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See detailLes plantes tropicales, sources potentielles de médicaments antipaludiques 
Frederich, Michel ULiege

Scientific conference (2017, December 06)

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See detailConsommation des médicaments antipaludiques : Analyse des échantillons et caractéristiques des pharmacies en territoires périurbains de Kinshasa
Mavungu Landu, Don Jethro ULiege; Frederich, Michel ULiege; Hubert, Philippe ULiege et al

Conference (2017, November 23)

Contexte et objectif : Le paludisme causé par le Plasmodium falciparum demeure un problème majeur de santé publique. Le traitement avec des antipaludiques de bonne qualité est une composante importante ... [more ▼]

Contexte et objectif : Le paludisme causé par le Plasmodium falciparum demeure un problème majeur de santé publique. Le traitement avec des antipaludiques de bonne qualité est une composante importante dans le contrôle de cette maladie. Cependant en Afrique centrale, plus de 25% des médicaments serait contrefaits ou de qualité inférieure, situation qui serait encore plus dramatique dans les territoires périurbains. Afin de permettre une sensibilisation des populations vivant dans ces milieux, une étude a été menée dans le but d’évaluer l’existant au niveau sanitaire pharmaceutique. Méthode : Dans le contexte ci-mentionné, une étude préliminaire et prospective a été menée dans les territoires périurbains de la Ville de Kinshasa durant la période allant du 22 février au 10 décembre 2016. Les médicaments antipaludéens les plus consommés ont été identifiés à l’aide d’une enquête auprès de 1150 ménages et 88 pharmacies. Quinze échantillons de Quinine et trente échantillons de poudre pour suspension d’Artéméther et de Luméfantrine ont été collectés. L’analyse de la qualité de ces médicaments a été réalisée au moyen de méthodes séparatives génériques utilisant la technique de chromatographie liquide à haute performance couplé à un détecteur à barrettes de diodes. Une caractérisation a été également effectuée dans 150 établissements pharmaceutiques sur base des normes édictées par le Ministère de la Santé Publique congolais. Résultats : Les enquêtes auprès des ménages et des pharmacies révèlent de manière concordante que le médicament antipaludéen le plus consommé était la quinine, suivie de la combinaison artémether-luméfantrine. Le résultat des analyses des échantillons d’antimalariques (ou antipaludéens) montre qu’un échantillon de Quinine sur trois (33,3%) et trois poudres pour suspension d’Artéméther et de Luméfantrine sur cinq (60%) ne contenaient pas la concentration prévue en Artéméther et/ou en Luméfantrine. Par ailleurs, le résultat des observations évoque qu’aucun établissement pharmaceutique ne respectait l’ensemble des normes du Ministère de la Santé Publique. Conclusion : Cette étude nous apprend qu’en territoires périurbains de Kinshasa, la Quinine est l’antipaludéen le plus consommé, suivie de la combinaison Artéméther-Luméfantrine. Un échantillon sur trois (33,3%) de Quinine et trois échantillons sur cinq (60%) de la combinaison Artéméther-Luméfantrine sont non conformes. Quant aux pharmacies existantes, aucune d’entre elles ne respecte l’ensemble des normes minimales édictées par le Ministère de la Santé Publique de la RDC. [less ▲]

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See detailL’ethnopharmacologie, à l’origine de nombreux médicaments
Frederich, Michel ULiege

Conference (2017, November 10)

L’ethnopharmacologie peut être définie comme « l’étude scientifique interdisciplinaire des matières d’origine végétale, animale ou minérale, et des savoirs et pratiques s’y rattachant, que les sociétés ... [more ▼]

L’ethnopharmacologie peut être définie comme « l’étude scientifique interdisciplinaire des matières d’origine végétale, animale ou minérale, et des savoirs et pratiques s’y rattachant, que les sociétés mettent en œuvre à des fins thérapeutiques, curatives, préventives ou diagnostiques ». De nombreux médicaments indispensables aujourd’hui sont issus de ces connaissances traditionnelles : on peut citer par exemple l’universelle Aspirine®, provenant du saule, ou la quinine, médicament du paludisme, issu du quinquina Sud-Américain. Aujourd’hui encore, selon l’OMS, 80% de la population mondiale a recourt, en première intention, aux plantes médicinales pour se soigner. Néanmoins, ces connaissances traditionnelles sont aujourd’hui menacées, que ce soit pour des raisons d’appauvrissement de la biodiversité, ou de déstructuration des sociétés et des connaissances traditionnelles. 1. Fleurentin, J. Traditions thérapeutiques et médecine de demain. 2011. Editions Ouest-France. [less ▲]

