Arabian Journal of Chemistry
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2024
·
IF 5.3
Xiaohai Chen,Fengsheng Hong,Hualu Wu,Yuxin Shen,Hailun Xia,Ren-ai Xu,Lu Shi
The primary objective of this study was to investigate the effects of baicalein and fangchinoline on the metabolism of abemaciclib. We hypothesized that these two natural compounds could significantly affect the metabolism of abemaciclib by inhibiting the activity of the CYP3A4 enzyme, thus potentially increasing its concentration in the body. In vitro , rat liver microsomes (RLM) and human liver microsomes (HLM) were employed to explore the inhibitory effects and mechanisms of baicalein and fangchinoline on abemaciclib. In vivo , twelve healthy male Sprague-Dawley (SD) rats were randomly assigned to three groups: Group A (control group), Group B (baicalein), and Group C (fangchinoline). The concentrations of abemaciclib and its metabolite N-desethylabemaciclib (M2) were evaluated using ultra performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS). Finally, molecular docking method was employed to understand the interaction between abemaciclib and baicalein. It was indicated by the in vitro findings that both baicalein and fangchinoline inhibited abemaciclib metabolism in RLM through a mixed mechanism of competitive and non-competitive inhibition pathway. In HLM, baicalein inhibited abemaciclib metabolism by employing a hybrid mechanism of uncompetitive and non-competitive inhibition, while fangchinoline exhibited its inhibition in a competitive manner. In vivo , pharmacokinetic experiments revealed significant increases for AUC (0-t) and AUC (0-∞) of abemaciclib in Group B and Group C when compared to Group A, while the plasma clearance (CLz/F) of abemaciclib exhibited significant reductions. Moreover, molecular docking studies showed that both abemaciclib and baicalein docked to the active pocket of CYP3A4. This study demonstrated that the co-administration of baicalein or fangchinoline significantly affected the metabolism of abemaciclib, providing valuable insights for its clinical application.
研究领域:
药理学
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分子生物学
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临床医学
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INTERNATIONAL JOURNAL OF PHARMACEUTICS
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2022
·
IF 6.51
Shuai Liu,Xintao Gao,Yaqi Wang,Jing Wang,Xueju Qi,Kehong Dong,Dayong Shi,Xiaochen Wu,Chuanlong Guo
Silk fibroin (SF) is a natural polymeric biomaterial widely used in the preparation of drug delivery systems . Herein, silk fibroin peptide (SFP) was self-assembled into nanofibers , encapsulated a poorly water-soluble drug baicalein (SFP/BA NFs), and then used to protect against cisplatin-induced acute kidney injury (AKI). Specifically, the SFP/BA NFs significantly enhanced the aqueous dispersity, storage stability, and in vitro antioxidant activity of BA. SFP/BA NFs increased the drug uptake and localization to mitochondria. In vitro results demonstrated that SFP/BA NFs can relieve the cisplatin-induced HK-2 cell damage, and inhibit the cisplatin-induced accumulation of reactive oxygen species (ROS) and mitochondrial membrane potential (MMP) disruption. Mechanism studies demonstrated that SFP/BA NFs may exert nephroprotective effects by inhibiting both the cisplatin-induced DNA damage and the cGAS/STING pathway activation. In vivo results showed that cisplatin treatment resulted in decreased body weight, increased serum creatinine (SCr), and increased blood urea nitrogen (BUN) levels, while SFP/BA NFs reversed the above symptoms. Furthermore, SFP/BA NFs reversed the cisplatin-induced abnormal changes of antioxidant enzymes (e.g., SOD and GSH), and inhibited the cisplatin-induced DNA damage as well as the activation of cGAS/TING. Above all, our results revealed the potential of SFP/BA NFs to protect against cisplatin-induced AKI.
