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Synthetic hispidin, a PKC inhibitor, is more cytotoxic toward cancer cells than normal cells in vitro
Synthetic hispidin was found to inhibit isoform β of protein kinase C (IC50 of 2 × 10-6 mol/L), but not E. coli and placental type XV alkaline phosphatases. Expand
Exploring the active site of Trypanosoma brucei phosphofructokinase by inhibition studies: specific irreversible inhibition.
This work deals with the phosphofructokinase enzyme (PFK) of the parasite Trypanosoma brucei, offering an opportunity to develop biologically active compounds against the sleeping sickness, the causative agent of which is the trypanosome. Expand
In vitro inhibitory effects of palmatine from Enantia chlorantha on Trypanosoma cruzi and Leishmania infantum
In an attempt to establish the components responsible for the use of Enantia chlorantha against cutaneous leishmaniasis in local traditional medicine, a well-known palmatine has been isolated inExpand
Antitrypanosomal alkaloids from Polyalthia suaveolens (Annonaceae): their effects on three selected glycolytic enzymes of Trypanosoma brucei.
Stem barks of Polyalthia suaveolens were phytochemically studied and yielded a new indolosesquiterpene alkaloid, named polysin, and four hitherto known alkaloids, which exhibited interesting inhibitory effects on selected glycolytic enzymes. Expand
Trypanocidal activity of bergenin, the major constituent of Flueggea virosa, on Trypanosoma brucei.
Bergenin showed an inhibitory effect on the growth of the bloodstream form of Trypanosoma brucei with an IC50 value of 1 microM. Expand
Antitrypanosomal activity of polycarpol from Piptostigma preussi (Annonaceae).
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. PolycarpolExpand
Xylopioxyde and other bioactive kaurane-diterpenes from Xylopia aethiopica Dunal (Annonaceae)
A new cytotoxic ent-kaurane-type diterpene named xylopioxyde has been isolated from the fruits of Xylopia aethiopica Dunal together with three known compounds, namely 15a-acetoxy-ent- kaur-16-en-19 oic acid (xylopic acid) and two new selective trypanocidal stereoisomers. Expand
Crystal structure of Trypanosoma cruzi glyceraldehyde-3-phosphate dehydrogenase complexed with an analogue of 1,3-bisphospho-d-glyceric acid.
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 glycosomalExpand
Inhibition of both Trypanosoma brucei bloodstream form and related glycolytic enzymes by a new kolavic acid derivative isolated from Entada abyssinica.
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 EastExpand
Selective inhibition of Trypanosoma cruzi GAPDH by "bi-substrate" analogues.
A new series of "bi-substrate" analogues have been synthesized as potential inhibitors of the glyceraldehyde-3-phosphate dehydrogenase and one lead compound has been identified that inhibits theExpand