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See detailThe quality of artemether-lumefantrine combination and characteristics of pharmacies in the periurban areas of kinshasa
Mavungu Landu, Don Jethro ULiege; Liégeois, Sophie; Manzambi Kuwekita, Joseph ULiege et al

Conference (2017, October 18)

QUALITÉ DE LA COMBINAISON THERAPEUTIQUE ARTEMETHER-LUMEFANTRINE ET CARACTÉRISTIQUES DES PHARMACIES EN TERRITOIRES PÉRIURBAINS DE KINSHASA Mavungu Landu DJ.1,2, Liégeois S., Manzambi Kuwekita J.3,4, Mbinze ... [more ▼]

QUALITÉ DE LA COMBINAISON THERAPEUTIQUE ARTEMETHER-LUMEFANTRINE ET CARACTÉRISTIQUES DES PHARMACIES EN TERRITOIRES PÉRIURBAINS DE KINSHASA Mavungu Landu DJ.1,2, Liégeois S., Manzambi Kuwekita J.3,4, Mbinze J.5, Mavungu Nsiona J.6,Hubert P.1, Michel B.2,7, Gretry L.8, Minga Kwete M.9, Reginster J-Y.3, Frédérich M.1, Marini Djang'Eing'A R.1 1 Département de Pharmacie, Université de Liège, Liège, Belgique; 2 Ecole Régionale Postuniversitaire d’Aménagement et de Gestion intégrés des Forêts et Territoires tropicaux, Kinshasa, RDC; 3 Département des Sciences de la Santé Publique, Université de Liège, Liège, Belgique; 4 Section de Santé Communautaire, Institut Supérieur des Techniques Médicales de Kinshasa, Kinshasa, RDC; 5 Département de Galénique et d’Analyse des Médicaments, Université de Kinshasa, Kinshasa, RDC; 6 Division Provinciale de la Santé, Kinshasa, RDC; 7 Faculté Universitaire des Sciences Agronomiques de Gembloux, Université de Liège, Gembloux, Belgique; 8 Plateforme Afrique Centrale, PACODEL, Kinshasa, RDC; 9 Secure drug, Kinshasa, RDC. Introduction: Le paludisme causé par le Plasmodium falciparum demeure un problème majeur de santé publique. Le traitement avec des antipaludiques de bonne qualité est une composante importante dans le contrôle de cette maladie. Cependant en Afrique centrale, plus de 25% des médicaments serait contrefaits ou de qualité inférieure, situation qui serait encore plus dramatique dans les territoires périurbains. Objectif: Afin de permettre une sensibilisation des populations vivant dans ces milieux, une étude a été menée dans le but d’évaluer l’existant au niveau sanitaire pharmaceutique. Méthodes: Dans le contexte ci-mentionné, une étude préliminaire et prospective a été menée dans la zone de santé de Mont Ngafula 1 située dans les territoires périurbains de la Ville de Kinshasa durant la période allant du 22 février au 10 décembre 2016. Trente échantillons de poudre pour suspension d’artéméther et de luméfantrine ont été collectés. L’analyse de la qualité de ces médicaments a été réalisée au moyen de méthodes séparatives génériques utilisant la technique de chromatographie liquide à haute performance couplé à un détecteur à barrettes de diodes. Une caractérisation a été également effectuée dans 127 établissements pharmaceutiques sur base des normes édictées par le Ministère de la Santé Publique congolais. Résultats: Le résultat des analyses des échantillons d’antimalariques (ou antipaludéens) montre qu’une poudre pour suspension d’artéméther et de luméfantrine sur trois (33,3%) ne contenait pas la concentration prévue en artéméther et/ou en luméfantrine. Par ailleurs, le résultat des observations évoque qu’aucun établissement pharmaceutique ne respectait l’ensemble des normes du Ministère de la Santé Publique. Conclusion: Cette étude nous apprend qu’en territoires périurbains de Kinshasa, un échantillon sur trois (33,3%) de la combinaison Artéméther-Luméfantrine est non conforme, les suspensions sont sous-dosées. Quant aux pharmacies existantes, aucune d’entre elles ne respecte l’ensemble des normes minimales édictées par le Ministère de la Santé Publique de la RDC. [less ▲]

