BIOCONJUGATE CHEMISTRY
·
2023
·
IF 4.7
Lancong Liu,Wenfeng Ding,Lili He,Yi Yang,Fuyi Guan,Xinlin Sun,Yan Peng,Xue Chen,Wenhao Zhao,Yu Xiao,Pei Luo
Myocardial ischemia/reperfusion (MI/R) injury is an unresolved clinical challenge. The blockade of binding fibrinogen by glycoprotein IIb/IIIa (GPIIb–IIIa) inhibitors has become a new therapeutic approach against MI/R injury. In this study, we modified the RGD structure to combine with scutellarin and synthesized a novel peptide, scutellarin–HomoArg–Gly–Asp–Trp–NH2 (WK001). Herein, reported experimental and docking evidence indicates that WK001 provides immediate and potent platelet inhibition, with stronger inhibition of platelet aggregation than eptifibatide and scutellarin. In particular, it is administered intravenously to prevent thrombus formation and attenuate myocardial fibrosis progression in vivo. Therefore, WK001 could be developed as an antiplatelet drug to treat thrombosis-associated diseases, such as stroke and myocardial infarction.
研究领域:
药理学
·
心血管医学
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DOI
PubMed
高影响因子
Plant Diversity
·
2020
·
IF 1.864
Xing Huang,Weiqi Li,Xudong Zhang
Exploring approaches to regulate meristem is of special importance and broad interest. In this study, we found that the flavonoid scutellarin, which has a 6-hydroxyl and a 7-glucoside, increased root length through the transcription factor NUTCRACKER (NUC). This root lengthening disappeared in NUC -knockout and reappeared in NUC -rescue plants. Scutellarin induced NUC expression and promoted the division of cortex/endodermal initials. In contrast, naringenin, which has same chemical backbone but without 6-hydroxyl and with 7-hydroxyl group, showed the opposite or no effects. Our results demonstrate that scutellarin promotes root length through NUC-mediated regulatory pathways and reveal that flavonoids with and without the 6-hydroxyl and 7-glucoside have positive and negative effects on meristem size, respectively.
研究领域:
植物生物学
·
分子遗传学
·
发育生物学
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DOI
PubMed
高影响因子
DRUG DELIVERY
·
2020
·
IF 4.902
Rongqiang Liao,Ying Liu,Pin Lv,Di Wu,Meiling Xu,Xiaoyuan Zheng
A novel β-cyclodextrin pendant polymer (ε-PL-CD), composed of poly(ε-lysine) (ε-PL) main chain and glycine-β-cyclodextrin (Gly-CD) side chains, was prepared by a simple two-step procedure. The ε-PL-CD was investigated as a drug carrier of hydrophobic drug scutellarin (SCU). The characterization and complexation mode of the SCU:ε-PL-CD were researched in both solution and solid state by means of photoluminescence spectroscopy, 1H and 2D NMR, X-Ray powder diffraction (XRPD), thermal gravimetric analysis, Particle size and Zeta potential. The solubility test indicated that the solubilizing ability of SCU:ε-PL-CD was significantly improved compared with SCU:β-CD and free SCU. Besides, in vitro cell experiment, it was found that SCU:ε-PL-CD has a strong inhibitory effect on the growth and invasion of tumor cells. The present study provides useful information for ε-PL-CD as a drug carrier material.
