Caffeic acid phenethyl ester (CAPE), as one of the main active ingredients of the natural product propolis, shows the unique biological activities such as anti-tumor, anti-oxidation, anti-inflammatory, immune regulation, and so on. These have attracted the attention of many researchers to explore the compound with potent biological activities. This review aims to summarize its bioactivities, synthetic methods and derivatives, which will be helpful for further study and development of CAPE and its derivatives.
1 March 2014 in Pharmacology Biochemistry and Behavior
Scutellarein, the main metabolite of scutellarin in vivo, has relatively better solubility, bioavailability and bio-activity than scutellarin. However, it is very difficult to obtain scutellarein in nature compared with scutellarin. Therefore, the present study focused on establishing an efficient route for the synthesis of scutellarein by hydrolyzing scutellarin. The in vitro antioxidant activities of scutellarein were evaluated by measuring its scavenging capacities toward DPPH, ABTS+•, •OH free radicals and its protective effect on H2O2-induced cytotoxicity in PC12 cells using MTT assay method. The results showed that essential point to the synthesis was the implementation of H2SO4 in 90% ethanol in N2 atmosphere; scutellarein had stronger antioxidant activity than scutellarin. The results have laid the foundation for further research and the development of scutellarein as a promising candidate for ischemic cerebrovascular disease.
A highly efficient synthesis of alkyl ferulates under microwave irradiation is described. The time of these reactions ranged from 3 to 5 minutes, which was much shorter than the traditional synthetic methods, and the alkyl ferulates were obtained in higher yields.
4 August 2014 in Expert Opinion on Therapeutic Patents
The MMPs are involved in tissue remodeling. An imbalance between the inhibition and activation of MMPs results in excessive degradation of the extracellular matrix, which leads to some diseases including cancer, rheumatoid arthritis, osteoarthritis, heart disease and neurodegenerative diseases such as stroke. In this review, recent advances in the research of MMP inhibitors are reviewed. This updated review summarized new patents on MMP inhibitors within January 2011 - December 2013. This review gives the latest development in the area of MMP inhibitors, which aim to treat disease processes associated with the MMPs. Structure-based design techniques have been used successfully in the search of selective MMP inhibitors, and these inhibitors can also be derived from natural products. Furthermore, imaging 'in vivo' technologies have been developed in order to follow the drug distribution to the targeted tissues, and to quantify the drug efficiency.