INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2023
·
IF 8.2
Guangming Chen,Nan Jiang,Junping Zheng,Haiming Hu,Huabing Yang,Aizhen Lin,Baifei Hu,Hongtao Liu
In this study, two homogeneous polysaccharides (APS-A1 and APS-B1) were isolated from Astragalus membranaceus by DEAE-52 cellulose and Sephadex G-100 column chromatography. Their chemical structures were characterized by molecular weight distribution, monosaccharide composition, infrared spectrum, methylation analysis, and NMR. The results revealed that APS-A1 (2.62 × 10 6 Da) was a 1,4-α-D-Glc p backbone with a 1,4,6-α-D-Glc p branch every ten residues. APS-B1 (4.95 × 10 6 Da) was a heteropolysaccharide composed of glucose, galactose, and arabinose (75.24:17.27:19.35). Its backbone consisted of 1,4-α-D-Glc p , 1,4,6-α-D-Glc p , 1,5-α-L-Ara f and the sidechains composed of 1,6-α-D-Gal p and T-α/β-Glc p . Bioactivity assays showed that APS-A1 and APS-B1 had potential anti-inflammatory activity. They could inhibit the production of inflammatory factors (TNF-α, IL-6, and MCP-1) in LPS-stimulated RAW264.7 macrophages via NF-κB and MAPK (ERK, JNK) pathways. These results suggested that the two polysaccharides could be potential anti-inflammatory supplements.
研究领域:
药理学
·
免疫学
·
生物化学
·
分子生物学
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产品关联
DOI
PubMed
高影响因子
MACROMOLECULAR CHEMISTRY AND PHYSICS
·
2011
·Vol. 212
·期 17
·1900-1909
·
IF 2.437
Wenguang Leng,Shuxue Zhou,Limin Wu
Nail/spindle-shaped polyaniline is synthesized by chemically oxidizing aniline with ammonium persulfate in a near-neutral aqueous medium using PVP as the stabilizing agent. The type of dispersing agent, APS content and aniline concentration have obvious impacts on the morphology of the resulting polyaniline. Typically, in the concentration ranges of 1.5–6 × 10 −4 M PVP and 0.02–0.05 M aniline and for molar ratios [APS]:[aniline] of 0.4:1 to 0.8:1, nail/spindle-shaped polyaniline can be obtained. A possible mechanism is proposed to elucidate the formation process.
研究领域:
材料科学
·
化学
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产品关联
DOI
高影响因子
ACS Sustainable Chemistry & Engineering
·
2016
·
IF 5.267
Yao Tan,Yongzhuang Liu,Wenshuai Chen,Yixing Liu,Qingwen Wang,Jian Li,Haipeng Yu
Cellulose nanocrystal has been widely used as a reinforcement filler in waterborne coatings, but the application of cellulose nanofiber (CNF) as a filler is difficult because of inhomogeneous dispersion. Herein, a facile and effective strategy to improve the dispersion of CNFs in the polymer matrix by mixing with γ-aminopropyltriethoxysilane (APS) is presented. The APS dosages 0.08–0.48 wt % to 0.3 wt % CNFs were investigated, and the dosage 0.16% was found to achieve a superior stability of CNFs in the aqueous solution. The APS(0.16%)-modified CNFs were then incorporated and demonstrated distributing uniformly in the waterborne acrylic coating. The as-prepared coatings retain high light transmittance around 90%, and display improved mechanical properties. The composite coatings show a maximum 500% improvement in Young’s modulus, two-level improvement in hardness, and 35% reduction in abrasion loss as compared with those of neat coating. These results reveal that APS modification induces the homogeneous dispersion of CNFs in aqueous solution, and turns the CNF into an ideal reinforced filler for waterborne coatings.
