E. Manuela Garrido

Abstract Emerging threats to human health require a concerted effort to search for new treatment therapies. One of the biggest challenges is finding medicines with few or no side effects. Natural products have historically contributed to major advances in the field of pharmacotherapy, as they offer special characteristics compared to conventional synthetic molecules. Interest in natural products is being revitalized, in a continuous search for lead structures that can be used as models for the development of new medicines by the pharmaceutical industry. Chromone and chromanones are recognized as privileged structures and useful templates for the design of diversified therapeutic molecules with potential pharmacological interest. Chromones and chromanones are widely distributed in plants and fungi, and significant biological activities, namely antioxidant, anti-inflammatory, antimicrobial, antiviral, etc., have been reported for these compounds, suggesting their potential as lead drug candidates. This review aims to update the literature published over the last 6 years (2018-2023) regarding the natural occurrence and biological activity of chromones and chromanones, highlighting the recent findings and the perspectives that they hold for future research and applications namely in health, cosmetic, and food industries.

Abstract Adherence to topical treatments is low and is known to be influenced by the vehicle properties. Betamethasone dipropionate (BD) is an anti-inflammatory steroid, used in psoriasis treatment in the form of an ointment, cream, or solution. The aim of this work was to develop a new vehicle for BD, focusing on the preferences of patients with psoriasis as a strategy to improve treatment adherence. Two vehicles with an aqueous external phase were explored: an emulgel and a hydrogel based on a cyclodextrin inclusion complex used to improve the aqueous solubility of BD. Since BD solubilization was not fully achieved in the hydrogel, only the emulgel was selected for further characterization. This new vehicle (emulgel) is characterized by its white, shiny appearance and good spreading properties. In comparison with petrolatum, a lower residue, higher evaporation rate, lower stickiness, and reduced ability to stain polyester fabric were observed. This vehicle also showed shear thinning behavior. The impact of this new vehicle on adherence to topical treatments should be further confirmed in clinical settings.

Abstract The emergence of a large number of new psychoactive substance (NPS) on the global drug market poses a significant risk to public health and a challenge to drug control systems. Over the last decades, electrochemical sensing of illicit drugs has experienced a very significant growth, since these techniques can provide fast, portable, sensitive and low-cost detection alternatives for the analysis of drugs, metabolites and/or transformation products in different matrices. To understand and clarify the oxidative mechanism of piperazine designer drugs, the voltammetric profile of psychoactive piperazine derivatives 1-phenylpiperazine (PhPIP), 3-chlorophenylpiperazine (mCPP), 3-trifluoromethylphenylpiperazine (TFMPP), 4-fluorophenylpiperazine (pFPP) and benzylpiperazine (BZP) has been investigated at a glassy carbon electrode. The data found showed the crucial role of the aromatic amine, present in PhPIP, mCPP, pFPP and TFMPP molecular' structures, on the oxidative profiles. The voltammetric behavior of BZP is quite different from those found for the other piperazines under study due to the nature of the amine group present in BZP molecular' structure, benzylic instead of an aromatic amine. This work can be a helpful contribution to the ability to predict and identify metabolites and the development of new analytical approaches that can allow the rapid and specific quantitative detection of psychoactive piperazine derivatives.

Abstract The importance of isothiazole and of compounds containing the isothiazole nucleus has been growing over the last few years. Isothiazolinones are used in cosmetic and as chemical additives for occupational and industrial usage due to their bacteriostatic and fungiostatic activity. Despite their effectiveness as biocides, isothiazolinones are strong sensitizers, producing skin irritations and allergies and may pose ecotoxicological hazards. Therefore, their use is restricted by EU legislation. Considering the relevance and importance of isothiazolinone biocides, the present review describes the state-of-the-art knowledge regarding their synthesis, antibacterial components, toxicity (including structure-activity-toxicity relationships) outlines, and (photo)chemical stability. Due to the increasing prevalence and impact of isothiazolinones in consumer's health, analytical methods for the identification and determination of this type of biocides were also discussed.

Abstract Caffeic acid phenethyl ester (CAPE) is a bioactive polyphenolic compound obtained from propolis extract. Although it has a broad therapeutic potential, the bioavailability of CAPE is limited, due to reduced solubility and poor plasmatic stability. Efforts to reduce these pharmacokinetic drawbacks resulted in the synthesis of caffeic acid phenethyl amide (CAPA). Cyclodextrins have been proved as promising excipients for the formulation of active ingredients. Herein, we report the inclusion complexation behavior and binding ability of CAPE and CAPA with hydroxypropyl-beta-cyclodextrin (HP-beta-CD). The supramolecular interactions were examined through UV and FTIR spectroscopy, DSC, H-1 NMR and 2D ROESY. The CAPE/HP-beta-CD and CAPA/HP-beta-CD inclusion complexes stability constants were determined to be, respectively, 2911.6 and 584.6 M-1 in water and 2866.2 and 700.1 M-1 at physiological pH. The aqueous solubility increased notably, proving that HP-beta-CD can be potentially useful to improve the biological, chemical and physical properties of CAPE and CAPA.