研究领域:
药学
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纳米技术
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生物医学工程
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肾脏生理学
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毒理学
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Journal of Materials Chemistry B
·
2026
·
IF 6.2
Naijun Dong,Chuanxiang Wei,Xiaoshi He,Min Li,Bo Tan,Jiajun Fang,Yuesheng Dong,Yaqin Sun,Zhilong Xiu,Yongxin Qin,Xiaoguang Xu
Chronic diabetic wounds are difficult to treat due to persistent hyperglycemia, oxidative stress, and bacterial infections. Antibiotic therapy is prone to drug resistance, and likewise, photothermal therapy suffers from the risk of thermal injury to surrounding healthy tissues. This study developed a polyacrylic acid (PAA)-based eutectogel (EG) loaded with baicalein (BAI) and MXene nanosheets (BAI–MXene/PAA EG), which integrates multiple functions including anti-inflammatory, antioxidant, antimicrobial and pro-angiogenic properties. MXene generated a low-temperature photothermal effect at ca. 45 °C under near-infrared (NIR) irradiation. The incorporation of baicalein further improved the antibacterial and anti-inflammatory properties of the eutectogel with desired biosafety and biocompatibility. BAI–MXene/PAA EG exhibited excellent antibacterial performance against multidrug-resistant (MDR) E. coli and MDR S. aureus, with bacterial survival rates as low as 0.03% and 0.22%, respectively. In addition, BAI–MXene/PAA EG promoted the proliferation of HUVECs and HaCaT cells and effectively scavenged intracellular ROS. In vivo studies confirmed that BAI–MXene/PAA EG promoted cell proliferation and induced angiogenesis. By combining nanomaterials with active components from traditional Chinese medicine, this research provides new insights into the future development of wound dressings and holds great potential in the clinical treatment of diabetic infected wounds.
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Materials Today Bio
·
2026
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IF 11
Jinfan Yang,Kaihong Shi,Jiachen Wang,Huimin Liu,Yang Zhang,Xiaoyu Guang,Siyuan Wang,Wenxi Lei,Yuxiao Wang,Mingqian Tan,Xiaobin Ma,Hao Wu
Oral ulcers, a prevalent mucosal disorder, are clinically managed by topical corticosteroids and immunosuppressants to alleviate symptoms. However, conventional therapies suffer from suboptimal drug bioavailability, inconsistent efficacy, and potential adverse effects. To address these limitations, using natural carbohydrate polymer hyaluronic acid (HA) with excellent biocompatibility, as the main substrate, we constructed the osmolality-responsive immediate-release microneedles (MNs) platform (GA@BA&Ast MNs) co-loading baicalein (BA) and astaxanthin (Ast) for oral ulcer therapy, which effectively addresses traditional treatment bottlenecks via responsive immediate-release and efficient absorption. The platform's core innovation lies in its dynamically controllable release mechanism, which is triggered specifically by the oral microenvironment. Its osmolality-responsive mechanism, relying on HA-Ca 2+ dynamic coordination network dissociation in oral fluid, enables rapid disintegration and delivery speed superior to conventional microneedles, with good mechanical strength for irritation-free mucosal penetration and 85.3%/87.1% cumulative BA/Ast release within 20 min. In the rat model, GA@BA&Ast MNs significantly accelerated ulcer healing, increased collagen deposition and VEGF expression by 41.22% and 47.05%, and exerted complementary antibacterial, anti-inflammatory, and ROS scavenging effects by promoting epithelial migration and angiogenesis. This responsive MNs platform overcomes the limitations of hydrophobic drug delivery, providing a promising universal strategy for localized orofacial diseases, such as oral ulcers, oral fibrosis, and oral cancer. Download: Download high-res image (346KB) Download: Download full-size image
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Chinese Medicine
·
2026
·Vol. 21
·期 1
·138
·
IF 7.4
Lu Yao,Rong Xinqian,Wei Lini,Yang Jingwen,Zhang Kaiqi,Tan Yong,Zhao Ning,He Xiaojuan,Lu Cheng,Li Li
Background Allergic asthma (AA) may result in repeated episodes of chest constriction and coughing. In its most serious manifestations, it can cause death by asphyxiation. Currently, no efficacious therapeutic interventions exist to avert or counteract these serious outcomes. Baicalein (BAI) is a core quality marker of the traditional Chinese medicine Scutellaria baicalensis , but the mechanism of its oral action remains unclear. Objective Assess the therapeutic efficacy of BAI in AA mice models and investigate its mechanism of action. Study design and methods Evaluate the efficacy of BAI on ovalbumin-induced AA mice. To assess alterations in the pulmonary and gut microbial communities, 16S rRNA sequencing was employed. The integrity and restoration of the lung and intestinal epithelial lining were evaluated via immunohistochemistry. Furthermore, gas chromatography–mass spectrometry quantified fecal levels of short-chain fatty acids (SCFAs) in AA mice, and flow cytometry was used to analyze the content of ILC2 cells in colon tissue. Finally, the role of beneficial bacteria and their metabolites in inhibiting AA was further confirmed through fecal microbiota transplantation (FMT). Results Oral BAI effectively alleviated AA-related lung epithelial damage and microbiota dysbiosis, while elevating the production of the tight junction proteins. Moreover, BAI mitigated colonic epithelial damage, inhibited ILC2s activation in the colon, enriched the abundance of gut probiotics capable of producing SCFAs, especially Akkermansia muciniphila (A. muciniphila) , and increased the content of SCFAs such as propionic acid in feces. The FMT experiment conducted after gavage with broad-spectrum antibiotics confirmed that BAI mediated reversal of microbial dysbiosis plays a key role in the treatment of AA, significantly increasing the expression of GPR41 mRNA in colon tissue and inhibiting the activation of ILC2s. Conclusion The potential prebiotic BAI mitigates AA via targeting A. muciniphila and its metabolites, which consequently inhibits epithelial damage and type 2 immune activation. Graphical
The alternative text for this image may have been generated using AI.
