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Studies on Induction of Salivary Cysteine Proteinase Inhibitor by Isoproterenol

异丙肾上腺素诱导唾液半胱氨酸蛋白酶抑制剂的研究

基本信息

批准号：
02807214
负责人：
NAITO Yukio
金额：
$ 0.96万
依托单位：
Nagoya University
依托单位国家：
日本
项目类别：
Grant-in-Aid for General Scientific Research (C)
财政年份：
1990
资助国家：
日本
起止时间：
1990 至 1991
项目状态：
已结题

项目摘要

Rat cystain S(RSC), a cysteine proteinase inhibitor belonging to family 2 of the cystatin superfamily. (1)Papain(Ki : O. l nM)and ficin(Kl : 0.2 nM)were inhibited strongly, and bromelain and cathepsin C partially. The proteinases were inhibited by RSC competitively. However, trypsin, kalllkrein and pepsin did not inhibit by RSC. (2)When RSC was reduced and S-carboxymethylated, the proteinases inhibitory activity was lost completly. Complex formation between papain and RSC was 1 : 1 molar ratio. (3)The proteinase inhibitory activity of RSC was stable to extremes of pH 1-12 for I hour at 37 ﾟC) and to heat treatment (100 ﾟC for 1 hour). (4)Cysteine proteinases are important in the penetration of human tissue by microorganism. Anti-bacteria activity of RSC was tested to seventeen strains including of oral bacteriaby disc diffusion analysis. We found that RSC have anti-bacterial activity against Bacteroides gingivalis, an oral bacterium suspected of being a pathogen of periodontal disease(minimum effective dose : 75 mug/disc). (5)Treatment of rats with the beta-adrenergic-agonist, isoproterenol, produces hypertrophy and hyperplasia of submandibular glands and induces a large quantity of RSC. However, biological rule of the responses did not understand. When papain, a cysteine proteinase of plant(papaya), was administered into the oral cavity of rats of 8 weeks age, a dramatic increase in the level of RSC in enlarged submandibular glands. The magnitude of induction of RSC and enlargement of the glands were correlated with the dose of papain and duration of the treatment. We tested to specify on the respence in kind of proteinase. We found that ficin, a cysteine proteinase of plant(Ficus), and trypsin, a serine proteinase of pancreas, had same activity. We proposed that induction of the RSC in the submandibular glands by oral administration of the proteinases is a biological response which plays a role in preventing injury exgeneous proteinases.

大鼠半胱氨酸蛋白酶抑制剂S（RSC），属于半胱氨酸蛋白酶抑制剂超家族2的半胱氨酸蛋白酶抑制剂。（1）木瓜蛋白酶（Ki：O. lnM）和无花果蛋白酶（KI：0.2nM）被强烈抑制，并且菠萝蛋白酶和组织蛋白酶C被部分抑制。蛋白酶被RSC竞争性抑制。而胰蛋白酶、激肽释放酶和胃蛋白酶不受RSC的抑制。（2）RSC被还原和S-羧甲基化后，蛋白酶抑制活性完全丧失。木瓜蛋白酶和RSC之间的复合物形成为1：1的摩尔比。（3）RSC的蛋白酶抑制活性在pH 1-12、37 ℃、1h和100 ℃、1h的热处理条件下稳定。（4）半胱氨酸蛋白酶在微生物穿透人体组织中起重要作用。用纸片扩散法测定RSC对17株口腔致病菌的抑菌活性。我们发现RSC对牙龈拟杆菌（一种被怀疑是牙周病病原体的口腔细菌）具有抗菌活性（最低有效剂量：75 μ g/盘）。（5）用β-肾上腺素能激动剂异丙肾上腺素处理大鼠，引起颌下腺肥大和增生，并诱导大量RSC。然而，生物学的反应规则并不了解。当木瓜蛋白酶，半胱氨酸蛋白酶的植物（木瓜），被管理到口腔的大鼠8周龄，一个显着增加的RSC的水平在扩大的下颌下腺。诱导RSC和腺体增大的幅度与木瓜蛋白酶的剂量和治疗时间相关。我们对蛋白酶的反应进行了详细的试验。我们发现植物（榕属）的半胱氨酸蛋白酶无花果蛋白酶和胰腺的丝氨酸蛋白酶胰蛋白酶具有相同的活性。我们提出，通过口服蛋白酶诱导下颌下腺RSC是一种生物学反应，其在防止外源性蛋白酶损伤中起作用。