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1.  New Antimalarial Hits from Dacryodes edulis (Burseraceae) - Part I: Isolation, In Vitro Activity, In Silico “drug-likeness” and Pharmacokinetic Profiles 
PLoS ONE  2013;8(11):e79544.
The aims of the present study were to identify the compounds responsible for the anti-malarial activity of Dacryoedes edulis (Burseraceae) and to investigate their suitability as leads for the treatment of drug resistant malaria. Five compounds were isolated from ethyl acetate and hexane extracts of D. edulis stem bark and tested against 3D7 (chloroquine-susceptible) and Dd2 (multidrug-resistant) strains of Plasmodium falciparum, using the parasite lactate dehydrogenase method. Cytotoxicity studies were carried out on LLC-MK2 monkey kidney epithelial cell-line. In silico analysis was conducted by calculating molecular descriptors using the MOE software running on a Linux workstation. The “drug-likeness” of the isolated compounds was assessed using Lipinski criteria, from computed molecular properties of the geometry optimized structures. Computed descriptors often used to predict absorption, distribution, metabolism, elimination and toxicity (ADMET) were used to assess the pharmacokinetic profiles of the isolated compounds. Antiplasmodial activity was demonstrated for the first time in five major natural products previously identified in D. edulis, but not tested against malaria parasites. The most active compound identified was termed DES4. It had IC50 values of 0.37 and 0.55 µg/mL, against 3D7 and Dd2 respectively. In addition, this compound was shown to act in synergy with quinine, satisfied all criteria of “Drug-likeness” and showed considerable probability of providing an antimalarial lead. The remaining four compounds also showed antiplasmodial activity, but were less effective than DES4. None of the tested compounds was cytotoxicity against LLC-MK2 cells, suggesting their selective activities on malaria parasites. Based on the high in vitro activity, low toxicity and predicted “Drug-likeness” DES4 merits further investigation as a possible drug lead for the treatment of malaria.
doi:10.1371/journal.pone.0079544
PMCID: PMC3836662  PMID: 24282507
2.  Isolation and identification of an antiparasitic triterpenoid estersaponin from the stem bark of Pittosporum mannii (Pittosporaceae) 
Objective
To screen for antiparasitic properties of Pittosporum mannii Hook (Pittosporaceae) through in vitro bioassay tests and to identify the bioactive compound(s).
Methods
The stem bark of Pittosporum mannii was harvested in Bali Nyonga in January 2007. The CH2Cl2 and MeOH extracts were tested in vitro for antiparasitic activity. NF54 (an airport strain of unknown origin and sensitive to all known drugs) and K1 (a clone originating from Thailand and resistant to chloroquine/pyrimethamine) strains were used for the antiplasmodial screening while Leishmania donovani MHOM-ET-67/L82 was used for antileishmanial testing. 1H and 13C NMR spectra were recorded on a Bruker AMX-500 spectrometer using CDCl3 as solvent. EIMS were recorded on a double-focusing mass spectrometer (Varian MAT 311A) while HREIMS were recorded on a JEOL HX 110 mass spectrometer.
Results
The MeOH extract was active on both the chloroquine-resistant (K1) strain (IC50=4.3 µg/mL) and on the macrophages of Leishmania donovani (IC50=8.6 µg/mL). The CH2Cl2 extract was considered inactive on both parasites (IC50>5.0 µg/mL and 21.7 µg/mL respectively). Compound 1, a constituent that precipitated from the MeOH extract, showed pronounced activity on both Plasmodium falciparum and Leishmania donovani parasites (IC50=1.02 and 1.80 µg/mL respectively) with artemisinin and miltefosine included as reference drugs. Its structure was identified as 1-O-[apha-L-(Rhamnopyranosyl]-23-acetoxyimberbic acid 29-methyl ester, a pentacyclic triterpenoid estersaponin.
