INTERNATIONAL IMMUNOPHARMACOLOGY
·
2016
·
IF 2.551
Zhilin Qi,Shimei Qi,Liefeng Ling,Jun Lv,Zunyong Feng
Salidroside (SAL) is an active ingredient isolated from the Rhodiola rosea , has potent anti-inflammatory effect, but the mechanism is still elusive. The purpose of this study is to verify the effects of SAL on LPS-induced inflammatory response and investigate the possible underlying molecular mechanism. RAW264.7 cells were pre-incubated with SAL for 2 h, then stimulated with or without LPS for another 16 h. The levels of TNF-α, MCP-1, IL-6, and PGE2 were detected by ELISA , and the production of NO was determined by nitrite analysis. The expression levels of nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) were detected by Western blotting . In RAW264.7 cells and murine peritoneal macrophages, the activation of signal molecules was also measured by Western blot. The nuclear translocation of STAT3 was determined by Laser confocal and nucleocytoplasmic separation experiments. Our results showed that SAL attenuated the productions of TNF-α, IL-6, MCP-1, PGE2 and NO dose dependently. SAL also suppressed LPS-induced expressions of iNOS and COX-2 significantly. Further studies revealed that SAL down-regulated the phosphorylation of JAK2-STAT3 signaling pathway and reduced the nuclear translocation of STAT3 induced by LPS in RAW264.7 cells and primary peritoneal macrophages. In addition, consistent with the results in vitro, in the model of mice acute lung injury (ALI) induced by LPS, SAL reduced the infiltration of inflammatory cells and decreased the levels of serum TNF-α and IL-6 obviously. Taken together, these data indicated that SAL exerted anti-inflammatory action via down-regulating LPS-induced activation of JAK2-STAT3 pathway and suppressing STAT3 transfer into the nucleus at least in part.
研究领域:
药理学
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免疫学
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细胞生物学
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炎症
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DOI
PubMed
高影响因子
BIOCATALYSIS AND BIOTRANSFORMATION
·
2023
·
IF 1.8
Jue Chen,Qibin Cheng,Qianqian Ma,Yuqi Wu,Liwei Zhang
This study aimed to establish a novel method for catalysing salidroside synthesis by immobilized β-D-glucosidase with deep eutectic solvents (DESs) as a new green non-aqueous medium. To this end, the catalytic properties of β-D-glucosidase (i.e. activity, stability, and enzymatic properties) were analysed within sixteen different DESs systems. Although most DESs significantly improved enzyme stability, they also reduced enzymatic activity. This was verified at the molecular level by employing fluorescence spectroscopy to evaluate conformational changes in β-D-glucosidase molecules. Subsequently, chitosan microspheres were used to immobilize β-D-glucosidase; the structures of the microspheres and immobilized enzyme were observed by scanning electron microscopy (SEM). Through single factor experiments and application of a response surface design, the optimal conditions for production of salidroside by the reaction of tyrosol with immobilized β-D-glucosidase were established. These conditions comprised 80 vol% ChCl/G (1:2), 50 °C reaction temperature, 5.8 pH, 100 h reaction time, 45 U/mL enzyme dosage, and a tyrosol/D-glucose molar ratio of 10. Under these conditions, the average conversion rate of the tyrosol substrate was 31.6%. Moreover, a salidroside crude product was obtained with a purity >70% (g/g) and a substrate conversion rate of immobilized β-D-glucosidase >50% of its initial value after five repeated uses. Collectively, this study establishes a novel green reaction system for the efficient preparation of salidroside and other glycoside compounds, while also providing a theoretical foundation for the analysis of β-D-glucosidase catalytic reactions in DESs systems.
