Isolation and in vitro antiplasmodial activities of alkaloids from Teclea trichocarpa: In vivo antimalarial activity and X- ray crystal structure of normelicopicine


Muriithi, MW; Abraham, WR; Addae-Kyereme, J; Scowen, I; Croft, SL; Gitu, PM; Kendrick, H; Njagi, ENM; Wright, CW; (2002) Isolation and in vitro antiplasmodial activities of alkaloids from Teclea trichocarpa: In vivo antimalarial activity and X- ray crystal structure of normelicopicine. Journal of natural products, 65 (7). pp. 956-9. ISSN 0163-3864 DOI: https://doi.org/10.1021/np0106182

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Abstract

Seven alkaloids have been isolated from Teclea trichocarpa including four, normelicopicine (1), arborinine (2), skimmianine (6), and dictamnine (7), that are reported for the first time in addition to the previously reported alkaloids melicopicine (3), tecleanthine (4), and 6-methoxytecleanthine (5). The structure of 1 was confirmed by single-crystal X-ray crystallography. Two alkaloids, 1 and 2, displayed limited in vitro activities against Plasmodium falciparum strains HB3 and K1, but there appeared to be little cross-resistance with chloroquine. Alkaloid 1 was found to have some activity against P. berghei in mice (32% suppression of parasitaemia at a dose of 25 mg x kg(-1) x day(-1)), but unlike chloroquine it did not inhibit beta-haematin formation in a cell-free system; 1 was found to have low in vitro cytotoxicity to KB cells (IC50 > 328 microM).

Item Type: Article
Keywords: C-13 nmr-spectra, plasmodium-falciparum, acridone alkaloids, malaria, chemistry, Acridines, chemistry, isolation & purification, pharmacology, Alkaloids, chemistry, isolation & purification, pharmacology, Animal, Antimalarials, chemistry, isolation & purification, pharmacology, Chloroquine, analogs & derivatives, pharmacology, Crystallography, X-Ray, Erythrocytes, Female, Human, Inhibitory Concentration 50, KB Cells, drug effects, Kenya, Magnetic Resonance Spectroscopy, Mice, Mice, Inbred BALB C, Microbial Sensitivity Tests, Molecular Conformation, Molecular Structure, Plant Leaves, chemistry, Plants, Medicinal, chemistry, Plasmodium berghei, drug effects, Plasmodium falciparum, drug effects, Quinolines, chemistry, isolation & purification, pharmacology, Rutaceae, chemistry, Spectroscopy, Fourier Transform Infrared
Faculty and Department: Faculty of Infectious and Tropical Diseases > Dept of Immunology and Infection
Research Centre: Malaria Centre
PubMed ID: 12141852
Web of Science ID: 177226800002
URI: http://researchonline.lshtm.ac.uk/id/eprint/16581

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