AQUACULTURE
·
2025
·
IF 3.9
Yun-Yao Tu,Jie Leng,Na Zhang,Qin Yang,Hong-Yu Tang,Cheng-Ke Zhu,Wei-Wei Zeng,Ming-Ji Lv,Song Zhu
Tilapia lake virus (TiLV) has caused serious deadly epidemics and still remains a devastating threat to tilapia aquaculture worldwide, with no practical therapeutic measures. In the study, anti-TiLV activities of 22 kinds of drugs are checked to develop a potential strategy for TiLV control. Safety of the selected drugs to E-11 cells is firstly evaluated to determine their maximum safe concentration (MSC). For preliminary screening in vitro , three 10-fold gradient-diluted drug concentrations (10 −2 , 10 −1 and 10 0 * MSC) are prepared. Baicalin shows the strongest inhibition activity on TiLV-induced cytopathic effects with an inhibition rate close to 80 % at 100 mg/L, and followed by favipiravir and amantadine hydrochloride. Baicalin can completely suppress viral infection at 200 mg/L as verification by Western blot and RT-qPCR analysis, and the 90 % inhibitory concentrations of baicalin on TiLV is 61.33 mg/L. Baicalin shows no obvious anti-TiLV activity by pre-treatment of E-11 cells before TiLV infection, while the infectivity of TiLV is significantly weakened following baicalin treatment, and baicalin has a strong anti-TiLV activity at the post-entry stage of TiLV infection. Besides, baicalin shows no obvious effects on the TiLV attachment to E-11 cells, but has significant inhibition on TiLV multiplication. Therefore, baicalin may have a direct virucidal effect, and/or block the viral genome translation and replication. For anti-TiLV activity evaluation in vivo , baicalin can improve the survival rate of TiLV-infected Nile tilapia ( Oreochromis niloticus ) to 81.8 % following treatment with 10 μg/g baicalin for 3 times, while that was 54.5 % for TiLV-infected tilapia without baicalin treatment. Moreover, the viral titers in liver of TiLV-infected tilapia are generally decreased after baicalin treatment. Results so far indicated that baicalin is a promising therapeutic drug against TiLV infection, providing a potential strategy for TiLV control and promoting the healthy development of tilapia aquaculture.
研究领域:
水产养殖学
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病毒学
·
药物开发
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DOI
高影响因子
Heliyon
·
2024
·
IF 3.4
Xin Yang,Junxian Li,Chunlan Shan,Xuqin Song,Jian Yang,Hao Xu,Deyuan Ou
In the present study, we investigated whether baicalin could reduce the damage caused to RAW264.7 cells following infection with H6N6 avian influenza virus. In addition, we studied the expression of autophagy-related genes. The morphological changes in cells were observed by hematoxylin and eosin (H&E) staining, and the inflammatory factors in the cell supernatant were detected by enzyme-linked immunosorbent assay (ELISA). Transmission electron microscopy (TEM) was used to detect the levels of RAW264.7 autophagosomes, and western blotting and immunofluorescence were used to detect the protein expression of autophagy marker LC3. Quantitative reverse transcriptase-polymerase chain reaction (qRT-PCR) was used to detect the mRNA transcription levels of autophagy key factors. The results showed that different doses of baicalin significantly reduced the H6N6 virus-induced damage of RAW264.7 cells. The contents of interleukin (IL)-1β, IL-2, IL-6, and tumor necrosis factor (TNF)-α in the cell supernatant significantly decreased. In addition, the protein expression of LC3 and Beclin-1, ATG12, ATG5 the mRNA levels were significantly decreased. This study showed that baicalin can reduce cell damage and affect the H6N6-induced autophagy level of RAW264.7 cells.
