Scutellaria Baicalensis Georgi Research Articles

A Review on Radix Scutellariae: A Traditional Chinese Medicine with Great Medicinal Significant

Abstract Radix Scutellariae (RS) refers to the root of Scutellaria baicalensis Georgi (SBG) plant. This plant belongs to family Lamiaceae. There are many common names of RS such as huang chin, huang lien, huang qin, huangqin, and wogon. SBG plant is spreading throughout many Asian countries such as China, Japan, North and South Korea, Mongolia and Russia. The aim of this review is to focus on the ingredients, medicinal uses, pharmacological activity, toxicology, adverse effects, precautions, and dosage of RS. RS contains baicalein, baicalin, wogonin, wogonoside, and oroxylin A ingredients. RS is used in the treatment of fever, nausea and vomiting, acute dysentery, jaundice, coughs, carbuncles and sores, and threatened abortion. RS is applied in the treatment of allergies, arteriosclerosis, diarrhea, dermatitis, and hypertension. Pharmacology activity of RS includes experimental pharmacology and clinical pharmacology. Experimental pharmacology contains hepatoprotective, anti-inflammatory, antioxidant, antimicrobial, anti-tumor, antiviral, central nervous system, enzyme inhibition, immunological, platelet aggregation inhibition, and smooth muscle activities. Injection of water extract of RS (12–15 g/kg, intragastrically) to dogs without any toxic effects and the oral intake of 4–5 g/kg of this extract to dogs three times/day for 8 weeks did not induce any toxic effects. There are no carcinogenesis, mutagenesis, and impairment of fertility, pregnancy, teratogenic effects or any other effects of RS. RS possesses many pharmacological activities and it is used to treat many diseases and without any toxic effect to any organs.

Integration of metabolomics and network pharmacology to reveal the protective mechanism underlying Wogonoside in acute myocardial ischemia rats

Ethnopharmacological relevanceIn traditional medicine, both Scutellaria baicalensis Georgi (SBG) and the traditional formulas composed of it have been used to treat a wide range of diseases, including cancer and cardiovascular. Wogonoside (Wog) is the biologically active flavonoid compound extracted from the root of SBG, with potential cardiovascular protective effects. However, the mechanisms underlying the protective effect of Wog on acute myocardial ischemia (AMI) have not yet been clearly elucidated. Aim of the studyTo explore the protective mechanism of Wog on AMI rats by comprehensively integrating traditional pharmacodynamics, metabolomics, and network pharmacology. MethodsThe rat was pretreatment with Wog at a dose of 20 mg/kg/d and 40 mg/kg/d once daily for 10 days and then ligated the left anterior descending coronary artery of rats to establish the AMI rat model. Electrocardiogram (ECG), cardiac enzyme levels, heart weight index (HWI), Triphenyltetrazolium chloride (TTC) staining, and histopathological analyses were adopted to evaluate the protective effect of Wog on AMI rats. Moreover, a serum metabolomic-based UHPLC-Q-Orbitrap MS approach was performed to find metabolic biomarkers and metabolic pathways, and network pharmacology analysis was applied to predict targets and pathways of Wog in treating AMI. Then, the network pharmacology and metabolomic results were integrated to elucidate the mechanism of Wog in treating AMI. Finally, RT- PCR was used to detect the mRNA expression levels of PTGS1, PTGS2, ALOX5, and ALOX15 to validate the result of integrated metabolomics and network analysis. ResultsPharmacodynamic studies suggest that Wog could effectively prevent the ST-segment of electrocardiogram elevation, reduce the myocardial infarct size, heart weight index, and cardiac enzyme levels, and alleviate cardiac histological damage in AMI rats. Metabolomics analysis showed that the disturbances of metabolic profile in AMI rats were partly corrected by Wog and the cardio-protection effects on AMI rats involved 32 differential metabolic biomarkers and 4 metabolic pathways. In addition, the integrated analysis of network pharmacology and metabolomics showed that 7 metabolic biomarkers, 6 targets, and 6 crucial pathways were the main mechanism for the therapeutic application of Wog for AMI. Moreover, the results of RT-PCR showed that PTGS1, PTGS2, ALOX5, and ALOX15 mRNA expression levels were reduced after treatment with Wog. ConclusionWog exerts cardio-protection effects on AMI rats via the regulation of multiple metabolic biomarkers, multiple targets, and multiple pathways, our current study will provide strong scientific evidence supporting the therapeutic application of Wog for AMI.

