RESUMO
Background: Helminthiasis is endemic in Chad and constitutes a public health problem, particularly among school-age children. The aim of this study was to evaluate the anthelmintic activity of extracts of Khaya anthotheca and Faidherbia albida used in Chad by traditional healers for the treatment of helminthiasis. Methods: The anthelmintic activity was assessed against Heligmosomoides polygyrus and Caenorhabditis elegans larvae using the Worm Microtracker. Embryonated eggs, L1, L2, and L3 larvae of H. polygyrus were obtained after 24 h, 48 h, and 7 days of coproculture and L4 larvae of C. elegans culture using standard procedures. One hundred microliters of extracts at various concentrations, with albendazole and distilled water were, put in contact with 100 µL of H. polygyrus suspension (containing 50 parasites at various developmental stages) in a microplate and incubated for 20 h at 25°C in the Worm Microtracker. The same procedure was adopted for C. elegans, but with 180 µL of OP50. 19 µL of C. elegans suspension (containing 50 larvae) was put in contact with 1 µL of extract at various concentrations and incubated in the Worm Microtracker. Docking studies were carried out using the Schrodinger Maestro software's Glide module. The score function in the software was used to rank and group distinct possible adduct structures generated by molecular docking. Results: The aqueous and ethanolic extracts of F. albida at a concentration of 2.5 mg/mL showed the same activity as albendazole (100 ± 0.00) on hatching. The IC50s of the aqueous extracts of the two plants (IC50: 0.6212 mg/mL and 0.71 mg/mL, respectively) were comparable on egg hatching of H. polygyrus with no significant difference (p ≥ 0.05) with respect to the ethanol extracts (IC50: 0.70 mg/mL and 0.81 mg/mL, respectively). There was no significant difference between the percentage inhibition of extracts and albendazole on the L1 larvae of H. polygyrus (p ≥ 0.05). The aqueous extracts acted more effectively than the ethanol extracts on the L1 larvae of H. polygyrus with an IC50 of 0.5588 and â¼9.858e - 005 mg/ml, respectively, for K. anthotheca and F. albida. The aqueous extracts of K. anthotheca and F. albida on L3 larvae of H. polygyrus had inhibitory percentages of 92.6 ± 0.62 and 91.37 ± 0.8 at 2.5 mg/mL which were lower than albendazole (100 ± 0.00). The aqueous extracts of K. anthotheca and F. albida on C. elegance showed IC50 of 0.2775 µg/mL and 0.5115 µg/mL, respectively, and were more effective than the ethanol extracts. Examining K. anthotheca and F. albida through the interaction with the protein receptor and its results also confirmed our assumption that the compound used has hydroxyl and carbonyl groups as well as aromatic rings and is exposed to phenolic and flavonoid groups in a more specific way, and it shows a better inhibitory effect. Conclusions: This study scientifically validates the use of extracts of the two plants in the traditional treatment of helminthiasis. However, it will be necessary to evaluate the in vivo anthelmintic activity and toxicity. Examining the ADME properties of these compounds also supports the potential of these ligands to be transformed into pharmaceutical forms.
RESUMO
Background: Malaria is the leading cause of morbidity and mortality in African countries. We aimed this study at evaluating the in vitro antiplasmodial, antioxidant, and cytotoxicity activity of Lophira lanceolata extracts. Method: The aqueous and ethanol extracts were obtained by maceration. It tested in vitro the extracts against Plasmodium falciparum 3D7 and multiresistance Dd2. Macrophage cell lines (RAW 264.7 cells) and red blood cells were used for cytotoxicity tests. The antioxidant activity was assessed by 1,1-diphenyl-2-picrylhydrazine (DPPH), hydrogen peroxide (H2O2), nitric oxide (NO) reduction, and ferric reducing antioxidant power (FRAP) scavenging. Results: The in vitro antiplasmodial results showed that the ethanol extract was the most active, with IC50 of 24.51 ± 4.77 µg/mL and 31.86 ± 3.10 µg/mL, respectively, on the resistant Dd2 and sensitive 3D7 strains unlike the aqueous which indicated moderate activity with an IC50 of 51.36 ± 4.86 µg/mL and 56.36 ± 4.27 µg/mL, respectively, on the resistant Dd2 and sensitive (3D7) strains. However, the ethanol extract had the highest activity, with an IC50 of 8.153 g/mL, 1915 g/mL, 30.81 g/mL, and 54.66 g/mL, respectively, for DPPH, H2O2, NO, and FRAP, while the aqueous extract had an IC50 of 6.724, 2387681, 185.7, and 152.0 g/mL, respectively, for DPPH, H2O2, NO, and FRAP. The cytotoxicity test reveals that both extracts do not promote red blood cell haemolysis. They presented weak activity against RAW 264.7 cells and red blood cells. Conclusion: According to these findings, the aqueous and ethanol extracts have antiplasmodial and antioxidant activity but with no cytotoxic effects on red blood cells or RAW cells. However, it will be important to investigate the in vivo antiplasmodial and antioxidant activity of these extracts.
RESUMO
BACKGROUND: One of the most dangerous Plasmodium species is Plasmodium falciparum. Hence, it causes a higher rate of mortality. The resistance of Plasmodium falciparum to the ACT (Artemisinin-based Combination Therapies) has led to the search for new antimalarial drugs. The purpose of this research was to assess the in vivo antiplasmodial activity of Entandrophragma cylindricum ethyl acetate extract to provide a scientific basis for the use of this medicinal plant to treat malaria. METHODS: Entandrophragma cylindricum stem bark powder was macerated in ethyl acetate to obtain the extract. The extract liquid filtrate was concentrated, evaporated and dry using a Rotavapor. The Peter and Rane test were used for the suppressive and curative antiplasmodial activities at different doses (125, 250 and 500 mg/kg). A positive and negative control groups were administered chloroquine (5 mg/kg) and 10% hypromelose, respectively. To assess the parasitemia of the mice a thin blood smear was made. RESULTS: The ethyl acetate extract completely (100%) inhibited the development of P. berghei in the suppressive test at the dose of 500 mg/kg while that of the curative test was inhibited at 95%. The extract-treated group (500 mg/kg) and (Chloroquine (5 mg/kg) group all survived. The negative control group recorded a 100% mortality rate. CONCLUSION: The present study provides scientific confirmation on the use of E. cylindricum stem bark as an antiplasmodial remedy. However, the identification of the mode of action and the purification of the active compounds are necessary for further studies.