| Title : Isolation and characterization of N98-1272 A, B and C, selective acetylcholinesterase inhibitors from metabolites of an actinomycete strain - Zheng_2007_J.Enzyme.Inhib.Med.Chem_22_43 |
| Author(s) : Zheng ZH , Dong YS , Zhang H , Lu XH , Ren X , Zhao G , He JG , Si SY |
| Ref : J Enzyme Inhib Med Chem , 22 :43 , 2007 |
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Abstract :
A high throughput screening was carried out in order to search for inhibitors of acetylcholinesterase (AChE) from microorganism metabolites. An actinomycete strain was found to produce active compounds named N98-1272 A, B and C with IC50 of 15.0, 11.5, 12.5 microM, respectively. Structural studies revealed that the three compounds are identical to the known antibiotics, Manumycin C, B and A. Kinetic analyses showed that N98-1272 C (Manumycin A) acted as a reversible noncompetitive inhibitor of acetylcholinesterase, with a Ki value of 7.2 microM. The cyclohexenone epoxide part of the structure plays a crucial role in the inhibitory activity against AChE. Compared with Tacrine, N98-1272 A, B, and C exhibit much better selectivity toward AChE over BuChE. |
| PubMedSearch : Zheng_2007_J.Enzyme.Inhib.Med.Chem_22_43 |
| PubMedID: 17373546 |
Zheng ZH, Dong YS, Zhang H, Lu XH, Ren X, Zhao G, He JG, Si SY (2007)
Isolation and characterization of N98-1272 A, B and C, selective acetylcholinesterase inhibitors from metabolites of an actinomycete strain
J Enzyme Inhib Med Chem
22 :43
Zheng ZH, Dong YS, Zhang H, Lu XH, Ren X, Zhao G, He JG, Si SY (2007)
J Enzyme Inhib Med Chem
22 :43