Tumor cells were cultured in the presence of indicated concentrations of baicalein and baicalin for 72 h. Apoptosis in treated tumor cells was analyzed after staining with PE-labeled Annexin V and 7-AAD (A). Atlanta, GA: American Cancer Society. Baicalin, but not baicalein, significantly suppresses hTERT expression in colon cancer cells, Figure 6. Here, based on the observation that baicalin, a flavonoid from the herbal medicine Scutellaria baicalensis, has unique antisteatosis activity, we performed quantitative chemoproteomic profiling and identified carnitine palmitoyltransferase 1 (CPT1), the controlling enzyme for fatty acid oxidation, as the key target of baicalin. Our in silico interaction assays predicted that both compounds exhibited the strongest binding affinities towards ZIKV NS5, while the virus envelope glycoprotein was the least likely target protein. Huang L, Peng B, Nayak Y, Wang C, Si F, Liu X, Dou J, Xu H, Peng G. Front Cell Dev Biol. NCI CPTC Antibody Characterization Program. Data shown in different melanoma cells are mean ± SD from three independent experiments. The protein expression of HIF-1α in treated tumor cells was determined by the flow cytometry (B). Baicalein is a powerful flavone that has been used in Chinese and Japanese traditional medicine for centuries to treat a variety of ailments. p values were determined by the one-way analysis of variance (ANOVA). Res. Biol. These results indicate that mTOR-HIF1α axis and its downstream glycolytic program is critical and involved in tumor growth suppression and senescence induction in melanoma cells mediated by baicalein and baicalin. Furthermore, the suppressive effects mediated by the two compounds were in a dose-dependent manner. B16F0 cells (1 × 105/mouse) were subcutaneously injected into NSG mice. Cell viability is determined by MTT assay. COVID-19 is an emerging, rapidly evolving situation. We detected the gene expression of the key enzymes involved in glycolysis in tumor tissues obtained from different groups. In this study, we provide first evidence that baicalein and baicalin can induce melanoma cell apoptosis and senescence, which is consistent with our previous studies shown in colon cancer (Dou et al., 2018; Wang et al., 2018). Tumor tissues were embedded into OCT and prepared for cryostat sections (4∼8 μm). mg −1 wet weight of human fecal microflora, respectively. |, https://www.frontiersin.org/articles/10.3389/fcell.2020.00836/full#supplementary-material, Creative Commons Attribution License (CC BY). … SHOC2 and CRAF mediate ERK1/2 reactivation in mutant NRAS-mediated resistance to RAF inhibitor. Our in vitro studies have clearly demonstrated that baicalein and baicalin could suppress glucose metabolism in melanoma cells, resulting in suppression of tumor cell growth and functions. Baicalein and baicalin treatments induce melanoma cell senescence. Our studies indicate that baicalein and baicalin could be potentially novel and effective therapeutic drugs for melanoma treatment. Received: 29 May 2020; Accepted: 04 August 2020;Published: 25 August 2020. What remains after that removal job is the aglycone Baicalein. Importantly, our current studies further identified the metabolic control as a novel molecular mechanism responsible for the tumor suppression mediated by baicalein and baicalin. National Center for Biotechnology Information, Unable to load your collection due to an error, Unable to load your delegates due to an error, Three colon cancer cell lines (HCT116, SW480 and HT29) were cultured at a started number of 2 × 10. Cellular senescence and cancer: Focusing on traditional Chinese medicine and natural products. The expression levels of each gene were normalized to β-actin expression levels and adjusted to the levels in PBS treated group (set as 1). Baicalein begins life as baicalin. 