The Pharmaceutical and Chemical Journal

10-16

Authors: Ugwu, Melvin N, Asuk, Atamgba A, Eteng, Mbeh U, Amaku, Etetim E

Benign prostatic hyperplasia (BPH) is an age-related disease, as the prostate enlarges, the layer of tissue surrounding it stops it from expanding, causing the gland to press against the urethra. The symptoms of BPH vary, but the most common is problems with urination which makes life unbearable. We investigated seed extract of Nigerian indigenous plant Prosopis africana (PA) effect on BPH. BPH was induced in male rats weighing 250-350g through exogenous administration of testosterone and estradiol. A total of 25 rats were divided into five groups. One group was used as a control and the other groups received subcutaneous injections of the two hormones. Groups 1 to 2 were treated orally with different doses of extracts and group 3 received finasteride, group 4 was left untreated and group 5 served as normal control. After forty-five days of treatment with the extract the animals were sacrificed blood collected through cardiac puncture for biochemical analysis. The prostate were harvested and weighed. Treatment with extract caused a significant decrease in the size of the enlarged prostate in a dose related manner (p<0.05) when compared with the BPH control group. Progressive weight gain occurred in extract and finasteride treated groups. The level of cholesterol and LDL-C were significantly reduced when compared to the BPH control. There was no significant change in HDL concentration in all groups. The significant reduction of cholesterol and LDL supported by reduced prostate weight suggest that the extract hold potentials for reversal and reduction of induced BPH in rats model.

24-30

Authors: E.I. Okoye, A.E. Usiakpebru

This work analyzed ten capsules of amocycillin 500 mg each from drug resolving stores (shop 1), Opaclsas Pharmacy (shop 2), Happy Home Pharmacy (shop 3), Cheff Pharmacy Ltd (shop 4) Chimezie Medicine Stores (shop 5). The anti-hypertensive drugs (Nifedipine, 20 mg) were obtained from drug resolving stores (shop 1), Happy Home Pharmacy (shop 2), Cheff Pharmacy (shop 3), Chimezie Medicine stores (shop 4) and D-Global Pharmacy (shop 5). All capsules and tablets were obtained from different locations in Asaba. The analysis carried out on them are disintegration time, percentage uniformity of weight and percentage active ingredients they contain. The disintegration time for amoxicillin obtained from shop 1, shop 2, shop 3, shop 4 and shop 5 are: 11 minutes, 7 minutes, 8 minutes, 9 minutes and 10 minutes respectively. The percentage uniformity of weight for the five amoxicillin are 100 % each. The percentage active ingredients were found to be 104.9 %, 108.1 %, 109.98 %, 103.2 % and 109.3 % respectively. The disintegration time, percentage uniformity of weight and percentage active ingredients conformed to British pharmacopeia specifications. The disintegration time for the five antihypertensive drugs were found to be: 120 minutes, 20 seconds, 18 seconds, 25 seconds and 20 seconds respectively. The percentage uniformity of weight for the five antihypertensive drugs are 100 % each. The percentage active ingredients for them are 102.5 %, 95.4 %, 107.6 %, 101.5 % and 92.8 % respectively. Again, the disintegration time, percentage uniformity of weight and percentage active ingredients, all conformed to B.P. specification.

38-48

Authors: Akwasi Acheampong, Lydia T. Amankwaa, Isaac O. Afriyie, Kennedy A. Baah

Microdesmis puberula is a plant that is used in traditional medicine for the treatment of diarrhea, stomach-ache, intestinal worms, menstrual complaints, sterility, miscarriage, loss of virility and venereal diseases, treat skin conditions, renal pain, severe headache, erectile dysfunction, and snake bite. In this work, methanol and petroleum ether extracts of the stem of Microdesmis puberula were evaluated for phytochemical constituents, antimicrobial activity and antioxidant activity. DPPH scavenging assay and total antioxidant capacity were used for the determination of the antioxidant activity. The agar well diffusion method was used to determine the antimicrobial activities of the extracts against the test organisms, Klebsiellapneumonia, Bacillussubtilis, Salmonella typhi, Enterococcus faecalis, Neisseria gonorhoeae, Escherichia coli, Pseudomonas aeruginosa, Streptococcus pyrogenes, Staphylococcus aureus and Candida albicans. The broth dilution method was used to determine the minimum inhibitory concentrations (MIC) of the methanol and petroleum ether extracts. The methanol extract exhibited antimicrobial activity against both Gram-positive and Gram-negative test organisms with zones of growth inhibition ranging from 12 to 16 mm in the agar well diffusion test, but the petroleum ether did not exhibit antimicrobial activity as it recorded no zone of growth inhibition. The methanol extract was active against the test organisms with MIC range of 6.25 to 12.5 mg/mL and that of petroleum ether ranged from 50 to 200 mg/mL. The reference drug showed activity between 1.56 to 25 mg/mL. The IC50 of the methanol and petroleum ether extract, and the reference drug with regard to the DPPH scavenging activity, were 1.1µg/mL, 1.2 µg/mL and 0.2 µg/mL respectively. Both the methanol and petroleum ether extracts exhibited antimicrobial and antioxidant activity.

