The Pharmaceutical and Chemical Journal

11-16

Authors: Aimen Sohail, Tayyaba Ishaq, Ramisha Ashraf, Isra Shahid, Ghazala Yaqub

Arsenic contamination in drinking water is an issue worldwide, which have caused massive impacts on human health. Various countries have reported to have high amount of arsenic in their drinking water i.e. Canada, United States, Chile, Bolivia, El Salvador, Nicaragua, Slovenia, Mexico, Bangladesh, India and others. People in rural areas rely on ground water for drinking purposes so removing arsenic from ground water is a significant challenge. In case of drinking water treatment where the requirement is to reduce few parts per billion the technologies have various limitation and prospects. This paper reviews latest technologies of arsenic treatment (coagulation, sorptive process, adsorption, oxidation, membrane process, biological process, emerging techniques). The technologies should meet basic technical criteria for its implication, the biggest challenge is to apply these technologies in setting where arsenic is high in amount and saving the community by promoting safe drinking water.

23-33

Authors: Adam Buczkowski, Artur Stepniak, Pawel Urbaniak, Bartlomiej Palecz

Spectroscopic examinations of flutamide solubility and 1H NMR measurements (flutamide and cyclocreatine) show that in aqueous solutions, molecules of the antitumor drugs tested stronger interact with macromolecules of cationic PAMAM G5-NH2 dendrimer compared with hydroxyl PAMAM G5-OH dendrimer. Solubility measurements show that cationic PAMAM G5-NH2 dendrimer macromolecules combine more ( 1.40 ± 0.16) flutamide molecules compared with PAMAM-OH G5 ( 0.45 ± 0.15). The results of 1H NMR spectroscopic measurements imply that the combination of flutamide with both dendrimers proceeds with the macromolecule functional groups placed on their surface.

40-47

Authors: Nasrin Sohrabi, Hamid Reza Zare, Sahar Shir Ali Nasab

In this paper, the electrochemical behavior of [H5PMo10V2O40] modified electrode glassy carbon electrode ([H5PMo10V2O40]/GCE) and its interaction with calf thymus DNA (ctDNA) were investigated using voltammetry. Modified electrode showed two pair of peaks at A1 (0.00) and A2 (0.179) during the anodic peaks sweep, while the counterpart to the two cathodic peaks are C1 (-0.014) and C2 (0.142) respectively in cyclic voltammetry. The redox property of this modified electrode at various solution pH values and various scan rates were studied using cyclic voltammetry. The linear plot of peak potential EP versus pH was obtained with corresponding slopes 52 m V/ pH. The apparent charge transfer rate constant, ks, and transfer coefficient, α, for electron transfer between [H5PMo10V2O40] and GCE were calculated as 25.203 ± 3.586 and 0.514 (in pH=3), respectively. Binding constant (K = 4.65 X 104 M-1) and binding site size (s =0.5) of modified electrode by ctDNA were obtained by nonlinear fit analysis of voltammetric data based on an electrochemical equation, which was derived to examine the interaction of DNA and reversibly electroactive compounds.

58-60

Authors: Robson Fernandes de Farias

In the present work, a quantum chemical study (Semi-empirical,PM6 method) is performed using nitrogen mustards (HN1, HN2 and HN3) as subjects in order to demonstrate that there is a close relationship between pharmacological activity and parameters such as formation enthalpy and number of conformers, which could, consequently, be employed as reliable QSAR descriptors. To the studied nitrogen mustards, a very simple equation relating log P, ΔHof and the number of conformers (Nc) was found: log P = [(log -ΔHof + logNc)/2]-0.28.

68-72

Authors: Umar M Sani

The use of herbal remedies, including corn silk, classified as Stigma Maydis or Zea mays, are popular as an alternative to standard Western allopathic medicine for a variety of problems, including prostate disorders, a diuretic as well as for bedwetting and obesity. In the present study the antidiabetic potential of methanol extract of cooked, dried and pulverized Stigma Maydis was assessed in alloxan-induced diabetic albino mice. Hyperglycemia was induced by the injection of 150 mg/kg (i.p.) of alloxan monohydrate freshly dissolved in physiological saline. Doses (250, 500 and 750 mg/kg) per os, of the extract were separately administered to three groups of five diabetic mice each in the study. The activity was compared with reference standard glibenclamide (2 mg/kg, p.o.) and negative control of physiological saline. Treatment of the alloxan-induced diabetic mice with the methanol extract of Stigma Maydis decreased the raised blood glucose levels in a dose-dependent manner. The methanol extract exhibited relatively significant (P<0.05) anti-diabetic effect after 72 h and 96 h of treatment with the doses of 500 and 750 mg/kg body weight, respectively. Results of phytochemical screening of the methanol extract of cooked Stigma Maydis have indicated the presence of cardiac glycoside, steroids, terpenoids, alkaloids, flavonoids, carbohydrates and anthraquinones.