The ethanol extract of Scutellaria baicalensis Georgi attenuates complete Freund's adjuvant (CFA)-induced inflammatory pain by suppression of P2X3 receptor

Ethnopharmacological relevanceScutellaria baicalensis Georgi (SBG) is a perennial herb with anti-inflammatory, antibacterial, and antioxidant activities, which is traditionally used to treat inflammation of respiratory tract and gastrointestinal tract, abdominal cramps, bacterial and viral infections. Clinically, it is often used to treat inflammatory-related diseases. Research has shown that the ethanol extract of Scutellaria baicalensis Georgi (SGE) has anti-inflammatory effect, and its main components baicalin and baicalein have analgesic effects. However, the mechanism of SGE in relieving inflammatory pain has not been deeply studied. Aim of the studyThis study aimed to evaluate the analgesic effect of SGE on complete Freund's adjuvant (CFA)-induced inflammatory pain rats, and to investigate whether its effect on relieving inflammatory pain is associated with regulation of P2X3 receptor. Materials and methodsThe analgesic effects of SGE on CFA-induced inflammatory pain rats were evaluated by measuring mechanical pain threshold, thermal pain threshold, and motor coordination ability. The mechanisms of SGE in relieving inflammatory pain were explored by detecting inflammatory factors levels, NF-κB, COX-2 and P2X3 expression, and were further verified by addition of P2X3 receptor agonist (α, β me-ATP). ResultsOur results revealed that SGE can notably increase the mechanical pain threshold and thermal pain threshold of CFA-induced inflammatory pain rats, and markedly alleviate the pathological damage in DRG. SGE could suppress the release of inflammatory factors including IL-1β, IL-6, TNF-α and restrain the expression of NF-κB, COX-2 and P2X3. Moreover, α, β me-ATP further exacerbated the inflammatory pain of CFA-induced rats, while SGE could markedly raise the pain thresholds and relieve inflammatory pain. SGE could attenuate the pathological damage, inhibit P2X3 expression, inhibit the elevation of inflammatory factors caused by α, β me-ATP. SGE can also inhibit NF-κB and ERK1/2 activation caused by α, β me-ATP, and inhibit the mRNA expression of P2X3, COX-2, NF-κB, IL-1β, IL-6 and TNF-α in DRG of rats induced by CFA coupled with α, β me-ATP. ConclusionsIn summary, our research indicated that SGE could alleviate CFA-induced inflammatory pain by suppression of P2X3 receptor.

The Pharmacological Efficacy of Baicalin in Inflammatory Diseases.

Baicalin is one of the most abundant flavonoids found in the dried roots of Scutellaria baicalensis Georgi (SBG) belonging to the genus Scutellaria. While baicalin is demonstrated to have anti-inflammatory, antiviral, antitumor, antibacterial, anticonvulsant, antioxidant, hepatoprotective, and neuroprotective effects, its low hydrophilicity and lipophilicity limit the bioavailability and pharmacological functions. Therefore, an in-depth study of baicalin's bioavailability and pharmacokinetics contributes to laying the theoretical foundation for applied research in disease treatment. In this view, the physicochemical properties and anti-inflammatory activity of baicalin are summarized in terms of bioavailability, drug interaction, and inflammatory conditions.

Analysis of quality differences between Scutellaria baicalensis Georgi and Scutellaria rehderiana Diels based on phytochemistry and bioactivity evaluation

Scutellaria baicalensis Georgi (SG) and Scutellaria rehderiana Diels (SD) belong to the same genus of Scutellaria in the Labiatae (Lamiaceae) family. SG is confirmed as the medicinal source according to the Chinese Pharmacopeia, but SD is often used as a substitute for SG due to its abundant plant resources. However, the current quality standards are far from sufficient to judge the quality differences between SG and SD. In this study, an integrated strategy of “biosynthetic pathway (specificity) - plant metabolomics (difference) - bioactivity evaluation (effectiveness)” was established to evaluate this quality differences. First, an ultrahigh-performance liquid chromatography-quadrupole time-of-flight mass spectrometry (UHPLC-Q/TOF-MS/MS) method was developed for the identification of chemical components. The abundant components information was obtained and the characteristic constituents were screened according to the location in the biosynthetic pathway as well as species specificity. Then, plant metabolomics combined with multivariate statistical analysis to find differential components between SG and SD. The chemical markers for quality analysis were determined based on the differential and characteristic components, and the content of each marker was tentatively evaluated through the semi-quantitative analysis of UHPLC-Q/TOF-MS/MS. Finally, the anti-inflammatory activity of SG and SD was compared by measuring the inhibitory effect on the release of NO from lipopolysaccharide (LPS)-stimulated RAW 264.7 cells. Under this analytical strategy, a total of 113 compounds were tentatively identified in both SG and SD, among which baicalein, wogonin, chrysin, oroxylin A 7-O-β-D-glucuronoside, pinocembrin and baicalin were selected as chemical markers due to their species characteristics and differentiation. The contents of oroxylin A 7-O-β-D-glucuronoside and baicalin was higher in SG, and the others were higher in SD. In addition, both SG and SD exhibited prominent anti-inflammatory activity, but SD was less effective. The analysis strategy combining phytochemistry and bioactivity evaluation realized the scientific evaluation of the intrinsic quality differences between SG and SD, which provides a reference for fully utilizing and expanding the medicinal resources, and also provides a reference for the comprehensive quality control of herbal medicines.