57-61

Authors: Nagwa S. Zayed, Mustafa N.S., I.M. El-Berry, Samson Daudet Medza Mve, Haba A.E. Soliman

Current study aimed to maximize multiplication rate, growth parameters and producing superior plantlets which can tolerate acclimatization conditions of Conadria fig cultivar through utilizing of Thidiazuron (TDZ), isopentenyladenine (2iP) separately. Shoots- that passed establishment stage- were cultured on MS medium that contained different concentrations of TDZ and 2iP (0.5,1 and 1.5 mg/l). In addition, activated charcoal and auxin type indole-3-acetic acid (IAA) and indole-3-butyric acid (IBA) were applied in rooting stage to evaluate their influences on root formation. Data indicated that number of shoots was produced on lower concentration of 0.5 mg/l 2iP while, 0.5 mg/l TDZ improved shoot thickness. Also, supplementation of the culture medium with 1.5 mg/l TDZ raised chlorophyll content. However, the optimal combination for number of roots and root length was 1.0 mg/l IBA+0.1mg/l IAA. Meanwhile, using of 1.0 mg/l IBA+0.1 mg/l IAA or 0.1 mg/l IAA increased root percentage (100%) as compared with auxin free medium plus activated charcoal, On another hand no beneficial effect was obtained from adding 0.1 mg/l IAA and1.0mg/l IBA+0.1mg/l IAA to the culture medium when root percentage was concerned. Conclusion of current study was gathering both of 2iP and TDZ since each hormone had a positive impact on proliferation rate, plantlet growth performance and chlorophyll content of fig (Conadria cv.), thereby gathering both of them may lead to promising results. Also, more studies should be carried out to state the optimum combination of TDZ and 2iP to produce ideal proliferation rate with vigor plantlets.

77-83

Authors: Ukpanukpong R.U., Bassey S.O., Edoamodu C.E., Ugor J.A., Omang W.A., Odutuga, A.A.

This study was aimed at investigating the haematological and histological effects of ethanolic leaves extract of Jatropha curcas on Plasmodium berghei infected mice. Forty eight mice weighing between 22-24g were assigned into six study groups of eight mice each. Forty mice were parasitized by Plasmodium berghei and used for extract and orthodox treated groups while eight mice were unparasitized. Group 1 was designated as positive control, group 2 was parasitized and designated as negative control. Group 3 was parasitized and designated as orthodox treated group of 100mg/kg body weight of Lonart DS. Group 4 to 6 were parasitized groups and treated with 400mg/kg, 100mg/kg and 200mg/kg body weight of ethanolic extract of Jatropha curcas leaves. Haematological parameters analyzed were hemoglobin (Hb), packed cell volume (PCV) and white blood cell (WBC). The hematological and histological investigations in groups 3, 4, 5 and 6 in orthodox and extract treated mice with 400mg/kg, 100mg/kg and 200mg/kg body weight of ethanolic extract of Jatropha curcas leaves showed significant reduction in their parasitemia levels compared to negative control group. The ameliorating effect of extract treated groups showed anti-plasmodia and anti-anemic activities which were confirmed in the histological tissues of Plasmodium berghei infected mice.

