ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS
·
2018
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IF 3.118
Yichuan Xiao,Jiantao Ye,Ying Zhou,Junjun Huang,Xiawen Liu,Biyun Huang,Liu Zhu,Bo Wu,Genshui Zhang,Yi Cai
AMP-activated protein kinase (AMPK) is a central regulator of multiple metabolic pathways. It has been shown that activation of AMPK could inhibit fibroblast proliferation and extracellular matrix (ECM) accumulation, thereby suppressing cardiac fibrosis. Baicalin , the major component found in skullcap, possesses multiple protective effects on the cardiovascular system. However, little is known about the effect of baicalin on cardiac fibrosis and the molecular mechanism by which baicalin exerts its anti-fibrotic effects has not been investigated. In this study, we revealed that baicalin could inhibit cell proliferation , collagen synthesis , fibronectin (FN) and Connective tissue growth factor (CTGF) protein expression in cardiac fibroblasts induced by angiotensin Ⅱ (Ang Ⅱ). It also ameliorated cardiac fibrosis in rats submitted to abdominal aortic constriction (AAC). Moreover, baicalin inhibited transforming growth factor-β (TGF-β)/Smads signaling pathway stimulated with Ang Ⅱ through activating AMPK. Subsequently, we also demonstrated that baicalin attenuated Ang Ⅱ-induced Smad3 nuclear translocation, and interaction with transcriptional coactivator p300, but promoted the interaction of p300 and AMPK. Taken together, these results provide the first evidence that the effect of baicalin against cardiac fibrosis may be attributed to its regulation on AMPK/TGF-β/Smads signaling, suggesting the therapeutic potential of baicalin on the prevention of cardiac fibrosis and heart failure.
研究领域:
心脏病学
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药理学
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分子生物学
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DOI
PubMed
高影响因子
Evidence-based Complementary and Alternative Medicine
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2018
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IF 2.064
Peng Pang,Ke Zheng,Sizhi Wu,Huachong Xu,Li Deng,Yucong Shi,Xiaoyin Chen
The objective of this study is to investigate the effects of baicalin on controlling the pulmonary infection and improving the prognosis in influenza A virus (IAV) infection. PCR and western blot were used to measure the changes of some key factors in RLRs signaling pathway. MSD electrochemiluminescence was used to measure the expression of pulmonary inflammatory cytokines including IFN-γ, TNF-α, IL-1β, IL-2, IL-4, IL-5, IL-6, IL-10, IL-12p70, and KC/GRO. Flow cytometry was used to detect the proportion of Th1, Th2, Th17, and Treg. The results showed that IAV infection led to low body weight and high viral load and high expression of RIG-I, IRF3, IRF7, and NF-κB mRNA, as well as RIG-I and NF-κB p65 protein. However, baicalin reduced the rate of body weight loss, inhibited virus replication, and downregulated the key factors of the RLRs signaling pathway. Besides, baicalin reduced the high expression inflammatory cytokines in lung and decreased the ratios of Th1/Th2 and Th17/Treg to arouse a brief but not overviolent inflammatory response. Therefore, baicalin activated a balanced host inflammatory response to limit immunopathologic injury, which was helpful to the improvement of clinical and survival outcomes.
研究领域:
药理学
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免疫学
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病毒学
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DOI
PubMed
高影响因子
INTERNATIONAL IMMUNOPHARMACOLOGY
·
2021
·
IF 4.932
Xiaoqi Sun,Xiaotian Wang,Qianqian He,Muqing Zhang,Li Chu,Yang Zhao,Yongchao Wu,Jianping Zhang,Xue Han,Xi Chu,Zhonglin Wu,Shengjiang Guan
Baicalin (BA), a kind of flavonoids compound, comes from Scutellaria baicalensis Georgi (a kind of perennial herb) and has beneficial effects on the cardiovascular system through anti-oxidant, anti-inflammation, and anti-apoptosis actions. However, the therapeutic effects and latent mechanisms of BA on arsenic trioxide (ATO)-induced cardiac toxicity has not been reported. The present research was performed to explore the effects and mechanisms of BA on ATO-induced heart toxicity. Male Kunming mice were treated with ATO (7.5 mg/kg) to induce cardiac toxicity. After the mice received ATO, BA (50 and 100 mg/kg) was administered for estimating its cardioprotective effects. Statistical data demonstrated that BA treatment alleviated electrocardiogram abnormalities and pathological injury caused by ATO. BA could also lead to recovery of CK and LDH activities to normal range and cause a decrease in MDA levels and ROS generation, augmentation of SOD, CAT, and GSH activities. We also found that BA caused a reduction in the expression of proinflammatory cytokines, such as TNF-α and IL-6. Moreover, BA attenuated ATO-induced apoptosis by promoting the expression of Bcl-2 and suppressing the expression of Bax and caspase-3. TUNEL test result demonstrated BA caused impediment of ATO-induced apoptosis. Furthermore, BA treatment suppressed the high expression of TLR4 , NF-κB and P-NF-κB caused by ATO. In conclusion, these results indicate that BA may alleviate ATO-induced cardiac toxicity by restraining oxidative stress, apoptosis, and inflammation, and its mechanism would be associated with the inhibition of the TLR4/NF-κB signaling pathway.
