Pharmaceutics
·
2026
·Vol. 18
·期 2
·243
·
IF 6.9
Yunshi Zhi,Li Pan,Wenjun Xiong,Thomas Chuen Lam,Huihui Xiao,Chi Wai Do
Background:Glaucoma requires therapies that extend beyond intraocular pressure (IOP)-lowering strategies, and baicalein (BA) offers dual IOP-lowering and neuroprotective potential. This study evaluated the pharmacokinetics of BA and its major metabolite baicalin (BG) in mouse eyes and serum after intravitreal (IVT) and oral administration to determine whether non-invasive oral dosing can achieve IVT-comparable ocular exposure.Methods:BA was administered via IVT injection (100 μM) or oral gavage (20 and 200 mg/kg) in mice, and concentrations of BA and BG in serum and ocular tissues were quantified using a validated ultra-performance liquid chromatography–mass spectrometry (UHPLC/MS) method.Results:After IVT, ocular BA peaked at 331.56 ± 17.75 ng/g at 5 min and declined to 7.13 ± 0.79 ng/g at 4 h, with minimal systemic exposure. Oral administration achieved comparable or higher peak ocular BA levels (380.43 ± 52.85 ng/g at 15 min for 20 mg/kg; 309.70 ± 24.75 ng/g at 5 min for 200 mg/kg), with markedly higher ocular area under the concentration–time curve (AUC: 2455.48 ± 667.83 h·ng/g for 200 mg/kg and 1224.88 ± 751.13 h·ng/g for 20 mg/kg) versus IVT (247.07 h·ng/g). Serum BA and BG peaked at 5 min after oral dosing, with systemic BG exposure substantially exceeding BA.Conclusions:Non-invasive oral BA dosing achieves ocular concentrations comparable to IVT injection, with significantly greater overall exposure and favorable pharmacokinetic profiles. This study provides the first demonstration in mice that non-invasive oral BA administration can replace invasive IVT delivery, establishing a strong rationale for its clinical development in glaucoma and retinal disease management.
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Gastroenterology Research and Practice
·
2020
·
IF 1.806
Geng Chen,Shuodong Wu
This study was aimed at investigating the effect of baicalin on experimental cholesterol gallstones in mice. The mouse gallstone model was induced by feeding with a lithogenic diet, and cholesterol stones were found in the gallbladder. The lithogenic diet caused elevation of triglycerides, cholesterol, and low-density lipoprotein concentrations and descent of high-density lipoprotein concentration in serum. Hyperplasia and inflammatory infiltration were observed in the gallbladder wall of lithogenic diet-fed mice. We also found the increase of cholesterol content and the decrease of bile acid in bile. Real-time PCR and western blot results demonstrated that the expression levels of two enzymes (cholesterol 7α-hydroxylase (CYP7a1) and sterol 12α-hydroxylase (CYP8b1)) to catalyze the synthesis of bile acid from cholesterol were decreased and that two cholesterol transporters (ATP-binding cassette transporter G5/G8 (ABCG5/8)) were increased in the liver of lithogenic diet-fed mice. The lithogenic diet also led to enhanced activity of alanine aminotransferase and aspartate aminotransferase in serum; increased concentrations of tumor necrosis factor-α, interleukin- (IL-) 1β, IL-6, and malondialdehyde; and decreased superoxide dismutase activity in the liver, suggesting inflammatory and oxidative stress. In addition, liver X receptor alpha (LXRα) was increased in the liver. After gavage of baicalin, the lithogenic diet-induced gallstones, hyperlipidemia, gallbladder hyperplasia, inflammation, and oxidative stress in liver and cholesterol metabolism disorders were all alleviated to some degree. The expression of LXRα in the liver was inhibited by baicalin. In addition, the LXRα agonist T0901317 aggravated lithogenic diet-induced harmful symptoms in mice, including the increase of gallstone formation, hyperlipidemia, hepatic injury, inflammation, and oxidative stress. In conclusion, we demonstrated that baicalin played a protective role in a lithogenic diet-induced gallstone mouse model, which may be mediated by inhibition of LXRα activity. These findings may provide novel insights for prevention and therapy of gallstones in the clinic.