研究领域:
药剂学
·
生物化学
·
材料科学
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产品关联
DOI
PubMed
高影响因子
Materials Science & Engineering C-Materials for Biological Applications
·
2016
·
IF 3.42
Qi Qin,Xue Ma,Xiali Liao,Bo Yang
As a prerequisite of gene delivery in living cells, DNA condensation has attracted more and more attention. In order to improve the efficiencies of polyamine-β-cyclodextrin-based cationic polyrotaxanes (PR-EDA and PR-DETA) as DNA condensation materials, we have designed and prepared two novel scutellarin-grafted cationic polyrotaxanes (PR-EDA-SCU and PR-DETA-SCU), in which scutellarins (SCU), the planar molecules, were conjugated on the cyclodextrin molecules of PR-EDA and PR-DETA. These materials were characterized by 1D and 2D NMR, XRD, TG and DSC. The electrophoresis assays showed that pDNA condensation efficiencies of PR-EDA and PR-DETA were better than that of PR-EDA and PR-DETA. The complexes of PR-EDA, PR-DETA, PR-EDA-SCU and PR-DETA-SCU with pDNA were further investigated by zeta potential and atomic force microscopy analysis. The results indicated that the planar structure of SCU played an important role in improvement of pDNA condensation efficiencies of PR-EDA-SCU and PR-DETA-SCU. The satisfactory pDNA condensation abilities of PR-EDA-SCU and PR-DETA-SCU could be helpful in designing non-viral gene delivery vectors to control gene expression and delivery.
研究领域:
生物化学
·
分子生物学
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材料科学
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产品关联
DOI
PubMed
高影响因子
Advanced Healthcare Materials
·
2026
·
IF 9.6
Fei Xia,Qingchao Tu,Yinan Liu,Junzhe Zhang,Mengyue Fan,Linying Zhong,Yuanfeng Fu,Pengbo Guo,Huanhuan Pang,Yuqing Meng,Qiaoli Shi,Jigang Wang,Chong Qiu
Chronic diabetic wounds suffer from persistent inflammation, oxidative stress, and impaired angiogenesis. This study develops a carrier-free Cu-SCU hydrogel via self-assembly of scutellarin (SCU) and copper ions (Cu 2 ⁺), without polymers or excipients. Spectroscopic analyses and molecular dynamics simulation confirm Cu-SCU coordination, yielding an injectable hydrogel with mechanical integrity. In vitro, Cu-SCU demonstrates excellent biocompatibility, potent ROS scavenging, and immunomodulation by polarizing macrophages to the reparative M2 phenotype. It also exhibits strong hemostatic activity, promoting RBC/platelet aggregation and accelerating coagulation in vitro and in vivo (liver hemorrhage and tail-amputation models). In diabetic full-thickness wounds, Cu-SCU significantly accelerates healing, enhances re-epithelialization, collagen deposition, and vascular maturation. Analyses reveal reduced neutrophilic infiltration, diminished pro-inflammatory cytokines, and sustained M2 macrophage presence. Proteomic analysis and Western blot validation results demonstrated that it promotes angiogenesis by regulating the MAPK, cGMP-PKG, VEGF, and HIF-1 signaling pathways, as well as upregulating the expression of key pathway proteins including HIF-1α, CDC42, and HK2. Cu-SCU hydrogel promotes healing through multifaceted mechanisms: redox regulation, immune modulation, and pro-angiogenic activation. This simple, biocompatible, and efficacious platform offers a promising alternative to carrier-based systems for chronic wound therapy.
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DOI
PubMed
高影响因子
JOURNAL OF POLYMER RESEARCH
·
2024
·Vol. 31
·期 2
·1-10
·
IF 2.6
Liu Chengchao,Sui Kun,Liu Jiuhong,Wang Zhongwei,Chen Long,Yu Qing
Scutellaria baicalensis (SBC) richly possess active ingredients to satisfy the conditions for functional applications. Herein, the active components of SBC are extracted and introduced into linear low-density polyethylene (LLDPE) to perform as functional additives. The thermal oxygen stability, processing stability, ultraviolet (UV) stability, flame retardancy and mechanical properties are comprehensively investigated. Compared with pure LLDPE, the oxidation induction time (OIT) of LLDPE incorporating SBC extractive (SBE) increased ca. 24 times. The combination of SBE and antioxidant 626 produce more superior antioxidant capacity (OIT of 99.7 min is achieved), revealing an outstanding synergistic effect. After UV irradiation, the carbonyl index variation of the LLDPE adding SBE is less than 50% of that of pure LLDPE. The TGA test showed that SBE was involved in the free radical elimination process. Moreover, the horizontal burning time increases by 37 s with the introduction of both SBE and antioxidant 626. Those results adequately manifest that SBE is a natural, high-performance multi-function additive for LLDPE. This study validly expands the multi-functional application of natural substances into polyolefins, which is a great benefit to the green development of polymer-based composites.
