2. Academic Validation
  3. Synergistic multi-target anti-inflammatory mechanisms of luteolin, chikusetsusaponin IVa and carabrone in Houyanqing formula

Synergistic multi-target anti-inflammatory mechanisms of luteolin, chikusetsusaponin IVa and carabrone in Houyanqing formula

  • J Ethnopharmacol. 2025 Jul 24:351:120096. doi: 10.1016/j.jep.2025.120096.
Caifeng Li 1,  Jianye Quan 2,  Ge Li 2,  Wei Liu 2,  Tong Lei 3,  Xuxia Cao 4,  Junxian Cao 2,  Lanyibo Liu 2,  Zhenkun Li 5,  Peng Chen 6,  Hongjun Yang 7
Affiliations

Affiliations

  • 1 Experimental Research Center, China Academy of Chinese Medical Sciences, Beijing, 100700, China; Analysis of Complex Effects of Proprietary Chinese Medicine, Hunan Provincial Key Laboratory, Yongzhou, Hunan Province, 425199, China.
  • 2 Experimental Research Center, China Academy of Chinese Medical Sciences, Beijing, 100700, China.
  • 3 Institute of Basic Theory for Chinese Medicine, China Academy of Chinese Medical Sciences, Beijing, 100700, China.
  • 4 School of Pharmacy, Binzhou Medical University, Yantai, 264003, China.
  • 5 Changchun University of Chinese Medicine, Changchun City, 130117, China. Electronic address: jxjmclzk@163.com.
  • 6 Experimental Research Center, China Academy of Chinese Medical Sciences, Beijing, 100700, China; Analysis of Complex Effects of Proprietary Chinese Medicine, Hunan Provincial Key Laboratory, Yongzhou, Hunan Province, 425199, China. Electronic address: sdzpchenpeng@qq.com.
  • 7 Experimental Research Center, China Academy of Chinese Medical Sciences, Beijing, 100700, China; Analysis of Complex Effects of Proprietary Chinese Medicine, Hunan Provincial Key Laboratory, Yongzhou, Hunan Province, 425199, China. Electronic address: hongjun0420@vip.sina.com.
PMID: 40473148 DOI: 10.1016/j.jep.2025.120096
Abstract

Ethnopharmacological relevance: Identifying the effective active ingredients in herbs, screening their targets, and elucidating their mechanisms of action may represent a crucial strategy for discovering new combination drugs. Houyanqing (HYQ) formula is a patented plant extract approved for marketing in China, which exhibits good anti-inflammatory effects in clinical practice. However, it is currently unclear which chemical components play the main anti-inflammatory role.

Aim of the study: This study aims to study the anti-inflammatory components of HYQ, and discover new targeted anti-inflammatory combination drugs through pharmacological research of traditional medicines.

Materials and methods: In this study, material components of HYQ both in vitro and in vivo were analyzed, and the anti-inflammatory effects was also evaluated by cell inflammation model and high-throughput detection methods. Subsequently, we analyzed the anti-inflammatory targets of these three components by a systematic chemical biology method, and further confirmed the anti-inflammatory efficacy of these molecular combinations.

Results: Three main components were identified that play a role in anti-inflammation: luteolin, chikusetsusaponin IVa, and carabrone. After target screening and validation, we found Chikusetsusaponin IVa binds to p50 and reduces the level of p50. Luteolin inhibits the interaction between p50 and annexin A2, thereby downregulating the transcription of inflammatory factors. Carabrone can reduce the levels of the pro-inflammatory mediator LTB4. The three components in HYQ formula work synergistically to exert anti-inflammatory effects by targeting different molecular entities and participating in various mechanisms.

Conclusions: The three key components of HYQ that enter the bloodstream exert synergistic anti-inflammatory effects by targeting different molecular entities and engaging in various mechanisms. The implementation of this research not only helps in understanding anti-inflammatory pharmacology of HYQ formula, but also provides a new strategy for screening combination anti-inflammatory molecules from traditional medicine.

Keywords

Anti-inflammation; Combination drugs; Natural products targets.

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