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The team of Ma Hongyue and Duan Jinao from Nanjing University of Chinese Medicine collaborated with the team of Xu Huaiqiang from the Shanghai Institute of Materia Medica, Chinese Academy of Sciences. They selected three key active components, 5-OH-DMT and others, from bufotenin, and systematically analyzed their "structure - target - effect - toxicity - activity" relationships. At the atomic resolution level, they revealed the molecular mechanism by which the components selectively activate the 5-HT1A receptor subtypes. This research provided solid molecular pharmacological support for the classic pharmacological properties of bufotenin and also offered an example for explaining the differences in the component spectra of traditional Chinese medicine and their correlations with pharmacological effects. The related study was titled "Structural pharmacology of bufotenine derivatives in activating the 5-HT1A receptor for therapeutic potential in depression and anxiety" and was published in Research. Citation: Shu-jie Li, Qing-ning Yuan, Wen-yuan Wu, Zhi-han Chen, Duo Chen, Hong Shan, Qin-yu Chu, Wen Hu, Kai Wu, Tao Liu, et al. Structural Pharmacology of Bufotenine Derivatives in Activating the 5-HT1A Receptor for Therapeutic Potential in Depression and Anxiety. Research. 2025; 8:0987. DOI: 10.34133/research.0987 https://spj.science.org/doi/10.34133/research.0987
1 Research Background
Toad venom was first recorded in "The Pharmacological Treatise", and as a traditional precious medicinal herb, it holds an important position in the treasure house of traditional Chinese medicine. The "Compendium of Materia Medica" states that it "cures sores, ulcers, and all kinds of malignant swellings", and has the efficacy of "opening orifices, awakening the mind, and eliminating toxins and swelling". The Ming Dynasty physician Zhang Jingyue in "The Complete Works of Jingyao" even mentioned that toad venom "is good at resolving depression and breaking hard lumps", emphasizing its function of regulating qi and relieving depression. Over thousands of years, toad venom has been the core medicinal ingredient of classic formulas such as "Six God Pills" and "Plum Blossom Tongue Drops", playing a unique therapeutic role in clinical practice.
According to traditional Chinese medicine theory, depression belongs to the category of "depression syndrome", closely related to liver qi stagnation and loss of nourishment of the mind. The "Huangdi Neijing · Suwen" states: "Wood depression is relieved by stimulation" and "Fire depression is released by stimulation", emphasizing that the treatment of depression syndrome should be based on promoting circulation. Toad venom is warm in nature and belongs to the meridians of heart and liver, capable of "dispelling wind and fire depression" and "opening orifices and awakening the mind", which is in line with the modern anti-depression treatment concept. However, the mechanism of action of traditional Chinese medicine has long been in a state of "knowing the result but not the reason", restricting the modernization process of traditional Chinese medicine. Deciphering the molecular code of the "opening orifices and awakening the mind" and "dispelling fire depression" pharmacological properties of toad venom is precisely the key to the inheritance and innovation of traditional Chinese medicine.
2 Research Progress
The research team led by Professor Ma Hongyue/Duan Jinao from Nanjing University of Chinese Medicine, based on more than ten years of in-depth research on the efficacy substances of toad venom, collaborated with Professor Xu Huaiqiang from the Shanghai Institute of Pharmaceutical Science of the Chinese Academy of Sciences. The research team selected key components (5-OH-DMT, 5-MeO-DMT, 5-OH-TMT) from natural toad toxins with different medicinal properties (awakening the mind, hallucinogenic, and detoxifying) to systematically analyze their "structure-target-effect-toxinicity" relationship. At the atomic resolution level, they revealed the molecular mechanism of selective activation of serotonin receptors (5-HTR) subtypes by toad coloramines under different medicinal property labels. This research provides a solid molecular pharmacological basis for the modern interpretation of the "dispelling wind and fire depression" and "opening orifices and awakening the mind" pharmacological properties of traditional Chinese medicine toad venom, and helps to understand why the component spectra of the same medicinal herb from different sources or processed products can produce completely different pharmacological properties.
