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Asian Pacific Journal of Tropical Medicine 2009年第3期2卷 7-14页

作者： Festus BC okoye patience o.osadebe Department of Pharmaceutical and Medicinal Chemistry Faculty of Pharmaceutical SciencesUniversity of NigeriaNsukka410001Enugu StateNigeria

objective:Alchornea floribunda leaves are widely used in ethnomedicinal management of inflammatory disorders. The present work is aimed at investigating this folkloric ***:The anti-inflammatory effect of the leaf extracts and fractions was investigated in experimental animal models of acute and chronic inflammation. The possible mechanisms by which the two most active fractions,hexane(HE) and ethyl acetate(EF) exert their effects were also ***:The crude extract(200 mg/kg) showed moderate inhibition of egg albumen-induced edema in rats(%edema inhibition = 54.69) at 4 *** and EF showed very high activity(%edema inhibition of 81.25 and 67.19 respectively at 200 mg/kg) at 4h as compared to the control. Both fractions ameliorated arthritis induced by formaldehyde in *** 400 mg/kg,HE evofeed a significant irritation of gastric mucosa in ***(200 mg/kg,p.o.) significantly inhibited leucocytes(%inhibition = 36.79) migration in vivo,but could not stabilize heat and hypotonicity-indueed lysis of human erythrocyte at 200 and 400μg/mL in *** investigation revealed the presence of terpenoids and steroids in HE and flavonoids,tannins and saponins in ***:These results suggest that the leaves of Alchornea floribunda possess anti-inflammatory activity in acute and chronic *** activity may derive from a combination of inhibition of prostaglandin synthesis and leucocytes *** phytochemical constituents detected in HE and EF may account for the anti-inflammatory activity.

关键词： Alchornea floribunda Anti-inflammatory Arthritis Leucocytes migration Membrane stabilization Plant extracts

Antimotility effects of extracts and fractions of Eastern Nigeria mistletoe(Loranthus micranthus Linn)

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Asian Pacific Journal of Tropical Medicine 2012年第7期5卷 556-560页

作者： patience o osadebe Chika C Abba Matthias o Agbo Department of Pharmaceutical and Medicinal Chemistry University of NigeriaNsukkaEnugu StateNigeria

objective:To evaluate the antimotility activity of Eastern Nigerian mistletoe[Loranthus micranthus（***） Linn]parasitic on six different host trees *** nitida,Persia americana,Kola accuminata,Irvingia gabonensis,Citrus simensis and Pentacletra macrophylla （***）.Methods:The antimotility of the methanol extracts and solvent fractions were evaluated in castor oil induced diarrheoa in ***:The methanol extracts（200 mg/kg, i.p.） inhibited defeacation significantly（P on（75.73%to 93.33%） more than that of atropine sulphate（2 mg/kg,i.p.） which inhibited defeacation by 80.0%.The methanol extract（200 mg/kg,i.p.） of L micranthus parasitic on *** exhibited significant（Pon in gastrointestinal transit（67.6%） more than that of atropine sulphate（2 mg/kg,Lp.） which inhibited gastrointestinal transit by 26.4%.The solvent fractions of L micranthus parasitic on *** at dose levels of 150 mg/kg inhibited significantly the gastrointestinal transit of *** F5 exhibited inhibitory activity which was comparable to loperamide（73.3%）. Conclusions:The methanol extract of L micranthus parasitic on *** exhibits higher antimotility activity that other *** solvent fractions could serve as source of novel antimotility agents.

关键词： Loranthus micranthus Fractination Gastrointestinal transit Atropine

Phytochemical analysis,hepatoprotective and antioxidant activity of Alchornea cordifolia methanol leaf extract on carbon tetrachloride-induced hepatic damage in rats

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Asian Pacific Journal of Tropical Medicine 2012年第4期5卷 289-293页

作者： patience o osadebe Festus BC okoye Philip F Uzor Nneka R Nnamani Ijeoma E Adiele Nkemakonam C obiano Department of Pharmaceutical and Medicinal Chemistry Faculty of Pharmaceutical SciencesUniversity of NigeriaNsukka41001Enugu StateNigeria

objective:To investigate the hepatoprotective and antioxidant activities of Alchornea cordifolia (***) leaf ***:Various solvent fractions of the methanol extract of the leaf of the *** ***(Fam:Euphorbiaceae) were evaluated for hepatoprotective activity by carbon tetrachloride-induced liver damage in *** degree of protection was measured by using biochemical parameters such as serum glutamate oxalate transaminase(SGoT/ AST),serum glutamate pyruvate transaminase(SCPT/ALT),alkaline phosphatase(ALP) and total *** in vitro antioxidant activity of the extract was also evaluated by the I,I-diphenyl 2-picrylhydrazyl(DPPH) free radical scavenging *** extract was subjected to preliminary phytoehemical ***:The ethyl acetate and chloroform fractions,at a dose of 300 mg/kg,produced significant(Poprolection by decreasing the activities of the serum enzymes and bilirubin while there were marked scavenging of the DPPH free radicals by the *** effects were comparable to those of the standard drugs used for the respective experiments,silymarin and ascorbic ***,flavonoids,saponins and tannins were delected in the phylochemical ***:From this study,it was concluded that the plant of *** possesses hepatoprotective as well as antioxidant activities and these activities reside mainly in the ethyl acetate and acetone fractions of methanol leaf extract.

