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Scutellaria baicalensis has been used for the treatment of digestive system disorders for thousands of years in China and other regions. Modern research have revealed its therapeutic efforts in digestive system tumors. Thus, to review the updated progress of S. baicalensis and its main flavonoids in the treatment of digestive system tumors in the past 10 years, this article summarized the therapeutic effect and molecular mechanisms of S. baicalensis and its 5 flavonoids on tumors in oral cavity, esophagus, stomach, colon, liver, pancreas by inhibiting tumor cell proliferation, inducing autophagy, stimulating immune response, and increasing drug sensitivity. In conclusion, S. baicalensis and its flavonoids could be applied to treat digestive system tumors with different type of methods. [ABSTRACT FROM AUTHOR]

High mortality and disability have been principally linked with traumatic brain injury (TBI) with this condition being a principal issue in public health. Currently, there is no reliable pharmaceutical agent to salvage the damage caused by TBI. Baicalein (BCL), a traditional Chinese medicine active ingredient, has preliminarily shown repair activity on brain injury. However, BCL has poor water solubility and bioavailability, which culminates in rapid elimination in vivo. Herein, we sought to solve the above‐mentioned challenges that are associated with the application of this flavonoid by preparing BCL‐loaded long‐circulating liposomes (BLC‐Lips) via thin‐film hydration method. Subsequently, BLC‐Lips were applied to TBI model mice to evaluate their effect on brain injury repair. The results showed that the prepared BLC‐Lips exhibited smaller sized nanoparticles, excellent polydispersed index (PDI), and zeta (ζ)‐potential with stable property. After loading of BCL into the liposomes, we estimated the physicochemical properties of BLC‐Lips to be roughly 87.98% (encapsulation efficiency [EE]) and 7.56% (loading capacity of the drug). Administration of BLC‐Lips through oral route increased aqueous solubility, bioavailability, and time for in vivo circulation of BCL. Moreover, the BLC‐Lips could improve outcomes of histological and neurological motor function and reduce inflammatory cytokines and neurotoxicity after TBI. Taken together, the long‐circulating liposomes may serve as a new approach to potentially prolong drug circulation in vivo and increased bioavailability of BCL for TBI treatment. [ABSTRACT FROM AUTHOR]

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Aim & objective: Combinatorial delivery of Doxorubicin (DOX) and Baicalein (BAC) has a potential to improve breast cancer treatment by mitigating the cardiotoxicity induced by DOX. The nanoformulation has been optimized and subjected to pharmacokinetic studies using LC-MS/MS. Materials & methods: Nanoformulation bearing DOX and BAC was optimized using quality by design approach and method validation was done following USFDA guidelines. Results: The particle size, PDI and zeta potential of developed nanoformulation were 162.56 ± 2.21 nm, 0.102 ± 0.03 and -16.5 ± 1.21 mV, respectively. DOX-BAC-SNEDDs had a higher AUC0-t values of 6128.84 ± 68.71 and 5896.62 ± 99.31 ng/mL/h as compared with DOX-BAC suspension. Conclusion: These findings hold promise for advancing breast cancer treatment and facilitating therapeutic drug monitoring. Graphical Abstract Mechanistic scheme of DOX-BAC-loaded SNEDDs development and its characterization using LC-MS/MS. Article highlights Baicalein (BAC) lowers cardiac oxidative stress which reduces the cardiotoxicity associated with Doxorubicin (DOX). Combination therapies enhance efficacy by targeting multiple disease pathways simultaneously, improving treatment outcomes and reducing drug resistance. The Quality by Design approach was employed in optimizing the self-nanoemulsifying drug delivery system. Currently, there is no published bioanalytical method utilizing either LC-MS/MS or HPLC for simultaneous determination of both DOX and BAC. Both DOX and BAC were resolved using mobile phase of 0.1% v/v FA in milli-Q water and 0.1% v/v FA in MeOH (20:80%v/v) with a flow rate of 0.3 mL/min. USFDA guidelines were employed for assessing several validation factors, including recovery, stability studies, specificity, accuracy and percent relative standard deviation. The co-estimation of DOX and BAC in rat plasma in order to generate an oral P.K. profile was successfully demonstrated using the developed LC-MS/MS. [ABSTRACT FROM AUTHOR]

ABSTRACT The human papillomavirus (HPV) 33 is a high‐risk strain that causes lesions with potential cancerous outcomes. Its E2 protein regulates the viral protein transcription and life cycle maintenance. The DNA binding domain (DBD) of the E2 protein plays a crucial role in the viral life cycle. The DBD region of the E2 protein is particularly interesting for targeting and finding potential inhibitors to inhibit its function or dimerization. Given the limited research on HPV 33 and its proteins, the present work delved into the interaction of two natural polyphenolic compounds, resveratrol, and baicalein, with the E2 DBD of HPV 33 using biophysical and in silico studies. Fluorescence studies of the E2 DBD‐polyphenol complexes showed fluorescence quenching with a binding constant of the order of 106 M−1. Circular dichroism data reveal conformational changes upon binding with the polyphenols, possibly due to distinct binding sites of the E2 DBD. Differential scanning calorimetry exhibited higher melting temperatures for the two complexes than alone DBD, suggesting the complexes' stability. ITC experiment suggested favorable binding reactions with kd values in the micromolar range. Molecular docking and dynamic simulation studies revealed that the resveratrol binds to the helical region and baicalein near the central dimeric interface of E2 DBD with a good binding affinity, forming a stable protein‐ligand complex during the run of 100 ns simulation. Therefore, the current study identifies both polyphenolic compounds as promising candidates for potential antiviral drug development. [ABSTRACT FROM AUTHOR]

Summary: Baicalein is a functional flavonoid that has been intensively studied for its health benefits. Loading baicalein in oil‐in‐water (O/W) emulsions could provide advantages for its application in foods. This work investigated the characteristics of O/W emulsions loaded with baicalein formulated by combination of vegetable oils and homogenisation pressures. Rice bran oil (RBO) and coconut oil (CCO), classified as long‐chain triglycerides and medium‐chain triglyceride, were used in the homogenisation process at 600–1200 bar. The rice bran oil‐in‐water emulsion loaded with baicalein (RBOb/W) produced at 1200 bar provided the emulsion with the smallest particle size of the surface‐weighted mean diameter (d3,2) of 220 nm. The result showed that loading baicalein into RBO could reduce the particle size of O/W emulsion while it increased the particle size of coconut oil‐in‐water emulsion loaded with baicalein (CCOb/W). The RBOb/W and CCOb/W emulsions were physically stable in terms of droplet size during storage at 4 °C for 28 days. The change in viscosity of freshly prepared emulsion loaded with baicalein was dominant compared with the emulsion unloaded baicalein, however, the viscosity profiles of emulsions loaded with baicalein are like emulsions unloaded with baicalein after storage. The influence of baicalein on the viscoelastic properties of emulsion was observed in the storage modulus (G′) at low frequencies. These results suggest that baicalein could potentially interfere with the stabilising effect of Tween 20, contribute to droplet interactions, and migrate from the surface of RBO but not CCO. High baicalein retention of 91–98% was observed in the RBOb/W emulsions. This study recommends that RBO is preferable over CCO to produce O/W emulsion loaded with baicalein in terms of droplet size, stability and retention. It would be useful information to produce functional ingredients for the food industry. [ABSTRACT FROM AUTHOR]

