Genistein in 1:1 inclusion complexes with ramified cyclodextrins: theoretical, physicochemical and biological evaluation.

Genistein is one of the most studied phytocompound in the class of isoflavones, presenting a notable estrogenic activity and in vitro and/or in vivo benefits in different types of cancer such as those of the bladder, kidney, lung, pancreatic, skin and endometrial cancer. A big inconvenience for drug development is low water solubility, which can be solved by using hydrophilic cyclodextrins. The aim of this study is to theoretically analyze, based on the interaction energy, the possibility of a complex formation between genistein (Gen) and three different ramified cyclodextrins (CD), using a 1:1 molar ratio Gen:CD. Theoretical data were correlated with a screening of both in vitro and in vivo activity. Proliferation of different human cancer cell lines, antimicrobial activity and angiogenesis behavior was analyzed in order to see if complexation has a beneficial effect for any of the above mentioned activities and if so, which of the three CDs is the most suitable for the incorporation of genistein, and which may lead to future improved pharmaceutical formulations. Results showed antiproliferative activity with different IC50 values for all tested cell lines, remarkable antimicrobial activity on Bacillus subtilis and antiangiogenic activity as revealed by CAM assay. Differences regarding the intensity of the activity for pure and the three Gen complexes were noticed as explained in the text. The data represent a proof that the three CDs can be used for furtherer research towards practical use in the pharmaceutical and medical field.

A comparative study on the biological activity of essential oil and total hydro-alcoholic extract of Satureja hortensis L.

Satureja hortensis L. presents an increased interest due to its chemical composition, abundant in monoterpenes, aglyconic and glycosylates flavonoids, and phenolic acids, leading to important biological activity. The present study compared the biological activity of volatile oil (VO) and total hydro-alcoholic extract (TE) of Satureja hortensis L. in terms of: i) antioxidant activity; ii) antimicrobial activity; and iii) viability, migration and proliferation on two healthy cell lines (keratinocytes-HaCaT and fibroblasts-1BR3) and two melanoma cell lines (human-A375 and murine-B164A5). Antioxidant activity of VO and TE showed maximal values around 72%. Antimicrobial screening highlighted the inhibitory capacity of VO against all seven tested bacteria strains, with the most pronounced effect against S. aureus and C. albicans, while TE exerted only a slight activity against three bacteria strains. VO showed greater efficacy than TE on both tumor cell lines (A375 and B164A5), the activity of the compounds was higher when low concentrations were used (5, 10 and 25 µM) while at high concentrations (50 and 100 µM) the percentages of viability were increased.

The Cytotoxic Effects of Betulin-Conjugated Gold Nanoparticles as Stable Formulations in Normal and Melanoma Cells.

Gold nanoparticles are currently investigated as theranostics tools in cancer therapy due to their proper biocompatibility and increased efficacy related to the ease to customize the surface properties and to conjugate other molecules. Betulin, [lup-20(29)-ene-3ß, 28-diol], is a pentacyclic triterpene that has raised scientific interest due to its antiproliferative effect on several cancer types. Herein we described the synthesis of surface modified betulin-conjugated gold nanoparticles using a slightly modified Turkevich method. Transmission electron microscopy (TEM) imaging, dynamic light scattering (DLS), scanning electron microscopy (SEM) and energy-dispersive X-ray spectroscopy (EDX) were used for the characterization of obtained gold nanoparticles. Cytotoxic activity and apoptosis assessment were carried out using the MTT and Annexin V/PI apoptosis assays. The in vitro results showed that betulin coated gold nanoparticles presented a dose-dependent cytotoxic effect and induced apoptosis in all tested cell lines.