研究领域:
药理学
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肝病学
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代谢性疾病
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分子生物学
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高影响因子
ANALYTICAL AND BIOANALYTICAL CHEMISTRY
·
2026
·
IF 3.8
Bo Chunmiao,Han Xiaoyu,Tang Xiaofan,Zhao Weilong
Efficient adsorption and sensitive detection of baicalin (BAI) are essential for maximizing its medical value. In this work, a rhodamine B (Rb)-encapsulated metal–organic framework (MOF)@boric acid–modified covalent organic framework (COF) composite material (Rb-MOF@COF-BA) was designed for high-capacity adsorption and high-sensitivity detection of BAI. Specifically, the Zr-based MOF of UiO-66 was prepared with Zr 4+ and 2-aminoterephthalic acid, during which Rb was encapsulated, resulting in strong red fluorescence. The –NH 2 group on the Rb-MOF surface then reacted with 2,5-dimethoxyterephthalaldehyde and coupled with the ligand 1,3,5-tris(4-aminophenyl)benzene to integrate the COF. Subsequently, to enhance the recognition of cis -diol-containing BAI through boron affinity, Rb-MOF@COF was functionalized with (4-ethynylphenyl)boronic acid via aza-Diels–Alder cyclization, obtaining the Rb-MOF@COF-BA composite with blue fluorescence. For BAI, Rb-MOF@COF-BA demonstrated a high adsorption capacity of 114.2 mg g −1 and reached equilibrium within 200 min. Additionally, the Rb-MOF@COF-BA composite displayed dual emissions at 440 and 580 nm, enabling its use as a ratiometric fluorescence sensor for BAI detection, accompanied by a visible blue-to-red spectral transition. The resulting radiometric fluorescence method demonstrated linear ranges of 0.2−3.0 and 3.0−20.0 μmol L −1 with a low detection limit of 0.0173 μmol L −1 for BAI. This analytical method was employed to identify and quantify BAI in Yinhuang oral solution, yielding favorable results that confirmed the potential of this ratiometric detection for practical applications. Graphical
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ENT-EAR NOSE & THROAT JOURNAL
·
2021
·
IF 1.697
Ming Yang,Xiaoyan Zhu,Feida Fu,Qinghua Guo,Xiaopu Zhu,Yang Xu,Xiaotian Yan,Xinya He,Xu Wang
Objective:Rhinosinusitis is a global health problem affecting millions of people around the world. Baicalin is a bioactive compound isolated from medicinal plant Scutellaria baicalensis Georgi. The present study aims to investigate potential effects of baicalin on clinicopathological changes in nasal/sinus mucosa in a mouse model.Methods:A mouse model of sinonasal inflammation induced by high dose of ovalbumin was applied to evaluate effects of baicalin. Rhinosinusitis symptoms, histopathological features, levels of histamine, immunoglobulin E (IgE), IL-17A, IL-10, and balance of regulatory T cell (Treg)/T-helper 17 (Th17) responses were examined.Results:Baicalin significantly relieved rhinosinusitis symptoms in mice, reduced histopathological changes, and suppressed serum levels of histamine and IgE in a dose-dependent manner. In lymphocytes of mice, baicalin modulated balance of Treg/Th17 proportions by attenuating Th17 cells and enhancing Treg cells, respectively. The serum IL-17A was decreased and IL-10 was increased in mice treated by baicalin. In addition, baicalin promoted levels of Smad protein 3 (p-Smad3) and forkhead box P3 (FOXP3) to promote Treg cells while suppressed levels of p-Stat3 and retineic-acid-receptor-related orphan nuclear receptor γt (RORγt) to inhibit Th17 cells.Conclusions:These data demonstrate that baicalin effectively ameliorates sinonasal inflammation in a mouse model by recovering the immunological balance of Treg/Th17 responses. Our finding highlights the potential value of baicalin for the treatment of rhinosinusitis.