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See detailDrepakis : Contribution to the management of Sickle cell disease in the city of Kisangani (D.R. Congo)
Marini Djang'Eing'A, Roland ULiege; Batina Agasa, Salomon; Gulbis, Béatrice et al

Conference (2017, October 06)

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See detailInvestigation of content of Panda oleosa (Pierre), a plant used in Kisangani areas for its antihyperglycemic activity
Katemo Muhoya, Frédéric; Kadima Ntokamunda, Justin; Njakarinala Ranarivelo et al

Conference (2017, October 05)

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See detailPreliminary Phytochemical Content and Antidiabetic Potential Investigations of Panda oleosa (Pierre) Used in Kisangani Areas
Katemo Muhoya, Frédéric; Kadima Ntokamunda, Justin; Njakarinala Ranarivelo et al

in American Journal of Analytical Chemistry (2017), 8

Panda oleosa Pierre (POP), a tropical plant tree, has been used in traditional medicine in Kisangani city and around to treat various diseases including diabètes and HIV/AIDs. This study aims to evaluate ... [more ▼]

Panda oleosa Pierre (POP), a tropical plant tree, has been used in traditional medicine in Kisangani city and around to treat various diseases including diabètes and HIV/AIDs. This study aims to evaluate the chemical composition of POP extracts while setting up chromatographic fingerprints for their quality control, and the anti-hyperglycemic potential of trunk bark aqueous extracts of POP. Common chemical reactions were used for identification of main secondary metabolic groups. Thin layer chromatography was used to set up several chromatographic fingerprints of water and alcoholic extracts while evaluating chemical composition. Oral glucose tolerance test served to induce hyperglycemia in a rabbit model. The extracts were given as 25 mg/kg, 50 mg/kg, and 100 mg/kg body weight, 30 minutes before loading animals with glucose 4 g/kg. Blood samples were collected at various times: just before extracts (T-30), before (T0) and after glucose load (T30, T60, T120, and T180). Blood glucose levels were measured with One Touch Glucometer. The identification tests revealed the presence of saponins (3.58%), tannins (5%); alkaloids, quinones, flavonoids, and terpenes sterols could not be formerly detected by the reagents used. Interesting chromatographic spots were observed whose behaviors are of catechic tannin proanthocyanes. The extract significantly reduced glucose levels in dose dependent manner as compared to control and glibenclamide reference groups. The average of mean percentage of reduction in glucose level at T120 with the extract 100 mg/kg was close to that of glibenclamide 0.25 mg/kg (49% and 40.2%). These findings back the traditional use of the plant to treat diabetic patients and constitute a foundation for an extensive study to find a new antidiabetic phythomedicine. [less ▲]

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See detailIn vitro antiplasmodial and cytotoxic activities of sesquiterpene lactones from Vernonia fimbrillifera Less. (Asteraceae)
Bordignon, Annélise ULiege; Frederich, Michel ULiege; Ledoux, Allison ULiege et al

in Natural Product Research (2017)

According to the World Health Organization (WHO 2016 WHO. 2016. World Malaria report 2016 [Internet]; [cited 2016 Dec 20]. Available from: https://www.who.int/malaria/publications/world-malaria-report ... [more ▼]

