Antioxidant properties and subchronic toxicity of the standardized extract of LAMIC, a phytomedicine prototype based on aqueous extracts from trunk bark of Lannea microcarpa Engl and K. Krause

Aims: This study investigated the antioxidant activity and the 90 days subchronic toxicity of the standardized LAMIC phytomedicine prototype based on aqueous extracts from Lannea microcarpa trunk bark. Methods: Three spectrophotometric methods were used to evaluated the antioxidant activity of LAMIC which were 2,2-Diphenyl-1-picrylhydrazyl (DPPH) free radical, 2,2’-azinobis(3-ethylbenzolin-6-sulphonate) (ABTS) radical scavenging assays and ferric reducing antioxidant power (FRAP) assays. For the standardized LAMIC subchronic toxicity study, male and female Wistar rats were used by daily oral administration at doses of 500, 1000 and 1500 mg/kg bw consecutively for 90 days. Results: The LAMIC extract exhibit better inhibitory activity against DPPH radical than ABTS radical with respective IC50 values of 45.38±3.21 µg/mL and 66.45±18.76 µg/mL, while FRAP assay exhibit antioxidant activity of 211.34±15.92 mmol EAA/g. Subchronic oral administration of LAMIC was well-tolerated at all tested doses. No behavioral and physiological changes and mortality were observed. The LAMIC extract did not present any impact on general hematological parameters and biochemical parameters. Moreover, no significant changes were raised in organ and body weight of treated groups compared to the Control group. Conclusion: These results support that LAMIC prototype was a valuable source of natural antioxidants and no toxicity was associated to its long terms oral consumption in rats indicating a potential application as a cardiovascular protective formulation. Keywords: LAMIC–Lannea microcarpa–Standardization–Antioxidant–Subchronic toxicity. &nbsp

Characterization of anti-inflammatory and anticancer properties of Agelanthus dodoneifolius (DC) Polh. & Wiens (Loranthaceae) used in traditional medicine plant in Burkina Faso