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ANALYTICAL AND BIOANALYTICAL CHEMISTRY
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2014
·Vol. 407
·期 2
·509-519
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IF 3.578
He Hongliang,Gu Xiaoli,Shi Liying,Hong Junli,Zhang Hongjuan,Gao Yankun,Du Shuhu,Chen Lina
Highly selective molecularly imprinted mesoporous silica polymer (SBA-15@MIP) for baicalein (BAI) extraction was synthesized using a surface molecular imprinting technique on the SBA-15 supporter. Computational simulation was used to predict the optimal functional monomer for the rational design of SBA-15@MIP. Meanwhile, high adsorption capacity was obtained when a suitable yield of molecularly imprinted polymers (MIPs) layer was grafted onto the surface of SBA-15. Characterization and performance tests of the obtained polymer revealed that SBA-15@MIP possessed a highly ordered mesoporous structure, reached saturated adsorption within 60 min, and exhibited higher sorption capacity to the target molecule BAI compared with non-imprinted mesoporous silica polymer (SBA-15@NIP) and SBA-15. Finally, SBA-15@MIP was successfully applied to solid-phase extraction (SPE) coupled with high-performance liquid chromatography and ultraviolet detection (HPLC-UV) for the determination of trace BAI in plasma samples. Mean recoveries of BAI through the molecularly imprinted solid-phase extraction (MISPE) sorbent, non-imprinted solid-phase extraction (NISPE) sorbent, and SBA-15 solid-phase extraction (SBA-15-SPE) sorbent were 94.4, 22.7, and 10.7 %, respectively, and the relative standard deviations were 2.9, 2.6, and 3.6 %, respectively. These results reveal that SBA-15@MIP as a SPE sorbent has good applicability to selectively separate and enrich trace BAI from complex samples.
Synthesis procedure of SBA-15@MIP
研究领域:
分析化学
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材料科学
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CURRENT ISSUES IN MOLECULAR BIOLOGY
·
2025
·Vol. 47
·期 6
·450
·
IF 3
Qiming Miao,Lu Sun,Jiayuan Wu,Xinyue Zhu,Juer Liu,Roger Ruan,Guangwei Huang,Shengquan Mi,Yanling Cheng
The advancement of modern lifestyles has precipitated excessive consumption of energy-dense foods, driving the escalating global burden of lipid metabolism dysregulation-related pathologies—including obesity, type 2 diabetes mellitus (T2DM), non-alcoholic fatty liver disease (NAFLD), and cardiovascular disorders—which collectively pose a formidable challenge to global public health systems. The almond hull, as a by-product of almond processing, is rich in polyphenolic compounds with demonstrated antioxidant, anti-inflammatory, and lipid-lowering potential, though its precise hypo-lipidemic mechanisms remain elusive. In this study, polyphenols were extracted from almond hulls using 50% ethanol with ultrasound-assisted extraction, followed by preliminary purification via solvent partitioning. The ethyl acetate fraction was analyzed by liquid chromatography–mass spectrometry (LC-MS). Network pharmacology and molecular docking were employed to investigate the interactions between key bioactive constituents (e.g., quercetin, baicalein, and kaempferol) and targets in lipid metabolism-related pathways. Molecular dynamics (MD) simulations further evaluated the stability of the lowest-energy complexes. Results revealed that the ethyl acetate fraction exhibited potent pancreatic lipase inhibitory activity (IC50 = 204.2 µg/mL). At 0.1 mg/mL after 24 h treatment, it significantly reduced free fatty acids (FFAs)-induced intracellular triglyceride accumulation (p< 0.01) and enhanced cellular antioxidant capacity. Network pharmacology and in vitro studies suggest almond hull extract modulates PI3K-AKT signaling and improves insulin resistance, demonstrating lipid-lowering effects. These findings support its potential in functional foods and pharmaceuticals, though further in vivo validation and mechanistic investigations are required.