研究领域:
免疫学
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药理学
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病理学
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分子生物学
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MOLECULES
·
2021
·Vol. 26
·期 8
·2322
·
IF 4.412
Yunchang Fan,Di Wu,Sheli Zhang
Baicalin which has multiple biological activities is the main active component of the root ofScutellaria baicalensisGeorgi (SBG). Although its isolation and purification by adsorption methods have aroused much interest of the scientific community, it suffered from the poor selectivity of the adsorbents. In this work, an environmentally benign method was developed to prepare ionic liquids (ILs) grafted silica by using IL 1-butyl-3-methylimidazolium bis(trifluoromethylsulfonyl)imide ([C4mim]NTf2) and ethanol as reaction media. The IL 1-propyl-3-methylimidazolium chloride ([C3mim]Cl) grafted silica ([C3mim]+Cl−@SiO2) was used to adsorb and purify baicalin from the root extract ofScutellaria baicalensisGeorgi (SBG). Experimental results indicated that the adsorption equilibrium can be quickly achieved (within 10 min). The adsorption behavior of [C3mim]+Cl−@SiO2for baicalin was in good agreement with Langmuir and Freundlich models and the adsorption was a physisorption process as suggested by Dubinin–Radushkevich model. Compared with commercial resins, [C3mim]+Cl−@SiO2showed the strongest adsorption ability and highest selectivity. After desorption and crystallization, a purity of baicalin as high as 96.5% could be obtained. These results indicated that the ILs grafted silica materials were promising adsorbents for the adsorption and purification of baicalin and showed huge potential in the purification of other bioactive compounds from natural sources.Keywords:ionic liquids (ILs);grafted silica;adsorption;baicalin;purification
研究领域:
天然产物化学
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植物化学
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TALANTA
·
2016
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IF 4.035
Kai Sheng,Lu Wang,Huichao Li,Lina Zou,Baoxian Ye
The present paper reported an one-pot synthesis of Co nanoparticles doped amino-graphene nanocomposites (Co-amino-Gr), involving in situ generation of Co nanoparticles (NPs). The simultaneous reduction of graphene oxide (GO) and Co 2+ to produce Co-amino-Gr had been achieved under mild reaction conditions using an environmentally benign reducing agent, glycine. By combining the merits of amino-Gr and the Co NPs, a highly sensitive electrochemical sensor was erected to detect baicalin based on the Co-amino-Gr nanocomposites. Under optimum conditions, the response peak currents were linear related with baicalin concentrations in the range of 1.0×10 −8 –8.0×10 −7 mol L −1 with a lower detection limit of 5.0×10 −9 mol L −1 (S/N=3). Additionally, the proposed method was used to detect baicalin in the medicinal capsules with satisfactory results.
研究领域:
材料科学
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分析化学
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纳米技术
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药物分析
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JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2019
·
IF 2.606
Jing Li,Qian Chen,Shurong Zhang,Qihua Jiang,Jingchuan Shang,Liping Zhou,Qiang Li,Shanshan Li,Shan Shi,Yang Li,Wei Li
Baicalin (BCL) is a flavonoid compound with demonstrated potential therapeutic benefits, but the clinical advancements are limited mainly due to its poor aqueous solubility. A guest-host supermolecular inclusion complex of mono-6- O -α-maltosyl-β-cyclodextrin (G2-β-CD) with BCL was developed to improve the aqueous solubility of BCL. The resultant inclusion complex was characterized by DSC , FT-IR, P-XRD, 1 HNMR, 2D-ROESY and SEM analysis . Solubility test suggested that G2-β-CD markedly improved the solubility of BCL and showed A L type phase diagrams. The spectral shifts suggested that the phenyl moiety is buried deeper than the chromen moiety and protrudes from the 6-hydroxyl side of G2-β-CD. Molecular docking verified the experimental findings and supported the insertion of benzene ring of BCL into G2-β-CD cavity via hydrophobic interactions and possible hydrogen bonds . The enhanced bioavailability of the inclusion complex was reflected in earlier T max , higher C max and larger AUC 0-∞ than that of BCL after its oral administration. Taken together, these findings suggested that the solid inclusion complex BCL-G2-β-CD may serve as valuable BCL solid dosage form with good solubility and dissolution rate.
