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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2023 · IF 8.2

Structural characterization and anti-inflammatory activity of polysaccharides from Astragalus membranaceus

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
✓ 已验证 产品关联 DOI PubMed 高影响因子
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MACROMOLECULAR CHEMISTRY AND PHYSICS · 2011 ·Vol. 212 ·期 17 ·1900-1909 · IF 2.437

Fabrication of Polyaniline: Nail/Spindle-Shaped Morphology

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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ACS Sustainable Chemistry & Engineering · 2016 · IF 5.267

Homogeneous Dispersion of Cellulose Nanofibers in Waterborne Acrylic Coatings with Improved Properties and Unreduced Transparency

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.

CAS / MDL: 7727-54-0
研究领域: 材料科学 · 化学工程
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Materials Today Communications · 2025 · IF 4.5

LDHs-APS/GO composite coating on AZ31B magnesium alloy for enhanced anti-corrosion property

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.

CAS / MDL: 7727-54-0 1310-73-2
研究领域: 材料科学 · 腐蚀与防护
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2020 · IF 5.162

Characterization and antitumor activity of novel exopolysaccharide APS of Lactobacillus plantarum WLPL09 from human breast milk

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 · 分子生物学 · 药理学
✓ 已验证 DOI PubMed 高影响因子
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ACTA PHARMACOLOGICA SINICA · 2016 ·Vol. 37 ·期 4 ·545-554 · IF 3.166

Absorptive interactions of concurrent oral administration of (+)-catechin and puerarin in rats and the underlying mechanisms

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
✓ 已验证 DOI PubMed 高影响因子
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ACTA PHARMACOLOGICA SINICA · 2013 ·Vol. 34 ·期 7 ·939-950 · IF 2.354

Characterization of a novel curcumin analog P1 as potent inhibitor of the NF-κB signaling pathway with distinct mechanisms

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
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ACTA PHARMACOLOGICA SINICA · 2015 ·Vol. 36 ·期 7 ·863-873 · IF 2.912

Intestinal absorption characteristics of imperialine: in vitro and in situ assessments

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.

CAS / MDL: 52-53-9
研究领域: 药理学 · 中药学 · 药学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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ACTA PHARMACOLOGICA SINICA · 2018 ·Vol. 39 ·期 10 ·1681-1692 · IF 3.562

Delivery of mitochondriotropic doxorubicin derivatives using self-assembling hyaluronic acid nanocarriers in doxorubicin-resistant breast cancer

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
✓ 已验证 DOI PubMed 高影响因子
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ACTA PHARMACOLOGICA SINICA · 2012 ·Vol. 33 ·期 7 ·909-917 · IF 1.953

Tissue cholesterol content alterations in streptozotocin-induced diabetic rats

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.

CAS / MDL: 57-88-5
研究领域: 内分泌学 · 代谢学 · 药理学 · 神经科学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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ACTA PHARMACOLOGICA SINICA · 2016 ·Vol. 37 ·期 7 ·941-949 · IF 3.166

Silibinin and indocyanine green-loaded nanoparticles inhibit the growth and metastasis of mammalian breast cancer cells in vitro

Sun Hui-ping,Su Jing-han,Meng Qing-shuo,Yin Qi,Zhang Zhi-wen,Yu Hai-jun,Zhang Peng-cheng,Wang Si-ling,Li Ya-ping

Aim: To improve the therapeutic efficacy of cancer treatments, combinational therapies based on nanosized drug delivery system (NDDS) has been developed recently. In this study we designed a new NDDS loaded with an anti-metastatic drug silibinin and a photothermal agent indocyanine green (ICG), and investigated its effects on the growth and metastasis of breast cancer cells in vitro . Methods: Silibinin and ICG were self-assembled into PCL lipid nanoparticles (SIPNs). Their physical characteristics including the particle size, zeta potential, morphology and in vitro drug release were examined. 4T1 mammalian breast cancer cells were used to evaluate their cellular internalization, cytotoxicity, and their influences on wound healing, in vitro cell migration and invasion. Results: SIPNs showed a well-defined spherical shape with averaged size of 126.3±0.4 nm and zeta potential of −10.3±0.2 mV. NIR laser irradiation substantially increased the in vitro release of silibinin from the SIPNs (58.3% at the first 8 h, and 97.8% for the total release). Furthermore, NIR laser irradiation markedly increased the uptake of SIPNs into 4T1 cells. Under the NIR laser irradiation, both SIPNs and IPNs (PCL lipid nanoparticles loaded with ICG alone) caused dose-dependent ablation of 4T1 cells. The wound healing, migration and invasion experiments showed that SIPNs exposed to NIR laser irradiation exhibited dramatic in vitro anti-metastasis effects. Conclusion: SIPNs show temperature-sensitive drug release following NIR laser irradiation, which can inhibit the growth and metastasis of breast cancer cells in vitro .

CAS / MDL: 22888-70-6
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
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ACTA PHARMACOLOGICA SINICA · 2016 ·Vol. 37 ·期 8 ·1091-1100 · IF 3.166

Hesperidin alleviates rat postoperative ileus through anti-inflammation and stimulation of Ca2+-dependent myosin phosphorylation

Xiong Yong-jian,Chu Hong-wei,Lin Yuan,Han Fang,Li Ya-chan,Wang Ai-guo,Wang Fu-jin,Chen Da-peng,Wang Jing-yu

Aim: Postoperative ileus (POI) is a postoperative dysmotility disorder of gastrointestinal tract, which remains one of the most perplexing problems in medicine. In the present study we investigated the effects of hesperidin, a major flavonoid in sweet oranges and lemons, on POI in rats. Methods: SD rats were administered hesperidin (5, 20, and 80 mg·kg −1 ·d −1 , ig) for 3 consecutive days. POI operation (gently manipulating the cecum for 1 min) was performed on d 2. The gastrointestinal motility and isolated intestinal contraction were examined 1 d after the operation. Then the myosin phosphorylation and inflammatory responses in cecum tissue were assessed. Smooth muscle cells were isolated from rat small intestine for in vitro experiments. Results: The gastric emptying and intestinal transit were significantly decreased in POI rats, which were reversed by administration of hesperidin. In ileum and cecum preparations of POI rats in vitro , hesperidin (2.5–160 μmol/L) dose-dependently increased the spontaneous contraction amplitudes without affecting the contractile frequency, which was blocked by the myosin light chain kinase (MLCK) inhibitor ML-7 or verapamil, but not by TTX. Furthermore, administration of hesperidin increased the phosphorylation of MLC 20 in the cecum tissue of POI rats. Moreover, administration of hesperidin reversed the increased levels of inflammatory cytokines, iNOS and COX-2 in cecum tissue of POI rats. In freshly isolated intestinal smooth muscle cells, hesperidin (5–80 μmol/L) dose-dependently increased the intracellular Ca 2+ concentration as well as the phosphorylation of MLC 20 , which was abrogated by ML-7 or siRNA that knocked down MLCK. Conclusion: Oral administration of hesperidin effectively alleviates rat POI through inhibition of inflammatory responses and stimulation of Ca 2+ -dependent MLC phosphorylation.

研究领域: 药理学 · 胃肠病学 · 外科
✓ 已验证 DOI PubMed 高影响因子
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