Antiplasmodial and Haem Transition Activities of Tannin and Glycoside Fractions of Phyllanthus amarus
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1683-1708
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Sep 22, 2025
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10.58578/ajstea.v3i5.7460
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Authors:Akpor Ugochukwu Blessed1
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Abstract
Malaria remains a major public health threat, particularly in Nigeria, amid rising resistance of Plasmodium falciparum to existing therapies, underscoring the need for new, effective, and affordable antimalarials. This study aimed to evaluate the antiplasmodial activity of Phyllanthus amarus tannin and glycoside extracts and to assess their effects on haem-related mechanisms. Standard procedures were used to prepare crude extracts, which were tested against sensitive P. falciparum 3D7 strains; parasite growth inhibition and haem transition inhibition assays were conducted, and performance was benchmarked against chloroquine. Key findings show that the tannin extract reduced parasite growth (albeit less than chloroquine, p < 0.05) with IC₅₀ = 3.09 µg/mL, whereas the glycoside extract exhibited minimal activity (IC₅₀ = 14.45 µg/mL) compared with chloroquine (IC₅₀ = 0.41 µg/mL). Neither extract significantly inhibited haem transition, in contrast to chloroquine, suggesting possible interference at early stages of haem oligomerisation while haem remains in solution. The study concludes that the tannin extract demonstrates promising antiplasmodial activity, while the glycoside extract does not. The contribution and implication are that the antimalarial properties of P. amarus observed in vitro and in vivo may be partly attributable to its tannin content, warranting further investigation as a candidate for antimalarial development.
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Phyllanthus amarus; Plasmodium falciparum; Tannins; Glycosides; Antiplasmodial Activity; IC₅₀; Haem Oligomerisation
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Blessed, A. U. (2025). Antiplasmodial and Haem Transition Activities of Tannin and Glycoside Fractions of Phyllanthus amarus. Asian Journal of Science, Technology, Engineering, and Art, 3(5), 1683-1708. https://doi.org/10.58578/ajstea.v3i5.7460
Authors retain copyright and grant the journal right of first publication with the work simultaneously licensed under a Creative Commons Attribution-NonCommercial-ShareAlike 4.0 International License that allows others to share the work with an acknowledgement of the work's authorship and initial publication in this journal.
References
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Basilico, N., Pagani, E., Monti, D., Olliaro, P. and Taramelli, D. (1998). A microtitre-based method for measuring the Haem Polymerization Inhibitory Activity (HPIA) of antimalarial drugs. Journal of Antimicrobial Chemotherapy, 42:55-60.
Bello, M. and Ibaba, H. (2020). Effect of Crude Ethanolic Leaf Extract of Phyllanthus amarus and Highly Active Antiretroviral Therapy (Tenofovir-Lamivudine Combination) in Wistar Rats. Direct Research Journal of Health and Pharmacology, 8(5):52-64.
Bethel, K., Kojo, A., Jeffery, L., Claudia, A. and Regina, A. (2019). In Vitro Assessment of Antiplasmodial Activity and Cytotoxicity of Polyathia longofolia Leaf Extracts on Plasmodium falciparum Strain NF54. Malaria Research and Treatment, 9.
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Faremi, T. Y., Suru, S. M., Fasunso, M. A. and Obioha, U. E. (2008). Hepatoprotective potentials of Phyllanthus amarus against ethanol-induced oxidative stress in rats. Food Chemistry and Toxicology, 46:2658-2664.
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Garcia, J. E., Alvaro, P. and Manuel, E. P. (2006). Development Biology of Sporozoite-Host Interactions in Plasmodium falciparum Malaria: Implications for Vaccine Design. Clinical Microbiology Reviews, 19(4):686-707.
Gerald, N., Babita, M. and Sanjai, K. (2011). Mitosis in the Human Malaria Parasite Plasmodium falciparum. American Society for Microbiology, 10(4):474-482.
Gleadow, R. M. and Moller, B. L. (2014). Cyanogenic glycosides: synthesis, physiology and phenotypic plasticity. Annual Review of Plant Biology, 46:2658-2664.
Green, B. O. (2007). Journal of Pharmaceutical Science, 1(3):23-29.
Hasler, C. M. and Blumberg, J. B. (1999). Symposium on Phytochemicals: Biochemistry and Physiology. Journal of Nutrition, 129:756-757.
