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Anti-Cancer Agents in Medicinal Chemistry 2017

Phytochemical Analysis with Antioxidant and Cytotoxicity Studies of the Bioactive Principles from Zanthoxylum capense (Small Knobwood).

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Olusola Bodede
Shakira Shaik
Moganavelli Singh
Roshila Moodley

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Abstrè

BACKGROUND

Zanthoxylum capense (small knobwood) is a South African species known for a wide range of anecdotal uses. However, there is a dearth of information on its phytoconstitutional make-up, specifically its knobs, with only a few reports on the bioactive compounds that could justify its ethnomedicinal use.

OBJECTIVE

This work aimed to identify the active principles in Z. capense and evaluate their cytotoxicity against breast cancer tumor cells.

METHODS

Extracts from the stem bark, knobs and leaves were purified using chromatographic methods and characterized using spectroscopic techniques. Cytotoxicity of isolated compounds was evaluated on mammalian MCF-7, Caco-2 tumor cell lines and HEK295, a normal kidney cell line.

RESULTS

The following compounds were isolated from the plant: a quaternary benzophenanthridine-type alkaloid (chelerythrine) along with its alkanoamine derivative (6-hydroxydihydrochelerythrine), an indolopyridoquinazoline alkaloid (rutaecarpine), an alkyl p-coumaric acid ester (dodecyl-trans-p-coumarate), a lignan (sesamin), a flavanol (catechin), two triterpenoids (lupeol and sitosterol) and two pigments (pheophytin a and lutein). In the cytotoxicity study, all tested samples decreased the viability of the MCF-7 tumor cells by at least 23% at concentration 1 μg mL-1 and Caco-2 tumor cells by at least 15% at concentration 5 μg mL-1 but a mild toxic effect on HEK295 across the tested samples.

RESULTS

The following compounds were isolated from the plant: a quaternary benzophenanthridine-type alkaloid (chelerythrine) along with its alkanoamine derivative (6-hydroxydihydrochelerythrine), an indolopyridoquinazoline alkaloid (rutaecarpine), an alkyl p-coumaric acid ester (dodecyl-trans-p-coumarate), a lignan (sesamin), a flavanol (catechin), two triterpenoids (lupeol and sitosterol) and two pigments (pheophytin a and lutein). In the cytotoxicity study, all tested samples decreased the viability of the MCF-7 tumor cells by at least 23% at concentration 1 μg mL-1 and Caco-2 tumor cells by at least 15% at concentration 5 μg mL-1 but a mild toxic effect on HEK295 across the tested samples.

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