Etienne Tsamo

In vitro antimicrobial activity of extracts and compounds of some selected medicinal plants from Cameroon

AIM OF THE STUDY Seven extracts and eight compounds from four selected Cameroonian medicinal plants, Solanecio mannii Hook f. (Asteraceae), Monodora myristica Dunal (Annonaceae), Albizia gummifera (J.F. Gmel) C.A. Smith (Fabaceae/Mimosoideae) and Glyphaea brevis (Spreng) Monachino (Tiliaceae), traditionally used for the treatment of hepatitis, parasites and other infectious diseases, were tested in vitro for their antimicrobial activity against Gram-positive (5 species) and Gram-negative (4 species) bacteria species and pathogenic yeasts (2 Candida species), to establish whether or not they have antimicrobial activity and to validate scientifically their use in traditional medicine. MATERIALS AND METHODS The agar disc diffusion and the microbroth dilution methods were used to determine the zone of inhibition between the edge of the filter paper and the edge of the inhibition area (IZ) and the minimal inhibitory concentration (MIC) respectively. RESULTS The most active extracts against Candida albicans and Candida krusei were respectively the cyclohexane extract from the fruits of Monodora myristica and the ethyl acetate extract from the stem bark of Albizia gummifera (MIC=6.3 microg/ml for both extracts). The lowest MIC value (1.6 microg/ml) for purified compounds was obtained on Candida albicans with a mixture of linear aliphatic primary alcohols (n-C24H50O to n-C30H62O), with n-hexacosanol (1b) as major compound and mixture of fatty acid esters of diunsaturated linear 1,2-diols (6). CONCLUSION These results afford ground informations for the potential use of the crude extracts of these species as well as of some of the isolated compounds in bacterial and fungal infections.

Leishmanicidal and Cholinesterase Inhibiting Activities of Phenolic Compounds from Allanblackia monticola and Symphonia globulifera

In a preliminary antiprotozoal screening of several Clusiaceae species, the methanolic extracts of Allanblackia monticola and Symphonia globulifera showed high in vitro leishmanicidal activity. Further bioguided phytochemical investigation led to the isolation of four benzophenones: guttiferone A (1), garcinol (2), cambogin (3) and guttiferone F (4), along with three xanthones: allanxanthone A (5), xanthone V1 (6) and globulixanthone C (7) as active constituents. Compounds 1 and 6 were isolated from S. globulifera leaves, while compounds 2-5 were obtained from A. monticola fruits. Guttiferone A (1) and F (4) showed particulary strong leishmanicidal activity in vitro, with IC50 values (0.2 microM and 0.16 microM, respectively) comparable to that of the reference compound, miltefosine (0.46 microM). Although the leishmanicidal activity is promising, the cytotoxicity profile of these compounds prevent at this state further in vivo biological evaluation. In addition, all the isolated compounds were tested in vitro for their anticholinesterase properties. The four benzophenones showed potent anticholinesterase properties towards acetylcholinesterase (AChE) and butylcholinesterase (AChE). For AChE, the IC50 value (0.66 microM) of garcinol (2) was almost equal to that of the reference compound galanthamine (0.50 microM). Furthermore, guttiferone A (1) and guttiferone F (4) (IC50 = 2.77 and 3.50 microM, respectively) were more active than galanthamine (IC50 = 8.5) against BChE.

Cytotoxic and antiplasmodial xanthones from Pentadesma butyracea.

Four new xanthones, butyraxanthones A-D (1-4), were isolated from the stem bark of Pentadesma butyracea, together with six known xanthones (5-10) and a triterpenoid (lupeol). The structures of 1-4 were established by spectroscopic methods. Compounds 1-10 were tested in vitro for antiplasmodial activity against a Plasmodium falciparum chloroquine-resistant strain and for cytotoxicity against a human breast cancer cell line (MCF-7). Nearly all of these xanthones exhibited good antiplasmodial activity, and some of them also demonstrated potent cytotoxicity.

Bioactive Constituents of the Stem Bark of Beilschmiedia zenkeri

Phytochemical investigation of the stem bark of Beilschmiedia zenkeri led to the isolation of four new methoxylated flavonoid derivatives, (2S,4R)-5,6,7-trimethoxyflavan-4-ol (1), (2S,4R)-4,5,6,7-tetramethoxyflavan (2), beilschmieflavonoid A (3), and beilschmieflavonoid B (4), together with seven known compounds. The structures of 1-4 were established by spectroscopic methods, and their relative configurations confirmed by X-ray crystallographic and CD analysis. The isolated compounds were evaluated in vitro for their antibacterial activity against three strains of bacteria, Pseudomonas agarici, Bacillus subtilis, and Streptococcus minor, and for their antiplasmodial activity against Plasmodium falciparum, chloroquine-resistant strain W2.