研究领域:
药理学
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毒理学
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心脏病学
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DOI
PubMed
高影响因子
Journal of Functional Foods
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2018
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IF 3.47
Ni Zeng,Guowen Zhang,Xing Hu,Junhui Pan,Zhisheng Zhou,Deming Gong
Suppression of xanthine oxidase (XO) may contribute to control hyperuricemia and gout. In this study, baicalein and baicalin, two dietary flavones, were found to inhibit the formation of uric acid and generation of superoxide anion (O 2 − ) catalysed by XO through interaction with primary amino acid residues located in flavin adenine dinucleotides center of XO. Baicalein or baicalin binding to XO mainly facilitated by hydrophobic interactions and hydrogen bonds resulted in more compact of XO structure. The concentration profiles and pure spectra of the components extracted from highly overlapping spectral signal by multivariate curve resolution–alternating least squares chemometrics algorithm confirmed the formation of complexes and monitored the reaction kinetics process between XO and these flavones. Furthermore, the isobolographic analysis found that baicalein or baicalin exhibited a moderate synergy on the inhibition of XO when it combined with allopurinol as well as the joint use of baicalein and baicalin.
研究领域:
药理学
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生物化学
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医学
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DOI
高影响因子
ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS
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2022
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IF 4.114
Pan Li,Yuwei Chen,Xiumei Ke,Ruoyu Zhang,Ling Zuo,Meng Wang,Zhiwei Chen,Xianqin Luo,Jianwei Wang
Baicalin is a flavonoid compound abundant in multiple edible and medicinal plants such as Scutellaria baicalensis Georgi . In this study, we provide evidence to support the fact that baicalin ameliorates alcohol-induced hepatic steatosis via regulating SREBP1c elicited PNPLA3 competitive binding to ATGL . Results showed that baicalin significantly attenuated the development of metabolic disorders and hepatic steatosis in alcohol-induced rats after four weeks of treatment. It was evident that baicalin treatment significantly normalized the serous contents of hepatic triglyceride (TG), alanine aminotransferase (ALT), and aspartate aminotransferase (AST), and attenuated the increase of hepatic vacuolization and Oil Red O staining area caused by alcohol. Meanwhile, baicalin relieves alcohol-induced hepatic fibrosis by masson staining and RT-qPCR analysis. Mechanistically, alcohol aggravated the nuclear expression of SREBP1c, which contributed to the high expression of PNPLA3 and FASN , thereby enhancing the binding of PNPLA3 to ABHD5 , and indirectly impairing the binding ability between ATGL and ABHD5, ultimately causing a decline in the hydrolysis capacity in liver lipid droplets . As expected, these alcohol-induced pathobolism were reversed by baicalin treatment both in vivo and in vitro . In conclusion, this study has demonstrated that baicalin can protect against alcohol-induced hepatic lipid accumulation by activating hepatic lipolysis via suppressing SREBP1c elicited PNPLA3 competitive binding to ATGL. Baicalin is a promising natural product for preventing alcohol-induced hepatic steatosis.
