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ISSUE 25

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               July - September 2015, Volume 10 No 25 pp 93-120

Table of Contents

About the Cover

A most important feature for the success of any planned reaction is the selection of a suitable solvent: solvents influence both chemical reactivity and reaction rates. The term “solvent polarity” lacks an exact definition, but it is generally used to encompass all of the intermolecular interactions of which the solvent is capable. Polar solvents have large dipole moments; they contain bonds between atoms with very different electronegativities, such as oxygen and hydrogen, polar reactants will dissolve in polar solvents and non-polar solvents dissolve non-polar compounds best. The present investigation was carried out to find out the antiplasmodial potential of crude seaweed extracts with three different polaritic solvents. Among the seaweed extracts tested, the crude extracts of Sargassum wightii and Valaniopsis pachynema exhibited excellent antiplasmodial activity of IC50 < 3.125 μg. ml-1 in all the three solvents (Petroleum ether, Ethyl acetate and ethyl alcohol) used at 48 h of incubation. This activity is highly comparable to the activity of positive control artemether (IC50 < 3.125 μg. ml-1). Statistical analysis reveals that, the significant in vitro antiplasmodial activity (P < 0.05) was observed between the concentration and time of exposure. The chemical injury to erythrocytes was done and its shows no morphological changes in erythrocytes by all the three solvent extracts. The results revealed that, the crude seaweed extract of S.wightii and V. pachynema collected from South West coast of India possess variable drug bioavailability for the development of antiplasmodial agents (Ref: Margret beula J, Sona Selva Malar S, Prasannakumar S, Ravikumar S, Kumaran R. Variable drug bio availability of native seaweeds in India for antimalarial therapeutics. Drug Discovery, 2015, 10(25), 93-99); (Image: http://preview.turbosquid.com).

ANALYSIS

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Variable drug bio availability of native seaweeds in India for antimalarial therapeutics

Margaret beula J, Sona Selva Malar S, Prasannakumar S, Ravikumar S, Kumaran R

A most important feature for the success of any planned reaction is the selection of a suitable solvent: solvents influence both chemical reactivity and reaction rates. The term “solvent polarity” lacks an exact definition, but it is generally used to encompass all of the intermolecular interactions of which the solvent is capable. Polar solvents have large dipole moments; they contain bonds between atoms with very different electronegativities, such as oxygen and hydrogen, polar reactants will dissolve in polar solvents and non-polar solvents dissolve non-polar compounds best. The present investigation was carried out to find out the antiplasmodial potential of crude seaweed extracts with three different polaritic solvents. Among the seaweed extracts tested, the crude extracts of Sargassum wightii and Valaniopsis pachynema exhibited excellent antiplasmodial activity of IC50 < 3.125 μg. ml-1 in all the three solvents (Petroleum ether, Ethyl acetate and ethyl alcohol) used at 48 h of incubation. This activity is highly comparable to the activity of positive control artemether (IC50 < 3.125 μg. ml-1). Statistical analysis reveals that, the significant in vitro antiplasmodial activity (P < 0.05) was observed between the concentration and time of exposure. The chemical injury to erythrocytes was done and its shows no morphological changes in erythrocytes by all the three solvent extracts. The results revealed that, the crude seaweed extract of S.wightii and V. pachynema collected from South West coast of India possess variable drug bioavailability for the development of antiplasmodial agents.

Drug Discovery, 2015, 10(25), 93-99

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OPINION

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Calcium Supplementation: Cardiovascular Cure or Curse?

Shashi K Agarwal

Calcium supplements are taken by more than half of middle aged or older US women. Although better bone health is the purported reason, data supporting this association is only marginal. Several epidemiological studies have observed cardiovascular event protection with a high intake of milk and/or dairy products - main sources of dietary calcium. Recent clinical studies however suggest a detrimental effect on the cardiovascular system with their use. This article looks at evidence based data on the use of calcium supplements and their relationship to cardiovascular events.

Drug Discovery, 2015, 10(25), 100-102

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RESEARCH

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Mucosal wound healing and anti peptic ulcer effect of Gongronema latifolium in rats