Antiplasmodial activity of extracts from seven medicinal plants used in malaria treatment in Cameroon

AIM OF THE STUDY In a search for new plant-derived biologically active compounds against malaria parasites, we have carried out an ethnopharmacological study to evaluate the susceptibility of cultured Plasmodium falciparum to extracts and fractions from seven Cameroonian medicinal plants used in malaria treatment. We have also explored the inhibition of the Plasmodium falciparum cysteine protease Falcipain-2. MATERIALS AND METHODS Plant materials were extracted by maceration in organic solvents, and subsequently partitioned or fractionated to afford test fractions. The susceptibility of erythrocytes and the W2 strain of Plasmodium falciparum to plant extracts was evaluated in culture. In addition, the ability of annonaceous extracts to inhibit recombinant cysteine protease Falcipain-2 was also assessed. RESULTS AND DISCUSSION The extracts showed no toxicity against erythrocytes. The majority of plant extracts were highly active against Plasmodium falciparumin vitro, with IC(50) values lower than 5 microg/ml. Annonaceous extracts (acetogenin-rich fractions and interface precipitates) exhibited the highest potency. Some of these extracts exhibited modest inhibition of Falcipain-2. CONCLUSION These results support continued investigation of components of traditional medicines as potential new antimalarial agents.

Prenylated Xanthones as Potential P-Glycoprotein Modulators

Dimethylallyl (DMA) derivatives of a naturally occurring xanthone (decussatin 1) were prepared. Their activity as potential P-glycoprotein inhibitors was monitored by affinity of direct binding and compared to that of corresponding DMA-flavones. Both classes of compounds exhibited the same structure-activity relationships. Decreasing polarity enhanced the binding affinity for the P-glycoprotein C-terminal cytosolic domain since DMA derivatives were more active, but unsubstituted hydroxyl group close to the carbonyl was required for efficient activity.

Spathodic acid: A triterpene acid from the stem bark of Spathodea campanulata

Abstract A new triterpene acid, spathodic acid and the sistosterol-3- O -β- d -glucopyranoside were isolated from the stem bark of Spathodea campanulata . The structure of the new compound was established by chemical and spectral analysis.

Entilins A and B, two novel heptanortriterpenoid derivatives from entandrophragma utile (meliaceae): Structural elucidation using 2d nmr long-range δC/δH correlation experiments

Entilin A and its 2-acetate, entilin B, isolated from the stem bark of Entandrophragma utile have been assigned structures 1 and 2 mainly by using deductive arguments to interpret 2D NMR long-range δC/δH correlation experiments.

Spathoside, a cerebroside and other antibacterial constituents of the stem bark of Spathodea campanulata.

Spathoside, a new cerebroside was isolated from the stem bark of Spathodea campanulata, besides known compounds (n-alkanes, linear aliphatic alcohols, sitosterol and their esters, β-sitosterol-3-O-β-D-glucopyranoside, oleanolic acid, pomolic acid, p-hydroxybenzoic acid and phenylethanol esters). The structures of the isolated compounds were established by spectroscopic studies. The antibacterial activity of the isolated compounds against a wide range of microorganisms was examined. They inhibited significantly the growth of some gram-positive and -negative bacteria.

Potent antiplasmodial extracts from Cameroonian Annonaceae

AIM OF THE STUDY In a search for new antimalarial leads, we have carried out a preliminary ethnopharmacological study with the aim of evaluating the in vitro antiplasmodial activity of extracts from thirteen Annonaceae species growing in Cameroon, and of assessing the acute toxicity of promising fractions in Swiss albino mice. MATERIALS AND METHODS Plants were selected on the basis of an ethnobotanical survey carried out in four sites in centre and south regions of Cameroon (Yaoundé neighbourhoods, Kon-Yambetta, Ngobayang and Mbalmayo) on Annonaceae plants locally used to treat malaria and related symptoms. The choice of the sites was mainly based on environmental factors enabling mosquito breeding, cosmopolitan areas regrouping people from different cultural origins, areas with limited access to health centers, and areas with people relying exclusively on traditional medical practices. Collected materials were extracted by maceration in 95% ethanol. The crude extract was partitioned using organic solvents and the fractions afforded were evaluated for antiplasmodial activity in culture against the W2 strain of Plasmodium falciparum. Promising fractions (methanol fractions) were assessed for their acute toxicity in Swiss albino mice. RESULTS From the results achieved, 37 (31.3%) out of 118 extracts tested exhibited antiplasmodial activity, with IC(50) values ranging from 1.07 μg/ml to 9.03 μg/ml. Of the active extracts, 29 (78.4%) were methanol fractions, 21 (72.4%) of which inhibited the parasites with IC(50)<5 μg/ml. The promising fractions proved to be safe through oral administration in mice. CONCLUSIONS The activities and toxicity profiles of methanol fractions indicate that they deserve to be further investigated in detail for antimalarial lead discovery.