研究领域:
材料科学
·
化学工程
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产品关联
DOI
高影响因子
Materials Today Communications
·
2025
·
IF 4.5
Ying Wang,Yan Zhang,Xingyi Zhou,Yang Cheng,Lin Liu,Xiaobing Zhao,Ningyi Yuan,Jianning Ding
The high active chemical properties of magnesium (Mg) alloys result in poor corrosion resistance, limiting their applications. Herein, a tri-layer composite coating with strong bonding force containing layered double hydroxide (LDH), 3-aminopropyltriethoxysilane (APS) and graphene oxide (GO) was fabricated onto the AZ31B Mg alloys surface by in-situ growth and self-assembly methods. The results showed that the corrosion resistance of Mg alloy was greatly improved after coated with the three-layer composite coating. Compared with Mg alloy, the corrosion current density of LDHs-APS/GO composite was reduced by 4 orders of magnitude. It was related to the synergistic effect of the strong binding force, the ion exchange capacity and the good barrier effect of the composite coating.
研究领域:
材料科学
·
腐蚀与防护
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产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2020
·
IF 5.162
Bensheng Jiang,Linlin Tian,Xiaoli Huang,Zhengqi Liu,Kaiying Jia,Hua Wei,Xueying Tao
Two exopolysaccharides, NPS and APS, were isolated from L. plantarum WLPL09 and purified by ion-exchange chromatography. The structural analyses showed that molecular weight of NPS and APS were 72.60 kDa and 33.22 kDa, respectively. NPS was mainly composed of mannose and glucose, in molar ratio of 85.35:14.65, while APS was composed of mannose, glucose and galactose, in molar ratio of 89.69:8.65:1.66. In in vitro antitumor assays, APS displayed strong anti-proliferative effect against HepG2 hepatocellular carcinoma cells and HCT-8 colon adenocarcinoma cells in a dose-dependent manner. Morphological and flow cytometry analyses revealed that APS strongly induced apoptosis of HepG2 and HCT-8, especially for HCT-8. Furthermore, APS significantly up-regulated the mRNA level of apoptosis-related genes in cancer cells, and remarkably improved the activities of caspase-3, -8 and -9 in HepG2, caspase-3 and -8 in HCT-8. These results suggest APS might be explored as a potential, natural antitumor agent for functional food.
研究领域:
微生物学
·
肿瘤学
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分子生物学
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药理学
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DOI
PubMed
高影响因子
ACTA PHARMACOLOGICA SINICA
·
2013
·Vol. 34
·期 7
·939-950
·
IF 2.354
Peng Yan-min,Zheng Jian-bin,Zhou Yu-bo,Li Jia
Aim: Curcumin has shown promising anticancer activity, which relies on its inhibition on NF-κB pathway. In this study, we characterized the pharmacological profile of a novel curcumin analog P1 and elucidate the related mechanisms. Methods: HEK293/NF-κB cells, stably transfected with an NF-κB-responsive luciferase reporter plasmid, were generated for high-throughput screen (HTS). Eight cancer cell lines, including PC3, COLO 205, HeLa cells etc . were tested. Cell viability was assessed using the sulforhodamine B (SRB) assays. Cell apoptosis was evaluated using FACS, immunocytochemistry, and Western blotting. H 2 -DCFDA and MitoSOX Red were used to detect cellular and mitochondrial reactive oxygen species (ROS). The mitochondrial function was evaluated using mitochondrial oxygen consumption assay. Results: P1, a tropinone curcumin, was found in HTS targeting the NF-κB pathway. Its IC 50 value in inhibition of TNF-α-induced NF-κB activation was 0.8 μmol/L, whereas its IC 50 values in inhibiting the growth of A549 and HeLa cells were 1.24 and 0.69 μmol/L, respectively, which was 20- to 30-fold more potent than curcumin. The inhibition of P1 on the NF-κB pathway was further addressed in HeLa cells. The compound up to 10 μmol/L did not affect the binding of NF-κB to DNA, but markedly inhibited NF-κB nuclear translocation, IκB degradation and IκB kinase phosphorylation. The compound (1 and 3 μmol/L) concentration-dependently induced ROS generation, whereas curcumin up to 20 μmol/L had no effect. P1-induced ROS generation was mainly localized in mitochondria, and reversed by NAC. Moreover, the compound significantly enhanced TNF-α-induced apoptosis. Conclusion: P1 is a novel curcumin analog with potent anticancer activities, which exerts a distinct inhibition on the NF-κB pathway.
