Apoptosis-mediated antiproliferative activity of friedolanostane triterpenoid isolated from the leaves of Garcinia celebica against MCF-7 human breast cancer cell lines.

The leaves of Garcinia celebica strongly inhibit the proliferation of MCF-7 human breast adenocarcinoma cell lines. The present study focused on investigating the active anticancer and antiproliferative compound from the G. celebica leaves and assessing its mechanism of action. Ethanol extracts of G. celebica were fractionated based on their polarity using n-hexane, ethyl acetate and water. The antiproliferative properties were tested in vitro against MCF-7 human breast cancer cell lines using the 3-(4,5-dimethylthiazolyl-2)-2,5-diphenyltetrazolium bromide assay. The active compound was subsequently isolated using column chromatography and identified by nuclear magnetic resonance. The characterized compound was also tested for its antiproliferative properties and the mechanism by which it induces apoptosis in MCF-7 cells by western blot analysis of the activated apoptotic proteins. This resulted in the isolation of a friedolanostane triterpenoid, which was determined to be methyl-3α, 23-dihydroxy-17,14-friedolanstan-8,14,24-trien-26-oat. This compound inhibited MCF-7 cell proliferation in a time- and dose-dependent manner with IC50 values of 82 and 70 µM for the 24 and 48 h treatments, respectively. Furthermore, the western blot analysis suggested that the compound exerted its anticancer activities by promoting apoptosis through the inhibition of the oncogenic protein Akt, thereby increasing the expression of poly (ADP-ribose) polymerase (PARP) protein. These results suggest that methyl-3α,23-dihydroxy-17,14-friedolanstan-8,14,24-trien-26-oat is the anticancer compound found in G. celebica, providing a basis for its potential use in cancer disease management.

Apoptosis induced in MCF-7 human breast cancer cells by 2',4'-dihydroxy-6-methoxy-3,5-dimethylchalcone isolated from Eugenia aquea Burm f. leaves.

During a previous study that aimed to identify anticancer agents within primate-consumed plants, the present group identified that Eugenia aquea (E. aquea) possessed potential as a source of anticancer agents. The ethanol extract of E. aquea leaves exhibited strong inhibitory activity against the proliferation of the human breast adenocarcinoma MCF-7 cell line. The inhibition of proliferation was determined using an MTT assay. The present study was performed to isolate the active compound within the E. aquea leaves that generated the aforementioned activity, and resulted in the isolation of 2',4'-dihydroxy-6-methoxy-3,5-dimethylchalcone, which was identified through the analysis of spectroscopic data. This compound was examined for its inhibitory activity against the MCF-7 cell line using a MTT assay, and the ability of 2',4'-dihydroxy-6-methoxy-3,5-dimethylchalcone to induce apoptosis through the activation of the poly(adenosine diphosphate-ribose) polymerase (PARP) protein was also investigated. The results of the present study revealed that the isolated compound inhibited cell proliferation in a dose-dependent manner, possessed an IC50 of 74.5 µg/ml (250 µM) and promoted apoptosis via the activation of PARP. It was concluded that these results indicated a requirement for additional investigations into 2',4'-dihydroxy-6-methoxy-3,5-dimethylchalcone in order to provide a basis for the use of this compound in the management of cancer.