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Frontiers in Bioengineering and Biotechnology · 2022 · IF 6.064

Multifunctional Baicalin-Modified Contact Lens for Preventing Infection, Regulating the Ocular Surface Microenvironment and Promoting Corneal Repair

Yue Luo,Luying Liu,Yuzhen Liao,Ping Yang,Xiaoqi Liu,Lei Lu,Jiang Chen,Chao Qu

Corneal injury inevitably leads to disruption of the ocular surface microenvironment, which is closely associated with delayed epithelial cell repair and the development of infection. Recently, drug-loaded therapeutic contact lenses have emerged as a new approach to treating corneal injury due to their advantages of relieving pain, promoting corneal repair, and preventing infection. However, few therapeutic contact lenses could modulate the ocular surface’s inflammation and oxidative stress microenvironment. To address this, in this study, we covalently immobilized multifunctional baicalin (BCL), a flavon molecular with anti-inflammatory, anti-oxidative stress, and antibacterial capabilities, onto the surface of the contact lens. The BCL-modified contact lens showed excellent optical properties, powerful antibacterial properties, and non-toxicity to endothelial cells. Furthermore, the BCL-modified contact lens could significantly modulate the ocular surface microenvironment, including inhibition of macrophage aggregation and resistance to epithelium damage caused by oxidative stress. In animal models, BCL-modified corneal contact lens effectively promoted corneal epithelial cells repair. These excellent properties suggested that multifunctional BCL molecules had great application potential in the surface engineering of ophthalmic medical materials.

CAS / MDL: 21967-41-9 124-09-4
研究领域: 眼科学 · 药学 · 生物医学工程
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Results in Chemistry · 2022 · IF 0

Detection of Baicalin capsule and Scutellariae Radix based on nitrogen-doped carbon dots as a fluorescence probe

Weiqing Cheng,Shuihua Wu,Daifang Wang,Yongming Lou

Nitrogen-doped fluorescent carbon dots (N-CDs) were prepared via hydrothermal synthesis method using citric acid and ethylenediamine as raw materials. The synthesized N-CDs were characterized by transmission electron microscopy (TEM) and multi-spectroscopic techniques. A fluorescent sensor based on the inner filter effect (IFE) was successfully established using synthesized carbon dots to detect the content of Baicalin in Baicalin capsule and the quality of Scutellariae Radix. The Baicalin linear range of the method is 1.6–72 μg·mL −1 (r = 0.9992), the detection limit is 1.0 μg·mL −1 (3-foldσ), and the precision was 0.2%. Furthermore, the N-CDs probe was used to evaluate quality of Scutellariae Radix.

CAS / MDL: 7440-70-2 107-15-3
研究领域: 药学 · 分析化学
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COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS · 2023 · IF 5.2

Ultra-sensitive Baicalin electrochemical sensor based on γ-cyclodextrin supramole derived N,Zn double-doped carbon nanosphere

Mengting Zhang,Xuejia Huang,Jiejun Li,Yuhong Li,Pengcheng Zhao,Junjie Fei,Yixi Xie

Baicalin (Bn) is the main component of the Chinese patent medicine Baicalin Tablet which is used for the auxiliary treatment of acute, chronic hepatitis and persistent hepatitis. Herein, an ultrasensitive electrochemical sensor was manufactured based on the nitrogen and zinc double doped carbon nanospheres(ZnN-CNS) derived from γ-cyclodextrin self-assembled supermolecules with ZnCl 2 . The sensing nanomaterials were characterized and investigated by X-ray diffraction (XRD), transmission electron microscopy (TEM), raman spectroscopy (RS), and scanning electron microscopy (SEM), etc. Under the optimized optimal environment, the linear detection range of the prepared sensor for Bn was ranged from 1 × 10 −8 to 7.5 × 10 −7 M, where the LOD was 7.17 × 10 −8 M with a sensitivity of 220 A/M. Good accuracy and desirable recovery results for the detection of Bn in real samples (Bear bile scutellaria eye drops and Shuanghuanglian oral liquid) were also observed. This work provides a new idea about the detection of Bn as well as the application of novel binary doped carbon materials .

