Scutellaria baicalensis

BACKGROUND: Chronic stress is prevalent in most societies, impairing cognition, mood, and social functioning. Research suggests that supplements containing extracts from Scutellaria baicalensis root and Crataegus laevigata fruits may offer support in this regard. AIMS: To investigate the acute and chronic effects of a S. baicalensis, C. laevigata, and magnesium/chromium containing herbal supplement on psychological well-being, cognition, and sleep in subjectively stressed but principally healthy adults. METHODS: Forty-three participants (35 analysed) aged 18-75 years received the herbal supplement and a placebo for 15 days. Psychological well-being, and sleep were measured after 7 and 15 days of treatment. Cognitive performance was evaluated following a bolus dose of two tablets and after 15 days, with and without an observed multitasking stressor. RESULTS: The herbal supplement significantly improved performance on a task of attention and working memory (as evidenced by a reduction in serial 3's subtraction errors) following an acute dose and improved working memory performance (an increase in the number of correct serial 7's subtraction) during the stressor, irrespective of dose. Cognitive effects were less consistent in the absence of the stressor. Chronic supplementation improved mood and anxiety, reducing total mood disturbance, anger/hostility, and Trait anxiety scores. A higher proportion of subjects experienced ⩾30% gains in social satisfaction scores after 7 days. No serious adverse effects were reported. CONCLUSIONS: The herbal supplement is safe and enhances mood, reduces subjective anxiety, and improves cognition under stress, though cognitive effects are variable without stress exposure.The study was registered on clinicaltrials.gov (identifier: NCT05757050).

PURPOSE: Oroxylin A (OA) is a flavonoid, obtained from the root of Scutellaria baicalensis Georgi which is a traditional Chinese herbal, with antitumor and other pharmacological activities. OA tablets are an innovative drug, and a formal single ascending and multiple dose pharmacokinetic (PK) trial was conducted in humans to evaluate the required to determine the safety and tolerability of OA as well as the effect of food on its PK parameters profile. METHODS: This clinical study consisted of three parts: single ascending dose (400[n = 3], 800, 1600 and 2400 mg OA [n = 8/group] and placebo [n = 6]), multiple dose (1600 or 2400 mg OA [n = 8 / group] and placebo [n = 4] once daily), and food effects (1600 mg OA single dose [n = 12]). RESULTS: No dose-limiting toxic events (DLT), no serious adverse events (SAEs) or death occurred, and incidence of gastrointestinal AEs were higher in multiple doses than in single dose. OA appeared rapidly in plasma; tmax was approximately 0.17 ~ 5.0 h. The Cmax of OA approximately increased in dose-proportional manner (Cmax slope 1.114), and the AUC0-t increased less than dose increasing (AUC0-t slope 0.7513). After 10 days of continuous administration, OA presented a moderate cumulative effect (1.51-1.73-fold). High-fat diet can increase the Cmax of OA (1.6-fold), and its metabolites increased more significantly (p < 0.05), there was no effect of food on tmax or terminal half-life. CONCLUSIONS: The safety and PK profile support once-daily administration of OA, and considering the effects of food, it is recommended to administrate OA tablet after meals in further clinical studies. TRIAL REGISTRATION NUMBER: ChiCTR2100051434 http://www.chictr.org/cn/ ; Date of registration: 23 Sep., 2021. © 2025. The Author(s), under exclusive licence to Federación de Sociedades Españolas de Oncología (FESEO).

Background/Objectives: The global prevalence of mental health disorders, particularly anxiety and depression, has increased significantly, with rates further elevated by the COVID-19 pandemic. Conventional pharmacological treatments, while effective, often lead to side effects that can impact patient adherence and quality of life. This has driven interest in safer, natural adjunctive therapies. Crocus sativus L. (Iridaceae) (saffron) and Scutellaria baicalensis Georgi (Lamiaceae) (scutellaria) have individually shown potential, in humans and animals, respectively, as mood regulators, with bioactive compounds that modulate neurotransmitter systems and possess anti-inflammatory and anxiolytic effects. This study aimed (1) to explore the efficacy and safety of scutellaria extracts in humans and (2) to test a possible synergistic effect when combining scutellaria and saffron on mood regulation in individuals experiencing mild-to-moderate depressive symptoms. Methods: In a randomized, double-blind, placebo-controlled trial, 180 participants with mild-to-moderate depressive symptoms were assigned to receive either scutellaria extract alone (SCUTELL'UP®), saffron extract alone (SAFFR'ACTIV®), a combination of scutellaria and saffron extracts (SAFFR'UP®), or a placebo for six weeks. The primary outcome was assessed using a standardized depression scale (Beck Depression Inventory). The secondary outcomes, including anxiety, emotional state, well-being level, and sleep quality, were all assessed using validated questionnaires. Safety and tolerability were evaluated throughout the study period. Results: The results confirmed the beneficial effects of saffron extract on depressive and anxious symptoms, as well as its role in improving sleep quality. For the first time in humans, scutellaria extract demonstrated a positive effect on mood regulation. Furthermore, a synergistic effect of the combination of these two extracts was identified, leading to enhanced improvements in depressive and anxious symptoms and emotional well-being among individuals with mild-to-moderate depression, compared to the placebo group. Minimal adverse effects were reported across all treatment group

Flavonoids, known for their neuroprotective properties, are abundant in Acacia catechu and Scutellaria baicalensis. Yet, human studies on their combined effects are limited. OBJECTIVE: This study evaluated the cognitive effects of combined Acacia catechu and Scutellaria baicalensis supplementation in healthy adults. METHODS: In a randomized, double-blind, placebo-controlled trial, 26 males and 59 females (N = 85; 43 ± 8 yrs) consumed the test product (TP) containing 240 mg stem extract of Scutellaria baicalensis and 51 mg heartwood extract of Acacia catechu (UP326, Unigen, Tacoma, WA USA) or placebo (PLA) for four weeks. Cognitive function and biomarkers were assessed throughout the study. RESULTS: Significant time effects (p < 0.001) were observed across cognitive function assessments, with no differences between groups. Energy and fatigue reports showed a significant time effect (p = 0.023), while no significant differences emerged in general health and well-being scores. Cortisol levels increased significantly over time across conditions (p = 0.005), but no significant changes were observed in change scores or individual visits. Interim (p = 0.023) and final (p = 0.004) absolute basophil levels differed significantly between groups, with no intergroup changes. No significant differences in BDNF, CRP, or health and safety biomarkers were detected between supplemental conditions or over time. DISCUSSION: Four-week daily TP supplementation significantly enhanced cognitive function without difference from placebo. However, no adverse events or significant blood marker changes were noted, suggesting TP supplementation is generally well-tolerated. Further research is warranted to explore the preventive and attenuating cognitive effects of this supplementation.Trial registration: ISRCTN.org identifier: ISRCTN16548309.

