Browsing by Author "Zoiku, F.K."
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Item Alkaloidal Extracts from Avicennia africana P. Beauv. (Avicenniaceae) Leaf: An Antiplasmodial, Antioxidant, and Erythrocyte Viable(Advances in Pharmacological and Pharmaceutical Sciences, 2024) Ahmed, M.A.; Ameyaw, E.O.; Zoiku, F.K.; et al.Background. Te emergence of drug-resistant parasites impedes disease management and eradication eforts. Hence, a rein vigorated attempt to search for potent lead compounds in the mangroves is imperative. Aim. Tis study evaluates in vitro antiplasmodial activity, antioxidant properties, and cytotoxicity of A. africana leaf alkaloidal extracts. Methods. Te A. africana leaves were macerated with 70% ethanol to obtain a total crude extract. Dichloromethane and chloroform-isopropanol (3 :1, v/v) were used to extract the crude alkaloids and quaternary alkaloids from the total crude. Te antiplasmodial activities of the alkaloidal extracts were performed against 3D7 P. falciparum chloroquine-sensitive clone via the SYBR Green I fuorescence assay with artesunate serving as the reference drug. Te alkaloidal extracts were further evaluated for antioxidant properties via the total antioxidant capacity (TAC), the total glutathione concentration (GSH), the DPPH (2,2-diphenyl-1-picrylhydrazyl) assay, and the ferric-reducing antioxidant power (FRAP) methods. Te cytotoxic activity of the alkaloidal extracts was tested on erythrocytes using a 3-(4,5-dimethylthiazol-2-yl)-5-diphenyltetrazolium bromide-MTTassay with little modifcation. Te phytocompounds in the alkaloidal extracts were identifed via gas chromatography-mass spectrometry (GC-MS) techniques. Results. Te total crude extract showed good antiplasmodial activity (IC50 = 11.890 µg/mL). Te crude and quaternary alkaloidal extracts demonstrated promising antiplasmodial efects with IC50 values of 6.217 and 6.285 µg/mL, respectively. Te total crude and alkaloidal extracts showed good antioxidant properties with negligible cytotoxicity on erythrocytes with good selectivity indices. Te GC-MS spectral analysis of crude alkaloidal extracts gave indole and isoquinoline alkaloids and several other compounds. Dexrazoxane was found to be the main compound predicted, with an 86% peak area in the quaternary alkaloidal extract. Conclusion. Te crude and quaternary alkaloidal extracts exhibited antiplasmodial activities and ability to inhibit oxidative stress with negligible toxicity on erythrocytes. Tis may be good characteristics to avoid oxidative stress related to Plasmodium infection in the treatment of malaria.Item Anti-malarial activity of the alkaloid, heptaphylline, and the furanocoumarin, imperatorin, from Clausena anisata against human Plasmodium falciparum malaria parasites: ex vivo trophozoitocidal, schizonticidal and gametocytocidal approach(Malaria Journal, 2023) Kumatia, E.K.; Zoiku, F.K.; Asase, A.; Tung, N.H.Background The erythrocytic stage of the life cycle of the malaria parasite, Plasmodium falciparum, consists of trophozoite, schizont and gametocyte stages in humans. Various anti-malarial agents target diferent stages of the parasite to produce treatment outcomes. This study reports on the stage-specifc anti-malarial activity of hepta phylline and imperatorin against human P. falciparum in addition to their cytotoxicity and selectivity indices (SI). Methods The compounds were isolated from Clausena anisata using column chromatography and their structures elucidated using NMR spectroscopy. The anti-malarial activity was determined by measuring the trophozoitocidal, schizonticidal and gametocytocidal activities of the compounds using the SYBR green assay. Cytotoxicity was evalu ated using the tetrazolium-based colorimetric assay. Results Heptaphylline and imperatorin produced trophozoitocidal, schizonticidal and gametocytocidal activi ties with IC50s of 1.57 (0.2317)–26.92 (0.3144) µM with those of artesunate (the standard drug) being 0.00024 (0.0036)–0.0070 (0.0013) µM. In the cytotoxicity assay, the compounds produced CC50S greater than 350 µM and SI of 13.76–235.90. Also, the