The emergence of the “super fungus” Candida auris poses a significant threat to human health, given its multidrug resistance and high mortality rates. Therefore, developing a new antifungal strategy is necessary. Our previous research showed that Baicalein (BE), a key bioactive compound from the dried root of the perennial herb Scutellaria baicalensis Georgi, has strong fungistatic properties against C. auris. Nevertheless, the antifungal activity of BE against C. auris and its mechanism of action requires further investigation. In this study, we explored how BE affects this fungus using various techniques, including scanning electron microscopy (SEM), Annexin V-FITC apoptosis detection, CaspACE FITC-VAD-FMK In Situ Marker, reactive oxygen species (ROS) assay, singlet oxygen sensor green (SOSG) fluorescent probe, enhanced mitochondrial membrane potential (MMP) assay with JC-1, DAPI staining, TUNEL assay and reverse transcription–quantitative polymerase chain reaction (RT-qPCR). Our findings revealed that BE induced several apoptotic features, including phosphatidylserine (PS) externalization, metacaspase activation, nuclear condensation and DNA fragmentation. BE also increased intracellular ROS levels and altered mitochondrial functions. Additionally, transcriptomic analysis and RT-qPCR validation indicated that BE may induce apoptosis in C. auris by affecting ribosome-related pathways, suggesting that ribosomes could be new targets for antifungal agents, in addition to cell walls, membranes, and DNA. This study emphasizes the antifungal activity and mechanism of BE against C. auris, offering a promising treatment strategy for C. auris infection. [ABSTRACT FROM AUTHOR]

Insulin resistance (IR) is the principal pathophysiological change occurring in diabetes mellitus (DM). Baicalein, a bioactive flavonoid primarily extracted from the medicinal plant Scutellaria baicalensis Georgi, has been shown in our previous research to be a potential natural glucagon-like peptide-1 receptor (GLP-1R) agonist. However, the exact therapeutic effect of baicalein on DM and its underlying mechanisms remain elusive. In this study, we investigated the therapeutic effects of baicalein on diabetes and sought to clarify its underlying molecular mechanisms. Our results demonstrated that baicalein improves hyperglycemic, hyperinsulinemic, and glucometabolic disorders in mice with induced diabetes via GLP-1R. This was confirmed by the finding that baicalein's effects on improving IR were largely diminished in mice with whole-body Glp1r ablation. Complementarily, network pharmacology analysis highlighted the pivotal involvement of the phosphatidylinositol-3-kinase (PI3K)/protein kinase B (AKT) insulin signaling pathway in the therapeutic actions of baicalein on IR. Our mechanism research significantly confirmed that baicalein mitigates hepatic and muscular IR through the PI3K/AKT signal pathway, both in vitro and in vivo. Furthermore, we demonstrated that baicalein enhances glucose uptake in skeletal muscle cells under IR conditions through the Ca2+/calmodulin-dependent protein kinase II (CaMKII)-adenosine 5′-monophosphate-activated protein kinase (AMPK)-glucose transporter 4 (GLUT4) signaling pathway in a GLP-1R-dependent manner. In conclusion, our findings confirm the therapeutic effects of baicalein on IR and reveal that it improves IR in liver and muscle tissues through the PI3K/AKT insulin signaling pathway in a GLP-1R dependent manner. Moreover, we clarified that baicalein enhances the glucose uptake in skeletal muscle tissue through the Ca2+/CaMKII-AMPK-GLUT4 signal pathway. [ABSTRACT FROM AUTHOR]

Renal proximal tubular cells are highly vulnerable to different types of assaults during filtration and reabsorption, leading to acute renal dysfunction and eventual chronic kidney diseases (CKD). The chemotherapeutic drug cisplatin elicits cytotoxicity causing renal tubular cell death, but its executing mechanisms of action are versatile and elusive. Here, we show that cisplatin induces renal tubular cell apoptosis and ferroptosis by disrupting glutathione (GSH) metabolism. Upon cisplatin treatment, GSH metabolism is impaired leading to GSH depletion as well as the execution of mitochondria-mediated apoptosis and lipid oxidation-related ferroptosis through activating IL6/JAK/STAT3 signaling. Inhibition of JAK/STAT3 signaling reversed cell apoptosis and ferroptosis in response to cisplatin induction. Using a cisplatin-induced acute kidney injury (CAKI) mouse model, we found that inhibition of JAK/STAT3 significantly mitigates cisplatin nephrotoxicity with a reduced level of serum BUN and creatinine as well as proximal tubular distortion. In addition, the GSH booster baicalein also reclaims cisplatin-induced renal tubular cell apoptosis and ferroptosis as well as the in vivo nephrotoxicity. In conclusion, cisplatin disrupts glutathione metabolism, leading to renal tubular cell apoptosis and ferroptosis. Rewiring glutathione metabolism represents a promising strategy for combating cisplatin nephrotoxicity.

BACKGROUND: Ferroptosis is a mode of programmed cell death distinct from apoptosis, necrosis, and other novel cellular deaths, which occurs mainly due to accumulated lipid peroxidation. Ferroptosis has been shown to be involved in the pathological process following subarachnoid hemorrhage. Baicalein, serving as an adept sequestered of iron, evinces its prowess by quelling lipid peroxidative cascades. Nonetheless, the enigma lingers as to whether baicalein possesses the capacity to ameliorate neuronal ferroptosis, elicited in the wake of early brain injury after subarachnoid hemorrhage. OBJECTIVE: To investigate the effect and mechanism of baicalein on neuronal ferroptosis after subarachnoid hemorrhage. METHODS: Primary neuronal cells were extracted from C57BL/6L fetal mice at 16-17 days of gestation. Hemoglobin was used to stimulate primary neuronal cells to simulate an in vitro subarachnoid hemorrhage model. The viability of primary neuronal cells treated with baicalein at concentrations of 5, 15, 25, 50, and 100 μmol/L for 24 hours was detected by CCK-8 assay to determine the optimal concentration of baicalein. Primary neuronal cells were divided into control group, hemoglobin group, and hemoglobin+baicalein group. The levels of reactive oxygen species and malondialdehyde in cells were detected by kits. The mRNA expressions of ferroptosis-related markers PTGS2, SLC7A11, and glutathione peroxidase 4 were detected by RT-PCR. The primary neuronal cells were further divided into control group, SLC7A11 inhibitor Erastin group, hemoglobin group, hemoglobin+baicalein group, and hemoglobin+baicalein+Erastin group. The expression of the ferroptosis related markers SLC7A11 and glutathione peroxidase 4 was detected by western blot assay. RESULTS AND CONCLUSION: (1) Baicalein (25 μmol/L) was selected as the following experimental concentration. (2) Compared with the hemoglobin group, the level of malondialdehyde and the level of reactive oxygen species were significantly decreased (P < 0.05) in the hemoglobin+baicalein group. (3) Compared with the hemoglobin group, the mRNA expression of PTGS2 significantly decreased, and the mRNA expression of SLC7A11 and glutathione peroxidase 4 significantly increased (P < 0.000 1) in the hemoglobin+baicalein group. (4) SLC7A11 inhibitor Erastin could reverse the baicalin-improved ferroptosis effect to a certain extent (P < 0.05). (5) The results showed that baicalein could alleviate the ferroptosis of neuronal cells after subarachnoid hemorrhage through the SLC7A11/ GPX4 pathway. [ABSTRACT FROM AUTHOR]

Methicillin-resistant Staphylococcus aureus (MRSA) mastitis poses a significant threat to dairy herds worldwide, given its resistance to methicillin and other β-lactam antibiotics, which often leads to treatment failure. Consequently, there is an urgent need for safe and effective alternative therapeutic approaches. Recent investigations have highlighted the potential of baicalein, a natural flavonoid known for its potent anti-inflammatory and antibacterial properties, especially its synergistic effects with β-lactam antibiotics against MRSA. However, the limited solubility and bioavailability of baicalein hinder its biomedical utility. The present study assessed the therapeutic efficacy of encapsulated baicalein in chitosan, forming a tricomplex with a β-lactam antibiotic, using a murine model of MRSA-induced mastitis. The experimental design comprised seven groups, each consisting of six mice. We evaluated the ability of various treatment regimens to mitigate histopathological alterations and bacterial burden induced by MRSA infection, aiming to elucidate underlying mechanisms. Our results revealed that tricomplex treatment significantly reduced bacterial load in mammary tissue and preserved tissue integrity, resulting in decreased inflammatory responses post-MRSA inoculation. In addition, tricomplex treatment markedly reduced mean leukocyte and neutrophil counts in blood and suppressed the matrix metalloproteinase-9 (MMP-9) concentration and C-reactive protein (CRP) response. Notably, the synergistic interaction between baicalein and amoxicillin was particularly pronounced. Our findings suggest that chitosan-encapsulated baicalein combined with a β-lactam antibiotic holds promise as a therapeutic option for MRSA-induced mastitis. Further investigations, particularly in target animal species, are warranted to comprehensively evaluate its clinical feasibility.

