Three New Cholinesterase Inhibitory Cassioates from Cassia Fistula

被引:5
作者
Aftab, Zahida [1 ]
Bushra [1 ]
Khan, Hidayatullah [2 ]
Khan, Dil Faraz [1 ]
Khan, Asifullah [3 ]
Ullah, Hamid [4 ]
Shahnaz [2 ]
Khan, Shafiullah [1 ]
机构
[1] Gomal Univ, Inst Chem Sci, Dera Ismail Khan, Kpk, Pakistan
[2] Univ Sci & Technol, Dept Chem, Bannu, Kpk, Pakistan
[3] Abdul Wali Khan Univ Mardan, Dept Biochem, Mardan, Kpk, Pakistan
[4] BUITEMS, Fac Arts & Basic Sci, Dept Chem, Takatu Campus, Quetta 87300, Pakistan
关键词
Cassia fistula; cassioates; isolation; cholinesterase inhibitory activity; ACETYLCHOLINESTERASE; BINDING; L;
D O I
10.1007/s11094-020-02124-y
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Three new compounds - cassioates D (4-((9E,11E)-dodeca-9,11-dien-1-yl)-3-methylcyclohexyl tetrahydro-2H-pyran-2-carboxylate), E (2-ethyl-3-methoxy-4,4,15,15-tetramethyl-4,5,6,7,8,9,10, 11,12,15,16,17-dodecahydro-1H-cyclopanta[alpha]phenanthren-16-yl propionate), and F ((E)-17-(2,6-dimethylhept-3-en-3-yl)-7-ethoxy-3-hydroxy-4-isopropyl-10-methyl-2-propoxy-2,3,4,7,10,11,12,13,14,15,16,17-dodecahydro-1H-cycl openta[alpha]phenanthren-12-ylpropionate) - were isolated from Cassia fistula Linn. The structures of these compounds were elucidated with the help of chemical and spectroscopic techniques. All the three cassioates (D - F) were checked for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory action in dose dependent manner. The IC50 (50% inhibitory effect) values of compounds E and F against AChE were 10.26 +/- 0.44 and 4.20 +/- 0.01 mu M while the values obtained against BChE were 14.03 +/- 0.21 and 7.59 +/- 0.04 mu M, respectively. Molecular docking based in silico inhibitory potential of compounds D - F against cholinesterase enzyme target is matching to bioassay screening results. At the same time, compound D showed feeble inhibition profile.
引用
收藏
页码:1069 / 1075
页数:7
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