Azikiwe CCA, Aroh GN, Enye JC, Amazu LU, Ifezulike CC

Background: The freshly leaves and stem of Gongronema latifolium is eaten as vegetables in most part of tropical Africa and used in treatment of peptic ulcer disease in folklore medicine. Objectives: The air dried methanolic leave extract was investigated for anti-peptic ulcer and mucosal wound healing effect on indomethacin-induced gastric and duodenal ulcers in rats in order to demonstrate the pharmacological activity of the plants and justify its use in healing. Method: Fresh green leaves and stems of Gongronema latifolium were harvested, air dried, macerated in methanol and evaporated to dryness using rotary evaporator. Phytochemistry was carried out on the crude extract. Acute toxicity study was carried out in mice to determine the LD50 and guide dosing. Forty five rats of average weight of 150grams were divided into nine metal cages (A-I) of five rats per group. All animals were acclimatised for a week and fasted for 24hours prior to commencement of experiment. Group A was used as pilot study to demonstrate the effect of indomethacin and received orally 30mg/kg of indomethacin. The animals were sacrificed after 24hours and gastric and duodenal mucosal bleeding spots were used as positive indicator of ulcer induction. The stomach and duodenum were sent for histology. Group A was later taken as positive control. Group B was given orally, 2ml/kg of drinking water only to act as negative control. Groups C and D were treated like A but, were sacrificed at 2 or 4wks to act as 2 and 4wks positive control respectively. Groups E to I were given orally, 30mg/kg of indomethacin and after 24hours were treated with either Gongronema latifolium or cimetidine. Two dosage regimens were used for the methanolic extract while treatment period lasted for 2 or 4wks before the animals were sacrificed. Their stomach and duodenum were weighed and examined for bleeding spots before being sent for histological study. Data were presented as mean±Standard deviation of organ weight and number of bleeding spots while comparative histological architecture was presented as micrograph. Statistical analysis was done with SPSS version 16.0 using one-way ANOVA and students t-test for comparative statistics. P≥0.05 was adjudged non significant. Results: Phytochemistry showed the richly presence of alkaloids and flavonoids in line with earlier findings. The LD50 was 1,581mg/kg(IP) in mice using Lorke’s 1983 method. All non treated (Groups C and D) animals died within three to four days of commencement of the experiment. There was no significant (P˃0.25) change in incised organ weight of treated animals compared to negative control animals. There were multiple bleeding spots on the gastric and duodenal mucosa of the positive (group A) control. The histology also exhibited multiple gastric and duodenal damages. These bleeding spots and mucosal damages were also demonstrated in animals that were given 2wks treatment with Gongronema latifolium but, to a much lesser extent. The results obtained with cimetidine were similar to those of 2wks high dose treatment with Gongronema latifolium. At 4wks treatment duration with both dosage regimens of Gongronema latifolium, no bleeding spot was demonstrated and the mucosal wound had healed as compared with the negative control. Conclusion: Gongronema latifolium possesses demonstrable anti-peptic ulcer and mucosal healing/repairing effects. These effects were greater than that of cimetidine, a standard anti-peptic ulcer agent. The study may justify the use of Gongronema latifolium in treatment of peptic ulcer disease by traditional medicine healers. Clinical trial in human is recommended.

Drug Discovery, 2015, 10(25), 103-112

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The potential organo-toxicity safety of Morpholine and Crinum jagus in rats

Azikiwe CCA, Amazu LU

Background: Crinum jagus is a medicinal plant used by traditional medicine healers and has active components as morpholine, hamayne and lycoline. Anticonvulsant and other activities of the plant exist in literature. Our previous work showed reno and hepatotoxicity. Aim: To carry out a comparative chronic toxicity study of Crinum jagus bulbs and pure morpholine in rats in order to demonstrate their organo-toxicity or safety at therapeutic doses. Methods: Animals consisted of 50 young rats of average starting-weight of 80.6grams and about 60 adult mice of average weight of 20.6grams. Crinum jagus was collected from Igbodo, Delta State of Nigeria while morpholine was got from Anuihe Herman- CHINA. The bulbs of Crinum jagus were air dried for about ten days when a constant weight was achieved, chopped and ground. 200grams each of the white paste was macerated in 2 litres each of water, ethanol and petroleum ether. The filtrates were evaporated to dryness pooled into one solid mass and further fractionated in 100ml each of petroleum ether, ethyl acetate and n-butanol. The filtrated-fractions were evaporated to semi-solid state and then pooled together before finally dried to a solid state. Acute toxicity study was carried on the fractionated extract and morpholine using Lorke’s and Karber’s methods respectively. High and low doses of both morpholine and fractionated extracts were chosen as one fifth and one tenth of their LD50 respectively (effective doses).Young albino rats of average weight of 80.6grams were divided into 5 groups (A-E) of seven females and three males per cage. 111.8mg/kg and 223.6mg/kg of fractionated extracts and 0.221mg/kg and 0.442mg/kg of morpholine were orally administered to the rats once daily for a total period of 13weeks. The last group was given 2ml of injection water to act as negative control. At the end of 13th week and beginning of the 14th week, the animals under anaesthesia were bled from the orbital sinus for hormonal assay test while the testes, ovaries, brain and hearts were excised, weighed, preserved in formalin then sent for histological study. Results: LD50 of fractionated extracts of Crinum jagus was got as 1,118.03mg/kg IP in mice while that of Morpholine was 2.22mg/kg IP in mice. The reproductive hormones of all animals treated with the two separate doses of fractionated extracts or morpholine were within reference ranges and compared with negative controls. The histology of the testes, ovaries, brains and hearts were essentially normal and compared with negative control. Conclusion: Chronic toxicity study affords us the opportunity to demonstrate the adverse effects of standard, prospective or new drugs. Morpholine and Crinum jagus bulbs extracts at therapeutic doses are non toxicity to the reproductive organs, brain and heart of adult rats.

Drug Discovery, 2015, 10(25), 113-120

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