% respectively while the respondents from the traditional birth home showed poor nutrient consumption.

Key words: Pregnant women, food frequency, nutrients, traditional birth home.