Le présent travail a porté sur l’évaluation des propriétés anti-inflammatoires et anticancéreuses de Agelanthus dodoneifolius (Loranthaceae), communément appelée «gui africain». Cette plante hémiparasite est utilisée en médecine traditionnelle africaine pour le traitement de pathologies chroniques telles que l’asthme, l’hypertension, des gastroentérites et le cancer. Actuellement, les maladies chroniques représentent un problème mondial de santé publique. En effet, elles constituent la première cause de mortalité dans le monde surtout dans les pays à revenu faible ou intermédiaire. Cette étude a été réalisée dans le but d’apporter une validation scientifique quant à certaines utilisations traditionnelles de Agelanthus dodoneifolius. Pour évaluer l’effet anti-inflammatoire de Agelanthus dodoneifolius, nous avons testé les différentes fractions de la plante sur la production des espèces réactives de l’oxygène, la libération et l’activité spécifique de la myéloperoxydase (MPO), enzyme libérée par le neutrophile au cours de la phagocytose pour détruire les microorganismes. L’identification et la quantification des composés a été faite grâce à une combinaison des méthodes chromatographiques, spectrophotométriques et spectrométriques. L’activité anticancéreuse de Agelanthus dodoneifolius a consisté, d’abord, à déterminer l’effet d’inhibition de croissance de diverses fractions de la plante, de la quercétine ainsi que de ses dérivés sur des lignées cellulaires cancéreuses. Nous avons ensuite déterminé les effets de la quercétine sur l’activité de plus de 300 kinases. Les résultats obtenus montrent qu’Agelanthus dodoneifolius est capable de moduler les activités biologiques des neutrophiles. En effet, le décocté aqueux et les fractions organiques de la plante inhibent de manière dose-dépendante la production des espèces réactives de l’oxygène, la dégranulation du neutrophile et l’activité spécifique de la myéloperoxydase. Nous avons pu identifier et quantifier dix composés polyphénoliques dont quatre acides phénoliques :l’acide gallique, l’acide coumarique, l’acide chlorogénique et l’acide ellagique et six flavonoïdes :la quercétine, le kaempférol, la catéchine, l’isoquercitrine ou quercétine 3-O-glucoside, la rutine et la miquelianine ou quercétine-3-O-glucuronide. Concernant l’activité anticancéreuse, les résultats montrent que seules les fractions à l’éther diéthylique et à l’acétate d’éthyle ont une activité antiproliférative. La quercétine a des effets inhibiteurs de croissance, cytostatiques et présente un large spectre d’activité sur plusieurs kinases surexprimées dans certains cancers. En conclusion, l’ensemble de ces résultats constitue des bases scientifiques qui pourraient justifier certaines utilisations traditionnelles de Agelanthus dodoneifolius. À notre connaissance, cette étude est la première à évaluer d’une part l’effet, in vitro, des différentes fractions de Agelanthus dodoneifolius sur des neutrophiles stimulés et sur la MPO et d’autre part l’effet inhibiteur de croissance de lignées cellulaires cancéreuses par certaines fractions de la plante. En outre, cette étude a permis pour la première fois d’identifier et de quantifier des composés polyphénoliques dans Agelanthus dodoneifolius. Les nombreuses propriétés de ces composés, notamment celles anti-inflammatoires et anticancéreuses, peuvent expliquer en partie les résultats reportés dans ce travail.This work focused on evaluating anti-inflammatory and anticancer activities of Agelanthus dodoneifolius (Loranthaceae), commonly called "African mistletoe". This plant is used in African traditional medicine for the treatment of chronic conditions such as asthma, hypertension, gastroenteritis and cancer. Currently, chronic diseases are a global public health problem. Indeed, they are the leading cause of death worldwide, especially in countries with low and middle income.The study was conducted to provide scientific validation for some traditional uses of Agelanthus dodoneifolius.To characterize the anti-inflammatory activity of Agelanthus dodoneifolius, we tested the different fractions of the plant on reactive oxygen species production, release and the specific activity of myeloperoxidase, an enzyme released by neutrophils during phagocytosis to destroy microorganisms. The identification and quantification of compounds were made through a combination of chromatographic, spectrophotometric and spectrometric techniques. The anticancer activity of Agelanthus dodoneifolius consisted, first, to determine, the antiproliferative effect of fractions of the plant, quercetin and its derivatives on cancer cell lines. Then, we determined the effects of quercetin on the activity of more than 300 kinases.The results show that Agelanthus dodoneifolius is capable of modulating the biological activities of neutrophils. In fact, the decoction aqueous and organic fractions of the plant inhibited in a dose-dependent manner the production of reactive oxygen species, degranulation of neutrophils and specific activity of myeloperoxidase. We were able to identify and quantify ten polyphenolic compounds including four phenolic acids: gallic acid, coumaric acid, chlorogenic acid and ellagic acid and six flavonoids: quercetin, kaempferol, catechin, isoquercitrin or quercetin 3-O-glucoside, rutin and miquelianin or quercetin-3-O-glucuronide.Regarding the anticancer activity, the results show that only fractions with diethyl ether and ethyl acetate have antiproliferative activity. Quercetin has antiproliferative and cytostatic effects and presents a broad spectrum of activity on several kinases overexpressed in certain cancers.In conclusion, all these findings are scientific basis that could justify some traditional uses of Agelanthus dodoneifolius. To our knowledge, this is the first study to evaluate the effect firstly, by in vitro tests, of the different fractions of Agelanthus dodoneifolius on stimulated neutrophils and the MPO and secondly the growth inhibitory effect of cancer cell lines by certain fractions. Also, this study is the first to identify and quantify the phenolic compounds in Agelanthus dodoneifolius. The many properties of these compounds, including anti-inflammatory and anticancer, may partly explain the results reported in the present work.Doctorat en Sciences biomédicales et pharmaceutiquesinfo:eu-repo/semantics/nonPublishe

Characterization of anti-inflammatory and anticancer properties of Agelanthus dodoneifolius (DC) Polh. & Wiens (Loranthaceae) used in traditional medicine plant in Burkina Faso