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INTERNATIONAL JOURNAL OF PHARMACEUTICS
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2025
·
IF 5.2
Xue Zhou,Ning Wang,Bin Zhao,Ziquan Liu,Pei Yu
Acute kidney injury (AKI) is characterized by high morbidity and mortality globally and serves as an independent risk factor for chronic kidney disease. Oxidative stress is the main pathogenic mechanism leading to acute kidney injury (AKI) and subsequent renal failure, which is characterized by excessive reactive oxygen species (ROS) and mitochondrial dysfunction. Treatment options for AKI remain supportive care, it is urgent to develop more viable therapeutic strategies. In this study, we engineered a nanodrug delivery system aiming to achieve precise treatment of AKI. The nanocarriers (Apt-NS) exhibited excellent serum stability and biocompatibility and were capable of specifically recognizing AKI renal tubular cells. Apt-NS were loaded with baicalein (BAI) to form a nanodrug delivery system (Apt-NS-BAI). In comparison to the BAI, Apt-NS-BAI demonstrated more pronounced effects in improving cell viability, scavenging ROS and anti-apoptosis. Simultaneously, in vivo animal experiments also confirmed that Apt-NS-BAI could recognize the injury site and exert biological functions of anti-apoptosis and alleviating renal damage. Overall, this study successfully constructed a nanodrug delivery system with the ability to target AKI renal tubular cells, enabling accurate and efficient delivery of baicalein to injury site and exerting protective functions against oxidative stress. This research offers novel insights into the precision treatment of AKI and contributes to the acceleration of the application of nanotechnology in kidney diseases.
研究领域:
药理学
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肾脏病学
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纳米医学
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BME Frontiers
·
2026
·
IF 9.1
Zengfeng Guo,Ningfeng Zhang,Junshen Huang,Wang Zhang,Yawei Hu,Shaochu Chen,Ming Gong,Jianhua Zhou,Jiancheng Yang,Jiawen Wu
Objective: This study aimed to investigate the protective effects and underlying mechanisms of baicalein against iron overload-induced osteoblast dysfunction and bone loss. Impact Statement: This research is the first to demonstrate that baicalein, a natural flavonoid, functions as a dual-action agent combining iron chelation and antioxidation to prevent iron overload-induced ferroptosis in osteoblasts, offering a novel therapeutic strategy for iron overload-related osteoporosis. Introduction: Iron overload contributes to osteoblast damage and osteoporosis through ferroptosis, an iron-dependent cell death pathway. Current treatments fail to simultaneously address iron accumulation and bone loss, highlighting the need for effective dual-function therapies. Methods: Using iron dextran-treated MC3T3-E1 osteoblasts and a murine iron overload model, we assessed the effects of baicalein on cell viability, osteogenic differentiation, ferroptosis markers, and the nuclear factor erythroid 2-related factor 2 (Nrf2)/glutathione peroxidase 4 (GPX4) pathway via biochemical assays, Western blot, and micro-computed tomography. Genetic and pharmacological inhibition of Nrf2 were applied to validate the mechanism. Results: Baicalein chelated iron, scavenged reactive oxygen species, and suppressed ferroptosis in osteoblasts, restoring differentiation under iron overload. It activated Nrf2 nuclear translocation and upregulated GPX4/solute carrier family 7-member 11 (SLC7A11) expression. In mice, baicalein reduced iron deposition, oxidative stress, and bone loss, and these effects were abolished by Nrf2 inhibition. Conclusion: Baicalein alleviates iron overload-induced osteoblast ferroptosis and osteoporosis by activating the Nrf2/GPX4 pathway, supporting its clinical potential as a therapeutic agent for iron-related bone disorders.
