<p>Quinolones and their analogues are a remarkable group of drugs that have multiple impacts on the human immune system. They are suspected to mediate anti-cancer and anti-inflammatory responses. However, due to their effectiveness in treating a number of significant diseases, such as genitourinary cancer and breast cancer, as well as their antiangiogenic and immunomodulatory qualities, interest in this group of traditional medicines has recently increased. Unfortunately, numerous side effects were observed, such as diarrhea, skin rashes, nausea, vomiting, bleeding, and abnormal liver functions. To overcome these restrictions and to enhance the pharmacological profile, research efforts are focusing on the synthesis and optimization of novel quinolone analogues that lack severe side effects. The present study focuses on the mechanism of action and the signaling pathway involving the 4-anilinoquinolinylchalcone derivative. The objective of the present work was to better understand the mechanism by which anti-fibrosis is mediated by screening 6 synthesized 4-anilinoquinolinylchalcone derivatives for their potential as novel anti-fibrosis therapeutics.</p> Graphical abstract <p></p>

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4-Anilinoquinolinylchalcone derivatives mediate antifibrotic effects through ERK/MRTF—a signaling pathway crosstalk

  • Padhmavathi Selvam,
  • Chih Hua Tseng,
  • Ching Tung Wang,
  • Yu-Yo Sun,
  • Yeh-Long Chen,
  • Yu-Tse Kao,
  • Hans-Uwe Dahms,
  • Chih Mei Cheng

摘要

Quinolones and their analogues are a remarkable group of drugs that have multiple impacts on the human immune system. They are suspected to mediate anti-cancer and anti-inflammatory responses. However, due to their effectiveness in treating a number of significant diseases, such as genitourinary cancer and breast cancer, as well as their antiangiogenic and immunomodulatory qualities, interest in this group of traditional medicines has recently increased. Unfortunately, numerous side effects were observed, such as diarrhea, skin rashes, nausea, vomiting, bleeding, and abnormal liver functions. To overcome these restrictions and to enhance the pharmacological profile, research efforts are focusing on the synthesis and optimization of novel quinolone analogues that lack severe side effects. The present study focuses on the mechanism of action and the signaling pathway involving the 4-anilinoquinolinylchalcone derivative. The objective of the present work was to better understand the mechanism by which anti-fibrosis is mediated by screening 6 synthesized 4-anilinoquinolinylchalcone derivatives for their potential as novel anti-fibrosis therapeutics.

Graphical abstract