ABSTRACT
CD38 is a multifunctional enzyme expressed in a variety of mammalian tissues, its catalytic activity was involved in a wide range of physiological processes. Based on the reported inhibitor of human CD38 NADase, 33 purine derivatives were designed and synthesized. The biological activity assay showed that compounds 20 and 38 exhibited almost the same extent of inhibitory activities on human CD38 NADase as the lead compound H2. The results also revealed that small substituents at C-6 of purine ring gave no obvious effect on inhibitory activity, but phenylpropionyl moiety at N-2 could affect the binding mode of the compound with CD38. This study provides a reliable basis for future rational design of inhibitors for CD38.
Subject(s)
ADP-ribosyl Cyclase 1/antagonists & inhibitors , Enzyme Inhibitors/chemistry , Purines/chemistry , Enzyme Inhibitors/chemical synthesis , Humans , Purines/chemical synthesisABSTRACT
OBJECTIVE: To extract and analyze fatty acids in leaves of L. chinense Oliver and L. chinense var. rubrum Yieh. METHODS: The fatty acids were extracted with Soxhlet extractor and identified by the GC-MS method. RESULTS: 31, 26 and 30 components were identified from the leaves of L. chinense, the green leaves and red leaves of L. chinense var. rubrum. There were 19, 14 and 16 kinds of fatty acid in the respective leaves, which accounted for 99.09%, 95.31% and 98.83% of the total extraction, respectively. The main components in the extraction were oleic acid (30.77%, 47.01%, 75.28%), linoleic acid (48.49%, 29.26%, 0%), hexadecanoic acid (9.83%, 8.87%, 11.71%), octadecanoic acid (3.86%, 3.18%, 4.88%) and docosanoic acid (2.37%, 2.17%, 2.58%). CONCLUSION: Many kinds of unsaturated fatty acids exist in leaves of L. chinense Oliver and L. chinense var. rubrum Yieh. The leaves of these two plants can be used as the traditional Chinese medicine.
