Phytochemical and biological investigations of Elaeodendron schlechteranum.
OBJECTIVE
Elaeodendron schlechteranum (Loes.) Loes. is a shrub or tree belonging to the family Celastraceae. In Tanzania, in addition to ethnopharmacological claims in treating various non-infectious diseases, the root and stem bark powder is applied on septic wounds, and the leaf paste is used for treatment of boils and carbuncles. The aim of this study was to identify the putative active constituents of the plant.


METHODS
Dried and powdered root bark was extracted and subjected to bioassay-guided fractionation, based on antibacterial, antiparasitic and anti-HIV activity. Isolated compounds were identified by spectroscopic methods, and evaluated for biological activity.


CONCLUSIONS
Bioassay-guided isolation led to the identification of tingenin B (22beta-hydroxytingenone) as the main antibacterial constituent. It was active against Bacillus cereus, Staphylococcus aureus and Escherichia coli (IC(50)<0.25 microg/mL). Furthermore, antiparasitic activity was observed against Trypanosoma cruzi (IC(50)<0.25 microg/mL), Trypanosoma brucei (<0.25 microg/mL), Leishmania infantum (0.51 microg/mL), and Plasmodium falciparum (0.36 microg/mL). Tingenin B was highly cytotoxic to MRC-5 cells (CC(50) 0.45 microg/mL), indicating a poor selectivity. Two inactive triterpenes, 3beta,29-dihydroxyglutin-5-ene and cangoronine methyl ester were also obtained. Phytochemical investigation of the anti-HIV active fractions led to the isolation and identification of three phenolic compounds, namely 4'-O-methylepigallocatechin, 4'-O-methylgallocatechin, and a new procyanidin dimer, i.e. 4',4'''-di-O-methyl-prodelphinidin B(4) or 4'-O-methylgallocatechin-(4alpha-->8)-4'-O-methylepigallocatechin. However, none of these showed anti-HIV activity.
Maregesi
Sheila M
SM
Department of Pharmaceutical Sciences, Faculty of Pharmaceutical, Biomedical and Veterinary Sciences, University of Antwerp, Antwerpen, Belgium.
Hermans
Nina
N
Dhooghe
Liene
L
Cimanga
Kanyanga
K
Ferreira
Daneel
D
Pannecouque
Christophe
C
Vanden Berghe
Dirk A
DA
Cos
Paul
P
Maes
Louis
L
Vlietinck
Arnold J
AJ
Apers
Sandra
S
Pieters
Luc
L
D000900:Anti-Bacterial Agents / Q000009:adverse effects / Q000302:isolation & purification / Q000494:pharmacology*; D019380:Anti-HIV Agents / Q000009:adverse effects / Q000302:isolation & purification / Q000494:pharmacology*; D000977:Antiparasitic Agents / Q000009:adverse effects / Q000302:isolation & purification / Q000494:pharmacology*; D029753:Celastraceae / Q000737:chemistry*; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D005347:Fibroblasts / Q000187:drug effects; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D021261:Parasitic Sensitivity Tests; D024301:Plant Bark / Q000737:chemistry; D010936:Plant Extracts / Q000009:adverse effects / Q000302:isolation & purification / Q000494:pharmacology*; D018517:Plant Roots / Q000737:chemistry
D000900:Anti-Bacterial Agents; D019380:Anti-HIV Agents; D000977:Antiparasitic Agents; D010936:Plant Extracts