作者: Lee, Jae Min ; Choi, Hyuk Soon ; Jeen, Yoon Tae ; Kim, Chang Duck ; Hong, Junghwa ; Um, Soon Ho ; Keum, Bora ; Kim, Yoonjin ; Sul, Donggeun ; Lim, Ji-Youn ; Chun, Hoon Jai ; Seo, Yeon Seok ; Kim, Ye Ji ; Kim, Eun Sun ; Lee, Hong Sik ; Ryu, Ho Sang

The present study investigated benexate hydrochloride betadex (BHB)-mediated ulcer healing, and changes to microcirculation modulated through nitric oxide synthase (NOS) and anti-inflammatory activity. A rat model of gastric mucosal injury was established through injection of a 60% acetic acid solution into the stomach. Following ulcer induction, the rats were administered BHB orally for 5 days at doses of 0, 100, 300 or 1,000 mg/kg. The highest dose of BHB was also administered with or without L-NG-nitroarginine methyl ester (L-NAME). The area of gastric ulcers was determined by planimetry, and expression of cyclooxygenases (COX), cytokines and NOS in stomach tissues were measured using western blotting. Compared with the control group, gastric ulcer size was significantly decreased in the 1,000 mg/kg BHB-treated group (P<0.05). Administration of BHB led to a significant increase in endothelial (e)NOS expression (P<0.05). Although acetic acid co-treatment with L-NAME induced more severe mucosal damage, BHB decreased COX expression and tumor necrosis factor-α levels when administered with the nitric oxide inhibitor, L-NAME (P<0.05). BHB exhibited protective effects in a rat model of gastric ulcers, which were associated with a decrease in pro-inflammatory cytokine levels and the activation of eNOS.

1996-08-01·Life Sciences3区 · 医学

Inhibition of constitutive nitric oxide synthase by benexate

3区 · 医学

Article

作者: Toshikazu Yoshikawa ; Yumiko Komori ; Yoshito Kumagai ; Toyoko Arimoto

We evaluated the inhibitory action of benexate (benzyl 2-[trans-4 -(guanidinomethyl) cyclohexylcarbonyloxy] benzoate hydrochloride beta-cyclodextrin clathrate), an anti-ulcer agent, on the formation of nitric oxide by stomach and brain enzyme preparations and on the purified neuronal nitric oxide synthase (NOS). Benexate markedly inhibited NOS activities of both stomach and brain preparations, with IC50 values of 68 and 29 microM, respectively. The results of double-reciprocal analysis suggested that the inhibition was competitive with an arginine substrate. Experiments with purified NOS revealed that benexate suppressed not only citrulline formation but also the oxidation of NADPH and the production of hydrogen peroxide by the enzyme. Taken together, it is indicated that benexate is an inhibitor for NOS in spite of the fact the drug elicits an increase in blood flow in a gastric mucosa.

1996-01-01·Journal of Antimicrobial Chemotherapy2区 · 医学

In-vitro and in-vivo antibacterial activity of plaunotol, a cytoprotective antiulcer agent, against Helicobacter pylori

2区 · 医学

Article

作者: Chika Ishii ; Hiroshi Yasuda ; Yukio Utsui ; Tetsufumi Koga ; Harumi Kawada ; Haruki Domon

Recently, some antiulcer agents have been reported to have antibacterial activity against Helicobacter pylori, which is highly associated with gastritis and peptic ulcers. In-vitro and in-vivo activity of plaunotol, a cytoprotective antiulcer agent, against H. pylori was investigated. Antibacterial activity of plaunotol against a standard strain (NCTC 11637) and 14 clinical isolates was compared with those of other cytoprotective antiulcer agents: benexate, sofalcone, teprenone, cetraxate, and gefarnate, by an agar dilution method. The MIC50 and MIC90 of plaunotol against 15 strains were 6.25 and 12.5 mg/L, respectively, making it the most potent of the cytoprotective antiulcer agents. The bactericidal effect of plaunotol was investigated using an in-vitro killing assay. Plaunotol at concentrations of more than 6 mg/L induced a rapid reduction of culture turbidity, with an extensive loss of viability, within 30 min. Observation by scanning electron microscopy revealed that plaunotol caused autolysis and treated cells were deformed. In-vivo activity of plaunotol against H. pylori was examined in a nude mouse gastritis model. Plaunotol significantly decreased the number of H. pylori in the stomach of nude mice. In addition, the antiulcer agent enhanced the antibacterial activity of amoxycillin or clarithromycin in the infection model.

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KEGG	Wiki	ATC	Drug Bank
D02452	盐酸贝奈克酯	A02B	-

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适应症	国家/地区	公司	日期
急性胃炎	日本	Kyowa Pharmaceutical Industry Co., Ltd.	1989-12-18
慢性胃炎	日本	Kyowa Pharmaceutical Industry Co., Ltd.	1989-12-18
胃溃疡	日本	Kyowa Pharmaceutical Industry Co., Ltd.	1987-10-02