Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2024 Jun;69(2):1244-1252.
doi: 10.1007/s11686-024-00850-x. Epub 2024 May 6.

Piperine Enhances Antimalarial Activity of Methyl Gallate and Palmatine Combination

Adegbenro P Adegunloye  1 , Joseph O Adebayo  2
Affiliations

Piperine Enhances Antimalarial Activity of Methyl Gallate and Palmatine Combination

Adegbenro P Adegunloye et al. Acta Parasitol. 2024 Jun.

Abstract

Purpose: Artemisinin combination therapies, the first-line antimalarials in Nigeria, have reportedly suffered multiple failures in malaria treatment, hence the search for novel combination of other compounds. Methyl gallate and palmatine have been reported to exhibit antiplasmodial activities but the antimalarial activity of their combination has not been evaluated. Therefore, the evaluation of the combination of methyl gallate and palmatine for antimalarial activity in vitro and in vivo in the presence of piperine was carried out.

Materials and methods: The inhibitory potential of methyl gallate and palmatine combination on β-hematin (hemozoin) formation was studied in vitro. Also, the antimalarial activity of methyl gallate and palmatine combination with/without a bioenhancer (piperine) was evaluated in Plasmodium berghei NK65-infected mice.

Results: Methyl gallate and palmatine in the ratio 3:2 acted synergistically in vitro and had the highest inhibitory effect (IC50 = 0.73 µg/mL) on β-hematin (hemozoin) formation. The 3:2 combination of methyl gallate and palmatine exhibited no antimalarial activity in vivo in the absence of piperine but caused reduction in parasitemia that exceeded 40% in the presence of piperine at the dose of 25 mg/kg body weight on days 6 and 8 post-inoculation in mice.

Conclusion: The 3:2 combination of methyl gallate and palmatine in the presence of piperine exhibited antimalarial activity in vivo, possibly by synergistic inhibition of hemozoin formation which may cause accumulation of haem within the food vacuole of Plasmodium spp. and its death.

Keywords: Antimalarial; Bioenhancer; Drug combination; Methyl gallate; Palmatine; Piperine.

PubMed Disclaimer

References

    1. WHO (2020) World malaria report 2020: 20 years of global progress and challenges. World Health Organization
    1. WHO (2018) World Malaria Report 2018. Geneva
    1. Schlitzer M (2008) Antimalarial drugs—what is in use and what is in the pipeline. Arch Pharm (Weinheim) 341:149–163. https://doi.org/10.1002/ardp.200700184 - DOI - PubMed
    1. Beshir K, Sutherland CJ, Merinopoulos I, Durrani N, Leslie T, Rowland M, Hallett RL (2010) Amodiaquine resistance in Plasmodium falciparum malaria in Afghanistan is associated with the pfcrt SVMNT allele at codons 72 to 76. Antimicrob Agents Chemother 54:3714–3716. https://doi.org/10.1128/aac.00358-10 - DOI - PubMed - PMC
    1. Witkowski B, Duru V, Khim N, Ross LS, Saintpierre B, Beghain J, Eam R (2017) A surrogate marker of piperaquine-resistant Plasmodium falciparum malaria: a phenotype–genotype association study. Lancet Infect Dis 17:174–183. https://doi.org/10.1016/S1473-3099(16)30415-7 - DOI - PubMed - PMC

LinkOut - more resources