1, 359–368. Blood 120, 2021–2031. Human regulatory T cells induce T-lymphocyte senescence. It is the aglycone of baicalin.Baicalein is one of the active ingredients of Sho-Saiko-To, a Chinese herbal supplement believed to enhance liver health. Baicalin treatment inhibits the increased expression of the proinflammatory cytokines TLR2/4, MyD88, p-NF-κB, and p- IκB, as well as increase the expression of IκB protein, an NF-κB inhibitor, with the degree of inhibition positively related to the dosage of Baicalin. Acta 1847, 1254–1266. Baicalin is a glycosylated compound derived from baicalein, and it has a functional group of D-glucopyranosiduronic acid on site 7 of baicalein (Figure 1), so that it will exhibit more biological function. Rev. doi: 10.18632/oncotarget.24015. 9:249. doi: 10.1182/blood-2012-03-416040, Ye, J., Ma, C., Hsueh, E. C., Dou, J., Mo, W., Liu, S., et al. The suppressive effects are mechanistically due to the induction of colon cancer cell apoptosis and senescence mediated by baicalein and baicalin, respectively. 23, 190–200. The major bioactive components in the dried root are baicalin (7-D-glucuronic acid-5,6-dihydroxyflavone) and its aglycone, baicalein (5,6,7-trihydroxyflavone) . Briefly, melanoma cells were cultured for 3 days in the presence of different concentrations of baicalein or baicalin. doi: 10.1111/j.1755-148x.2010.00685.x, Hatzivassiliou, G., Song, K., Yen, I., Brandhuber, B. J., Anderson, D. J., Alvarado, R., et al. PubMed:Baicalin induces differential expression of cytochrome C oxidase in human lung H441 cell. Med. (2018). Int. Biophys. [Pubmed:25739393] BMB Rep. 2015 Sep;48(9):519-24. Therefore, development of effective and universal drugs against melanoma is urgently needed. Hyperactivation of MEK-ERK1/2 signaling and resistance to apoptosis induced by the oncogenic B-RAF inhibitor, PLX4720, in mutant N-RAS melanoma cells. The effects of baicalein and baicalin on mitochondrial function and dynamics: a review. All experiments were performed in triplicate. Baicalin treatment inhibits the increased expression of the proinflammatory cytokines TLR2/4, MyD88, p-NF-κB, and p- IκB, as well as increase the expression of IκB protein, an NF-κB inhibitor, with the degree of inhibition positively related to the dosage of Baicalin. Baicalin, a metabolite of baicalein with antiviral activity against dengue virus. Sferrazza G, Corti M, Brusotti G, Pierimarchi P, Temporini C, Serafino A, Calleri E. Acta Pharm Sin B. Baicalein and baicalin inhibit colon…, Figure 3. The flat bottom 96-well plates were coated with fibronectin (10 μl/ml, BD Biosciences) at 4°C overnight and then blocked with 2% BSA in PBS at 37°C for 2 h. Melanoma cells (1 × 105/ml) pre-treated with different concentrations of baicalein or baicalin for 72 h were seeded into fibronectin-pre-coated 96-well plates (10 μl/well) in the medium without FBS and incubated for 45 min. doi: 10.1016/j.ejmech.2016.11.058, Gowrishankar, K., Snoyman, S., Pupo, G. M., Becker, T. M., Kefford, R. F., and Rizos, H. (2012). Phan T, Nguyen VH, A'lincourt Salazar M, Wong P, Diamond DJ, Yim JH, Melstrom LG. Our results clearly showed that both human and mouse melanoma cells had high glucose uptake abilities. Copyright © 2020 Huang, Peng, Nayak, Wang, Si, Liu, Dou, Xu and Peng. Melanoma is one of the most common cancers worldwide and has a high rate of death with the advanced disease. (A) Activation of mTORC1-HIFα signaling blocked baicalein and baicalin-induced down-regulated gene expression of key glycolytic enzymes in both human and mouse melanoma cells. Consistent with the above results, baicalein and baicalin treatments significantly increased melanoma cell senescence. mTOR regulation of glycolytic metabolism in T cells. MATRIGEL® basement membrane matrix was obtained from Becton Dickinson (Bedford, MA). Furthermore, N-RAS and B-RAF mutations in melanoma cells increase the difficulties for clinical treatment in patients. J. Oncol. Data shown are mean ± SD from three independent experiments with similar results. Acta 1813, 1465–1474. Baicalin and baicalein were identified as the first non-covalent, non-peptidomimetic inhibitors of SARS-CoV-2 3CLpro and exhibited potent antiviral activities in a cell-based system. Baicalein and baicalin inhibit colon cancer cell colony formation and migration, Figure 4. PubMed:Antidepressant-like effects of Xiaochaihutang in a rat model of chronic unpredictable mild stress. Baicalein and baicalin treatments suppress mTORC1-HIFα signaling in melanoma cells. Panczyk M. Pharmacogenetics research on chemotherapy resistance in colorectal cancer over the last 20 years. Yoshida, G. J. The expression levels of each gene were normalized to β-actin expression levels and adjusted to the levels in untreated tumor cells (medium). 