The Multifaceted Role of Baicalein in Cancer Management Through Modulation of Cell Signalling Pathways

Overview

Journal Molecules

Publisher MDPI

Specialty Biology

Date 2022 Nov 26

PMID 36432119

Authors

Arshad Husain Rahmani

Ahmad Almatroudi

Amjad Ali Khan

Ali Yousif Babiker

Malak Alanezi

Khaled S Allemailem

Affiliations

Soon will be listed here.

Abstract

The roles of medicinal plants or their purified bioactive compounds have attracted attention in the field of health sciences due to their low toxicity and minimal side effects. Baicalein is an active polyphenolic compound, isolated from and plays a significant role in the management of different diseases. Epidemiologic studies have proven that there is an inverse association between baicalein consumption and disease severity. Baicalein is known to display anticancer activity through the inhibition of inflammation and cell proliferation. Additionally, the anticancer potential of baicalein is chiefly mediated through the modulation of various cell-signaling pathways, such as the induction of apoptosis, autophagy, cell cycle arrest, inhibition of angiogenesis, signal transducer and activator of transcription 3, and PI3K/Akt pathways, as well as the regulation of other molecular targets. Therefore, the current review aimed to explore the role of baicalein in different types of cancer along with mechanisms of action. Besides this, the synergistic effects with other anti-cancerous drugs and the nano-formulation based delivery of baicalein have also been discussed.

Citing Articles

Review on role of honey in disease prevention and treatment through modulation of biological activities.

Rahmani A, Babiker A Open Life Sci. 2025; 20(1):20251069.

PMID: 40059876 PMC: 11889511. DOI: 10.1515/biol-2025-1069.

The Role of HK2 in Tumorigenesis and Development: Potential for Targeted Therapy with Natural Products.

He K, Tao F, Lu Y, Fang M, Huang H, Zhou Y Int J Med Sci. 2025; 22(4):790-805.

PMID: 39991762 PMC: 11843137. DOI: 10.7150/ijms.105553.

Mechanistic insights into the role of traditional Chinese medicine in treating gastric cancer.

Chen Z, Yu T, Wang Y, Li J, Zhang B, Zhou L Front Oncol. 2025; 14:1443686.

PMID: 39906672 PMC: 11790455. DOI: 10.3389/fonc.2024.1443686.

Comparison of Free Flavonoids and the Polyphenol Content in the Bran of a Newly Developed Sorghum Variety and Two Commercially Available Sorghum Varieties.

Santos M, Tanaka N, Kasuga S, Tanabe K, Hayashi C, Mizuno M Metabolites. 2024; 14(11).

PMID: 39590864 PMC: 11596866. DOI: 10.3390/metabo14110628.

Quercetin inhibits the epithelial-mesenchymal transition and reverses CDK4/6 inhibitor resistance in breast cancer by regulating circHIAT1/miR-19a-3p/CADM2 axis.

Li X, Niu C, Yi G, Zhang Y, Jin W, Zhang Z PLoS One. 2024; 19(7):e0305612.

PMID: 38990915 PMC: 11239024. DOI: 10.1371/journal.pone.0305612.

References

Li P, Hu J, Shi B, Tie J . Baicalein enhanced cisplatin sensitivity of gastric cancer cells by inducing cell apoptosis and autophagy via Akt/mTOR and Nrf2/Keap 1 pathway. Biochem Biophys Res Commun. 2020; 531(3):320-327. DOI: 10.1016/j.bbrc.2020.07.045. View

Zhao X, Qu J, Liu X, Wang J, Ma X, Zhao X . Baicalein suppress EMT of breast cancer by mediating tumor-associated macrophages polarization. Am J Cancer Res. 2018; 8(8):1528-1540. PMC: 6129485. View

Chen Y, Wu C, Shieh J, Wu J, Chen H, Chung T . Baicalein Triggers Mitochondria-Mediated Apoptosis and Enhances the Antileukemic Effect of Vincristine in Childhood Acute Lymphoblastic Leukemia CCRF-CEM Cells. Evid Based Complement Alternat Med. 2013; 2013:124747. PMC: 3580913. DOI: 10.1155/2013/124747. View

Sui X, Han X, Chen P, Wu Q, Feng J, Duan T . Baicalin Induces Apoptosis and Suppresses the Cell Cycle Progression of Lung Cancer Cells Through Downregulating Akt/mTOR Signaling Pathway. Front Mol Biosci. 2021; 7:602282. PMC: 7876332. DOI: 10.3389/fmolb.2020.602282. View