trophozoitocidal and schizonticidal activities of the compounds were more pronounced than their gametocytocidal activity. Imperatorin was 42.04% more trophozoitocidal than hepthaphyline. However, hepthaphyline has more schizonticidal and gametocytocidal properties than imperatorin. Conclusion Heptaphylline and imperatorin are promising anti-malarial agents, since they possess potent anti-malar ial activity with weak cytotoxicity on RBCs. However, imperatorin is a better anti-malarial prophylactic agent whereas heptaphylline is a better malaria treatment agent.Item Assessment Of Antiplasmodial Activities Of Selected Herbal Products Used For The Treatment Of Malaria In Ghana(University Of Ghana, 2022-12) Zoiku, F.K.Malaria continues to be a menace in many parts of the world and remains a global public health problem, contributing to high morbidity and mortality especially in developing countries including Ghana. Even though Artermisinin-based Combination Therapies (ACTs) still remain efficacious in the treatment of malaria, most of the populace in Ghana rely heavily on medicinal plants and herbal preparations for the treatment of malaria and other infectious diseases. The seven herbal products were selected based on a preliminary survey conducted on knowledge, perception and consumption of herbal products in Greater Accra Region. The most commonly used Antimalarial herbal medications selected were Away, Givers, Osompa, Typhofa, Malatyphs, Aseda and Geo Manuel Herbal drugs. These herbal drugs were therefore assessed for their antiplasmodial activities using in vitro and ex vivo sensitivity testing on chloroquine (CQ)-sensitive (3D7), CQ-resistant (Dd2) strains of Plasmodium falciparum and Plasmodium berghei. The SYBR-Green 1 fluorescence-based method was used for the analysis. The results showed IC50 values ranging from 1.16μg/ml to 56 μg/ml for all the Plasmodium strains. However, there was a significant difference between the IC50 values of the standard control drugs (p<0.05) for both 3D7 and Dd2 strains. For the mechanism of action, a simple colorimetric inhibition of heme crystallization method was used and the IC50 were determined which ranged from 1.86μg/ml to 122.2μg/ml for the herbal drugs. Cytotoxicity of the herbal drugs were assessed with MTT assay using human red cells and selectivity index ranged from 4.42 to 405.60 with cell viabilities above 60% indicating no in vitro cytotoxic effects to the human red cells. To determine the heavy metal and electrolyte contents of the herbal drugs, atomic spectrometry method was used and the results ranged from 0.1mg/Kg to 12.8mg/kg of the heavy metals with significant differences (p<0.05) among all the seven herbal products. For the electrolytes, results ranged from 1.1mg/kg to 1400mg/Kg with no significant difference (p>0.05) among the herbal drugs. The pH of the selected herbal drugs determined were below 5 (3.56-4.61) indicating acidic nature of the herbal products. High Performance Liquid Chromatography (HPLC) was used to determine the fingerprint of the seven herbal products and the result indicated the presence of varying active compounds from 9 to 16 with no similarities in retention times (min) as compared to other standard drugs used. In conclusion, these results show that the selected herbal drugs have antiplasmodial activities with no cytotoxic effect to human red cells but slightly acidic in natureItem In vitro and in silico anti-malarial activity and cytotoxicity of n-hexyl 1-O-rutinoside (a glycoside) isolated from Annickia polycarpa (DC.) Setten and Maas ex I.M. Turner (Annonaceae)(Journal of Ethnopharmacology, 2023) Kumatia, E.K.; Zoiku, F.K.; Asase, A.; Tung, N.H.Ethnopharmacological relevance: Annickia polycarpa leaf is an effective anti-malarial agent. However, its chemical constituents have not been isolated and assayed against any pathogen. Aim of the study: To isolate and characterize anti-malarial compound(s) from the leaf of A. polycarpa. Materials and methods: Bioassay-guided fractionation was employed to isolated the compound (AL1) from the chloroform fraction (ALCF) of the