关键词： Alchornea cordifolia Antioxidant Carbon tetrachloride DPPH model Hepatoprolective Phytochemical analysis

Aqueous Solubility Enhancement of Mirtazapine: Effect of Cosolvent and Surfactant

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Pharmacology & Pharmacy 2015年第10期6卷 471-476页

作者： Kenneth E. Ezealisiji Chika J. Mbah patience o. osadebe Department of Pharmaceutical Chemistry Faculty of Pharmaceutical Sciences University of Port Harcourt Port Harcourt Nigeria Department of Pharmaceutical and Medicinal Chemistry Faculty of Pharmaceutical Sciences University of Nigeria Nsukka Nigeria

The poor aqueous solubility of drugs is a challenging problem faced by pharmaceutical scientists in drug formulation. Cosolvency and micellization techniques have been severally used to enhance the solubility of poorly aqueous soluble drugs. Mirtazapine, a tetracyclic antidepressant used for the treatment of moderate to severe depression and anxiety, has very poor aqueous solubility. The objective of the study was to investigate the effect of solubilizing agents (cosolvents and surfactants) on the aqueous solubility of mirtazapine while envisaging that any significant improvement in its aqueous solubility could contribute towards alleviating the withdrawal symptoms often associated with the drug. The solubility of mirtazapine was determined at room temperature in aqueous mixtures of cosolvents (propylene glycol and polyethylene glycol 400) and surfactants (polysorbate 20, polysorbate 80 and sodium lauryl sulfate). An exponential increase in mirtazapine solubility was observed when total drug solubility in water-cosolvent system was plotted against cosolvent fraction volume. Polyethylene glycol 400 gave larger solubilization capacity (σ) when compared to propylene glycol. With the surfactants, linear relationship between the total solubility of the drug in water-surfactant mixtures and surfactant concentration was noted. Sodium lauryl sulfate showed the largest solubilization power (k) when compared to the nonionic surfactants (polysorbate 20 and polysorbate 80 respectively). A linear relationship between standard free energy and partition coefficient was also observed. The result of the study shows that aqueous solubility of mirtazapine is significantly improved by cosolvency and micellization and therefore there exists the possibility of improving the withdrawal symptoms often experienced with the drug. It also suggests that large free energy is required for drugs with high partition coefficients to permeate the biological membrane.

关键词： Mirtazapine Cosolvency Micellization Aqueous Solubility

Immunomodulatory activity of a lupane triterpenoid ester isolated from the eastern Nigeria mistletoe,Loranthus micranthus(Linn)

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Asian Pacific Journal of Tropical Medicine 2011年第7期4卷 514-522页

作者： omeje Edwin ogechukwu osadebe patience ogoamaka Nworu Chukwuemeka Sylvester Akira Kawamura Peter Proksch Department of Pharmaceutical and Medicinal Chemistry Faculty of Pharmaceutical SciencesUniversity of Nigeria410001NsukkaNigeria Department of Pharmacology and Toxicology Faculty of Pharmaceutical SciencesUniversity of Nigeria410001NsukkaNigeria Department of Chemistry Hunter College of CUNYThe City University of New YorkU.S.A Department of Pharmaceutical Biology Heinrich-Hein UniversityDusseldorfGermany

objective:To provide further evidence for the ethnomedicinal use of the Eastern Nigeria mistletoe,Loranthus micranthus(***),as an ***:Solvent fractions from the crude extract of the mistletoe plant was obtained and screened by the cell mediated delayed type hypersensitivity reaction(DTHR) model in *** the immunomodulatory potentials of a major lupane triterpenoid ester isolated from an active hexane fraction of the Eastern Nigeria mistletoe was *** lupeol-based triterpenoid esters: 7β15α-dihydroxyl-lup-20(29)-ene-3β-palmitate(Ⅰ),7β,15α-dihydroxyl-lup-20(29)- ene-3β-stearate(Ⅱ) and 7β,15α-dihydroxyl-lup-20(29)-ene-3β-decadecanoate(Ⅲ) were isolated from the plant leaves epiphyting on a local kola nut tree and were characterized. Compound 1 was subjected to cell proliferation studies using C57H1/6 splenocvtes at three dose levels(5.25 and 100μg/mL) in presence of ***,the effect of this compound on IL-8 receptor expression was evaluated at three doses(1,5 and 10μg/mL) using the real time polymerase chain reaction ***:This triterpenoid ester produced some enhancement of the splenocytes at the tested doses but at doses higher than 5μg/mL caused inhibition of the IL-8 receptor ***:The present findings support the ethnomedicinal use of the Eastern Nigeria Mistletoe in the management of diseases affecting the immune *** trilerpenoid(s) have some immunomodulatory abilities on splenocytes and IL-8 receptors and may partly account lor the overall immunomodulatory activity of this plant.