Integrated analysis of topoisomerase I inhibitors from flavonoids of Scutellaria baicalensis Georgi using bioaffinity ultrafiltration UPLC-TripleTOF MS/MS, molecular docking and target-based multiple complex networks

Scutellaria baicalensis Georgi (SBG) has been widely used as medical plant in East Asia with remarkable anti-cancer activity. However, the underlying mechanisms are still confused. In this study, an integrated analysis was conducted to screen topoisomerase I (topo I) inhibitors from flavonoids of SBG and investigate the anti-cancer mechanisms, containing bioaffinity ultrafiltration UPLC-ESI-TripleTOF-MS/MS, molecular docking, and multiple complex networks. The SBG extract exhibited notable cytotoxic activity on Hela cells. Five flavonoids were identified as potential topo I inhibitors, including skullcapflavone II, wogonin, chrysin, oroxylin A, and tenaxin I. Their ESI-MS/MS spectra showed that RDA reaction and neutral molecule loss were the main fragment patterns. Docking results demonstrated that π–π interaction and the formation of hydrogen bond contributed most to their binding with topo I. The selected compounds, related target proteins and pathways were integrated into target-based multiple complex networks, which consisted of three subnetworks. Statistical and topological analysis of these networks revealed a series of characteristics, including scale-free property with power-law degree distribution, Poisson degree distribution, and small-world property. Chrysin, wogonin, and oroxylin A exhibited as main active components with much higher degree values. Chemical carcinogenesis-receptor activation (hsa05207) was considered as critical pathway due to remarkable centrality indexes. Additionally, potential synergistic effect of wogonin and chrysin was observed on the conversion of supercoiled DNA to relaxed forms. These results improved current understanding of flavonoid-rich plants on the treatment of cancer. Moreover, the multi-disciplinary approach provided a new strategy for the research of natural products from medical plants.

The protective effects of baicalin for respiratory diseases: an update and future perspectives.

Background: Respiratory diseases are common and frequent diseases. Due to the high pathogenicity and side effects of respiratory diseases, the discovery of new strategies for drug treatment is a hot area of research. Scutellaria baicalensis Georgi (SBG) has been used as a medicinal herb in China for over 2000years. Baicalin (BA) is a flavonoid active ingredient extracted from SBG that BA has been found to exert various pharmacological effects against respiratory diseases. However, there is no comprehensive review of the mechanism of the effects of BA in treating respiratory diseases. This review aims to summarize the current pharmacokinetics of BA, baicalin-loaded nano-delivery system, and its molecular mechanisms and therapeutical effects for treating respiratory diseases. Method: This review reviewed databases such as PubMed, NCBI, and Web of Science from their inception to 13 December 2022, in which literature was related to "baicalin", "Scutellaria baicalensis Georgi", "COVID-19", "acute lung injury", "pulmonary arterial hypertension", "asthma", "chronic obstructive pulmonary disease", "pulmonary fibrosis", "lung cancer", "pharmacokinetics", "liposomes", "nano-emulsions", "micelles", "phospholipid complexes", "solid dispersions", "inclusion complexes", and other terms. Result: The pharmacokinetics of BA involves mainly gastrointestinal hydrolysis, the enteroglycoside cycle, multiple metabolic pathways, and excretion in bile and urine. Due to the poor bioavailability and solubility of BA, liposomes, nano-emulsions, micelles, phospholipid complexes, solid dispersions, and inclusion complexes of BA have been developed to improve its bioavailability, lung targeting, and solubility. BA exerts potent effects mainly by mediating upstream oxidative stress, inflammation, apoptosis, and immune response pathways. It regulates are the NF-κB, PI3K/AKT, TGF-β/Smad, Nrf2/HO-1, and ERK/GSK3β pathways. Conclusion: This review presents comprehensive information on BA about pharmacokinetics, baicalin-loaded nano-delivery system, and its therapeutic effects and potential pharmacological mechanisms in respiratory diseases. The available studies suggest that BA has excellent possible treatment of respiratory diseases and is worthy of further investigation and development.