Abstract Purpose To verify the effect and mechanism of baicalein in the treatment of periodontitis through network pharmacology, molecular docking and in vitro experiments. Methods Firstly, multiple databases were used to predict targets of baicalein and periodontitis. And the screened key target genes of baicalein for treating periodontitis were subjected to GO and KEGG analysis; then these targets were analyzed by molecular docking techniques. In vitro experiments including CCK-8, RT-qPCR, ELISA and Immunofluorescence were conducted to validate the efficacy of baicalein in treating periodontitis. Results Seventeen key targets were screened from the databases, GO and KEGG analysis of these targets revealed that baicalein may exert therapeutic effects through regulating TNF, PI3K-Akt, HIF-1 and other signaling pathways. Molecular docking analysis showed that baicalein has good binding potential to several targets. In vitro cellular assays showed that baicalein inhibited the expression of TNF-α, MMP-9, IL-6 and MCP1 in P.g-LPS-induced macrophages at both the mRNA and protein level. And the immunofluorescence intensity of iNOS, a marker of M1 type macrophages, which mainly secretes inflammatory factors, was significantly reduced. Conclusion Baicalein has the characteristics and advantages of “multicomponent, multitarget, and multipathway” in the treatment of periodontitis. In vitro cellular assays further confirmed the inhibitory effect of baicalein on the secretion of inflammatory factors of macrophages in periodontitis models, providing a theoretical basis for further study of the material basis and molecular mechanism of baicalein in the treatment of periodontal diseases.

OBJECTIVE: Endothelial cells play a critical role in maintaining vascular function and kinetic homeostasis, but excessive accumulation of palmitic acid (PA) may lead to endoplasmic reticulum stress and trigger endothelial cell dysfunction. Baicalin (BCL), a natural plant extract, has received widespread attention for its biological activities in anti-inflammation and anti-oxidative stress. However, the mechanism of BCL on PA-induced endothelial cell dysfunction is unclear. Therefore, the aim of this study was to investigate whether BCL could inhibit PA-induced endoplasmic reticulum stress and thus attenuate endothelial cell dysfunction. METHODS: Human umbilical vein endothelial cells (HUVECs) were divided into Control, PA, PA + BCL-10 μM, PA + BCL-20 μM, and PA + BCL-50 μM groups. The PA group was treated with PA (200 μM), while the PA + BCL groups were co-treated with different concentrations of BCL (10 μM, 20 μM, 50 μM) for 24 hours. Cell viability was detected by MTT. Cell migration ability was determined by Transwell assay, apoptosis level by flow cytometry, and tube formation ability by tube formation assay. Finally, the levels of apoptosis-related proteins (Bax, Bcl-2, and cleaved caspase-3) and angiogenesis-related proteins (VEGFA and FGF2) were detected by western blot, MMP-9, as well as the protein levels of endoplasmic reticulum stress biomarkers (GRP78, CHOP, PERK, and ATF4). RESULTS: The results at the cellular level showed that cell viability, migration ability and tube formation ability of PA-induced HUVECs were significantly reduced, while apoptosis level was significantly increased. However, administration of different concentrations of BCL significantly enhanced PA-induced cell viability, migration ability and tube formation ability of HUVECs while inhibiting apoptosis. The results of protein levels showed that the protein levels of Bax and cleaved caspase-3 were observably up-regulated in the cells of the PA group, while the protein level of Bcl-2 was significantly down-regulated; compared with the PA group, the protein levels of Bax and cleaved caspase-3 were much lower and the Bcl-2 protein level was much higher in the PA + BCL group. Additionally, the protein levels of VEGFA, FGF2 and MMP-9 were raised and those of GRP78, CHOP, PERK and ATF4 were lowered in the PA + BCL group of cells in a concentration-dependent manner. CONCLUSION: BCL significantly attenuates PA-induced endothelial cell dysfunction by inhibiting endoplasmic reticulum stress. [ABSTRACT FROM AUTHOR]

Hepatocellular carcinoma (HCC) is a significant global health concern. However, there are limited effective treatments available for it. The use of natural products in the management and treatment of HCC is gaining more attention. Baicalein is a flavonoid compound that has been reported to have antitumor activities in HCC. However, the direct binding targets of baicalein are still unknown. Therefore, we used the DNA‐programmed affinity labeling method to identify the target of baicalein and validated its function in HCC cells. We set blank and competitive DNA probes as negative controls. The results showed that baicalein had 136 binding targets, of which 13 targets were differently expressed in HCC tissues. The enriched cellular process of these targets was apoptosis, which involved MAPK9. We tested the binding affinity of baicalein with MAPK9 as 89.7 nM (Kd) by surface plasmon resonance and analyzed the binding sites by virtual docking. Notably, the binding of baicalein with MAPK9 increased the protein levels of MAPK9 itself and the related downstream apoptosis signaling, triggering the apoptosis of HCC cells. However, the inhibitor of MAPK9, SP600125, blocked the baicalein‐induced apoptosis, and the amounts of MAPK9 and downstream molecules were also decreased, indicating that baicalein acted through MAPK9 to induce apoptosis of HCC cells. In conclusion, we used the DNA‐programmed affinity labeling method to identify the direct‐binding target MAPK9 of baicalein and validated its function in baicalein‐induced apoptosis of HCC cells, which would be helpful to understand and use baicalein in HCC therapy. [ABSTRACT FROM AUTHOR]

Methicillin-resistant Staphylococcus aureus (MRSA) mastitis poses a significant threat to dairy herds worldwide, given its resistance to methicillin and other b-lactam antibiotics, which often leads to treatment failure. Consequently, there is an urgent need for safe and effective alternative therapeutic approaches. Recent investigations have highlighted the potential of baicalein, a natural flavonoid known for its potent anti-inflammatory and antibacterial properties, especially its synergistic effects with b-lactam antibiotics against MRSA. However, the limited solubility and bioavailability of baicalein hinder its biomedical utility. The present study assessed the therapeutic efficacy of encapsulated baicalein in chitosan, forming a tricomplex with a b-lactam antibiotic, using a murine model of MRSA-induced mastitis. The experimental design comprised seven groups, each consisting of six mice. We evaluated the ability of various treatment regimens to mitigate histopathological alterations and bacterial burden induced by MRSA infection, aiming to elucidate underlying mechanisms. Our results revealed that tricomplex treatment significantly reduced bacterial load in mammary tissue and preserved tissue integrity, resulting in decreased inflammatory responses post-MRSA inoculation. In addition, tricomplex treatment markedly reduced mean leukocyte and neutrophil counts in blood and suppressed the matrix metalloproteinase-9 (MMP-9) concentration and C-reactive protein (CRP) response. Notably, the synergistic interaction between baicalein and amoxicillin was particularly pronounced. Our findings suggest that chitosan-encapsulated baicalein combined with a b-lactam antibiotic holds promise as a therapeutic option for MRSA-induced mastitis. Further investigations, particularly in target animal species, are warranted to comprehensively evaluate its clinical feasibility. [ABSTRACT FROM AUTHOR]

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. [ABSTRACT FROM AUTHOR]

