Tropical Journal of Pharmaceutical Research

Original Research Article | OPEN ACCESS

Anti-cancer and anti-trypanosomal properties of alkaloids from the root bark of Zanthoxylum leprieurii Guill and Perr

Fabian I Eze^1,2 , Xavier Siwe-Noundou^2,3, Michelle Isaacs³, Srinivas Patnala⁴, Patience O Osadebe¹, Rui WM Krause^2,3

¹Department of Pharmaceutical and Medicinal Chemistry, University of Nigeria, Nsukka 410001, Nigeria; ²Nanomaterials and Medicinal Organic Chemistry Laboratory, Department of Chemistry; ³Marine Natural Products Chemistry Laboratory, Department of Biochemistry and Microbiology; ⁴Faculty of Pharmacy, Rhodes University, Grahamstown 6140, South Africa.

For correspondence:- Fabian Eze Email: fabian.eze@unn.edu.ng Tel:+2348064714208

Accepted: 21 October 2020 Published: 30 November 2020

Citation: Eze FI, Siwe-Noundou X, Isaacs M, Patnala S, Osadebe PO, Krause RW. Anti-cancer and anti-trypanosomal properties of alkaloids from the root bark of Zanthoxylum leprieurii Guill and Perr. Trop J Pharm Res 2020; 19(11):2377-2383 doi: 10.4314/tjpr.v19i11.19

© 2020 The authors.
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Abstract

Purpose: To isolate the anti-cancer and anti-trypanosomal principles of Zanthoxylum leprieurii, a medicinally versatile wild tropical plant used for managing tumours, African trypanosomiasis, and inflammation in southeastern Nigeria.

Methods: The pure compounds were isolated using chromatographic methods. The structural elucidation of the pure compounds was based on their NMR (1D and 2D) and mass spectral data as well as chemical test results. Structure-activity relationships were based on the structural differences among the compounds. The cytotoxicity of the extracts and compounds (1, 2, 3, and 4) was evaluated in HeLa (human cervix adenocarcinoma) cell line while the trypanocidal activities were evaluated on Trypanosoma brucei brucei.

Results: Two acridone alkaloids, 1-hydroxy-3-methoxy-10-methylacridin-9 (10H)-one, named fabiocinine (1), and 1-hydroxy-2,3-dimethoxy-10-methylacridin-9 (10H)-one (arborinine, 2), together with a furoquinoline alkaloid, skimmianine (3), and a chelerythrine derivative, 6-acetonyl-5,6-dihydrochelerythrine (4) were isolated from the root bark of Zanthoxylum leprieurii. Skimmianine (3) exhibited cytotoxicity and anti-trypanosomal IC₅₀ of 12.8 and 13.2 µg/mL respectively (p < 0.05). Compound (1) and arborinine (2) were selectively cytotoxic to HeLa cells with cytotoxicity IC₅₀ of 28.49 and 62.71 µg/mL, respectively, while (4) did not show significant activity (p < 0.05).

Conclusion: Zanthoxylum leprieurii root bark contains cytotoxic and trypanocidal compounds, and is thus a potential source of anti-cancer and anti-trypanosomal leads.

Keywords: Zanthoxylum leprieuri, Root bark, Anti-cancer, Anti-trypanosomal, Cytotoxicity, Alkaloids