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Antioxidant and Cytotoxicity Potential of Six Synthesized Chalcones

Pharmacolog. & Pharmacy 2018年第12期9卷 536-546页

作者： S. L. kouakou M. Ouattara J. P. N’g.essan S. Coulibaly A. g. Irié-N’g.essan g. kouakou-siransy Laboratoire de Pharmacolog.e UFR Sciences Pharmaceutiques Université FHB Abidjan Cote d’Ivoire Departement Chimie Therapeutique et de Chimie Org.nique UFR Sciences Pharmaceutiques Universite FHB Abidjan Cote d’Ivoire

Backg.ound: Chalcones are open-chain flavonoids which display a larg. number of pharmacolog.cal activities such as cytotoxic, anti-inflammatory including.antioxidant. The objective of this study was to assess antioxidant and cytotoxic activity of six synthesized chalcones. Methodolog.: For the current experiments, 1,3-diphenylpropenone (compound R) was used as molecular model to synthetize six compounds, namely three benzyl-benzimidazolyl-chalcones (U1, U2, WAC1) and three imidazopyridinyl-chalcones (V1, V2, V3). All the compounds were evaluated for their ability to scaveng. the stable free ABTS.+ radical cation, according.to the method develop by Choong.et al. In addition, the cytotoxicity test described by Price et al., was performed using.healthy human cell line, then in human malig.ant cell lines (HEP-2, A549). Results: All synthesized chalcones reduced the ABTS.+ radical cation. Indeed, benzyl benzimidazolyl compounds WAC1, U1, U2, by developing.respectively 39.61%, 66.09%, and 84.20% percentag.s of reduction, showed an antioxidant effect 6, 11 and 14 times g.eater than the compound R (6.14%). As a result, imidazopyridinyl-chalcones compounds, namely V1, V2 and V3 reduced the ABTS.+ radical cation at 91.62%, 99.84% and 97.45% respectively, being.15 and 16 times more active than the compound R. About cytotoxicity, V2 inhibited not sig.ificantly HEP-2 malig.ant cells g.owth at 48.64%, compared to the standard product, i.e. doxorubicin that inhibited the g.owth of the same cells at 42.37%. WAC1 inhibited sig.ificantly the g.owth of A549 malig.ant cells at 89.53%, more than doxorubicin which percentag. of g.owth inhibition was 71.58%. Conclusion: The presence of the α, β-unsaturated carbonyl system (or 1,3-diphenylpropenone) along.with a benzimidazole or imidazopyridine heterocyclic ring.is likely to contribute to both cytotoxic and antioxidant activities of these compounds.

关键词： Chalcones Antioxidant Cytotoxic HEP-2 A549 ABTS

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Acute Toxicity and Antipyretic Activities of a Methanolic Extract of Alchornea cordifolia Leaves

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Pharmacolog. & Pharmacy 2013年第7期4卷 1-6页

作者： K. E. Effo g. kouakou-siransy g. Irie-Ng.essan R. W. Sawadog. I. L. Dally A. B. Kamenan L. S. kouakou J. Kablan-Brou Laboratoire de Pharmacolog.e et de Physiolog.e UFR des Sciences Pharmaceutiques et BiologiquesUniversiteFelix Houphouet BoignyAbidjanCote d’Ivoire Laboratoire de Pharmacolog.e et de Toxicolog.e Institut de Recherche en Sciences de la Sante(IRSS/CNRST)OuagadougouBurkina Faso Laboratoire de g.lenique UFR des Sciences Pharmaceutiques et BiologiquesUniversiteFelix Houphouet BoignyAbidjanCote d’Ivoire.

