Abstract：
:Human kidney-type glutaminase (KGA) is an important target that is often over expressed in many cancer cells but very few effective inhibitors of this enzyme have yet reached clinical trials. Caudatan A and caudatan B, two undescribed tetracyclic flavans with an unusual ether bond between the C-4 and C-2' were isolated from the roots of Ohwia caudata (Thunb.) H.Ohashi. Caudatan A exhibited stronger inhibitory activity and caudatan B showed moderate effect from the results of inhibitory activities evaluations on KGA. The molecular docking and primary structure-activity relationship analysis revealed that the less steric hindrance at ring A was necessary to the effect. Therefore, combined its better solubility than that of bis-2-(5-phenylacetimido-1,2,4-thiadiazol-2-yl)ethyl sulfide (BPTES), caudatan A might be the potential candidate as the inhibitor of KGA for further studies.
journal_name
Phytochemistryjournal_title
Phytochemistryauthors
Sun Y,Feng X,Liu X,Qian C,Che X,Cao F,Jin S,Meng Ddoi
10.1016/j.phytochem.2018.04.013subject
Has Abstractpub_date
2018-08-01 00:00:00pages
22-28eissn
0031-9422issn
1873-3700pii
S0031-9422(18)30099-2journal_volume
152pub_type
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