Novel cholinesterase inhibitory effect of α-spinasterol isolated from the leaves of Acacia auriculiformis A. CUNN Ex. Benth (Fabaceae)

Purpose: To investigate the in vitro anticholinesterase, α-glucosidase and antioxidant activities of α-spinasterol isolated from Acacia auriculiformis leaves.Methods: The powdered leaves of Acacia auriculiformis were extracted with 70 % ethanol and the dried hydroalcoholic extract was suspended in water and partitioned with ethyl acetate and n-butanol to give their soluble fractions. The in vitro inhibitory activities of α-spinasterol were determined against cholinesterase and, α-glucosidase enzymes, and free radical scavenging potentials using (1,1-diphenyl-2-picrylhydarzyl (DPPH) and 2,2-azino-bis (3-Ethylbenzothiazoline-6-sulphonic acid (ABTS) antioxidantassays.Results: The compound, α-spinasterol, exhibited moderate anticholinesterase activity (IC50 value of 44.19±2.59 μg/mL which was significantly  different at (p < 0.05) when compared to the standard galanthamine (IC50 value of 1.73 ± 1.10 μg/mL). It also displayed a good α-glucosidase  inhibitory activity with IC``` value of 8.65 ± 1.71μg/mL which was not significantly different when compared to the standard, acarbose with IC50 value of 2.79±0.81 μg/mL. This compound, however, exhibited weak free radical scavenging activities at 26.93 ± 0.00 and 35.16 ±.0.26 % inhibition of DPPH+ and ABTS+ radicals as compared to ascorbic acid and Trolox (73.88 ± 0.04 and 99.82 ± 0.00%) respectively.Conclusion: The results show that α-spinasterol isolated from Acacia auriculiformis exerts potent inhibitory effect against cholinesterase enzyme which might serve as a lead in the search for drugs against Alzheimer disease and diabetes mellitus. Keywords: Acacia auriculiformis, α-Spinasterol, Galanthamine, Acarbose, Trolox, Ascorbic aci

Effects Of Artesunate Alone And In Combination With Folic Acid On The Liver And Serum Iron Level Of Male Wistar Rats. Udobre et al. Effects of Artesunate Alone and In Combination with Folic Acid on the Liver and Serum Iron Level of Male Wistar Rats Effect

ABSTRACT The effects of oral administration of artesunate alone and with folic acid on the liver and on the serum levels of iron were assessed in eighty-one male wistar rats with a mean weight of 180 g (172-188 g). Thirty-six rats received artesunate of graded doses ; another thirty-six rats received a combination of artesunate and folic acid; while normal saline was administered to the remaining nine rats which served as the negative control group. Comparison of means of results was done with the student's ttest at a 95% level of significance. The results showed that in rats treated with 6.00 mg/kg of artesunate alone, there was a significant decrease in liver weight from 3.25±0.55 to 2.64±0.12g. Necrosis of the hepatocytes as revealed by liver histology also occurred. The serum iron level rose significantly from 784±11.49 mol/L to 1773±11.32 mol/L. It was also found that folic acid reversed metabolic and tissue disorder associated with lower doses of artesunate but offered partial relief to the same disorders associated with higher doses of the drug. This is evident by the decrease in serum iron and the the healthy cytoarchitecture of the liver

Antimicrobial activity of compounds isolated from the leaves of Aspilia africana (Pers.) C. D. Adams (Asteraceae)

