Meng P, Xie C, Geng P, Qi X, Zheng F, Bai F
Nankai University, Tianjin 300071, China.
Prikl Biokhim Mikrobiol. 2013 Mar-Apr;49(2):181-9. doi: 10.7868/s0555109913020104.
The search for the effective and safe a-glucosidase and alpha-amylase inhibitors from Actinomycetaceae being antidiabetic agents is actual problem. Twenty one Streptomyces spp. of soil samples collected from different places of China were screened for the ability to produce this kind of inhibitory activities. Fermentation broth of isolated strains had absorbance between 350-190 nm. The Streptomyces strains PW003, ZG636, and ZG731 were characterized by special absorption at 280, 275, and 400 nm, respectively. Ten of the collected actinomycete strains had the ability to inhibit alpha-glucosidase or/and alpha-amylase and the fermentation broth of the same strain had inhibitory activity varied greatly depending on the enzyme source. In the process to screen the leading compounds used as antidiabetic agents, human alpha-glucosidase and alpha-amylase were revealed as the best used in trail compared with the same enzymes from other sources. Active alpha-glucosidase inhibitor was isolated from Streptomyces strain PW638 fermentation broth and identified as acarviostatin 103 by MS and N MR spectrometry. Its IC50 value was 1.25 and 12.23 microg/mL against human intestinal N-terminal maltase-glucoamylase and human pancreatic alpha-amylase, respectively.
从放线菌科中寻找有效且安全的α-葡萄糖苷酶和α-淀粉酶抑制剂作为抗糖尿病药物，是一个亟待解决的实际问题。对从中国不同地区采集的土壤样本中的21株链霉菌进行了筛选，以检测它们产生此类抑制活性的能力。分离菌株的发酵液在350 - 190nm处有吸光度。链霉菌菌株PW003、ZG636和ZG731分别在280、275和400nm处有特殊吸收峰。所收集的10株放线菌菌株具有抑制α-葡萄糖苷酶或/和α-淀粉酶的能力，且同一菌株的发酵液对不同来源的酶的抑制活性差异很大。在筛选用作抗糖尿病药物的先导化合物的过程中，与其他来源的相同酶相比，人α-葡萄糖苷酶和α-淀粉酶被证明是筛选试验中最适用的。从链霉菌菌株PW638的发酵液中分离出了活性α-葡萄糖苷酶抑制剂，并通过质谱和核磁共振光谱鉴定为阿维菌素103。其对人肠道N-末端麦芽糖酶-葡糖淀粉酶和人胰腺α-淀粉酶的IC50值分别为1.25和12.23μg/mL。
