Prenylated flavanone derivatives isolated from Erythrina addisoniae are potent inducers of apoptotic cell death

NoExtracts of Erythrina addisoniae are frequently used in the traditional medicine of Western Africa, but insufficient information about active compounds is available. From the stem bark of E. addisoniae, three (1, 2, 4) and three known (3, 5, 6) flavanones were isolated: addisoniaflavanones I and II, containing either a 2″,3″-epoxyprenyl moiety (1) or a 2″,3″-dihydroxyprenyl moiety (2) were shown to be highly toxic (MTT assay: EC50 values of 5.25 ± 0.7 and 8.5 ± 1.3 μM, respectively) to H4IIE hepatoma cells. The cytotoxic potential of the other isolated flavanones was weaker (range of EC50 values between 15 and >100 μM). Toxic effects of addisoniaflavanone I and II were detectable after 3 h (MTT assay). Both compounds induced an apoptotic cell death (caspase-3/7 activation, nuclear fragmentation) in the hepatoma cells and, at high concentrations, also necrosis (membrane disruption: ethidium bromide staining). Formation of DNA strand breaks was not detectable after incubation with these compounds (comet assay). In conclusion, the prenylated flavanones addisoniaflavanones I and II may be of interest for pharmacological purposes due to their high cytotoxic and pro-apoptotic potential against hepatoma cells

In vitro and in silico evaluation of anticholinesterase and antidiabetic effects of furanolabdanes and other constituents from Graptophyllum pictum (Linn.) Griffith

peer reviewe

In Vitro and In Silico Evaluation of Anticholinesterase and Antidiabetic Effects of Furanolabdanes and Other Constituents from Graptophyllum pictum (Linn.) Griffith.

peer reviewedGraptophyllum pictum is a tropical plant noticeable for its variegated leaves and exploited for various medicinal purposes. In this study, seven compounds, including three furanolabdane diterpenoids, i.e., Hypopurin E, Hypopurin A and Hypopurin B, as well as with Lupeol, β-sitosterol 3-O-β-d-glucopyranoside, stigmasterol 3-O-β-d-glucopyranoside and a mixture of β-sitosterol and stigmasterol, were isolated from G. pictum, and their structures were deduced from ESI-TOF-MS, HR-ESI-TOF-MS, 1D and 2D NMR experiments. The compounds were evaluated for their anticholinesterase activities against acetylcholinesterase (AChE) and butyrylcholinesterase (BchE), as well as their antidiabetic potential through inhibition of α-glucosidase and α-amylase. For AChE inhibition, no sample had IC50 within tested concentrations, though the most potent was Hypopurin A, which had a percentage inhibition of 40.18 ± 0.75%, compared to 85.91 ± 0.58% for galantamine, at 100 µg/mL. BChE was more susceptible to the leaves extract (IC50 = 58.21 ± 0.65 µg/mL), stem extract (IC50 = 67.05 ± 0.82 µg/mL), Hypopurin A (IC50 = 58.00 ± 0.90 µg/mL), Hypopurin B (IC50 = 67.05 ± 0.92 µg/mL) and Hypopurin E (IC50 = 86.90 ± 0.76 µg/mL). In the antidiabetic assay, the furanolabdane diterpenoids, lupeol and the extracts had moderate to good activities. Against α-glucosidase, lupeol, Hypopurin E, Hypopurin A and Hypopurin B had appreciable activities but the leaves (IC50 = 48.90 ± 0.17 µg/mL) and stem (IC50 = 45.61 ± 0.56 µg/mL) extracts were more active than the pure compounds. In the α-amylase assay, stem extract (IC50 = 64.47 ± 0.78 µg/mL), Hypopurin A (IC50 = 60.68 ± 0.55 µg/mL) and Hypopurin B (IC50 = 69.51 ± 1.30 µg/mL) had moderate activities compared to the standard acarbose (IC50 = 32.25 ± 0.36 µg/mL). Molecular docking was performed to determine the binding modes and free binding energies of Hypopurin E, Hypopurin A and Hypopurin B in relation to the enzymes and decipher the structure-activity relationship. The results indicated that G. pictum and its compounds could, in general, be used in the development of therapies for Alzheimer's disease and diabetes

Les aires protégées de l'Extrême-Nord Cameroun entre politiques de conservation et pratiques locales

Septembre 2007This research aims to evaluate the impact of public policies of conservation and management of protected areas in view of local logics from exploitation of natural resources. Within the framework of this reflexion, we try to consider the weight of the national policies of conservation on the evolution of the protected areas from Far North of Cameroon. This research proposes to answer the following question: the dynamics analyzing of the land occupation makes it possible to judge effectiveness of the conservation policy in protected areas from the Far North of Cameroon? To characterize and evaluate the dynamics of the vegetation, the adopted method privileges a double entry taking of account at the same time spatialization and the institutional speech. This way, the exploitation at the same time of the historical and legal data, cartographic data and satellite images acquired on successive dates will be supplemented by statements of land and socio-economic investigations. The whole of collected information will constitute the data base necessary for creation of Geographic Information System (GIS), an indispensable tool for the long-lasting resources management of protected areas.Cette recherche a pour objectif d'évaluer l'impact des politiques publiques de conservation et de gestion des aires protégées face aux logiques paysannes d'exploitation des ressources et de développement. Dans le cadre de cette réflexion, nous tentons d'estimer le poids réel des politiques nationales de conservation des aires protégées de l'Extrême-Nord Cameroun. Cette recherche se propose de répondre à la question suivante : l'analyse de la dynamique de l'occupation du sol à l'intérieur et autour des aires protégées permetelle de juger de l'efficacité de la politique de conservation dans les aires protégées de l'Extrême- Nord Cameroun ? Pour caractériser et évaluer la dynamique de la végétation, la méthode retenue privilégie une double entrée prenant en compte à la fois la spatialisation et le discours. De la sorte, l'exploitation à la fois des données historiques et juridiques, des données cartographiques et des images satellites acquises à des dates successives est complétée par des relevés de terrain et des enquêtes socio-économiques. L'ensemble des informations collectées constitue la base de données nécessaire pour la création d'un Système d'information Géographique (SIG), outil indispensable à la gestion durable des ressources dans les aires protégées

Data for: New Triterpene saponins from the stem of Acacia kamerunensis (Mimosaceae)

Supporting Information