Sesquiterpene Lactone-Rich Extract of Tithonia diversifolia (Hemsley) A. Gray (Asteraceae) suppresses Trypanosoma brucei brucei in both In Vivo and In Vitro Experimental Models

doi.org/10.26538/tjnpr/v6i8.18

Authors

  • Edith O. Diovu Department of Pharmacognosy and Environmental Medicines, Faculty of Pharmaceutical Sciences, University of Nigeria Nsukka, 410001 Enugu State, Nigeria
  • Chibuzo O. Onah Department of Pharmacology and Toxicology, Faculty of Pharmaceutical Sciences, University of Nigeria Nsukka, 410001 Enugu State, Nigeria
  • Kelvin E. Odo Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmaceutical Sciences, University of Nigeria Nsukka, 410001 Enugu State, Nigeria
  • Ifeyinwa N. Amaechina Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmaceutical Sciences, University of Nigeria Nsukka, 410001 Enugu State, Nigeria
  • Uchechukwu D. Akpadolu Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmaceutical Sciences, University of Nigeria Nsukka, 410001 Enugu State, Nigeria
  • Adanne Judith Nwodo Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmaceutical Sciences, University of Nigeria Nsukka, 410001 Enugu State, Nigeria
  • Chinedu A.T. Chah Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmaceutical Sciences, University of Nigeria Nsukka, 410001 Enugu State, Nigeria
  • Chidiogor M. Akupue Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmaceutical Sciences, University of Nigeria Nsukka, 410001 Enugu State, Nigeria
  • Charles O. Nnadi Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmaceutical Sciences, University of Nigeria Nsukka, 410001 Enugu State, Nigeria

Keywords:

Animal trypanosomiasis,, Cytotoxicity,, Sesquiterpene lactones,, Tithonia diversifolia

Abstract

Tithonia diversifolia has continued to play vital roles in phytomedicine due to its ethnopharmacological relevance, medicinal properties and agricultural applications. Its richness in sesquiterpene lactones has also continued to generate interest due to its diverse pharmacological activities, structure-activity relationships, and pharmacokinetics. The study evaluated the anti-trypanosomal and cytotoxic activities of the sesquiterpene lactone (STL) constituents of Tithonia diversifolia using in vivo mouse and in vitro experimental models. The T. diversifolia methanol extract was fractionated by solvent-solvent partitioning in n-hexane, EtOAc, and n-butanol and further separated by the vacuum liquid chromatographic (VLC) method. The in vitro anti-trypanosomal and cytotoxic activities were evaluated using resazurin- based cell viability assays. The in vivo anti-trypanosomal activity was determined using a hematocrit-based packed cell volume analysis and rapid matching counting of Trypanosoma brucei brucei inhibition methods in a mouse model. The two STL-enriched sub-fractions (VLC- 3 and VLC-4) obtained from the VLC separation displayed significant (p < 0.05) in vitro activity against Trypanosoma brucei with IC50 values of 0.88 and 0.52 µg/mL respectively and SI of 44 and 165 respectively. In the in vivo mouse model, a 400 mg/kg dose of VLC-3 and VLC-4 elicited a 100% clearance of the parasites within 16 and 14 days post-induction of parasitemia compared with a similar effect of the positive control drug, diminazene aceturate on day 12. The strong in vivo/in vitro anti-trypanosomal activity of T. diversifolia STL represents a promising starting point for discovering potent trypanocidal agents against T.b. brucei, the major cause of animal African trypanosomiasis.

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Published

2022-08-01

How to Cite

O. Diovu, E., O. Onah, C., E. Odo, K., N. Amaechina, I., D. Akpadolu, U., Judith Nwodo, A., … O. Nnadi, C. (2022). Sesquiterpene Lactone-Rich Extract of Tithonia diversifolia (Hemsley) A. Gray (Asteraceae) suppresses Trypanosoma brucei brucei in both In Vivo and In Vitro Experimental Models: doi.org/10.26538/tjnpr/v6i8.18. Tropical Journal of Natural Product Research (TJNPR), 6(8), 1268–1273. Retrieved from https://tjnpr.org/index.php/home/article/view/1305