研究领域:
药剂学
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分子生物学
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高影响因子
PHARMACEUTICAL BIOLOGY
·
2022
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IF 3.889
Hui Wang,Qingtao Jiang,Lizhu Zhang
Context Baicalin, a flavonoid extracted from radix scutellariae, possesses various pharmacological effects, including protective effects on renal interstitial fibrosis (RIF), but its possible role and mechanisms have not been fully elucidated.Objective This study explores the protective effects and mechanisms of baicalin on RIF.Materials and methods C57BL/6 male mice were divided into six groups: sham, model, low baicalin, middle baicalin, high baicalin and positive drug groups. The unilateral ureteral obstruction (UUO) model of RIF was constructed and treated with baicalin doses (10, 20 and 40 mg/kg) and a positive control drug (valsartan, 8 mg/kg). H&E staining was used to observe the pathological changes in renal tissues, Masson staining was performed to evaluate collagen deposition in renal tissues, and immunohistochemical examination was adopted to determine α-SMA and extracellular matrix (ECM) expression. Primary mouse fibroblasts were isolated, extracted and treated with baicalin and/or TGF-β. qRT-PCR and enzyme-linked immunosorbent assay (ELISA) were applied to detect the inflammatory responses. Moreover, ECM and TGF-β/Smad expression levels were evaluated by western blot assay.Results Baicalin ameliorated RIF in UUO mice by inhibiting fibrosis and inflammatory responses. The TGF-β/Smad pathway was significantly suppressed in the UUO mouse model. Additionally, baicalin significantly inhibited ECM expression and inflammatory factors in fibroblasts treated with TGF-β. TGF-β/Smad pathway activation was significantly decreased in fibroblasts.Discussion and conclusions These findings support the use of baicalin as a potential therapeutic option for the treatment of RIF by possibly inhibiting the TGF-β/Smad signalling pathway.
研究领域:
药理学
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肾病学
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分子生物学
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TOXICOLOGY AND APPLIED PHARMACOLOGY
·
2017
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IF 3.791
Yi Cai,Wanqing Ma,Yichuan Xiao,Bo Wu,Xiaobing Li,Fengrong Liu,Jianhua Qiu,Genshui Zhang
Baicalin is a major flavonoid compound purified from Scutellariae radix , which has been described as an herb in the Chinese Pharmacopoeia. Previous studies have suggested baicalin possessed extensive anti-inflammatory, anti-cancer, anti-viral properties. However, up to known, there have been no reports of safety and toxicity in the rats following oral administration of baicalin. In this present study, we showed the first evidence that treatment of baicalin (400, 800 and 1600 mg/kg/day) induced significantly kidney injury and fibrosis . The collagen synthesis and fibrosis-related protein expression were increased in the kidney of Sprague-Dawley (SD) rats after treatment with high doses of baicalin. We further investigated the potential molecular mechanism of baicalin-mediated renal fibrosis and revealed that baicalin activated the transforming growth factor-β (TGF-β)/Smad signaling pathway in a dose-dependent manner. Moreover, we also observed that baicalin induced Smad3 interaction with transcriptional coactivator p300 accompanying with increment of Smad3 acetylation . Our results may contribute to better understanding of the future pharmacological and toxicological studies of Scutellaria baicalensis Georgi and its active compounds on the human disease.
研究领域:
药理学
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毒理学
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分子生物学
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高影响因子
NEW JOURNAL OF CHEMISTRY
·
2022
·Vol. 46
·期 34
·16341-16351
·
IF 3.925
Wanjun Jiang,Shiyu Wu,Guorong Fan,Zongde Wang,Shangxing Chen,Yangping Wen,Peng Wang
The extraordinary properties and unique structure of porous carbon have rapidly turned it into a new favorite in the development and application of high-performance electrocatalytic sensors. Nitrogen, phosphorus co-doped hollow porous carbon microspheres (PRM-HPAs) as an oxidase-like electrocatalytic sensor for baicalin were successfully developed by two-stage activation using both 3-aminophenol and formaldehyde as carbon sources, phosphoric acid as an activator and dopant, and N-dehydroabietoyl-L-alanine as a soft-template. Low-temperature activation in air is the key to obtaining the hollow structure, and increases the content of oxygen-containing groups. High-temperature activation with phosphoric acid in nitrogen significantly increases the micropore content of PRM-HPA, and realizes phosphorus doping. The introduction of a soft-template can effectively prevent the agglomeration of carbon particles, and form uniformly dispersed hollow carbon microspheres. The PRM-HPA with a specific surface area of 1388 m2 g−1, pore volume of 0.69 m3 g−1, and pore size of 17 Å displays excellent electrocatalytic ability, oxidase-like characteristics, and an excellent electrochemical response of about 118-fold enhancement for baicalin in linear ranges of 0.03–7.99 μM with a low limit of detection of 4.3 nM. This work will open a new pathway for the preparation of co-doped hollow porous carbon microspheres and the application of renewable rosin resource.