研究领域:
药理学
·
肿瘤学
·
细胞生物学
·
分子生物学
✓ 已验证
DOI
PubMed
高影响因子
ACTA PHARMACOLOGICA SINICA
·
2016
·Vol. 37
·期 4
·545-554
·
IF 3.166
Su Hui-fang,Lin Qing,Wang Xin-yi,Fu Yao,Gong Tao,Sun Xun,Zhang Zhi-rong
Aim: (+)-Catechin and puerarin are polyphenol and flavonoid, respectively, in green tea and foodstuffs. They exhibit potent antioxidant activity and are widely used for treating cardiocerebrovascular diseases. The aim of this work was to investigate the potential interactions between (+)-catechin and puerarin following concurrent oral administration in rats, and their absorption mechanisms in Caco-2 cell monolayers. Methods: Pharmacokinetic studies were conducted in male rats received (+)-catechin (140 mg/kg, po ) and/or puerarin (200 mg/kg, po ). The cell uptake and transport behavior in Caco-2 cell monolayers and the interactions of the two compounds were analyzed. Results: When (+)-catechin and puerarin were administered concurrently, the AUC 0-12 h and C max values of puerarin were 2.48-fold and 3.91-fold, respectively, as large as those of puerarin alone; the AUC 0-12 h and C max values of (+)-catechin were decreased to 57.62% and 77.55%, respectively, compared with those of (+)-catechin alone. In Caco-2 cell monolayers, (+)-catechin (300 and 600 μmol/L) significantly increased the cell uptake and transport of puerarin, whereas puerarin (300 and 600 μmol/L) significantly decreased the cellular uptake and transport of (+)-catechin. Furthermore, both cyclosporine A (P-glycoprotein inhibitor) and MK-571 (MRP-2 inhibitor) significantly increased the cellular uptake and transport of (+)-catechin and puerarin. Conclusion: Concurrent oral administration of (+)-catechin and puerarin significantly increased the absolute oral bioavailability of puerarin, but decreasing that of (+)-catechin. The competitive efflux of (+)-catechin and puerarin by P-glycoprotein and MRP-2 might lead to this interaction during their absorption process in the small intestine.
研究领域:
药理学
·
药剂学
·
细胞生物学
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DOI
PubMed
高影响因子
ACTA PHARMACOLOGICA SINICA
·
2015
·Vol. 36
·期 7
·863-873
·
IF 2.912
Lin Qing,Ling Li-qin,Guo Ling,Gong Tao,Sun Xun,Zhang Zhi-rong
Aim: Imperialine is an effective compound in the traditional Chinese medicine chuanbeimu (Bulbus Fritillariae Cirrhosae ) that has been used as antitussive/expectorant in a clinical setting. In this study we investigated the absorption characteristics of imperialine in intestinal segments based on an evaluation of its physicochemical properties. Methods: Caco-2 cells were used to examine uptake and transport of imperialine in vitro , and a rat in situ intestinal perfusion model was used to characterize the absorption of imperialine. The amount of imperialine in the samples was quantified using LC-MS/MS. Results: The aqueous solubility and oil/water partition coefficient of imperialine were determined. This compound demonstrated a relatively weak alkalinity with a pKa of 8.467±0.028. In Caco-2 cells, the uptake of imperialine was increased with increasing pH in medium, but not affected by temperature. The apparent absorptive and secretive coefficient was (8.39±0.12)×10 −6 cm/s and (7.78±0.09)×10 −6 cm/s, respectively. Furthermore, neither the P-glycoprotein inhibitor verapamil nor Niemann-Pick C1-Like 1 transporter inhibitor ezetimibe affected the absorption and secretion of imperialine in vitro . The in situ intestinal perfusion study showed that the absorption parameters of imperialine varied in 4 intestinal segments (duodenum, jejunum, ileum and colon) with the highest ones in the colon, where a greater number of non-ionized form of imperialine was present. Conclusion: The intestinal absorptive characteristics of imperialine are closely related to its physicochemical properties. The passive membrane diffusion dominates the intestinal absorption of imperialine.