研究领域:
药理学
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肝病学
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代谢学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
Pharmaceutics
·
2023
·Vol. 15
·期 1
·257
·
IF 5.4
Lixing Xu,Enhe Bai,Yangbo Zhu,Jiayi Qin,Xiao Du,Haiqin Huang
Gastric ulcer is one of the most common gastrointestinal diseases, and natural products have obvious advantages in the treatment of gastrointestinal diseases. Baicalin (Bai) extracted from scutellaria baicalensis exhibits anti-inflammatory, antioxidant, and anti-apoptotic activities. Herein, a pH-responsive sodium alginate/polyaspartate/CaCO3(SA/[email protected]3) in situ hydrogel was established for the oral delivery of Bai. In this study, we detected the gelling properties, mechanical strength, in vitro erosion, and in vitro release behavior of the hydrogels. Meanwhile, the efficiency of Bai/SA/[email protected]3hydrogel on ethanol-induced acute gastric ulcers, acetic acid-induced chronic gastric ulcers, and H2O2-stimulated human gastric epithelial GES-1 cells was explored. The pathological examination revealed that Bai-loaded hydrogel alleviated acute and chronic gastric ulcers. In vivo and in vitro results further confirmed that Bai/SA/[email protected]3in situ hydrogels significantly relieved oxidative stress injury. Moreover, through Western blot assay, Bai/SA/[email protected]3hydrogel was also found to dramatically increase the proteins levels of NRF2, HO-1, and Bcl2, and reduce levels of p-JNK, cleaved-caspase-3 and Bax; through flow cytometry, it was observed to significantly inhibit the H2O2-induced apoptosis of GES-1 cells. Importantly, the Bai/SA/[email protected]3in situ hydrogel system showed better anti-gastric ulcer efficiency than free drug, and could serve as a potential drug delivery system for the clinical treatment of gastric ulcers.Keywords:gastric ulcer;pH-responsive in situ gelation;baicalin;sustained release;oxidative stress
研究领域:
药学
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胃肠病学
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药物递送系统
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生物医学工程
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DOI
PubMed
高影响因子
JOURNAL OF MOLECULAR LIQUIDS
·
2024
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IF 5.3
Xiaoxiao Gu,Dongmei Li,Haoyang Yuan,Cailing Li,Dinghua Yu,Guowei Wang,Shuang Li
Baicalin is a flavonoid compound extracted from the Scutellaria baicalensis plant. It possesses strong free radical scavenging ability and has a wide range of medical applications in antibacterial, anti-inflammatory, and anti-tumor fields. However, its limited solubility in water restricts its application. In this study, we prepared SL-DMEA by the amidation of acidic sophorolipids and N, N-dimethylethanolamine, while SL-TMEAI was synthesized via the quaternization of SL-DMEA with iodomethane. The structures of SL-DMEA and SL-TMEAI were confirmed by 1 H NMR, FT-IR, and Mass spectra. Surface tension and micelle microenvironment indicated that SL-DMEA and SL-TMEAI exhibit superior surface activity. Furthermore, the solubility of baicalin in aqueous solutions containing SL-DMEA and SL-TMEAI was approximately 70 mg/L and 75 mg/L, while it was only 18 mg/L in SL-COOH solution, which were significantly higher than the solubility in pure water (4 mg/L). Similarly, SL-DMEA and SL-TMEAI can enhance the antioxidant activity of baicalin. Specifically, in the SL-TMEAI aqueous solution, the free radical scavenging rate of baicalin was increased by 10 %–20 %. Density functional theory calculations revealed that SL-DMEA and SL-TMEAI formed stable hydrogen bonds with baicalin molecules, which can increase the solubility of baicalin in water and expose the groups that react with free radicals in the solution, thereby enhancing the antioxidant activity. These results demonstrated that SL-DMEA and SL-TMEAI could significantly enhance the solubility and antioxidating of baicalin in water through a hydrotropy mechanism.
研究领域:
生物化学
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药物化学
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材料科学
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DOI
高影响因子
Gastroenterology Research and Practice
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2020
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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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DOI
PubMed
高影响因子
Journal of Cosmetic Dermatology
·
2025
·Vol. 24
·期 2
·e70024
·
IF 2.5
Liang Chen,Fudi Wang,Xiaoyun Hu,Nihong Li,Ying Gao,Fengfeng Xue,Ling Xie,Min Xie
Objective To develop a stable and efficient delivery system for baicalin, a flavonoid with potential antioxidant and antiaging properties, to overcome its limitations in solubility, stability, and skin permeability. Methods Baicalin was encapsulated using ATP synthase molecular motor technology into bio-vesicles derived from yeast/bacillus cell membranes, forming “motor baicalin” (MB). The liposome baicalin (LB), baicalin raw material (BRM), and bio-vesicles were used for comparison. The stability, transdermal penetration, and antioxidant activity of MB, LB, BRM, and bio-vesicles were evaluated through in vitro and in vivo tests. Results MB formed a stable core-shell structure, significantly enhancing the water solubility and long-term stability of baicalin. The tests confirmed superior transdermal penetration and antioxidant activity of MB, evidenced by increased expression of SOD, CAT, and GSH-Px enzymes and improved cell proliferation and migration. Clinical trials demonstrated significant reductions in wrinkle depth and improvements in skin elasticity. Conclusion This study presents a promising approach to improving the stability and transdermal delivery of baicalin. MB showcases potent antioxidant and antiaging properties, making it a valuable component in skincare products.