Conclusions
The present study constitutes the first report on the antiparasitic activity of this plant and provides some support for the traditional use of the plant in the treatment of malaria. The plant has therefore been identified as a potential source for the discovery of antiparasitic lead compounds.
doi:10.1016/S2222-1808(13)60089-4
PMCID: PMC4027329
Phytochemical; Pittosporum; Antiplasmodial; Triterpenoid; Saponins
3.  Bioassay-guided discovery of antibacterial agents: in vitro screening of Peperomia vulcanica, Peperomia fernandopoioana and Scleria striatinux 
Background
The global burden of bacterial infections is high and has been further aggravated by increasing resistance to antibiotics. In the search for novel antibacterials, three medicinal plants: Peperomia vulcanica, Peperomia fernandopoioana (Piperaceae) and Scleria striatinux (Cyperaceae), were investigated for antibacterial activity and toxicity.
Methods
Crude extracts of these plants were tested by the disc diffusion method against six bacterial test organisms followed by bio-assay guided fractionation, isolation and testing of pure compounds. The minimum inhibitory (MIC) and minimum bactericidal (MBC) concentrations were measured by the microdilution method. The acute toxicity of the active extracts and cytotoxicity of the active compound were performed in mice and mammalian cells, respectively.
Results
The diameter of the zones of inhibition (DZI) of the extracts ranged from 7–13 mm on Escherichia coli and Staphylococcus aureus of which the methylene chloride:methanol [1:1] extract of Scleria striatinux recorded the highest activity (DZI = 13 mm). Twenty-nine pure compounds were screened and one, Okundoperoxide, isolated from S. striatinux, recorded a DZI ranging from 10–19 mm on S. aureus. The MICs and MBCs indicated that the Peperomias had broad-spectrum bacteriostatic activity. Toxicity tests showed that Okundoperoxide may have a low risk of toxicity with an LC50 of 46.88 μg/mL.
Conclusions
The antibacterial activity of these plants supports their use in traditional medicine. The pure compound, Okundoperoxide, may yield new antibacterial lead compounds following medicinal chemistry exploration.
doi:10.1186/1476-0711-11-10
PMCID: PMC3403929  PMID: 22549052
Resistance; Medicinal plants; Antibacterial compound; Toxicity
4.  Hypericum lanceolatum (Hypericaceae) as a potential source of new anti-malarial agents: a bioassay-guided fractionation of the stem bark 
Malaria Journal  2011;10:167.
Background
Malaria is a major public health threat in Africa, and traditional medicine continues to play a key role in its control especially in rural areas. A bioassay-guided fractionation was carried out in order to evaluate the anti-malarial potential and the safety of the methanol extract of the Hypericum lanceolatum stem bark.
Methods
The anti-plasmodial activity was assayed by the lactate dehydrogenase method (pLDH) against the multidrug-resistant W2mef laboratory strain, and a field isolate (SHF4) of Plasmodium falciparum. Cytotoxicity tests were carried out using the LLC-MK2 monkey kidney epithelial cells.
Results
Five compounds were isolated from the most active and least cytotoxic ethylacetate sub-extract: betulinic acid (HLT1), 2,2',5,6'-tetrahydroxybenzophenone (HLT2), 5-hydroxy-3-methoxyxanthone (HLT3), 3-hydroxy-5-methoxyxanthone (HLT4) and HLT0 (yet to be identified). Three of the tested compounds presented significant anti-plasmodial activities (with 50% inhibitory concentration, IC50 < 5 μM), with 5-hydroxy-3-methoxyxanthone exerting the highest activity, followed by HLT0 and betulinic acid. All the compounds with significant anti-plasmodial activity were non-cytotoxic, except betulinic acid which showed a 50% cytotoxic concentration, CC50 of 25 μg/mL.
Conclusions
These findings justify the use of H. lanceolatum stem bark as anti-malarial by traditional healers of Western Cameroon, and could constitute a good basis for further studies towards development of new drug candidates or phytomedicines for malaria.
doi:10.1186/1475-2875-10-167
PMCID: PMC3131257  PMID: 21682873
5.  In Vitro Antiplasmodial Activity and Cytotoxicity of Extracts of Selected Medicinal Plants Used by Traditional Healers of Western Cameroon 
Malaria Research and Treatment  2011;2011:561342.
