Polyphenols of Chinese Skullcap Roots: from Chemical Profiles to Anticancer Effects

Overview

Journal RSC Adv

Publisher Royal Society of Chemistry

Specialty Chemistry

Date 2022 May 9

PMID 35530094

Authors

Lingchong Wang

Dapeng Zhang

Ning Wang

Sha Li

Hor-Yue Tan

Yibin Feng

Affiliations

Soon will be listed here.

Abstract

Great efforts have been made to identify the principle bioactive constituents of Chinese herbs and to unravel the molecular mechanisms behind their anticancer effects. (Huangqin or Chinese skullcap) is a widely consumed herbal medicine and has been historically used in anticancer therapy in China and other countries. Chinese skullcap generates many active chemicals in the root and is abundant in polyphenols, which act as its anti-cancer ingredients. It contains around 53 polyphenols in total: 50 flavonoids and 3 stilbenes. The polyphenols have similar chemical structures since they are derived from similar biochemical synthetic pathways. According to the literature, as the active chemicals of the skullcap root, 18 polyphenols exhibit evident anticancer activities. They can be developed not only as novel candidates and precursors in anticancer drug screening, but also as important tools and agents in cancer pharmacology. We comprehensively elaborated the anticancer pharmacological properties of crude polyphenolic extracts and 12 other single compounds excluding the six well-known polyphenols, , baicalein, baicalin, wogonin, wogonoside, chrysin and verbascoside. In this review, we also discussed the possible mechanisms of the anticancer effect of several skullcap polyphenols. Overall, this paper provides a unique path to understand the anticancer properties of Chinese skullcap as well as guidance to find novel anticancer drugs from a natural polyphenolic reservoir.

Citing Articles

The Effect of the Extraction Conditions on the Antioxidant Activity and Bioactive Compounds Content in Ethanolic Extracts of Root.

Dzieciol M, Wala K, Wroblewska A, Janda-Milczarek K Molecules. 2024; 29(17).

PMID: 39275001 PMC: 11397618. DOI: 10.3390/molecules29174153.

Research progress on pharmacological properties and application of probiotics in the fermentation of Georgi.

Guo F, Li C, Dou J, Liang J, Chen Z, Xu Z Front Nutr. 2024; 11:1407182.

PMID: 38903628 PMC: 11187263. DOI: 10.3389/fnut.2024.1407182.

Therapeutic and immune-regulation effects of Georgi polysaccharide on pseudorabies in piglets.

Shu X, Zhang X, Zhang Y, Shu Y, Wang Y, Zhang Z Front Vet Sci. 2024; 11:1356819.

PMID: 38500605 PMC: 10944897. DOI: 10.3389/fvets.2024.1356819.

Challenges in Medicinal and Aromatic Plants DNA Barcoding-Lessons from the Lamiaceae.

Nazar N, Howard C, Slater A, Sgamma T Plants (Basel). 2022; 11(1).

PMID: 35009140 PMC: 8747715. DOI: 10.3390/plants11010137.

References

Zhang L, Pu Z, Wang J, Zhang Z, Hu D, Wang J . Baicalin inhibits hypoxia-induced pulmonary artery smooth muscle cell proliferation via the AKT/HIF-1α/p27-associated pathway. Int J Mol Sci. 2014; 15(5):8153-68. PMC: 4057725. DOI: 10.3390/ijms15058153. View

Holzner S, Brenner S, Atanasov A, Senfter D, Stadler S, Nguyen C . Intravasation of SW620 colon cancer cell spheroids through the blood endothelial barrier is inhibited by clinical drugs and flavonoids in vitro. Food Chem Toxicol. 2017; 111:114-124. DOI: 10.1016/j.fct.2017.11.015. View

Sonoda M, Nishiyama T, Matsukawa Y, Moriyasu M . Cytotoxic activities of flavonoids from two Scutellaria plants in Chinese medicine. J Ethnopharmacol. 2004; 91(1):65-8. DOI: 10.1016/j.jep.2003.11.014. View

Zhao L, Sha Y, Zhao Q, Yao J, Zhu B, Lu Z . Enhanced 5-fluorouracil cytotoxicity in high COX-2 expressing hepatocellular carcinoma cells by wogonin via the PI3K/Akt pathway. Biochem Cell Biol. 2013; 91(4):221-9. DOI: 10.1139/bcb-2012-0077. View

Wang C, Li X, Wang Q, Mehendale S, Yuan C . Selective fraction of Scutellaria baicalensis and its chemopreventive effects on MCF-7 human breast cancer cells. Phytomedicine. 2009; 17(1):63-8. PMC: 2789205. DOI: 10.1016/j.phymed.2009.07.003. View

