Abstract
New therapies for leukemia are urgently needed due to adverse side effects, tumor resistance and lack of selectivity of many chemotherapeutic agents in clinical use. Ageratum conyzoides has been used in folklore medicine for managing leukemia and other cancers. Thus, this study aimed to investigate the effects of fractions, sub-fractions and purified compounds from the ethanol leaf extracts of A. conyzoides against Jurkat cells-model for acute T cell leukemia. A two-dimensional purification process using normal phase flash, followed by reverse phase purification was necessary to isolate pure methoxy-flavones, which were further characterized by Nuclear Magnetic Resonance (NMR) and MS-MS. The effect of fractions or pure compounds on cell viability was determined using either the MTT reagent or CellTiter-Blue® assay, while the caspase-3 and -7 activation was tested with Caspase-Glo® 3/7 assay. Prediction of compounds’ drug disposition profiles in vivo was measured with biomimetic affinity chromatography methodologies. Key words: Ageratum conyzoides, methoxy-flavones, Jurkat, biomimetic affinity chromatography, cell viability.
Highlights
Medicinal plants remain an important source for the discovery of promising anticancer compounds
Fractionation of the crude extract by normal-phase flash chromatography resulted in six fractions; A to F, of which A, B and C eluted within heptane, D within ethylacetate and E and F within methanol (Figure 1)
The cell viability of Jurkat cells was unaffected by sub-fractions 1 and 2, as well as 4 through 6
Summary
Medicinal plants remain an important source for the discovery of promising anticancer compounds. Notable examples include vincristine and vinblastine isolated from Catharanthus roseus as well as taxol isolated from Taxus brevifolia for the treatment of leukemia (Moudi et al., 2013). These therapies are beneficial, problems such as adverse side effects, tumor resistance and lack of cancer cell selectivity are often reported. To improve current treatment modalities, the search for novel anticancer agents with minimal side effects is imperative.
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