Idowu, O., Soniran, O., Ajana, O. and Aworinde, D. (2010). Ethnobotanical survey of antimalarial plants used in Ogun State, Sothwest Nigeria. African Journal of Pharmacy and Pharmacology, 4(2):55-60.
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Ngemenya, M. N, Mbah, A. J. and Tane, P. (2006). Antibacterial effects of some Cameroonian medicinal plants against common pathogenic bacteria. African Journal of Traditional, Complementary and Alternative Medicines, 3(2):84-93.
Oronsaye, F. E. (2017). Treatment of malaria using new plant Phyllantus amarus. Journal of Bacteriology and Parasitology, 8(3):61.
Onyesom, I. (2021). Sample of a Research Prosposal. Research project workbook for undergraduate, 5.
Onyesom, I., Ehioma, J., Elu, C., Opajobi, A. O. and Uzuegbu U. E. (2020). Cytotoxicity and antiplasmodial activity of alkaloid extract prepared from eight African medicinal plants used in Nigeria. Thai Journal of Pharmaceutical Sciences, 44(4):237-244.
Onyesom, I. and Adu, F. (2015). Phyllanthus amarus possesses malarial curative and pancreatic tonic potentilas in experimental mice. Thai Journal of Chemical and Pharmaceutical Research, 7(5):7-15.
Onyesom, I., Onumaechi, I. F., Ehiwaro, J. and Dagana, R. (2015). Antiplasmodial Activity of Phyllanthus amarus Preserves Renal Function in Plasmodium berghei Infected Mice. European Journal of Medicinal Plants, 5(1):109-116.
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Oyewole, O. I., Oyedara, O. O., Olabiyi, B. F. and Fasanya, T. S. (2013). Phtyochemical, antimicrobial and toxicity studies of Phyllanthus amarus whole plant extract. International Journal of Bioassays, 2(3):519-523.
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Senior, K. (2008). Climate change and infectious disease: A dangerous liason? The lancet, 8(2):11-15.
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Sherman, I. W. (1998). A brief history of malaria and discovery of the parasites’s life cycle. In Malaria: Parasite Biology, Pathogenesis and Protection; Sherman, I. W.; American Society for Microbiology Press: Washington, DC, 3−10.
Sigala, P., Crowley, J., Samantha, H., Jeffery, P. and Daniel, G. (2012). Direct test of enzymatic heme degradation by the malaria parasite Plasmodium falciparum. Journal of Biological Chemistry, 287(45):37793-37807.
Sinha, S., Medhi, B. and Sehgal, R. (2014). Challenges of drug-resistant malaria. Parasite, 21:61.
Strum, A., Amino, R., Claudia, V., Regen, T., Retzlaff, S., Rennenberg, A., Krueger, A., Pollok, J., Menard, R. and Volka, T. (2017). Manipulation of host hepatocytes by the malaria parasite for delivery into liver sinusoids. National Library of Medicine, 313(5791):1287-1290.
Talman, A., Domarle, O., Ellis, F., Ariey, F. and Robert, V. (2004). Gametocytogenesis: the puberty of Plasmodium falciparum. Malaria Journal, 3(24):1.
Trampuz, A., Jereb, M., Igor, M. and Rajesh, M. P. (2003). Clinical review: Severe malaria. National Library of Medicine, 7(4):315-323.
Ukoha, P. O., Egbonu, A. C., Obasi, L. E and Ejikeme, P. M. (2011). Tannins and other phytochemicals of the Samanaea saman pods and their antimicrobial activities. African Journal of Pure and Applied Chemistry, 5(8):237-244.
Vaughan, A. M. and Stefan, H. I. (2017). Malaria Parasite Liver Infection AND Exoerythrocytic Biology. Cold Spring Harbor Perspective in Medicine, 7(6):a025486.
Wongsrichanalai, C, and Meshnick, S. R. (2008). Declining artesunate-mefloquine efficacy against falciparum malaria on the Cambodia-Thalian border. Emerging Infectious Disease, 14(5):716-719.
White, N. J. (2008). Qinghaosu (artemisinin): The price of success. Science, 320(5874):330–34.
World Health Organization (2009). World malaria report 2009. WHO, Geneva.
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World Health Organization (2013). World malaria report 2013. WHO, Geneva.
World Health Organization (2019). World malaria report 2019. WHO, Geneva.
World Health Organization (2020). World malaria report 2020. WHO, Geneva.