研究领域:
材料科学
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分析化学
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药物分析
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AMERICAN JOURNAL OF CHINESE MEDICINE
·
2023
·
IF 5.7
Xingguan Yang,Jiahui Han,Zhirong Huan,Ce Xu,Qiubo Wang,Xin Ge
Hemorrhagic shock (HS) is defined as a reduction in tissue oxygenation and organ dysfunction due to severe blood loss. Lung injury is a frequent complication of HS. Baicalin, isolated from Radix Scutellariae , has been reported to profile the antitumor, anti-oxidative, anti-inflammatory, and antibacterial roles in various pathological processes. Nevertheless, the effects of baicalin on HS-induced lung injury are unclear. This study aims to examine the therapeutic effects of baicalin on lung injury. We first established the lung injury rat models by withdrawing blood in the femoral artery followed by resuscitation. A pathological analysis showed that HS-administrated rats presented severe capillary leakage and pulmonary edema, while baicalin therapy alleviated the symptoms. Baicalin therapy reduced the number of macrophages and neutrophils in bronchoalveolar lavage fluid and decreased the expression and activity of myeloperoxidase (neutrophile infiltration marker) in the lung tissues of HS rats, indicating that baicalin alleviated HS-induced infiltration of inflammatory cells. The secretion of inflammatory cytokines, including interleukin (IL)-1 β , IL-6, IL-18, and tumor necrosis factor α (TNF- α ), as well as the activation of the nucleotide-binding oligomerization domain-like receptor family pyrin domain-containing-3 (NLRP3) inflammasome, were inhibited by baicalin administration. Furthermore, we found that the NF- κ B pathway, a canonical pro-inflammatory pathway, was also blocked after treatment with baicalin in HS-evoked rats, as indicated by the decreased expression of p65 and p65 phosphorylation in the lung tissues. In summary, we infer that baicalin may exert a protective role in HS-induced lung injury by suppressing the activation of NLRP3 inflammasome via the NF- κ B pathway.
研究领域:
药理学
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免疫学
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病理生理学
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分子生物学
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高影响因子
ELECTROCHIMICA ACTA
·
2026
·
IF 5.8
Yuchuan Zhu,Xinyu Huang,Ruoxi Yang,Ruoyao Tong,Changqing Lu,Ruirui Yue
One-pot synthesis of rGO/PEDOT:PSS/Ru composite for targeted flavonoid sensing. • PEDOT:PSS prevents rGO restacking and enables uniform Ru nanoparticle dispersion. • Interfacial coupling downshifts Ru d-band center to accelerate oxidation kinetics. • Ternary architecture greatly minimizes charge-transfer resistance at the interface. Flavonoid quantification is essential for pharmaceutical and food quality control, yet direct electrochemical detection is hindered by sluggish heterogeneous electron-transfer kinetics and limited current responses at trace concentrations on unmodified electrodes. We report an electrochemical sensing platform based on an rGO/PEDOT:PSS/Ru nanocomposite. Structural characterization indicates that π-π stacking between rGO and PEDOT:PSS prevents graphene restacking, enabling uniform Ru nanoparticle distribution. Crucially, interfacial electronic coupling within the ternary network downshifts the d-band center of the Ru nanoparticles, thereby accelerating the electro-oxidation kinetics. Electrochemical kinetic analyses reveal that the analytes undergo an adsorption-controlled, two-electron and two-proton (2e - /2H + ) transfer pathway. This architecture significantly minimizes charge-transfer resistance and expands the electroactive surface area. Differential pulse voltammetry delivered linear ranges of 0.006–65.0 μM (rutin), 0.05–70.0 μM (quercetin), and 0.02–50.0 μM (baicalin), with detection limits of 3.7, 17.3, and 6.3 nM, respectively. The sensor maintained consistent responses over 15 days and exhibited reliable selectivity against common interferents. Recovery studies in Sophora japonica, onion, and Scutellaria baicalensis extracts correlated with UV–Vis reference data, illustrating how coupling conducting polymers with redox-active nanoparticles can modulate interfacial electron-transfer pathways for targeted electrochemical sensing. Download: Download high-res image (354KB) Download: Download full-size image
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