According to the World Health Organization (WHO 2016 WHO. 2016. World Malaria report 2016 [Internet]; [cited 2016 Dec 20]. Available from: https://www.who.int/malaria/publications/world-malaria-report-2016/report/en/ [Google Scholar] ), malaria caused at least 429 000 deaths globally in 2015. Among these, 70% were children under the age of five and 99% were due to the parasite species Plasmodium falciparum. The fight against this major public health problem is threatened by the rapid emergence and spread of parasite strains resistant towards available approved treatments. Urgent efforts are therefore needed to identify new antimalarial drugs. As such, our research groups decided to study Reunion Island as a potential source for the discovery of new antiplasmodial metabolites. This natural patrimony has been identified as a biodiversity hotspot due to its numerous endemic species and its preserved ecosystems (Myers et al. 2000 Myers N, Mittermeier RA, Mittermeier CG, DaFonesca GAB, Kent J. 2000. Biodiversity hotspots for conservation priorities. Nature. 403:853–858.10.1038/35002501 [CrossRef], [PubMed], [Web of Science ®], [Google Scholar] ). The National Botanical Conservatory of the Mascarenes indicates that Vernonia fimbrillifera Less. is an endemic species from Reunion Island, locally named ‘bois de source’, which grows in the humid tropical forest (Lavergne and Véra 1989 Lavergne R, Véra R. 1989. Etude ethnobotanique des plantes utilisées dans la pharmacopée traditionnelle à La Réunion [Ethnobotanical study of plants used in the traditional pharmacopoeia of Reunion Island]. Paris: Agence de coopération culturelle et technique. [Google Scholar] ). To the best of our knowledge, neither phytochemical nor pharmacological works have been performed up to now on V. fimbrillifera. This study isolated and determined the structure of three antiplasmodial sesquiterpene lactones. Compounds were additionally tested in vitro for their cytotoxicity and their selectivity indices were established. [less ▲]

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See detailDevelopment of an HPTLC method for determination of hypoglycin A in aqueous extracts of seedlings and samaras of Acer species.
Habyarimana, Jean Belt Adélite ULiege; Baise, Etienne; Douny, Caroline ULiege et al

E-print/Working paper (2017)

Hypoglycin A (HGA) is a toxin contained in seeds of the sycamore maple tree (Acer pseudoplatanus). Ingestion of this amino acid causes equine atypical myopathy (AM) in Europe. Another variety, A. negundo ... [more ▼]

Hypoglycin A (HGA) is a toxin contained in seeds of the sycamore maple tree (Acer pseudoplatanus). Ingestion of this amino acid causes equine atypical myopathy (AM) in Europe. Another variety, A. negundo, is claimed to be present where AM cases were reported in the US. For unknown reasons, occurrence of this disease has increased. It is important to define environmental key factors that may influence toxicity of samaras from Acer species. In addition, the content of HGA in seedlings needs to be determined since AM outbreaks, during autumn period when the seeds fall but also during spring when seeds are germinating. The present study aims to validate a reliable method using high performance thin layer chromatography for determination and comparison of HGA in samaras and seedlings. The working range of the method was between 20 μg HGA to 408 μg HGA per ml water, corresponding to 12 - 244 mg/kg fresh weight or 40 - 816 mg/kg dry weight, taking into account of an arbitrary average dry matter content of 30%. Instrumental limit of detection and limit of quantification were of 10 µg HGA/ml and 20 µg HGA/ml water, respectively. Instrumental precision was 4% (RSD on 20 repeated measurements) while instrumental accuracy ranged between 86% and 121% of expected value. The HGA recovery of the analytical method estimated from spiked samaras and seedlings samples ranged between 63 and 103%. The method was applied to 9 samples of samaras from Acer pseudoplatanus, A. platanoides and A. campestre and 5 seedlings samples from A. pseudoplatanus. The results confirm detection of HGA in samaras from A. pseudoplatanus and the absence of detection in samaras of other tested species. They also suggest that detected levels of HGA are highly variable. This confirmed the suitability of the method for HGA detection in samaras or seedling. [less ▲]

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See detailInsect fatty acids: A comparison of lipids from three Orthopterans and Tenebrio molitor L. larvae
Paul, Aman ULiege; Frederich, Michel ULiege; Caparros Megido, Rudy ULiege et al

in Journal of Asia-Pacific Entomology (2017), 20(2), 337-340

In order to explore some potential insect sources of food lipids, the lipid compositions of three Orthopterans (Acheta domesticus, Conocephalus discolor and Chorthippus parallelus) were analyzed and ... [more ▼]

In order to explore some potential insect sources of food lipids, the lipid compositions of three Orthopterans (Acheta domesticus, Conocephalus discolor and Chorthippus parallelus) were analyzed and compared with those of Tenebrio molitor larvae. A. domesticus, Co. discolor, Ch. parallelus and T. molitor larvae were found to contain approximately 15%, 13%, 10% and 32% lipids on dry weight, respectively. The lipids from three Orthopterans contain much higher amounts of essential fatty acids than those of T. molitor larvae. The two Orthopterans of the suborder Ensifera i.e., A. domesticus and Co. discolor contain linoleic acid in major quantities, while Ch. parallelus of the suborder Caelifera, contain α-linolenic acid in major quantities. The consumption of linoleic and α-linolenic fatty acid is linked with numerous health promoting effects. The factors that contribute to differences in fatty acid profiles of these insects are being discussed. At last the nutritional parameters including polyunsaturated to saturated and omega 6 to omega 3 fatty acid ratios of these insect lipids are also being discussed to understand the potential role of these lipids in human nutrition. [less ▲]

