Letter to the editor

An up-to-date overview of baicalein and its biological and pharmacological activities

Hyeon Ji Yeo1, Jung Hun Lee2, Sun Sik Kong3, Mun Hyoung Ahn4, Jiye Rhee4, Chang Ha Park4[*]

1Honam National Institute of Biological Resources, 99 Gohadoangil, Mokpo, 587262, Republic of Korea

2Department of Digital Healthcare Convergence, Songho University, 210 Namsan-Ro, Hoengseong-Eup, Hoengseong-Gun, Gangwon-Do, Republic of Korea

3College of General Education, Namseoul University, 91 Daehak-ro, Seonghwan-eup, Seobuk-gu, Cheonan-si, Chungcheongnam-do 31020, Republic of Korea

4Department of Smart Farm, Namseoul University, 91 Daehak-ro, Seonghwan-eup, Seobuk-gu, Cheonan-si, Chungcheongnam-do 31020, Republic of Korea

EXCLI J 2025;24:Doc1056

 



Baicalein (5,6,7-trihydroxyflavone) is a representative flavone found in Scutellaria spp., particularly Scutellaria baicalensis and S. lateriflora (Zhu et al., 2024[24]) Baicalein can be biosynthesized from phenylalanine, an initial precursor, with serial enzymatic reactions mediated by phenylalanine ammonialyase, cinnamate 4-hydroxylase, cinnamate-CoA ligase, chalcone synthase, chalcone isomerase, flavone synthase II, and flavone 6-hydroxylase (Yeo et al., 2025[22]). Baicalein is beneficial to human health owing to its antioxidant, anti-inflammatory, anti-cancer, anti-diabetic, antimicrobial, anti-aging, cardioprotective, neuroprotective, respiratory-protective, gastroprotective, liver-protective, and kidney-protective effects (Munjal et al., 2024[15]). In particular, baicalein has received attention as an antitumor agent owing to its high efficacy and low toxicity in the treatment of malignant tumors (Lei et al., 2024[11]). This letter provides an overview of the recent studies conducted to assess the biological and pharmacological properties of baicalein (Table 1(Tab. 1); References in Table 1: Chen et al., 2024[1]; Chi et al., 2025[2]; Dong et al., 2024[3]; Du et al., 2025[4]; Fang et al., 2024[5]; Guo et al., 2024[6]; Hao et al., 2025[7]; Huang et al., 2024[8]; Jin et al., 2024[9]; Lai et al., 2024[10]; Li et al., 2024[13], 2025[12]; Liu et al., 2024[14]; Park et al., 2024[16]; Ren et al., 2024[17]; Wang et al., 2024[18], 2024[19], 2025[20]; Xu et al., 2025[21]; Zhang et al., 2025[23]).

Declaration

Acknowledgments

Funding for this paper was provided by Chungcheongnam-do Regional Innovation System for Education (RISE) Project.

Conflicts of interest

The authors declare no conflict of interest.

 