Guo Z, Hu X, Xing Z, Xing R, Lv R, Cheng X . Baicalein inhibits prostate cancer cell growth and metastasis via the caveolin-1/AKT/mTOR pathway. Mol Cell Biochem. 2015; 406(1-2):111-9. PMC: 4502300. DOI: 10.1007/s11010-015-2429-8. View

Pulido R, Baker S, Barata J, Carracedo A, Cid V, Chin-Sang I . A unified nomenclature and amino acid numbering for human PTEN. Sci Signal. 2014; 7(332):pe15. PMC: 4367864. DOI: 10.1126/scisignal.2005560. View

Ma G, Liu C, Wei B, Qiao J, Lu T, Wei H . Baicalein inhibits DMBA/TPA-induced skin tumorigenesis in mice by modulating proliferation, apoptosis, and inflammation. Inflammation. 2012; 36(2):457-67. DOI: 10.1007/s10753-012-9566-y. View

Zhou Q, Wang S, Zhang H, Lu Y, Wang X, Motoo Y . The combination of baicalin and baicalein enhances apoptosis via the ERK/p38 MAPK pathway in human breast cancer cells. Acta Pharmacol Sin. 2009; 30(12):1648-58. PMC: 4007493. DOI: 10.1038/aps.2009.166. View

Yan H, Xin S, Wang H, Ma J, Zhang H, Wei H . Baicalein inhibits MMP-2 expression in human ovarian cancer cells by suppressing the p38 MAPK-dependent NF-κB signaling pathway. Anticancer Drugs. 2015; 26(6):649-56. DOI: 10.1097/CAD.0000000000000230. View

10.

Tsujii M, DuBois R . Alterations in cellular adhesion and apoptosis in epithelial cells overexpressing prostaglandin endoperoxide synthase 2. Cell. 1995; 83(3):493-501. DOI: 10.1016/0092-8674(95)90127-2. View

11.

Panda P, Mukhopadhyay S, Das D, Sinha N, Naik P, Bhutia S . Mechanism of autophagic regulation in carcinogenesis and cancer therapeutics. Semin Cell Dev Biol. 2015; 39:43-55. DOI: 10.1016/j.semcdb.2015.02.013. View

12.

Bie B, Sun J, Guo Y, Li J, Jiang W, Yang J . Baicalein: A review of its anti-cancer effects and mechanisms in Hepatocellular Carcinoma. Biomed Pharmacother. 2017; 93:1285-1291. DOI: 10.1016/j.biopha.2017.07.068. View

13.

Chen C, Huang L, Huang C, Lin C, Lee Y, Lu F . Baicalein, a novel apoptotic agent for hepatoma cell lines: a potential medicine for hepatoma. Nutr Cancer. 2001; 38(2):287-95. DOI: 10.1207/S15327914NC382_19. View

14.

Chen F, Zhuang M, Zhong C, Peng J, Wang X, Li J . Baicalein reverses hypoxia-induced 5-FU resistance in gastric cancer AGS cells through suppression of glycolysis and the PTEN/Akt/HIF-1α signaling pathway. Oncol Rep. 2014; 33(1):457-63. DOI: 10.3892/or.2014.3550. View

15.

Zhang J, Lv H, Jiang K, Gao Y . Enhanced bioavailability after oral and pulmonary administration of baicalein nanocrystal. Int J Pharm. 2011; 420(1):180-8. DOI: 10.1016/j.ijpharm.2011.08.023. View

16.

Liu T, Gong W, Tan Z, Lu W, Wu X, Weng H . Baicalein inhibits progression of gallbladder cancer cells by downregulating ZFX. PLoS One. 2015; 10(1):e0114851. PMC: 4305301. DOI: 10.1371/journal.pone.0114851. View

17.

Plotnikov A, Flores K, Maik-Rachline G, Zehorai E, Kapri-Pardes E, Berti D . The nuclear translocation of ERK1/2 as an anticancer target. Nat Commun. 2015; 6:6685. DOI: 10.1038/ncomms7685. View

18.

Li W, Pi J, Zhang Y, Ma X, Zhang B, Wang S . A strategy to improve the oral availability of baicalein: The baicalein-theophylline cocrystal. Fitoterapia. 2018; 129:85-93. DOI: 10.1016/j.fitote.2018.06.018. View

19.

Park Y, Choi J, Jung H, Kim B, Kim C, Park S . Baicalein inhibits tumor progression by inhibiting tumor cell growth and tumor angiogenesis. Oncol Rep. 2017; 38(5):3011-3018. DOI: 10.3892/or.2017.6007. View

20.

Gao X, Xue X, Ma Y, Zhang S . Effect of baicalein on the expression of SATB1 in human breast cancer cells. Exp Ther Med. 2015; 9(5):1665-1669. PMC: 4471683. DOI: 10.3892/etm.2015.2329. View