研究领域:
生物催化
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酶工程
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绿色化学
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药学
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化工
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DOI
高影响因子
Journal of Functional Biomaterials
·
2023
·Vol. 14
·期 3
·150
·
IF 4.8
Shengnan He,Fang Xie,Wuyue Su,Haibin Luo,Deliang Chen,Jie Cai,Xuechuan Hong
Atopic dermatitis (AD) is the most common heterogeneous skin disease. Currently, effective primary prevention approaches that hamper the occurrence of mild to moderate AD have not been reported. In this work, the quaternized β-chitin dextran (QCOD) hydrogel was adopted as a topical carrier system for topical and transdermal delivery of salidroside for the first time. The cumulative release value of salidroside reached ~82% after 72 h at pH 7.4, while in vitro drug release experiments proved that[email protected]([email protected]) has a good, sustained release effect, and the effect of[email protected]on atopic dermatitis mice was further investigated.[email protected]could promote skin repair or AD by modulating inflammatory factors TNF-α and IL-6 without skin irritation. The present study also evaluated NIR-II image-guided therapy (NIR-II, 1000–1700 nm) of AD using[email protected]The treatment process of AD was monitored in real-time, and the extent of skin lesions and immune factors were correlated with the NIR-II fluorescence signals. These attractive results provide a new perspective for designing NIR-II probes for NIR-II imaging and image-guided therapy with[email protected]Keywords:the quaternized β-chitin/dextran hydrogel;imaging in the second near-infrared window (NIR-II);atopic dermatitis;Rhodiola rosea;treatment
研究领域:
药学
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生物医学工程
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材料科学
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皮肤病学
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产品关联
DOI
PubMed
高影响因子
MEDICINAL CHEMISTRY RESEARCH
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2012
·Vol. 22
·期 5
·2524-2530
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IF 1.271
Guo Yibing,Zheng Cheng,Xu Wen,Si Yongxing,Dou Sufeng,Yang Yumin
Abstract Salidroside, a phenylpropanoid glycoside isolated from a traditional Chinese medicinal plant Rhodiola rosea L. displays a broad spectrum of pharmacological properties. It has been found to play a hepatoprotective role in liver diseases through inhibiting apoptosis of hepatocytes and proliferation of hepatic stellate cells, decreasing serum aminotransferase, reversing hepatic fibrosis, and improving liver function. In this study as an ongoing study on the discovery and development of new hepatoprotective agents, about 12 novel glycosides were synthesized, and 2,2-diphenyl-1-picrylhydrazyl radical scavenge activity of each glycoside was evaluated. 2-(3,4,5-trihydroxyphenyl)ethyl β- d -glucopyranoside ( 4g ) and 2-(3,4,5-trihydroxyphenyl)ethyl β- d -galactopyranoside ( 4h ) exhibited significant activity prior to salidroside with an IC 50 value of 38.05 and 35.85 μM, respectively. The hepatoprotective effect of compounds 4g and 4h on CCl 4 -induced cytotoxicity in LO2 cells was assessed for further research. Graphical abstract 2-(3,4,5-Trihydroxyphenyl)ethyl β- d -glucopyranoside ( 4g ) and 2-(3,4,5-trihydroxyphenyl)ethyl β- d -galactopyranoside ( 4h ) exhibited significant hepatoprotective activity prior to salidroside.
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DOI
高影响因子
MICROCHEMICAL JOURNAL
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2024
·
IF 4.9
Qingbin Xu,Linchun Shi,Weijun Kong,Jing Wang,Peigen Xiao,Jinxin Liu
A meticulously engineered bacillus-shaped CoNi ZIF-MXene@MWCNT carbon cloth (CC) composite was synthesized through a one-step immersion method, which was employed in the development of a novel electrochemical (EC) sensor for the sensitive detection of salidroside (SAL) in Rhodiola. Characterization of the CoNi ZIF-MXene@MWCNT CC was conducted using scanning electron microscopy (SEM), X-ray photoelectron spectroscopy (XPS), energy-dispersive X-ray spectroscopy (EDS), and EC methods. The bacillus-shaped composite showcased an exceptionally high rate of active site exposure, superior conductivity, and electrocatalytic efficiency, attributed to the synergistic effects of the constituent materials. The remarkable electrocatalytic capability facilitated the redox reaction of SAL, marked by a significant enhancement in the current signal. This led to a concentration-dependent response enabling the quantitative detection of SAL. The mechanism of the redox reaction might be the oxidation of the phenolic hydroxyl group of SAL. Demonstrating high sensitivity, selectivity, and stability, this novel bacillus-shaped composite-based EC sensor achieved a low detection limit (LOD) of 0.0958 µ g/mL for SAL, within an effective linear range of 0.5–500 µg/mL. Importantly, the EC sensor proved to be adept at practical detection of SAL in Rhodiola samples with complex matrices, and the salidroside content of Rhodiola crenulata was much higher than that of Rhodiola rosea , indicating that Rhodiola crenulata may have a higher medicinal value, offering a promising avenue for rapid and sensitive detection of SAL.
