Antiplasmodial and GABA(A)-benzodiazepine receptor binding activities of five plants used in traditional medicine in Mali, West Africa.
ABSTRACT Extracts of five medicinal plants: Boscia angustifolia, Cissus quadrangularis, Securidaca longipedunculata, Stylosanthes erecta and Trichilia emetica, used traditionally in Malian traditional medicine were screened for in vitro antiplasmodial activity and GABA(A)-benzodiazepine receptor binding activity. Four extracts showed significant antiplasmodial activities, with the dichloromethane extract of leaf of Securidaca longipedunculata being the most active (IC(50) of 7 microg/ml [95% CI: 5-9]). The dichloromethane extract of leaf of Trichilia emetica, in addition to its antiplasmodial activity (IC(50): 12 microg/ml [95% CI: 12-14]), exhibited a good binding activity to the GABA(A)-benzodiazepine receptor, while water and methanol extracts of the same plant did not show any activity. A strong GABA(A)-receptor complex binding activity was observed in the methanol extract of aerial part of Stylosanthes erecta. The results in this study justify some of the traditional indications of the plants investigated and may thus be candidates for Improved Traditional Medicines in Mali.
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ABSTRACT: Plasmodium falciparum relies on anion channels activated in the erythrocyte membrane to ensure the transport of nutrients and waste products necessary for its replication and survival after invasion. The molecular identity of these anion channels, termed "new permeability pathways" is unknown, but their currents correspond to up-regulation of endogenous channels displaying complex gating and kinetics similar to those of ligand-gated channels. This report demonstrates that a peripheral-type benzodiazepine receptor, including the voltage dependent anion channel, is present in the human erythrocyte membrane. This receptor mediates the maxi-anion currents previously described in the erythrocyte membrane. Ligands that block this peripheral-type benzodiazepine receptor reduce membrane transport and conductance in P falciparum-infected erythrocytes. These ligands also inhibit in vitro intraerythrocytic growth of P falciparum. These data support the hypothesis that dormant peripheral-type benzodiazepine receptors become the "new permeability pathways" in infected erythrocytes after up-regulation by P falciparum. These channels are obvious targets for selective inhibition in anti-malarial therapies, as well as potential routes for drug delivery in pharmacologic applications.Blood 07/2011; 118(8):2305-12. · 9.06 Impact Factor
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ABSTRACT: The present study was performed to explore the antihyperglyceamic activity of ethanolic extract of leaves of Cissus quadrangularis against alloxan induced diabetic rats. Ethanolic extract of C. quadrangularis and glyburide were administered orally in alloxan induced diabetic rats. In the acute study, the serum glucose level was estimated at 0, 2, 4, 6 and 24 h after drug administration. The subacute study involved repeated administration of the drugs for 28 days, a serum glucose level estimated at 7, 14, 21 and 28 days. In the OGTT, D-glucose (2.5 g/kg) was administered in diabetic rats half an hour after pre-treatment with EtCQ and glyburide. Serum glucose levels were estimated 30 min prior to glucose administration and at 0, 30, 60 and 120 min after glucose loading. In EtCQ (400 mg/kg), the onset was 4 h, the peak effect was 6 h but the effect waned at 24 h. In subacute study, repeated administration (once a day for 28 days) of the glyburide and EtCQ caused a significant reduction in the serum glucose level as compared to the vehicle treated group. EtCQ (400 mg/kg) treatment prevented a decrease in the body weight of the diabetic rats. In the OGTT, EtCQ (200 & 400 mg/kg) increased the glucose threshold at 30 min after the administration of glucose. The EtCQ (400 mg/kg) showed significant antihyperglyceamic activity than EtCQ (100 and 200 mg/kg). It can be concluded that ethanolic extract of C. quadrangularis has antihyperglyceamic activity.Journal of Applied Pharmaceutical Sciences. 01/2013; 3(1):73-77.
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ABSTRACT: The present study was to determine the efficacies of anti-parasitic activities of synthesized silver nanoparticles (Ag NPs) using stem aqueous extract of Cissus quadrangularis against the adult of hematophagous fly, Hippobosca maculata (Diptera: Hippoboscidae), and the larvae of cattle tick, Rhipicephalus (Boophilus) microplus (Acari: Ixodidae). Contact toxicity method was followed to determine the potential of parasitic activity. Twelve milliliters of stem aqueous extract of C. quadrangularis was treated with 88ml of 1mM silver nitrate (AgNO(3)) solution at room temperature for 30min and the resulting solution was yellow-brown color indicating the formation extracellular synthesis of Ag NPs. The synthesized Ag NPs were characterized with UV-visible spectroscopy, X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), Field emission scanning electron microscope (FESEM) and energy dispersive X-ray (EDX) spectroscopy. The synthesized Ag NPs were recorded by UV-visible spectrum at 420nm and XRD patterns showed the nanoparticles crystalline in nature. FTIR analysis confirmed that the bioreduction of Ag((+)) ions to Ag NPs were due to the reduction by capping material of plant extract. FESEM image of Ag NPs showed spherical and oval in shape. By using the Bragg's Law and Scherrer's constant, the average mean size of synthesized Ag NPs was 42.46nm. The spot EDX analysis showed the complete chemical composition of the synthesized Ag NPs. The mortality obtained by the synthesized Ag NPs from the C. quadrangularis was more effective than the aqueous extract of C. quadrangularis and AgNO(3) solution (1mM). The adulticidal activity was observed in the aqueous extract, AgNO(3) solution and synthesized Ag NPs against the adult of H. maculata with LC(50) values of 37.08, 40.35 and 6.30mg/L; LC(90) values of 175.46, 192.17 and 18.14mg/L and r(2) values of 0.970, 0.992 and 0.969, respectively. The maximum efficacy showed in the aqueous extract, AgNO(3) solution and synthesized Ag NPs against the larvae of R. (B.) microplus with LC(50) values of 50.00, 21.72 and 7.61mg/L; LC(90) values of 205.12, 82.99 and 22.68mg/L and r(2) values of 0.968, 0.945and 0.994, respectively. The present study is the first report on antiparasitic activity of the experimental plant extract and synthesized Ag NPs. This is an ideal eco-friendly and inexpensive approach for the control of H. maculata and R. (B.) microplus.Experimental Parasitology 06/2012; 132(2):156-65. · 2.15 Impact Factor