We found that culture with medium, melanoma cells contained around 2–10% apoptotic cells (around 10% in Mel586 and SK-MEL-2, and below 5% in A375 and B16F0 tumor cells). However, unlike the effect in colon cancer cells, treatment with baicalein induced more senescent cell populations in both human and mouse melanoma cell lines than that of baicalin treatment in those melanoma cells (Figures 4A,B). doi: 10.1016/j.ccr.2010.11.023, Wang, C. Z., Zhang, C. F., Chen, L., Anderson, S., Lu, F., and Yuan, C. S. (2015). Health Benefits of Baicalein These studies clearly indicate that baicalein and baicalin could be potential novel and universal drugs for melanoma therapy. Baicalein and baicalin treatments suppress mTORC1-HIFα signaling in melanoma cells. (2012). Immunity 43, 435–449. After 4 days post tumor injection (tumor size reached around 5 × 5 mm), the tumor-bearing mice were administrated with baicalein (80 mg/kg), baicalin (80 mg/kg), or PBS control through intraperitoneal injection, respectively at every other day for 2 weeks. Tumor volume was calculated on the basis of two-dimensional measurements. Front. We observed that the numbers and sizes of tumor cell colonies were significantly decreased in SK-MEL-2 and A375 tumor cells after treatment with baicalein or baicalin (Figures 2A,B). Metabolic reprogramming: the emerging concept and associated therapeutic strategies. Baicalein and baicalin inhibit colon cancer cell growth and proliferation, Figure 2. Epub 2020 Sep 3. 2020 Oct;10(10):1814-1834. doi: 10.1016/j.apsb.2019.12.019. 363, 809–819. Antiviral activity of baicalin against influenza A (H1N1/H3N2) virus in cell culture and in mice and its inhibition of neuraminidase. J. Neurotrauma 31, 1599–1606. After 4 days post tumor injection (tumor size reached around 5 × 5 mm), the tumor-bearing mice were administrated with baicalein (80 mg/kg), baicalin (80 mg/kg), or PBS control through intraperitoneal injection, respectively at every other day for 2 weeks. Phan T, Nguyen VH, A'lincourt Salazar M, Wong P, Diamond DJ, Yim JH, Melstrom LG. Science 345:1250684. doi: 10.1126/science.1250684, Chiu, Y. W., Lin, T. H., Huang, W. S., Teng, C. Y., Liou, Y. S., Kuo, W. H., et al. A substantial amount of baicalin (34–63%) was methylated to oroxylin A and its conjugates in various organs during absorption. Blood 120, 2021–2031. Mol. 5, 722–728. Cancer Res. Med. MEK targeting in N-RAS mutated metastatic melanoma. (B) Representative image of B16F0 tumors obtained from the indicated groups at the endpoint of the experiments (day 17). The anti-tumor effects mediated by baicalein and baicalin are independent of N-RAS and B-RAF mutation statuses in melanoma cells. In our effort to identify how baicalein and baicalin molecularly inhibit melanoma growth, we demonstrated that baicalein and baicalin can metabolically reprogram melanoma cells via inhibition of glucose uptake and downregulation of the key enzymes in glucose transport and glycolysis in tumor cells. 255, 316–326. **p < 0.01 compared with the medium control group. It is converted from baicalin by an enzymatic reaction, which removes a large part of the chemical structure. Baicalein is a flavone, a type of polyphenolic flavonoid, that is extracted from the roots of Scutellaria baicalensis and Scutellaria lateriflorathat have a wide variety of health benefits. The incorporation of [3H]-thymidine was measured with a liquid scintillation counter (PerkinElmer, Waltham, MA, United States). Pharmacol. B16F0 cells (1 × 105/mouse) were subcutaneously injected into NSG mice. Scutellaria ba … Baicalin, along with its aglycone baicalein, is a positive allosteric modulator of the benzodiazepine site and/or a non-benzodiazepine site of the GABA A receptor. Virol. Baicalein (Purity 98.5%) and baicalin (Purity 91.5%) were purchased from the Kanghua Company (Nanjing, Jiangsu, China) and were dissolved in dimethyl sulfoxide (DMSO, Sigma, St. Louis, Mo, United States). 132, 1850–1859. doi: 10.1073/pnas.1014769108. (B,C) Baicalein and baicalin treatments down-regulated HIF1α protein and mRNA expression in melanoma cells. Baicalin and its aglycon baicalein are flavonoids extracted from Scutellaria baicalensis, an important traditional Chinese herb. Furthermore, the “Warburg effect” has been widely accepted as a common feature of metabolic reprogramming in tumors, and tumor cells depend on aerobic glycolysis for maintaining biosynthesis and functions (Warburg, 1956; Koppenol et al., 2011). 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