Background: Incidences of serious failures in the treatment of infectious disease by antibiotics caused by the emergence and spread of drug resistant strains of the microorganisms/multiple drug resistant bacteria have led to new global search for more effective anti-infective microbial agents from natural sources. This study intends to examine the anti-microbial potentials of the leaves of Aspilia africana, which is employed in the treatment of wounds and sores by traditional medical practitioners in Nigeria. Objective: To evaluate the anti-microbial potentials of the isolates from leaves of Aspilia africana (Pers.) C. D. Adams (Aristeraceae), using isolated clinical strains of pathogens such as Staphylococcus aureus, Methicillin Resistant Staphylococcus aureus (MRSA), Streptococcus pyogenes, Bacillus substilis, Proteus vulgaris, Salmonella typhi, Shigella dysenteriae, Escherichia coli, Klebsiella pneumonia, Candida albicans and Candida stellafoidea. Methodology: Three compounds isolated from butanol fraction of the methanol extract of the dried powdered leaves of Aspilia africana through repeated silica gel column-chromatography and sephadex gel filtration, were evaluated for anti-microbial potentials using Agar-well diffusion method. Results: The isolated compounds identified as oleanolic acid, ursolic acid, and corosolic acid by 1D, 2D-NMR and FITR spectroscopic analyses inhibited the growth of all the pathogens with inhibition diameters ranging between 25 – 33 mm compared with the standard drugs used. The MIC, MBC/MFC of the plant extracts ranged from between 5.00 and 10.00 mg/mL while that of the isolated compounds ranged between 0.0125 and 0.0500mg/mL Discussion: From the results, we conclude that isolated compounds namely oleanolic acid, ursolic acid and corosolic acid are the bioactive constituents responsible for the anti-microbial activity of Aspilia africana. Key words: Aspilia africana, Anti-microbial, Oleanolic acid, Ursolic acid, Corosolic aci

Effect of Methanol Leaf Extract of Nauclea latifolia on Albino Mice Infected with Plasmodium berghei berghei

Background: In Nigeria the leaf decoction of Nauclea latifolia is taken to treat malaria and sexually transmitted diseases. This study intends to generate a scientific data in support of the traditional use of the leaves in malaria treatment. Objective: To investigate the antiplasmodial effect of the methanol extract of the leaves of Nauclea latifolia on chloroquine sensitive Plasmodium berghei berghei in  experimentally infected albino mice. Materials and Methods: The fresh leaves of Nauclea latifolia were collected, dried under shade, ground into powder and macerated in methanol for 72 hrs. The dried extract was stored at -4 °C for use. Thirty (30) mice were divided into five groups (A,B,C,D,E). Group A received 10 ml/kg/day of distilled water (negative control). Groups B, C and D received 370, 740 and 1110 mg/kg/day of the extract respectively. Group E received 1.2 mg/kg/day of artesunate (positive control). This experiment was repeated for suppressive, prophylactic and curative tests. Results: The extract produced considerable antiplasmodial activity in all the three tests evaluated compared to the standard drug (artesunate). The extract reduced parasitaemia significantly (p<0.05) in a dose dependent manner. Bioactive constituents of the plant could be responsible for the antiplasmodial activity Conclusion: The result of the study supports the need for continued search for components of traditional medicine as potential antimalarial agents. Keywords: Malaria, Nauclea latifolia, mice, Plasmodium berghei berghe

Betulin, a Newly Characterized Compound in Acacia auriculiformis Bark, Is a Multi-Target Protein Kinase Inhibitor

International audienceThe purpose of this work is to investigate the protein kinase inhibitory activity of constituents from stem bark. Column chromatography and NMR spectroscopy were used to purify and characterize betulin from an ethyl acetate soluble fraction of acacia bark. Betulin, a known inducer of apoptosis, was screened against a panel of 16 disease-related protein kinases. Betulin was shown to inhibit Abelson murine leukemia viral oncogene homolog 1 (ABL1) kinase, casein kinase 1ε (CK1ε), glycogen synthase kinase 3α/β (GSK-3 α/β), Janus kinase 3 (JAK3), NIMA Related Kinase 6 (NEK6), and vascular endothelial growth factor receptor 2 kinase (VEGFR2) with activities in the micromolar range for each. The effect of betulin on the cell viability of doxorubicin-resistant K562R chronic myelogenous leukemia cells was then verified to investigate its putative use as an anti-cancer compound. Betulin was shown to modulate the mitogen-activated protein (MAP) kinase pathway, with activity similar to that of imatinib mesylate, a known ABL1 kinase inhibitor. The interaction of betulin and ABL1 was studied by molecular docking, revealing an interaction of the inhibitor with the ABL1 ATP binding pocket. Together, these data demonstrate that betulin is a multi-target inhibitor of protein kinases, an activity that can contribute to the anticancer properties of the natural compound and to potential treatments for leukemia