Therapeutic Potential of Bioactive Components from Scutellaria baicalensis Georgi in Inflammatory Bowel Disease and Colorectal Cancer: A Review.

Scutellaria baicalensis Georgi (SBG), an herbal medicine with various biological activities, including anti-inflammatory, anticancer, antiviral, antibacterial, and antioxidant activities, is effective in treatment of colitis, hepatitis, pneumonia, respiratory infections, and allergic diseases. This herbal medicine consists of major active substances, such as baicalin, baicalein, wogonoside, and wogonin. Inflammatory bowel disease (IBD) comprises a group of inflammatory conditions of the colon and small intestine, with Crohn's disease and ulcerative colitis being the main types. IBD can lead to serious complications, such as increased risk of colorectal cancer (CRC), one of the most common cancers worldwide. Currently, there is no cure for IBD, and its incidence has been increasing over the past few decades. This review comprehensively summarizes the efficacy of SBG in IBD and CRC and may serve as a reference for future research and development of drugs for IBD and cancer treatment.

Potential Therapeutic Mechanism of Scutellaria baicalensis Georgi against Ankylosing Spondylitis Based on a Comprehensive Pharmacological Model.

Scutellaria baicalensis Georgi (SBG) has significant anti-inflammatory and immune-modulating activities and is widely used in the treatment of inflammatory and autoimmune diseases. However, the mechanism of SBG in the treatment of ankylosing spondylitis (AS) remains to be elucidated. Differentially expressed genes (DEGs) related to AS were analyzed based on two GEO gene chips. The DEGs were merged with the data derived from OMIM, GeneCards, and PharmGKB databases to ascertain AS-related targets. Active components of SBG and their targets were acquired from the TCMSP database. After overlapping the targets of AS and SBG, the action targets were acquired. Subsequently, protein-protein interaction (PPI) network and core target screening were conducted using the STRING database and Cytoscape software. Moreover, the DAVID platform was used to perform Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) analyses of action targets. Finally, the affinity of major active components and core targets was validated with molecular docking. A total of 36 active components of SBG were acquired from TCMSP database. Among these, the main active components were baicalein, wogonin, and oroxylin A. The PPI network and screening showed TNF, IL-6, CXCL8, PTGS2, and VEGFA as core targets associated SBG against AS. GO and KEGG analyses indicated that SBG participated in various biological processes, via regulating IL-17, TNF, and NF-κB signaling pathways. Molecular docking results confirmed a strong binding activity between the main active components and the core targets. The therapeutic mechanism of SBG associated with AS can be characterized as a multicomponent, multitarget, and multipathway mechanism. SBG may be a promising therapeutic candidate for AS.

Regulatory mechanism of Scutellaria baicalensis Georgi on bone cancer pain based on network pharmacology and experimental verification.

Scutellaria baicalensis Georgi (SBG) may relieve bone cancer pain (BCP) by regulating cell proliferation, angiogenesis, and apoptosis. The mechanism of SBG in the treatment of BCP remains to be further explored. The active compounds and targets of SBG were obtained from the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform (TCMSP) and SwissTargetPrediction databases. BCP-related targets were screened from NCBI and GeneCards databases. Additionally, Cytoscape software was applied to construct network diagrams, and OmicShare platform was used to enrich Gene Ontology (GO) and pathways. Finally, the verification of active compounds and core targets was performed based on quantitative real-time PCR (qRT-PCR). Interestingly, we identified baicalein and wogonin as the main active components of SBG. A total of 41 SBG targets, including VEGFA, IL6, MAPK3, JUN and TNF, were obtained in the treatment of BCP. In addition, pathways in cancer may be an essential way of SBG in the treatment of BCP. Experimental verification had shown that baicalein and wogonin were significantly related to BCP core targets. The active components of SBG have been clarified, and the mechanism of the active components in treating BCP has been predicted and verified, which provides an experimental and theoretical basis for the in-depth elucidation of the pharmacodynamics material basis and mechanism of SBG.