研究领域: 分析化学 · 纳米技术 · 药学 · 材料科学
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JOURNAL OF NANOBIOTECHNOLOGY · 2024 ·Vol. 22 ·期 1 ·1-19 · IF 10.6

Baicalin nanodelivery system based on functionalized metal-organic framework for targeted therapy of osteoarthritis by modulating macrophage polarization

Huang Lanli,Yao Yi,Ruan Zhuren,Zhang Shengqing,Feng Xianjing,Lu Chun,Zhao Jinmin,Yin Feiying,Cao Cunwei,Zheng Li

Intra-articular drugs used to treat osteoarthritis (OA) often suffer from poor pharmacokinetics and stability. Nano-platforms as drug delivery systems for drug delivery are promising for OA therapy. In this study, we reported an M1 macrophage-targeted delivery system Bai@FA-UIO-66-NH2 based on folic acid (FA) -modified metal-organic framework (MOF) loaded with baicalin (Bai) as antioxidant agent for OA therapy. With outstanding biocompatibility and high drug loading efficiency, Bai@FA-UIO-66-NH2 could be specifically uptaken by LPS-induced macrophages to serve as a potent ROS scavenger, gradually releasing Bai at the subcellular level to reduce ROS production, modulate macrophage polarization to M2, leading to alleviation of synovial inflammation in OA joints. The synergistic effect of Bai@FA-UIO-66-NH2 on macrophage polarization and ROS scavenging significantly improved the therapeutic efficacy of OA, which may provide a new insight into the design of OA precision therapy.

研究领域: 药理学 · 纳米技术 · 药物递送系统 · 免疫学 · 骨科
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CELLULOSE · 2020 ·Vol. 27 ·期 8 ·4831-4846 · IF 4.21

Advantages of Scutellaria baicalensis extracts over just baicalin in the ultrasonically assisted multi-functional treatment of linen fabrics

Li Huimin,Li Zhengrui,Liu Yixin,Li Minghua

Abstract Recently plant extracts with intrinsic properties of green, safe and eco-friendly were more often integrated with textiles to endow the fabric with multi-functions such as anti-microbial, anti-oxidation and anti-ultraviolet. Therefore, it is worthwhile to study the role of active constituents in plant extracts on the functionalization of textiles. Herein, Scutellaria baicalensis (chinese skullcap) extracts (SBE) and its main active ingredient, baicalin, were effectively combined with linen fabric by means of impregnation and ultrasonic treatment respectively. The treated linen fabrics were characterized by SEM, FTIR, XRD, TGA, DTG analysis and the relevant functions such as anti-microbial activity, antioxidant activity and ultraviolet protection ability as well as durability of functionalities were also comparatively assessed. It was found that even with the same content of baicalin, the corresponding functions of the linen fabric treated by SBE are obviously better than treated by baicalin. The advantages of the SBE over just baicalin on the functionalization of linen fabric was analyzed and verified by experiments. The conclusion of this work will guide the quantitative addition of plant extracts on textile functional treatment. Graphic abstract

研究领域: 纺织科学 · 植物化学 · 材料科学
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COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS · 2026 · IF 5.4

Concentration-dependent burst release of baicalin from a borate ester-based dynamic hydrogel for enhanced infected wound healing

Dong Zhang,Jing Gao,Xu Cheng,Ruidan Zhang,Jianbo Zhang,Gengchao Kuang,Huan Lu,Jincheng Zhu,Yamin Qiao,Sijia Ge,Ning Yang

A versatile BCAP hydrogel was developed for in‑situ solubilization and controlled delivery of poorly‑soluble baicalin. • Reversible borate ester bonds afford high baicalin loading and unique concentration‑dependent burst release. • BCAP hydrogel exerts favorable antibacterial and hemostatic effects, accelerating infected wound healing. • This strategy addresses the solubility bottleneck of natural baicalin and inspires the design of advanced wound dressings. Infectious wounds present a formidable clinical challenge characterized by persistent bacterial colonization, excessive hemorrhage, and impaired healing. Baicalin (BA), a natural flavonoid with potent antibacterial and anti-inflammatory activities, is severely constrained by its negligible aqueous solubility. Herein, a multifunctional dynamic hydrogel (BCAP) was engineered via free radical polymerization utilizing polyethyleneimine (PEI), acrylamide (AM), and 3-carboxyphenylboronic acid (CPBA) to facilitate the in-situ solubilization and controlled delivery of BA. The BCAP hydrogel achieves high-load BA integration through reversible borate ester linkages between CPBA and the catechol moieties of BA, supported by a hydrophilic PEI/AM interpenetrating network. Notably, the system exhibits a unique concentration-dependent burst release profile, enabling an immediate therapeutic dosage critical for acute infection management. Both in vitro and in vivo evaluations confirm that the BCAP hydrogel possesses superior antibacterial efficacy, rapid hemostatic kinetics, and the capacity to accelerate wound closure by down-regulating pro-inflammatory cytokines and stimulating angiogenesis. This study offers a synergistic molecular-engineering strategy to overcome the solubility barriers of natural bioactive compounds while providing a high-performance multifunctional dressing for infectious wound management. Download: Download high-res image (118KB) Download: Download full-size image