96-116

Authors: Nermien Z. Ahmed, Shaimaa R. Ibrahim

Doxorubicin (Dox) is a chemotherapy drug used for treatment of wide variety of cancers and the most effective antitumor agents, soon proved to be hampered by such serious problems as the development of cardiotoxicity and heart damage by producing free radicals and oxidative stress along the period of treatment. The current study aims at evaluating the cardio protective effect of Cymbopogon citrates known as lemon grass (LG) and the role of trace element selenium (SE), which is an essential element possessing antioxidant properties and has protective effects against toxicity of some drugs, in attenuating cardiac and heart damages induced by doxorubicin alone and in combination. Animals were divided into seven groups each of seven rats, normal control group; selenium group received (1.5mg/kg b. w., orally) for 7 days, LG group received (200mg/kg b.w. orally) for 7 days and doxorubicin -treated group injecting doxorubicin i.p. 48hrs before decapitation at a dose of (20 mg/kg b.w. / i.p). The doxorubicin - treated animals were divided into 3 groups, one (doxorubicin + SE), second group (doxorubicin + LG) and the third group (doxorubicin+ SE+ LG). Serum CK-MB, LDH, as cardiac damage markers; ALT, AST as indicator of hepatic damage and Urea, creatinine as indicator of renal damage, were measured. MDA, TAC, ROS, TP and genomic DNA, as cardiac oxidative status indices and cardiac antioxidant capacity, were also estemated. Histopathological changes in cardiac tissues were examined. Doxorubicin induced significant increase in serum lactate dehydrogenase (LDH); CK-MB; alanine aminotransferase activities, Urea, Creatinine, malondialdehyde levels, reactive oxygen species (ROS) contents. However, significant reduction in total antioxidant capacity (TAC) and total proteins (TP) were observed. Selenium and Lemon Grass pretreatment caused significant decrease in serum LDH and CK-MB levels; ALT, AST, Urea, Creatinine in serum, significant decrease in cardiac malondialdehyde, whereas, significant elevation in cardiac total antioxidant capacity (TAC) and Total protein (TP), compared to doxorubicin -treated group. Histopathological examination of cardiac heart, liver and kidney tissues confirmed with the previous biochemical results, also, genomic DNA of cardiac heart tissues confirmed with the previous biochemical results. Chronic doxorubicin administration caused cardio toxicity and DNA damage. Selenium (SE) and Lemon Grass (LG) pretreated exerted significant protection against DOX-induced cardiac damage.

123-135

Authors: Adriana Teixeira, Márcio P. de Souza, Thais A. P. Bartiê, Ariovaldo Bolzan, Leonel T. Pinto

The reaction of hemoglobin with oxygen allows oxygenation of the body, ensuring homeostasis and cell survival. Although it occurs in four reversible, successive, and cooperative steps, the reaction is usually treated as a one-step reaction. This article aims to point out experimental and theoretical aspects relevant to the kinetic study of this reaction, but which are generally not taken into account. Just the oxyhemoglobin deoxygenation is discussed, since this step is easier to perform experimentally when compared to oxygenation. Oxyhemoglobin was obtained from the reduction of meta-hemoglobin by size exclusion liquid chromatography using sodium dithionite. Deoxygenation of oxyhemoglobin was performed by rapid mixing with interrupted flow, also using sodium dithionite, but in the absence of oxygen. From the experimental results, the dissociation constant was determined considering the pseudo-first order model. Subsequently, experimental questions were discussed, such as the contribution of at least two hemoglobin conformations in the measured absorbance and theoretical questions, such as limitations of the first order pseudo model. The results indicate that a more complete model is needed to describe oxyhemoglobin deoxygenation as well as a more sophisticated treatment in the experimental data, considering that more than one hemoglobin conformation has a significant absorbance value at a given wavelength.

145-152

Authors: Daniela V. Pencheva, Katia S. Ivancheva, Mina V.Rumenkina, Aleksandrina M. Al-Dzhasem, Ivan N. Ivanov

Objectives: The main goal of the provided experiments was to test the influence of the used in the Disc Diffusion Method (DDM) Mueller Hinton agar (MHA) and to establish its reflection on the interpretation of the antimicrobial test. Methods: This study is based on developed microbiological methodology and outworked protocol for qualification of the Mueller Hinton agar when it is used in Disc Diffusion Method in order to obtain reliable and reproducible results on quality indicators for MHA, appointed by the Clinical and Laboratory Standards Institute (CLSI) and European Committee on Antimicrobial Susceptibility Testing (EUCAST). Results: Conducted studies showed the influence of the used medium MHA or MHA II on the zones of inhibition of antimicrobial discs in DDM, which can impact the interpretation of antibiotic susceptibility of isolates. This kind of testing of the medium MHA gives also the opportunity to establish some deviations in the activity of the antimicrobials used in the production of antimicrobial discs. In serial experiments was encountered a problem with the activity of Gentamicin substance that affects the quality of produced batches antimicrobial discs with him. Conclusions: The experiments established the influence of the used medium MHA or MHA II on the zones of inhibition of antimicrobial discs in DDM. The used protocol with microbiological testing was very helpful as for evaluation of the MHA and for establishment of antimicrobials activity deviations.