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See detailPolyphenolic profile and biological activities of the leaves and aerial parts of Echinocystis lobata (Michx.) Torr. et A.Gray (Cucurbitaceae)
Ielciu, Irina-Ioana ULiege; Vlase, Laurian; Frederich, Michel ULiege et al

in Farmacia (2017), 65(2), 179-183

The aim of the present study consisted in the quantification of the polyphenols in leaves and aerial parts of Echinocystis lobata (Michx.) Torr. et A.Gray and testing its biological potential. Analysis of ... [more ▼]

The aim of the present study consisted in the quantification of the polyphenols in leaves and aerial parts of Echinocystis lobata (Michx.) Torr. et A.Gray and testing its biological potential. Analysis of polyphenols was performed by a HPLC-MS method. Antioxidant activity of the extracts was tested by DPPH, CUPRAC, FRAP, TEAC, EPR and SNPAC assays. Cytotoxic activity was assessed on cancerous and healthy cell lines. Anti-plasmodial tests were performed on two strains of Plasmodium falciparum. Ethanolic extracts of E. lobata contain mainly p-coumaric acid, isoquercitrin, rutin, quercitrin and kaempferol. Biological assays showed a significant antioxidant effect and no cytotoxic and anti-plasmodial activity. These results offer a new perspective on E. lobata, proving it as an important source of antioxidant compounds. [less ▲]

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See detailUnguiculin A and Ptilomycalins E-H, Antimalarial Guanidine Alkaloids from the Marine Sponge Monanchora unguiculata.
Campos, Pierre-Eric; Wolfender, Jean-Luc; Quieroz, Emerson F. et al

in Journal of Natural Products (2017), 80

Chemical study of the CH2Cl2-MeOH (1:1) extract from the sponge Monanchora unguiculata collected in Madagascar highlighted five new compounds, one acyclic guanidine alkaloid, unguiculin A (1) and four ... [more ▼]

Chemical study of the CH2Cl2-MeOH (1:1) extract from the sponge Monanchora unguiculata collected in Madagascar highlighted five new compounds, one acyclic guanidine alkaloid, unguiculin A (1) and four pentacyclic alkaloids, ptilomycalins E-H (2-5), along with four known compounds: crambescidin 800 (6) and crambescidin 359 (7), crambescidic acid (8), and fromiamycalin (9). Their structures were elucidated by 1D and 2D NMR spectra and HRESIMS data. All compounds were evaluated for their cytotoxicity against KB cells and their antiplasmodial activity. The new ptilomycalin E (2) and the mixture of the new ptilomycalins G (4) and H (5) showed promising cytotoxicity against KB cells with IC50 values of 0.85 and 0.92 μM, respectively. Ptilomycalin F (3) and fromiamycalin (9) exhibited promising activity against Plasmodium falciparum with IC50 values of 0.23 and 0.24 μM, respectively [less ▲]

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See detailCyclotheonellazoles A–C, Potent Protease Inhibitors from the Marine Sponge Theonella aff. swinhoei
Issac, Michal; Aknin, Maurice; Gauvin-Bialecki, Anne et al

in Journal of Natural Products (2017), 80

he extract of a sample of the sponge Theonella aff. swinhoei collected in Madagascar exhibited promising in vitro antiplasmodial activity. The antiplasmodial activity was ascribed in part to the known ... [more ▼]

he extract of a sample of the sponge Theonella aff. swinhoei collected in Madagascar exhibited promising in vitro antiplasmodial activity. The antiplasmodial activity was ascribed in part to the known metabolite swinholide A. Further investigation of the extract afforded three unusual cyclic peptides, cyclotheonellazoles A–C (1–3), which contain six nonproteinogenic amino acids out of the eight acid units that compose these natural products. Among these acids the most novel were 4-propenoyl-2-tyrosylthiazole and 3-amino-4-methyl-2-oxohexanoic acid. The structure of the compounds was elucidated by interpretation of the 1D and 2D NMR data, HRESIMS, and advanced Merfay’s techniques. The new compounds were found to be nanomolar inhibitors of chymotrypsin and sub-nanomolar inhibitors of elastase, but did not present antiplasmodial activity. [less ▲]