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CURRENT MEDICINAL CHEMISTRY
·
2024
·Vol. 32
·期 30
·6603-6621
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IF 3.5
Junyan Liu,Shanshan Guo,Junhua Gong,Lue Cheng,Jiefu Luo,Mingxiang Cheng,Shengwei Li,Jianping Gong,Degong Jia
BackgroundThe complex etiology of Ischemia-Reperfusion Injury (IRI) induced by liver transplantation (LT) and the “one-target-focused” method limit the development of effective therapeutic interventions. We aimed to reveal the specific active ingredients and mechanisms involved in the Chinese herb Scutellaria baicalensis Georgi (SBG) in alleviating IRI in LT.MethodsThe active ingredients and potential macromolecular targets of SBG were screened through related databases. The differentially expressed genes of LT were obtained from GSE151648. The protein-protein interaction network was constructed by the STRING database, and Cytoscape 3.7.1 was used to construct a compound-target-disease network. GO and KEGG enrichment analyses were performed on the DAVID database. Finally, the main active components of SBG and the corresponding mechanisms were verified in a donation after circulatory death (DCD) rat LT model.ResultsThirty-two active ingredients of SBG and their targets were identified, and a total of 38 intersection targets were obtained. GO function and KEGG pathway enrichment analyses demonstrated that the plasma membrane and its components play an important role. Molecular docking showed baicalein, the core component of SBG, had a strong binding ability to all hub targets. Next, in DCD rats, baicalein was proven to improve liver function, alleviate pathological injury and apoptosis, and increase the survival rate. Baicalein also significantly affected the expression of 7 hub genes. Furthermore, baicalein could inhibit ferroptosis by inhibiting phospholipid peroxidation.ConclusionBaicalein, the main component of SBG, could alleviate IRI, affect the expression of hub genes, and inhibit ferroptosis in LT.
研究领域:
药理学
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肝胆外科学
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分子生物学
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中医药学
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移植免疫学
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细胞死亡机制
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药物代谢
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TOXICOLOGY AND APPLIED PHARMACOLOGY
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2021
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IF 4.219
Huilong Xiang,Huan Lei,Ziyuan Liu,Yongjie Liu,Yang Li,Yinsheng Qiu,Lingyun Xu
Oxidative stress and inflammation in kidney are the main causes for hyperuricemic nephropathy (HN). Baicalin and baicalein , two flavonoids , have anti-inflammatory and anti-oxidative effects and they are interconvertible in the body. In this study, both baicalin and baicalein were administered by intragastric administration (i.g.) or intraperitoneal injection (i.p.) at the dose of 50 mg kg −1 , once a day for 15 consecutive days to HN mice, a model established by i.g. of yeast extract combined with i.p. of potassium oxonate . In HN mice, baicalin and baicalein reduced serum uric acid (SUA) levels and protected kidneys by anti-inflammatory and anti-oxidative effects. Mechanistically, the effect of baicalin and baicalein on reducing SUA levels might due to their inhibitory effect on xanthine oxidase (XO) activity in vivo and in vitro . Furthermore, the mechanisms of baicalin and baicalein against HN were analyzed with network pharmacology and molecular docking technology . The network pharmacology indicated that the protective effects of baicalin and baicalein against HN were mainly related to their down-regulating effects on TLRs , NF-κB, MAPK, PI3K/AKT and NOD-like receptor signaling pathways. Molecular docking indicated high binding affinity of baicalin/baicalein to targets such as AKT1 and MAPK1 . In summary, baicalin and baicalein are promising drug candidates for the treatment of HN by inhibiting XO activity, reducing inflammation and cell apoptosis through down-regulating TLRs/NLRP3/NF-κB, MAPK, PI3K/AKT/NF-κB pathways.
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CANCER SCIENCE
·
2020
·Vol. 111
·期 10
·3802-3812
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IF 4.966
Xiaolong Zhang,Qinli Ruan,Yiqian Zhai,Dandan Lu,Chen Li,Yahan Fu,Zihui Zheng,Ying Song,Jun Guo
Baicalein, a flavonoid phytochemical, has been shown to be effective as an anti-metastatic agent for various cancers, especially for non-small-cell lung cancer (NSCLC). However, the underlying mechanism of how baicalein targets cellular processes during NSCLC cell invasion and metastasis remains elusive. In this study, we found that non-cytotoxic concentrations of baicalein still retained anti-dissemination activity both in vitro and in vivo. Using a genetic encoding tension probe based on Förster resonance energy transfer (FRET) theory, baicalein was shown to significantly decrease ezrin tension by downregulating cellular ezrin S -nitrosylation (SNO) levels in NSCLC cells in the inflammatory microenvironment. Decreased ezrin tension inhibited the formation of an aggressive phenotype of NSCLC cell and leader cell in collective migration, and subsequently suppressed NSCLC dissemination. Baicalein restrained SNO-mediated ezrin tension by decreasing iNOS expression levels. Overall this study demonstrates the novel mechanism used by baicalein to suppress NSCLC invasion and metastasis from a mechanopharmacology perspective and illustrates a new direction for drug development.
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