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- Antibacterial activity of ionic liquids based on betalactamantibiotics against resistant bacteriaPublication . Dias, Vitorino; Santos, Miguel; PrudĂȘncio, Cristina; Noronha, JoĂŁo P.; Grilo, InĂȘs R.; Sobral, Rita G.; Dias, Ana Rita; Branco, LuĂs C.; Ferraz, RicardoThe cases of antibiotic resistance are increasing and becoming more and more common, giving rise to a new problem for public health. Therefore, the discovery of new antibiotics is important and necessary.
- Antiproliferative organic salts derived from betulinic acid: Disclosure of an ionic liquid selective against lung and liver cancer cellsPublication . Silva, Ana Teresa; Cerqueira, Maria JoĂŁo; PrudĂȘncio, Cristina; Fernandes, Maria Helena; Costa-Rodrigues, JoĂŁo; Teixeira, CĂĄtia; Gomes, Paula; Ferraz, RicardoIn the last few years, we have been witnessing an increasing interest in ionic liquids (ILs) and organic salts, given their potential applications in biological and pharmaceutical sciences. We report the synthesis and in vitro evaluation of novel organic salts combining betulinate, known for its anticancer properties, with antimalarial drugs, primaquine, chloroquine, and mepacrine, and also with the trihexyltetradecylphosphonium ([P6,6,6,14]) cation. The salts were screened for their in vitro activity against tumor lines HepG2 (liver), MG63 (osteosarcoma), T47D (breast), A459 (lung), and RKO (colon), and also on normal human fibroblasts. All betulinates prepared displayed antiproliferative properties, with the trihexyltetradecylphosphonium betulinate standing out for its higher selectivity. This unprecedented disclosure of a betulinic acid (BA)-derived IL with selective antitumor activity constitutes a relevant first step toward development of novel anticancer therapies based on BA-derived IL.
- Surfing the third wave of ionic liquids: a brief review on the role of surface-active ionic liquids in drug development and DeliveryPublication . Silva, Ana Teresa; Teixeira, CĂĄtia; PrudĂȘncio, Cristina; Marques, Eduardo F.; Gomes, Paula; Ferraz, RicardoThe relevance of ionic liquids (ILs) is now well established in many fields, as their unique properties make them appealing as 1)â greener alternatives to organic solvents (first-generation ILs), 2)â tunable task-specific materials (second-generation ILs), and 3)â multifunctional players in life and pharmaceutical sciences (third-generation ILs). This third wave of ILs encompasses a wide range of compounds, from bioactive molecules with single or even dual therapeutic action, to potential ingredient molecules for drug formulation and transport systems. In this context, the focus of this review is the emergent role of surface-active ionic liquids (SAILs) in drug development and delivery.
- Tackling bacterial resistance using antibiotics as ionic liquids and organic saltsPublication . Santos, Miguel M.; Grilo, InĂȘs R.; Ferraz, Ricardo; Madeira, Diogo A.; Soares, BĂĄrbara M.; InĂĄcio, NĂșria; Pinheiro, LuĂs; Petrovski, Zeljko; PrudĂȘncio, Cristina; Sobral, Rita G.; Branco, LuĂs C.Bacterial resistance to current antibiotics has a major impact on worldwide human health, leading to 700K deaths every year. The development of novel antibiotics did not present significant progress, namely regarding clinical trials, over the last years due to low returns. Thus, innovative alternatives must be devised to tackle the continuous rise of antimicrobial resistance. Ionic Liquids and Organic Salts from Active Pharmaceutical Ingredients (API-OSILs) have risen in academia for over 10 years as an efficient formulation for drugs with low bioavailability and permeability, as well as reduction or elimination of polymorphism, thereby potentially enhancing their pharmaceutical efficiency. To the best of our knowledge, our group is the first to perform research on the development of API-OSILs from antibiotics as a way to improve their efficiency. More specifically, we have successfully combined ampicillin, penicillin and amoxicillin as anions with biocompatible organic cations such as choline, alkylpyridiniums and alkylimidazoliums. In this communication, we present our latest developments in the synthesis and physicochemical (DSC) characterization of OSILs from these antibiotics, in addition to in vitro antimicrobial activity data, in particular towards MRSA and multi-resistant E. coli, as well as sensitive strains of gram-positive and gram-negative bacteria.
- Ionic liquids as active pharmaceutical ingredientsPublication . Ferraz, Ricardo; Branco, LuĂs C.; PrudĂȘncio, Cristina; Noronha, JoĂŁo Paulo; Petrovski, ĆœeljkoIonic liquids (ILs) are ionic compounds that possess a melting temperature below 100â°C. Their physical and chemical properties are attractive for various applications. Several organic materials that are now classified as ionic liquids were described as far back as the mid-19th century. The search for new and different ILs has led to the progressive development and application of three generations of ILs: 1)â The focus of the first generation was mainly on their unique intrinsic physical and chemical properties, such as density, viscosity, conductivity, solubility, and high thermal and chemical stability. 2)â The second generation of ILs offered the potential to tune some of these physical and chemical properties, allowing the formation of âtask-specific ionic liquidsâ which can have application as lubricants, energetic materials (in the case of selective separation and extraction processes), and as more environmentally friendly (greener) reaction solvents, among others. 3)â The third and most recent generation of ILs involve active pharmaceutical ingredients (API), which are being used to produce ILs with biological activity. Herein we summarize recent developments in the area of third-generation ionic liquids that are being used as APIs, with a particular focus on efforts to overcome current hurdles encountered by APIs. We also offer some innovative solutions in new medical treatment and delivery options.