研究领域:
病毒学
·
药理学
·
免疫学
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2025
·
IF 8.5
Yurou Chen,Kun Sun,Yujie Lin,Jiaxuan Li,Ningzhe Wang,Qingfeng Ban,Xibo Wang
To improve the emulsion properties of soybean protein isolate (SPI), the effect of baicalin (BC) concentrations on the structure, antioxidant properties, and emulsion stability of SPI-BC conjugates were investigated. Structure analysis revealed that BC induced structural depolymerization and unfolding of SPI through the formation of covalent bonds (C N and C S), increasing hydrophilicity, stabilizing the interface, and enabling the formation of smaller oil droplets. The increase in zeta potential of SPI-BC conjugates enhanced electrostatic repulsion between droplets, preventing aggregation, while the strengthened interfacial protein network improved viscosity, shear stress, and thixotropic recovery, thereby significantly stabilizing the emulsion structure. The addition of 0.4 mg/mL BC exhibited the optimal emulsification performance, increasing emulsion stability by 35.4 %. Moreover, SPI-BC emulsions demonstrated enhanced stability against various environmental stressors (storage, heating, pH, ionic strength, and oxidation). These findings confirmed that BC covalent modification enhanced the structural properties of SPI and improved the stability of protein-based emulsions through structural regulation. This study provides new insights into the potential of BC in improving SPI functionality.
研究领域:
食品科学
·
生物化学
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产品关联
DOI
PubMed
高影响因子
Chinese Journal of Integrative Medicine
·
2024
·
IF 2.2
Li Gang-gang,Chu Xiu-feng,Xing Ya-min,Xue Xia,Ihtisham Bukhari,Liang Xin-feng,Xu Ji-xuan,Mi Yang,Zheng Peng-yuan
Objective To observe the therapeutic effects and underlying mechanism of baicalin against colon cancer. Methods The effects of baicalin on the proliferation and growth of colon cancer cells MC38 and CT26. WT were observed and predicted potential molecular targets of baicalin for colon cancer therapy were studied by network pharmacology. Furthermore, molecular docking and drug affinity responsive target stability (DARTS) analysis were performed to confirm the interaction between potential targets and baicalin. Finally, the mechanisms predicted by in silico analyses were experimentally verified in-vitro and in-vivo . Results Baicalin significantly inhibited proliferation, invasion, migration, and induced apoptosis in MC38 and CT26 cells (all P <0.01). Additionally, baicalin caused cell cycle arrest at the S phase, while the G 0 /G 1 phase was detected in the tiny portion of the cells. Subsequent network pharmacology analysis identified 6 therapeutic targets associated with baicalin, which potentially affect various pathways including 39 biological processes and 99 signaling pathways. In addition, molecular docking and DARTS predicted the potential binding of baicalin with cyclin dependent kinase inhibitor 2A (CDKN2A), protein kinase B (AKT), caspase 3, and mitogen-activated protein kinase (MAPK). In vitro , the expressions of CDKN2A, MAPK, and p-AKT were suppressed by baicalin in MC38 and CT26 cells. In vivo , baicalin significantly reduced the tumor size and weight (all P <0.01) in the colon cancer mouse model via inactivating p-AKT, CDKN2A, cyclin dependent kinase 4, cyclin dependent kinase 2, interleukin-1, tumor necrosis factor α , and activating caspase 3 and mouse double minute 2 homolog signaling (all P <0.05). Conclusion Baicalin suppressed the CDKN2A protein level to prevent colon cancer and could be used as a therapeutic target for colon cancer.
研究领域:
肿瘤学
·
药理学
·
分子生物学
·
细胞生物学
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DOI
PubMed
高影响因子
CHEMICAL ENGINEERING RESEARCH & DESIGN
·
2025
·
IF 3.9
Ze Yu Lian,Fu Zhen Gao,Run Xiang Qin,Jing Qiang Ma,Xue Zhong Wang
Baicalin as a flavonoid compound exhibits diverse and significant pharmacological activities. Nevertheless, its intrinsically poor aqueous solubility has been an obstacle to its clinical application. To overcome this limitation, this study devised an innovative crystallization strategy, thereby enabling the controllable synthesis of baicalin nanocrystals. Initially, the crystallization process of baicalin microcrystals in a stirred tank crystallizer was optimized, and the effects of parameters such as additive types, equivalents, stirring rates, and crystallization temperatures on the particle size and morphology of crystals were explored. Subsequently, technologies including X-ray diffraction (XRD), proton nuclear magnetic resonance spectroscopy (¹H NMR), online microscopy imaging, and pH monitoring were utilized to elucidate the crystallization mechanism of baicalin, thereby laying the theoretical foundation for the preparation of baicalin nanocrystals. Finally, this study innovatively introduced an impinging jet crystallizer, based on the foregoing research findings. In contrast to the traditional reactors, this device integrates the advantages of both impinging jet reactor and batch crystallizer, which can simultaneously strengthen the micro- and macro-mixing processes. This dual-scale modulation strategy achieves precise kinetic control by synchronizing nucleation enhancement with growth suppression and regulation. To identify the optimal process parameters of the impinging jet crystallizer, a computational fluid dynamics (CFD) simulation and experimental research were combined. Eventually, the baicalin nanocrystals featuring an average particle size of less than 300 nm and spherical morphology were successfully prepared.
