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Review

Bitter Chinese Herbal Medicine Exerts Pharmacological Effects via TAS2Rs: A Systematic Review from Natural Ligands to Therapeutic Potential

by
Lian Li
1,2,†,
Ruitong Dong
1,3,†,
Shibu Feng
4,
Yan Huang
1,5,
Xin Li
1,5,
Hanyun Que
1,2,
Huan Li
1,6,
Peng Wang
1,7,
Leu-Kim Fey
8,
Yi Zhang
4,
Zhaotong Cong
1,5,* and
Sanyin Zhang
1,5,*
1
Innovative Institute of Chinese Medicine and Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China
2
School of Preclinical Medicine, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China
3
School of Clinical Medicine, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China
4
School of Ethnic Medicine, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China
5
Institute of Herbgenomics, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China
6
School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China
7
School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China
8
M Kandiah Faculty of Medicine and Health Sciences, Universiti Tunku Abdul Rahman, Kajang 43000, Malaysia
*
Authors to whom correspondence should be addressed.
†
These authors contributed equally to this work.
Int. J. Mol. Sci. 2026, 27(7), 3073; https://doi.org/10.3390/ijms27073073
Submission received: 1 February 2026 / Revised: 15 March 2026 / Accepted: 23 March 2026 / Published: 27 March 2026
(This article belongs to the Special Issue G Protein-Coupled Receptor Signaling and Regulation, 2nd Edition)
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Abstract

Bitter compounds may function not only as taste substances but also as important active constituents mediating therapeutic effects. Their recognition is primarily mediated by bitter taste receptors (TAS2Rs), which exert pharmacological effects, such as regulating glucose metabolism, anti-inflammatory properties, and immune modulation, aligning closely with the therapeutic effects of bitter Chinese herbal medicine (BCHM). Contemporary pharmacological research has increasingly underscored the therapeutic potential of bitter traditional Chinese medicine (TCM), particularly through their bioactive constituents in the prevention and treatment of diverse pathological conditions. Here, we systematically review the diversity of bitter compounds from TCM and features of TAS2Rs, including their tissue distribution, physiological functions, structural characteristics, signal transduction mechanisms, and single-nucleotide polymorphisms. While numerous bitter phytochemicals have been characterized as agonists of TAS2Rs, the precise physiological functions and underlying molecular mechanisms mediated by TAS2R activation remain incompletely elucidated. This knowledge gap is largely attributable to several methodological and biological challenges, including the widespread tissue distribution of TAS2Rs, the complexity of their downstream signaling cascades, and the structural and functional heterogeneity of bitter compounds. This review outlines theoretical foundations, future perspectives and challenges for the drug development of TAS2R from BCHM.
Keywords: Chinese herbal medicine; bitter taste receptors; pharmacological effects; signaling pathway Chinese herbal medicine; bitter taste receptors; pharmacological effects; signaling pathway

Share and Cite

MDPI and ACS Style

Li, L.; Dong, R.; Feng, S.; Huang, Y.; Li, X.; Que, H.; Li, H.; Wang, P.; Fey, L.-K.; Zhang, Y.; et al. Bitter Chinese Herbal Medicine Exerts Pharmacological Effects via TAS2Rs: A Systematic Review from Natural Ligands to Therapeutic Potential. Int. J. Mol. Sci. 2026, 27, 3073. https://doi.org/10.3390/ijms27073073

AMA Style

Li L, Dong R, Feng S, Huang Y, Li X, Que H, Li H, Wang P, Fey L-K, Zhang Y, et al. Bitter Chinese Herbal Medicine Exerts Pharmacological Effects via TAS2Rs: A Systematic Review from Natural Ligands to Therapeutic Potential. International Journal of Molecular Sciences. 2026; 27(7):3073. https://doi.org/10.3390/ijms27073073

Chicago/Turabian Style

Li, Lian, Ruitong Dong, Shibu Feng, Yan Huang, Xin Li, Hanyun Que, Huan Li, Peng Wang, Leu-Kim Fey, Yi Zhang, and et al. 2026. "Bitter Chinese Herbal Medicine Exerts Pharmacological Effects via TAS2Rs: A Systematic Review from Natural Ligands to Therapeutic Potential" International Journal of Molecular Sciences 27, no. 7: 3073. https://doi.org/10.3390/ijms27073073

APA Style

Li, L., Dong, R., Feng, S., Huang, Y., Li, X., Que, H., Li, H., Wang, P., Fey, L.-K., Zhang, Y., Cong, Z., & Zhang, S. (2026). Bitter Chinese Herbal Medicine Exerts Pharmacological Effects via TAS2Rs: A Systematic Review from Natural Ligands to Therapeutic Potential. International Journal of Molecular Sciences, 27(7), 3073. https://doi.org/10.3390/ijms27073073

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