Fourteen arylsemicarbazone derivatives were synthesized and evaluated in order to find agents with potential anticancer activity. Cytotoxic screening was performed against K562, HL-60, MOLT-4, HEp-2, NCI-H292, HT-29 and MCF-7 tumor cell lines. Compounds 3c and 4a were active against the tested cancer cell lines, being more cytotoxic for the HL-60 cell line with IC50 values of 13.08 μM and 11.38 μM, respectively. Regarding the protein kinase inhibition assay, 3c inhibited seven different kinases and 4a strongly inhibited the CK1δ/ε kinase. The studied kinases are involved in several cellular functions such as proliferation, migration, cell death and cell cycle progression. Additional analysis by flow cytometry revealed that 3c and 4a caused depolarization of the mitochondrial membrane, suggesting apoptosis mediated by the intrinsic pathway. Compound 3c induced arrest in G1 phase of the cell cycle on HL-60 cells, and in the annexin V assay approximately 50% of cells were in apoptosis at the highest concentration tested (26 μM). Compound 4a inhibited cell cycle by accumulation of abnormal postmitotic cells at G1 phase and induced DNA fragmentation at the highest concentration (22 μM).

Because of the increasing demand for natural products, the development of nanoformulations containing natural active ingredients requires in‐depth knowledge of the substances used, methods of obtaining, and stability profiles to ensure product quality, efficacy, and safety. Considering this, the bibliography of the last five years presented in databases (PubMed and Science Direct) was discussed in this work, discussing the study with medicinal plants to obtain active metabolites with therapeutic properties, as well as the different nano‐systems responsible for carrying these molecules. Due to the wealth of biodiversity found in the world, many species are submitted to the extraction process for several purposes. However, identifying, classifying, and quantifying the constituents of herbal matrices are crucial steps to verify their therapeutic potential. In addition, knowing the techniques of production and elaboration of nanotechnology products allows the optimization of the incorporation of herbal extracts as an innovation target. For studies to be successful, it is necessary to exhaust experimental results that guarantee the efficacy, safety, and quality of natural nanosystems, with the objective of obtaining reliable answers in nanotechnology therapy.

Resumo Esse trabalho descreve o desenvolvimento de novas fases estacionárias(FE) sorvidas e imobilizadas para cromatografia liquida de alta eficiência (CLAE), utilizando suporte de sílica recoberta com o polímero poli[dimetilsiloxano-co-(3-aminopropil) metilsiloxano]. O processo de imobilização da FE ocorreu através de tratamento térmico nas seguintes condições: 80ºC, 120ºC e 150ºC por um período de 16 h. As FE foram caracterizadas por testes cromatográficos, sendo que a avaliação cromatográfica ocorreu por meio da separação de misturas testes (MT), e as eficiências apresentadas pelas FE ficaram entre 35100 e 45400 pratos por metro.