PURPOSE: To investigate the effect of Scutellaria baicalensis Georgi gargle on oral health and changes in oral bacteria among orthodontic patients. METHODS: About 110 cases of oral fixed orthodontic patients were screened from January 2020 to June 2022 at Taizhou Hospital in Zhejiang Province. They were randomly divided into the experimental group (receiving compound S. baicalensis Georgi gargle once a day) and the control group (receiving 0.9% NS gargle once a day), with 55 cases in each group. Gingival samples were collected from both groups before and 3 months after the orthodontic surgery for bacterial culture, and the differences between the 2 groups of patients in Plaque Index (PLI), gingival bleeding index (sBl), and periodontal depth (PD) before and after the operation were compared. Results: The detection levels of PLI, PD, and sBI in the experimental group were lower than those in the control group (P < .05) 3 months after orthodontic surgery (P < .05); after orthodontic correction for 3 months, there was a significant difference in coccus, bacillus, Campylobacter, Clostridium, Helicobacter, and filamentous bacteria between the experimental group and the control group (P < .05); and Porphyromonas gingivalis, Fusobacterium nucleatum, Bacteroides forsythus (B.f), and Agglomerata actinomycetes in the 2 groups were statistically significant after 3 months of orthodontic treatment (P < .05). CONCLUSION SUBSECTIONS: In fixed orthodontic treatment, S. baicalensis Georgi gargle can effectively inhibit oral pathogens and maintain periodontal health.

Baicalein is a biologically important flavonoid in extracted from the Scutellaria baicalensis Georgi, which can effectively inhibit the influenza virus. This study aimed to analyze the safety and pharmacokinetic (PK) characteristics of baicalein tablets in healthy Chinese subjects and provide more information for phase II clinical trials. In this multiple-ascending-dose placebo-controlled trial, 36 healthy subjects were randomized to receive 200, 400, and 600 mg of baicalein tablet or placebo once daily on day 1 and day 10, 3 times daily on days 4-9. All groups were intended to produce safety and tolerability outcomes (lowest dose first). Blood and urine samples were collected from subjects in the 600 mg group for baicalein PK analysis. Our study had shown that Baicalein tablet was generally safe and well-tolerated. All adverse events were mild and resolved without any intervention except one case of fever reported in the 600 mg group, which was considered as moderate but not related with baicalein as judged by the investigator. Oral baicalein tablets were rapidly absorbed with peak plasma levels being reached within 2 h after multiple administration. The highest urinary excretion of baicalein and its metabolites peaked in 2 h, followed by 12 h, with a double peak trend. © 2021 The Authors. Clinical and Translational Science published by Wiley Periodicals LLC on behalf of the American Society for Clinical Pharmacology and Therapeutics.

ETHNOPHARMACOLOGICAL RELEVANCE: Scutellaria baicalensis (Huang-Qin in Chinese) is a dry root of the perennial herb Scutellaria baicalensis Georgi, which has been used extensively in current prescriptions. Scutellaria baicalensis is an herb high in flavonoids, and baicalein is the one flavonoid found in the highest amount in Scutellaria baicalensis. AIM OF THE STUDY: Influenza virus could cause mild respiratory tract illness to severe pneumonia and even death. Baicalein has been proved to be one of the effective components against the influenza virus. However, there have been few reports on human trials of baicalein. The purpose of this study was to evaluate the safety of baicalein in vivo and analyze its pharmacokinetic characteristics. MATERIALS AND METHODS: Three randomized studies were conducted to evaluate the pharmacokinetics (PK), safety, tolerability, and food effects of baicalein tablets. In the 7-month single-dose safety study, 60 subjects were enrolled and randomized to receive 100-800 mg baicalein tablets or placebo. In the single-dose PK study, 40 subjects were enrolled and randomized to receive 200 mg, 400 mg, 600 mg, 800 mg baicalein tablets. In the study of food effect on PK of baicalein, an additional 10 subjects were enrolled in the 400 mg group, this part of the trial lasted for 7 months. Blood and urine samples for PK analysis were collected at a pre-specified time. PK properties in both fasted and fed states were evaluated, as well as safety and tolerability. RESULTS: Among the 80 subjects who were evaluable for the single-dose safety and tolerability, 56 adverse events (AEs) were observed in 32/80 subjects, of which 49 events were from 28/68 subjects in baicalein group and 7 events were from 4/12 subjects in placebo group. All AEs were mild and resolved without any medical intervention. The most common AEs were elevated high-sensitivity C-reactive protein (hs-CRP) level and high triglycerides. After a single administration of baicalein tablets (200 mg, 400 mg, 600 mg, or 800 mg), Cmax were 280.44, 628.80, 845.20, 489.55 ng/mL; AUC0-∞ were 2035.57, 2939.31, 4494.88, and 3754.43 h*ng/mL, respectively. And t1/2z ranged from 7.80 to 14.91 h. The

Chlamydia trachomatis (C. trachomatis) infection is a prevalent sexually transmitted disease worldwide. Although antibiotics are the standard first-line treatment, the rising incidence of treatment failure highlights the need for alternative therapeutic strategies. Baicalin, a natural flavonoid compound extracted from Scutellaria baicalensis, is known to possess antimicrobial properties. This study aimed to evaluate the anti-chlamydial effects of baicalin. Our results showed that baicalin significantly inhibited the growth of multiple C. trachomatis serovars (A, D, and L2) in HeLa cells, as indicated by reductions in inclusion number and size, as well as decreased cHSP60 level. Moreover, baicalin markedly diminished the production of infectious progeny. Mechanistic investigations suggest that the anti-chlamydial effect of baicalin likely involves direct targeting of elementary bodies to impair their infectivity, rather than interfering with host cell pathways. Furthermore, baicalin exhibited a synergistic inhibitory trend when combined with azithromycin. These findings indicate that baicalin is a promising novel therapeutic candidate for combating C. trachomatis infections.