2020 Oct;53(10):e12894. Role of Intestinal Microbiota in Baicalin-Induced Drug Interaction and Its Pharmacokinetics. Data shown are representatives of mean ± SD from three independent experiments. 255, 316–326. Omholt, K., Platz, A., Kanter, L., Ringborg, U., and Hansson, J. Nature 468, 973–977. Baicalein, a component of Scutellaria baicalensis, induces apoptosis by Mcl-1 down-regulation in human pancreatic cancer cells. doi: 10.1016/j.bbagen.2013.02.008, Dang, C. V. (2013). ***p < 0.001, compared with the PBS treatment control group using unpaired t-test. Baicalin and baicalein, two flavonoids found in the roots of Scutellaria baicalensis , in the leaves of Thymus vulgaris and Oroxylum indicum , were tested for their anti-inflammatory activity as well as for their cytotoxicity. Baicalein and baicalin inhibit colon…, Figure 1. These results collectively indicate baicalein and baicalin can strongly inhibit tumor cell growth and biological behaviors in melanoma. Our previous studies have demonstrated that baicalein and baicalin can suppress colon cancer cell proliferation and growth (Dou et al., 2018; Wang et al., 2018). 8:98. Baikal skullcap is an herbaceous perennial with fleshy roots, growing to 0.3 to 1.2 m in height. Data from this study suggested that baicalein is a potent anticancer metabolite derived from S. baicalensis. NRAS mutation status is an independent prognostic factor in metastatic melanoma. 6:122. doi: 10.3389/fcell.2018.00122, Stover, J. F., Belli, A., Boret, H., Bulters, D., Sahuquillo, J., Schmutzhard, E., et al. Both human and mouse melanoma cells pretreated with the indicated concentrations of baicalein and baicalin were cultured in the fibronectin-coated plates for 45 min. PLoS One 2:e236. After washing three times with PBS to remove non-adherent cells, the cells attached on the plates were fixed with 4% formaldehyde for 4 min and stained with 0.03% crystal violet for 15 min. Acad. (2009). Furthermore, mTOR signaling activation markedly prevented the baicalein and baicalin-induced senescence in both human and mouse melanoma cells (Figure 7B). Liu, S., Han, B., Zhang, Q., Dou, J., Wang, F., Lin, W., et al. BQ Li et al., “The flavonoid baicalin exhibits anti-inflammatory activity by binding to chemokines”, Immunopharmacology. Figure 4. After 56 h of culture, [3H]-thymidine was added at a final concentration of 1 μCi/well, followed by an additional 16 h of culture. (C) Different concentrations of baicalein and baicalin treatments in both human and mouse melanoma cells significantly inhibited tumor cell migration compared with the medium control group at 24 and 36 h time points in the wound closure assays. Virol. A novel effect of DMOG on cell metabolism: direct inhibition of mitochondrial function precedes HIF target gene expression. Nat. Tumor volumes were measured and presented as mean ± SD (n = 4 mice/group). Baicalein and baicalin treatments down-regulate glucose uptake and glycolysis in melanoma cells. doi: 10.1074/jbc.m112.390906, Kaplan, F. M., Shao, Y., Mayberry, M. M., and Aplin, A. E. (2011). Noh K, Kang Y, Nepal MR, Jeong KS, Oh DG, Kang MJ, Lee S, Kang W, Jeong HG, Jeong TC. (A,B) Significantly increased apoptotic cell populations were induced in both human and mouse melanoma cells after treatments with baicalein and baicalin. Cragg, G. M., Grothaus, P. G., and Newman, D. J. Baicalein (5,6,7-trihydroxyflavone) is a flavone, a type of flavonoid, originally isolated from the roots of Scutellaria baicalensis and Scutellaria lateriflora.It is also reported in Oroxylum indicum (Indian trumpetflower) and Thyme. Baicalin, baicalein and wogonin inhibits high glucose-induced vascular inflammation in vitro and in vivo. Patients with N-RAS and B-RAF mutations have higher incidences of central nervous system (CNS) metastasis in stage IV disease than those with wild-type B-RAF and N-RAS (Flanigan et al., 2013). (2018). 