Recent Advances in the Development of "Curcumin Inspired" Compounds as New Therapeutic Agents.

Despite a huge body of research in the past two decades investigating the antioxidant, antiinflammatory, anti-microbial, and anti-carcinogenic properties of curcumin (CUR), a CUR-based antitumor drug is yet to be developed. Lack of success in achieving this goal stems from CUR's unfavorable biophysicochemical features, particularly poor solubility, low bioavailability, and rapid metabolism, coupled with a complex biological profile making it difficult to determine its mechanism of action. A significant body of literature aimed at improving its physicochemical properties through synthesis or by designing delivery methods has been published, and the progress in these areas has been reviewed. The present review aims to summarize recent progress in the synthesis of structurally diverse "curcumin-inspired" compounds along with computational docking and bioassay studies, through which a number of promising analogs have been identified that warrant further study.

Circular RNA: biogenesis, degradation, functions and potential roles in mediating resistance to anticarcinogens.

Aim: This review aims to systematically describe the biogenesis and degradation of circular RNAs (circRNAs), discusses the major functions of circRNAs, introduces the mechanisms by which circRNAs play a role in cancer, comprehensively summarize the relationship between circRNAs and anticarcinogen resistance as well as underlying specific mechanisms in multiple cancers. Materials & methods: We screened and analyzed large quantity of scientific papers which associated with circRNAs, noncoding RNAs, function, cancer, drug resistance and chemoresistance, and then summarized in Figures 1 & 2 & Table 1. Results & conclusion: The biogenesis, degradation and function of circRNAs are specially compared with other noncoding RNAs, it can affect cancer pathogenesis and progression and are implicated in mediating resistance to various anticarcinogens in various types of cancer.

Efeito redutor do Viagra (Citrato de Sildenafila) sobre a frequência de tumores epiteliais induzidos pela Doxorrubicina em Drosophila melanogaster / Viagra (Sildenafil citrate) reduced the frequency of epithelial tumors induced by doxorubicin in Drosophila melanogaster

O consumo de medicamentos está entre as principais causas de desenvolvimento do câncer. Faz-se, então, necessário investigar os efeitos de drogas amplamente consumidas no mundo, como é o caso do Viagra® (Citrato de Sildenafila - CS). O objetivo do presente estudo foi avaliar o efeito modulador do CS na carcinogênese induzida pela Doxorrubicina (DXR), por meio do Teste para Detecção de Clones de Tumores Epiteliais em Drosophila melanogaster. Foram utilizadas duas linhagens mutantes do organismo teste (wts e mwh) no intuito de obter larvas heterozigotas wts +/+ mwh, que foram tratadas com três concentrações de CS: 10 mM, 20 mM e 40 mM, isoladamente e em associação com a DXR. Constatou-se que o CS não exerceu efeito carcinogênico nas concentrações isoladamente avaliadas. Quando em associação com a DXR, propiciou efeito redutor sobre as frequências dos tumores induzidos por ela, conferindo papel anticarcinogênico ao CS. Acredita-se que este efeito seja devido a uma supra-regulação da via de apoptose dependente de caspase e ao impedimento do crescimento celular promovido pelo fármaco utilizado. As evidências obtidas comprovam o efeito protetor tumoral atribuído ao Viagra® nas condições experimentais propostas.(AU)

Drug consumption is among the leading causes of cancer development. Therefore, it is necessary to investigate the effects of drugs widely consumed in the world, as the case of Viagra® (Sildenafil Citrate - SC). The objective of the study was to evaluate the modulatory effect of SC on the carcinogenicity induced by Doxorubicin (DXR) by the Test for Detection of Epithelial Tumor Clones in Drosophila melanogaster. Two mutant lines (wts and mwh) were used in order to obtain heterozygous wts+/+mwh larvae, which were treated with three concentrations of CS: 10 mM, 20 mM and 40 mM, alone and in combination with doxorubicin. We verified that SC had no carcinogenic effect at the concentrations evaluated alone. In association with DXR, it was provided a reduced effect of tumor-induced, conferring anticarcinogenic role to SC. It is believed that this effect is due to up-regulation of the caspase-dependent apoptosis and the impediment of cell growth promoted by the drug used. Evidence obtained confirms the tumor protective effect attributed to Viagra® under experimental conditions. (AU)

Competitive interactions of anti-carcinogens with serum albumin: a spectroscopic study of bendamustine and dexamethasone with the aid of chemometrics.

Interactions between the anti-carcinogens, bendamustine (BDM) and dexamethasone (DXM), with bovine serum albumin (BSA) were investigated with the use of fluorescence and UV-vis spectroscopies under pseudo-physiological conditions (Tris-HCl buffer, pH 7.4). The static mechanism was responsible for the fluorescence quenching during the interactions; the binding formation constant of the BSA-BDM complex and the binding number were 5.14×10(5)Lmol(-1) and 1.0, respectively. Spectroscopic studies for the formation of BDM-BSA complex were interpreted with the use of multivariate curve resolution - alternating least squares (MCR-ALS), which supported the complex formation. The BSA samples treated with site markers (warfarin - site I and ibuprofen - site II) were reacted separately with BDM and DXM; while both anti-carcinogens bound to site I, the binding constants suggested that DXM formed a more stable complex. Relative concentration profiles and the fluorescence spectra associated with BDM, DXM and BSA, were recovered simultaneously from the full fluorescence excitation-emission data with the use of the parallel factor analysis (PARAFAC) method. The results confirmed that on addition of DXM to the BDM-BSA complex, the BDM was replaced and the DXM-BSA complex formed; free BDM was released. This finding may have consequences for the transport of these drugs during any anti-cancer treatment.