LAUSR

Helicobacter pylori (H. pylori) infection plays a critical role in pathogenesis of gastric ulcer and gastric cancer. Thus, the eradication of H. pylori could prevent the onset of these diseases. At present the standard therapy against H. pylori infection is a combination therapy of a proton pump inhibitor and two antibiotics such as clarithromycin and amoxicillin. However, there exist H. pylori strains that show resistance against these antibiotics. Furthermore, adverse effect of these antibiotics against intestinal bacteria is unavoidable. We previously discovered a novel compound, intervenolin, from the culture broth of Nocardia sp. ML96-86F2. Intervenolin is a very unique compound having both antitumor and anti-H. pylori activities. To create a potent anti-H. pylori compound, we synthesized various derivatives of intervenolin. Among them we identified compounds that show selective anti-H. pylori activity in vitro without effect on other bacteria including intestinal bacteria. Oral monotherapy of the derivative exerts a significant eradicative effect against H. pylori-infected mice more than the standard combination therapy. Taken together, we have successfully created a potent new anti-H. pylori compound. Citation Format: Manabu Kawada, Tomokazu Ohishi, Hikaru Abe, Chigusa Hayashi, Chiharu Sakashita, Shun-ichi Ohba, Hiroyuki Inoue, Masayuki Igarashi, Takumi Watanabe, Masakatsu Shibasaki. Anti-Helicobacter pylori activity of a novel derivative of intervenolin [abstract]. In: Proceedings of the AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics; 2017 Oct 26-30; Philadelphia, PA. Philadelphia (PA): AACR; Mol Cancer Ther 2018;17(1 Suppl):Abstract nr A122.