Purpose: To verify the effect and mechanism of baicalein in the treatment of periodontitis through network pharmacology, molecular docking and in vitro experiments. Methods: Firstly, multiple databases were used to predict targets of baicalein and periodontitis. And the screened key target genes of baicalein for treating periodontitis were subjected to GO and KEGG analysis; then these targets were analyzed by molecular docking techniques. In vitro experiments including CCK-8, RT-qPCR, ELISA and Immunofluorescence were conducted to validate the efficacy of baicalein in treating periodontitis. Results: Seventeen key targets were screened from the databases, GO and KEGG analysis of these targets revealed that baicalein may exert therapeutic effects through regulating TNF, PI3K-Akt, HIF-1 and other signaling pathways. Molecular docking analysis showed that baicalein has good binding potential to several targets. In vitro cellular assays showed that baicalein inhibited the expression of TNF-α, MMP-9, IL-6 and MCP1 in P.g-LPS-induced macrophages at both the mRNA and protein level. And the immunofluorescence intensity of iNOS, a marker of M1 type macrophages, which mainly secretes inflammatory factors, was significantly reduced. Conclusion: Baicalein has the characteristics and advantages of "multicomponent, multitarget, and multipathway" in the treatment of periodontitis. In vitro cellular assays further confirmed the inhibitory effect of baicalein on the secretion of inflammatory factors of macrophages in periodontitis models, providing a theoretical basis for further study of the material basis and molecular mechanism of baicalein in the treatment of periodontal diseases. [ABSTRACT FROM AUTHOR]

Staphylococcus aureus, a Gram-positive bacterium, is a predominant pathogen associated with various infections. The rapid emergence of antibiotic resistance has intensified the challenge of managing fracture-related infections in severe osteoporotic patients. Rifampicin, a potent antimicrobial agent employed against fracture and implant-related infections, necessitates combination therapies due to its susceptibility to antibiotic resistance. In this study, we explored the potential of baicalein, a bioactive flavonoid from Oroxylum indicum and Scutellaria baicalensis, in combination with rifampicin against S. aureus biofilms invitro. The minimum inhibitory concentration of baicalein and rifampicin were determined as 500 µg/mL and 12.5 ng/mL respectively. The synergistic activity of baicalein and rifampicin was determined by the fractional inhibitory concentration index (FICI) using checkerboard assay. The results showed the FICI of baicalein and rifampicin was lesser than 0.5, demonstrating synergistic effect. Furthermore, the efficacy of baicalein and rifampicin, both individually and in combination, was evaluated for biofilm inhibition and eradication. Scanning electron microscopy and confocal laser microscopy also confirmed that the synergistic combinations effectively removed most of the biofilms and partially killed pre-formed biofilms. In conclusion, the findings demonstrate that baicalein is as effective as rifampicin in inhibiting and eradicating S. aureus biofilms. Their combination exhibits synergistic effect, enhancing their bactericidal effect in completely eradicating S. aureus biofilms. The findings of this research underscore the research potential of combining baicalein and rifampicin as a novel therapeutic strategy against S. aureus biofilms, offering a promising direction for future research in the treatment of fracture-related S. aureus infections. [ABSTRACT FROM AUTHOR]

BACKGROUND: The development of steroid-induced osteonecrosis of the femoral head is a complex process involving multiple mechanisms. There is still no standard therapeutic drug for early intervention of this disease. Current studies have shown that baicalein has various pharmacological activities such as regulating lipid metabolism, bone metabolism, apoptosis and anti-oxidative stress, which provides an idea for the prevention and treatment of steroid-induced osteonecrosis of the femoral head. OBJECTIVE: To observe the preventive effect of baicalein against steroid-induced osteonecrosis of the femoral head and to investigate its possible mechanism. METHODS: Thirty-six 10-week-old male Sprague-Dawley rats were randomly divided into three groups (n=12 per group): blank control group, model group, and baicalein intervention group. In the model group and baicalein intervention group, intraperitoneal lipopolysaccharide and intramuscular injection of methylprednisolone sodium succinate were performed for modeling, while normal saline was used as a substitute for the modeling drug in the blank control group. Baicalein 300 mg/kg was administered by gavage (once a day for 6 weeks) at the time of initial intramuscular glucocorticoid injection in the baicalein intervention group, and baicalein was replaced by normal saline in the other two groups. The serum level of malondialdehyde in rats was detected at 2 weeks of the experiment. Blood lipid indicators and bone formation metabolic markers were detected at 6 weeks of the experiment, the histomorphometric changes of the femoral head were analyzed by hematoxylin-eosin staining, anti-tartaric acid phosphatase staining and TUNEL staining, and the femoral head was subjected to Micro-CT scanning and three-dimensional reconstruction of the bone in order to analyze the alterations of bone tissue structure and parameters. RESULTS AND CONCLUSION: The serum levels of malondialdehyde, triglyceride, β-collagen type I carboxy-terminal peptide were increased and the serum levels of bone specific alkaline phosphatase and pre-collagen type I amino-terminal peptide were decreased in the model group compared with the blank control group (P < 0.05). The serum level of malondialdehyde decreased in the baicalein intervention group compared with the model group (P < 0.05), but there was no significant difference between the baicalein intervention group and blank control group (P > 0.05). The serum level of triglyceride was higher in the baicalein intervention group than the blank control group (P < 0.05), but had no significant difference between the baicalein intervention group and model group (P > 0.05). There were also no significant differences in the levels of bone specific alkaline phosphatase and β-collagen type I carboxy-terminal peptide between the baicalein intervention group and the other two groups (P > 0.05). The serum level of the baicalein intervention group was lower in the baicalein intervention group than the blank control group (P < 0.05) but had no significant difference between the baicalein intervention group and model group (P > 0.05). Histomorphological analysis of the femoral head showed that the rate of bone empty lacuna, osteoclast counting and cell apoptosis rate in the femoral head of model group rats were significantly higher than those of the other two groups (P < 0.05). There was a significant increase in the number of adipocytes in the bone marrow cavity of the femoral head, bone trabeculae were thinned and sparsely arranged with more disruptions in the continuity. The incidence of osteonecrosis was higher in the model group (75%) than in the baicalein intervention group (25%; bilateral and unilateral exact significance results were both 0.05). There was also an increase in the number of adipocytes in the bone marrow cavity of the femoral head in the baicalein intervention group, and the trabecular changes were roughly similar to those in the model group. Micro-CT results showed that bone volume fraction, trabecular thickness, trabecular number, and bone mineral density decreased and trabecular separation increased in the model group compared with the blank control group (P < 0.05). Overall significant bone mass loss was observed in the model group. Bone tissue parameters in the baicalein intervention group were significantly improved than those in the model group, which were reflected in bone volume fraction, trabecular thickness and trabecular separation (P < 0.05), and trabecular number and bone mineral density had no significant difference between the baicalein intervention group and blank control group (P > 0.05). Although baicalein failed to significantly ameliorate dyslipidemia and promote bone formation in rats with steroid-induced osteonecrosis of the femoral head, it could reduce the incidence of steroid-induced osteonecrosis of the femoral head by reducing oxidative stress damage, decreasing cell apoptosis, inhibiting osteoclasts, suggesting its effectiveness in the early prevention of steroid-induced osteonecrosis of the femoral head. [ABSTRACT FROM AUTHOR]

Introduction: Almonertinib is an important third-generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) exhibiting high selectivity to EGFR-sensitizing and T790M-resistant mutations. Almonertinib resistance is a major obstacle in clinical use. Baicalein possesses antitumor properties, but its mechanism of antitumor action against almonertinib-resistant non-small cell lung cancer (NSCLC) remains unelucidated. Methods: CCK-8 assay was used to examine the survival rate of H1975/AR and HCC827/AR cells following treatment for 24 h with different concentrations of baicalein, almonertinib or their combination. The changes in colony formation ability, apoptosis, and intracellular reactive oxygen species (ROS) levels of the treated cells were analyzed using colony formation assay and flow cytometry. Western blotting was performed to detect the changes in protein expressions in the cells. The effects of pre-treatment with NAC on proliferation, apoptosis, and PI3K/Akt signaling pathway were observed in baicalein- and/or almonertinibtreated cells. A nude mouse model bearing subcutaneous HCC827/AR cell xenograft were treated with baicalein (20 mg/kg) or almonertinib (15 mg/kg), and the tumor volume and body mass changes was measured. Results: Both baicalein and almonertinib represses the viability of HCC827/AR and H1975/AR cells in a concentration-dependent manner. Compared with baicalein or almonertinib alone, the combined application of the two drugs dramatically attenuates cell proliferation; triggers apoptosis; causes cleavage of Caspase-3, PARP, and Caspase-9; downregulates the protein expressions of p-PI3K and p-Akt; and significantly inhibits tumor growth in nude mice. Furthermore, baicalein combined with almonertinib results in massive accumulation of reactive oxygen species (ROS) and preincubation with N-acetyl-Lcysteine (ROS remover) prevents proliferation as well as inhibits apoptosis induction, with partial recovery of the decline of p-PI3K and p-Akt. Discussion: The combination of baicalein and almonertinib can improve the antitumor activity in almonertinib-resistant NSCLC through the ROS-mediated PI3K/Akt pathway. [ABSTRACT FROM AUTHOR]