Scutellaria baicalensis Georgi regulates REV-ERBα/BMAL1 to protect against skin aging in mice.

Scutellaria baicalensis Georgi (SBG) is a traditional Chinese medicine widely used to treat disorders such as hypertension, dysentery and hemorrhaging. Here, we aimed to assess the pharmacological effects of SBG on skin aging and to investigate the underlying mechanisms. Mice with skin aging were established by treatment with D-galactose and ultraviolet-B. SBG (topical application) showed a protective effect on skin aging in mice, as evidenced by less formation of skin wrinkles, higher levels of SOD (superoxide dismutase) and HYP (hydroxyproline) as well as a lower level of MDA (malondialdehyde). In the meantime, skin MMP-1 and p53 expression were lower, epidermis was thinner and collagen amount was higher in SBG-treated mice. Anti-skin aging effects of SBG were also confirmed in NIH3T3 and HaCaT cells, as well as in mouse primary dermal fibroblasts and human primary epidermal keratinocytes. Furthermore, we found that loss of Rev-erbα (a known repressor of Bmal1) up-regulated skin BMAL1 (a clock component and a known anti-aging factor) and ameliorated skin aging in mice. Moreover, SBG dose-dependently increased the expression of BMAL1 in the skin of aged mice and in senescent NIT3H3 cells. In addition, based on a combination of Gal4 chimeric, luciferase reporter and expression assays, SBG was identified as an antagonist of REV-ERBα and thus an inducer of BMAL1 expression. In conclusion, SBG antagonizes REV-ERBα to up-regulate BMAL1 and to protect against skin aging in mice.

Deciphering the pharmacological mechanisms of Scutellaria baicalensis Georgi on oral leukoplakia by combining network pharmacology, molecular docking and experimental evaluations

BackgroundOral leukoplakia (OLK), an uncharacterized pathological condition that occurs as a white patch in the oral mucosa, is the most common precancerous condition. Scutellaria baicalensis Georgi (SBG) is a medicinal plant with a wide range of pharmacological effects. Increased evidence shows that SBG has potential therapeutic effects on OLK. However, the therapeutic mechanisms of SBG against OLK have not yet been completely elucidated. PurposeThis study aimed to clarify the active components and multi-target mechanisms of SBG against OLK via network pharmacology, molecular docking and experimental evaluations. Study design and methodsThe active components and related targets of SBG were screened by the TCMSP database and Swiss Target Prediction database. Potential therapeutic targets of OLK were collected using the GeneCards and OMIM databases. Then, we established protein-protein interaction (PPI), compound-target-disease (C-T-D), and compound-target-pathway (C-T-P) networks by Cytoscape to identify the main components, core targets, and pharmacological pathways of SBG against OLK via applying data mining techniques and topological parameters. Metascape database was utilized for GO and KEGG pathway analysis. Molecular docking techniques were used to estimate the binding force between the components and the hub genes. Subsequently, a series of in vitro experiments, specifically CCK-8 assay, clone formation assay, wound healing assay, flow cytometry, RT-qPCR and western blotting were conducted for further verification. ResultsThere were 25 active components and 31 related target genes in SBG against OLK. PPI analysis showed that Akt1, VEGFA, EGFR, HIF1A and PTGS2 shared the highest centrality among all target genes. KEGG pathway analysis found that PI3K-Akt signaling pathway may occupy core status in the anti-OLK system. Molecular docking results showed that the main active components of SBG had a strong binding affinity to the hub genes. In vitro experiments showed that the leading component baicalein may inhibit proliferation, block cells in the S phase, induce DOK cell apoptosis, and downregulate the mRNA expression of 5 hub genes by inhibiting PI3K/Akt signaling pathway activation. ConclusionThe most predominant component of SBG against OLK was baicalein and the key pathway was PI3K/Akt. The main components and hub genes had robust binding abilities. In vitro experiments showed that baicalein could inhibit the proliferation of DOK cells, induce apoptosis, block the cell cycle, and inhibit the mRNA expression level of the hub genes by inhibiting the PI3K/Akt pathway.