78-90

Authors: Tanu Dadhich, Manish Kumar, Kamla Pathak

The purpose of the study was to develop a capsulated delivery system of surface solid dispersion (SSD) of loperamide (LOP) for intestinal delivery that has potential for enhanced drug release. For the preparation of SSDs, crospovidone, croscarmellose sodium and avicel PH 101 were screened for swelling capacity and in vitro drug adsorption. SSDs were prepared by solvent evaporation method and the SSD prepared with crospovidone (drug to carrier ratio of 1:3) showed highest in vitro dissolution of 82.50% in 60 min. The optimized SSD3 was evaluated for micromeritic properties and characterized by XRD, DSC, SEM and FTIR. SSD3 was filled in Eudragit S 100 coated capsules SSD3 showed promising site specific drug delivery with release of 76.25% in 6 h. The developed dosage form has potential to protect loperamide from being released in the upper part of the GI system and thereby target to intestine.

98-109

Authors: Said Al-Alawi, Said Al-Habsi, Fahad Al-Buasidi, Khalifa Al-Muqbali, Mohammed Hussiani Mohammed Al-Falahi, Alka Ahuja

In order to ensure the optimum therapeutic effect of drug it is necessary to prepare the proper dosage form. Solubility is a significant physicochemical factor affecting absorption of drug and its therapeutic effectiveness. Poorly water soluble compounds have both solubility and dissolution related problems which can dramatically affect their bioavailability resulting in reduction of their therapeutic efficacy. To overcome such a problem solid dispersions of poorly soluble drugs like Cefixime, Valsartan and Ibuprofen were prepared and evaluated. Suitable carriers such as PVP K30 and HMPC etc. in different ratios were chosen. They were prepared by physical mixing and kneading method. The standard curves were prepared for cefixime, ibuprofen and valsartan in methanol. The release studies were carried out and compared. The results showed a marked increase in release of the drug from solid dispersions compared to the drug in its pure form. The percentage of the drug released for Ibuprofen increased from 12.78 to 52.4% (1:1 ratio), 70.2% (1:2 ratio) and 68.2% (1:3 ratio). The use of cefixime with hydroxypropymethylcellulose (HPMC) greatly improved the solubility of the drug and enhanced its dissolution rate. The percentage of the drug released increased from 13.2 to 31.4% (1:1 ratio), 34.9% (1:2 ratio) and 43.9% (1:3 ratio). The ratios which showed the best release were considered as the optimized formulations.

119-124

Authors: Suman Malik, Bharti Jain, Amar Sohail Mirza, Archana Singh

Schiff bases are the compounds which are mainly formed by the condensation of the aldehydes and amines. Benzothiazole is a privileged heterocyclic scaffold having a benzene ring fused with a five membered thiazole ring. A few Substituted 1, 3-benzothiazole derivatives are an important class of heterocyclic compounds. In recent years heterocyclic compounds analogues and derivatives have attracted strong interest due to their biological and pharmacological properties. Benzothiazole moiety is very small but it posses different biological activities. Not only benzothiazole but its different substituted derivatives also give different biological activities. Researches carried out on benzothiazole moiety had established promising antimicrobial activities like antimalarial, antifungal, anti tubercular, antiviral as well as antitumor, analgesic and anti-inflammatory activities.