Candida auris, a rapidly spreading multi-drug‐resistant fungus, is causing lethal infections under certain conditions globally. Baicalin (BE), an active ingredient extracted from the dried root of Scutellaria baicalensis Georgi, exhibits antifungal activity. However, studies have shown the distinctive advantages of Traditional Chinese medicine in combating fungal infections, while the effect of BE, an active ingredient extracted from the dried roots of Scutellaria baicalensis Georgi, on C. auris, remains unknown. Therefore, this study aims to evaluate the potential of BE as an antifungal agent against the emerging multidrug‐resistant C. auris. Various assays and models, including microbroth dilution, time growth curve analysis, spot assays, adhesion tests, flocculation test, cell surface hydrophobicity assay, hydrolase activity assays, XTT assay, violet crystal assay, scanning electron microscope (SEM), confocal laser scanning microscope (CLSM), flow cytometry, Live/dead fluorescent staining, reactive oxygen species (ROS), cell wall assay, aggregation assay, porcine skin model, Galleria mellonella larvae (G. mellonella larvae) infection model, and reverse transcription–quantitative polymerase chain reaction (RT-PCR) were utilized to investigate how baicalein suppresses C. auris through possible multifaceted mechanisms. The findings indicate that BE strongly inhibited C. auris growth, adhesion, and biofilm formation. It also effectively reduced drug resistance and aggregation by disrupting the cell membrane and cell wall while reducing colonization and invasion of the host. Transcriptome analysis showed significant modulation in gene expression related to different virulence factors post‐BE treatment. In conclusion, BE exhibits significant effectiveness against C. auris, suggesting its potential as a viable treatment option due to its multifaceted suppression mechanisms. Schematic representation of this study. Baicalein (BE) can effectively hinder the growth and colonization of C. auris by disrupting the expression of multiple virulence factors. This results in a strong antifungal effect, providing protection to the host from infection. [ABSTRACT FROM AUTHOR]

Radiation resistance is a crucial factor influencing therapeutic outcomes in colorectal cancer (CRC). Baicalein (BE), primarily derived from Scutellaria baicalensis, has demonstrated anti‐CRC properties. However, the impact of BE on the radiosensitivity of CRC remains unclear. This study aimed to evaluate the radiosensitization effects of BE and elucidate its mechanism in CRC radiotherapy. We established an in vitro radioresistant cell model (CT26‐R) using parental CRC cells (CT26) subjected to ionizing radiation (IR). CT26‐R cells were pretreated with or without BE, followed by transfection with pcDNA‐NC and pcDNA‐JAK2. The proliferation of CT26‐R cells treated with BE and IR was assessed using a colony formation assay. A CRC animal model was developed in BALB/c mice via CT26‐R cell transplantation. The radiosensitizing effect of BE on CRC was evaluated in vivo. TUNEL assay was conducted to detect apoptosis in tumor tissue. The expression levels of p‐STAT3, JAK2, PD‐L1, and SOCS3 in vitro and in vivo were measured by western blotting. Our results demonstrated that BE significantly increased radiosensitivity in vitro and in vivo and enhanced apoptosis in tumor tissues. Additionally, BE significantly downregulated the expression of p‐STAT3, JAK2, and PD‐L1, and significantly upregulated SOCS3 expression. These in vivo effects were reversed by pcDNA‐JAK2. In summary, our data suggest that BE enhances CRC radiosensitivity by inhibiting the JAK2/STAT3 pathway. [ABSTRACT FROM AUTHOR]

Scutellaria baicalensis, commonly known as Chinese Skullcap, is a traditional herb with a long history of cultural use in Chinese medicines. This review focuses on a comprehensive summary of the morphological description, bioactive compounds, drug-herb interactions, and pharmacological activities of Scutellaria baicalensis, as well as its therapeutic applications. A wide-ranging search using databases such as PubMed, Scopus, Google Scholar, and advanced search on the Web was conducted for data collection from prior studies. The plant root contains major active constituents including flavonoids and flavo-glycosides such as wogonin, baicalein, baicalin, oroxylin A, scutellarein, and norwogonin. These compounds have demonstrated a variety of pharmacological activities, combating inflammation, oxidative stress, cancer, neuronal disorders, and liver disorders. Chinese Skullcap represents a promising avenue for potential pharmacotherapeutic formulation advancement, emphasizing the need for further scientific exploration and clinical trials. [ABSTRACT FROM AUTHOR]

Myocarditis is an inflammatory disease of the cardiac muscle and one of the primary causes of dilated cardiomyopathy. Group B coxsackievirus (CVB) is one of the leading causative pathogens of viral myocarditis, which primarily affects children and young adults. Due to the lack of vaccines, the development of antiviral medicines is crucial to controlling CVB infection and the progression of myocarditis. In this study, we investigated the antiviral effect of baicalein, a flavonoid extracted from Scutellaria baicaleinsis. Our results demonstrated that baicalein treatment significantly reduced cytopathic effect and increased cell viability in CVB3-infected cells. In addition, significant reductions in viral protein 3D, viral RNA, and viral particles were observed in CVB3-infected cells treated with baicalein. We found that baicalein exerted its inhibitory effect in the early stages of CVB3 infection. Baicalein also suppressed viral replication in the myocardium and effectively alleviated myocarditis induced by CVB3 infection. Our study revealed that baicalein exerts its antiviral effect by inhibiting the activity of caspase-1 and viral protease 2A. Taken together, our findings demonstrate that baicalein has antiviral activity against CVB3 infection and may serve as a potential therapeutic option for the myocarditis caused by enterovirus infection. [ABSTRACT FROM AUTHOR]

Objective: Baicalein, one of the most abundant flavonoids found in Chinese herb Scutellaria baicalensis Georgi, exhibits pharmacological activities against various cancers. However, the precise pharmacological mechanism of baicalein in treating castration-resistant prostate cancer (CRPC) remains elusive. This study aimed to elucidate the potential mechanism of baicalein against CRPC through a combination of network pharmacology and experimental approaches, thereby providing new avenues for research in CRPC treatment. Methods: The pharmacological and molecular properties of baicalein were obtained using the TCMSP database. Baicalein-related targets were collected from multiple sources including SwissTarget Prediction, PharmMapper and CTD. Targets related to CRPC were acquired from DisGeNET, GeneCards, and CTD. The protein-protein interaction (PPI) was analyzed using STRING 11.5, and Cytoscape 3.7.2 software was utilized to explore the core targets of baicalein on CRPC. GO and KEGG pathway enrichment analysis were performed using DAVID database. Cell experiments were carried out to confirm the validity of the targets. Results: A total of 131 potential targets of baicalein for the treatment of CRPC were obtained. Among them, TP53, AKT1, ALB, CASP3, and HSP90AA1, etc., were recognized as core targets by Cytoscape 3.7.2. GO function enrichment analysis yielded 926 entries, including 703 biological process (BP) terms, 84 cellular component (CC) terms and 139 molecular function (MF) terms. The KEGG pathway enrichment analysis unveiled 159 signaling pathways, mainly involved in Pathways in cancer, prostate cancer, AGE-RAGE signaling pathway in diabetic complications, TP53 signaling pathway, and PI3K-Akt signaling pathway, etc. Cell experiments confirmed that baicalein may inhibit the proliferation of CRPC cells and induce cell cycle arrest in the G1 phase. This effect could be associated with the TP53/CDK2/cyclin E1 pathway. In addition, the results of CETSA suggest that baicalein may directly bind to TP53. Conclusion: Based on network pharmacology analysis and cell experiments, we have predicted and validated the potential targets and related pathways of baicalein for CRPC treatment. This comprehensive approach provides a scientific basis for elucidating the molecular mechanism underlying the action of baicalein in CRPC treatment. Furthermore, these findings offer valuable insights and serve as a reference for the research and development of novel anti-CRPC drugs. [ABSTRACT FROM AUTHOR]

