Suppressive Effects of Tranilast on Pulmonary Fibrosis and Activation of Alveolar Macrophages in Mice Treated with Bleomycin: Role of Alveolar Macrophages in the Fibrosis

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• Polaprezinc, an insoluble zinc complex of L-carnosine, exhibits anti-ulcer effects by acting directly on mucosal lesions. The disposition of polaprezinc in the stomach was studied to clarify the usefulness of its structure as an insoluble complex. The time courses of <SUP>14</SUP>C-radioactivity in the gastric contents and gastric tissues were parallel to those of <SUP>65</SUP>Zn after oral administration of a mixture of <SUP>14</SUP>-Cpolaprezinc and <SUP>65</SUP>Zn-polaprezinc (<SUP>14</SUP>C-, <SUP>65</SUP>Zn-polaprezinc) to rats. The gastric contents of <SUP>14</SUP>C-polaprezinc and <SUP>65</SUP>Zn-polaprezinc were greater than those of <SUP>14</SUP>C-L-carnosine and <SUP>65</SUP>ZnSO<SUB>4</SUB>. Mean residence times (MRT) of <SUP>14</SUP>C-polaprezinc and <SUP>65</SUP>Zn-polaprezinc in the stomach were almost the same (ca. 2 hr), and they were double those of <SUP>14</SUP>C-L-carnosine and <SUP>65</SUP>ZnSO<SUB>4</SUB>. In gastric tissues, the area under the concentration curves (AUC<SUB>0-8 hr</SUB>) of <SUP>14</SUP>C-polaprezinc and <SUP>65</SUP>Zn-polaprezinc were 1.7 times greater than those of <SUP>14</SUP>C-L-carnosine and <SUP>65</SUP>ZnSO<SUB>4</SUB>, respectively. After administration of <SUP>14</SUP>C-, <SUP>65</SUP>Zn-polaprezinc to rats with acetic acid-induced ulcers, <SUP>14</SUP>C and <SUP>65</SUP>Zn-radioactivities in the ulcerous sites were very similar and greater than those of <SUP>14</SUP>C-, <SUP>65</SUP>Zn-polaprezinc dissolved in acid. In conclusion, polaprezinc is retained in the stomach longer and adheres to the ulcerous sites more than zinc or L-carnosine. The characteristics of this compound may arise from its insolubility and contribute to its strong pharmacological action.

• 社団法人 日本薬理学会の論文
• 1995-04-01

著者

• Tanaka Hiroyuki

  Department Of Cardiology Kurashiki Central Hospital

• Nagai Hiroichi

  富山医科薬科大学和漢薬研究所

• NAGAI Hiroichi

  Department of Pharmacology, Gifu Pharmaceutical University

• MORI Hiroshi

  Department of Pharmacology, Gifu Pharmaceutical University

• Koda Akihide

  岐阜薬科大学 薬

• Timmerman Henk

  Leiden/amsterdam Center For Drug Research Division Of Medicinal Chemistry Vrije University

• Koda A

  Gifu Pharmaceutical Univ. Gifu Jpn

• Mori Hiroshi

  Department Of Architecture Graduate School Of Engineering Nagoya University

• Nemoto Hideo

  Laboratory Of Medical Chemistry Graduate School Of Medicine And Pharmaceutical Sciences University O

• KAWADA Kenji

  Gifu College of Medical Technology

• KODA AKIHIDE

  Department of Pharmacology, Gifu College of Pharmacy

• Nojima Hiroshi

  Department Of Pharmacology Faculty Of Pharmaceutical Sciences Ohu University

• Nagai Hiroichi

  Department Of Clinical Pharmacology Gifu Pharmaceutical University

• Koda Akihide

  Department Of Pharmacology Gifu College Of Pharmacy

• Koda Akihide

  Department Of Pharmacology Gifu Pharmaceutical University

• Nojima Hiroshi

  Laboratory Of Medical Chemistry Graduate School Of Medicine And Pharmaceutical Sciences University O

• Tanaka Hiroyuki

  Department Of Anesthesia And Clinical Research Institute National Hospital Organization Kyushu Medic

• Tanaka Hiroyuki

  Laboratory Of Bioresponses And Regulation United Graduate School Of Drug Discovery And Medical Infor

• Mori Hiroshi

  Department Of Pharmacology Gifu Pharmaceutical University

• Mori Hiroshi

  Department Of Applied Physics Okayama University Of Science

• Nagai Hiroichi

  Department Of Applied Pharmacology Graduate School Of Medicine And Pharmaceutical Sciences University Of Toyama

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