Le présent travail a porté sur l’évaluation des propriétés anti-inflammatoires et anticancéreuses de Agelanthus dodoneifolius (Loranthaceae), communément appelée «gui africain». Cette plante hémiparasite est utilisée en médecine traditionnelle africaine pour le traitement de pathologies chroniques telles que l’asthme, l’hypertension, des gastroentérites et le cancer. Actuellement, les maladies chroniques représentent un problème mondial de santé publique. En effet, elles constituent la première cause de mortalité dans le monde surtout dans les pays à revenu faible ou intermédiaire. Cette étude a été réalisée dans le but d’apporter une validation scientifique quant à certaines utilisations traditionnelles de Agelanthus dodoneifolius. Pour évaluer l’effet anti-inflammatoire de Agelanthus dodoneifolius, nous avons testé les différentes fractions de la plante sur la production des espèces réactives de l’oxygène, la libération et l’activité spécifique de la myéloperoxydase (MPO), enzyme libérée par le neutrophile au cours de la phagocytose pour détruire les microorganismes. L’identification et la quantification des composés a été faite grâce à une combinaison des méthodes chromatographiques, spectrophotométriques et spectrométriques. L’activité anticancéreuse de Agelanthus dodoneifolius a consisté, d’abord, à déterminer l’effet d’inhibition de croissance de diverses fractions de la plante, de la quercétine ainsi que de ses dérivés sur des lignées cellulaires cancéreuses. Nous avons ensuite déterminé les effets de la quercétine sur l’activité de plus de 300 kinases. Les résultats obtenus montrent qu’Agelanthus dodoneifolius est capable de moduler les activités biologiques des neutrophiles. En effet, le décocté aqueux et les fractions organiques de la plante inhibent de manière dose-dépendante la production des espèces réactives de l’oxygène, la dégranulation du neutrophile et l’activité spécifique de la myéloperoxydase. Nous avons pu identifier et quantifier dix composés polyphénoliques dont quatre acides phénoliques :l’acide gallique, l’acide coumarique, l’acide chlorogénique et l’acide ellagique et six flavonoïdes :la quercétine, le kaempférol, la catéchine, l’isoquercitrine ou quercétine 3-O-glucoside, la rutine et la miquelianine ou quercétine-3-O-glucuronide. Concernant l’activité anticancéreuse, les résultats montrent que seules les fractions à l’éther diéthylique et à l’acétate d’éthyle ont une activité antiproliférative. La quercétine a des effets inhibiteurs de croissance, cytostatiques et présente un large spectre d’activité sur plusieurs kinases surexprimées dans certains cancers. En conclusion, l’ensemble de ces résultats constitue des bases scientifiques qui pourraient justifier certaines utilisations traditionnelles de Agelanthus dodoneifolius. À notre connaissance, cette étude est la première à évaluer d’une part l’effet, in vitro, des différentes fractions de Agelanthus dodoneifolius sur des neutrophiles stimulés et sur la MPO et d’autre part l’effet inhibiteur de croissance de lignées cellulaires cancéreuses par certaines fractions de la plante. En outre, cette étude a permis pour la première fois d’identifier et de quantifier des composés polyphénoliques dans Agelanthus dodoneifolius. Les nombreuses propriétés de ces composés, notamment celles anti-inflammatoires et anticancéreuses, peuvent expliquer en partie les résultats reportés dans ce travail.This work focused on evaluating anti-inflammatory and anticancer activities of Agelanthus dodoneifolius (Loranthaceae), commonly called "African mistletoe". This plant is used in African traditional medicine for the treatment of chronic conditions such as asthma, hypertension, gastroenteritis and cancer. Currently, chronic diseases are a global public health problem. Indeed, they are the leading cause of death worldwide, especially in countries with low and middle income.The study was conducted to provide scientific validation for some traditional uses of Agelanthus dodoneifolius.To characterize the anti-inflammatory activity of Agelanthus dodoneifolius, we tested the different fractions of the plant on reactive oxygen species production, release and the specific activity of myeloperoxidase, an enzyme released by neutrophils during phagocytosis to destroy microorganisms. The identification and quantification of compounds were made through a combination of chromatographic, spectrophotometric and spectrometric techniques. The anticancer activity of Agelanthus dodoneifolius consisted, first, to determine, the antiproliferative effect of fractions of the plant, quercetin and its derivatives on cancer cell lines. Then, we determined the effects of quercetin on the activity of more than 300 kinases.The results show that Agelanthus dodoneifolius is capable of modulating the biological activities of neutrophils. In fact, the decoction aqueous and organic fractions of the plant inhibited in a dose-dependent manner the production of reactive oxygen species, degranulation of neutrophils and specific activity of myeloperoxidase. We were able to identify and quantify ten polyphenolic compounds including four phenolic acids: gallic acid, coumaric acid, chlorogenic acid and ellagic acid and six flavonoids: quercetin, kaempferol, catechin, isoquercitrin or quercetin 3-O-glucoside, rutin and miquelianin or quercetin-3-O-glucuronide.Regarding the anticancer activity, the results show that only fractions with diethyl ether and ethyl acetate have antiproliferative activity. Quercetin has antiproliferative and cytostatic effects and presents a broad spectrum of activity on several kinases overexpressed in certain cancers.In conclusion, all these findings are scientific basis that could justify some traditional uses of Agelanthus dodoneifolius. To our knowledge, this is the first study to evaluate the effect firstly, by in vitro tests, of the different fractions of Agelanthus dodoneifolius on stimulated neutrophils and the MPO and secondly the growth inhibitory effect of cancer cell lines by certain fractions. Also, this study is the first to identify and quantify the phenolic compounds in Agelanthus dodoneifolius. The many properties of these compounds, including anti-inflammatory and anticancer, may partly explain the results reported in the present work.Doctorat en Sciences biomédicales et pharmaceutiquesinfo:eu-repo/semantics/nonPublishe