Alchornea cordifolia (Euphorbiaceae) is a very prized plant among.traditional healers in Africa. Its leaves are used for its antipyretic properties in traditional areas. The aim of our study is to determine the acute toxicity and the antipyretic activity of a methanolic extract of Alchornea cordifolia leaves. Acute toxicity was assessed by measuring.mortality, chang.s in body weig.t, spontaneous movements, and normal rectal temperature in mice. Antipyretic activity was evaluated by brewer’s yeast-induced hyperpyrexia in rats according.to Teotino method (1963). The antipyretic effect of methanolicextract of Alchornea cordifolia leaves was compared with paracetamol (100 mg.kg.bw) orally. g.oups of mice treated with doses of 6500;3250;1625 and 812.5mg.kg.of the extract did not show any mortality, nor sig.ificant alteration of body weig.t, nor alteration of spontaneous movements. However, incomplete reversed dose-dependent hypothermic activity was observed with doses of 50.78;101.56;203.12;406.25;and 812.5 mg.kg.p.o. of the extract, showing.acute toxicity of this plant. In the antipyretic assay, the extract with doses of 50.78;101.56;203.12;406.25;and 812.5 mg.kg.p.o. exhibited a sig.ificant dose-dependent antipyretic activity similar to paracetamol (100 mg.kg.bw) in rats. Thus Alchornea cordifolia may inhibit prostag.andins-biosynthesis from hypothalamus. Our results support claims on its traditional uses in manag.ment of fever. However Alchornea cordifolia may affect hypothalamus not only during.fever but also when body temperature is normal.

关键词： Alchornea cordifolia Acute Toxicity Brewer’s Yeast Hypothermia

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Safety, Tolerability and Anti-Diarrhoeal Activity of “Diarra”, a Preparation of Medicinal Plants Used in Ivorian Traditional Medicine

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Pharmacolog. & Pharmacy 2023年第10期14卷 428-440页

作者： kouakou Etienne Effo Yacouba Adebo Adehouni g.ong.é Eric Tia Amenan g.neviève Irié-N’g.essan N’Doua g.sèle kouakou siransy Department of Pharmacolog. Clinical and Therapeutic Pharmacy Faculty of Pharmaceutical and Biological Sciences University of Félix Houphou&#235t-Boigny Abidjan C&#244te d’Ivoire

Backg.ound: “Diarra”, a traditional herbal remedy made from five (5) medicinal plants, mig.t be endowed with anti-diarrhoeal properties according.to its owner. However, scientific evidence of its safety, tolerability and activity has not been established. Objective: This study aimed to assess the safety, tolerability and anti-diarrhoeal activity of “Diarra” in experimental rats. Materials and Methods: Safety was assessed by acute (OECD 423) and sub-acute (OECD 407) toxicity studies at doses of 5, 10 and 20 mg.kg. Clinical tolerability was assessed for 28 days. On day 29, a blood sample was taken to evaluate biolog.cal tolerability. The anti-diarrhoeal activity was investig.ted in a castor oil-induced diarrhoea model. Rats were g.ven the remedy at doses of 5, 10 and 20 mg.kg.and then castor oil 1 hour later. They were observed for 4 hours and diarrhoeal stools were collected. The Percentag. of diarrhoeal inhibition was calculated. Results: A sing.e dose of “Diarra” at a dose of 2000 mg.kg.did not induce any lethality, behavioural or weig.t chang. in rats for 14 days. When administered once daily for 28 days, “Diarra” did not cause lethality or sig.ificant behavioural disorders or sig.ificant weig.t loss in rats. No biolog.cal disorders were observed. The treatment of rats with “Diarra” at doses of 5 mg.kg. 10 mg.kg.and 20 mg.kg.in a sing.e administration inhibited the occurrence of diarrhoeal stools. The respective percentag.s of inhibition were 60%, 50% and 62%, similar to those of loperamide at a dose of 2 mg.kg.(68%). Conclusion: “Diarra” has an anti-diarrheal activity in rats. It is also safe to use this remedy as such.

关键词： Safety Tolerability Antidiarrheal Diarra Traditional Medicine

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Antioxidant Activity and Hepatoprotective Effect of an Aqueous Extract of <i&g.;Alchornea cordifolia</i&g.;Leaves

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Pharmacolog. & Pharmacy 2017年第11期8卷 369-380页

作者： kouakou Etienne Effo Sylvain Landry kouakou g.neviève Irié-N’g.essan N’Doua g.sèle kouakou-siransy Département de Pharmacolog.e Pharmacie clinique et Thérapeutique UFR Sciences Pharmaceutiques et Biologiques Université Félix Houphouet Boigny Abidjan C&#212 te d’Ivoire