研究领域:
药剂学
·
制药工程
·
材料科学
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产品关联
DOI
高影响因子
Biomed Research International
·
2022
·
IF 3.246
Liping Chen,Bo Fan,Huan Gu,Liuqing Yang,Xiaofang Li
The aim of the present study was to explore the potential pharmacological mechanism of baicalin by combining network pharmacology prediction and the experimental verification of alopecia. Networks of baicalin-associated targets and alopecia-related genes were constructed using the STRING database. Potential targets and pathways associated with the therapeutic efficacy of baicalin were identified via enrichment analysis using Cytoscape and the database for annotation, visualization and integrated discovery (Metascape). The back hair of C57BL/6J mice was removed with depilatory cream to verify the therapeutic effect of baicalin. Human hair dermal papilla cells (HHDPCs) were used to explore the mechanism of action of baicalin. Network pharmacology analysis revealed that the potential targets of baicalin mainly include protein serine/threonine kinase, Src protein, epidermal growth factor receptor, and insulin-like growth factor 1 (IGF1), which were indicated to mediate neutrophil degranulation and regulation of cell-cell adhesion, vesicle lumen, cytoplasmic vesicle, membrane raft, and endopeptidase activity. Multiple pathways were identified, such as proteoglycans in cancer, PI3K/AKT, and forkhead box O signaling pathways. Following baicalin treatment for the experimental mice, the coverage, length, and weight of the hair increased in a baicalin dose-dependent manner. Moreover, the histological evaluation showed that the number of hair follicles increased after baicalin treatment and melanin formation were pronounced. In addition, baicalin induced an increase in the phosphorylated p-AKT, p-glycogen synthase kinase-3 β , p-PI3K, TGF- β 1, and vascular endothelial growth factor levels. Furthermore, the activation levels of key protein p-AKT were increased. Baicalin induced the proliferation of HHDPCs in vitro and significantly upregulated p-AKT, IGF1, and alkaline phosphatase. In conclusion, the present study revealed that the pharmacological mechanisms of baicalin in alopecia therapy were associated with the proliferation of DPCs, the activation of the AKT pathway, and the transmission of downstream signals, indicating that baicalin is a potential drug candidate for the clinical treatment of hair loss.
研究领域:
药理学
·
分子生物学
·
皮肤病学
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DOI
PubMed
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
·
2019
·
IF 3.571
Xuan Xin,Mengmeng Zhang,Xiao-Feng Li,Guanglei Zhao
Enzymatic acylation is commonly used to increase the lipophilicity of flavonoids. However, the absence of primary hydroxyl groups makes it challenging to acylate baicalin using traditional acylation methods. In this study, an enzymatic esterification strategy was developed to introduce fatty-acid chains into baicalin at its carboxyl group, hence successfully synthesizing a new series of baicalin ester derivatives in nonaqueous media. Under the optimal reaction conditions, up to 95% conversion of baicalin was achieved. Antimicrobial evaluation of the baicalin ester derivatives indicated a corresponding increase to that of C log P values, with a cutoff effect at C log P = 5.2. Baicalin ester derivatives with C log P values of 4.9–5.2 exhibited the most potent antimicrobial activity. Interestingly, the introduction of medium-length fatty alcohol chains not only increased lipophilicity but also endowed them with membrane-disrupting properties. This study, therefore, provides an understanding of the esterification of flavonoid glycosides and a prospective application of the ester derivatives.