163-173

Authors: Akanksha Sharma, Vishal Garg, Manish Kumar Gupta, Vijay Sharma

Febuxostat, is a medication used in the treatment of chronic gout and hyperuricemia. Febuxostat is a non-purine xanthine oxidase. It is a BCS class II drug. It exhibits poor bioavailability about 49% which is attributed to its poor bioavailability and poor solubility. The present work was aimed to overcome its limitation of poor solubility. Drug and beta cyclodextrin complexes were prepared in the ratio 1:1 and 1:2. Studies show that solubility was better for 1:2 ratio (855.20 µg/ml) as compared to that of pure drug (10.50 µg/ml). Tablets were prepared by using ingredients such as Beta-Cyclodextrin, Crospovidone, Locust Bean Gum, Crosscarmellose, Microcrystalline Cellulose, Mannitol, Magnesium Stereate, Sodium Saccharine.

182-190

Authors: Srihari Murthy

Around forty percent of new chemical entities (NCEs) are reported to be poorly soluble in water. This translates to poor bioavailability and, thereby, limits the development of these molecules as drug candidates. It is suggested that nanoformulations of poorly-water soluble NCEs/Drugs are viable routes to increase the bioavailability of these molecules. The role of particle size in molecular dissolution is discussed. Different nanostructures that can incorporate poorly-water soluble NCEs/Drugs and which have been previously reported in the literature such as nanoemulsions, nanosuspensions and nanoscale NCE/Drug-Polymer composites are presented. Methods for the preparation of these nanostructures are discussed. Characterization techniques such as Powder X-Ray Diffraction (PXRD), Dynamic Light Scattering (DLS), Zeta Potential Measurement, Scanning Electron Microscopy (SEM), Transmission Electron Microscopy (TEM), Atomic Force Microscopy (AFM) and Differential Scanning Calorimetry (DSC) are discussed. Finally, an example of an NCE-Polymer Nanocomposite is presented.

196-203

Authors: Tran Vu Phuong, Phan Van Ha Lam, Cao Ngoc Diep

The objectives of this study were analysis of the secondary metabolite products from extract of marine Streptomyces sp. strain ND7a which isolated from sponges at Ha Tien Sea, Kien Giang province, Vietnam. Six bioactive compounds were identified in the organic solvent hexan-aceton and aceton-methanol. The identification of bioactive chemical compounds is based on the peak area, retention time, molecular weight and molecular formular. GC-MS analysis of Streptomyces sp. strain ND7a revealed the existence of the 2-Pentanone, 4-hydroxy-4-methyl, Cyclohexasiloxane, dodecamethyl, Cycloheptasiloxane, tetradecamethyl, Oxime-, methoxy-phenyl, Hexanedioic acid, bis(2-ethylhexyl) ester and Diisooctyl phthalate.

211-224

Authors: Nguyen Tan Binh, Phan Van Ha Lam, Cao Ngoc Diep

The objectives of this study were analysis of the secondary metabolite products from extract of marine Penicillium citrinum strain ND7a which isolated from sponges at Ha Tien Sea, Kien Giang province, Vietnam. Sixteen bioactive compounds were identified in the organic solvent hexan-aceton and aceton-methanol. The identification of bioactive chemical compounds is based on the peak area, retention time, molecular weight and molecular formular. GC-MS analysis of Penicillium citrinum strain ND7a revealed the existence of the 9-Hexadecenoic acid, Hexadecane, n-Hexadecanoic acid, Heptacosane, Octadecane, 3-ethyl-5-(2-ethylbutyl), Tributyl acetylcitrate, 17-Pentatriacontene, Hexanedioic acid, bis(2-ethylhexyl) ester, Bis(2-ethylhexyl) phthalate (in organic solvent hexan-aceton) and Oxime-, methoxy-phenyl, 2-Hydroxy-gamma-butyrolactone, 7,9-Di-tert-butyl-1-oxaspiro(4,5)deca-6,9-diene-2,8-dione, Pentadecanoic acid, 14-methyl-, methyl ester, Hexadecanoic acid, 1-(hydroxymethyl)-1,2-ethanediyl ester, Stigmasterol, γ-Sitosterol (in organic solvent aceton-methanol).

232-239

Authors: Xinming Yu, Meng Zhao, Pingfang Han, Xiaoping Lv

In this paper, two kinds of preparation methods were used to synthesize CdO nanoparticles. NaOH and citric acid were severally mixed with cadmium nitrate to produce the nanocatalyst via precipitation and sol-gel auto-combustion method respectively. The reactants were either ultrasonicated or mechanically shear-mixed for comparison. And the synthesised samples were characterized for their size and structure using X-Ray diffraction (XRD) and scanning electron microscopy (SEM) techniques. And some molecular groups containing in the nanoparticle were detected by Fourier transformer Infra Red (FT-IR).The result revealed that the catalyst prepared by precipitation method under ultrasonic irradiation possesses the better surface characteristics and optical property, which means that theoretically it will shows great photocatalytic properties in the chemical reaction.