References

1. Chen J, Zhang Q, Xu W, Li Z, Chen X, Luo Q, et al. Baicalein upregulates macrophage TREM2 expression via TrKB-CREB1 pathway to attenuate acute inflammatory injury in acute-on-chronic liver failure. Int Immunopharmacol. 2024;139:112685
2. Chi F, Cheng C, Liu K, Sun T, Zhang M, Hou Y, et al. Baicalein disrupts the KEAP1-NRF2 interaction to alleviate oxidative stress injury by inhibiting M1 macrophage polarization. Free Radic Biol Med. 2025;227:557-69
3. Dong Y, He G, Chen K, He X, Pan M, Huang X, et al. Baicalein promotes KDM4E to induce BICD1 and inhibit triple‐negative breast cancer progression by blocking PAR1 signaling. Mol Carcinog. 2024;63:1288-302
4. Du L-x, Gao X-y, Ren X-q, Yang Y-y, Ding Y-y, Xu A, et al. Baicalein ameliorates chronic itch in ACD mice by suppressing the spinal astrocytic STAT3–LCN2 cascade. Acta Pharmacol Sin. 2025;46:366-79
5. Fang C, Liu X, Zhang F, Song T. Baicalein Inhibits Cerebral Ischemia-Reperfusion Injury through SIRT6-Mediated FOXA2 Deacetylation to Promote SLC7A11 Expression. eNeuro. 2024;11(10):ENEURO.0174-24.2024
6. Guo S, Zhou L, Liu X, Gao L, Li Y, Wu Y. Baicalein alleviates cisplatin-induced acute kidney injury by inhibiting ALOX12-dependent ferroptosis. Phytomedicine. 2024;130:155757
7. Hao B, Lin S, Liu H, Xu J, Chen L, Zheng T, et al. Baicalein tethers CD274/PD-L1 for autophagic degradation to boost antitumor immunity. Autophagy. 2025;21:917-33
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9. Jin Y, Wu Q, Pan S, Zhou Q, Liu H, Zhang Q, et al. Baicalein enhances cisplatin sensitivity in cervical cancer cells by promoting cuproptosis through the Akt pathway. Biomed Pharmacother. 2024;179:117415
10. Lai J-q, Zhao L-l, Hong C, Zou Q-m, Su J-x, Li S-j, et al. Baicalein triggers ferroptosis in colorectal cancer cells via blocking the JAK2/STAT3/GPX4 axis. Acta Pharmacol Sin. 2024;45:1715-26
11. Lei C, Yu Y, Zhu Y, Li Y, Ma C, Ding L, et al. The most recent progress of baicalein in its anti-neoplastic effects and mechanisms. Biomed Pharmacother. 2024;176:116862
12. Li J, Zhang D, Wang S, Yu P, Sun J, Zhang Y, et al. Baicalein induces apoptosis by inhibiting the glutamine-mTOR metabolic pathway in lung cancer. J Adv Res. 2025;68:341-57
13. Li Y-y, Peng Y-q, Yang Y-x, Shi T-j, Liu R-x, Luan Y-y, et al. Baicalein improves the symptoms of polycystic ovary syndrome by mitigating oxidative stress and ferroptosis in the ovary and gravid placenta. Phytomedicine. 2024;128:155423
14. Liu Z, Zheng X, Li N, Wang Z. Baicalein suppresses inflammation and attenuates acute lung injury by inhibiting glycolysis via HIF‑1α signaling. Mol Med Report. 2024;31(1):18
15. Munjal K, Goel Y, Gauttam VK, Chopra H, Singla M, Gupta S, et al. Molecular targets and therapeutic potential of baicalein: a review. Drug Target Insights. 2024;18:30
16. Park W, Jang H, Kim HS, Park SJ, Lim W, Song G, et al. Therapeutic efficacy and anti-inflammatory mechanism of baicalein on endometriosis progression in patient-derived cell line and mouse model. Phytomedicine. 2024;130:155469
17. Ren H, Feng J, Hong M, Liu Z, Muyey DM, Zhang Y, et al. Baicalein attenuates oxidative damage in mice haematopoietic cells through regulation of PDGFRβ. Mol Cell Probes. 2024;76:101966
18. Wang T, Wang S, Jia X, Li C, Ma X, Tong H, et al. Baicalein alleviates cardiomyocyte death in EAM mice by inhibiting the JAK-STAT1/4 signalling pathway. Phytomedicine. 2024;128:155558
19. Wang W, Tang Y, Zhuo X, Yang J, Gao Z, Li C, et al. Baicalein targets MAPK9 to induce apoptosis of hepatocellular carcinoma cells. Chem Biol Drug Des. 2024;104(3):e14623
20. Wang X, Zhou Y, Liu Y, Mo T, Chen Z, Zhang Y, et al. Baicalein Reduces Pyroptosis of Acinar Cells in Hyperlipidemic Acute Pancreatitis by Inhibiting M1 Polarization of Macrophages via the HMGB1/TLR4/ NLRP3 Pathway. Inflammation. 2025;epub ahead of print
21. Xu Y, Xu L, Jian X, Wang Q, Li Z, Ge H. Baicalein attenuates ovalbumin-induced allergic rhinitis through the activation of nuclear receptor subfamily 4 group a member 1. Immunol Res. 2025;73(1):32
22. Yeo HJ, Shin SY, Park SU, Park CH. Postharvest wounding treatment influences flavone production and biological activities of the hairy root cultures of Scutellaria baicalensis. Chem Biol Technol Agricult. 2025;12(1):13
23. Zhang Z, Zhang X, Yang Y, Wang H, Yang X, Xuan L, et al. Baicalein protects against heart failure by improving mitochondrial dysfunction and regulating endoplasmic reticulum stress to reduce apoptosis in vitro and in vivo. Int J Immunopathol Pharmacol. 2025;39:03946320251315800
24. Zhu L, Zhang Y, Zhu W, Ji J, Bai X, Huang P. The evaluation of the interaction of baicalein (5, 6, 7-trihydroxyflavone) with human IgG and a glioblastoma multiforme (GBM) cell line. Arab J Chem. 2024;17 (10):105949
 
 
 

Table 1: The biological and pharmacological activities of baicalein according to recent studies

[*] Corresponding Author:

Chang Ha Park, Department of Smart Farm, Namseoul University, 91 Daehak-ro, Seonghwan-eup, Seobuk-gu, Cheonan-si, Chungcheongnam-do 31020, Republic of Korea; Tel.: +82-41-580-3254, eMail: parkch@nsu.ac.kr