Etude des propriétés antioxydante et cytotoxique des extraits aqueux des feuilles de Agelanthus dodoneifolius(Loranthaceae)

Congrès de la SPTC (Société de Pharmacotoxicologie cellulaire)info:eu-repo/semantics/nonPublishe

DPPH free radical scavenging activity of two extracts from agelanthus dodoneifolius (Loranthaceae) leaves

Agelanthus dodoneifolius (Loranthaceae) commonly named African mistletoe is traditionally used in Burkina Faso as a decoction for the treatment of asthma, stomach-ache and cardiovascular diseases. The current study was designed to assess the DPPH free radical scavenging effect and the flavonoid and phenolic contents of the decoction and maceration extracts from Agelanthus dodoneifolius leaves. Moreover, the phytochemical analysis was also carried out. The decoction and maceration were prepared in water. Phytochemical analysis was realized according to the standard protocols. The scavenging activity was determined using the radical 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. The flavonoid and phenolic contents were assessed using the Neu and Folin-Ciocalteu reagents, respectively. The phytochemical investigation showed the presence of flavonoid, tannins, steroids, triterpenes, carotenoids, anthocyanins and sugars in Agelanthus dodoneifolius dried and powdered leaves. Both decoction and maceration exhibited a significant dose-dependent radical scavenging activity with EC50 values of 8.20 ± 0.25 and 13.20 ± 0.37 μg/mL, respectively. This significant radical scavenging effect may be attributed to their richness in flavonoid and phenolic compounds. This study enhances the ability of Agelanthus dodoneifolius leaves as excellent natural source for antiradical scavenging. Therefore, the results may be taken account for the development of an herbal medicine to treat diseases related to an oxidative damage.SCOPUS: ar.jinfo:eu-repo/semantics/publishe

Quercetin inhibits a large panel of kinases implicated in cancer cell biology.

Flavonoids are polyphenolic secondary metabolites from plants that possess a common phenylbenzopyrone structure (C6-C3-C6). Depending upon variations in their heterocyclic C-ring, flavonoids are categorised into one of the following groups: flavones, flavonols, flavanones, flavanols, anthocyanidins, isoflavones or chalcones. Flavonols include, among others, the molecules quercetin, myricetin and kaempferol. The anticancer activity of flavonols was first attributed to their electron-donating ability, which comes from the presence of phenolic hydroxyl groups. However, an emerging view is that flavonoids, including quercetin, may also exert modulatory actions in cells by acting through the protein kinase and lipid kinase signalling pathways. Data from the current study showed that 2 μM quercetin, a low concentration that represents less than 10% of its IC50 growth-inhibitory concentration as calculated from the average of eight distinct cancer cell lines, decreased the activity of 16 kinases by more than 80%, including ABL1, Aurora-A, -B, -C, CLK1, FLT3, JAK3, MET, NEK4, NEK9, PAK3, PIM1, RET, FGF-R2, PDGF-Rα and -Rß. Many of these kinases are involved in the control of mitotic processes. Quantitative video microscopy analyses revealed that quercetin displayed strong anti-mitotic activity, leading to cell death. In conclusion, quercetin partly exerts its anticancer activity through the inhibition of the activity of a large set of kinases. Quercetin could be an interesting chemical scaffold from which to generate novel derivatives possessing various types of anti-kinase activities.Comparative StudyJournal ArticleResearch Support, Non-U.S. Gov'tSCOPUS: ar.jinfo:eu-repo/semantics/publishe

Modulatory activities of Agelanthus dodoneifolius (Loranthaceae) extracts on stimulated equineneutrophils and myeloperoxidase activity

info:eu-repo/semantics/publishe

Modulatory activities of Agelanthus dodoneifolius (Loranthaceae) extracts on stimulated equine neutrophils and myeloperoxidase activity

