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- Antitumor Activity of Ionic Liquids Based on AmpicillinPublication . Ferraz, Ricardo; Costa-Rodrigues, Joao; Fernandes, Maria H.; Santos, Miguel M.; Marrucho, Isabel M.; Rebelo, Luís Paulo N.; Prudêncio, Cristina; Noronha, João Paulo; Petrovski, Željko; Branco, Luís C.Significant antiproliferative effects against various tumor cell lines were observed with novel ampicillin salts as ionic liquids. The combination of anionic ampicillin with appropriate ammonium, imidazolium, phosphonium, and pyridinium cations yielded active pharmaceutical ingredient ionic liquids (API-ILs) that show potent antiproliferative activities against five different human cancer cell lines: T47D (breast), PC3 (prostate), HepG2 (liver), MG63 (osteosarcoma), and RKO (colon). Some API-ILs showed IC50 values between 5 and 42 nm, activities that stand in dramatic contrast to the negligible cytotoxic activity level shown by the ampicillin sodium salt. Moreover, very low cytotoxicity against two primary cell lines—skin (SF) and gingival fibroblasts (GF)—indicates that the majority of these API-ILs are nontoxic to normal human cell lines. The most promising combination of antitumor activity and low toxicity toward healthy cells was observed for the 1-hydroxyethyl-3-methylimidazolium–ampicillin pair ([C2OHMIM][Amp]), making this the most suitable lead API-IL for future studies.
- Integração do metabolismo do tecido ósseoPublication . Costa-Rodrigues, João
- Can lycopene be considered an effective protection against cardiovascular disease?Publication . Costa-Rodrigues, João; Pinho, O.; Monteiro, PedroLycopene is a bioactive component mainly found in tomato. It is characterized by a high antioxidant potential, the highest among carotenoids. Mainly due to this property, lycopene has been suggested to display many beneficial effects, including its potential cardioprotective role. Despite some contradictory observations, which appear to be mainly caused by discrepancies in the different experimental protocols applied in the different studies, growing evidence points to clear benefits of lycopene in the maintenance of cardiovascular function and health. The knowledge about lycopene's preventive effects in atherosclerosis, and other cardiovascular diseases, must be translated into changes in food patterns, aiming to increase the consumption of tomato, tomato-containing products, or other foods with high lycopene content, which can have an important impact on cardiovascular disease, particularly in countries where this represents a major public health concern.
- Testing the variability of PSA expression by different human prostate cancer cell lines by means of a new potentiometric device employing molecularly antibody assembled on graphene surfacePublication . Rebelo, Tânia S.C.R.; Noronha, João P.; Galésio, Marco; Santos, Hugo; Diniz, Mário; Sales, M. Goreti F.; Fernandes, Maria H.; Costa-Rodrigues, JoaoProstate Specific Antigen (PSA) is widely used as a biomarker for prostate cancer. Recently, an electrochemical biosensor for PSA detection by means ofmolecularly imprinted polymers (MIPs)was developed. Thiswork evaluated the performance and the effectiveness of that PSA biosensor in screening the biomarker PSA in biological mediawith complex composition, collected fromdifferent human prostate cell line cultures. For that, the prostate cancer LNCaP and PC3 cells, and the non-cancerous prostate cell line PNT2 were cultured for 2, 7 and 14 days in eitherα-MEMor RPMI in the presence of 10% or 30% fetal bovine serum. Human gingival fibroblastswere used as a non-cancerous non-prostatic control. The different culture conditions modulated cellular proliferation and the expression of several prostate markers, including PSA. The electrochemical biosensor was able to specifically detect PSA in the culture media and values obtained were similar to those achieved by a commercial Enzyme- Linked Immunosorbent Assay (ELISA) kit, the most commonly used method for PSA quantification in prostate cancer diagnosis. Thus, the tested biosensor may represent a useful alternative as a diagnostic tool for PSA determination in biological samples.
- Complex osteoclastogenic inductive effects of nicotine over hydroxyapatitePublication . Costa-Rodrigues, João; Rocha, Isabel; Fernandes, Maria H.Cigarette smoke is associated to pathological weakening of bone tissue, being considered an important playmaker in conditions such as osteoporosis and periodontal bone loss. In addition, it is also associated with an increased risk of failure in bone regeneration strategies. The present work aimed to characterize the effects of nicotine on human osteoclastogenesis over a hydroxyapatite substrate. Osteoclast precursors were maintained in the absence or presence of the osteoclastogenesis enhancers M-CSF and RANKL, and were further treated with nicotine levels representative of the concentrations observed in the plasma and saliva of smokers. It was observed that nicotine at low concentrations elicit an increase in osteoclast differentiation, but only in the presence of M-CSF and RANKL it was also able to significantly increase the resorbing ability of osteoclasts. A slight downregulation of NFkB pathway and an increase in the production of TNF-α and, particularly PGE2, were involved in the observed effects of nicotine. At high concentrations, nicotine revealed cytotoxic effects, causing a decrease in cell density. In conclusion, nicotine at levels found in the plasma of the smokers, has the ability to act directly on osteoclast precursors, inducing its osteoclastogenic differentiation. The stimulatory behavior appears to be dependent on the stage of osteoclastic differentiation of the precursor cells, which means, in the absence of M-CSF and RANKL, it only favors the initial stages of osteoclast differentiation, while in the presence of the growth factors, a significant increase in their resorbing ability is also achieved.
