Relevance of Fluorinated Ligands to the Design of Metallodrugs for Their Potential Use in Cancer Treatment.

Fluorination of pharmaceutical agents has afforded crucial modifications to their pharmacological profiles, leading to important advances in medicinal chemistry. On the other hand, metallodrugs are considered to be valuable candidates in the treatment of several diseases, albeit with the caveat that they may exhibit pharmacological disadvantages, such as poor water solubility, low bioavailability and short circulating time. To surmount these limitations, two approaches have been developed: one based on the design of novel metallodrug-delivering carriers and the other based on optimizing the structure of the ligands bound to the metal center. In this context, fluorination of the ligands may bring beneficial changes (physicochemical and biological) that can help to elude the aforementioned drawbacks. Thus, in this review, we discuss the use of fluorinated ligands in the design of metallodrugs that may exhibit potential anticancer activity.

Mechanochemistry: A Green Approach in the Preparation of Pharmaceutical Cocrystals.

Mechanochemistry is considered an alternative attractive greener approach to prepare diverse molecular compounds and has become an important synthetic tool in different fields (e.g., physics, chemistry, and material science) since is considered an ecofriendly procedure that can be carried out under solvent free conditions or in the presence of minimal quantities of solvent (catalytic amounts). Being able to substitute, in many cases, classical solution reactions often requiring significant amounts of solvents. These sustainable methods have had an enormous impact on a great variety of chemistry fields, including catalysis, organic synthesis, metal complexes formation, preparation of multicomponent pharmaceutical solid forms, etc. In this sense, we are interested in highlighting the advantages of mechanochemical methods on the obtaining of pharmaceutical cocrystals. Hence, in this review, we describe and discuss the relevance of mechanochemical procedures in the formation of multicomponent solid forms focusing on pharmaceutical cocrystals. Additionally, at the end of this paper, we collect a chronological survey of the most representative scientific papers reporting the mechanochemical synthesis of cocrystals.

In Vitro and In Vivo Antifungal Activity of Clove (Eugenia caryophyllata) and Pepper (Piper nigrum L.) Essential Oils and Functional Extracts Against Fusarium oxysporum and Aspergillus niger in Tomato (Solanum lycopersicum L.).

In this study, hydrodistillation was used to obtain essential oils (EOs) from pepper (Piper nigrum L.) and clove (Eugenia caryophyllata) and co-hydrodistillation (addition of fatty acid ethyl esters as extraction co-solvents) was used to obtain functional extracts (FEs). Antifungal activity of EOs and FEs was evaluated by determination of minimum inhibitory concentration (MIC) against Fusarium oxysporum and Aspergillus niger. The results showed that pepper (Piper nigrum) and clove (Eugenia caryophyllata) essential oils and their functional extracts are effective in vitro at concentrations from 400 to 500 ppm after 10 days of culturing. The essential oils and functional extracts were used on tomato fruit samples at three different concentrations: 350, 400, and 450 ppm5. Clove essential oil reduced the growth of Aspergillus niger from 50% to 70% and Fusarium oxysporum to 40%. The functional extracts (FEs) of clove and pepper, mixed with ethyl decanoate (FEs-C10), were the best combination for protecting the tomato fruit in vivo against both phytopathogenic fungi. Gas chromatography-mass spectrometry (GC-MS) was used to identify eugenol as the principal compound in clove oil and limonene, sabinene, and ß-caryophyllene in pepper oil.