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<p>Malaria continues to pose a major public health challenge, especially in Sub-Saharan Africa, due to increasing resistance to existing therapies such as artemisinin-based treatments. The detoxification of free heme into hemozoin within <i>Plasmodium falciparum</i> is a critical survival mechanism and a validated antimalarial target. This study explores the antimalarial potential of phytochemicals isolated from the root bark of <i>Bombax costatum</i> using the β-hematin inhibition model, a well-validated in vitro assay that simulates the heme detoxification process in malaria parasites. Four compounds, identified as catechin, epicatechin, lupeol and catechin-7-O-glucoside were isolated and characterized via chromatographic and spectroscopic techniques and their ability to inhibit β-hematin formation was assessed. All four compounds demonstrated dose-dependent inhibition of β- hematin formation with IC₅₀ values of 3.168, 2.942, 5.888, and 3.651&#xa0;µg/mL for Compound HB1 (catechin), HB2 (epicatechin), HB3 (lupeol), and HB4 (catechin-7-O-glucoside) respectively, compared to 0.707&#xa0;µg/mL for chloroquine. Although less potent than the standard drug, the isolated compounds showed significant activity, validating the traditional use of <i>B. costatum</i> and highlighting the heme detoxification pathway as a plausible mechanism. These findings suggest that the phytochemicals in <i>B. costatum</i> may serve as promising lead compounds for future antimalarial drug development, particularly in the search for plant-based, affordable therapies suited for resource-limited, malaria-endemic regions.</p>

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In vitro antimalarial activity of phytochemicals from Bombax costatum via inhibition of β-hematin formation

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2026年2月10日

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  • Hassan Ali Bila,
  • Garba Dauda,
  • Amina Busola Olorukooba,
  • Dlama Stephen,
  • Khadijah Isa Imam

摘要

Malaria continues to pose a major public health challenge, especially in Sub-Saharan Africa, due to increasing resistance to existing therapies such as artemisinin-based treatments. The detoxification of free heme into hemozoin within Plasmodium falciparum is a critical survival mechanism and a validated antimalarial target. This study explores the antimalarial potential of phytochemicals isolated from the root bark of Bombax costatum using the β-hematin inhibition model, a well-validated in vitro assay that simulates the heme detoxification process in malaria parasites. Four compounds, identified as catechin, epicatechin, lupeol and catechin-7-O-glucoside were isolated and characterized via chromatographic and spectroscopic techniques and their ability to inhibit β-hematin formation was assessed. All four compounds demonstrated dose-dependent inhibition of β- hematin formation with IC₅₀ values of 3.168, 2.942, 5.888, and 3.651 µg/mL for Compound HB1 (catechin), HB2 (epicatechin), HB3 (lupeol), and HB4 (catechin-7-O-glucoside) respectively, compared to 0.707 µg/mL for chloroquine. Although less potent than the standard drug, the isolated compounds showed significant activity, validating the traditional use of B. costatum and highlighting the heme detoxification pathway as a plausible mechanism. These findings suggest that the phytochemicals in B. costatum may serve as promising lead compounds for future antimalarial drug development, particularly in the search for plant-based, affordable therapies suited for resource-limited, malaria-endemic regions.