Isolation and Characterization of α-Glucosidase Inhibitor Produced by Bacillus sp. SKU31-1 Strain

In the course of screening for ${\alpha}$-glucosidase inhibitor produced by microorganism, the active compound was isolated from the culture filtrate of Bacillus sp. SKU31-1 using a series of chromatography procedures. The structure of the active compound was elucidated as 5-amino-1-hydroxymethyl-1, 2, 3, 4-cyclohexanetetrol on the basis of spectroscopic evidence obtained and comparison with data from the literature. The active compound showed potent inhibitory activity against ${\alpha}$-glucosidase with an $IC_{50}$ value of $1.9{\mu}M$ for maltose and 4.9 mM for sucrose. A Lineweaver-Burk plot indicated that its inhibition of ${\alpha}$-glucosidase was competitive, with a $K_i$ value of 0.15 mM.

Bacillus sp. SKU31-1가 생산하는 α-Glucosidase 저해제 분리 및 특성 조사

미생물 기원의 ${\alpha}$-glucosidase 저해제를 탐색하는 과정에서 토양에서 분리한 균주인 Bacillus sp. SKU31-1 배양액에서 강력한 저해제 compound K을 일련의 크로마토그래피 방법에 의해 분리 정제하였고 $^1H$ NMR, $^{13}C$ NMR, $^1H-^1H$ COSY spectra 분석과 문헌조사를 통해 5-amino-1-hydroxymethyl-1,2,3,4-cyclohexanetetrol로 동정되었다. Compound K의 ${\alpha}$-glucosidase 저해 활성은 $IC_{50}$값이 maltose 기질에서는 $1.9{\mu}M$이고, sucrose 기질 사용시 4.9 mM이었다. Lineweaver Burk plot에 의해 $K_i$값이 0.15 mM 로 강력한 경쟁적 저해제 임이 밝혀졌다.