研究领域:
材料科学
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化学工程
·
植物学
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DOI
高影响因子
INTERNATIONAL IMMUNOPHARMACOLOGY
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2020
·
IF 3.943
He-Tao Bian,Gao-Hua Wang,Jun-Jie Huang,Liang Liang,Ling Xiao,Hui-Ling Wang
Depression is a complex and heterogeneous mental disorder. Yet, the mechanisms behind depression remain elusive. Increasing evidence suggests that inflammatory reaction and microglia activation are involved in the pathogenesis of depression. Scutellarin has been found to have anti-inflammatory and antioxidant effects in various diseases. The aim of the present study was to investigate the anti-depressant effects and potential mechanism of scutellarin in the lipopolysaccharide (LPS)-induced depression animal model. The behavioral tests showed that scutellarin administration ameliorated LPS-induced depressive-like behaviors. Additionally, the scutellarin treatment inhibited reactive oxygen species (ROS) generation. Western blot analysis results showed that scutellarin pretreatment suppressed LPS-induced the protein levels of NLRP3 , caspase-1, and IL-1β. Furthermore, immunostaining results showed that scutellarin pretreatment inhibited LPS-induced microglia activation in the hippocampus of rats. These findings suggest that scutellarin effectively improves LPS-induced inflammation-related depressive-like behaviors by inhibiting LPS-induced neuroinflammation and microglia activation, possibly via regulation of the ROS/NLRP3 signaling pathway and microglia activation. Thus, scutellarin may serve as a potential therapeutic strategy for depression.
研究领域:
神经科学
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药理学
·
免疫学
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产品关联
DOI
PubMed
高影响因子
BIOLOGICAL & PHARMACEUTICAL BULLETIN
·
2021
·Vol. 44
·期 6
·780-788
·
IF 2.233
Fu Li,Suping Wang,Manxiang Niu
Gastric cancer is one of the most common malignancies with a high mortality rate world. This study intends to make clear the role and mechanism of the Scutellarin (Scu), a flavonoid isolated from Erigeron breviscapus (Vant.) Hand.-Mazz, in regulating the evolvement of gastric cancer. We selected different doses of Scu to treat gastric cancer cells (MGC-803 and AGS). Then, cell counting kit-8 (CCK8) assay was conducted to verify the proliferation of tumor cells, while flow cytometry was adopted to test the apoptosis rate. Meanwhile, Western blot was conducted to examine epithelial–mesenchymal transition (EMT) markers and the expression of phosphatase and tensin homolog (PTEN)/phosphatidylinositol 3-kinase (PI3K) and apoptosis-related proteins (Bax, Bcl2 and Caspase3). Moreover, xenograft tumor experiment in nude mice was established to verify the effect of Scu on tumor growth. Furthermore, the knockdown model of PTEN was constructed, and the influence of PTEN on the anti-tumor effect of Scu was investigated. As a result, Scu inhibited cell proliferation, EMT and promoted the apoptosis in gastric cancer dose-dependently. Additionally, Scu attenuated tumor cell growth in vivo. Besides, Scu enhanced the expression of PTEN while reduced the phosphorylated level of PI3K. Moreover, the mechanistic study proved that Scu inactivated PI3K by up-regulating PTEN, thus dampening tumor progression. In conclusion, Scu dampened the growth and EMT of gastric cancer by regulating the PTEN/PI3K pathway.
