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Identification of compounds with cytotoxic activity from the leaf of the Nigerian medicinal plant, Anacardium occidentale L. (Anacardiaceae)Taiwo, Bamigboye J., Fatokun, Amos A., Olubiyi, O.O., Bamigboye-Taiwo, O.T., van Heerden, F.R., Wright, Colin W. 2017 February 1922 (has links)
Yes / Cancer is now the second-leading cause of mortality and morbidity, behind only heart disease,
necessitating urgent development of (chemo)therapeutic interventions to stem the growing
burden of cancer cases and cancer death. Plants represent a credible source of promising drug
leads in this regard, with a long history of proven use in the indigenous treatment of cancer. This
study therefore investigated Anacardium occidentale, one of the plants in a Nigerian Traditional
Medicine formulation commonly used to manage cancerous diseases, for cytotoxic activity.
Bioassay-guided fractionation, spectroscopy, Alamar blue fluorescence-based viability assay in
cultured HeLa cells and microscopy were used. Four compounds: zoapatanolide A (1),
agathisflavone (2), 1, 2-bis (2,6-dimethoxy-4-methoxybenzoyl) ethane (Anacardicin, 3) and
methyl gallate (4) were isolated, with the most potent being zoapatanolide A with an IC50 value
of 36.2 ± 9.8 μM in the viability assay. To gain an insight into the likely molecular basis of their observed cytotoxic effects, Autodock Vina binding free energies of each of the isolated
compounds with seven molecular targets implicated in cancer development (MAPK8, MAPK10,
MAP3K12, MAPK3, MAPK1, MAPK7 and VEGF), were calculated. Pearson correlation
coefficients were obtained with experimentally-determined IC50 in the Alamar blue viability
assay. While these compounds were not as potent as a standard anti-cancer compound,
doxorubicin, the results provide reasonable evidence that the plant species contains compounds
with cytotoxic activity. This study provides some evidence of why this plant is used ethnobotanically
in anti-cancer herbal formulations and justifies investigating Nigerian medicinal
plants highlighted in recent ethno-botanical surveys. / This work was supported by a British Council Researcher Links Travel Grant 2013 to TBJ, a South Africa’s National Research Foundation (NRF) Grant No 98345, 2016 to FRVH and an academic staff funding provided to AAF by the School of Pharmacy, University of Bradford, UK.
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