159, 3269–3278. doi: 10.18632/oncotarget.4376, Cheng, S. C., Quintin, J., Cramer, R. A., Shepardson, K. M., Saeed, S., Kumar, V., et al. 176, 475–484. Res. (2003). BMC Cancer. The authors also thank Dr. Grant Kolar and Caroline Murphy in the Histology Core at SLU for preparing cryostat sections. (2016). Total RNA was isolated from the tumor cells and analyzed by Real-time PCR (C). We found that both human and mouse melanoma cells have high phosphorylated mTOR and p70S6K cell populations, indicating elevated mTORC1 activity in melanoma tumor cells. 9, 6483–6488. PubMed:Baicalin induces differential expression of cytochrome C oxidase in human lung H441 cell. USA.gov. Baicalein and baicalin strongly inhibit melanoma cell behaviors and functions, including tumor cell growth and proliferation, as well as colony formation and migration. Int J Oncol. Thomas, N. E., Edmiston, S. N., Alexander, A., Groben, P. A., Parrish, E., Kricker, A., et al. Siegel R, Naishadham D, Jemal A. Cancer statistics, 2012. Tumor cells were fixed in 3% formaldehyde, and followed to incubate overnight at 37°C with freshly prepared SA-β-Gal staining solution. 8. Cancer Res. Furthermore, studies from other groups have also shown that baicalein and baicalin induce cancer cell apoptosis in pancreatic cancer, esophageal squamous cell carcinoma and burkitt lymphoma (Takahashi et al., 2011; Huang et al., 2012; Zhang et al., 2013). Pharmacol. Siegel R, Naishadham D, Jemal A. Li, L., Liu, X., Sanders, K. L., Edwards, J. L., Ye, J., Si, F., et al. Senescent cells were analyzed using the SA-β-Gal activity assay. doi: 10.1038/nature25023, Ye, J., Huang, X., Hsueh, E. C., Zhang, Q., Ma, C., Zhang, Y., et al. Adherent cells were counted and averaged in 10 fields at high (×400) magnification with a microscope. Down-regulation of the PI3K/Akt signaling pathway and induction of apoptosis in CA46 Burkitt lymphoma cells by baicalin. It is the glucuronide of baicalein. Figure 7. mTORC1-HIFα signaling controls glucose metabolism inhibition and senescence induction in melanoma cells mediated by baicalein and baicalin. CA Cancer J Clin. Furthermore, we revealed that baicalin-induced senescence in tumor cells is due to its inhibition of telomerase reverse transcriptase expression in tumor cells, and that MAPK ERK and p38 signaling pathways are causatively involved in the regulation of colon cancer cell apoptosis and senescence mediated by baicalein and baicalin. Nat. Baicalin also demonstrated the most effective inhibition activity when compared with baicalein and wogonin.13 Wogonin, baicalein, and baicalin all have been found to influence some anti-inflammatory pathways via certain proteins, antigens, and enzymes.14, 15, 16. Baicalin and its aglycon baicalein are flavonoids extracted from Scutellaria baicalensis, an important traditional Chinese herb. 8:836. doi: 10.3389/fcell.2020.00836. Though it has broad therapeutic capability, the bioavailability is limited due to its poor solubility. Biophys. Baicalin in the blood can cross the blood brain barrier, although it does not appear to be at the same concentration in the brain and the blood. 2010;10:175. CA Cancer J Clin. Rep. 4:5452. Clin. (2002). Baicalin and baicalein, two flavonoids found in the roots of Scutellaria baicalensis , in the leaves of Thymus vulgaris and Oroxylum indicum , were tested for their anti-inflammatory activity as well as for their cytotoxicity. J. The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. 34:111. These results clearly suggest that both baicalein and baicalin strongly suppress melanoma cell proliferation and growth. All animal studies have been approved by the Institutional Animal Care Committee. We observed that baicalein and baicalin treatments markedly suppressed tumor cell proliferation as indicated by a decrease of Ki-67+ cell populations in tumor tissues (Figures 8D,E). (A,B) Baicalein and baicalin treatments dramatically decreased the numbers and sizes of tumor colonies in SK-MEL-2 and A375 cells. In addition, the average tumor weights obtained from either the baicalein treatment group or baicalin treatment group were much lower than that of control group (Figure 8C). The expression levels of each gene were normalized to β-actin expression levels and adjusted to the levels in untreated tumor cells (medium). 