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DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2024
·
IF 7.7
Shouhui Yi,Rongqiang Liao,Wei Zhao,Zuojin Liu
Stimulus-responsive nanomaterials , particularly with targeting capabilities, have garnered significant attention in the cancer therapy. However, the biological safety of these innovative materials in vivo remains unknown, posing a hurdle to their clinical application. Here, a pH/H 2 O 2 dual-responsive and targeting nano carrier system (NCS) was developed using core shell structure of Fe 3 O 4 mesoporous silicon (MSN@Fe 3 O 4 ) as main body, scutellarin (SCU) as antitumor drug and polymer cyclodextrin (PCD) as molecular switch (denoted as PCD@SCU@MSN@Fe 3 O 4 , abbreviated as NCS). The NCS, with an average particle size of 100 nm, displayed exceptional SCU loading capacity, a result of its uniform radial channel structure. The in vitro investigation under condition of pH and H 2 O 2 indicated that NCS performed excellent pH/H 2 O 2 -triggered SCU release behavior. The NCS displayed a higher cytotoxicity against tumor cells (Huh7 and HCT116) due to its pH/H 2 O 2 dual-triggered responsiveness, while the PCD@MSN@Fe 3 O 4 demonstrated lower cytotoxicity for both Huh7 and HCT116 cells. In vivo therapeutic evaluation of NCS indicates significant inhibition of tumor growth in mouse subcutaneous tumor models, with no apparent side-effects detected. The NCS not only enhances the bioavailability of SCU, but also utilizes magnetic targeting technology to deliver SCU accurately to tumor sites. These findings underscore the substantial clinical application potential of NCS.
研究领域:
药学
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生物医学工程
·
肿瘤学
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产品关联
DOI
PubMed
高影响因子
MOLECULES
·
2018
·Vol. 23
·期 12
·3225
·
IF 3.098
Qianru Liu,Xican Li,Xiaojian Ouyang,Dongfeng Chen
To explore whether and how glucuronidation affects pyrogallol-type phytophenols, scutellarein and scutellarin (scutellarein-7-O-glucuronide) were comparatively investigated using a set of antioxidant analyses, including spectrophotometric analysis, UV-vis spectra analysis, and ultra-performance liquid chromatography coupled with electrospray ionization-quadrupole time-of-flight tandem mass spectrometry (UPLC-ESI-Q-TOF-MS/MS) analysis. In spectrophotometric analyses of the scavenging of 1,1-diphenyl-2-picrylhydrazyl (DPPH•), 2,2′-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS+•), and 2-phenyl-4,4,5,5-tetramethylimidazoline-1-oxyl 3-oxide radicals (PTIO•) and the reduction of Cu2+ions, scutellarein showed lower IC50values than scutellarin. However, in•O2−-scavenging spectrophotometric analysis, scutellarein showed higher IC50value than scutellarin. The analysis of UV-Vis spectra obtained after the Fe2+-chelating reaction of scutellarin showed a typical UV-Vis peak (λmax= 611 nm), while scutellarein showed no typical peak. In UPLC-ESI-Q-TOF-MS/MS analysis, mixing of scutellarein with DPPH•yielded MS peaks (m/z678, 632, 615, 450, 420, 381, 329, 300, 288, 227, 196, 182, 161, and 117) corresponding to the scutellarein-DPPH adduct and an MS peak (m/z570) corresponding to the scutellarein-scutellarein dimer. Scutellarin, however, generated no MS peak. On the basis of these findings, it can be concluded that glucuronidation of pyrogallol-type phytophenol antioxidants has a dual effect. On the one hand, glucuronidation can decrease the antioxidant potentials (except for•O2−scavenging) and further lower the possibility of radical adduct formation (RAF), while on the other hand, it can enhance the•O2−-scavenging and Fe2+-chelating potentials.Keywords:scutellarein;scutellarin;pyrogallol-type phytophenol;structure-activity relationship;glucuronidation;antioxidant
研究领域:
植物化学
·
药理学