Multidrug-resistant Klebsiella pneumoniae (MDR-KP) infections present a global health crisis, with escalating resistance to last-line antibiotics. Traditional Chinese medicines (TCMs) demonstrate multi-component synergy against resistant pathogens. This study deciphered the antibacterial mechanisms of bioactive TCM components targeting MDR-KP through integrative pharmacology and experimental validation. Four core TCMs (Scutellaria baicalensis, Forsythia suspensa, Lonicera japonica, Aloe vera) were screened via Chinese Pharmacopoeia and TCMSP database. Network pharmacology identified core components and enriched pathways. Clinically isolated MDR-KP strains (resistant to meropenem, polymyxin E, and tigecycline) were characterized. Synergistic effects were evaluated using checkerboard assays, biofilm quantification, and membrane permeability assays. Molecular docking and RT-qPCR analyzed target interactions, while ELISA and CCK-8 assessed anti-inflammatory activity and cytotoxicity. Consequently, luteolin, wogonin, and kaempferol were identified as key components targeting PI3K/AKT and MAPK pathways. Their triple combination (2/4/8 μg/mL) exhibited potent synergy (FIC = 0.38), reducing biofilm biomass by 68% (p < 0.001) and extracellular polysaccharide thickness from 15.1 μm to 3.1 μm (p < 0.001). Flow cytometry confirmed a 144.8% increase in membrane permeability. Molecular docking revealed high-affinity binding to PI3K (- 6.78 kcal/mol), AKT1 (- 6.60 kcal/mol), and MAPK1 (- 7.24 kcal/mol), with RT-qPCR showing significant downregulation of these genes (p < 0.001). The combination suppressed LPS-induced TNF-α and IL-6 release by 72% and 65%, respectively, while maintaining 95.5% cell viability at therapeutic concentrations. In Conclusion, this study unveils a triple-action mechanism of luteolin-wogonin-kaempferol against MDR-KP, simultaneously disrupting resistance pathways, biofilms, and hyperinflammation. The regimen offers a safe, multi-target therapeutic strategy for combating drug-resistant infections. © 2025. The Author(s), under exclusive licence to Springer-Verlag GmbH Germany, part of Springer Nature.

BACKGROUND: The synergistic use of Danggui (Angelica sinensis, As) and Huangqin (Scutellaria baicalensis or Scutellaria baicalensis Georgi, SbG; As-SbG) exhibits a notable therapeutic effect on metabolic dysfunction-associated steatohepatitis (MASH). However, the underlying pharmacological mechanisms of their synergistic action have not yet been fully elucidated. PURPOSE: This study aims to evaluate the therapeutic efficacy of the synergistic application of As-SbG on MASH induced by various dietary patterns, and to identify the specific potential active compounds, underlying pharmacological mechanisms, and key therapeutic targets responsible for its anti-MASH effects. METHODS: Two MASH animal models induced by methionine- and choline- deficient (MCD) diet and high-fat/high-cholesterol (HFHC) diet were constructed to compare the efficacy of As, SbG and As-SbG synergistic treatment on adipose tissue and liver tissue during MASH progression. Potential mechanistic pathways and key molecular targets were identified through proteomics analysis. The chemical components of As-SbG were characterized using ultrahigh performance liquid chromatography-high resolution mass spectrometry (UPLC-HRMS). The interactions between the identified bioactive components and the key targets from proteomics were further validated using molecular docking methods, focusing on As-SbG's therapeutic potential. Based on these bioinformatics findings, qRT-PCR, immunofluorescence staining, and Western blotting were employed to elucidate the regulatory mechanisms of As-SbG combination therapy on lipid metabolism, inflammation, and apoptosis-related pathways in both in vitro and in vivo MASH models. RESULTS: Compared with single-flavor administration of As and SbG, As-SbG synergistic administration significantly restored the balance among different phenotypes, functions, and sizes of various adipose tissues in MASH-induced mice under different dietary conditions, ameliorated hepatic steatosis and liver damage. Proteomic analysis revealed that the potential synergistic therapeutic effects of As-SbG on MASH were primarily associated with pathways involved in fat metabolism, anti-inflammatory response

Diffuse large B-cell lymphoma (DLBCL) is among the most aggressive hematological malignancies and patients are commonly treated with combinatorial immunochemotherapies such as R-CHOP. Till now, the prognoses are still variable and unsatisfactory, depending on the molecular subtype and the treatment response. Developing effective and tolerable new agents is always urgently needed, and compounds from a natural source have gained increasing attentions. Wogonin is an active flavonoid extracted from the traditional Chinese herbal medicine Scutellaria baicalensis Georgi and has shown extensive antitumor potentials. However, the therapeutic effect of wogonin on DLBCL remains unknown. Here, we found that treatment with wogonin dose- and time-dependently reduced the viability in a panel of established DLBCL cell lines. The cytotoxicity of wogonin was mediated through apoptosis induction, along with the loss of mitochondrial membrane potential and the downregulation of BCL-2, MCL-1, and BCL-xL. In terms of the mechanism, wogonin inhibited the PI3K and MAPK pathways, as evidenced by the clear decline in the phosphorylation of AKT, GSK3β, S6, ERK, and P38. Furthermore, the combination of wogonin and the BCL-2 inhibitor venetoclax elicited synergistically enhanced killing effect on DLBCL cells regardless of their molecular subtypes. Finally, administration of wogonin significantly impeded the progression of the DLBCL tumor in a xenograft animal model without obvious side effects. Taken together, the present study suggests a promising potential of wogonin in the treatment of DLBCL patients either as monotherapy or an adjuvant for venetoclax-based combinations.