Medicinal plants play a key role in malaria control in Africa, especially in remote areas where health facilities are limited. In order to assess their acclaimed potentials, eleven extracts were prepared from seven selected plants commonly used in Western Cameroon, and tested both for their antiplasmodial activity and cytotoxicity. The antiplasmodial activity was assessed using Lactate Dehydrogenase Assay (pLDH) and the cytotoxicity estimated on LLC-MK2 monkey kidney epithelial cells. Seven extracts from five different plants were significantly active, with very weak or no cytotoxicity. The Dacryodes edulis leaves showed the highest activity (IC50 of 6.45 μg/mL on 3D7 and 8.2 μg/mL on DD2) followed by the leaves of Vernonia amygdalina (IC50 of 8.72 and 11.27 μg/mL on 3D7 and DD2 resp.) and roots of V. amygdalina (IC50 of 8.72 μg/mL on 3D7), Coula edulis leaves (IC50 of 13.80 μg/mL and 5.79 μg/mL on 3D7 and DD2 resp.), Eucalyptus globulus leaves (IC50 of 16.80 μg/mL and 26.45 μg/mL on 3D7 and DD2) and Cuviera longiflora stem bark (IC50 of 20.24 μg/mL and 13.91 μg/mL on 3D7 and DD2). These findings justify the use of five of the seven plants in malaria treatment by traditional healers of Western Cameroon.
doi:10.4061/2011/561342
PMCID: PMC3265286  PMID: 22312569
6.  Selective activity of extracts of Margaritaria discoidea and Homalium africanum on Onchocerca ochengi 
Background
The current treatment of onchocerciasis relies on the use of ivermectin which is only microfilaricidal and for which resistant parasite strains of veterinary importance are increasingly being detected. In the search for novel filaricides and alternative medicines, we investigated the selective activity of crude extracts of Margaritaria discoidea and Homalium africanum on Onchocerca ochengi, a model parasite for O. volvulus. These plants are used to treat the disease in North West Cameroon.
Methods
Sixteen crude extracts were prepared from various parts of M. discoidea and H. africanum using different organic solvents. The filaricidal activities were determined in vitro. Cytotoxicity of the active extracts was assessed on monkey kidney epithelial cells in vitro and the selectivity indices (SI) of the extracts determined. Acute toxicity of the promising extracts was investigated in mice.
Results
Four out of the 16 extracts showed microfilaricidal activity based on motility reduction, whereas, none showed macrofilaricidal activity based on the MTT/formazan assay. The methylene chloride extract of H. africanum leaves (HLC) recorded the lowest IC50 of 31.25 μg/mL and an IC100 of 62.5 μg/mL. The SI for the active extracts ranged from 0.5 - 2.63. No form of acute toxicity was observed in mice. Phytochemical analysis revealed the presence of anthraquinones, sterols and terpenoids in the promising extracts.
Conclusions
The non-polar extracts of M. discoidea and H. africanum are potential sources of new microfilaricidal lead compounds, and the results support their use in traditional medicine.
doi:10.1186/1472-6882-10-62
PMCID: PMC2987330  PMID: 21029456
7.  The Antimalarial Potential of Medicinal Plants Used for the Treatment of Malaria in Cameroonian Folk Medicine 
Malaria remains one of the leading public health problems in Cameroon as in other parts of Sub-Saharan Africa. In the past decades, this situation has been aggravated by the increasing spread of drug-resistant Plasmodium falciparum strains. New antimalarial drug leads are therefore urgently needed. Traditional healers have long used plants to prevent or cure infections. This article reviews the current status of botanical screening efforts in Cameroon as well as experimental studies done on antimalarial plants. Data collected from 54 references from various research groups in the literature up to June 2007 shows that 217 different species have been cited for their use as antimalarials in folk medicine in Cameroon. About a hundred phytochemicals have been isolated from 26 species some among which are potential leads for development of new antiamalarials. Crude extracts and or essential oils prepared from 54 other species showed a wide range of activity on Plasmodium spp. Moreover, some 137 plants from 48 families that are employed by traditional healers remain uninvestigated for their presumed antimalarial properties. The present study shows that Cameroonian flora represents a high potential for new antimalarial compounds. Further ethnobotanical surveys and laboratory investigations are needed to fully exploit the potential of the identified species in the control of malaria.
PMCID: PMC2816552  PMID: 20161952

Results 1-7 (7)