关键词： Lupane triterpenoid Loranthus micranthus Eastern Nigeria mistletoe Interleukin-8 Cell proliferation Anti-inflammatory

Seasonal variation for the antidiabetic activity of Loranthus micranthus methanol extract

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Asian Pacific Journal of Tropical Medicine 2010年第3期3卷 196-199页

作者： patience ogoamaka osadebe Edwin ogechukwu omeje Philip Felix Uzor Ernest Kenechukwu David Damian Chiedozie obiorah Department of Pharmaceutical and Medicinal Chemistry Faculty of Pharmaceutical SciencesUniversity of Nigeria

objective:To determine the season in which the Eastern Nigeria mistletoe,Loranthus micranthus,parasitic on Persea americana possesses optimum antidiabetic activity and to determine the seasonal variation in the ***:The antidiabetic activities of the aqueous methanol extracts of the leaves of Eastern Nigeria mistletoe,Loranthus micranthus, harvested in two seasons of the year,the onset of rainy season(April) and the peak of rainy season(July) were *** tests were carried out on six(6) groups(A-F) of alloxaninduced diabetic *** A and B received 200 mg/kg and 400 mg/kg of the April sample extracts respectively while groups C and D received same doses of the July sample extracts. Group E and F which were the positive and negative controls received 10 mg/kg of glibenclamide and 2 ml/kg of 3%tween 20 *** blood glucose levels of the animals were monitored hourly with a glucometer for six *** phytochemical analysis of the plant extracts were also carried out by standard ***:The results showed that group A and B exhibited significant(Pon in the fasting blood sugar(FBS) level of the animals(38.9%and 39.2%respectively) with maximum reduction observed at the 5th and 6th hour respectively compared to glibenclamide(71.3%).Group C showed no significant (P>0.05) FBS reduction(15.9%) while group D exhibited highly significant(Pon (47.5%) with the maximum reduction occurring after 6 *** phytochemical analysis of the crude methanol extracts revealed the presence of carbohydrates,glycosides,saponins, tannins,flavonoids,steroids,terpenoids,acidic compounds,resins and *** were present in different proportions in both ***:This study shows that there is a seasonal, dose-dependent variation in the chemical composition viz-a-viz the antidiabetic activity of the plant under *** activity is highest at the peak of the rainy season.

关键词： Antidiabetic activity Loranthus micranthus Methanol extract Phytochemical analysis Seasonal variation

Antidiabetic principles of Loranthus micranthus *** on Persea americana

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Asian Pacific Journal of Tropical Medicine 2010年第8期3卷 619-623页

作者： patience ogoamaka osadebe Edwin ogechukwu omeje Sylvester Chukwuemeka Nworu Charles okechukwu Esimone Philip Felix Uzor Ernest kenechukwu David John Uchechukwu Uzoma Department of Pharmaceutical and Medicinal Chemistry Faculty of Pharmaceutical Sciences University of NigeriaNsukka410001NsukkaEnugu StateNigeria Department of Pharmacology and Toxicology Faculty of Pharmaceutical SciencesUniversity of NigeriaNsukka.410001NsukkaEnugu StateNigeria Departrment of Pharmaceutics Faculty of Pharmaceutical SciencesUniversity of NigeriaNsukka410001NsukkaEnugu StateNigeria Department of Pharmaceutical and Medicinal Chemistry Faculty of Pharmaceutical SciencesUniversity of NigeriaNsukka410001NsukkaEnugu StateNigeria

objective:To explore antidiabetic principles of the Eastern Nigeria mistletoe,Loranlhus micranthus Linn,parasitic on Persea ***:The weakly acidic fraction of the aqueous methanol extract of the leaves of Loranlhus micranthus(Linn.) was isolated and tested for its antidiabetic *** isolation of the weakly acidic fraction was carried out following established physico-chemical based ***,alloxan-induced diabetic rats were treated intraperitoneally(ip) with 250 mg/kg and 400 mg/kg of the weakly acidic fraction, glibenclamide 10 mg/kg(positive control) and 2 mg/kg of 3%v/v tween 20(negative control).The sugar levels of the treated and untreated animals were determined by withdrawing the blood at regular intervals and testing them with an automated *** phytochemical analysis of the acidic fraction was carried out using standard *** techniques were employed in the subsequent isolation and purification of the constituents of the weakly acidic ***:It was shown that the maximum effect of the weakly acidic fraction was obtained at 24 hours after administration and was found to be statistically comparable with that of the positive *** phytochemical analysis revealed the presence of steroids,terpenoids, alkaloids,flavonoids,glycosides,carbohydrates,saponins,and acidic compounds in the crude extract and carbohydrates,*** and oil in the weakly acidic *** purification of the weakly acidic fraction of the methanol extract using thin layer chromatography shows that toluene:methanol:diethyl amine(3:1:1) and chloroform:methanol:diethyl amine (9:1:1) are the best solvent system for the isolation of the various components of the weakly acidic fraction of the crude methanol extract of Loranlhus ***:The present study has led to the conclusion that the weakly acidic fraction of the plant under study has the potent antidiabetic activity and that t

关键词： Antidiabetic isolation Loranthus micranthus Thin layer chromatography Weakly acidic fraction