Antiplasmodial Properties and Cytotoxicity of Endophytic Fungi from Symphonia globulifera (Clusiaceae)

Ateba JET, Toghueo RMK, Awantu AF, et al. Antiplasmodial Properties and Cytotoxicity of Endophytic Fungi from Symphonia globulifera (Clusiaceae). JOURNAL OF FUNGI. 2018;4(2): UNSP 70.There is continuing need for new and improved drugs to tackle malaria, which remains a major public health problem, especially in tropical and subtropical regions of the world. Natural products represent credible sources of new antiplasmodial agents for antimalarial drug development. Endophytes that widely colonize healthy tissues of plants have been shown to synthesize a great variety of secondary metabolites that might possess antiplasmodial benefits. The present study was carried out to evaluate the antiplasmodial potential of extracts from endophytic fungi isolated from Symphonia globulifera against a chloroquine-resistant strain of Plasmodium falciparum (PfINDO). Sixty-one fungal isolates with infection frequency of 67.77% were obtained from the bark of S. globulifera. Twelve selected isolates were classified into six different genera including Fusarium, Paecilomyces, Penicillium, Aspergillus, Mucor, and Bipolaris. Extracts from the 12 isolates were tested against PfINDO, and nine showed good activity (IC50 < 10 mu g.mL(-1)) with three fungi including Paecilomyces lilacinus (IC50 = 0.44 mu g.mL(-1)), Penicillium janthinellum (IC50 = 0.2 mu g.mL(-1)), and Paecilomyces sp. (IC50 = 0.55 mu g.mL(-1)) showing the highest promise. These three isolates were found to be less cytotoxic against the HEK293T cell line with selectivity indices ranging from 24.52 to 70.56. Results from this study indicate that endophytic fungi from Symphonia globulifera are promising sources of hit compounds that might be further investigated as novel drugs against malaria. The chemical investigation of active extracts is ongoing

Antiplasmodial and cytotoxic activities of flavonoids and arylbenzofuran derivatives from Morus mesozygia

Morus mesozygia Stapf (Moraceae) is a plant found in many regions and used in treating many diseases including malaria and fever. Fractionation of the methanolic extract of its stem bark, using various chromatographic methods has led to the isolation and identification of 3 flavonoids: artocarpesin, artochamin C and kushenol E. And 4 arylbenzofuran derivatives: moracin M, moracin C, moracin L and mulberofuran F. The methanolic extract and the seven isolated compounds were tested for antiplasmodial activity against the chloroquine-resistant FcB1 Plasmodium falciparum strain and cytotoxicity on MCF-7 human breast cancer cells. Relating to the antiplasmodial activity, it was found that all compounds were active against the FcB1 strain of Plasmodium with artocarpesin, koushenol E and mulberrofuran F showing particular potency (with the median inhibitory concentrations IC50 = 2.5-2.6 μg/ml). Cytotoxicity tests performed on MCF-7 cells revealed all the IC50 varying from &lt;1.0 to 5.0 ± 0.6 μg/mL. A structure – activity relationship is discussed

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

The antiplasmodial agents of the stem bark of Entandrophragma angolense (Meliaceae).

In the search of active principles from the stem bark of Entandrophragma angolense, we submitted the compounds isolated from the dichloromethane – methanol (1:1) extract of the stem bark to antimalarial test against chloroquine resistant strain W2 of Plasmodium falciparum malaria parasite. Only 7&#945;-obacunyl acetate and a cycloartane derivative exhibited a good activity, with IC50s of 2 and 5.4 &#956;g/ml respectively. Other compounds were moderately active. Keywords:Plasmodium falciparum; Meliaceae;Entandrophragma angolense; Limonoids; Fatty acids; Triterpenoids; 7&#945;-obacunyl acetate; 24-methylenecycloartenol; anti-plasmodial activity. African Journal of Traditional, Complementary and Alternative Medicines Vol. 4 (2) 2007: pp. 135-13

Antimalarial activity in crude extracts of some Cameroonian medicinal plants

Fifteen crude extracts from the stem bark and seeds of four medicinal plants, viz: Entandrophragma angolense, Picralima nitida, Schumanniophyton magnificum and Thomandersia hensii were tested in vitro for their antimalarial activity against the chloroquine-resistant Plasmodium falciparum W2 strain. The results showed that the extracts of these plants possessed some antimalarial activity, the methanol extract of Picralima nitida demonstrating the highest activity in vitro. Further isolation and identification of some active compounds from these plants will justify their common use in traditional medicine for the treatment of malaria or fever in Cameroon.Keywords: Entandrophragma angolense; Picralima nitida; Schumanniophyton magnificum; Thomandersia hensii; Plasmodium falciparum; Antimalarial activity The African Journal of Traditional, Complementary and Alternative Medicines Vol. 4 (1) 2007: pp. 107-11

In Vitro anti-malarial activity of limonoids from two meliacious plants

Four limonoids, atomasin A 1, atomasin B 2, entilin A 3 and entilin B 4 from Entandrophragma candollei and Entandrophragma utile (Meliaceae) were tested for in vitro antimalarial activity against Plasmodium falciparum chloroquine–resistant W2 strain. Three limonoids (1, 3, 4) were moderately active with IC50 values between 11.6 and 28.2 µg/mL. atomasin B was devoid of activity. The in vitro activities of the compounds were further analysed using fresh isolates of P. falciparum among which three were chloroquine–resistant. The comparison of the mean IC50 values of atomasin A and entilin B did show any significant difference between chloroquine-resistant and –sensitive isolates. Keywords: Plasmodium falciparum; Antimalarial activity; Meliaceae; Limonoids; Entandrophragma candollei; Entandrophragma utile. West African Journal of Pharmacology and Drug Research Vol. 21 (1&2) 2005: pp. 39-4

Effects of Mondia whitei extracts on the contractile responses of isolated rat vas deferens to potassium chloride and adrenaline

Objective: To investigate the effects of the methylene chloride:methanol (CH2Cl2:MeOH, 1:1) extract of the dried roots of Mondia whitei Linn and its hexane and methanol fractions on potassium chloride (KCl) and adrenaline (Adr)-induced contractions of rat vas deferens. Materials and Methods: Isolated strips of normal adult rat vas deferens were mounted in a Ugo Basile single-organ bath containing Krebs solution. Cumulative concentration-response curves of KCl (1-7 x 10-2 M ) and adrenaline (1.21-8.45 x 10-7 M ) were established in the absence and presence of M. whitei (50-400 μg/ml). In separate experiments, after obtaining a stable plateau of contractions with KCl (60 m M ), M. whitei samples (50-400 μg/ml) were added cumulatively to relax the preparation. In KCl (60 m M ), containing depolarizing medium, cumulative concentration-contraction curve to CaCl2 (2-14 x 10-2 M ) was elicited in the absence and presence of the hexane fraction of M. whitei (50-400 μg/ml). Results: All the M. whitei samples produced rightward shift of the concentration-response curves to KCl and Adr. At high concentration of the plant extracts (400 μg/ml), a decrease of the maximal response to the contractile agents was observed compared with that obtained with the control. All the three extracts produced concentration-dependent relaxation of the plateau of contraction induced by KCl and the hexane fraction appeared to be the more potent. In calcium-free physiological salt solution, the hexane fraction of M. whitei produced rightward shift to the concentration-response curve to CaCl2 and completely abolished the contractile effect of calcium at high concentration (400 μg/ml). Conclusion: It is concluded that M. whitei extracts antagonized the contractile responses to KCl and Adr in isolated rat vas deferens, which could be due to the blockade of voltage-operated calcium channels