Baicalein (5,6,7-trihydroxyflavone: C15H10O5, a typical flavonoid), the predominated component of Scutellaria baicalensis Georgi (a traditional Chinese medicine, i.e., Huang Qin), has been simulating great interests due to its various promising and advantage. Numerous molecular properties can be theoretically investigated by quantum chemistry calculation based on the density functional theory, producing stable and reliable results comparable to the case through experimental method. In this work, we systematically studied the molecular properties of baicalein by performing the analyses (geometry, infrared spectrum, bond order, molecular orbital, density of states, localized molecular orbital, localized orbital locator, electron localization function, π-electron population, aromaticity, electrostatic potential, atomic charge, etc.) based on the theoretical quantum chemistry computation with the setup of B3LYP/def2-TZVP. No doubt, our work will provide assistance and theoretical guidance for further research on the component from the traditional Chinese medicine, such as the baicalein involved in this paper, in the future. [ABSTRACT FROM AUTHOR]

Copyright of Journal of Food Safety & Quality is the property of Journal of Food Safety & Quality Editorial Department and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Neurodegenerative diseases (NDDs) represent a category of serious illnesses characterized by the progressive deterioration of neuronal structure and function. The exploration of natural compounds as potential therapeutic agents has gained increasing attention in recent years owing to their wide range of pharmacological activities and minimal side effects. Baicalin (BAI) and baicalein (BE), polyphenolic flavonoids, derived from the root of Scutellaria baicalensis, evidently show potential in treating NDDs. This review provides an overview of the current understanding of the roles of BAI and BE in alleviating neuroinflammation, a pivotal pathological process implicated in various NDDs. Studies conducted prior to clinical trials have shown that BAI and BE exert protective effects on the nervous system in different animal models of NDDs. Furthermore, mechanistic studies indicate that BAI and BE exert anti-inflammatory effects by inhibiting pro-inflammatory cytokines, suppressing microglial activation, and regulating microglial phenotypes. These effects are mediated through the modulation of inflammatory signaling cascades, including Toll-like receptor 4 (TLR4), mitogen-activated protein kinase (MAPK), amp-activated protein kinase (AMPK), NOD-like receptor thermal protein domain-associated protein 3 (NLRP3) inflammasome, and nuclear factor erythroid 2-related factor 2 (Nrf2)/hemoglobin oxygenase-1 (HO-1). Overall, BAI and BE exhibit promising potential as natural compounds with anti-inflammatory properties and offer innovative therapeutic approaches for managing NDDs.

Despite years of development in cancer therapy, achieving successful cancer treatment remains a major research topic. Primary means of cancer treatment include chemotherapy, radiotherapy, and surgery. However, these modalities are associated with limitations and adverse effects on normal tissues. Therefore, there is a search for novel therapeutic approaches that will increase the efficacy of the available treatment while minimizing side effects. Naturally occurring bioactive chemicals such as flavonoids have long been used in traditional medicine to treat various illnesses. Baicalein, an active ingredient in Scutellaria baicalensis Georgi, is utilised in traditional medicine to treat conditions such as hypertension, cardiovascular disease, inflammation, and infections. This review focuses on summarizing the data available on cancer prevention and treatment usage of baicalein. Baicalein is thought to prevent cancer progression by inducing apoptosis, autophagy, and genome instability, and its ability to promote chemo-potentiation, anti-metastatic effects, and regulate specific signalling molecules and transcription factors. Baicalein can be a promising option for cancer treatment, either alone or in combination with established anticancer drugs.

Baicalein, usually obtained after the removal of 7-O-β-D-glucuronic acid from baicalin, has strong pharmacological activity. In this study, a novel strategy for efficient and eco-friendly preparation of baicalein was established by high-temperature-little-acid hydrolysis of baicalin. The effects of inorganic acids, solvents, solid–liquid ratio, HCl concentration and hydrolysis duration on the yield of baicalein were investigated by one-factor-at-a-time experiment. Then, an orthogonal experiment design was conducted for the optimal hydrolysis conditions, namely, baicalin was boiled in n-BuOH solution containing 0.50% HCl (w/v) at 130°C for 2.0 h with solid–liquid ratio at 1:25 (g/mL). In the 60-fold scale-up experiment, the yield of baicalein was achieved at 83.5% ± 6.3%, and its purity was increased from 74.2% to 98.7% after purification. Compared with reported methods, acid consumption per unit product of the newly developed strategy was approximately 80 times lower than that of conventional acid hydrolysis, and time consumption was substantially reduced. Overall, the novel strategy showed great prospects for a cleaner large-scale production of baicalein, which provides a new alternative desirable for the preparation of natural products with high efficiency and low consumption in the pharmaceutical industry.

Scutellaria baicalensis has been used for the treatment of digestive system disorders for thousands of years in China and other regions. Modern research have revealed its therapeutic efforts in digestive system tumors. Thus, to review the updated progress of S. baicalensis and its main flavonoids in the treatment of digestive system tumors in the past 10 years, this article summarized the therapeutic effect and molecular mechanisms of S. baicalensis and its 5 flavonoids on tumors in oral cavity, esophagus, stomach, colon, liver, pancreas by inhibiting tumor cell proliferation, inducing autophagy, stimulating immune response, and increasing drug sensitivity. In conclusion, S. baicalensis and its flavonoids could be applied to treat digestive system tumors with different type of methods.

Baicalein, a nutritional phenolic bioactive small molecule present in the roots of Scutellaria baicalensis and Scutellaria lateriflora, shows promising therapeutic effects against a wide range of cancer cells. However, its potential binding with blood carrier proteins and its anticancer mechanisms have not been well investigated. In this study, the interaction between baicalein and immunoglobulin G (IgG) was analyzed by analyzing intrinsic fluorescence, ellipticity changes, as well as molecular docking. The anticancer effects of baicalein against a glioblastoma multiforme (GBM) cell line, U87MG, and one normal immortalized human astrocytes were assessed by MTT, real-time PCR, caspase assay, and western blot. It was shown that the fluorescence quenching mechanism of human IgG by baicalein was based on a static quenching, where one binding site was responsible for the formation of baicalein-IgG complex derived by the formation of hydrogen bonds and van der Waals forces. A molecular docking study indicated that tyrosine residues (Tyr 91 and Tyr 98) were mostly involved in the binding site of baicalein to IgG. The cellular assay demonstrated that baicalein induced U87MG cell line death with an IC50 concentration of 73.19 µM, whereas normal astrocytes depicted over 82.94% portion of viability at 100 µM baicalein. The Bax mRNA overexpression, Bcl-2 mRNA downexpression, as well as the elevation of caspase-9 and caspase-3 activities confirmed that baicalein could effectively trigger the apoptosis of U87MG cells. Moreover, it was explored that baicalein downregulated the expression of the Axl/STAT3 signaling pathway in the U87MG cells, which is responsible for cellular proliferation and growth. In conclusion, these data may provide useful information regarding the pharmaceutical application of baicalein.

