Modulation of protein-ligand interactions in the presence of ZIF-8: Spectroscopy and molecular dynamics simulation.

In this paper, we investigated the protein-ligand interactions in the presence of ZIF-8 using multi-spectroscopic approaches and molecular dynamics simulation. Fluorescence experiments and molecular docking results showed that ZIF-8 did not change the type of quenching and interaction force between ciprofloxacin (CIP) and human serum albumin (HSA), but made the binding constant of HSA-CIP to be smaller, suggesting that ZIF-8 maybe accelerate the dissociation of CIP from HSA-CIP complex. Moreover, the effect of ZIF-8 on the physiological function of HSA was explored. Multi-spectroscopic methods revealed that ZIF-8 did not significantly alter the microenvironment of amino acid groups, but cause a slight decrease in the content of α-helical conformation, and a sparse and flexible structure of the protein backbone. These peculiarities might lead to the diminution of HSA's ability to control drugs. In short, ZIF-8 might enhance drug effect due to affecting the binding of drugs to proteins. However, the present study is only a preliminary investigation of the suitability of ZIF-8 as a drug carrier in vitro, and subsequent in vivo experimental studies will be required to further confirm the idea.

Recent Progresses in Chalcone Derivatives as Potential Anticancer Agents.

Chalcones are members of the flavonoid family and act as intermediates in the biosynthesis of flavonoids, which are widespread in plants. Meanwhile, chalcones are important precursors for synthetic manipulations and act as mediators in the synthesis of useful therapeutic compounds, which have demonstrated a wide range of biological activities. Numerous studies have reported the synthesis and medicinal significance of chalcone derivatives. Cancer is one of the major causes of death worldwide. Although various therapies have been proposed for diverse types of cancer, their associated limitations and side effects urged researchers to develop more safe, potent and selective anticancer agents. Based on the literature review, the presence of chalcone derivatives as the main component, a substituent, or a side-chain in different biologically active compounds could serve as a reliable platform for synthetic organic chemists to synthesize new compounds bearing this moiety, owing to their similar or superior activities compared to those of the standards. The diversity of the chalcone family also lends itself to broad-spectrum biological applications in oncology. This review, therefore, sheds light on the latest structure and the anticancer potency of different synthetics (bearing other anticancer pharmacophores based on simple, functional groups, and dimer chalcone derivatives) and natural chalcone hybrids. It is confirmed that the information compiled in this review article, many chalcone hybrids have been found with promising anticancer activities. Therefore, this review may be convenient for designing novel chalcone molecules with enhanced medicinal properties according to the structure of the compounds.