The rise in antibiotic resistance among bacterial pathogens, particularly Staphylococcus aureus, has become a critical global health issue, necessitating the search for novel antimicrobial agents. S. aureus uses various mechanisms to resist antibiotics, including the activation of efflux pumps, biofilm formation, and enzymatic modification of drugs. This study explores the potential of baicalein, a bioflavonoid from Scutellaria baicalensis, in modulating tetracycline resistance in S. aureus by inhibiting efflux pumps. The synergistic action of baicalein and tetracycline was evaluated through various assays. The minimum inhibitory concentration (MIC) of baicalein and tetracycline against S. aureus was 256 and 1.0 μg/mL, respectively. Baicalein at 64 μg/mL reduced the MIC of tetracycline by eightfold, indicating a synergistic effect (fractional inhibitory concentration index: 0.375). Time-kill kinetics demonstrated a 1.0 log CFU/mL reduction in bacterial count after 24 hours with the combination treatment. The ethidium bromide accumulation assay showed that baicalein mediated significant inhibition of efflux pumps, with a dose-dependent increase in fluorescence. In addition, baicalein inhibited DNA synthesis by 73% alone and 92% in combination with tetracycline. It also markedly reduced biofilm formation and the invasiveness of S. aureus into HeLa cells by 52% at 64 μg/mL. These findings suggest that baicalein enhances tetracycline efficacy and could be a promising adjunct therapy to combat multidrug-resistant S. aureus infections.

Breast cancer is a major health concern and the leading cause of death among women worldwide. Standard treatment often involves surgery, radiotherapy, and chemotherapy, but these come with side effects and limitations. Researchers are exploring natural compounds like baicalin and baicalein, derived from the Scutellaria baicalensis plant, as potential complementary therapies. This study investigated the effects of baicalin and baicalein on the cytotoxic, proapoptotic, and genotoxic activity of doxorubicin and docetaxel, commonly used chemotherapeutic drugs for breast cancer. The analysis included breast cancer cells (MCF-7) and human endothelial cells (HUVEC-ST), to assess potential effects on healthy tissues. We have found that baicalin and baicalein demonstrated cytotoxicity towards both cell lines, with more potent effects observed in baicalein. Both flavonoids, baicalin (167 µmol/L) and baicalein (95 µmol/L), synergistically enhanced the cytotoxic, proapoptotic, and genotoxic activity of doxorubicin and docetaxel in breast cancer cells. In comparison, their effects on endothelial cells were mixed and depended on concentration and time. The results suggest that baicalin and baicalein might be promising complementary agents to improve the efficacy of doxorubicin and docetaxel anticancer activity. However, further research is needed to validate their safety and efficacy in clinical trials.

Ritonavir, an excellent inhibitor of CYP3A4, has recently been combined with nirmatrelvir to form Paxlovid for the treatment of severe acute respiratory syndrome coronavirus 2 infections. The root of Scutellaria baicalensis Georgi (S. baicalensis), a traditional Chinese medicinal (TCM) herb commonly used to treat heat/inflammation in the lung and digestive tracts, which are major organs targeted by viral infections, contains flavones that can influence the CYP3A metabolism pathway. To investigate the ability of ritonavir to cross the bloodbrain barrier (BBB) and its potential herb-drug interactions with an equivalent TCM clinical dose of S. baicalensis, multisite microdialysis coupled with an LCMS/MS system was developed using rat model. Pretreatment with S. baicalensis extract for 5 days, which contains less flavones than those used in previous studies, had a significant influence on ritonavir, resulting in a 2-fold increase in the total concentration of flavones in the blood and brain. Treatment also boosted the maximum blood concentration of flavones by 1.5-fold and the maximum brain concentration of flavones by 2-fold, all the while exerting no noticeable influence on the transfer ratio across the bloodbrain barrier. These experimental results demonstrated that the use of a typical traditional Chinese medicinal dose of S. baicalensis is sufficient to influence the metabolic pathway and synergistically increase the concentration of ritonavir in rats.

Despite considerable advances in cancer treatment, chemotherapy remains a cornerstone in breast cancer therapy. Therefore, reducing chemoresistance and adverse effects of chemotherapy is a priority. In this regard, Baicalin (BA) is the dominant natural flavonoid extracted from the roots of Scutellaria baicalensis showed fascinating antitumor activity in many types of cancers, including breast cancer. The present study aimed to explore the chemopreventive and antitumor action of baicalin alone and in combination with 5-FU in addition to its ability to enhance the antitumor effect of 5-FU on breast cancer using the Ehrlich solid tumor-mice model. MATERIALS AND METHODS: A total of 70 female mice were divided into seven groups (1st group, saline group; 2nd group, DMSO group; 3rd group, BA+EST group; 4th group, EST group; 5th group, EST+5-FU; 6th group, EST+BA group; 7th group, EST+5-FU+BA).tumors were assessed by weight and histopathological examination. Inflammation, angiogenesis, and apoptosis were examined by ELISA, qRT-PCR, and immunohistochemical examinations. RESULTS: showed that pre-treatment with baicalin and treatment with baicalin and/or 5-FU significantly reduced inflammation and angiogenesis indicated by suppression of NF-kB/ IL-1β and VEGF amplification loop with marked elevation in apoptosis indicated by up-regulation of apoptotic caspase-3, pro-apoptotic p53, Bax and downregulation of anti-apoptotic Bcl-2. CONCLUSION: BA is a promising preventive or adjuvant therapy in breast cancer treatment with 5-FU mainly via cooperative inhibition of inflammation, angiogenesis, and triggering apoptotic cell death.

ETHNOPHARMACOLOGICAL RELEVANCE: Gegen Qinlian Decoction (GQD) (including: Puerariae lobatae (Willd.) Ohwi, radix; (short for Gengen) Glycyrrhiza uralensis Fisch., root and rhizome (short for Gancao), honeyed; Coptis chinensis Franch., rhizome (short for Huanglian); Scutellaria baicalensis Georgi, radix, boiled (short for S. baicalensis) has been widely used to treat inflammatory bowel disease (IBD) and colorectal cancer (CRC). To explore compatibility mechanism of GQD could be of advantage to investigate the complex principle of TCM, which might be conducive to the exploration of the modernization of TCM. AIM OF REVIEW: In this study, a strategy based on system pharmacology was constructed to uncover the multi-target regulation and compatibility mechanism of GQD on the Wnt signaling pathways. MATERIAL AND METHODS: The pharmacological network of GQD was constructed by TCMSP, DAVID, Uniprote database. The cell growth inhibitory effects of puerarin (PUE), wogonin (WOG), berberine (BER), and glycyrrhetinic acid (GLY) on SW480 cells were assessed using CCK-8 assay. The multi-target regulation and compatibility mechanism of combination PUE with GLY were examined by RNA-seq, HPLC-QQQ/MS, qRT- PCR and Western blot analysis. RESULTS: Network pharmacology analysis indicated that PUE, WOG, BER and GLY were the active components in GQD and had a synergistic effect on the targets of the Wnt signaling pathway. Additionally, pharmacological experiments revealed that WOG, BER, and GLY inhibited activity of colorectal cancer (CRC) cell lines SW480 cells, and that PUE only exhibited effective antitumour activity when combined with GLY. CTNNB1, CCND1 and SMAD4 were identified as synergistic targets inhibited by PUE-GLY. Moreover, PUE-GLY could influence the Wnt signaling pathway by upregulating GSK3B and downregulating CTNNB1 synergistically. It also showed that GLY could effectively increase the intracellular content of PUE based on HPLC-QQQ/MS analysis, and this process was achieved by influencing the targets of the membrane's pathway, such as cell adhesion molecules, focal adhesion, and tight junctions. CONCLUSION: GLY was revealed a multi-target mechanism, which could downregu