研究领域:
药理学
·
生物催化
·
有机合成
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产品关联
DOI
PubMed
高影响因子
CURRENT MOLECULAR MEDICINE
·
2019
·Vol. 19
·期 5
·376-386
·
IF 2.196
Chen Yun,Yao Fangke,Ming Ke,Shi Jintong,Zeng Ling,Wang Deyun,Wu Yi,Hu Yuanliang,Liu Jiaguo
Background: Duck virus hepatitis (DVH) caused by duck hepatitis A virus type 1 (DHAV-1) is a malignant disease in ducklings, causing economic losses in the duck industry. However, there is still no antiviral drug against DHAV-1 in the clinic. Objective: Our aim is to investigate
the anti-DHAV-1 effect of baicalin, which is a flavonoid derived from the Chinese medicinal herb huangqin (Scutellaria baicalensis Georgi). Methods: Here, we first detected its anti-DHAV-1 ability in vitro and in vivo. At the same time, the inhibition of baicalin on DHAV-1 reproduction
was determined. Finally, we tested and verified the anti-oxidative and immuno-enhancing roles of baicalin on its curative effect on DVH. Results: Baicalin possessed anti-DHAV-1 effect. It improved the cytoactive of DEH which was infected by DHAV-1 as well as reduced the DHAV-1 reproduction
in DEH. Under baicalin treatment, mortality of ducklings infected by DHAV-1 decreased, additionally the DHAV-1 level and liver injury in such ducklings were significantly reduced or alleviated. The in vitro mechanism study indicated baicalin inhibited DHAV-1 reproduction via interfering the
viral replication and release. Furthermore, the in vivo mechanism study manifested both the anti-oxidative and immuno-enhancing abilities of baicalin, which played crucial roles in its curative effect on DVH. Conclusion: This study may provide a scientific basis for developing baicalin
as one or a part of the anti-DHAV-1 drugs.
研究领域:
兽医学
·
病毒学
·
药理学
✓ 已验证
DOI
PubMed
高影响因子
AMERICAN JOURNAL OF CHINESE MEDICINE
·
2020
·Vol. 48
·期 01
·143-160
·
IF 3.682
Meng-Jie Wang,Chun-Hua Yang,Yue Jin,Chang-Biao Wan,Wei-He Qian,Fei Xing,Xiang Li,Yuan-Yuan Liu
Baicalin is a flavonoid extracted from Scutellariae Radix and shows a variety of biological activities as reducing lipids, diminishing inflammation, and inhibiting bacterial infection. However, there is no report of baicalin against CVB3 infection. In this study, we found that baicalin can reduce viral titer in a dose-dependent manner in vitro at a dose with no direct virucidal effect. Moreover, we revealed that baicalin can also improve survival rate, reduce heart weight/body weight ratio, prevent virus replication, and relieve myocardial inflammation in the acute viral myocarditis mouse model induced by CVB3. Then, in order to explore the mechanism of baicalin inhibiting CVB3 replication, we respectively examined the expression of autophagosome marker LC3-II by Western blot, tested the concentration of free fatty acid (FFA) and cholesterol (CHO) by commercial kits, detected the mRNA levels of fatty acid synthase (Fasn) and acetyl coenzyme a carboxylase (ACC) by RT-PCR, and observed the lipid content of cells by fluorescence staining. The results showed that CVB3 infection increased autophagosome formation and lipid content in HeLa cells, but these changes were significantly blocked by baicalin. Finally, in order to confirm that baicalin inhibits viral replication and reduces autophagosome formation by reducing cellular lipids, we added exogenous palmitate to cell culture supernatants to promote intracellular lipid synthesis and found that palmitate did not alter LC3-II and CVB3/VP1 expression in HeLa cells with or without CVB3 infection. Interestingly, palmitate can reverse the inhibitory effect of baicalin on autophagosome formation and viral replication. In conclusion, our results indicated that lipids play an important role in CVB3 replication, and the effect of baicalin against CVB3 was associated with its ability to reduce cellular lipid synthesis to limit autophagosome formation.