- Recycling Old Antibiotics with Ionic LiquidsPublication . PrudĂȘncio, Cristina; Vieira, MĂłnica; Van der Auweraer, Seppe; Ferraz, RicardoAntibiotics are considered one of the great âmiraclesâ of the 20th century. Now in the 21st century in the post-antibiotic era, the miracle is turning into a nightmare, due to the growing problem of the resistance of microorganisms to classic antimicrobials and the non-investment by the pharmaceutical industry in new antimicrobial agents. Unfortunately, the current COVID-19 pandemic has demonstrated the global risks associated with uncontrolled infections and the various forms of impact that such a pandemic may have on the economy and on social habits besides the associated morbidity and mortality. Therefore, there is an urgent need to recycle classic antibiotics, as is the case in the use of ionic liquids (ILs) based on antibiotics. Thus, the aim of the present review is to summarize the data on ILs, mainly those with antimicrobial action and especially against resistant strains. The main conclusions of this article are that ILs are flexible due to their ability to modulate cations and anions as a salt, making it possible to combine the properties of both and multiplying the activity of separate cations and anions. Also, these compounds have low cost methods of production, which makes it highly attractive to explore them, especially as antimicrobial agents and against resistant strains. ILs may further be combined with other therapeutic strategies, such as phage or lysine therapy, enhancing the therapeutic arsenal needed to fight this worldwide problem of antibacterial resistance. Thus, the use of ILs as antibiotics by themselves or together with phage therapy and lysine therapy are promising alternatives against pathogenic microorganisms, and may have the possibility to be used in new ways in order to restrain uncontrolled infections.
- Ecotoxicological effect of 1-(2-hydroxyethyl)-3- methylimidazolium chloride and cetylpyridinium chloride towards the microalgae Chlorella vulgarisPublication . Pacheco, Elisabete; Ferraz, Ricardo; PrudĂȘncio, Cristina; Barros, PiedadeIonic liquids (ILs) are salts that are stable over their melting temperature and are made exclusively of ions. ILs have received considerable interest due to their unique properties. The growing interest in ILs predicts an increase of their manufacture and use at industrial scale, which may result in the increased release of these compounds into the environment. In the past years, ILs have been used as a greener alternative to hazardous conventional solvents.
- Bioactivity of ionic liquids based on valproate in SH-SY5Y human neuroblastoma cell linePublication . Dias, Ana Rita; Ferraz, Ricardo; Costa-Rodrigues, JoĂŁo; Santos, Andreia F. M.; Jacinto, Manuel L.; PrudĂȘncio, Cristina; Noronha, JoĂŁo Paulo; Branco, LuĂs C.; Petrovsk, ĆœeljkoThe search for alternative and effective therapies to fight cancer is one of the main goals of the pharmaceutical industry. Recently, ionic liquids (ILs) have emerged as potential therapeutic agents with antitumor properties. The goal of this study was to synthesize and evaluate the bioactivity of different ILs coupled with the active pharmaceutical ingredient (API) valproate (VPA) as an antitumor agent. The toxicity of the prepared ionic liquids was evaluated by the MTT cell metabolic assay in human neuroblastoma SH-SY5Y and human primary Gingival Fibroblast (GF) cell lines, in which they showed inhibitory effects during the study period. In addition, low cytotoxicity against GF cell lines was observed, suggesting that these compounds are not toxic to human cell lines. [C2OHDMiM][VPA] demonstrated an outstanding antitumor activity against SH-SY5Y and lower activity against the non-neoplastic GF line. The herein assessed compounds played an important role in the modulation of the signaling pathways involved in the cellular behavior. This work also highlights the potential of these ILs-API as possible antitumor agents.
- Bioactivity of ionic liquidsPublication . Ferraz, Ricardo; Teixeira, CĂĄtia; Gomes, Paula; PrudĂȘncio, CristinaIonic liquids (ILs) were discovered a century ago, but it was only three decades ago that they started to catch the attention of the scientific commu- nity. ILs are defined as organic salts composed of an organic cation and an organic or inorganic anion2,3 that are stable below their melting point.
- Production and characterization of natural and synthetic compounds for treating hormone resistant tumorsPublication . Oliveira, Ana Isabel; Pinho, ClĂĄudia; Vieira, MĂłnica; Ferraz, Ricardo; Cruz, Agostinho; PrudĂȘncio, CristinaFrom previous and on-going studies, natural compounds/extracts isolated from Taraxacum hispanicum, Ionic Liquids (ILs) based on ampicillin and quinoxalines emerged as potential anticancer. Although described as potentially antitumor compounds, the mechanisms undergoing cytotoxicity remain unknown. Therefore, production of these kind of compounds were carry out in order to have a better understanding of their bioactivity.