ABSTRACT: The pressing issue of the moment affecting public health is antimicrobial resistance. Methicillin-resistant Staphylococcus aureus (MRSA) is an emerging pathogen that is proven to be resistant to a range of antibiotics like penicillins, cephalosporins, other β ββ-lactam antibiotics, and carbapenems. Baicalein, a phytochemical of the traditional Chinese herb, Scutellaria baicalensis has an inhibitory effect on different bacteria. The current study aimed to investigate the synergistic effect of baicalein and β ββlactam antibiotics (amoxicillin and ampicillin) against methicillin-resistant S. aureus (MRSA). The minimum inhibitory concentrations (MICs) of baicalein and β-lactam antibiotics (amoxicillin and ampicillin) against the MRSA were determined through the broth dilution method. The determination of synergism was tested by checkerboard tube dilution and time-kill assay procedure. The combination of baicalein with amoxicillin showed more potent synergy against MRSA strain compared to the combination of baicalein and ampicillin. The fractional inhibitory concentration indices (FICI) of amoxicillin + baicalein varied from 0.19 to 0.50. The fractional inhibitory concentration (FIC) indices of ampicillin + baicalein varied from 0.19 to 0.25. These findings offer significant evidence that the amoxicillin combined with baicalein showed potent synergistic activity against MRSA in vitro and might offer promising therapeutic implications for MRSA infections.

Objective To investigate the effects of baicalein on T helper cells (Th) 1/2, obestatin and 5-hydroxytryptamine (5-HT) in rats with ulcerative colitis. Methods Forty SPF grade male SD rats were randomly divided into normal group (group N), model group (group M), sulfasalazine group (group S), and baicalein group (group B), with 10 rats in each group. The ulcerative colitis models were established in group M, S and B by trinitrobenzenesulfonic acid. After successful modeling, 0.3 g/kg sulfasalazine was given to group S by gavage, and 50 mg/kg baicalein was given to group B by gavage. Group N and group M were given the same volume of normal saline by gavage at the same time. The disease activity index (DAI) score and colon mucosa damage index (CMDI) score of rats were evaluated, and the pathological morphology of colon tissue was detected by hematoxylin and eosin staining. The protein expression of Th1 cytokine interferon-γ (IFN-γ) and Th2 cytokine interleukin-4 (IL-4) in colon tissues was detected by western blot, and the levels of obestatin and 5-HT in rat serum were detected by ELISA. Results All rats were successfully modeled. The DAI score and CMDI score were significantly increased in group M compared to those in group N (P

Objective To explore the effect of baicalein on myocardial fibrosis in experimental autoimmune myocarditis (EAM) mice and its mechanism. Methods Twenty BalB/C mice were divided into blank group, EAM group, baicalein group, and dexamethasone group, with 5 mice in each group. On days 0 and 7, all the mice except those in the blank group were subcutaneously injected with 200 μL of complete Freund’s adjuvant and α-MyHC peptide emulsion. Starting from day 8, the mice in the EAM group, baicalein group, and dexamethasone group were intragastrically administered sodium carboxymethyl cellulose, baicalein, and dexamethasone, respectively. Echocardiography was performed on day 21 of administration to determine left ventricular ejection fraction (LVEF), shortening fraction (LVFS), left ventricular end-diastolic internal diameter (LVIDd), and left ventricular end-systolic internal diameter (LVIDs) in mice across all groups. On day 21, the mice from all groups were euthanized by cervical dislocation and their heart tissues were collected for HE staining and Masson staining. Flow cytometry was used to detect the proportion of Th17/Treg cells among the splenocytes. Real-time fluorescence quantitative PCR (RT-qPCR) and Western blot were used to analyze the mRNA and protein expression of Collagen Ⅰ, matrix metalloproteinase-1 (MMP-1), interleukin 17A (IL-17A), Treg transcription factor (FOXP3), and IL-10 in the cardiac tissue of mice. Results Echocardiographic results showed that the LVEF and LVFS of mice in baicalein group were significantly higher than those in the EAM group (F=51.55,35.38,q=8.08,5.97,P

Baicalin and baicalein are the primary flavonoids derived from the desiccated root of Scutellaria baicalensis, which is a member of the Lamiaceae family; these flavonoids have diverse pharmacological properties and show significant potential for the management of central nervous system disorders. Multiple studies have indicated that these substances effectively reduce the severity of illnesses such as depression, stroke, and degenerative disorders of the central nervous system by exerting antioxidant and anti-inflammatory effects, regulating programmed cell death, and reducing mitochondrial malfunction. Recent studies have highlighted the connection between the accumulation of iron and the ability of baicalein to protect the nervous system. Given the diverse therapeutic effects of baicalein, this review aims to thoroughly investigate the regulatory pharmacological mechanisms through which baicalein influences the development of central nervous system disorders. By elucidating these mechanisms, this review contributes to the development of therapeutic approaches that target disorders of the central nervous system.

The brain-derived neurotrophic factor (BDNF) plays a crucial role during neuronal development as well as during differentiation and synaptogenesis. They are important proteins present in the brain that support neuronal health and protect the neurons from detrimental signals. The results from the present study suggest BDNF expression can be increase up to ~8-fold by treating the neuroblastoma cells SHSY-5Y with an herbal extract of Oroxylum indicum (50 μg/mL) and ~5.5-fold under lipopolysaccharides (LPS)-induced inflammation conditions. The Oroxylum indicum extract (Sabroxy) was standardized to 10% oroxylin A, 6% chrysin, and 15% baicalein. In addition, Sabroxy has shown to possess antioxidant activity that could decrease the damage caused by the exacerbation of radicals during neurodegeneration. A mode of action of over expression of BDNF with and without inflammation is proposed for the Oroxylum indicum extract, where the three major hydroxyflavones exert their effects through additive or synergistic effects via five possible targets including GABA, Adenoside A2A and estrogen receptor bindings, anti-inflammatory effects, and reduced mitochondrial ROS production. [ABSTRACT FROM AUTHOR]

Carbon dots (CDs) have emerged as significant fluorescent nanomaterials due to their bright, stable fluorescence, good biocompatibility, facile synthesis, etc. They are widely used in various scientific and practical applications, particularly in combination with mesoporous, florescent, or magnetic nanomaterials to enhance their properties. Recent research has focused on employing CDs and their composites in drug analysis, drug loading, biological imaging, disease diagnosis, and temperature sensing, with a growing interest in their biological and medical applications. In this study, we synthesized blue-fluorescent S, N-co-doped CDs (cys-CDs) using hydrothermal synthesis with L-cysteine and sodium citrate. These resulting cys-CD particles were approximately 3.8 nm in size and exhibited stable fluorescence with a quantum yield of 0.66. By leveraging the fluorescence quenching of the cys-CDs, we developed a rapid and sensitive method for baicalein detection, achieving high sensitivity in the low micromolar range with a detection limit for baicalein of 33 nM. Our investigation revealed that the fluorescence-quenching mechanism involved static quenching and inner-filter effect components. Overall, cys-CDs proved to be effective for accurate quantitative baicalein detection in real-world samples. [ABSTRACT FROM AUTHOR]

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. [ABSTRACT FROM AUTHOR]

The pressing issue of the moment affecting public health is antimicrobial resistance. Methicillin-resistant Staphylococcus aureus (MRSA) is an emerging pathogen that is proven to be resistant to a range of antibiotics like penicillins, cephalosporins, other b-lactam antibiotics, and carbapenems. Baicalein, a phytochemical of the traditional Chinese herb, Scutellaria baicalensis has an inhibitory effect on different bacteria. The current study aimed to investigate the synergistic effect of baicalein and b-lactam antibiotics (amoxicillin and ampicillin) against methicillin-resistant S. aureus (MRSA). The minimum inhibitory concentrations (MICs) of baicalein and b-lactam antibiotics (amoxicillin and ampicillin) against the MRSA were determined through the broth dilution method. The determination of synergism was tested by checkerboard tube dilution and time-kill assay procedure. The combination of baicalein with amoxicillin showed more potent synergy against MRSA strain compared to the combination of baicalein and ampicillin. The fractional inhibitory concentration indices (FICI) of amoxicillin + baicalein varied from 0.19 to 0.50. The fractional inhibitory concentration (FIC) indices of ampicillin + baicalein varied from 0.19 to 0.25. These findings offer significant evidence that the amoxicillin combined with baicalein showed potent synergistic activity against MRSA in vitro and might offer promising therapeutic implications for MRSA infections. [ABSTRACT FROM AUTHOR]

