Background

Cancer poses a health threat, with an increased incidence worldwide. Thus, it is essential to develop new natural anticancer agents. Dypsis pembana (H.E.Moore) Beentje & J.Dransf (DP) is an ornamental plant belonging to the family Arecaceae. This study aimed to isolate and identify phytoconstituents from the leaves of this plant and evaluate their in vitro cytotoxic activities.

Methods

Different chromatographic techniques were applied to fractionate the hydro-alcoholic extract of DP and separate the major phytoconstituents. The isolated compounds were structurally elucidated based on their physical and spectroscopic data. The in vitro cytotoxic activities of the crude extract and fractions thereof were evaluated against human colon carcinoma (HCT-116), human breast carcinoma (MCF-7), and human hepatocellular carcinoma (HepG-2) cell lines via MTT assay. Moreover, selected isolates were tested against HepG-2 cell line. Molecular docking analysis was performed to investigate the interactions of these compounds with two potential targets, the human topoisomerase IIα and cyclin-dependent kinase 2 enzymes.

Results

Thirteen diverse compounds were reported for the first time from DP, providing significant chemotaxonomic biomarkers. Among tested compounds, vicenin-II (7) was the most cytotoxic against HepG-2 cell line, with an IC₅₀ value of 14.38 µg/mL, followed by isovitexin (13) (IC₅₀ of 15.39 µg/mL). These experimental findings were complemented by molecular docking, which demonstrated that vicenin-II exhibited superior enzyme-binding affinities to the studied vital targets and shed light on the structure–activity relationships among the investigated flavone-C-glycosides members.

Conclusion

The phytochemical profile of DP was characterized for the first time, reflecting chemotaxonomic data about the concerned species, genus, or even the family. Biological and computational findings revealed that vicenin-II and isovitexin are possible lead structures as inhibitors of the human topoisomerase IIα and cyclin-dependent kinase 2 enzymes.

Quercetin is a bioactive flavonoid widely used as a health supplement. Quercetin was formulated in different dermatological preparations
as gel, emulgel and microemulsion gel. Different gel bases were used for the preparation of quercetin gel as sodium carboxymethylcellulose
(NaCMC), Carbopol 934 and Pluronic F-127. Also different formulae of both emulgel and microemulsion gel were prepared using different gel
bases and surfactants. These formulations were evaluated for their drug content, in vitro release of the drug from cellophane membrane and skin
permeability through hairless mouse skin. The antibacterial activity against Gram positive and Gram negative organisms was also studied. The
results of the drug release indicated that the highest release was obtained from the microemulsion gel followed by gel and emulgel, respectively.
The same results were obtained for drug penetration through hairless mouse skin. Analysis of the data according to different kinetic mechanisms
revealed that the release pattern of the drug from the tested bases followed zero-order and the Higuchi diffusion model. Results also indicated an
excellent activity against all tested organisms and the inhibition zone was dependent on the type of formulation used.