The skin, as the body's largest organ, is vital for protecting against environmental stressors, regulating temperature, and preventing water loss. Here, we examined the potential of a mixture of five traditional Korean herbal extracts-Cimicifuga racemosa, Paeonia lactiflora, Phellodendron amurense, Rheum rhaponticum, and Scutellaria baicalensis-referred to as herbal medicine composite 5 (HRMC5) for enhancing skin health and managing menopausal symptoms. High-performance liquid chromatography identified 14 bioactive compounds, including flavonoids, phenolic acids, anthraquinones, and alkaloids. In vitro studies revealed an optimal concentration of 0.625 g/L for cell survival and UV protection, with the mixture demonstrating significant wound-healing properties comparable to epidermal growth factor. HRMC5 exhibited anti-inflammatory effects by downregulating COX2 expression and upregulating the key skin barrier proteins. A 4-week clinical trial involving 20 postmenopausal women showed significant improvements in skin redness, hemoglobin concentration, and skin moisture content. Visual analog scale assessments indicated substantial reductions in facial flushing severity and the associated sweating. The topical application of HRMC5 cream offered potential advantages over ingested phytoestrogens by reducing the systemic side effects. These findings suggest that HRMC5 is a promising non-invasive treatment for vasomotor symptoms in menopausal women and overall skin health, warranting further research on its long-term efficacy and safety in larger populations. The efficacy of herbal medicines on anxiety and depression in peri- and postmenopausal women: A systematic review and meta-analysis. Shahmohammadi A(1), Ramezanpour N(2), Mahdavi Siuki M(2), Dizavandi F(3), Ghazanfarpour M(4), Rahmani Y(1), Tahajjodi R(5), Babakhanian M(6). Author information: (1)Clinical Research Development Center, Imam Ali and Taleghani Hospital, Kermanshah University of Medical Sciences, Kermanshah, Iran. (2)Mashhad University of Medical Sciences, Mashhad, Iran. (3)Department of Nursing and Midwifery, School of Nursing and Midwifery, Mashhad University of Medical Sciences, Mashhad, Iran. (4

Metformin is a widely prescribed antidiabetic agent, whereas Scutellaria baicalensis (SB) is a commonly used medicinal herb for treatment of type 2 diabetes (T2D). Gut microbiota is involved in pathophysiology of metabolic diseases including T2D, and intestinal microbiota may be one of the important therapeutic targets for the ailment. This study was conducted to investigate the effects of SB combined with metformin on treatment of T2D while evaluating changes in the gut microbiota composition. Patients with T2D were randomized into control and treatment groups. Subjects who had already been prescribed metformin were allotted to additional SB (3.52 g/day) group or placebo group. The initial treatment session was 8 wk, and after washout period for 4 wk they were crossed over to the opposite treatment for another 8 wk. The influence of SB and placebo on the intestinal microbiota was analyzed by MiSeq system based on 16S rRNA gene. Glucose tolerance was lower in the SB group than the placebo group. Similarly, the relative RNA expression of TNF-α was significantly reduced after SB treatment. SB treatment influenced the gut microbiota, especially Lactobacillus and Akkermansia, which showed remarkable increases after SB treatment. Some subjects showed high liver enzyme levels after SB treatment, and their microbiota composition at baseline differed with subjects whose liver enzymes were not affected. We also predicted that selenocompound metabolism was increased and naphthalene degradation was decreased after SB treatment. These results suggest that SB with metformin treatment may improve the glucose tolerance and inflammation and influence the gut microbiota community in T2D.

BACKGROUND: Though several neuroprotective agents have been evaluated as potential treatments for acute ischemic stroke, none have demonstrated a definitive treatment efficacy, which remains elusive. HT047 is an herbal extract of Scutellaria baicalensis and Pueraria lobata, both of which have been widely used to treat ischemic stroke in traditional Korean medicine. The aims of this trial are to investigate whether HT047 can improve neurologic status, particularly motor function, in acute ischemic stroke patients, and to determine the safety of HT047. METHODS: A multicenter, double-blind, randomized, placebo-controlled, 3-arm parallel group, phase II trial will be conducted in patients who have had an acute ischemic stroke within the past 14 days. The participating patients must have a Fugl-Meyer assessment (FMA) motor score ≤55, with arm or leg weakness, and Korean version of the National Institutes of Health Stroke scale (K-NIHSS) score of ≥4 and ≤15. Seventy-eight participants will be randomized in a 1:1:1 ratio and given high-dose HT047 (750 mg 3 times a day), low-dose HT047 (500 mg 3 times a day), or a placebo for 12 weeks. The primary endpoint is the change in FMA motor score between baseline and week 12. Secondary endpoints are as follows: the change in FMA motor score at weeks 4 and 8 from baseline; the change in FMA motor score at weeks 4, 8, and 12 from baseline according to the timing of treatment initiation (either within 1 week, or 1-2 weeks), or according to the presence of prognostic risk factors (hypertension, diabetes, dyslipidemia, etc); the change in K-NIHSS and Korean versions of the modified Rankin scale (K-mRS) and the modified Barthel index at weeks 4 and 12 from baseline; and the proportion of subjects at week 12 with a K-NIHSS score of 0 to 2, or with K-mRS scores of 0, ≤1, and ≤2. DISCUSSION: This study is a 1st-in-human trial of HT047 to explore the efficacy and safety in acute ischemic stroke patients. The results will provide the appropriate dosage and evidence of therapeutic benefit of HT047 for stroke recovery. TRIAL REGISTRATION: ClinicalTrials.gov (NCT02828540) Registered July 11, 2016.

