Phytochemistry and preliminary biological evaluation of Cyathostemma argenteum, a malaysian plant used traditionally for the treatment of breast cancer

Abstract

Bioassay guided fractionation of the roots of Cyathostemma argenteum using the brine shrimp resulted in the isolation of two uncommon flavanones, 2,5-dihydroxy-7-methoxy flavanone 1 and 2,5-dihydroxy-6,7-dimethoxy flavanone 2 while the stem bark yielded the related compounds 5-hydroxy-7-methoxy flavone 3 and 5-hydroxy-6,7-dimethoxy flavone 4. The alkaloids liriodenine 5 and discretamine 6 as well as benzyl benzoate 7 were isolated from the roots and 6 was also isolated from the stembark. In cytotoxicity tests using four human breast cancer cell lines, 1 and 2 were weakly toxic to MCF-7 cells (IC(50) = 19.6 and 19.0 microM, respectively) but showed little activity against MCF-7 cells resistant to doxorubicin or against two oestrogen receptor-deficient cell lines. Compound 5, but not 6 and 7, was moderately cytotoxic against all four cell lines. These results are discussed in the context of the traditional use of C. argenteum in the treatment of breast cancer.

Scoulerine affects microtubule structure, inhibits proliferation, arrests cell cycle and thus culminates in the apoptotic death of cancer cells

“…Controversially, our results are in contrast with that reported by Khamis and colleagues. They determined only moderate cytotoxic activity of discretamine (scoulerine) with IC 50 over 3000 µM using four human breast cancer (MCF-7, MCF-7ADR, MDA-MB435 and MT-1) cell lines and MTT assay 13 . Here, however, scoulerine inhibited the proliferation of MCF-7 cells at 10 µM, as measured by means of the xCELLigence system in view of the cell-growth inhibition profile under real-time.…”

Review on pharmacological activities of liriodenine

“…Furthermore, liriodenine has been demonstrated to block cell cycle progression at the G2/M phase by reduction of G1 cyclin D1, accumulation of G2 cyclin B1 and the decrease of enzymatic activity of the cyclin B1/cyclin-dependent kinase 1 complex in human A549 lung cancer cells . Liriodenine, isolated from the roots of Cyathostemma argenteum, has been reported to exhibit moderate cytotoxic activity against breast cancer cell lines (Khamis et al, 2004). The anti-cell activity of liriodenine from Liriodendron tulipifera has been shown to have effects on human melanoma A375.S2 cells (Chiu et al, 2012).…”

Liriodenine enhances the apoptosis effect of valproic acid in human colon cancer cells through oxidative stress upregulation and Akt inhibition

“…In some anti-cancer studies, Li exerts a moderately cytotoxic effect against human breast cancer cell lines [6]. In Litreated human lung cancer cells, cell cycle progression is blocked at the G 2 /M phase by the reduction of G 1 cyclin D1 and the accumulation of G 2 cyclin B1.…”