Yuan, X., Nicole, R., Hanna, K., Ana, B., David, A., John D., Emma, L., Amit, R. and Iqbal, H. (2016). Regulation of intracellular heme trafficking revealed by subcellular reporters. Proceeding of the National Academy of Science of the United States of America, 113(35):E5144-E5152.
Zaidan, M., Rin, N. and Badrul, A. (2005). In vitro screening of live local medicinal plants for antibacterial activity using disc diffusion method. Tropical Biomedicine, 22:165-170.
Ajala, T. O., Igwilo, C. I., Oreagba, I. A. and Odeku, O. A. (2011). The antiplasmodial effect of the extracts and formulated capsules of Phyllanthus amarus on Plasmodium yoelii infection in mice. Asian Pacific Journal of Tropical Medicine, 4(4):283-287.
Ameen, O. A., Hamid, A. A., Yusuf, Q., Njoku, O. G., Oseni, T. O. and Jamiu, W. (2021). Quantitative and Qualitative Assessment of Phytochemicals in Methanolic Extracts of Hurricane Weed (Phyllanthus amarus Schumach &Thonn) Plant. Journal of Applied Science and Environment Management, 25(2):159-165.
Arrow, K. J., Panosian. C. and Gelband, H. (2004). Saving Lives, Buying Time: Economics of Malaria Drugs in an Age of Resistance [Online: https://books.google.com/books?id=PL8EmnGt71sC&pg=PA141]. National Academies Press, 141 [Accessed: October 29, 2021].
Ashley, E. A., Dhorda, M., Fairhurst, R. M., Amaratunga, C. and Lim, P. (2014). Spread of artemisinin resistance in Plasmodium falciparum malaria. New England Journal of Medicine., 371 (5): 411–423.
Basilico, N., Pagani, E., Monti, D., Olliaro, P. and Taramelli, D. (1998). A microtitre-based method for measuring the Haem Polymerization Inhibitory Activity (HPIA) of antimalarial drugs. Journal of Antimicrobial Chemotherapy, 42:55-60.
Bello, M. and Ibaba, H. (2020). Effect of Crude Ethanolic Leaf Extract of Phyllanthus amarus and Highly Active Antiretroviral Therapy (Tenofovir-Lamivudine Combination) in Wistar Rats. Direct Research Journal of Health and Pharmacology, 8(5):52-64.
Bethel, K., Kojo, A., Jeffery, L., Claudia, A. and Regina, A. (2019). In Vitro Assessment of Antiplasmodial Activity and Cytotoxicity of Polyathia longofolia Leaf Extracts on Plasmodium falciparum Strain NF54. Malaria Research and Treatment, 9.
Brito-Arias, M. (2007). Springer. Synthesis and Characterization of Glycosides, 68-132.
Caraballo, H. and King, K. (2014). Emeergency Department Management of Mosquito-Borne illness: Malaria, Dengue and West Nile Virus. Emergency Medicine Practice, 16:1-23.
Carter, R. and Mendis, K. N. (2002). Evolutionary and historical aspects of the burden of malaria. Clinical Microbiology Review, 15:564−594.
Chung, J. (2012). Heme metabolism and erythropoiesis. National Library of Medicine, 19(3):156-162.
Cowman, A. F., Berry, D. and Baum, J. (2012). The cellular and molecular basis for malaria parasite invasion of the human red blood cell. Journal of Cell Biology, 198(6):961-971.
Dolara, P., Luceri, C., De Filippo, C., Femia, A. P., Giovannelli, L., Carderni, G., Cecchini, C., Silvi, S., Orpianesi, C., Cresci, A., (2005). Red wine polyphenols influence carcinogenesis, intestine microflora, oxidative damage and gene expression profiles of colonic mucosa in F344 rats. Mutation Research, 591:237-246.
Dondorp, A. M., Yeung, S., White, L., Nguon, C., Day, N. P., Socheat, D. and Von, S. L. (2010). Artemisinin resistance: Current status and scenarios for containment. National Review of Microbiology, 8(4):272–280.
Egan, T. J., Ross, D. C. and Adams, P. A. (1994). Quinoline anti-malarial drugs inhibit spontaneous formation of β-hematin (malaria pigment). Federation of European Biochemical Societies letters, 352(1):54-57.
Elujoba, A. (2005). Medicinal properties of plants with oral health implication. Proceedings of the 2nd Dr. David Barnes’ Memorial Public Health Symposium, 25th March 2003, Organized by Regional Centre for Oral Health Research and Training for Africa, Jos, in collaboration with WHO Regional Office, Brazzaville, 2(1):46-61.
