Browsing by Author "et al."

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    Antitrypanosomal and Anthelminthic Properties of Ethanol Extracts of Carica papaya Linn. and Ceiba pentandra (L) Gaertn
    (Hindawi, 2022) Obeng, A. W.; Boakye, Y. D.; Boamah, V. E.; Oppong-Kyekyeku,J; Brobbey, A. A.; et al.
    The most common diseases that affect low-income countries are helminthosis and trypanosomosis. In Ghana, and in many other African countries, herbal treatment of various diseases is still common. In the present study, we sought to determine the antitrypanosomal and anthelminthic activities of Carica papaya and Ceiba pentandra. The ethanol extracts of Carica papaya stem bark (PPSe) and leaves (PPLe) and ethanol extracts of Ceiba pentandra stem bark (CPSe) and leaves (CPLe) were screened against Trypanosoma brucei brucei and Pheretima posthuma worms in vitro. CPSe exhibited strong antitrypanosomal activity, while the other extracts exhibited moderate activity against T. b. brucei. All the extracts showed weak selective indices (SI) when tested on Jurkat cell lines, which is indicative of a potential toxic effect. When the extracts were screened against P. posthuma worms, only PPSe and CPSe were able to kill the worms after the exposure time at concentrations of 2.5, 5, and 10 mg/mL. PPSe was again the only extract that potentiated the anthelminthic activity of albendazole against P. posthuma worms. Preliminary phytochemical screening and GC-MS analysis revealed the presence of compounds with antitrypanosomal and anthelminthic properties. The results confirmed the potential of C. papaya and C. pentandra as remedies for trypanosomosis and helminthosis and also gives credence to their folkloric use.
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    Synthesis, molecular docking studies and ADME prediction of some new triazoles as potential antimalarial agents
    (Elsevier, 2021-11) Brobbey, A.; Addotey, J. N.; Danquah, C. A.; et al.
    The challenges concerning the control of malaria remain due to the continuous emergence of drug resistant strains. Over the years, the use, misuse, and abuse of antimalarials have created a conducive environment for the development of resistant Plasmodium falciparum strains. We herein report on the synthesis, characterization and antimalarial activity of a library of seven novel 1,2,3-triazoles as part of the drug discovery campaign against drug-resistant Plasmodium falciparum. The interactions of the triazoles with plasmepsin II, plasmepsin IV, falcipain-2 and the heme detoxifying protein-all key proteins of Plasmodium falciparum degradosequesterome (Dsq) were also investigated by molecular docking. The compounds 3a-d, 4–6 were synthesized by CuAAC click reaction in good to excellent yields of 73–98% and characterized by melting point, UVvisible, infrared and nuclear magnetic resonance (1H and 13C) and MS techniques. Compounds 3a-d displayed high in vitro potency (IC50s: 0.62–22.11 ug/ml) against the chloroquine-resistant Dd2 lab strain of Plasmodium falciparum and low toxicity (SI > 1 except compound 4) to human erythrocytes. Computational studies indicated that the compounds 3a-3d had an absorption of 76–91%, and they were category III acute oral toxins (LD50 from 500 to 5000 mg/kg). The molecular docking study suggests that compounds 3a-d interacted with plasmepsin IV and the heme detoxifying protein with high affinity and a moderate affinity for falcipain-2. Keywords: Antimalarial; Click reaction; Docking; Plasmodium falciparum; Triazoles