研究领域:
病毒学
·
药理学
·
分子生物学
✓ 已验证
DOI
PubMed
高影响因子
Viruses-Basel
·
2015
·Vol. 7
·期 8
·4756-4771
·
IF 3.353
Xiang Li,Yuanyuan Liu,Tingting Wu,Yue Jin,Jianpin Cheng,Changbiao Wan,Weihe Qian,Fei Xing,Weifeng Shi
Baicalin is a flavonoid compound extracted fromScutellariaroots that has been reported to possess antibacterial, anti-inflammatory, and antiviral activities. However, the antiviral effect of baicalin on enterovirus 71 (EV71) is still unknown. In this study, we found that baicalin showed inhibitory activity on EV71 infection and was independent of direct virucidal or prophylactic effect and inhibitory viral absorption. The expressions of EV71/3D mRNA and polymerase were significantly blocked by baicalin treatment at early stages of EV71 infection. In addition, baicalin could decrease the expressions of FasL and caspase-3, as well as inhibit the apoptosis of EV71-infected human embryonal rhabdomyosarcoma (RD) cells. Altogether, these results indicate that baicalin exhibits potent antiviral effect on EV71 infection, probably through inhibiting EV71/3D polymerase expression and Fas/FasL signaling pathways.Keywords:baicalin;enterovirus 71;3D polymerase;apoptosis
研究领域:
病毒学
·
药理学
·
分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
RSC Advances
·
2022
·Vol. 12
·期 14
·8737-8742
·
IF 4.036
Zhen-Zhen Wang,Yuan Jia,Guoqiang Wang,Hongjuan He,Lihua Cao,Yanmei Shi,Mingsan Miao,Xiu-Min Li
Baicalin has been demonstrated to have multiple pharmacological activities but low solubility. Various baicalin hydrogels have been used to improve its solubility and break its limitation in clinical applications. However, traditional baicalin hydrogels contain numerous ingredients and usually show low baicalin loading capacity. Herein, we discovered a dynamic covalent hydrogel only consisting of baicalin and inorganic borate, in which baicalin is considered as the carrier and drug without other ingredients. The dynamic boronate bonds endow the hydrogel with excellent degradability and multi-stimuli-responsiveness. Moreover, the hydrogel displayed remarkable thixotropy, moldability, and self-healing properties. And the biocompatible baicalin hydrogel exhibited significant antibacterial activities, and can be considered as a potential drug delivery system for biomedical applications.
研究领域:
药剂学
·
材料科学
·
生物医学工程
·
化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
BioNanoScience
·
2025
·Vol. 15
·期 4
·1-10
·
IF 3.2
Ding Ziyang,Lei Shiqi,Zhou Chang,Wang Xinming,Quan Yanling,Jiang Zhongliang,Ni Qingqing,Ma Ke,Chen Wei
Hepatocellular carcinoma (HCC), as a highly lethal malignant tumor, ranks as the sixth most common cancer and the third leading cause of human death worldwide. Traditional treatment methods are limited by toxic side effects and drug resistance. This study focuses on the poorly water-soluble herb release characteristics of multi-layer coaxial nanofibers (NFs) tubes in hepatic artery embolization (TACE). A PVP/PCL core-shell structure was developed for the efficient loading and controlled release of baicalin (BG). The water-soluble PVP core ensured loading, while the compatible PCL shell enabled controlled release. Further sustained-release experiments simulated the treatment process. During in vitro release, the NFs shell showed a stable release rate after 20 h. Its cumulative release was 4.3% with a duration exceeding 1500 h. In contrast, the nanofiber core (NFC) layer exhibited rapid release and stabilized after 25 h. Accurate regulation of the release rate of the poorly water-soluble herb BG can be precisely controlled. This study provides innovative strategies for the treatment of HCC, which are expected to improve treatment efficacy and reduce side effects.
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产品关联
DOI
高影响因子
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