研究领域:
药理学
·
中药学
·
药学
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产品关联
DOI
PubMed
高影响因子
ACTA PHARMACOLOGICA SINICA
·
2018
·Vol. 39
·期 10
·1681-1692
·
IF 3.562
Liu Hui-na,Guo Ning-ning,Guo Wang-wei,Huang-Fu Ming-yi,Vakili Mohammad Reza,Chen Jie-jian,Xu Wen-hong,Wei Qi-chun,Han Min,Lavasanifar Afsaneh,Gao Jian-qing
Breast cancer is the leading cause of cancer-related death for women, and multidrug resistance (MDR) is the major obstacle faced by chemotherapy for breast cancer. We have previously synthesized a doxorubicin (DOX) derivative by conjugating DOX with triphenylphosphonium (TPP) to achieve mitochondrial delivery, which induced higher cytotoxicity in drug-resistant breast cancer cells than DOX itself. Due to its amphiphilicity, TPP-DOX is difficult to physically entrap in nanocarriers. Thus, we linked it to hyaluronic acid (HA) by a novel ionic bond utilizing the specific bromide ion of TPP to form supra-molecular self-assembled structures (HA-ionic-TPP-DOX). The product was analyzed uisng 1 H-NMR, 13 C-NMR and mass spectrometry. The HA nanocarriers (HA-ionic-TPP-DOX) were shown to self-assemble into spherical nanoparticles, and sensitive to acidic pH in terms of morphology and drug release. Compared with free DOX, HA-ionic-TPP-DOX produced much greater intracellular DOX accumulation and mitochondrial localization, leading to increased ROS production, slightly decreased mitochondrial membrane potential, increased cytotoxicity in MCF-7/ADR cells and enhanced tumor targeting in vivo. In xenotransplant zebrafish model with the MCF-7/ADR cell line, both TPP-DOX and HA-ionic-TPP-DOX inhibited tumor cell proliferation without inducing significant side effects compared with free DOX. In addition, we observed a better anti-tumor effect of HA-ionic-TPP-DOX on MCF-7/ADR cells in zebrafish than that of TPP-DOX treatment. Furthermore, HA-ionic-DOX-TPP exhibited favorable biocompatibility and anti-tumor effects in MCF-7/ADR tumor-bearing nude mice in comparison with the effects of TPP-DOX and DOX, suggesting the potential of HA-ionic-TPP-DOX for the targeted delivery and controlled release of TPP-DOX, which can lead to the sensitization of resistant breast tumors.
研究领域:
肿瘤学
·
药学
·
纳米技术
·
生物医学工程
·
癌症研究
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DOI
PubMed
高影响因子
ACTA PHARMACOLOGICA SINICA
·
2018
·Vol. 39
·期 9
·1522-1532
·
IF 3.562
Xue Cai-fu,Zhang Zhe,Jin Yan,Zhu Bin,Xing Jun-fen,Ma Guo,Xiang Xiao-qiang,Cai Wei-min
Liver metabolism is commonly considered the major determinant in drug discovery and development. Many in vitro drug metabolic studies have been developed and applied to understand biotransformation. However, these methods have disadvantages, resulting in inconsistencies between in vivo and in vitro experiments. A major factor is that they are static systems that do not consider the transport process in the liver. Here we developed an in vitro dynamic metabolic system (Bio-PK metabolic system) to mimic the human pharmacokinetics of tolbutamide. Human liver microsomes (HLMs) encapsulated in a F127'-Acr-Bis hydrogel (FAB hydrogel) were placed in the incubation system. A microdialysis sampling technique was used to monitor the metabolic behavior of tolbutamide in hydrogels. The measured results in the system were used to fit the in vitro intrinsic clearance of tolbutamide with a mathematical model. Then, a PBPK model that integrated the corresponding in vitro intrinsic clearance was developed to verify the system. Compared to the traditional incubation method, reasonable PK profiles and the in vivo clearance of tolbutamide could be predicted by integrating the intrinsic clearance of tolbutamide obtained from the Bio-PK metabolic system into the PBPK model. The predicted maximum concentration ( C
max ), area under the concentration-time curve (AUC), time to reach the maximum plasma concentration ( T
max ) and in vivo clearance were consistent with the clinically observed data. This novel in vitro dynamic metabolic system can compensate for some limitations of traditional incubation methods; it may provide a new method for screening compounds and predicting pharmacokinetics in the early stages, supporting the development of compounds.