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See detailMetabolomic study and pharmacological valorisation of species of the genus Psiadia endemic to Reunion and Mauritius islands.
Mahadeo, Keshika; Grondin, Isabelle; Kodja, Hippolyte et al

Poster (2017)

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See detailMicroscopic Features , Chromatographic Fingerprints and Antioxidant Property of Some Unconventional Green Leafy Vegetables Consumed in Bandundu , DR Congo
Bahati, Lydia Mangala; Kapepula, Paulin Mutwale; Kabamba, Nadège Ngombe et al

in Pharmacognosy Communications (2017), 7(4), 158--163

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See detailThe genus Psiadia: Review of traditional uses, phytochemistry and pharmacology.
Mahadeo, Keshika; Grondin, Isabelle; Kodja, Hippolyte et al

in Journal of Ethnopharmacology (2017), 210

ETHNOPHARMACOLOGICAL RELEVANCE: The genus Psiadia Jacq. ex. Willd. belongs to the Asteraceae family and includes more than 60 species. This genus grows in tropical and subtropical regions, being ... [more ▼]

ETHNOPHARMACOLOGICAL RELEVANCE: The genus Psiadia Jacq. ex. Willd. belongs to the Asteraceae family and includes more than 60 species. This genus grows in tropical and subtropical regions, being especially well represented in Madagascar and the Mascarene Islands (La Reunion, Mauritius and Rodrigues). Several Psiadia species have been used traditionally for their medicinal properties in Africa and the Mascarene Islands. Based on traditional knowledge, various phytochemical and pharmacological studies have been conducted. However there are no recent papers that provide an overview of the medicinal potential of Psiadia species. Therefore, the aim of this review is to provide a comprehensive summary of the botany, phytochemistry and pharmacology of Psiadia and to highlight the gaps in our knowledge for future research opportunities. MATERIALS AND METHODS: The available information on traditional uses, phytochemistry and biological activities of the genus Psiadia was collected from scientific databases through a search using the keyword 'Psiadia' in 'Google Scholar', 'Pubmed', 'Sciencedirect', 'SpringerLink', 'Web of Science', 'Wiley' and 'Scifinder'. Additionally, published books and unpublished Ph.D. and MSc. dissertations were consulted for botanical information and chemical composition. RESULTS: Historically, species of the genus Psiadia have been used to treat a wide range of ailments including abdominal pains, colds, fevers, bronchitis, asthma, rheumatoid arthritis, skin infections and liver disorders among others. Phytochemical works led to the isolation of flavonoids, phenylpropanoids, coumarins and terpenoids. Furthermore, phytochemical compositions of the essential oils of some species have been evaluated. Crude extracts, essential oils and isolated molecules showed in vitro pharmacological activities, such as antimicrobial, anti-viral, anti-inflammatory, antiplasmodial and antileishmanial activities. Crude extracts of Psiadia dentata and Psiadia arguta have specifically been found to be potentially useful for inhibition of growth of Plasmodium falciparum. However, pharmacological data on this particular genus is quite limited. Further research is necessary to determine the active compounds and the underlying mechanisms. [less ▲]

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See detailAntimalarial Activities of Alkyl Cyclohexenone Derivatives Isolated from the Leaves of Poupartia borbonica
Ledoux, Allison ULiege; St-Gelais, Alexis; Cieckiewicz, Ewa ULiege et al

in Journal of Natural Products (2017), 80(6), 1750-1757

Bioactivity-guided fractionation of the ethyl acetate extract of the leaves of Poupartia borbonica led to the isolation of three new alkyl cyclohexenone derivatives 1−3, and named Poupartone A−C. The ... [more ▼]

