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<p><i>Tripterygium wilfordii</i> Hook.f., commonly referred to as Thunder God Vine, is a vine used in traditional Chinese medicine to treat rheumatoid arthritis and psoriasis. Triptolide (TP), a diterpene triepoxide compound derived from <i>T. wilfordii</i> Hook.f., is known for its extensive pharmacological benefits, including antitumor, anti-inflammatory, immunosuppressive, antifertility, anticystogenic, neurotrophic, and neuroprotective properties. It represents the main active ingredient of <i>Tripterygium wilfordii</i> tablets and Tripterygium glycoside tablets, which are used clinically in China due to their anti-inflammatory and immunosuppressive effects. The diverse biological activities of TP make it an exceptional lead compound. However, its clinical application is significantly limited by poor solubility and severe toxicity. Despite the development of numerous TP analogs with the aim of improving water solubility or reducing toxicity, none have received clinical approval to date. Researchers have explored structural modifications, especially pro-drug strategies, to enhance solubility, enable targeted delivery, and reduce TP-related side effects. This review aims to discuss the advances made in pro-drug design for TP development, with an emphasis on recent advances in improving water solubility and reducing toxicity.</p>

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Pro-drug approaches to overcome poor solubility and toxicity of triptolide

  • 期刊论文

  • 发表日期：

    2025年8月6日

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  • Xinyue Zhang,
  • Xianye Chen,
  • Wei Song,
  • Zhihong Peng

摘要

Tripterygium wilfordii Hook.f., commonly referred to as Thunder God Vine, is a vine used in traditional Chinese medicine to treat rheumatoid arthritis and psoriasis. Triptolide (TP), a diterpene triepoxide compound derived from T. wilfordii Hook.f., is known for its extensive pharmacological benefits, including antitumor, anti-inflammatory, immunosuppressive, antifertility, anticystogenic, neurotrophic, and neuroprotective properties. It represents the main active ingredient of Tripterygium wilfordii tablets and Tripterygium glycoside tablets, which are used clinically in China due to their anti-inflammatory and immunosuppressive effects. The diverse biological activities of TP make it an exceptional lead compound. However, its clinical application is significantly limited by poor solubility and severe toxicity. Despite the development of numerous TP analogs with the aim of improving water solubility or reducing toxicity, none have received clinical approval to date. Researchers have explored structural modifications, especially pro-drug strategies, to enhance solubility, enable targeted delivery, and reduce TP-related side effects. This review aims to discuss the advances made in pro-drug design for TP development, with an emphasis on recent advances in improving water solubility and reducing toxicity.