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<p>Genipin, a natural blue pigment and bioactive compound derived from the fruit of <i>Gardenia jasminoides</i> Ellis., has long been used in traditional Chinese medicine to prevent and treat various inflammation-driven diseases. However, current literature on the comprehensive analysis of genipin as a therapeutic agent are scarce. In this review, we described the chemical and biochemical properties of genipin. Scientometric analysis revealed advances and future perspectives of genipin in preclinical studies. A network pharmacology study was used to elucidate the molecular pharmacological mechanisms and possible therapeutic potentials of genipin. The above results suggest that genipin has anti-inflammatory, antioxidant, anticancer, hepatoprotective, antidiabetic, antidepressant, neuroprotective, and other therapeutic effects, providing a therapeutic potential for inflammatory bowel disease, acute lung injury, cancer, diabetes, depressive disorder, Alzheimer's disease, and Parkinson’s disease in the clinical application. Currently, clinical trials of genipin are lacking. Owing to the liver toxicity of genipin, 18 optimized lead compounds were generated through the OptADMET platform. In the future, the study of genipin will focus mainly on optimizing drug structure, exploring pharmacological mechanisms, conducting clinical trials, studying combination therapies, developing new formulations, conducting long-term safety evaluations, and enhancing scientific communications. In summary, this scientific data-driven review provides a foundation for future research and development of genipin as a therapeutic agent.</p>

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A scientific data-driven review of natural product genipin for disease therapy

  • 期刊论文

  • 发表日期：

    2025年1月29日

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  • Dong Xu,
  • Tao Qiao,
  • Kai Gao,
  • Mei-Na Zhao,
  • Wei Zhang,
  • Xing-Ru Tao,
  • Jing-Wen Wang

摘要

Genipin, a natural blue pigment and bioactive compound derived from the fruit of Gardenia jasminoides Ellis., has long been used in traditional Chinese medicine to prevent and treat various inflammation-driven diseases. However, current literature on the comprehensive analysis of genipin as a therapeutic agent are scarce. In this review, we described the chemical and biochemical properties of genipin. Scientometric analysis revealed advances and future perspectives of genipin in preclinical studies. A network pharmacology study was used to elucidate the molecular pharmacological mechanisms and possible therapeutic potentials of genipin. The above results suggest that genipin has anti-inflammatory, antioxidant, anticancer, hepatoprotective, antidiabetic, antidepressant, neuroprotective, and other therapeutic effects, providing a therapeutic potential for inflammatory bowel disease, acute lung injury, cancer, diabetes, depressive disorder, Alzheimer's disease, and Parkinson’s disease in the clinical application. Currently, clinical trials of genipin are lacking. Owing to the liver toxicity of genipin, 18 optimized lead compounds were generated through the OptADMET platform. In the future, the study of genipin will focus mainly on optimizing drug structure, exploring pharmacological mechanisms, conducting clinical trials, studying combination therapies, developing new formulations, conducting long-term safety evaluations, and enhancing scientific communications. In summary, this scientific data-driven review provides a foundation for future research and development of genipin as a therapeutic agent.