Etta, H. (2008). Effects of Phyllanthus amarus on litter traits in albino rats. Scientific Research and Essay, 3(8):370-372.
Faremi, T. Y., Suru, S. M., Fasunso, M. A. and Obioha, U. E. (2008). Hepatoprotective potentials of Phyllanthus amarus against ethanol-induced oxidative stress in rats. Food Chemistry and Toxicology, 46:2658-2664.
Furnival-Adams, J., Olanga, E. A., Napier, M. and Garner, P. (2020). House modifications for preventing malaria. [Online: https://researchonline.lshtm.ac.uk]. Cochrane Database of Systematic Reviews, [Accessed: November 3, 2021].
Garcia, J. E., Alvaro, P. and Manuel, E. P. (2006). Development Biology of Sporozoite-Host Interactions in Plasmodium falciparum Malaria: Implications for Vaccine Design. Clinical Microbiology Reviews, 19(4):686-707.
Gerald, N., Babita, M. and Sanjai, K. (2011). Mitosis in the Human Malaria Parasite Plasmodium falciparum. American Society for Microbiology, 10(4):474-482.
Gleadow, R. M. and Moller, B. L. (2014). Cyanogenic glycosides: synthesis, physiology and phenotypic plasticity. Annual Review of Plant Biology, 46:2658-2664.
Green, B. O. (2007). Journal of Pharmaceutical Science, 1(3):23-29.
Hasler, C. M. and Blumberg, J. B. (1999). Symposium on Phytochemicals: Biochemistry and Physiology. Journal of Nutrition, 129:756-757.
Idowu, O., Soniran, O., Ajana, O. and Aworinde, D. (2010). Ethnobotanical survey of antimalarial plants used in Ogun State, Sothwest Nigeria. African Journal of Pharmacy and Pharmacology, 4(2):55-60.
Kaur, M. (2021). Tannins: Classification, properties and chemical tests. [Online] Available at: https://www.yourarticlelibrary.com/pharmagnosy/photochemical-screening/tannins-classification-properties-and-chemical-tests [Accessed November 3, 2021].
Nchinda, T. C. (2007). Malaria: a reemerging disease in Africa. Emerging Infectious Diseases, 4(3):398-403.
Neeraj, J., Shasany, A., Sundaresan, V., Rajkumar, S., Darokar, M., Bagchi, G., Gupta, A., Sushil, Kumar and Khanuja, S. (2003). Molecular diversity in Phyllanthus amarus assessed through Random Amplification Polymorphic DNA analysis. Central Institute of Medicinal and Aromatic Plants, 85(10):1454.
Ngasala, B., Mubi, M., Warsame, M., Petzold, G., Massele, A. Y., Gustafsson, L. L., Tomson, G., Premji, Z. and Bjorkman, A. (2008). Impact of training in clinical and microscopy diagnosis of childhood malaria on antimalarial drug prescription and health outcome at primary health care level in Tanzania: A randomized controlled trial. Malaria Journal, 7(1):1-11.
Ngemenya, M. N, Mbah, A. J. and Tane, P. (2006). Antibacterial effects of some Cameroonian medicinal plants against common pathogenic bacteria. African Journal of Traditional, Complementary and Alternative Medicines, 3(2):84-93.
Oronsaye, F. E. (2017). Treatment of malaria using new plant Phyllantus amarus. Journal of Bacteriology and Parasitology, 8(3):61.
Onyesom, I. (2021). Sample of a Research Prosposal. Research project workbook for undergraduate, 5.
Onyesom, I., Ehioma, J., Elu, C., Opajobi, A. O. and Uzuegbu U. E. (2020). Cytotoxicity and antiplasmodial activity of alkaloid extract prepared from eight African medicinal plants used in Nigeria. Thai Journal of Pharmaceutical Sciences, 44(4):237-244.
Onyesom, I. and Adu, F. (2015). Phyllanthus amarus possesses malarial curative and pancreatic tonic potentilas in experimental mice. Thai Journal of Chemical and Pharmaceutical Research, 7(5):7-15.
Onyesom, I., Onumaechi, I. F., Ehiwaro, J. and Dagana, R. (2015). Antiplasmodial Activity of Phyllanthus amarus Preserves Renal Function in Plasmodium berghei Infected Mice. European Journal of Medicinal Plants, 5(1):109-116.