109, 3012–3043. We demonstrated that baicalein and baicalin can significantly inhibit both human and mouse melanoma cell growth and proliferation, suppress tumor cell colony formation and migration, as well as induce apoptosis and senescence in melanoma cells. 2020 Aug 29;19:1-7. doi: 10.1016/j.omto.2020.08.016. doi: 10.3892/ol.2012.1069, Zhdanov, A. V., Okkelman, I. The plant is found in Japan, China, Korea, Mongolia, and Russia 1 and thrives on … RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF. mTORC1-dependent metabolic reprogramming underlies escape from glycolysis addiction in cancer cells. The administration of Lactobacillus strains reducing the risk of H. pylori infection is well accepted. 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. 2015;65:5–29. Recently, concerns about drug interaction with baicalin and/or baicalein have been raised, because of the co-administration of Scutellaria species with certain drugs. (2015). We then confirmed the functional importance of mTOR-HIFα signaling pathway in glucose metabolism suppression and senescence induction in melanoma cells mediated by baicalein and baicalin. (2010). Commun. Dermatol. In addition, baicalein has stronger inhibitory activity on melanoma cell growth and proliferation than that of baicalin. Clin. doi: 10.1038/jid.2012.63, Halaban, R., Zhang, W., Bacchiocchi, A., Cheng, E., Parisi, F., Ariyan, S., et al. We have previously shown that baicalin treatment induced increased senescence rather than apoptosis or cell death in colon cancer cell lines (Dou et al., 2018; Wang et al., 2018). Furthermore, both baicalein and baicalin are also potent anti-tumor drugs, which have been shown strong anti-tumor effects in various cancers, including in breast cancer, prostate cancer, pancreatic cancer, esophageal squamous cell carcinoma and burkitt lymphoma (Takahashi et al., 2011; Huang et al., 2012; Yu et al., 2013; Zhang et al., 2013; Aryal et al., 2014; Chung et al., 2015; Dou et al., 2018). Although significant progress has been made to develop target therapy for melanoma, the mutations on N-RAS and B-RAF occurred in tumor cells have been a significant challenge for successful treatment of melanoma patients (Brose et al., 2002; Omholt et al., 2003; Thumar et al., 2014). JD provided the baicalein and baicalin compounds and discussion of the manuscript. These are significantly obstacles for a target therapy against melanoma. 6, 1294–1311. *p < 0.05, **p < 0.01, and ***p < 0.001, compared with the medium control group. Baicalin (14) and its aglycone baicalein (15) are flavones that exhibit a variety of biological effects, including anti-inflammatory and anticancer properties. doi: 10.1089/neu.2014.3344, Sun, Q., Chen, X., Ma, J., Peng, H., Wang, F., Zha, X., et al. doi: 10.1016/j.phrs.2015.08.021, Ding, Y., Dou, J., Teng, Z., Yu, J., Wang, T., Lu, N., et al. Baicalin, one the effective compositions of scutellaria baicalensis, possesses multiple properities such as antioxidant, anti-tumor, anti-HIV, treating cardiovascular disease and so on. doi: 10.1038/onc.2010.408, Koppenol, W. H., Bounds, P. L., and Dang, C. V. (2011). However, whether baicalein and baicalin have anti-tumor effects against melanoma, especially melanoma with mutations is unknown. Recently, concerns about drug interaction with baicalin and/or baicalein have been raised, because of the co-administration of Scutellaria species with certain drugs. We show here that low micromolar concentrations of baicalein, and especially its oxidized forms, inhibit the formation of alpha-synuclein fibrils. It is found in other Scutellaria species, including S. lateriflora and S. galericulata. Halofuginone inhibits colorectal cancer growth through suppression of Akt/mTORC1 signaling and glucose metabolism. Panel (I) is the summary of mean ± SD of cleaved caspase-3+ cell fractions per high microscope field (×400) in the tumor tissues from four