Inhibitory Effect of .BETA.-Glucosyl-phenolic Hydroxamic Acids against Urease in the Presence of Microfloral .BETA.-Glucosidase.

• 朴 鐘伯

• 今村 理佐

• 小橋 恭一

• 伊藤 久富

• 宮崎 寿次

• 堀崎 寿雄

抄録

Three glucosyl-phenolic hydroxamates, 4-O-(β-D-glucopyranosyl) benzohydroxamic acid, 4-O-(β-D-glucopyranosyl) hippuric hydroxamic acid, and 3-[4-O-(β-D-glucopyranosyl) phenyl] propionohydroxamic acid (Glc-PPHA), were hydrolyzed to their corresponding aglycones by β-glucosidase of intestinal flora of rat without any major adverse hydrolysis in vitro. Inhibitory potency of these glucosyl-hydroxamates on urease was recovered to the same extent as that of the corresponding aglycone hydroxamates by preincubation for 2h with rat intestinal flora. p-Hydroxyphenylpropionohydroxamic acid inhibited noncompetitively jack-bean urease activity and its glucose-ligated form, Glc-PPHA inhibited it competitively. A single oral dose of Glc-PPHA tended to inhibit urease activity in proximal colon contents of rat at 6h after administration (p=0.06). After¹⁴C-urea was orally administered to rat, ¹⁴CO₂ was collected for to measure the ureolysis in vivo. Expired ¹⁴CO₂ was limited to 40% by a single oral dose of Glc-PPHA during 6h, and 75% of intestinal ureolysis was repressed during the first 1h in the breath test.

収録刊行物

• Ｂｉｏｌｏｇｉｃａｌ　＆　Ｐｈａｒｍａｃｅｕｔｉｃａｌ　Ｂｕｌｌｅｔｉｎ

  Ｂｉｏｌｏｇｉｃａｌ　＆　Ｐｈａｒｍａｃｅｕｔｉｃａｌ　Ｂｕｌｌｅｔｉｎ 18 (2), 208-213, 1995

  公益社団法人 日本薬学会

キーワード

• urease
• β-glucosidase
• hydroxamic acid
• rat intestine
• pro-drug
• hepatic coma

詳細情報

• CRID: 1390282679598147584
• NII論文ID: 110003640811
• NII書誌ID: AA10885497
• DOI: 10.1248/bpb.18.208
• COI: 1:CAS:528:DyaK2MXksVWrsb8%3D
• ISSN: 13475215
• ISSN: 09186158
• ISSN: http://id.crossref.org/issn/09186158
• PubMed: 7742785
• Web Site: http://www.jstage.jst.go.jp/article/bpb1993/18/2/18_2_208/_pdf
• 本文言語コード: en
• データソース種別:
  • JaLC
  • Crossref
  • PubMed
  • CiNii Articles
• 抄録ライセンスフラグ: 使用不可