Ouattara, L. P., Sanon, S., Mahiou-Leddet, V., Gansane, A., Baghdikian, B., Traore, A, Nebie, I., Traore, A. S., Azas, N., Ollivier, E. and Sirima, S. B. (2014). In vitro antiplasmodial activity of some medicinal plants of Burkina Faso. Parasitology Research, 113(1):405-416.
Owusu-Ofori, A. K., Parry, C. and Bates, I. (2010). Transfusion-transmitted malaria in countries where malaria is endemic: A review of the literature from sub-Saharan Africa. Clinical Infectious Diseases, 51(10):1192–1198.
Oyewole, O. I., Oyedara, O. O., Olabiyi, B. F. and Fasanya, T. S. (2013). Phtyochemical, antimicrobial and toxicity studies of Phyllanthus amarus whole plant extract. International Journal of Bioassays, 2(3):519-523.
Pagola, S., Stephen, P. W., Bohle, D. S., Kosar, A. D. and Madsen, S. K. (2000). The structure of malaria pigment beta-hematin. Nature, 404(6775):307-310.
Senior, K. (2008). Climate change and infectious disease: A dangerous liason? The lancet, 8(2):11-15.
Sharma, S., Gupta, P. and Sanjay, S. (2014). Effect of salts (NaCl and Na2CO3) on callus and suspension culture of steviol glycoside production. Applied biochemistry and biotechnology, 172(6):2894-2906.
Sherman, I. W. (1998). A brief history of malaria and discovery of the parasites’s life cycle. In Malaria: Parasite Biology, Pathogenesis and Protection; Sherman, I. W.; American Society for Microbiology Press: Washington, DC, 3−10.
Sigala, P., Crowley, J., Samantha, H., Jeffery, P. and Daniel, G. (2012). Direct test of enzymatic heme degradation by the malaria parasite Plasmodium falciparum. Journal of Biological Chemistry, 287(45):37793-37807.
Sinha, S., Medhi, B. and Sehgal, R. (2014). Challenges of drug-resistant malaria. Parasite, 21:61.
Strum, A., Amino, R., Claudia, V., Regen, T., Retzlaff, S., Rennenberg, A., Krueger, A., Pollok, J., Menard, R. and Volka, T. (2017). Manipulation of host hepatocytes by the malaria parasite for delivery into liver sinusoids. National Library of Medicine, 313(5791):1287-1290.
Talman, A., Domarle, O., Ellis, F., Ariey, F. and Robert, V. (2004). Gametocytogenesis: the puberty of Plasmodium falciparum. Malaria Journal, 3(24):1.
Trampuz, A., Jereb, M., Igor, M. and Rajesh, M. P. (2003). Clinical review: Severe malaria. National Library of Medicine, 7(4):315-323.
Ukoha, P. O., Egbonu, A. C., Obasi, L. E and Ejikeme, P. M. (2011). Tannins and other phytochemicals of the Samanaea saman pods and their antimicrobial activities. African Journal of Pure and Applied Chemistry, 5(8):237-244.
Vaughan, A. M. and Stefan, H. I. (2017). Malaria Parasite Liver Infection AND Exoerythrocytic Biology. Cold Spring Harbor Perspective in Medicine, 7(6):a025486.
Wongsrichanalai, C, and Meshnick, S. R. (2008). Declining artesunate-mefloquine efficacy against falciparum malaria on the Cambodia-Thalian border. Emerging Infectious Disease, 14(5):716-719.
White, N. J. (2008). Qinghaosu (artemisinin): The price of success. Science, 320(5874):330–34.
World Health Organization (2009). World malaria report 2009. WHO, Geneva.
World Health Organization (2012). World malaria report 2012. WHO, Geneva.
World Health Organization (2013). World malaria report 2013. WHO, Geneva.
World Health Organization (2019). World malaria report 2019. WHO, Geneva.
World Health Organization (2020). World malaria report 2020. WHO, Geneva.
Yuan, X., Nicole, R., Hanna, K., Ana, B., David, A., John D., Emma, L., Amit, R. and Iqbal, H. (2016). Regulation of intracellular heme trafficking revealed by subcellular reporters. Proceeding of the National Academy of Science of the United States of America, 113(35):E5144-E5152.
Zaidan, M., Rin, N. and Badrul, A. (2005). In vitro screening of live local medicinal plants for antibacterial activity using disc diffusion method. Tropical Biomedicine, 22:165-170.