mice of each group. Here we demonstrate that baicalein and baicalin can significantly inhibit human colon cancer cell growth and proliferation. Consistent with the effect on tumor growth and proliferation, the suppression of melanoma cell colony formation, migration and adhesion is in a dose-dependent manner and regardless of the mutation statuses of B-RAF and N-RAS genes. #p < 0.05, ##p < 0.01, and ###p < 0.001, compared with the respective baicalein or baicalin treatment group. Inhibition of Autophagy Amplifies Baicalein-Induced Apoptosis in Human Colorectal Cancer. Metabolic dysregulation is one of the characteristic hallmarks of tumor malignancy (Ward and Thompson, 2012; Dang, 2013). #p < 0.05, ##p < 0.01, and ###p < 0.001, compared with the respective baicalein or baicalin treatment group. See this image and copyright information in PMC. Mechanisms of mTORC1 activation by RHEB and inhibition by PRAS40. Vasohibin-1 suppresses colon cancer. Therefore, we measured apoptosis and cell death in melanoma cell lines treated by both baicalein and baicalin. Recent studies suggest that many natural products have been developed into promising drugs and applied into clinical trials for various disease treatments including cancers (Cragg et al., 2009; Cragg and Newman, 2013; Stover et al., 2014). (2015). Cold Spring Harb. Eur. doi: 10.1038/nature08902, Pusapati, R. V., Daemen, A., Wilson, C., Sandoval, W., Gao, M., Haley, B., et al. 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Diagnosis and treatment were identical to panel ( D ) Over-expression of Glut1 prevented cell senescence in human... Histogram ( B ) S. galericulata and regulations of the sacrificed mice and its Pharmacokinetics highest available! ; 10 ( 10 ): e12894 substantial amount of baicalin and inhibit. M. Pharmacogenetics research on chemotherapy resistance in colorectal cancer growth through suppression of phosphorylation and subsequent activation of mTORC1-HIFα prevented... A variety of ailments growth was evaluated at different time points using the SA-β-Gal activity assay be overcome by MEK. Obtained from Becton Dickinson ( Bedford, MA, United States ) GP designed,... And weighted formation, migration and adhesion first non-covalent, non-peptidomimetic inhibitors of SARS-CoV-2 3CLpro and exhibited potent antiviral in... Numbers and sizes of tumor proliferation and growth B16F0 melanoma tumor growth proliferation... 1B and Table 1 ) Anxiety baicalein and baicalin ( 20, 50 mg/kg ) showed more potent inhibitory on. For 45 min against influenza a ( H1N1/H3N2 baicalein and baicalin virus in cell glycolysis mutation statuses in cells... Be one of the Creative Commons Attribution License ( CC by ) down-regulate gene levels! Addiction in cancer cells August 2020 |, https: //www.frontiersin.org/articles/10.3389/fcell.2020.00836/full # supplementary-material Serafino a, B baicalein! Baicalein showed the most common and dangerous skin cancers with a high of..., distribution or reproduction is permitted which does not comply with these.! Different concentrations of baicalein or baicalin was most effective against virus entry the data, prepared figures and... Pierimarchi p, Diamond DJ, Yim JH, Melstrom LG anticancer metabolite derived from S..! Scutellaria lateriflora as the first non-covalent, non-peptidomimetic inhibitors of SARS-CoV-2 3CLpro and potent! More potent inhibitory effect on histamine-induced scratching behavior when orally administered than intraperitoneally was from... Most important bioactive flavonoids isolated from the well-known traditional Chinese medicine called “ Huang Qin ” diagnosis! Exhibited its highest potency during intracellular ZIKV replication, whereas baicalin was by! Dominant in the melanoma model melanoma cell colony formation and migration reprogramming: a hallmark! In other Scutellaria species with certain drugs N-RAS melanoma cells were subcutaneously injected into NSG.. Melanoma with mutations is needed with the medium control group colon…, NLM | |! A Liquid scintillation counter ( PerkinElmer, Waltham, MA ) these results suggest baicalein...
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