BACKGROUND AND OBJECTIVES: Baicalein, a flavonoid isolated from the root of Scutellaria baicalensis Georgi, is a neuroprotective agent under development to treat Parkinson's disease. This study investigated the pharmacokinetics, safety and tolerability of baicalein after a multiple-ascending-dose protocol in healthy Chinese volunteers. METHODS: In this single-center, double-blind, placebo-controlled, parallel-group study, participants were randomized to receive baicalein (n = 8 per dose regimen) or placebo (n = 2 per dose regimen). Dosing regimens were 200, 400, and 800 mg once daily on days 1 and 10, twice daily on days 3-9. Plasma, urine, and feces samples were assayed for baicalein and its predominant metabolite baicalin using validated HPLC-MS/MS methods. Pharmacokinetic parameters were computed using standard non-compartmental analysis. Dose proportionality was assessed with a method combining equivalence criterion and power model. Drug safety and tolerability were assessed by monitoring adverse events and laboratory parameters. RESULTS: Thirty-three of 36 enrolled participants completed the study. A total of 44 adverse events occurred in 23 participants. A steady-state concentration of analytes in plasma was achieved on day 8 after repeated dosing. Analytes concentrations and exposure increased with increasing dose. The dose proportionality constant (β) for AUCss of baicalein and baicalin was 0.922 (90 % confidence interval, 0.650-1.195) and 0.942 (90 % confidence interval, 0.539-1.345), respectively. The accumulation index varied from 1.66 to 2.07 for baicalein and from 1.68 to 2.45 for baicalin. CONCLUSION: In dose range of 200-800 mg, multiple-dose oral baicalein administration was safe and well tolerated, dose proportionality was inconclusive, and no serious accumulation of baicalein was observed.

Scutellaria baicalensis, a widely used medicinal herb in traditional Chinese medicine, is frequently employed in the treatment of diabetic nephropathy (DN). Its primary active constituent, baicalin, has shown significant therapeutic potential in animal models of DN; however, no comprehensive and systematic evaluation of its therapeutic effects and underlying mechanisms in DN has yet been conducted. This meta-analysis aimed to assess the efficacy of baicalin in DN treatment and elucidate its pharmacological mechanisms. Relevant studies were retrieved from databases including Web of Science, PubMed, Embase, CNKI, Wanfang Data, and VPCS, covering the literature up to November 2024. Study quality was evaluated using SYRCLE's risk of bias tool, and statistical analyses were performed with STATA 12. Primary outcomes included blood urea nitrogen (BUN), serum creatinine (SCR), and fasting blood glucose (FBG), while secondary outcomes encompassed urinary protein (UP), triglycerides (TG), total cholesterol (TC), inflammatory markers, fibrosis indicators, and oxidative stress parameters. Subgroup analyses, publication bias assessments, and sensitivity analyses were conducted to ensure result reliability. A total of 14 studies involving 221 rodents met the inclusion criteria. Baicalin significantly reduced BUN, SCR, FBG, TG, TC, UP, interleukin-6 (IL-6), interleukin-1 beta (IL-1β), tumor necrosis factor-alpha (TNF-α), malondialdehyde (MDA), and fibronectin (FN) levels while enhancing superoxide dismutase (SOD) activity. These findings suggest that baicalin improves kidney function, reduces proteinuria, corrects lipid metabolism, and alleviates inflammation, oxidative stress, and fibrosis. This meta-analysis concludes that baicalin exhibits significant therapeutic potential in DN models, acting via anti-inflammatory, antioxidant, and antifibrotic mechanisms. The Author(s). This is an open access article published by Thieme under the terms of the Creative Commons Attribution License, permitting unrestricted use, distribution, and reproduction so long as the original work is properly cited. (https://creativecommons.org/licenses/by/4.0/).

Baicalein from Scutellaria baicalensis influences miRNA expression in various cancers, affecting key signaling pathways (PI3K/AKT, Wnt/β-catenin, mTOR) and processes like tumor growth, apoptosis, and metastasis. miRNAs, as small non-coding RNAs, play crucial roles in the cancer pathogenesis-associated gene regulations. This study is aimed at systematically reviewing the effects of baicalein on miRNA expression in various cancers. A comprehensive systematic review was conducted following PRISMA guidelines to investigate the impact of baicalein on miRNA expression in cancer. Databases including PubMed, Scopus, and Web of Science were systematically searched using key search terms. Inclusion criteria encompassed studies reporting changes in miRNA expression following baicalein treatment in cancer cell lines and animal models. Data extraction and risk of bias assessment based on SYRCLE's risk of bias tool were performed to ensure methodological rigor and reliability of the findings. Fifteen studies meeting the inclusion criteria were included in the systematic review. Baicalein impacts miRNA expression in cancers like hepatocellular carcinoma, breast, cervical, ovarian, and gastric cancers, suggesting its potential as a multi-cancer therapeutic. Baicalein regulates tumor-related genes (HDAC10, MDM2, Bcl-2/Bax, and Cyclin E1) and signaling molecules (AKT, FOXO3α), affecting cell viability, apoptosis, and cell cycle, indicating targeted therapeutic potential. In vitro and in vivo studies show baicalein inhibits tumor growth, enhances apoptosis, and regulates cell proliferation, supporting its anticancer effects. Baicalein exhibits potential in modulating miRNA expression in cancer, offering avenues for therapeutic intervention. However, methodological rigor in future studies is essential to enhance the reliability and validity of findings. Comprehensive understanding of baicalein's effects on miRNA expression holds promise for developing novel cancer treatment strategies. © 2025. The Author(s), under exclusive licence to Springer-Verlag GmbH Germany, part of Springer Nature.

