Encapsulation of a 5FU-curcumin hybrid on bacterial nanocellulose for colorectal cancer treatment.

The traditional treatment of colorectal cancer (CRC) involves a combination of chemotherapy and synthetic and natural drugs. In this study, a hybrid compound of 5-fluorouracil-curcumin encapsulated in bacterial nanocellulose (BNC) was evaluated for CRC treatment. Bacterial nanocellulose was produced using K.

Correlations between in vitro gastrointestinal digestion of β-galactosidase/carboxymethylchitosan-silica dosage powder and its physicochemical properties.

Oral administration of β-galactosidase, which alleviate lactose intolerance symptoms, is challenging due to its instability throughout the gastrointestinal tract. The objective of this work was to make correlations between the in-vitro digestion and chemical characteristics of a β-galactosidase/carboxymethylchitosan-silica biocatalyst powder. This was obtained by a one-pot silica gel route assisted by carboxymethyl chitosan, using maltose as lyoprotectant.

3-styrylcoumarin scaffold-based derivatives as a new approach for leishmaniasis intervention: biological and molecular modeling studies.

Seven 3-styrylcoumarins were tested for antileishmanial activity against (Viannia) amastigotes. Cytotoxic activity was also evaluated against mammalian U-937 cells. The 3-methoxy-4-hydroxy coumarin derivative was the most active with an IC of 40.

New Hybrid Scaffolds Based on 5-FU/Curcumin: Synthesis, Cytotoxic, Antiproliferative and Pro-Apoptotic Effect.

A series of 5-FU-Curcumin hybrids were synthesized, and their structures were elucidated by spectroscopic analysis. The synthesized hybrid compounds were evaluated in different colorectal cancer cell lines (SW480 and SW620) and in non-malignant cells (HaCaT and CHO-K1), to determine their chemopreventive potential. Hybrids and presented the best IC value against the SW480 cell line with results of 17.

Resveratrol/Hydrazone Hybrids: Synthesis and Chemopreventive Activity against Colorectal Cancer Cells.

A series of resveratrol/hydrazone hybrids were obtained and elucidated by spectroscopic analysis. All compounds were evaluated against colorectal cancer cells (SW480 and Sw620) and nonmalignant cell lines (HaCaT and CHO-K1) to establish the selectivity index. Among the hybrids evaluated, compounds and displayed the highest cytotoxic activity with IC values of = 6.

Synthesis and Chemopreventive Potential of 5-FU/Genistein Hybrids on Colorectal Cancer Cells.

A series of 5-FU-Genistein hybrids were synthesized and their structures were elucidated by spectroscopic analysis. The chemopreventive potential of these compounds was evaluated in human colon adenocarcinoma cells (SW480 and SW620) and non-malignant cell lines (HaCaT and CHO-K1). Hybrid displayed cytotoxicity against SW480 and SW620 cells with IC values of 62.

Chemopreventive Effect on Human Colon Adenocarcinoma Cells of Styrylquinolines: Synthesis, Cytotoxicity, Proapoptotic Effect and Molecular Docking Analysis.

Seven styrylquinolines were synthesized in this study. Two of these styrylquinolines are new and were elucidated by spectroscopic analysis. The chemopreventive potential of these compounds was evaluated against SW480 human colon adenocarcinoma cells, its metastatic derivative SW620, and normal cells (HaCaT).

Novel Multipotent Amantadine-M30D Hybrids with Highly Selective Butyrylcholinesterase Inhibition and Neuroprotective Effects as Effective Anti-Alzheimer's Agents.

As a contribution to the development of new dual/multifunctional drugs, a novel therapeutical scaffold merging key structural features from memantine and M30D was designed, synthesized, and explored for its AChE/BuChE inhibitory activity and neuroprotective effects. All synthetized hybrids were not able to inhibit AChE, but most of them exhibit inhibition with high selectivity toward butyrylcholinesterase (BuChE). Notably, among the tested compounds, amantadine/M30D hybrids with six, seven, nine, and twelve methylene groups in the spacer (, , , and ) not only highlighted having the best potency and selective butyrylcholinesterase inhibition greater than 83% but also, particularly and , elicited considerable neuroprotection when evaluated in pretreatment conditions, by reducing injury effects caused by glutamate with maximum protection reached about 47.

Fe chelating quinoline-hydrazone hybrids with proven cytotoxicity, leishmanicidal, and trypanocidal activities.

Neglected tropical diseases cause great concern in developing countries where there are millions of reported infected humans. It is well known that chelating agents inhibit parasite growth by depriving them of iron, an essential nutrient for cell growth and division; therefore, in this work, we use computational methods to explore the Fe3+ chelating abilities of a set of 10 quinoline-hydrazone hybrids (28 substructures in total) whose cytotoxicity, leishmanicidal, and trypanocidal activities are known. We quantify stabilizing effects in the bare molecules as well as in the iron complexes and show how iron complexation reduces the structural space.