Unveiling the anti-senescence effects and senescence-associated secretory phenotype (SASP) inhibitory mechanisms of Scutellaria baicalensis Georgi in low glucose-induced astrocytes based on boolean network

BackgroundAstrocytes senescence has been demonstrated in the aging brain and Alzheimer's disease (AD). Moreover, lower glucose metabolism has been confirmed in the early stage of AD. However, whether low glucose could induce astrocytes senescence remain ambiguous. Studies have shown that the ethanol extracts of Scutellaria baicalensis Georgi (SGE) exert neuroprotective and anti-aging effects, while whether SGE could delay astrocytes senescence was unclear. PurposeThis study investigated the anti-senescence effect of SGE in low glucose-induced T98G cells and primary astrocytes, and explored the possible mechanisms based on boolean network. MethodsThe neuroprotective effects of SGE in low glucose-induced T98G cells were evaluated by measurement of cell viability, LDH, ROS and ATP. The anti-senescence effects of SGE were investigated by detection of senescence-associated β-galactosidase (SA-β-Gal), senescence-associated secretory phenotype (SASP), cell cycle and senescence-related markers. The possible mechanisms of SGE in delaying astrocytes senescence were discovered through integrating transcriptomics with boolean network, and validation experiments were further performed. ResultsOur results revealed that low glucose could induce astrocytes senescence, and SGE could delay astrocytes senescence by decreasing the staining rate of SA-β-gal, reducing secretions of SASP factors (IL-6, CXCL1, MMP-1), alleviating cell cycle arrest in G0/G1 phase, decreasing the formation of punctate DNA foci and down-regulating the expression of p16INK4A, p21 and γH2A.X. Transcriptomics and further verification results showed that SGE could markedly inhibit the mRNA expression levels of SASP factors (CXCL10, CXCL2, CCL2, IL-6, CXCR4, CCR7). Moreover, C-X-C motif chemokine 10 (CXCL10) was predicted to be the key SASP factor affecting the network stability by using boolean network. Further experiments validated that SGE could markedly reduce CXCL10 level, decrease the secretion of IL-6 and inhibit cell migration in CXCL10 induced primary astrocytes. ConclusionIn summary, our research unmasks that the anti-senescence effects of SGE were highly correlated with the suppression of SASP secretions, and CXCL10 mediated the SASP inhibition effect of SGE in low glucose-induced astrocytes. Our study highlights that the delay of astrocytes senescence and the inhibition of SASP might be a new mechanism of SGE for alleviating neurodegenerative diseases such as AD.

The root extract of Scutellaria baicalensis Georgi promotes β cell function and protects from apoptosis by inducing autophagy

Scutellaria baicalensis Georgi (SBG) is a traditional Chinese medicine with a remarkable remedial effect on diabetes mellitus. However, the precise mechanism involved has not been fully elucidated yet. Here, we aimed to explore the anti-diabetes effects of its traditional decoction in vitro and elucidate the autophagy-related mechanism. This study was designed to investigate the effects of the water extract of SBG (WSB) on the β cell viability, insulin secretion and the mechanism related to autophagy. Detection of insulin secretion using an enzyme immunoassay method, and analysis of apoptosis rate in MIN-6cells by the flow cytometry with PI and Annexin V-FITC staining. In addition, the autophagy levels and pathways were evaluated from the number of autophagosomes and the expression of autophagy-related proteins. 3-Methyladenine (3-MA) was used as the autophagy inhibitor. Autophagosomes were observed using a confocal microscopy, and autophagy-related proteins (LC3-II/I, p62, S6k, p-AMPK/AMPK, p-mTOR/mTOR) were measured by Western blot. Here we detected a significant increase in insulin release from MIN-6cells after treated with WSB. It is about 1.6 times as much as that of the control group with 2.8mM glucose and 2.2 times more than the 16.8mM glucose group. At the same time, WSB increased the number of autophagosomes and the ratio of LC3 Ⅱ/LC3 Ⅰ, indicating that autophagy were activated in MIN-6cells. When inhibiting autophagy, there was no significant difference in insulin release between the two groups. The apoptotic rate of the high glucose group was as high as 33.23%. After pretreatment with WSB, the apoptotic rate decreased to 14.95%, and increased to 22.57% when treated with 3-MA and WSB. At the same time, WSB treatment enhanced the phosphorylation of AMPK, but had no significant effect on the expression of mTOR and S6K. Our data suggested that WSB increased insulin secretion and reduced apoptosis under high glucose by inducing autophagy through the AMPK pathway, which elucidated the mechanism of WSB in the treatment of diabetes.

Exploring the Mechanism of Scutellaria baicalensis Georgi Efficacy against Oral Squamous Cell Carcinoma Based on Network Pharmacology and Molecular Docking Analysis.