Scutellarein is a flavonoid from Scutellaria baicalensis Georgi that has been shown to have a variety of pharmacological activities. This review aims to summarize the pharmacological and pharmacokinetic studies on scutellarein and provide useful information for relevant scholars. Pharmacological studies indicate that scutellarein possesses a diverse range of pharmacological properties, including but not limited to anti-inflammatory, antioxidant, antiviral, neuroprotective, hypoglycemic, hypolipidemic, anticancer, and cardiovascular protective effects. Further investigation reveals that the pharmacological effects of scutellarein are driven by multiple mechanisms. These mechanisms encompass the scavenging of free radicals, inhibition of the activation of inflammatory signaling pathways and expression of inflammatory mediators, inhibition of the activity of crucial viral proteins, suppression of gluconeogenesis, amelioration of insulin resistance, improvement of cerebral ischemia-reperfusion injury, induction of apoptosis in cancer cells, and prevention of myocardial hypertrophy, among others. In summary, these pharmacological studies suggest that scutellarein holds promise for the treatment of various diseases. It is imperative to conduct clinical studies to further elucidate the therapeutic effects of scutellarein. However, it is worth noting that studies on the pharmacokinetics reveal an inhibitory effect of scutellarein on uridine 5'-diphosphate glucuronide transferases and cytochrome P450 enzymes, potentially posing safety risks. © 2024 Deutsche Pharmazeutische Gesellschaft.

Depression is the most prevalent mental disorder, affecting more than 300 million adults worldwide each year, which can lead to serious economic and social problems. Antidepressants are usually the first-line treatment for depression, however, traditional antidepressants on the market have the disadvantage of low remission rates and may cause side effects to patients, therefore, the current focus in the field of depression is to develop novel therapeutic agents with high remission rates and few side effects. In this context, the antidepressant effects of natural compounds have received attention. Baicalin (baicalein-7-O-glucuronide) and its aglycone baicalein (5,6,7-trihydroxyflavone) are flavonoid compounds extracted from the root of Scutellaria baicalensis. Although lacking the support of clinical data, they have been shown to have significantly promising antidepressant activity in many preclinical studies through various rodent models of depression. This paper reviews the antidepressant effects of baicalin and baicalein in experimental animal models, with emphasis on summarizing the molecular mechanisms of their antidepressant effects including regulation of the HPA axis, inhibition of inflammation and oxidative stress, reduction of neuronal apoptosis and promotion of neurogenesis, as well as amelioration of mitochondrial dysfunction. Controlled clinical trials should be conducted in the future to examine the effects of baicalin and baicalein on depression in humans. © 2023. The Author(s), under exclusive licence to Springer Science+Business Media, LLC, part of Springer Nature.

BACKGROUND: Herbal medicine is a low-cost treatment and has been increasingly applied in obesity treatment. Gut microbiota (GM) is strongly associated with obesity pathogenesis. METHODS: We conducted a systematic review guided by the question: "Does the use of herbal medicine change the GM composition in obese individuals?" Randomized clinical trials with obese individuals assessing the effects of herbal medicine intervention in GM were retrieved from the Medline, Embase, Scopus, Web of Science, and Cochrane Library databases, including the Cochrane Controlled Trials Register. Two reviewers independently extracted data using standardized piloted data extraction forms and assessed the study-level risk of bias using an Excel template of the Cochrane "Risk of bias" tool 2-RoB 2. RESULTS: We identified 1094 articles in the databases. After removing duplicates and reading the title and abstract, 14 publications were fully evaluated, of which seven publications from six studies were considered eligible. The herbs analyzed were Moringa oleifera, Punica granatum, Scutellaria baicalensis, Schisandra chinensis, W-LHIT and WCBE. The analysis showed that Schisandra chinensis and Scutellaria baicalensis had significant effects on weight loss herbal intervention therapy composed by five Chinese herbal medicines Ganoderma lucidum, Coptis chinensis, Astragalus membranaceus, Nelumbo nucifera gaertn, and Fructus aurantii (W-LHIT) and white common bean extract (WCBE) on GM, but no significant changes in anthropometry and laboratory biomarkers. CONCLUSIONS: Herbal medicine modulates GM and is associated with increased genera in obese individuals.

Breast cancer is one of the most common malignancies in women, and exhibits high metastasis, recurrence and fatality rates. Novel therapies for breast cancer are constantly emerging, such as targeted therapy, oncolytic virotherapy, and immunotherapy. Despite their potential, these new therapies are still in their infancy, and chemotherapy remains the standard treatment for breast cancer. Therefore, it is of great significance to develop safe and efficient treatment drugs or adjuvants for breast cancer treatment. Traditional Chinese medicine (TCM) has a long clinical history in China, in which Scutellaria baicalensis Georgi exhibits favorable antibreast cancer activities. We therefore conducted a systematic review of the available literature to better understand the molecular mechanisms of S. baicalensis in breast cancer treatment. S. baicalensis and its active components (baicalein, baicalin, wogonin, wogonoside, oroxylin A and scutellarin) exhibited promising antibreast cancer activity through proliferation inhibition, apoptosis induction, invasion and metastasis blockading, and drug-resistance and non-coding RNA regulation. Additionally, senescence, autophagy, angiogenesis, and glycolysis mechanisms were observed to play a role in their antibreast cancer activity. Furthermore, multiple signaling pathways contributed to the antitumor effects of S. baicalensi, such as the NF-[Formula: see text]B, Wnt/[Formula: see text]-catenin, SATB1, Bcl2 family proteins, Caspase, PI3K/Akt, mTOR, ERK, p38-MAPK, TGF-[Formula: see text]/Smad, and Hippo/YAP pathways. This review provides valuable insights into the role of S. baicalensis as a breast cancer treatment and acts as a foundation for further investigations in this field.

