Molecular basis for establishing the environment in digestive tract by food components

丁香素和木麻黄素是从丁香花蕾甲醇提取物中分离得到的抑制大鼠肠道麦芽糖酶活性的两种化合物。与活性最高的合成五没食子酰基葡萄糖(PGG)的构效关系研究表明，其抑制活性依赖于分子中未偶联没食子酰基残基的数量。这些单宁还抑制了人类癌细胞Caco-2上表达的麦芽糖酶。另一方面，玫瑰茄茶的丙酮提取物对猪胰腺α-淀粉酶具有抑制活性。用比色法研究了海产品和海藻提取物对大肠杆菌β-葡萄糖苷酸酶的体外抑制作用。其中，干鱼(Katsuobushi)、棕藻Hizikia fusiformis和红藻Chdria crassica…的提取物更多的Ulis显示出抑制活性。从干燥的鳄鱼中获得的缓蚀剂被披露为肌苷酸。在核酸相关化合物中，腺苷和三磷酸对β-葡萄糖苷酸酶也有抑制作用。经鉴定，从羊栖菜中获得的抑制剂是一种游离脂肪酸的混合物。粗枝线虫抑制物的分离和结构鉴定正在进行中，研究了分子在1，2-二甲基肼直肠内注射诱导的异常隐窝灶(ACF)形成中的直接作用。以丁酸或脱氧胆酸(及其衍生物)为测试分子。直肠内注射丁酸对20 mM处ACF的形成有保护作用。另一方面，直肠内注射脱氧胆酸可显著增加ACF的大小。这些结果表明，实验动物直肠内注射是评价这类分子在早期癌变过程中作用的有用模型。较少

As the inhibitory principles against rat intestinal maltase, two ellagitannins, eugeniin and casuarictin, were isolated from the methanolic extracts of Clove buds. Structure-activity relationship study of the isolates together with synthetic pentagalloylglucose (PGG), which showed the highest activity , revealed that the inhibitory activity depended on the number of uncoupled galloyl residues in the molecule. These tannins also inhibited maltase expressed on a human carcinoma cell line, Caco-2. On the other hand, the acetone extracts of roselle tea, dried flower buds of Hibiscus sabdariffa, possessed an inhibitory activity against porcine pancreatic α-amylase. The active compound was identified as hibiscus acid.Inhibitory potencies of the extracts of seafood and algae against Escherichia coli β-glucuronidase were investigated by the colorimetric method in vitro. Among them, the extracts of dried bonito (katsuobushi), the brown alga Hizikia fusiformis, and the red alga Chondria crassica … More ulis showed the inhibitory activity. The inhibitor obtained from dried bonito was disclosed to be inosinic acid. Among nucleic acid-related compounds, adenylic acid and adenosine triphosphate also inhibited the β-glucuronidase. The inhibitor obtained from H. fusiformis was identified to be a mixture of free fatty acids. Isolation and structural elucidation of the inhibitor of C. crassicaulis is now in progress.Direct effect of molecules on the formation of aberrant crypt foci (ACF) induced by 1,2-dimethylhydrazine using the intrarectal injection was investigated. Butyric acid or deoxycholic acid (and the derivatives) was used as the test molecule. Intrarectal injection of butyric acid showed a protective effect on the ACF formation at 20 mM. On the other hand, intrarectal injection of deoxycholic acid significantly promoted the size of ACF. These results suggest that the intrarectal injection with experimental animal is useful model to assess the effect of such molecules on the early phase of carcinogenesis. Less