134-143

Authors: OD Omodamiro, MA Jimoh

Persea americana commonly known as avocado is classified in the flowering plant family ‘Lauraceae’. It is a medicinal plant that serves as both a preventive measure and a cure to several diseases. Ethanol seed extract of Persea americana was studied for in-vitro antioxidant activity and diuretic effect. Different models such as DPPH radical scavenging activity, Nitric oxide scavenging activity and Anti-lipid peroxidation activity were used to determine antioxidant activity. Acute toxicity testing was performed to determine therapeutic dose of the extract using the Litchfeild and Wilcoxon (1949) method using swiss albino mice weighing between 20-25 g. Healthy adult wistar albino rats of both sex weighing 120-180g was used to determine diuretic effect of the ethanol seed extract, volume of urine output was determined using the rat metabolic cages, Na+, K+, Cl- and HCO3- were determined using flame photometric method. Comparisons were made between the control and the different concentration of the extract which includes 500 mg/ml, 250 mg/ml, 125 mg/ml, 62.50 mg/ml, 31.25 mg/ml and they were represented using a one way analysis of variance (ANOVA). The results were expressed as mean± standard deviation using bar charts at P< 0.05 level of significance. Results revealed that ethanol seed extract of Persea americana exhibited its antioxidant activity in a concentration dependent manner, it scavenged DPPH radical by 87.55± 0.63, Nitric oxide radical by 91.44± 0.15, and lipid peroxidation by 75.51± 0.014 all at the dosage of 500mg/ml which is the maximum concentration. Volume of urine and electrolyte Na+, Cl- and K+ was increased significantly when compared to the normal control, HCO3- did not show any significant increase. The results clearly indicate that ethanol seed extract of Persea americana exhibit diuresis and has potential to scavenge free radicals.

150-156

Authors: S K Khalil1*, J G Mexal, I H Khalil, S Wahab, A Rehman, Z Hussain, A Khan, A Z Khan, M K Khattak

Pecan [Carya illinoensis (Wangenh.) C. Koch] faces serious problem of alternate bearing producing large number of fruits of low quality in one year, followed by small number of fruits in next year with low total fruit production. As a consequence, the farmers get low income over years. Ethephon application in the form of foliar is considered as an alternative method for fruit thinning, however, limited published information is available on pecan. Effect of different levels of ethephon as source of ethylene on pecan fruit thinning, yield and quality was evaluated in this research. Foliar ethephon; 200, 400, 600 ppm, water spray and control (No spray) were sprayed on 27 year old pecan cultivar ‘Wichita’ at New Mexico State University, Las Cruces, USA. The ethephon was used as a source of ethylene. The increase in leaf defoliation, chlorosis, and kernel quality with decrease in total kernel weight were significant. However, total number of nuts at harvest remained the same. Foliar ethephon applied at 600 ppm performed better compared with other treatments. In conclusion, the ethephon at the rate of 600 ppm as foliar spray produced good quality by reducing number of nuts in the excessive fruit loading year, which had resulted in greater fruit set in the following year. This may increase profit of the pecan growers on a regular basis.

169-177

Authors: Shammy Sarwar, Muhammad Ashikur Rahman, Md. Sohel Rana

Terminalia belerica Roxb. has a long ethnomedicinal tradition of being used as a remedial agent in various diseases. The present study aimed to investigate antioxidant and cytotoxic activity of the methanolic extract of T. belerica fruits. Antioxidant potential of the extract was evaluated by using the 2, 2-diphenyl-1-picrylhydrazyl (DPPH) scavenging assay, nitric oxide scavenging assay, reducing power and total antioxidant capacity and the hydrogen peroxide (H2O2) scavenging assay. The extract showed significant activities in all antioxidant assays compared to ascorbic acid in a dose dependent mode. In the DPPH, the NO and the H2O2 scavenging assays, the extract of T. belerica displayed significant antioxidant activities with the IC50 values of 179.16, 96.553 and 134.29 µg/mL, respectively. In addition to strong reducing power, total antioxidant activity of the extract was also found to increase in a dose dependent manner. The extract also showed moderate cytotoxic activity in brine shrimp lethality bioassay and the LC50 value was found to be 7.612 µg/mL. The analgesic activity was evaluated using acetic acid-induced writhing test in mice. The extract, at a dose of 500 mg/kg, showed a maximum of 19.71 % inhibition (p < 0.05) of writhing reaction compared to the reference drug diclofenac-sodium (66.96 %).