Backgrounds: Nasopharyngeal carcinoma is a common malignancy in the head and neck. Baicalein has been reported to exert the anticancer effects on various cancers. In this study, our aim was to explore the function of baicalein in the development of nasopharyngeal carcinoma and further investigate the potential underlying mechanisms. Methods: Cell Counting Kit (CCK)‐8 assay, EdU assay, sphere formation assay, flow cytometry, and transwell invasion assay were conducted to determine cell proliferation, stemness, apoptosis, and invasion, respectively. Western blot was performed to examine the protein levels of PCNA, MMP9, STMN1, β‐catenin, and Wnt3A. The mRNA level of STMN1 was assessed using real‐time quantitative polymerase chain reaction (RT‐qPCR). Xenograft tumor model was carried out to evaluate the effects of baicalein on tumor growth in vivo. Immunohistochemistry (IHC) assay was used to detect the levels of PCNA, MMP9, and STMN1 in tumor tissues from mice. Results: Baicalein significantly induced cell apoptosis and impeded cell proliferation, invasion, and stemness of nasopharyngeal carcinoma cells. STMN1 was highly expressed in nasopharyngeal carcinoma, and baicalein could directly downregulate STMN1 expression. STMN1 knockdown hampered the progression of nasopharyngeal carcinoma cells. Moreover, the effects of baicalein on cell proliferation, stemness, invasion, and apoptosis in nasopharyngeal carcinoma cells were harbored by STMN1 overexpression. Baicalein regulated STMN1 to inhibit the activation of the Wnt/β‐catenin pathway. SKL2001, an agonist of the Wnt/β‐catenin pathway, could reverse the effects of STMN1 knockdown on the progression of nasopharyngeal carcinoma. In addition, baicalein markedly impeded tumor growth in vivo. Conclusion: Baicalein regulated the STMN1/Wnt/β‐catenin pathway to restrain the development of nasopharyngeal carcinoma. [ABSTRACT FROM AUTHOR]

Copyright of Journal of South-Central Minzu University (Natural Science Edition) is the property of Journal of South-Central Minzu University (Natural Science Edition) Editorial Office and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Baicalein (B) has potential antioxidant properties, but it has not been tested as a ram semen extender. This study aimed to assess the impact of B on various sperm parameters and determine its potential influence on semen quality after the freeze-thawing process. During the breeding season, ejaculates were obtained from four rams with the aid of an artificial vagina. The collected mixed semen samples were divided into four groups: control (C; 0), B0.5 (0.5 mM), B1 (1 mM), and B2 (2 mM). After semen extension, the samples were loaded into 0.25 mL straws and stored for 2 h at 4°C prior to freezing in liquid nitrogen vapor and thawed in a water bath at 37°C. Among the groups, B0.5 demonstrated the highest progressive motility results, while B1 and B2 exhibited reduced motility (p < 0.05). In terms of high mitochondrial membrane potential, plasma membrane and acrosome integrity, and viability, B0.5 showed significantly superior outcomes to the other B groups (p < 0.05), although it was not significantly better than C. B1 displayed the highest plasma membrane integrity levels (p < 0.05). Notably, B2 displayed the lowest total antioxidant status levels among the groups (p < 0.05). The findings of this study suggested that the in vitro spermatological characteristics of ram spermatozoa such as progressive motility and chromatin integrity can be protected from the freeze-thawing process by using the 0.5 mM dose of baicalein as a semen extender. The treatment of sperm freezing might benefit from further in-depth research on the role of B in the improvement of cryoinjury and its underlying processes. [ABSTRACT FROM AUTHOR]

Porcine epidemic diarrhea virus (PEDV) has caused severe damage to the global pig industry in the past 20 years, creating an urgent demand for the development of associated medications. Flavonoids have emerged as promising candidates for combating coronaviruses. It is believed that certain flavonoids can directly inhibit the 3C-like protease (3CLpro), thus displaying antiviral activity against coronaviruses. In this investigation, we applied a flavonoid library to screen for natural compounds against PEDV 3CLpro. Baicalein and baicalin were found to efficiently inhibit PEDV 3CLpro in vitro, with the IC50 value of 9.50 ± 1.02 µM and 65.80 ± 6.57 µM, respectively. A docking analysis supported that baicalein and baicalin might bind to the active site and binding pocket of PEDV 3CLpro. Moreover, both baicalein and baicalin successfully suppressed PEDV replication in Vero and LLC-PK1 cells, as indicated by reductions in viral RNA, protein, and titer. Further investigation revealed that baicalein and baicalin mainly inhibited the early viral replication of the post-entry stage. Furthermore, baicalein showed potential effects on the attachment or invasion step of PEDV. Collectively, our findings provide experimental proof for the inhibitory effects of baicalein and baicalin on PEDV 3CLpro activity and PEDV infection. These discoveries may introduce novel therapeutic strategies for controlling porcine epidemic diarrhea (PED). [ABSTRACT FROM AUTHOR]

Staphylococcus aureus, a Gram-positive bacterium, is a predominant pathogen associated with various infections. The rapid emergence of antibiotic resistance has intensified the challenge of managing fracture-related infections in severe osteoporotic patients. Rifampicin, a potent antimicrobial agent employed against fracture and implant-related infections, necessitates combination therapies due to its susceptibility to antibiotic resistance. In this study, we explored the potential of baicalein, a bioactive flavonoid from Oroxylum indicum and Scutellaria baicalensis, in combination with rifampicin against S. aureus biofilms invitro. The minimum inhibitory concentration of baicalein and rifampicin were determined as 500 μg/mL and 12.5 ng/mL respectively. The synergistic activity of baicalein and rifampicin was determined by the fractional inhibitory concentration index (FICI) using checkerboard assay. The results showed the FICI of baicalein and rifampicin was lesser than 0.5, demonstrating synergistic effect. Furthermore, the efficacy of baicalein and rifampicin, both individually and in combination, was evaluated for biofilm inhibition and eradication. Scanning electron microscopy and confocal laser microscopy also confirmed that the synergistic combinations effectively removed most of the biofilms and partially killed pre-formed biofilms. In conclusion, the findings demonstrate that baicalein is as effective as rifampicin in inhibiting and eradicating S. aureus biofilms. Their combination exhibits synergistic effect, enhancing their bactericidal effect in completely eradicating S. aureus biofilms. The findings of this research underscore the research potential of combining baicalein and rifampicin as a novel therapeutic strategy against S. aureus biofilms, offering a promising direction for future research in the treatment of fracture-related S. aureus infections.

Platelet-derived growth factor receptor β (PDGFRβ) plays a crucial role in murine haematopoiesis. Baicalein (BAI), a naturally occurring flavonoid, can alleviate disease damage through anti-oxidative, anti-apoptotic, and anti-inflammatory mechanisms. However, whether BAI attenuates oxidative damage in murine haematopoietic cells by PDGFRβ remains unexplored. In this study, we utilized a tert-butyl hydroperoxide (TBHP)-induced BaF3 cell injury model and an ionising radiation (IR)-induced mice injury model to investigate the impact of the presence or absence of PDGFRβ on the pharmacological effects of BAI. In addition, the BAI-PDGFRβ interaction was characterized by molecular docking and dynamics simulations. The results show that a specific concentration of BAI led to increased cell viability, reduced reactive oxygen species (ROS) content, upregulated nuclear factor erythroid 2-related factor 2 (NRF2) expression, and its downstream target genes heme oxygenase 1 (HO-1) and NAD(P)H Quinone Dehydrogenase 1 (NQO1), and activated protein kinase B (AKT) pathway in cells expressing PDGFRβ plasmid and experiencing damage. Similarly, BAI elevated lineage−Sca1+cKIT+ (LSK) cell proportion, promoted haematopoietic restoration, enhanced NRF2-mediated antioxidant response in PDGFRβ+/+ mice. However, despite BAI usage, PDGFRβ knockout mice (PDGFRβ−/−) showed lower LSK proportion and less antioxidant capacity than the total body irradiation (TBI) group. Furthermore, we demonstrated an interaction between BAI and PDGFRβ at the molecular level. Collectively, our results indicate that BAI attenuates oxidative stress injury and helps promote haematopoietic cell recovery through regulation of PDGFRβ.