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1.
Inflammopharmacology ; 2017 May 19.
Artigo em Inglês | MEDLINE | ID: mdl-28526927

RESUMO

It has been demonstrated that peripheral infections accompanied by neuroinflammation may modify brain development or affect normal brain aging and represent major risk factors for the development of neurological disorders. A wide range of synthetic and natural compounds with anti-inflammatory properties have been evaluated in animal models of neuroinflammation and neurodegeneration as an adjuvant therapeutic strategy. In the present study we have demonstrated for the first time that sodium thiosulphate (STS), a known antidote approved for treatment of certain medical conditions, is capable of reducing brain inflammation caused by systemic LPS administration. STS reduced brain levels of pro-inflammatory cytokine interleukin-1ß (IL-1ß), cyclooxygenase-2 (COX-2), ionized calcium binding adaptor molecule 1 (Iba-1) and 18 kDa translocator protein (TSPO) in an animal model of systemic LPS-induced neuroinflammation. In addition, we demonstrated for the first time elevated TSPO expression in retinal ganglion cells layer after peripheral LPS challenge and inhibition of ocular TSPO expression after treatment with STS. We think that STS may be used as an adjuvant anti-inflammatory therapy for many pathological conditions associated with inflammation in the brain.

2.
Front Oncol ; 10: 605386, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-33312959

RESUMO

Gene mutations are strongly associated with tumor progression and are well known in cancer development. However, recently discovered epigenetic alterations have shown the potential to greatly influence tumoral response to therapy regimens. Such epigenetic alterations have proven to be dynamic, and thus could be restored. Due to their reversible nature, the promising opportunity to improve chemotherapy response using epigenetic therapy has arisen. Beyond helping to understand the biology of the disease, the use of modern clinical epigenetics is being incorporated into the management of the cancer patient. Potential epidrug candidates can be found through a process known as drug repositioning or repurposing, a promising strategy for the discovery of novel potential targets in already approved drugs. At present, novel epidrug candidates have been identified in preclinical studies and some others are currently being tested in clinical trials, ready to be repositioned. This epidrug repurposing could circumvent the classic paradigm where the main focus is the development of agents with one indication only, while giving patients lower cost therapies and a novel precision medical approach to optimize treatment efficacy and reduce toxicity. This review focuses on the main approved epidrugs, and their druggable targets, that are currently being used in cancer therapy. Also, we highlight the importance of epidrug repurposing by the rediscovery of known chemical entities that may enhance epigenetic therapy in cancer, contributing to the development of precision medicine in oncology.

3.
Heliyon ; 5(12): e03013, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31886429

RESUMO

PURPOSE: Dental caries is a multi-factorial oral disease, requiring a susceptible host, cariogenic microorganisms and suitable substrate. Caries is extended worldwide in spite of the availability of countless prophylactic means, including fluoride toothpaste and dental sealers. Many efforts have been made to achieve isolation of pure natural products for medicinal use. Flavonoids are bioactive polyphenol compounds possessing multidimensional effects such as antibacterial action. METHODS: The present study targeted the characterization of antibacterial and antifungal activity of various flavonoids (apigenin, catechin, luteolin, morin, myricetin, naringin, quercetin and rutin). Nine strains present in dental plaque were used: Agreggatibacter actinomycetemcomitans, Actinomyces naeslundii, Actinomyces viscosus, Enterococcus faecalis, Escherichia coli, Lactobacillus casei, Staphylococcus aureus, Streptococcus oralis and Streptococcus sanguinis as well as Candida albicans fungal strain. RESULTS: Results revealed that luteolin, morin, naringin, quercetin and rutin effectively inhibited bacterial and fungal growth. However, morin was the most effective flavonoid. CONCLUSION: It might then be concluded that flavonoids show bacteriostatic effect on all of tested bacteria and fungus.

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