Agelanthus dodoneifolius DC Danser (Loranthaceae) is used for the treatment of various diseases including asthma. The aqueous and hydroalcoholic extracts have been reported to have anti-inflammatory, spasmolytic and bronchorelaxant activities. The present study investigates the effects of the aqueous decoction and the diethyl ether, ethyl acetate and butanolic fractions of Agelanthus dodoneifolius DC Danser (Loranthaceae) on reactive oxygen species (ROS) production and myeloperoxidase (MPO) release by phorbol 12-myristate 13-acetate (PMA)-stimulated equine neutrophils and on purified equine MPO activity. ROS production and MPO release by the PMA-stimulated neutrophils were measured by the lucigenin-enhanced chemiluminescence and ELISA assays, respectively. Specific immunological extraction followed by enzymatic detection (SIEFED) was used to specifically measure the equine MPO activity. Identification and quantification of the individual and total phenolic and flavonoid compounds were performed using UPLG-MS/MS equipment and colorimetric methods involving Folin-Giocalteu and AlCl3, respectively. All the tested extracts displayed dose-dependent inhibitory effects on the oxidant activities of neutrophils; a stronger effect was observed with the organic fractions than the aqueous decoction. These findings could be correlated with a high content of phenolic and flavonoid compounds. The results confirm the previously shown anti-inflammatory effect of Agelanthus dodoneifolius and its potential use for the treatment of neutrophil-dependent inflammatory diseases.SCOPUS: ar.jinfo:eu-repo/semantics/publishe

Effet gastroprotecteur et potentiel mécanisme d’action antiulcéreuse d’extraits de fruits de Acacia nilotica var adansonii (Guill. et Perr.) O. Ktze (Mimosaceae)

Acacia nilotica est utilisée par les tradipraticiens dans la prise en charge des ulcères gastroduodénaux au Burkina Faso. L’objectif de cette étude était d’évaluer l’effet gastroprotecteur et le potentiel mécanisme d’action des extraits aqueux et hydroéthanolique des fruits secs de Acacia nilotica L. (Mimosaceae) sur un modèle d’ulcère gastrique induit par l’éthanol chez la souris. Un criblage phytochimique et un dosage des composés phénoliques ont été réalisés sur les extraits aqueux et hydroéthanolique des fruits secs de Acacia nilotica. L’étude de la toxicité et de l’effet gastroprotecteur a été évaluée chez la souris. Ensuite, une évaluation de l’effet spasmolytique, du pouvoir antioxydant avec les méthodes DPPH et ABTS des extraits ont été réalisés. La forte teneur en composés phénoliques et flavonoïdes totaux a été obtenue avec le décocté. La toxicité aiguë étudiée a permis de classer les extraits étudiés comme des substances faiblement toxiques. Le macéré hydroéthanolique a présenté le meilleur effet spasmolytique. L’étude de l’activité antiradicalaire par la méthode de DPPH a permis d’obtenir des CI50 qui ont varié de 6,79 ± 0,86 à 9,39 ± 0,01 μg/ml et la méthode ABTS a permis d’obtenir un TEAC qui a varié de 0,19 à 0,87 mg ET/g. Cependant le décocté aqueux a présenté le meilleur effet gastroprotecteur à la dose de 400 mg/kg avec 97,50 %. La forte teneur en composé phénoliques et les propriétés pharmacologiques des extraits pourraient justifier l’utilisation de Acacia nilotica par les tradipraticiens dans la prise en charge des ulcères gastroduodénaux.Mots-clés: Acacia nilotica, gastroprotecteur, antioxydant, spasmolytique, ulcèreEnglish Title: Gastroprotective effect and potential anti-ulcer mechanism of action of fruit extracts of Acacia nilotica var adansonii (Guill. et Perr.) O. Ktze (Mimosaceae)English AbstractIn Burkina Faso, medicinal plants are used by traditional healers in the of peptic ulcers including Acacia nilotica. This study was aimed to evaluate the gastroprotective effect of aqueous and aqueous-ethanolic extracts of A. nilotica dry fruits on a model of gastric ulcer induced by ethanol in mice. Phytochemical screening and determination of the phenolic compounds were carried out on the aqueous and aqueousethanolic extracts of dry fruits from A. nilotica. Also, a study of the toxicity and the gastroprotective effect was evaluated in NMRI mice. Then, an evaluation of spasmolytic effect on contractions induced by acetylcholine and barium chloride, of the antioxidant power with DPPH and ABTS methods of extracts were carried out. The highest content of phenolic and flavonoids was obtained with the aqueous extract. Acute toxicity allowed to classify the extracts as weakly toxic substances. Hydroethanolic extract showed the best released effect on contractions induced by acetylcholine and barium chloride. Extracts IC50 varied from 6.79 ± 0.86 to 9.39 ± 0.01μg/mL using DPPH method, and ABTS method TEAC ranged from 0.19mgET / g to 0.87mg ET / g. However aqueous decoction showed a better protection against gastric mucosa at dose of 400 mg/kg with 97.50%. High content of phenolic compounds and pharmacological effects of extracts justify Acacia nilotica use by traditional healer in peptic ulcer management.Keywords: Acacia nilotica, gastroprotective, antioxidant, spasmolytic, ulce