Carbohydrate Research p. 259 - 264 (1997)
Update date:2022-08-03
Topics:
Kameda, Yukihiko
Kawashima, Kanae
Takeuchi, Masayoshi
Ikeda, Kyoko
Asano, Naoki
Matsui, Katsuhiko
Manno- and galacto-validamines, which are epimers of validamine, were semi-synthesized by the configurational inversion of validamine, a pseudo-sugar analogue of α-D-glucopyranose that has inhibitory activity for α-glucosidases. The inhibitory activities of these analogues were determined against several mannosidases and galactosidases. Manno-validamine shows potent inhibition for the α-mannosidases (competitive, K(i) = 4.6 x 10-5 M for jack beans, and competitive, K(i) = 2.8 x 10-5 M for almonds), and galacto-validamine shows weak inhibition for the α-galactosidases (coffee bean and E. coli). The inhibitory effect of the epimers on the N-linked oligosaccharide-processing mannosidases involved in glycoprotein biosynthesis and lysosomal mannosidase from rat liver were also examined. Mannovalidamine shows potent inhibition on the endoplasmic reticulumal α-mannosidase (competitive, K(i) = 1.2 x 10-6 M), Golgi mannosidases IA, II (competitive, K(i) = 2.8 X 10-5 M), and lysosomal α-mannosidase (competitive, K(i) 1.7 x 10-5 M).
View MoreSuzhou Kangrun Pharmaceutical, Inc
Contact:86-512-63912376,63913329
Address:Building 2, No. 2358 ,Chang'an Rd, Wujiang Economic Development Zone Pioneering park, china
wuxi huabin bio-tech Co.,Ltd(expird)
Contact:86-0510-85133006
Address:hubin road NO157
jiangsu hualin chemical co.,ltd.
Contact:86-25-87787402
Address:jaingsu,china
website:http://www.debyesci.com
Contact:+85221376140
Address:Rm. 19C, Lockhart Ctr., 301-307 Lockhart Rd., Wan Chai
Contact:+86-15995924277
Address:WuZhongOu suzhou new south road 89
Doi:10.1016/S0022-328X(96)06635-1
(1997)Doi:10.1007/s11171-005-0048-y
(2005)Doi:10.1016/S0008-6215(00)85141-1
(1980)Doi:10.1016/j.tet.2004.05.029
(2004)Doi:10.1016/j.tetasy.2006.10.017
(2006)Doi:10.1039/b405275g
(2004)