Background Scutellaria baicalensis Georgi (SBG) has been widely shown to induce apoptosis and inhibit invasion and migration of various cancer cells. Increased evidence shows that SBG may be useful to treat oral squamous cell carcinoma (OSCC). However, the biological activity and possible mechanisms of SBG in the treatment of OSCC have not been fully elucidated. This study aimed to clarify the bioactive component and multitarget mechanisms of SBG against OSCC using network pharmacology and molecular docking. Methods Traditional Chinese Medicine Systems Pharmacology (TCMSP) database was used to predict the active components in SBG, and putative molecular targets of SBG were identified using the Swiss Target Prediction database. OSCC-related targets were screened by GeneCards, Online Mendelian Inheritance in Man (OMIM), and Therapeutic Target Database (TTD). Then, we established protein-protein interaction (PPI), compound-target-disease (C-T-D), and compound-target-pathway (C-T-P) networks by Cytoscape to identify the main components, core targets, and pharmacological pathways of SBG against OSCC via applying data mining techniques and topological parameters. Metascape database was utilized for Gene Ontology (GO) and pathway enrichment analysis. The potential interaction of the main components with core targets was revealed by molecular docking simulation, and for the correlation between core targets and OSCC prognosis analysis, the Kaplan–Meier Plotter online database was used. Results There were 25 active compounds in SBG and 86 genes targeted by OSCC. A total of 141 signaling pathways were identified, and it was found that the PI3K-Akt signaling pathway may occupy core status in the anti-OSCC system. GO analysis revealed that the primary biological processes were related to apoptosis, proliferation, and migration. Molecular docking results confirmed that core targets of OSCC had a high affinity with the main compounds of SBG. Conclusion Our study demonstrated multicomponent, multitarget, and multipathway characteristics of SBG in the treatment of OSCC and provided a foundation for further drug development research.

The Key Target and Molecular Mechanism of the Volatile Component of Scutellaria baicalensis Georgi in Acute Lung Injury Based on Network Pharmacology.

Ethnopharmacological relevance: Scutellaria baicalensis georgi is one of the most widely studied TCMs; its effects in ALI have been studied in a large number of experiments, and the efficacy of volatile oil from TCM remains to be studied. Aim: The volatile component of Scutellaria baicalensis georgi was selected to act on the key target of acute lung injury and was preliminarily studied for its specific molecular mechanism. Methods: The volatile active substances of Scutellaria baicalensis georgi were extracted by GC–MS, and the active ingredients related with the occurrence and development of acute lung injury were searched and matched by the TCMSP database. The pharmacologic data and analysis platform of TCM were used to retrieve and screen for the volatile active components and the possible therapeutic targets of Scutellaria baicalensis georgi. In addition, acute lung injury was searched in the disease target database to identify the corresponding disease target proteins, thereby establishing a protein–protein interaction network. Finally, the effects of wogonin on the apoptotic and inflammatory factors in the acute lung injury cell model were analyzed experimentally. Results: We identified 100 candidate targets and successfully constructed a complex target network. The targets identified by the above gene enrichment analysis played important roles in the autoimmune disease cell cycle apoptosis and related signaling pathways. The KEGG pathway analysis showed that most of the target genes were involved in the inflammatory response regulation of the TRP, PI3K-Akt, and IL-17 signaling pathways. The participation of wogonin in the specific regulatory pathways of PI3K-Akt signaling and IL-17 signaling was verified through experiments. In the lung-injured cell model, the results showed that wogonin inhibited the apoptosis of injured lung cells by inhibiting the expression of BAD gene and the activation of cleaved caspase-3 gene while increasing Bcl-2 expression. In addition, wogonin inhibited the expression of the abovementioned inflammatory factors and further inhibited the inflammatory response in the lung injury cells. Conclusion: The results of pharmacological network analysis can predict and explain the regulation mechanism of multi-target and multi-pathway of TCM components. This study identified the potential target and important pathway of wogonin in regulating acute lung injury. At the same time, the accuracy of network pharmacological prediction is also preliminarily verified by molecular biology experiment.

Pathway-based protein-protein association network to explore mechanism of α-glucosidase inhibitors from Scutellaria baicalensis Georgi against type 2 diabetes.

