ABSTRACT
BACKGROUND: Compared with traditional biological materials, self-assembling peptide RADA16 has gained much attention in biomedical fields such as three-dimensional cell culture, tissue repair, hemostasis and drug/protein release for its high water content, structural stability, good biocompatibility and nontoxic degradation products. OBJECTIVE: To review the basic structure and properties of self-assembling peptide RADA16 and the latest progress in biomedical research. METHODS: CNKI, Medline and PubMed databases were retrieved by using computer to search relevant articles about self-assembling peptide RADA16 published from 2005 to 2017. The key words were "self-assembling peptide hydrogel;RADA16; scaffold; tissue repair; hemostasis; drug/protein release" in Chinese and English, respectively. RESULTS AND CONCLUSION: Self-assembling peptide molecules can spontaneously form unique β-strand structures and self-assembly into nanofibers under physiological media or salt solution. As a new scaffold material for tissue engineering, it not only solves the problem of incompatibility between cells and material interface, but also has the advantages of simulating the extracellular matrix effectively, enhancing cell biological activity and maintaining three-dimensional environment. The self-assembling peptide RADA16 and its derivatives not only show good prospects for development and application in three-dimensional cell culture, tissue repair, hemostasis, and drug/protein release, but also face many challenges, such as how to integrate the self-assembling peptide with bio-macromolecular material, and how to control the damage to a target.
ABSTRACT
Inosine 5'-monophosphate dehydrogenase (IMPDH) is a rate-limiting enzyme in de novo biosynthesis of guanine and plays an important role in cell proliferation. In clinic, IMPDH inhibitors are mainly used in fields of anticancer, antiviral, anti-parasitic, and immunosuppressive chemotherapy. However, since there are usually great inter-and intra-individual variability between drug concentration and clinical effect of IMPDH inhibitors, the enzyme activity of IMPDH may be applied as a specific biomarker and combined with the pharmacokinetics (PK) monitoring to improve efficacy and safety of IMPDH inhibitors. This review aims to discuss the assay of IMPDH activity measurement and its clinical application in recent years and provide valuable insights and theoretical basis for the development of IMPDH inhibitors' pharmacodynamics monitoring.
ABSTRACT
It was found that psoralen derivative could perform a Friedel-Crafts acylation smoothly with acetic anhydride to give 5'-acetylpsoralen in a 73% yield. In the presence of boron trifluoride etherate, 5'-acetylpsoralen reacted with both aromatic amines and aliphatic amine smoothly to afford 5'-Schiff-base group substituted psoralen derivatives in 72%-92% yields. The novel synthetic method has the advantages of cheap materials, mild reaction conditions, good yields and high regioselectivity in the Friedel-Crafts acylation. Cell viability assay by MTT demonstrates that some of the psoralen derivatives 6 have antiproliferative activities.