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产品关联
DOI
PubMed
高影响因子
ADVANCED POWDER TECHNOLOGY
·
2022
·
IF 4.969
Rongqiang Liao,Dexi Jiang,Ying Liu,Pin Lv
In the present study, poly(ε-lysine)-cyclodextrin coated Fe 3 O 4 nanoparticles (PL-CD@Fe 3 O 4 ) were prepared by co-precipitation method. Then the PL-CD@Fe 3 O 4 nanoparticles were studied of the characterization and the selective separation performance for natural medicine (scutellarin). The experimental results showed that PL-CD@Fe 3 O 4 nanoparticles were successfully prepared with a particle size of about 30 nm and a saturation magnetization of 40 emu/g. When the nanoparticles were in the environment of pH = 7, the stability was the best, the adsorption capacity was the strongest, and the number of recyclable times was the most. Langmuir model deduced that the maximum adsorption capacity of the nanoparticles was 76.3 mg/g. In addition, the experimental results of using nanoparticles to separate SCU in the crude extract showed that the purity of SCU could be increased from 72.2% to 93.5% after repeated cyclic separation three times. Two dimensional NMR analysis showed that the selective separation of SCU by PL-CD@Fe 3 O 4 was mainly caused by the host–guest interaction between cyclodextrin and SCU. In conclusion, the PL-CD@Fe 3 O 4 nanoparticles are a very promising material for the extraction and separation of other similar natural drugs.
研究领域:
材料科学
·
药学
·
生物化学
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产品关联
DOI
高影响因子
PHYTOTHERAPY RESEARCH
·
2026
·
IF 8.1
Jianmei Zheng,Lu Cheng,Yingmin Wei,Mingshi Ren,Lei Wang,Jingwen Wang,Wuliu Zhou,Hui Huang,Feihua Wu
Metabolic dysfunction-associated steatotic liver disease (MASLD) is a prevalent chronic liver disorder with limited treatment and manifests as hepatic lipid accumulation. The reduction of nuclear receptor corepressor 1 (NCoR1) activates the nuclear receptor PPARα, which plays a crucial role in alleviating lipid accumulation. We found that Scutellarin (Scu) regulated autophagy-mediated NCoR1/PPARα to enhance fatty acid (FA) β-oxidation and peroxisome production, thereby alleviating the lipid accumulation of MASLD. We used palmitic acid (PA)-treated human hepatocellular carcinoma (HepG2) and alpha mouse liver 12 (AML12) cells, as well as high-fat diet-fed C57BL/6J mice to evaluate the protective effect of Scu on MASLD. Scu reduced the levels of total cholesterol, triglycerides, and lipid droplets, whereas it dose-dependently increased the levels of β-hydroxybutyrate. In addition, Scu increased mRNA and protein expression of PPARα and promoted the transcriptional activity of FA β-oxidation-related target genes. In vitro, inhibition of PPARα with small interfering RNA (siRNA) abolished the activation of FA β-oxidation by Scu. Cellular thermal shift assay and drug affinity responsive target stability demonstrated that Scu did not interact directly with PPARα. Moreover, Scu increased the protein expression of 70-kDa peroxisomal membrane protein and the mRNA expression of peroxisome biogenesis-related genes. These effects were reversed by PPARα-siRNA. Scu improved the impaired autophagy while reducing the mRNA and protein expression of NCoR1. Notably, Scu reduced the colocalization of NCoR1 with PPARα and increased its colocalization with the autophagosome GABARAP. 3-MA, an autophagy inhibitor, attenuated Scu-mediated protective effects by FA β-oxidation and peroxisome biogenesis both in vitro and in vivo. In summary, Scu reduces lipid accumulation by improving the impaired autophagy, decreasing NCoR1 expression to activate PPARα, thereby simultaneously enhancing FA β-oxidation and peroxisome biogenesis, ultimately ameliorating hepatic steatosis.
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DOI
PubMed
高影响因子
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