basified ethanol extract of A. polycarpa leaf (ALE). AL1 was characterized by LC-MS, 1D and 2D NMR spectroscopic analysis. Anti-malarial activity was evaluated against drug resistance Dd2 and drug sensitive 3D7 Plasmodium falciparum strains using the SYBR green assay. Cytotoxicity and mechanistic studies were determined using tetrazolium-based colorimetric assay and molecular docking respectively. Results: AL1 was characterized as n-hexyl 1-O-rutinoside. The IC50 values of ALE and ALCF against 3D7 and Dd2 P. falciparum strains ranges from 3.441 (0.3389) - 4.255 (0.2246) μg/mL. The IC50s obtained for n-hexyl 1-O-ruti noside and Artesunate (standard drug) were 7.71 (0.5473) and 0.001 (0.00008) nM against the 3D7 parasite strain respectively. Also, the efficacy of n-hexyl 1-O-rutinoside increased by 24.40% against the chloroquine resistance Dd2 P. falciparum strain whiles that of Artesunate decreased by 98.96%. Furthermore, ALE, ALCF and n-hexyl 1-O-rutinoside were weakly cytotoxic to human RBCs with high selectivity indices. N-hexyl 1-O-rutino side inhibits P. falciparum chloroquine resistance transporter (PfCRT) and dihydrofolate reductase-thymidylate synthase (PfDHFR-TS) better than chloroquine and pyrimethamine respectively. But, produced similar inhibi tion of P. falciparum 2-trans-enoyl -ACP-reductase (PfERN) as triclosan. Conclusion: These results show that A. polycarpa leaf and n-hexyl 1-O-rutinoside possessed profound anti-malarial activity and are not cytotoxic. N-hexyl 1-O-rutinoside could therefore, be developed into a new anti-malarial medicine. This is the first study to report the anti-malarial activity of n-hexyl 1-O-rutinoside and its isolation from the genus Annickia.Item In vitro and in silico anti-malarial activity and cytotoxicity of n-hexyl 1-O-rutinoside (a glycoside) isolated from Annickia polycarpa (DC.) Setten and Maas ex I.M. Turner (Annonaceae)(Journal of Ethnopharmacology, 2023) Kumatia, E.K.; Zoiku, F.K.; Asase, A.; Tung, N.H.Ethnopharmacological relevance: Annickia polycarpa leaf is an effective anti-malarial agent. However, its chemical constituents have not been isolated and assayed against any pathogen. Aim of the study: To isolate and characterize anti-malarial compound(s) from the leaf of A. polycarpa. Materials and methods: Bioassay-guided fractionation was employed to isolated the compound (AL1) from the chloroform fraction (ALCF) of the basified ethanol extract of A. polycarpa leaf (ALE). AL1 was characterized by LC-MS, 1D and 2D NMR spectroscopic analysis. Anti-malarial activity was evaluated against drug resistance Dd2 and drug sensitive 3D7 Plasmodium falciparum strains using the SYBR green assay. Cytotoxicity and mechanistic studies were determined using tetrazolium-based colorimetric assay and molecular docking respectively. Results: AL1 was characterized as n-hexyl 1-O-rutinoside. The IC50 values of ALE and ALCF against 3D7 and Dd2 P. falciparum strains ranges from 3.441 (0.3389) - 4.255 (0.2246) μg/mL. The IC50s obtained for n-hexyl 1-O-ruti noside and Artesunate (standard drug) were 7.71 (0.5473) and 0.001 (0.00008) nM against the 3D7 parasite strain respectively. Also, the efficacy of n-hexyl 1-O-rutinoside increased by 24.40% against the chloroquine resistance Dd2 P. falciparum strain whiles that of Artesunate decreased by 98.96%. Furthermore, ALE, ALCF and n-hexyl 1-O-rutinoside were weakly cytotoxic to human RBCs with high selectivity indices. N-hexyl 1-O-rutino side inhibits P. falciparum chloroquine resistance transporter (PfCRT) and dihydrofolate reductase-thymidylate synthase (PfDHFR-TS) better than chloroquine and pyrimethamine respectively. But, produced similar inhibi tion of P. falciparum 2-trans-enoyl -ACP-reductase (PfERN) as triclosan. Conclusion: These results show that A. polycarpa leaf and n-hexyl 1-O-rutinoside possessed profound anti-malarial activity and are not cytotoxic. N-hexyl 1-O-rutinoside could therefore, be developed into a new anti-malarial medicine. This is the first study to report the anti-malarial activity of n-hexyl 1-O-rutinoside and its isolation from the genus Annickia.