研究领域:
药剂学
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皮肤科学
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生物技术
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产品关联
DOI
PubMed
高影响因子
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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DOI
PubMed
高影响因子
Results in Chemistry
·
2025
·
IF 4.2
Jiabao Cai,Qian Zhang,Jiani Fan,Shengguang Chen
Baicalin, a flavonoid derived from Scutellaria baicalensis, exhibits broad antitumor activity. However, its effects on anaplastic thyroid cancer (ATC) C643 cells remain unclear. This study investigated the inhibitory capacity and underlying mechanisms of baicalin against C643 cells using both in vitro and in vivo models. In vitro, including CCK-8 viability assay, scratch-wound healing assay, Transwell migration, Annexin V-FITC/PI apoptosis, cell-cycle and JC-1 mitochondrial membrane potential assays demonstrated that baicalin reduced cell viability and migration in a concentration-and time-dependent manner, induced G2-phase arrest and decreased mitochondrial membrane potential. Integrated transcriptome sequencing identified BCL2 and the PI3K-AKT pathway as key targets. qPCR and Western blot confirmed that baicalin down-regulated BCL2 in a dose-dependent manner, selectively activated the PI3K-AKT cascade, promoted TP53 recruitment to the BAX/BIM promoters and up-regulated their transcription, accompanied by increased p-PI3K and p-AKT levels. In vivo, daily intraperitoneal administration of 50 mg/kg baicalin for 21 days led to a 55.6 % reduction in C643 xenograft volume. Immunohistochemistry revealed decreased BCL2 and Ki-67 expression in tumor tissues, indicating impaired anti-apoptotic activity and proliferative capacity. Importantly, histopathological examination of major organs (heart, liver, spleen, lung and kidney) showed no treatment-related toxicity, confirming the safety of baicalin. These findings demonstrate that baicalin is a safe, multi-target therapeutic candidate with a well-defined mechanism, offering a novel and effective targeted option for aggressive anaplastic thyroid cancer.
研究领域:
肿瘤学
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分子生物学
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药理学
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天然产物研究
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细胞生物学
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产品关联
DOI
高影响因子
RENAL FAILURE
·
2025
·
IF 3
Neng Bao,Ming-Jia Gu,Qiu-Ya Huang,Hai-Jian Sun,Xue-Xue Zhu,Xin Gu,Jin Wang,Xiang Yu,Qing-Bo Lu,Ya-Fen Yu
Purpose This study aims to investigate the protective effect of baicalin on sepsis-associated acute kidney injury (SA-AKI) and its molecular mechanism.Materials and methods An SA-AKI mouse model was established via lipopolysaccharide (LPS) injection. Baicalin’s effects on renal function, oxidative stress, and apoptosis were evaluated using histopathology, dihydroethidium, and terminal deoxynucleotidyl transferase dUTP nick end labeling staining. Bioinformatics, molecular docking, ribonucleic acid (RNA) sequencing, and Western blotting were employed to investigate the role of baicalin in regulating the peroxisome proliferator‑activated receptor‑γ (PPAR-γ)/uncoupling protein 1 (UCP1) pathway. Human kidney-2 cells were used for in vitro validation.Results In this study, baicalin significantly ameliorated LPS-induced acute kidney injury by modulating the PPAR-γ/UCP1 signaling pathway. Both in vivo and in vitro experiments revealed that baicalin attenuates inflammation, oxidative stress, and apoptosis while restoring mitochondrial function. RNA sequencing analysis revealed significant upregulation of PPAR-γ/UCP1 in the baicalin-treated group. Further molecular docking and molecular dynamics simulations confirmed a stable interaction between baicalin and UCP1. Validation via small interfering RNA-mediated knockdown of PPAR-γ and UCP1 revealed that inhibition of the PPAR-γ/UCP1 pathway abrogated baicalin’s protective effects, highlighting the critical role of this pathway in mediating baicalin’s renoprotection.Conclusion Baicalin protects against SA-AKI by activating the PPAR-γ/UCP1 signaling pathway. This study provides new insights into the mechanisms through which baicalin mitigates kidney injury in sepsis, suggesting its potential as a therapeutic agent for SA-AKI.
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DOI
PubMed
高影响因子
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