BACKGROUND: Regardless of major advances in diagnosis, prevention and treatment strategies, cancer is still a foreboding cause due to factors like chemoresistance, radioresistance, adverse side effects and cancer recurrence. Therefore, continuous development of unconventional approaches is a prerequisite to overcome foregoing glitches. Natural products have found their way into treatment of serious health conditions, including cancer since ancient times. The compound oroxylin A (OA) is one among those with enormous potential against different malignancies. It is a flavonoid obtained from the several plants such as Oroxylum indicum, Scutellaria baicalensis and S. lateriflora, Anchietea pyrifolia, and Aster himalaicus. PURPOSE: The main purpose of this study is to comprehensively elucidate the anticancerous effects of OA against various malignancies and unravel their chemosensitization and radiosensitization potential. Pharmacokinetic and pharmacodynamic studies of OA have also been investigated. METHOD: The literature on antineoplastic effects of OA was searched in PubMed and Scopus, including in vitro and in vivo studies and is summarized based on a systematic review protocol prepared according to Preferred Reporting Items for Systematic Reviews and Meta-Analyses guidelines. The term "oroxylin A" was used in combination with "cancer" and all the title, abstracts and keywords appeared were considered. RESULTS: In Scopus, a total of 157 articles appeared out of which 103 articles that did not meet the eligibility criteria were eliminated and 54 were critically evaluated. In PubMed, from the 85 results obtained, 26 articles were eliminated and 59 were included in the preparation of this review. Mounting number of studies have illustrated the anticancer effects of OA, and its mechanism of action. CONCLUSION: OA is a promising natural flavonoid possessing wide range of pleiotropic properties and is a potential anticancer agent. It has a great potential in the treatment of multiple cancers including brain, breast, cervical, colon, esophageal, gall bladder, gastric, hematological, liver, lung, oral, ovarian, pancreatic and skin. However, lack of pharmacokinetic studies

OBJECTIVE: To conduct a systematic review on the mechanism of action and use of traditional Chinese medicines (TCM) in allergic rhinitis treatment. BACKGROUND: Allergic rhinitis (AR) is a type I allergic disease of the immune system induced by immunoglobulin E mediated inflammation and is characterized by sneezing, nasal itching, paroxysmal nasal obstruction, mucosal edema, cough, and rhinorrhea. More than 500 million people have been affected by rhinitis worldwide in the past 20 years, leading to negative effects on health, quality of life, and social relationships. Currently, the trending medicines used in the case of AR include intranasal corticosteroids and oral H1 antihistamines, which are given as combinatorial medicines supplemented with immune therapy. These medications have been found to be very effective in either the short term or long term; however, they have been found to possess some serious side effects. Search Methodology. The information in this article on classical and traditional Chinese medications used to treat AR was derived from original papers and reviews published in Chinese and English language journals. Two Chinese databases (Wanfang and CNKI) and three English databases (Cochrane Library, PubMed, and Embase) were utilized for data gathering. RESULTS: Traditional Chinese remedies have been identified to influence the production of cytokines such as IL-5 and IL-6, which are key mediators of eosinophilic inflammation, TNF-α, which stimulates TH2 cells at the site of inflammation, and NF-кB, which is required for cytokine and IgE antibody production. TCM has also been shown to be successful in lowering histamine levels, preserving histological changes by decreasing the thickness of the lamina propria, and downregulating the expression of Orai1, STIM1, and TRYC1, showing low expression of Ca+2 channel proteins. CONCLUSION: In this review, we discussed a series of classical, traditional Chinese medications, including Centipeda minima, Scutellaria baicalensis, licorice root (Glycyrrhiza uralensis), and others, as potential antiallergic agents and investigate their in vivo effect upon the production of cytokines and release of histamines for

BACKGROUND: Yinzhihuang granule, consisting of extracts of Artemisia capillaris Thunb., Gardenia jasminoides Ellis, Lonicera japonica Thunb., and Scutellaria baicalensis Georgi is a well-known traditional Chinese patent medicine for patients with liver injury in China. However, the effects and safety of its use for pathologic jaundice in newborns require further systematic evaluation. PURPOSE: To systematically evaluate the efficacy and safety of Yinzhihuang granules for the treatment of neonatal pathologic jaundice and to provide clinical evidence. METHODS: Chinese databases (China Network Knowledge Infrastructure, Wan Fang Database, and VIP Database) and English databases (PubMed, EmBase, and the Cochrane Library) were thoroughly investigated through screening randomized controlled trials on Yinzhihuang granules for neonatal pathologic jaundice from the establishment of all databases to November 18, 2021. A meta-analysis was performed for selected data using STATA software. TSA software was used for trial sequential analyses of the total effective rate and adverse reactions. RESULTS: A total of 19 trials and 2,221 newborns with pathologic jaundice were included in this study. Outcome measures of clinical efficacy in the experimental group were higher than in controls, including total bilirubin (WMD = -30.34, 95% CI = -35.44 to -25.23, p < 0.001), direct bilirubin (WMD = -15.03, 95% CI = -23.54 to -6.52, p < 0.001), indirect bilirubin (WMD = -11.22, 95% CI = -17.50 to -4.95, p < 0.001), recovery time (WMD = -2.96, 95% CI = -3.92 to -2.00, p < 0.001), hospitalization time (WMD = -3.83, 95% CI = -4.89 to -2.76, p < 0.001), and liver function indices. There were statistically significant differences between the two groups. Likewise, the incidence of adverse reactions, including diarrhea, erythra, and fever decreased remarkably in the trial group (RR = 0.44, 95% CI = 0.33 to 0.59, p < 0.001). Publication bias did not exist. We verified the efficacy and safety of Yinzhihuang granules with phototherapy for pathologic jaundice in newborns according using TSA analysis. CONCLUSION: Yinzhihuang granules with phototherapy for neonatal pathologic jaundice are more effectiv

The medicinal plant Scutellaria baicalensis, commonly known as Chinese skullcap or Huang-Qin, has been used as a traditional medicine for several thousand years. The roots of this plant contain bioactive compounds, such as wogonin (WOG), wogonoside, baicalein, and baicalin. The aim of this article is to evaluate the therapeutic potential and mechanisms of action of WOG against different cancers. Numerous in vitro and in vivo studies have revealed that WOG exerts immense therapeutic potential against bladder cancer, breast cancer, cholangiocarcinoma, cervical cancer, colorectal cancer, gallbladder cancer, gastric cancer, glioblastoma, head and neck cancer, hepatic cancer, leukemia, lung cancer, lymphoma, melanoma, multiple myeloma, neuroblastoma, osteosarcoma, ovarian cancer, pancreatic cancer, prostate cancer, and renal cancer by regulating various cell signaling pathways. WOG, in combination with established chemotherapeutic drugs, improves the efficacy of treatment and lowers toxicity. Nevertheless, human trials are warranted to validate these findings. Numerous preclinical studies, combined with an extensive margin of safety and no severe side effects, underscore WOG's therapeutic potential as an anticancer drug. These studies propound the use of WOG as a potential anticancer candidate; however, further high-quality studies are required to firmly establish the clinical efficacy of WOG for the prevention and treatment of human malignancies. © 2022 John Wiley & Sons Ltd.