Bioactivity-guided fractionation of the ethyl acetate extract of the leaves of Poupartia borbonica led to the isolation of three new alkyl cyclohexenone derivatives 1−3, and named Poupartone A−C. The structures of the new compounds were elucidated by 1D and 2D NMR spectroscopic data analysis and MS, whereas calculated and experimental ECD spectra were used to define the absolute configurations. These compounds were active against 3D7 and W2 Plasmodium falciparum strains with IC50 values between 0.55 and 1.81 μM. In vitro cytotoxicity against WI38 human fibroblasts and the human cervical cancer cell line HeLa (WST-1 assay) showed that these compounds were also cytotoxic, but no hemolytic activity was observed for the extract and pure compounds. An in vivo antimalarial assay was performed on the major cyclohexenone using P. berghei-infected mice at a dose of 15 mg/kg/day ip. The assay revealed growth inhibition of 59.1 and 69.5% at days 5 and 7 postinfection, respectively, although some toxicity was observed. Zebrafish larvae were used as a model to determine the type of toxicity, and the results showed cardiac toxicity. The methanol extract was also studied, and it displayed moderate antiplasmodial properties in vitro. This extract contained the known flavonoids, quercetin, 3′-O-hydroxysulfonylquercetin, quercitrin, and isoquercitrin as well as ellagic acid, which showed high to low activity against the 3D7 P. falciparum strain. [less ▲]

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See detailAntihypertensive and vasorelaxant effects of aqueous extract of Artemisia campestris L. from Eastern Morocco.
Dib, Ikram; Tits, Monique ULiege; Angenot, Luc ULiege et al

in Journal of Ethnopharmacology (2017), 206

ETHNOPHARMACOLOGICAL RELEVANCE: Artemisia campestris L. (Asteraceae) has many traditional uses, among which treatment of diabetes and hypertension. AIM OF THE STUDY: This study was conducted in order to ... [more ▼]

ETHNOPHARMACOLOGICAL RELEVANCE: Artemisia campestris L. (Asteraceae) has many traditional uses, among which treatment of diabetes and hypertension. AIM OF THE STUDY: This study was conducted in order to confirm the antihypertensive and hypotensive effects of A. campestris L. aqueous extract (AcAE) and to explore the underlying mechanism of action of its vasorelaxant effect, besides the acute toxicity. Also, the chemical composition of AcAE was investigated. MATERIAL AND METHODS: the chemical content of AcAE was determined by using HPLC and NMR techniques. The antihypertensive effect was assessed indirectly by tail-cuff method on L-NAME induced hypertensive rats, while the hypotensive action was monitored intravenously by invasive method on normotensive rats. The vasorelaxant effect and vascular mechanism of action were studied in the presence of antagonists and blockers on aorta isolated from normotensive rats. On the other side, the acute toxicity was studied by oral feeding of extract to the mice. RESULTS: The global phytochemical profile of AcAE reveals the presence of several polyphenols as main components. A. campestris L. infusion was characterized by mono- and di-cinnamoyl compounds, with 3,5-dicaffeoylquinic (isochlorogenic A) acid being the main compound, followed by 5-caffeoylquinic (chlorogenic) acid. Vicenin-2 (apigenin 6,8-di-C-glucoside) appeared to be the most abundant compound among flavonoids. The daily treatment with AcAE at 150mg/Kg/day prevented the installation of hypertension on L-NAME hypertensive rats, and reduced SBP from 172mmHg up to 144mmHg. At the dose 40mg/Kg, AcAE provoked reduction of systolic (SBP), diastolic (DBP) and mean arterial pressure (MAP), without affecting the heart rate. Also, AcAE (10-2-2mg/ml) relaxed the precontracted aorta by 95.8 +/- 1.3%. The denudation and preincubation of aorta with atropine, calmidazolium, L-NAME, hydroxycobalamin, ODQ, 8-RP-Br-PET-cGMP, thapsigargin and verapamil attenuated the vasorelaxant response, while the pre-treatment with 4-AP, TEA, glibenclamide and BaCl2 did not alter this effect. The oral administration of AcAE (0-6g/Kg) reveals no mortality or toxicity. CONCLUSIONS: our study proved that AcAE possess an important antihypertensive, hypotensive and vasorelaxant effect, which is mediated via calmodulin-NO-cGC-PKG pathway, and via inhibition of calcium influx through voltage-operated calcium channels and activation of intracellular calcium mobilization into sarcoplasmic reticulum. Therefore, our findings give first evidence about the traditional use of A. campestris L. as antihypertensive plant. [less ▲]

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