186-191

Authors: EI Okoye, F Mbah

Three solvents extracts of flower and stalk of male Carica papaya were used to inhibit ten pathogenic bacteria. The ten bacteria investigated in this research were: Shigella Sonei, Streptococcus Pyrogenes, Escherichiacoli, Pseudomonas aeruginosa, Staphybcpccus aureus, Salmonella enteridis, Basilius cereus, Streptococcus faecalis, Neisseria gonorrhoeae, and Shigella dysenteriae. Three solvents were used in the extraction of active ingredientsin flower and stalk of male Carica papaya and they are distilled water, ethanol and n-hexane. Aqueous extract of flower and stalk of male Carica papaya could inhibit the ten test bacteria. These are: Fusarium verticilloids and Fusarium oxysporum. Ethanolic extract could not inhibit one out of ten test bacteria (Salmonella enteriditis). n-hexane extract could not inhibit three out of the ten test bacteria (S. Pyrogenes, S. enteriditis and N. gonorrhoeae). The minimum inhibitory concentrations (MIC) of ten bacteria investigated as mentioned above using three solvents were: aqueous extract, 0.05±0.01 mg/ml, 0.05±0.01 mg/ml, 0.05±0.01 mg/ml, 0.35±0.01 mg/ml, 0.05±0.01 mg/ml, 0.05±0.01 mg/ml, 0.05±0.01 mg/ml, 0.05±0.01 mg/ml, 0.05±0.01 mg/ml and 0.05±0.01 mg/ml respectively. The MIC for ethanolic extract were: 0.05±0.01 mg/ml, 0.25±0.01 mg/ml, 0.25±0.03 mg/ml, 0.05±0.01 mg/ml, 0.05±0.01 mg/ml, no inhibition, 0.05±0.01 mg/ml, 0.05±0.01 mg/ml, 0.05±0.01 mg/ml and 0.05±0.01 mg/ml respectively. The MIC for n-hexane extract are: 0.05±0.01 mg/ml, no inhibition, 0.05±0.01 mg/ml, 0.35 0.01, 0.05±0.01 mg/ml, no inhibition 0.05±0.01 mg/ml, 0.05±0.01 mg/ml no inhibition and 0.05±0.01 mg/ml respectively. The minimum bactericidal concentration (MBC) for ten test bacteria as mentioned above were: for aqueous extract 0.05±0.01 mg/ml, 0.30±0.01 mg/ml, 0.03±0.01 mg/ml, 0.15±0.01 mg/ml, 0.03±0.01 mg/ml, 0.03±0.01 mg/ml, 0.03±0.01 mg/ml, 0.05±0.01 mg/ml, 0.05±0.01 mg/ml, 0.03±0.01 mg/ml, and 0.03±0.01 mg/ml respectively. The MBC for ethanolic extract were: 0.05±0.01 mg/ml, 0.3±0.01 mg/ml, 0.02±0.01 mg/ml, 0.03±0.01 mg/ml, 0.05±0.01 mg/ml, no inhibition, 0.03±0.01 mg/ml, 0.02±0.01 mg/ml, 0.03±0.01 mg/ml and 0.02±0.01 mg/ml respectively. The MBC for n-hexane extract were: 0.05±0.01 mg/ml, no inhibition, 0.05±0.01 mg/ml, 0.02±0.01 mg/ml, 0.03±0.01 mg/ml no inhibition, no inhibition, 0.05±0.01 mg/ml, 0.05±0.01 mg/ml, no inhibition, and 0.03±0.01 respectively. Hence, crude solvent extracts of flower and stalk of male Carica papaya are antibiotic in nature.

202-207

Authors: Entesar O Al Tamimi*, Muna I Khalaf, Raghad A Abd Al-Jabar

The present work involves preparation of N-substituted phthalimide derivatives. The Performing of this research includes three steps: The first step of this work was includes preparation of potassium phthalimide. The second step involves preparation of N-alkyl phthalimide by reacting of phthalimide salte with (benzylchloride, PVC, adipoyl chloride, and Aryloyl chloride) respectively. The third step includes polymerization of unsaturated prepared compounds by using (BPO) as initiator with heating, and reaction of another mole of phthalimide salt with N-Adipoyl mono chloride phthalimide. All the prepared compounds in this work were characterized by recording their melting points, softening point, infrared (FT-IR) spectra, and 1H-NMR for some of them.

215-219

Authors: Ali Esmail Al-Snafi

In traditional Chinese and Japanese medicine, the seeds of the dodder (Cuscuta planiflora) are often harvested and ground into a fine powder, which was then made into tablets or encapsulated and taken to treat osteoporosis, osteoarthritis, general muscular pains. Dodder was employed in Ayurveda as a remedy for jaundice, as a mild laxative and a moderately potent analgesic. The preliminary phytochemical screening showed that Cuscuta planiflora contained polypenols, flavonoid, glycoside, alkaloids, carbohydrates, saponins, glycosides, phytosterols, triterpenoids and steroids. The previous pharmacological investigation showed that Cuscuta planiflora possessed antidepressant, anticonvulsant, antibacterial, cytotoxic and hepatoprotective effects. This review was designed to highlight the chemical constituents and pharmacological effects of Cuscuta planiflora.