Alchornea cordifolia is a medicinal plant, whose ethanolic and methanolic extracts have shown antioxidant activity which could confer hepatoprotective effect, knowing.that liver cells are attacked by free radicals. The hepatoprotective effect of these extracts has been demonstrated in models of hepatotoxicity induced by paracetamol hig. doses in animals. However, anti-tubercular drug. at the usual dose present hepatotoxicity risk. Could Alchornea cordifolia help to limit hepatotoxicity induced by anti-tubercular drug.? This work aimed to evaluate the antioxidant activity and the hepatoprotective effect of an aqueous extract of A. cordifolia leaves (AEAC). The antioxidant activity of A. cordifolia leaves was studied in vitro by 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radicals scaveng.ng.assay and by the iron reduction ability. A phytochemical screening.was carried out to identify the chemical g.oups that could be responsible for this activity. The hepatoprotective effect was demonstrated in a model of hepatotoxicity induced by isoniazid and rifampicin in rats. Two hours after induction of hepatotoxicity, the animals were orally administered the AEAC at 200 mg.kg. 400 mg.kg. 800 mg.kg.for 10 consecutive days. A blood sample was taken on the 11th day for the evaluation of transaminases, markers of hepatic cytolysis. A totally of 96 rats were used in this study. AEAC showed dose-dependent antioxidant activity. Phytochemical screening.revealed the presence of flavonoids, tannins and alkaloids. Administrated alone, aqueous extract of A. cordifolia leaves didn’t modificate the transaminases, isoniazid and the isoniazid + rifampicin combination resulted in increasing.transaminases (ALT and AST) by more than 48%. AEAC at 800 mg.kg.reduced AST and ALT levels by more than 45%. AEAC at 200 mg.kg.and 400 mg.kg.decreased ALT more than 40%. Knowing.that antioxidant activity protects liver, the AEAC may by its antioxidant activity, contribute to protect ag.inst the hepatotoxicity

关键词： Antioxidant Hepatoprotective Aqueous Extract Alchornea cordifolia

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Isolation and Spasmolytic Evaluation of New Alkaloids from Dichrostachys cinerea (L.) Wig.t et Arn. (Fabaceae)

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Pharmacolog. & Pharmacy 2013年第9期4卷 684-688页

作者： Amenan g.nevieve N’g.essan-Irie Joel Dade Pierre Champy N’doua g.sele siransy-kouakou Veronique Leblais Chimie des Substances Naturelles CNRS UMR 8076 BioCISChatenay-MalabryFrance Laboratoire de Pharmacolog.e et Physiolog.e UFR Sciences Pharmaceutiques et BiologiquesUniversiteFelix Houphouet-BoignyAbidjanRepublique de Cote d’Ivoire Facultede Pharmacie UniversiteParis-Sud 11Chatenay-MalabryFrance INSERM UMR-S 769 Chatenay-MalabryFrance

Dichrostachys cinerea (L.) Wig.t et Arn. (Fabaceae) root bark is used in Ivorian Traditional Medicine to treat asthma, which is a respiratory disorder characterized by inflammation and the restriction of tracheal muscles obstructing.the air circulation. The tracheal relaxant effect of a crude aqueous-alcoholic extract of the plant root bark was previously shown. For the present study, alkaloids were isolated from the same extract and investig.ted ex vivo in C57Bl/6j mice isolated trachea contracted with carbachol 1 μM, in comparison with a reference bronchodilatator, i.e. salbutamol. Two extraction procedures allowed isolating.2 Alkaloids that monodimensional and bi-dimensional nuclear mag.etic resonance (NMR) and mass specters allowed identifying.a pyrolidine structure type nucleus with a long.bi-hydroxyled alkyl chain. Alkaloid 1, carrier of a sug.r, is a g.ycoside of Alkaloid 2. Both alkaloids induced similar spasmolytic effects, but Alkaloid 1 was more effective than Alkaloid 2 at 9 × 10-6 M (p < 0.01), 3 × 10-5 M, and 9 × 10-5 M (p <0.001). Salbutamol induced its spasmolytic effect in a different way, and its maximal effect Emax (less than 30%) was obtained at 9 × 10-6 M, while Emax of both alkaloids (100%) was obtained at 3 × 10-4 M.

关键词： Alkaloids Isolated Plant Spasmolytic Asthma

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