ABSTRACT
A series of novel L-tyrosine derivatives were designed, synthesized and assayed for their inhibitory activities on matrix metalloproteinase 2 (MMP-2) and histone deacetylase 8 (HDAC-8). The results showed that these L-tyrosine derivatives exhibited inhibitory profiles against MMP-2 and HDAC-8. The compounds 6h (IC(50)=0.013 ± 0.001 µM) and 6j (IC(50)=0.017 ± 0.001 µM) were equal potent MMP-2 inhibitors to the positive control NNGH (IC(50)=0.014 ± 0.001 µM). As for HDAC-8 inhibition, some of the hydroxamate compounds, such as 6d (IC(50)=3.6 ± 0.2 µM) and 6c (IC(50)=5.8 ± 0.5 µM), were equal potent to the positive control SAHA (IC(50)=1.6 ± 0.1 µM). Structure-activity relationships were also briefly discussed.
Subject(s)
Matrix Metalloproteinase 2/metabolism , Matrix Metalloproteinase Inhibitors/chemistry , Matrix Metalloproteinase Inhibitors/pharmacology , Repressor Proteins/antagonists & inhibitors , Tyrosine/analogs & derivatives , Tyrosine/pharmacology , Drug Design , Histone Deacetylases/metabolism , Humans , Inhibitory Concentration 50 , Matrix Metalloproteinase Inhibitors/chemical synthesis , Models, Molecular , Repressor Proteins/metabolism , Tyrosine/chemical synthesisABSTRACT
OBJECTIVE: To design a new type minor smoke warming moxibustion cup for convenient use of both the physicians and the patients. METHODS: The double-deck minor smoke warming moxibustion cup is fixed on the part receiving moxibustion by vacuum adsorption; the filtration device on the upper can filtrate and adsorb the harmful substance in the moxa-smoke, and the device with a double-temperature control on the lower can sensitively regulate the moxibustion temperature. RESULTS: This new type minor smoke warming moxibustion cup has the advantages of minor smoke discharge, convenient fixation, sensitive regulation of temperature, saving moxibustion material, lasting action, safety, besides the advantages of traditional moxibustion. CONCLUSION: The new type minor smoke warming moxibustion cup can use for treatment and prevention of diseases, suitable to clinical treatment and family health care.
