preprint · Preprints.org
Phytochemical investigation of Tacca leontopetaloides tubers led to the isolation of two novel chalcones, named tarkalynins A and B, alongside taccalonolide A and its 12-propanoate derivative. Extraction of Zanthoxylum zanthoxyloides stem bark yielded taraxerol acetate, dihydrochelerythrin, and fagaramide. Tested against several parasites, dihydrochelerythrin and fagaramide demonstrated notable activity against Trypanosoma brucei brucei, its multi-drug-resistant clone, Trypanosoma evansi, and Leishmania mexicana. Additionally, tarkalynin A and taraxerol acetate exhibited activity against Trypanosoma equiperdum. None of the isolated compounds showed significant cross-resistance with established trypanocides, indicating efficacy against resistant parasites. Safety evaluations on human HEK293 cell lines revealed low cytotoxicity, with most isolates producing no growth inhibition at concentrations up to 100 or 200 micrograms per millilitre.
Parasitic infections caused by trypanosomes and Leishmania present persistent medical and veterinary problems, compounded by widespread resistance to current drugs. Discovering natural compounds that selectively target these parasites while showing low human cell toxicity and avoiding cross-resistance provides valuable avenues for designing new anti-parasitic therapies.
This work is at an early research stage, serving as initial lead discovery. Pharmaceutical developers and medicinal chemists could utilise these isolated natural compounds as starting templates to develop new anti-trypanosomal and anti-leishmanial drugs. Because the findings are currently limited to laboratory cell cultures, extensive in vivo efficacy testing, toxicology studies, and chemical optimisation are required before reaching real-world application.
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Phytochemical screening of extracts of Tacca leontopetaloides tubers, has afforded the isolation of two novel chalcones, tarkalynins A and B, along with taccalonolide A and its 12-propanoate. Screening of Zanthoxylum zanthoxyloides stem bark yielded taraxerol acetate, dihydrochelerythrin and fagaramide. These compounds were obtained through column and thin-layer chromatography and identified using NMR and LC-HRMS. The compounds were tested against Trypanosoma brucei brucei s427 and its multi-drug-resistant clone B48, against T. evansi, T. equiperdum, T. congolense, and against L. mexicana. Cytotoxicity was tested against the human HEK293 cell line. The highest activities were observed with dihydrochelerythrin and fagaramide against T. b. brucei s427 and B48, T. evansi, and L. mexicana with EC50 values of 0.5, 0.9, 0.4, and 1.9 µg/mL and of 4.4, 2.7, 2.7, and 3.3 µg/mL, respectively. In addition, tarkalynin A and taraxerol acetate displayed promising activity against T. equiperdum (EC50 = 7.1 and 9.98 µg/mL, respectively). None of these compounds showed significant cross-resistance with existing trypanocides (RF ≈ 1; P>0.05). The compounds displayed low toxicity to human cells, with most exhibiting no growth inhibition at concentrations of 100 or 200 µg/mL. This report provides further evidence of the potential of natural products for combating parasitic diseases.
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DOI: 10.20944/preprints202504.2020.v1
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