CAS / MDL: 1898-66-4 28752-68-3
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PHYTOMEDICINE · 2026 · IF 11.3

Baicalin targets AMPKα1 to alleviate microglial inflammation by increasing the protein stability of HDAC1 in hypoxic–ischemic encephalopathy

Rui Yin,Lu He,Liangli Dai,Ling Chen,Tao Liang,Jinli Han,Juan Chen

Background Hypoxic–ischemic encephalopathy (HIE) is a serious neonatal neurological disorder in which microglia-mediated acute neuroinflammation serves as a critical driver of disease progression. Our previous work revealed that H3K9 lactylation-driven microglial M1 polarization promotes neuroinflammation as a key mechanism in HIE. Baicalin, a natural compound isolated from the traditional Chinese herb Scutellaria baicalensis , is well known for its anti-inflammatory effect, but whether it can treat HIE through this anti-inflammatory effect remains unclear. Purpose This study aimed to determine whether baicalin can inhibit H3K9 lactylation-mediated microglial M1 polarization and neuroinflammation in HIE. Methods In vivo, an HIE rat model was established in which rats were treated with intraperitoneal injections of baicalin. In vitro, an oxygen‒glucose deprivation model was constructed using BV2 microglia. Network pharmacology and molecular docking were employed to predict and validate the potential targets of baicalin, after which functional assays were performed. Co-immunoprecipitation combined with mass spectrometry was further used to explore the underlying molecular mechanisms. Results Through network pharmacology analysis, molecular docking and validation experiments, we revealed that baicalin exerts its anti-inflammatory effects via the activation of adenosine 5′-monophosphate-activated protein kinase α subunit 1 (AMPKα1). Further co-immunoprecipitation and mass spectrometry analyses revealed that AMPKα1 activation promotes the phosphorylation of histone deacetylase 1 (HDAC1), a key delactylase, thus inhibiting the degradation of HDAC1 mediated by the E3 ligase ubiquitin protein ligase E3A (UBE3A). Finally, baicalin increases HDAC1 protein levels to inhibit H3K9 lactylation-mediated microglial M1 polarization via targeting AMPKα1. Conclusion These findings suggest that, when administered at an early stage after HIE, baicalin may contribute to the attenuation of HIE pathology, at least in part by increasing HDAC1 stability through AMPKα1- and UBE3A-mediated “phosphorylation–ubiquitination hierarchical regulation”, thereby reducing H3K9 lactylation and suppressing microglial M1 polarization. Download: Download high-res image (186KB) Download: Download full-size image

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RENAL FAILURE · 2026 · IF 3.8

Baicalin ameliorates podocyte injury and renal function impairment in idiopathic membranous nephropathy by inhibiting the AGE/RAGE signaling

