A dammarane derivative dihydrojujubogenin-2-en-1-one, which possesses a skeleton and pharmacophore partially similar to those of Territrem B, a potent AChE inhibitor, was synthesized via three different paths. The ant...A dammarane derivative dihydrojujubogenin-2-en-1-one, which possesses a skeleton and pharmacophore partially similar to those of Territrem B, a potent AChE inhibitor, was synthesized via three different paths. The anti-AChE activity of this compound and related analogue was measured.展开更多
In order to understand whether the ameliorating effect on old ages memory disorder by the root of Salvia miltiorhiza is related to the acetylcholinesterase （ACHE） inhibition, two main ingredients, salvianolic acid B...In order to understand whether the ameliorating effect on old ages memory disorder by the root of Salvia miltiorhiza is related to the acetylcholinesterase （ACHE） inhibition, two main ingredients, salvianolic acid B （1） and rosmarinic acid （2）, which were isolated from S. miltiorhiza water extract, were investigated in vitro by NMR relaxation rate in this work. The results showed that the proton selective relaxation rates and the molecular rotational correlation time of proton pairs for compounds 1 and 2 increased significantly by adding of AChE in mixing solution. The study reveals that the two compounds might bind to the enzyme and have ACHE inhibitory effect, which could contribute to the ameliorating effect at some extent on old ages memory disorder.展开更多
23 compounds containing pyranone pharmacophore of territrem B were designed and synthesized. Some of the analogues showed IC50 values of AChE inhibition at 10^-5 mol/L.
Two series of territrem B analogues (6, 11) were designed and synthesized from jujubogenin 2. Compound 11c inhibited AChE with the ratio of 70% at 10-4 mol/L. Compounds 5a, 5b, 6a and 11b showed moderate cytotoxicit...Two series of territrem B analogues (6, 11) were designed and synthesized from jujubogenin 2. Compound 11c inhibited AChE with the ratio of 70% at 10-4 mol/L. Compounds 5a, 5b, 6a and 11b showed moderate cytotoxicity on cultured KB cells at 10-6 mol/L. Compounds 5c and 6b alleviated injury arising from oxygen-glucose deprivation (OGD).展开更多
Two series of territrem B analogues (10a-10c and 18) have been designed and synthesized from jujubogenin 5a which was prepared from jujubogenin glycosides 5b obtained from the leaves of Zizyphus jujuba. The structur...Two series of territrem B analogues (10a-10c and 18) have been designed and synthesized from jujubogenin 5a which was prepared from jujubogenin glycosides 5b obtained from the leaves of Zizyphus jujuba. The structures of the new compounds were confirmed by H-, 1 13C-NMR and MS data. Compounds 10c and 18 showed weak inhibitory effect on AChE at 10-4 mol/L.展开更多
文摘A dammarane derivative dihydrojujubogenin-2-en-1-one, which possesses a skeleton and pharmacophore partially similar to those of Territrem B, a potent AChE inhibitor, was synthesized via three different paths. The anti-AChE activity of this compound and related analogue was measured.
基金The authors are grateful for supports by the National Natural Science Foundation of China （No. 90409015 and 20473013）.
文摘In order to understand whether the ameliorating effect on old ages memory disorder by the root of Salvia miltiorhiza is related to the acetylcholinesterase （ACHE） inhibition, two main ingredients, salvianolic acid B （1） and rosmarinic acid （2）, which were isolated from S. miltiorhiza water extract, were investigated in vitro by NMR relaxation rate in this work. The results showed that the proton selective relaxation rates and the molecular rotational correlation time of proton pairs for compounds 1 and 2 increased significantly by adding of AChE in mixing solution. The study reveals that the two compounds might bind to the enzyme and have ACHE inhibitory effect, which could contribute to the ameliorating effect at some extent on old ages memory disorder.
文摘23 compounds containing pyranone pharmacophore of territrem B were designed and synthesized. Some of the analogues showed IC50 values of AChE inhibition at 10^-5 mol/L.
文摘Two series of territrem B analogues (6, 11) were designed and synthesized from jujubogenin 2. Compound 11c inhibited AChE with the ratio of 70% at 10-4 mol/L. Compounds 5a, 5b, 6a and 11b showed moderate cytotoxicity on cultured KB cells at 10-6 mol/L. Compounds 5c and 6b alleviated injury arising from oxygen-glucose deprivation (OGD).
文摘Two series of territrem B analogues (10a-10c and 18) have been designed and synthesized from jujubogenin 5a which was prepared from jujubogenin glycosides 5b obtained from the leaves of Zizyphus jujuba. The structures of the new compounds were confirmed by H-, 1 13C-NMR and MS data. Compounds 10c and 18 showed weak inhibitory effect on AChE at 10-4 mol/L.
