The flavonoid, kaempferol-3-O-apiofuranosyl-7-O-rhamnopyranosyl, as a potential therapeutic agent for breast cancer with a promoting effect on ovarian function.

It is widely known that breast cancer cells eventually develop resistance to hormonal drugs and chemotherapies, which often compromise fertility. This study aimed to investigate the effect of the flavonoid, kaempferol-3-O-apiofuranosyl-7-O-rhamnopyranosyl (KARP), on 1) the viability of MCF-7 breast cancer cells and 2) ovarian function in rats. A dose-dependent decrease in MCF-7 cell survival was observed, and the IC50 value was found to be 48 µg/ml. Cells in the control group or those exposed to increasing concentrations of KARP experienced a similar generation of reactive oxygen species and induction of apoptosis. For the rats, estradiol levels correlated negatively to KARP dosages, although a recovery was obtained at administration of 30 mg/kg per day. Noteworthily, when compared against the control, this dosage led to significant increases in mRNA levels for CYP19, CYP17a, CCND2, GDF9, and INSL3 among the treatment groups, and ER1 and ER2 mRNA levels decreased in a dose-dependent manner. KARP shows great promise as an ideal therapy for breast cancer patients since it induced apoptosis and autophagy in cancerous cells without harming fertility in our animal model. Future investigations on humans are necessary to substantiate these findings and determine its efficacy as a general line of treatment.

Deverra tortuosa (Desf.) DC from Saudi Arabia as a new source of marmin and furanocoumarins derivatives with α-glucosidase, antibacterial and cytotoxic activities.

Deverra tortuosa (Desf.) DC (Syn. Pituranthos tortusus (Desf.) Benth. & Hook.f.) is a species belonging to the Apiaceae family that is common in the Northern Region of Saudi Arabia. The plant is well known in traditional medicine along the Arabian ecoregion. In the framework of the present study, the crude extract of n-hexane and ethyl acetate of the seeds were fractionated to purify major bioactive secondary metabolites. Five compounds were identified for the first time from the seeds of D. tortuosa: Marmin 1, Pituranthoside 2, Isoimperatorin 3, Bergapten 4 and Isopimpinellin 5. Their structures were elucidated using 1D and 2D NMR, (ESI)-MS and IR spectroscopic analyses. The cytotoxic, α-glucosidase and antibacterial activities of the pure phytochemicals were also evaluated.