Chengli Lou,Yijing Zhou,Bo Feng,Xiaoping Fan,Xiuqin Xu,Pingxin Hu,Xiangjing Wang

Idiopathic membranous nephropathy (IMN) is an autoimmune glomerular disease. Current immunosuppressive therapies often cause side effects and high recurrence rates, highlighting the need for new treatments. Baicalin (BAI), a flavonoid isolated from Scutellaria baicalensis, has anti-inflammatory and antioxidant properties. This study examined effects of BAI on IMN using in vitro mouse podocyte clone-5 (MPC-5) cells treated with zymosan-activated serum (ZAS) and in vivo mouse models induced with cationic bovine serum albumin (BSA). Treatments included the BAI and advanced glycation end products/receptor for advanced glycation end products (AGE/RAGE) agonist, advanced glycation end products - bovine serum albumin (AGE-BSA). Assessments included cell viability, apoptosis, reactive oxygen species (ROS), inflammatory cytokines, oxidative stress markers, renal function, and histopathology. Potential targets and pathways involved in BAI’s effect on IMN were identified using network pharmacology. Compared to the ZAS-induced MPC-5 cell group, BAI increased cell viability and reduced apoptosis in injured cells. Meantime, BAI significantly reduced the release of pro-inflammatory cytokines tumor necrosis factor α, monocyte chemotactic protein 1, and interleukin 6 and enhanced antioxidant capacity by increasing total superoxide dismutase levels while simultaneously decreasing oxidative stress markers ROS, malondialdehyde, and lactate dehydrogenase in IMN cell models. Similarly, BAI exhibited anti-inflammatory and anti-oxidative effects in an in vitro IMN model and protected renal function in IMN mice with IMN. In addition, BAI downregulated AGE and RAGE in both IMN cell models and mice, and reduced CD68 levels in IMN mice. However, the activation of the AGE/RAGE pathway by AGE-BSA weakened the protective effects of BAI in these IMN models. Collectively, BAI mitigated inflammation and oxidative stress in IMN by repressing the AGE/RAGE pathway, suggesting its potential as a promising therapeutic agent for IMN.

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PHYTOMEDICINE · 2025 · IF 8.3

Natural Baicalin Compound Microneedle: A Novel Therapeutic Strategy for Critical Limb Ischemia Through the Promotion of Muscle Differentiation

Haiya Ni,Zhiwei Zhao,Jun Wang,Yi Cheng,Jianing Liu,Ling Zhang,Guangjin Gao,Ziyu Wu,Ye Yuan,Min Zhou

Critical limb ischemia (CLI) results from inadequate blood perfusion in the extremities, leading to accelerated muscle cell apoptosis in mild cases and lower limb claudication in severe cases. It can therefore significantly reduce the quality of life of patients. In this study, baicalin (BA), a representative flavonoid, is shown to induce myogenic differentiation thus alleviating CLI. The underlying mechanism of action of BA primarily involves the direct activation of the Wnt/β-catenin signaling pathway and the drug metabolism enzyme cytochrome P450 (Cyp1a1) in muscle cells. To address the challenging aqueous solubility of flavonoids for in vivo applications, we designed an innovative composite microneedle patch (GEL+PUE+BA MNs). This delivery strategy not only overcomes the solubility limitations of flavonoids in vivo but also promotes the repair of ischemic muscle through localized intervention. It efficiently delivers BA to the ischemic site, stimulates the associated muscle cells, and induces their differentiation into skeletal muscle. This process markedly reduces the apoptotic cells and muscle loss in the lower extremities. Our study underscores the significant therapeutic effects of GEL+PUE+BA MNs as a biomaterial for treating hindlimb ischemia and highlights its considerable potential in managing CLI.

CAS / MDL: 21967-41-9 9000-70-8
研究领域: 生物医学工程 · 药理学 · 再生医学 · 药物递送系统 · 分子生物学
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APPLIED SURFACE SCIENCE · 2025 · IF 6.9

Effective flotation separation of dolomite and apatite utilizing baicalin as a green depressant: a mechanistic and experimental study

Pan Yu,Lingpan Du,Menglai Wang,Fengting Zhao,Runzhe Liu,Xiang Gong,Hongyu Lu,Fuhua Luo,Qi Zuo,Shuming Wen,Shaojun Bai

To address the challenge of separating dolomite from apatite via flotation, this research firstly employed Baicalin (BA) as an environment-friendly depressant and examined the underlying depression mechanism on apatite and dolomite in a sodium oleate (NaOL) collector system. Micro-flotation findings demonstrated effective separation of apatite and dolomite under conditions of 50 mg/L BA and 120 mg/L NaOL at pH 11.0. Zeta potential, adsorption capacity, FT-IR, and SEM-EDS analyses indicated that the dolomite surface exhibited a greater affinity for BA adsorption. Contact angle measurements showed that BA prominently reduced the surface hydrophobicity of dolomite while having a minimal impact on apatite’s surface hydrophobicity. XPS analysis confirmed that BA adsorption on the dolomite surface mainly involved chemisorption between –COO − groups and Ca and Mg sites, whereas a weaker physical adsorption occurred on the apatite surface. Molecular dynamics simulations (MDS) analysis showed that BA exhibited a greater affinity on the dolomite surface relative to apatite, thereby rendering the dolomite surface more hydrophilic than apatite. This study presents a novel methodology for the efficient and sustainable removal of dolomite from apatite, thereby advancing the theoretical understanding of flotation separation in apatite-dolomite systems.

