article · Molecules
Phytochemical analysis of Tacca leontopetaloides tubers and Zanthoxylum zanthoxyloides stem bark led to the isolation and characterisation of several natural compounds. From T. leontopetaloides, two novel chalcones named tarkalynins A and B were isolated alongside taccalonolide A and its derivative. Extracts from Z. zanthoxyloides yielded taraxerol acetate, dihydrochelerythrin, and fagaramide. The compounds were evaluated in vitro against several parasitic species, including Trypanosoma brucei brucei and its multidrug-resistant clone, Trypanosoma evansi, Trypanosoma equiperdum, Trypanosoma congolense, and Leishmania mexicana. Dihydrochelerythrin and fagaramide demonstrated the strongest antiparasitic effects against several of these pathogens. Additionally, tarkalynin A and taraxerol acetate were effective against Trypanosoma equiperdum. Crucially, the tested compounds showed no significant cross-resistance with current trypanocidal treatments and displayed low toxicity toward human embryonic kidney cells, highlighting their potential as leads for parasitic disease treatments.
Parasitic infections caused by Trypanosoma and Leishmania species represent major human health and veterinary challenges, often exacerbated by resistance to current treatments. Discovering plant-derived compounds that remain potent against drug-resistant strains while showing minimal toxicity to human cells offers viable new starting points for designing safer, next-generation therapeutics to combat these neglected tropical and animal diseases.
This work represents early-stage laboratory discovery suited to pharmaceutical and veterinary drug developers searching for novel antiparasitic leads. The identified molecules, notably dihydrochelerythrin and fagaramide, provide candidate structures for synthetic optimisation and preclinical in vivo testing against trypanosomiasis and leishmaniasis. However, extensive pharmacological profiling, formulation studies, and clinical trials will be necessary before any therapeutic application is realised.
AI-generated from the published abstract. Always read the original work before citing.
The 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. The 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 Trypanosoma evansi, Trypanosoma equiperdum and Trypanosoma congolense, and against Leishmania 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 1.37, 2.559, 1.09, and 5.44 µM and 17.8, 10.9, 10.9, and 13.3 µM, respectively. In addition, tarkalynin A and taraxerol acetate displayed promising activity against T. equiperdum (EC50 = 21.4 and 21.3 µM, 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 even 300 µM. This report provides further evidence of the potential use of natural products for combating parasitic diseases.
This page summarises published work. The authoritative version sits with the publisher.
DOI: 10.3390/molecules30112468
Is something wrong with this record? Report it or request removal.
Discussion
Have you built on this work, tried to replicate it, or seen it applied in practice? Share what you know. Verified researchers and MARATTO™ domain experts can open a discussion, and any member can reply. Contributions are reviewed before they appear.
No discussion yet. Open the first thread.
New to MARATTO™? Create a free account.
