Scholarlink

<p>Leishmaniasis is a neglected tropical disease posing significant global health challenges. Given the limited effective treatment options and associated constraints, many patients are unable to complete therapy. In this study, we report the remarkable leishmanicidal activity of onnamides derived from the marine sponge <i>Theonella</i> sp. against the promastigote form of <i>Leishmania major</i> (IC<sub>50</sub> = 0.2–140&#xa0;nM) and demonstrate their selectivity through cytotoxicity assessments on human hepatoma HepG2 cells. Structural-activity relationship (SAR) analyses were conducted using 6,7-dihydro-onnamide A and its analogs. Furthermore, we compared the action mechanisms of amphotericin B, the primary drug currently used for treatment, and the obtained onnamides. Based on biological evaluations and SAR studies, onnamides can be considered promising candidates for anti-leishmanial chemotherapy, warranting further investigation.</p>

错误：搜索内容不能为空，请输入英文关键词
错误：关键词超出字数限制，请精简
高级检索

Onnamides and a Novel Analogue, Onnamide G, as Potent Leishmanicidal Agents

  • 期刊论文

  • 出版模式：

    开放获取

  • 发表日期：

    2025年9月5日

查看全文
  • Takahiro Jomori,
  • Nanami Higa,
  • Trianda Ayuning Tyas,
  • Natsuki Matsuura,
  • Yudai Ueda,
  • Ayumi Suetake,
  • Shin Miyazaki,
  • Shuichi Watanabe,
  • Sei Arizono,
  • Yasuhiro Hayashi,
  • Ko Yasumoto,
  • Yuji Ise,
  • Toshiyuki Wakimoto,
  • Mina Yasumoto-Hirose,
  • Junichi Tanaka,
  • Kanami Mori-Yasumoto

摘要

Leishmaniasis is a neglected tropical disease posing significant global health challenges. Given the limited effective treatment options and associated constraints, many patients are unable to complete therapy. In this study, we report the remarkable leishmanicidal activity of onnamides derived from the marine sponge Theonella sp. against the promastigote form of Leishmania major (IC50 = 0.2–140 nM) and demonstrate their selectivity through cytotoxicity assessments on human hepatoma HepG2 cells. Structural-activity relationship (SAR) analyses were conducted using 6,7-dihydro-onnamide A and its analogs. Furthermore, we compared the action mechanisms of amphotericin B, the primary drug currently used for treatment, and the obtained onnamides. Based on biological evaluations and SAR studies, onnamides can be considered promising candidates for anti-leishmanial chemotherapy, warranting further investigation.