CAS / MDL: 21967-41-9
研究领域: 矿物加工 · 浮选化学 · 表面科学 · 环境工程 · 可持续采矿
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APPLIED SURFACE SCIENCE · 2025 · IF 6.9

Synergistic depression of copper-activated pyrite by Fe2+/baicalin system: a novel strategy for selective Zn-S flotation

Cuihuan Lv,Jinpeng Cai,Guohui Wang,Jiuxiu Chen,Hao Lai,Peilun Shen,Dianwen Liu

Organic depressants often exhibit low selectivity at high dosages, and introduce risks of concentrate dewatering. The combined depressants composed of inorganic and organic substances can significantly reduce reliance on organic depressant dosage, providing a promising solution to this challenge. In order to achieve highly efficient separation of sphalerite and pyrite in the CuSO 4 -butyl xanthate (PBX) flotation system, the combined depressant Fe 2+ / baicalin (BCL) was innovatively employed to inhibit copper-activated pyrite. The flotation tests indicate that compared with the single depressant BCL, the combined depressant Fe 2+ /BCL demonstrates superior selective inhibitory effects on copper-activated pyrite. For artificially mixed ores, a zinc concentrate is obtained with a zinc grade of 62.33 % and a zinc recovery of 93.86 % when the combined depressant of 10 mg/L Fe 2+ and 5 mg/L BCL are used, and the separation efficiency is significantly improved from 40.66 to 79.69 %. Adsorption characteristic studies indicated that BCL exhibits stronger affinity for copper-activated pyrite than for sphalerite. The introduced Fe 2+ provide additional active sites, thereby enhancing the depression effect on copper-activated pyrite. Following Fe 2+ /BCL modification, the adsorption of PBX on copper-activated pyrite was hindered, while having no substantial impact of that on sphalerite, which is also confirmed by molecular dynamics simulations. Therefore, the combined depressant Fe 2+ /BCL markedly widened the hydrophobicity difference between sphalerite and pyrite, creating the potential for their effective separation.

研究领域: 矿物加工 · 浮选化学 · 表面化学 · 提取冶金
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CARBOHYDRATE POLYMERS · 2025 · IF 12.5

Mannose-modified Prunus persica kernel protein nanoparticles loading baicalin coated with Lycium barbarum polysaccharide for ulcerative colitis treatment

Chunxiao Tao,Fazhen Luo,Yaxin Wang,Xiaoya Gao,Yuqi Cao,Keke Wang,Yan Xie

Baicalin (Ba) is a promising anti-inflammatory agent for treating ulcerative colitis (UC), but its efficacy is constrained by poor solubility and colon-targeting efficiency. Lycium barbarum polysaccharide (LBP), an anionic polysaccharide, not only restores gut microbiota dysbiosis but also exhibits excellent upper gastrointestinal stability and biocompatibility, making it a candidate for developing colon-targeted carriers. In this paper, the polymeric nanoparticles (Ba@MP/LBP NPs) were constructed using LBP, mannose, and Prunus persica kernel protein (PKP) for targeted delivery of baicalin to enhance its efficacy in UC treatment. The obtained Ba@MP/LBP NPs possessed core-shell spherical morphology, narrow particle-size distribution (∼230 nm), negative surface charge (−33.89 mV), and excellent baicalin encapsulation (94.26 %). With the aid of the LBP coating, Ba@MP/LBP NPs can tolerate upper gastrointestinal disturbances and transport Ba@MP NPs into colon, thereby facilitating baicalin uptake by inflammatory macrophages via mannose receptor-mediated endocytosis. Furthermore, the LBP coating strengthened Ba@MP NPs' ability to regulate the intestinal flora; hence, Ba@MP/LBP NPs can restore gut microbiota balance while suppressing pro-inflammatory factor secretion and oxidative stress, ultimately alleviating UC. More importantly, Ba@MP/LBP NPs exhibited favorable biosafety. Overall, this work is the first attempt to employ LBP and PKP as colon-targeting carriers, providing a promising nanomedicine for UC therapy.

CAS / MDL: 3458-28-4 599-79-1
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