- Antiproliferative organic salts derived from betulinic acid: Disclosure of an ionic liquid selective against lung and liver cancer cellsPublication . Silva, Ana Teresa; Cerqueira, Maria João; Prudêncio, Cristina; Fernandes, Maria Helena; Costa-Rodrigues, João; Teixeira, Cátia; 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.
- Nutrition education: challenges from a growing digital and social media ecosystemPublication . Costa-Rodrigues, JoãoThe present digital revolution that we are living is making dramatic changes not only in entertainment but especially in education. A few decades ago, entertainment/education was consumed passively, and was created by companies or experts that decided what people should see and learn. Nowadays, everyone can be both a consumer and a creator, and the created contents can virtually reach any people in any place. Another important issue regarding all of this changes is the availability and accessibility of digital media interfaces and devices, especially in children and teenagers. One of the contents that is more likely to be searched in digital media are nutrition-related issues. Brands and marketers have realized it and there is a strong investment in this field. Unfortunately, due to that there is a growing number of digital platforms that offer information about food and nutrition without any scientific background. Even worse, in a significant percentage of cases, the information is created and transmitted without the intervention of nutritionists.
- Involving forensic students in integrative learning—a project proposalPublication . Teixeira, A.; Azevedo, A.; Pérez-Mongiovi, D.; Caldas, I. M.; Costa-Rodrigues, JoãoIn our experience, university students enrolling in health science and forensic science degrees show difficulty in retaining and integrating basic scientific knowledge learned in their first academic year. Furthermore, in the forensic sciences case, many students have oversimplified and unrealistic expectations as a result of the exposure to crime TV shows, internet blogs, and other social media platforms. Our pedagogical proposal is focused on second-year university students, aiming at promoting effective learning and the integration of scientific knowledge from previous courses, in this particular example, molecular and cell biology and biochemistry, with more advanced forensic courses, such as forensic anthropology and odontology. Teams composed of students and tutors from the teaching staff, with the help of dichotomous keys, are challenged to analyze a crime scene and choose the relevant evidence to further investigate, determine the scientific approach, execute the experimental work, interpret the results and, finally, resolve the case. To assess the pedagogical advantages and the receptivity of this project, a survey is to be carried out among students, and respective statistical analysis is also proposed. Finally, we hope this project outline may be adapted to other subjects, and, therefore, be used to address different pedagogical questions in forensic studies.
- A Novel Approach for Bisphosphonates: Ionic Liquids and Organic Salts from Zoledronic AcidPublication . Teixeira, Sónia; Santos, Miguel M.; Ferraz, Ricardo; Prudêncio, Cristina; Fernandes, Maria H.; Costa-Rodrigues, Joao; Branco, Luís C.Novel ionic liquids and organic salts based on mono- or dianionic zoledronate and protonated superbases, choline and n-alkylmethylimidazolium cations, were prepared and characterized by spectroscopic and thermal analyses. Most of the prepared salts display amorphous structures and very high solubility in water and saline solutions, especially the dianionic salts. Among the zoledronate-based ionic compounds, those containing choline [Ch] and methoxyethylmethylimidazolium [C3 OMIM] cations appear to have significant cytotoxicity against human osteosarcoma cells (MG63) and low toxicity toward healthy skin fibroblast cells. Because osteosarcoma is a bone pathology characterized by an increase in bone turnover rate, the results presented herein may be a promising starting point for the development of new ionic pharmaceutical drugs against osteosarcoma.
- Modulation of human osteoclastogenesis and osteoblastogenesis by lycopenePublication . Costa-Rodrigues, João; Fernandes, Maria Helena; Pinho, Olívia; Monteiro, PedroLycopene is a lipid-soluble pigment that is mainly found in tomato. It is the carotenoid that presents the highest antioxidant potential, and due to that, it has been implicated in a decrease of the risk of several oxidative-stress-related disorders, such as cancer, inflammatory diseases and osteoporosis. Nevertheless, at the present, there is no detailed information about how lycopene affects bone metabolism. The aim of the present work was to characterize the cellular and molecular effects of lycopene on human osteoclast and osteoblast differentiation and function. It was observed that lycopene, at levels found in plasma after the ingestion of lycopene-containing products, decreased osteoclast differentiation but did not affect cell density/survival; calcium-phosphate resorbing ability was also decreased. On the other hand, osteoblast proliferation (via a decrease on apoptosis) and differentiation were increased in the presence of lycopene. The observed effects in both cell types appeared to be related to significant changes in MEK signaling pathway, but also in protein kinase C pathway in osteoclasts and NFkB signaling in osteoblasts. In conclusion, lycopene appears to promote an anabolic state of bone metabolism, stimulating osteoblastogenesis and inhibiting osteoclastogenesis, which may contribute to the promotion of a proper health status of bone tissue. This information might be relevant for the prevention and delay in the progression of osteolytic bone conditions.
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