Natural products have been widely used in the treatment of type 2 diabetes (T2D). However, their mechanisms are often obscured due to multi‐components and multi‐targets. The authors constructed a pathway‐based protein–protein association (PPA) network for target proteins of 13 α‐glucosidase inhibitors (AGIs) identified from Scutellaria baicalensis Georgi (SBG), designed to explore the underlying mechanisms. This network contained 118 nodes and 1167 connections. An uneven degree distribution and small‐world property were observed, characterised by high clustering coefficient and short average path length. The PPA network had an inherent hierarchy as C(k)∼k −0.71. It also exhibited potential weak disassortative mixing pattern, coupled with a decreased function Knn (k) and negative value of assortativity coefficient. These properties indicated that a few nodes were crucial to the network. PGH2, GNAS, MAPK1, MAPK3, PRKCA, and MAOA were then identified as key targets with the highest degree values and centrality indices. Additionally, a core subnetwork showed that chrysin, 5,8,2′‐trihydroxy‐7‐methoxyflavone, and wogonin were the main active constituents of these AGIs, and that the serotonergic synapse pathway was the critical pathway for SBG against T2D. The application of a pathway‐based protein–protein association network provides a novel strategy to explore the mechanisms of natural products on complex diseases.

Adsorption and Purification of Baicalin from Scutellaria baicalensis Georgi Extract by Ionic Liquids (ILs) Grafted Silica.

Baicalin which has multiple biological activities is the main active component of the root of Scutellaria baicalensis Georgi (SBG). Although its isolation and purification by adsorption methods have aroused much interest of the scientific community, it suffered from the poor selectivity of the adsorbents. In this work, an environmentally benign method was developed to prepare ionic liquids (ILs) grafted silica by using IL 1-butyl-3-methylimidazolium bis(trifluoromethylsulfonyl)imide ([C4mim]NTf2) and ethanol as reaction media. The IL 1-propyl-3-methylimidazolium chloride ([C3mim]Cl) grafted silica ([C3mim]+Cl−@SiO2) was used to adsorb and purify baicalin from the root extract of Scutellaria baicalensis Georgi (SBG). Experimental results indicated that the adsorption equilibrium can be quickly achieved (within 10 min). The adsorption behavior of [C3mim]+Cl−@SiO2 for baicalin was in good agreement with Langmuir and Freundlich models and the adsorption was a physisorption process as suggested by Dubinin–Radushkevich model. Compared with commercial resins, [C3mim]+Cl−@SiO2 showed the strongest adsorption ability and highest selectivity. After desorption and crystallization, a purity of baicalin as high as 96.5% could be obtained. These results indicated that the ILs grafted silica materials were promising adsorbents for the adsorption and purification of baicalin and showed huge potential in the purification of other bioactive compounds from natural sources.

Development of a Quantitative NMR Method for Direct and Simultaneous Determination of Four Flavonoids in Scutellaria baicalensis georgi Extracts

Introduction: Scutellaria Baicalensis Georgi (SBG), a Traditional Chinese Medicine (TCM) used for the treatment of antiviral therapy, contains many flavonoids. Materials and Methods: A simple, fast and accurate 1H quantitative nuclear magnetic resonance (1HqNMR) method was established for simultaneously determination of four flavonoids (Baicalin, Baicalein, Wogonin and Wogonoside) in SBG extract by using 3,4,5-trichloropyridine as an internal standard (IS). All the NMR determination work was performed at 308 K on an NMR sample tube inserted with a co-axial tube. The NMR sample tube was added with the sample (SBG extract and IS), the co-axial insert tube was added with D2O. Quantification of four flavonoids was carried out by calculating the relative peak area ratio of the selected proton signals from the target compounds and the IS. Results: The validated 1H-qNMR method was successfully used to determine the four flavonoids in 9 batches of SBG from different origins and the results were in good accordance with those obtained from HPLC. Conclusion: The established 1H-qNMR method could be used as a powerful tool for the quality control of SBG from different sources and had potential in the quantification of main components from other TCMs.

Synthesis of Baicalein Modified Cerium Oxide Nanoparticles for Inhibitory Activation of NF-κB and Mitogen-Activated Protein Kinase Signals in Rotenone-Induced Parkinsonian Rats

Baicalein is one of the chief flavones extracted from Scutellariabaicalensis georgi which was earlier reported for its neuroprotective efficacy against Parkinson's disease (PD). In the present study, a simple and efficient synthetic procedure for the preparation of CeO2NPs using Ce(NO3)3 as a primary precursor and baicalein as a stabilizing agent was proposed. Further, the neuroprotective response of baicalein stabilized CeO2 NPs against rotenone-stimulated parkinsonian diseased mice has been explored both in-vitro and in-vivo. From the experimental findings, it was also evident that baicalein exposure has enhanced the motor impairments, and hindered the pro-inflammatory cytokine release and blocked the NF-κB along with MAPK signaling pathway in rotenone-stimulated PD rat models.