研究领域:
药理学
·
药物代谢
·
生物医学工程
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产品关联
DOI
PubMed
高影响因子
ACTA PHARMACOLOGICA SINICA
·
2012
·Vol. 33
·期 7
·909-917
·
IF 1.953
Wang Xin-ting,Li Jia,Liu Li,Hu Nan,Jin Shi,Liu Can,Mei Dan,Liu Xiao-dong
Aim: Diabetes is associated with elevated serum total cholesterol level and disrupted lipoprotein subfractions. The aim of this study was to examine alterations in the tissue cholesterol contents closely related to diabetic complications. Methods: Intraperitoneal injection of streptozotocin was used to induce type 1 diabetes in adult male Sprague-Dawley rats. On d 35 after the injection, liver, heart, intestine, kidney, pancreas, cerebral cortex and hippocampus were isolated from the rats. The content of total and free cholesterol in the tissues was determined using HPLC. The ATP-binding cassette protein A1 (ABCA1) protein and ApoE mRNA were measured using Western blot and QT-PCR analyses, respectively. Results: In diabetic rats, the level of free cholesterol was significantly decreased in the peripheral tissues, but significantly elevated in hippocampus, as compared with those in the control rats. Diabetic rats showed a trend of decreasing the total cholesterol level in the peripheral tissues, but significant change was only found in kidney and liver. In diabetic rats, the level of the ABCA1 protein was significantly increased in the peripheral tissues and cerebral cortex; the expression of ApoE mRNA was slightly decreased in hippocampus and cerebral cortex, but the change had no statistical significance. Conclusion: Type 1 diabetes decreases the free cholesterol content in the peripheral tissues and increases the free cholesterol content in hippocampus. The decreased free cholesterol level in the peripheral tissues may be partly due to the increased expression of the ABCA1 protein.
研究领域:
内分泌学
·
代谢学
·
药理学
·
神经科学
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产品关联
DOI
PubMed
高影响因子
ACTA PHARMACOLOGICA SINICA
·
2017
·Vol. 38
·期 12
·1655-1662
·
IF 3.223
Dong Xin-yue,Lang Tian-qun,Yin Qi,Zhang Peng-cheng,Li Ya-ping
Breast cancer is the most vicious killer for women, and tumor metastasis is one of the leading causes of breast cancer therapy failure. In this study, a new pH-sensitive polymer (polyethylene glycol-block-poly[(1,4-butanediol)-diacrylate-β-N,N-diisopropylethylenediamine], BDP) was synthesized. Based on BDP, docetaxel/silibinin co-delivery micelles (DSMs) was constructed. DSM had a well-defined spherical shape under the transmission electron microscope with average hydrodynamic diameter of 85.3±0.4 nm, and were stable in the bloodstream but could dissociate to release the chemotherapeutic agents in the low pH environment of the endo/lysosomes in the tumor cells. Compared with free drugs, DSM displayed greatly enhanced cellular uptake, higher cytotoxicity and a stronger anti-metastasis effect against mouse breast cancer cell line 4T1. In 4T1 tumor-bearing mice treated with DSM (twice a week for 3 weeks), the inhibition rate on tumor growth and metastasis reached 71.9% and 80.1%, respectively. These results reveal that DSM might be a promising drug delivery system for metastatic breast cancer therapy.
研究领域:
肿瘤学
·
药剂学
·
生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）