Learn More
The trypanocidal activity of naturally occurring 6-(3,4-dihydroxystyryl)-4-hydroxy-2-pyrone (hispidin) prompted us to examine its cytotoxic activity toward normal and cancerous cells in culture. Hispidin synthesized in our laboratory to a high degree of purity (checked by 1H and 13C NMR spectroscopy) was shown to be cytotoxic (between 10-3 mol/L and 10-7(More)
In humans, there are four alkaline phosphatases, and each form exibits a characteristic pattern of tissue distribution. The availability of an easy method to reveal their activity has resulted in large amount of data reporting correlations between variations in activity and illnesses. For example, alkaline phosphatase from neutrophils of mothers pregnent(More)
This work deals with the phosphofructokinase enzyme (PFK) of the parasite Trypanosoma brucei. Inhibitors which are analogues of fructose-6-phosphate (F6P) derived from 2,5-anhydromannitol and therefore blocked in a closed conformation, both nonphosphorylated and phosphorylated, were designed. They provided information on this class of ATP-dependent PFK(More)
We report here the first crystal structure of a stable isosteric analogue of 1,3-bisphospho-d-glyceric acid (1,3-BPGA) bound to the catalytic domain of Trypanosoma cruzi glycosomal glyceraldehyde-3-phosphate dehydrogenase (gGAPDH) in which the two phosphoryl moieties interact with Arg249. This complex possibly illustrates a step of the catalytic process by(More)
In continuation of our study on medicinal plants of Cameroon, stem barks of Polyalthia suaveolens were phytochemically studied. This investigation yielded a new indolosesquiterpene alkaloid, named polysin (1) and four hitherto known alkaloids (2-5). Polysin (1) appeared as a competitive reversible inhibitor (K(i)=10 microM) of phosphofructo kinase (PFK) of(More)
A new kolavic acid derivative known from spectroscopic analyses as monomethyl ester-15-kolavic acid was isolated from the stem bark of Entada abyssinica, a plant traditionally used in West and East Africa for the management of sleeping sickness. The new derivative showed a strong and selective inhibitory activity on the GAPDH enzyme of Trypanosoma brucei(More)
The presence of bergenin in substantial amounts in the methanol leaves extract of Flueggea virosa (Euphorbiaceae) was established as a strong chemotaxomic point of differentiation between Flueggea virosa and Securinega virosa. Bergenin showed an inhibitory effect on the growth of the bloodstream form of Trypanosoma brucei with an IC50 value of 1 microM.
Polycarpol, sitosterol and sitosterol-3-O-beta-D-glucoside isolated for the first time from Piptostigma preussi (Annonaceae) occur regularly in some Annonaceae such as Piptostigma genus. Polycarpol exhibits interesting antitrypanosomal activity with an ED(50) value of 5.11 microM on Trypanosoma brucei cells. Moreover, it inhibits T. brucei glycolytic(More)
Phytochemical study of the stem bark of Enantia chlorantha resulted in the isolation of two protoberberines 1 and 2. These alkaloids as well as commercially available berberine were modified chemically and tested in vitro against Typanosoma brucei proliferation as well as on three targeted glycolytic enzymes. The inhibitory activities observed were in the(More)
In the search for new antiparasitic natural compounds from the medicinal plants from Cameroon, the new 22-hydroxyclerosterol, established as such on the basis of detailed chemical and spectroscopic analysis, was isolated from the hexane extract of the stem bark of Allexis cauliflora together with the known clerosterol. 22-Hydroxyclerosterol inhibited the(More)