RESUMEN
This research aimed to identify the phenolic profile and composition of the aerial parts of three native species used in traditional medicine in the Andean Altiplano of northern Chile: Clinopodium gilliesii (Benth.) Kuntze [Lamiaceae] (commonly known as Muña-Muña), Mutisia acuminata Ruiz & Pav. var. hirsuta (Meyen) Cabrera [Asteraceae] (commonly known as Chinchircoma), and Tagetes multiflora (Kunth), [Asteraceae] (commonly known as Gracilis), as well as to evaluate their potential inhibitory effects against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Polyphenolic enriched-extracts (PEEs) of the species were prepared and analyzed and the main components were quantified using HPLC-DAD. In total, 30 phenolic compounds were identified and quantified in all species, including simple phenolics, hydroxycinnamic acids, flavan-3-ols (monomers and polymers), flavanones, and flavonols. In addition, other main phenolics from the extracts were tentatively identified by ESI-MS-MS high-resolution analysis. T. multiflora extract showed the greatest anti-AChE and BChE activity in comparison with C. gilliesii and M. acuminata extracts, being the anti-AChE and BChE activity weak in all extracts in comparison to galantamine control. To comprise to better understand the interactions between cholinesterase enzymes and the main phenolics identified in T. multiflora, molecular docking analysis was conducted.
RESUMEN
Today, dendrimers are the main nanoparticle applied to drug delivery systems. The physicochemical characteristics of dendrimers and their versatility structural modification make them attractive to applied as a platform to bioactive molecules transport. Nanoformulations based on dendrimers enhance low solubility drugs, arrival to the target tissue, drugs bioavailability, and controlled release. This review describes the latter approaches on the transport of bioactive molecules based on dendrimers. The review focus is on the last therapeutic strategies addressed by dendrimers conjugated with bioactive molecules. A brief review of the latest studies in therapies against cancer and cardiovascular diseases, as well as future projections in the area, are addressed.
RESUMEN
Inclusion complexes based on ß-cyclodextrin (ß-CD) and antimicrobial compounds, were prepared by co-precipitation method, and characterized by entrapment efficiency (EE), thermal analysis, X-ray diffraction, 1H NMR spectroscopy, and water sorption. In addition, experiments associated to evaluate the effect of relative humidity on the release of active compounds and antifungal tests were performed. The analysis evidenced the encapsulation of active compounds into the ß-CD structure with EE of 91⯱â¯4.1% and 66⯱â¯2.1% for ß-CD/cinnamaldehyde and ß-CD/eugenol complexes, respectively. Additionally, high relative humidities favored the release of active compounds from inclusion complexes. On the other hand, inclusion complexes were able to control the growth of B. cinerea, which was evidenced by a reduction of its mycelialradial growth. Finally, specific interactions between the active compounds and ß-CD were evaluated through molecular dynamics simulation techniques. According to the obtained results, these complexes could be applied as additives in the design of antifungal packaging.