Haslam E, Lilley T, Cai Y, Martin R, Magnolato D . Traditional herbal medicines--the role of polyphenols. Planta Med. 1989; 55(1):1-8. DOI: 10.1055/s-2006-961764. View

Wei L, Dai Y, Zhou Y, He Z, Yao J, Zhao L . Oroxylin A activates PKM1/HNF4 alpha to induce hepatoma differentiation and block cancer progression. Cell Death Dis. 2017; 8(7):e2944. PMC: 5550876. DOI: 10.1038/cddis.2017.335. View

Kimura Y, Sumiyoshi M . Effects of various flavonoids isolated from Scutellaria baicalensis roots on skin damage in acute UVB-irradiated hairless mice. J Pharm Pharmacol. 2011; 63(12):1613-23. DOI: 10.1111/j.2042-7158.2011.01365.x. View

Mu R, Qi Q, Gu H, Wang J, Yang Y, Rong J . Involvement of p53 in oroxylin A-induced apoptosis in cancer cells. Mol Carcinog. 2009; 48(12):1159-69. DOI: 10.1002/mc.20570. View

10.

Lee M, Oh W, Kim B, Ahn S, Kang D, Sohn C . Inhibition of VHR dual-specificity protein tyrosine phosphatase activity by flavonoids isolated from Scutellaria baicalensis: structure-activity relationships. Planta Med. 2002; 68(12):1063-5. DOI: 10.1055/s-2002-36351. View

11.

Yang N, Zhao Y, Wang Z, Liu Y, Zhang Y . Scutellarin suppresses growth and causes apoptosis of human colorectal cancer cells by regulating the p53 pathway. Mol Med Rep. 2016; 15(2):929-935. DOI: 10.3892/mmr.2016.6081. View

12.

Wang C, Zhang C, Chen L, Anderson S, Lu F, Yuan C . Colon cancer chemopreventive effects of baicalein, an active enteric microbiome metabolite from baicalin. Int J Oncol. 2015; 47(5):1749-58. PMC: 4599184. DOI: 10.3892/ijo.2015.3173. View

13.

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

14.

Kavandi L, Lee L, Bokhari A, Pirog J, Jiang Y, Ahmad K . The Chinese herbs Scutellaria baicalensis and Fritillaria cirrhosa target NFκB to inhibit proliferation of ovarian and endometrial cancer cells. Mol Carcinog. 2013; 54(5):368-78. DOI: 10.1002/mc.22107. View

15.

Gao J, Morgan W, Sanchez-Medina A, Corcoran O . The ethanol extract of Scutellaria baicalensis and the active compounds induce cell cycle arrest and apoptosis including upregulation of p53 and Bax in human lung cancer cells. Toxicol Appl Pharmacol. 2011; 254(3):221-8. DOI: 10.1016/j.taap.2011.03.016. View

16.

Hussain I, Waheed S, Ahmad K, Pirog J, Syed V . Scutellaria baicalensis targets the hypoxia-inducible factor-1α and enhances cisplatin efficacy in ovarian cancer. J Cell Biochem. 2018; 119(9):7515-7524. DOI: 10.1002/jcb.27063. View

17.

Hou L, Chen L, Fang L . Scutellarin Inhibits Proliferation, Invasion, and Tumorigenicity in Human Breast Cancer Cells by Regulating HIPPO-YAP Signaling Pathway. Med Sci Monit. 2017; 23:5130-5138. PMC: 5673030. DOI: 10.12659/msm.904492. View

18.

Wu J, Chen Y, Liu X, Gao Y, Hu J, Chen H . Discovery of novel negletein derivatives as potent anticancer agents for acute myeloid leukemia. Chem Biol Drug Des. 2017; 91(4):924-932. DOI: 10.1111/cbdd.13159. View

19.

Ke Y, Bao T, Wu X, Tang H, Wang Y, Ge J . Scutellarin suppresses migration and invasion of human hepatocellular carcinoma by inhibiting the STAT3/Girdin/Akt activity. Biochem Biophys Res Commun. 2016; 483(1):509-515. DOI: 10.1016/j.bbrc.2016.12.114. View

20.

Park E, Zhao Y, Lian L, Kim Y, Sohn D . Skullcapflavone I from Scutellaria baicalensis induces apoptosis in activated rat hepatic stellate cells. Planta Med. 2005; 71(9):885-7. DOI: 10.1055/s-2005-871280. View