Butyrospermum parkii butter increased the photostability and in vivo SPF of a molded sunscreen system.

BACKGROUND: Ultraviolet (UV) radiation exposure is related to skin and lip tumors. Therefore, the development of photoprotective lipstick formulations is of utmost importance. AIMS: Considering the biological properties of Shea butter (Butyrospermum parkii), we assessed its potential as an adjuvant in a molded lipstick sunscreen system by in vivo tests and photostability. PATIENTS/METHODS: Shea butter was used in a photoprotective lipstick formulation at two different concentrations (10.0% and 15.0% w/w) associated with ethylhexyl methoxycinnamate (EHM) and titanium dioxide. Skin compatibility was assessed in vivo. The in vivo SPF value was determined according to the current recognized method. Additionally, the photostability of EHM was determined by high-performance liquid chromatography. RESULTS: By the cutaneous compatibility, the product presented no interference with skin barrier and no adverse reactions, thus proving its safety. The in vivo SPF assay showed that the highest concentration of Shea butter increased the in vivo SPF value of the sample by 35%, demonstrating it to be a booster in photoprotective lipstick formulations. Also, Shea butter was proved to enhance the photostability of EHM, a commonly used UVB filter available in several countries. CONCLUSION: Shea butter increased the photostability and in vivo SPF of a molded lipstick sunscreen.

Influence of Shea (Butyrospermum parkii) butter, TiO2 and ethylhexyl methoxycinnamate on physical parameters and in vitro photoprotective efficacy.

BACKGROUND: The development of photoprotective lipsticks containing natural bioactive compounds is a relevant current strategy to increase sun protection factor (SPF) value and lower the concentration of chemical UV filters, known for promoting sensitivity reactions. AIMS: Twelve photoprotective lipsticks were developed by Design of Experiment (DOE) and characterized to verify the influence of Shea butter (Butyrospermum parkii), titanium dioxide (TiO2 ), and ethylhexyl methoxycinnamate (EHM) on physical parameters and in vitro photoprotective efficacy. METHODS: The influence of Shea butter, TiO2, and EHM was evaluated by several parameters, such as melting point, colorimetry, thermal analysis by DSC, texture analysis, and sunscreen activity estimated in vitro. RESULTS: The construction of prediction models was possible for the following responses: maximum force by the cantilever test at 25 and 45°C; maximum distance by hardness test at 25°C; slope value at 25 and 45°C by the cantilever test; and UVA/UVB ratio and in vitro SPF. TiO2 and EHM contributed to changes on the in vitro SPF value; however, unexpectedly, Shea butter had no influence on this efficacy parameter. CONCLUSION: The assay allowed us to observe the influence of the variables in the analysis and to develop a response prediction model for some of the parameters assessed.

Synthesis, Molecular Modeling, and Evaluation of Novel Sulfonylhydrazones as Acetylcholinesterase Inhibitors for Alzheimer's Disease.

Alzheimer's disease (AD) is the most common type of dementia and related to the degeneration of hippocampal cholinergic neurons, which dramatically affects cognitive ability. Acetylcholinesterase (AChE) inhibitors are employed as drugs for AD therapy. Three series of sulfonylhydrazone compounds were designed, and their ability to inhibit AChE was evaluated. Fifteen compounds were synthesized and twelve of them had IC50 values of 0.64-51.09 µM. The preliminary structure-activity relationships indicated that the methylcatechol moiety and arylsulfonyl substituents generated better compounds than both the benzodioxole and alkylsulfonyl chains. Molecular dynamics studies of compound 6d showed that the interaction with the peripheral binding site of AChE was similar to donepezil, which may explain its low IC50 (0.64 µM). Furthermore, the drug-likeness of 6d suggests that the compound may have appropriate oral absorption and brain penetration. Compound 6d also presented antiradical activity and was not cytotoxic to LL24 cells, suggesting that this compound might be considered safe. Our findings indicate that arylsulfonylhydrazones may be a promising scaffold for the design of new drug candidates for the treatment of AD.