Two new peltogynoids, acanilol A (1) and acanilol B (2), were isolated from the stem bark of Acacia nilotica (L.) Delile, together with the known triterpene lupenone. The structures of the new compounds were established on the basis of their spectral data, mainly UV, NMR, and mass spectrometry. The new compounds were tested as kinase inhibitors against CDK1, GSK3, CK1, and DYRK1A, and acanilol B was identified as a DYRK1A inhibitor, with an IC₅₀ of 19 µM.

Phytochemical and Antisickling Studies of the Leaves of Hymenocardia acida Tul (Euphorbiaceae)

The leaves of the plants Daniellia oliveri (Fabaceae) and Ficus sycomorus (Moraceae) used in diarrhea treatment in Hausa ethnomedicine of Northern Nigeria were investigated. The study was carried out on parfused isolated rabbit jejunum and castor oil-induced diarrhea in mice. The n-butanol extracts: NBD and NBF (0.16- 3.2mg/ml) caused a dose-dependent relaxation of isolated rabbit jejunum. The acute toxicity test for NBD and NBT in mice established an i.p LD50 of > 4000mg/kg for D. oliveri and 1131.4mg/kg for F. sycomorus . In castor oilinduced diarrhea, 80% protection was observed for D. oliveri at doses of 200mg/kg and 60% protection was observed at 100mg/kg and 50mg/kg respectively. For F. sycomorus 100% protection was observed at doses of 120mg/kg and 60mg/kg, for the n-butanol extract. The antidiarrheal activity was comparable to loperamide 5mg/kg. The result revealed that the extracts have pharmacological activity against diarrhea. Keywords: Anti-diarrhea,castor oil,n-butanol extracts,tissue relaxation.African Journal of Traditional and Complementary Medicine Vol. 4 (4) 2007: pp. 524-528

Flavonoid glycosides from Byrsocarpus coccineus leaves. Schum and Thonn (Connaraceae)

The purpose of this work is to investigate the protein kinase inhibitory activity of constituents from Acacia auriculiformis 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.