研究领域:
电化学
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材料科学
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分析化学
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药学
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DOI
高影响因子
Discovery Medicine
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2024
·Vol. 36
·期 181
·266-277
·
IF 2
Luo X,Liao H,Peng J,Jiang X
Background Osteoarthritis (OA) is a common disease that causes pain to many older adults. Because the pathogenesis is not fully elucidated, effective drug therapies are currently lacking. This study aimed to determine how salidroside (Sal)-mediated reduction of osteoarthritis development in mice worked and to identify the underlying mechanism. Methods Using in vitro experiments, ATDC5 cells were treated with various concentrations of Sal and interleukin (IL)-1β for 24 hours to mimic OA. An enzyme-linked immunosorbent assay (ELISA) was conducted to detect the production of pro-inflammatory cytokines and reactive oxygen species (ROS). Western blotting was performed to observe the nuclear factor-kappa B (NF-κB) and nuclear factor erythroid 2-related factor 2 (Nrf2) pathways. In in vivo experiments, pathological examination was used to assess the effects of Sal on alleviating OA progression in mice. Nrf2 signaling and its downstream proteins were further tested by immunofluorescence analysis. Results The results showed that both pro-inflammatory cytokines and ROS were significantly reduced following Sal treatment in a concentration-dependent manner. Western blotting revealed that Sal could inhibit the expression of the NF-κB/hypoxia-inducible factor-2α pathway and activate the Nrf2/heme oxygenase-1 pathway. In vivo experiments showed that the cartilage surface in the saline-treated group eroded to a greater extent than the Sal-treated groups ( p < 0.001). Immunohistochemistry analysis revealed that matrix metallopeptidase (MMP) 9, MMP13, and a disintegrin and metalloproteinase with thrombospondin motifs-5 (ADAMTS-5) decreased expression level. In contrast, collagen-II and aggrecan increased in the Sal-treated groups compared to the saline-treated group. Conclusions Our findings indicate that Sal can alleviate OA progression by promoting anti-oxidant expression and inhibiting degradation enzyme expression. These findings suggest that Sal inhibits the NF-κB pathway and its downstream targets through up-regulating the Nrf2 pathway.
研究领域:
医学
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药理学
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DOI
PubMed
高影响因子
MOLECULES
·
2026
·Vol. 31
·期 19
·3575
·
IF 5.1
Xinran Wang,Ruixue Huang,Gan Yang,Yuxia He,Shi Yin
Salidroside is a bioactive compound extracted from the traditional Chinese medicinal plantRhodiola roseathat exerts differential regulatory effects on cell viability depending on cell type and physiological state. Sertoli cells are important testicular somatic cells that play multiple roles in nourishing, protecting, and supporting spermatogenic cells. Currently, the regulatory effects and underlying mechanisms of salidroside on Sertoli cells remain unclear. This study investigated the effects of different concentrations of salidroside on the viability and regulatory mechanisms of TM4 cells (mouse Sertoli cell line). The results showed that within the range of 25–600 μM, cell viability decreased with increasing salidroside concentration. Treatment with 600 μM salidroside inhibited proliferation, promoted apoptosis, and suppressed the expression of key genes related to Sertoli cell function. Transcriptome sequencing revealed that several glycolysis-related genes, includingLdha,Pfkl,Eno3, andEno1b, were significantly downregulated in salidroside-treated cells, accompanied by marked reductions in key glycolytic metabolites, including fructose-1,6-diphosphate (FDP), pyruvate, lactic acid, and ATP. Notably, overexpression of lactate dehydrogenase A (Ldha) rescued cell viability and proliferation, suppressed apoptosis, elevated both intracellular and extracellular lactate and ATP levels, and partially restored functional gene expression in 600 μM salidroside-treated cells. Overall, this study provides hitherto undocumented evidence of the regulatory effects and mechanisms of salidroside on TM4 cells, identifying theLdha–glycolytic axis as an in vitro cellular target of high-dose salidroside in Sertoli cells, which may inform future in vivo reproductive safety profiling pending pharmacokinetic validation.
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DOI
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2024
·
IF 7.7
Guosi Li,Wei Wang,Heng Guo,Shanyong Yi,Fang Wang,Shiping Huang,Nan Hu,Qilin Xu,Yongjun Zang,Bangxing Han,Xinjian Yin
Microbial glycosyltransferases efficiently synthesize glucosides and have garnered increasing interest. However, limited regioselectivity has impeded their broad application, particularly in the pharmaceutical industry. In this study, the UDP-glycosyltransferase YjiC from Bacillus licheniformis ( Bl YjiC) was engineered to achieve the bidirectional regioselective glycosylation of tyrosol and its derivatives. Initially, site-directed saturation mutagenesis was performed on two newly identified substrate-binding cavities in the acceptor pocket of Bl YjiC to provide a comprehensive blueprint of the interplay between mutations and function (mutability landscape). Iterative saturation mutagenesis was performed, guided by the mutability landscape. Two highly regioselective mutants M6 (M112L/I325Y/L70R/Q136E/I67E/M77R) and M2’ (M112D/I62L) were generated, exhibiting >99 % regioselectivity toward the alcoholic and phenolic hydroxyl of tyrosol, respectively, compared with the wild-type (product mixture: 51:49 %). Both mutants exhibited excellent regioselectivity toward several dihydroxy phenolic substrates, offering valuable biocatalysts for the regioselective synthesis of glucosides. Their application was confirmed in a short synthesis of salidroside (3.6 g/L) and icariside D2 (2.4 g/L), which exhibited near-perfect regioselectivity. This study provides valuable insights into future protein engineering of similar enzymes and opens new avenues for their practical applications.
研究领域:
生物化学
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合成生物学
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制药工程
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产品关联
DOI
PubMed
高影响因子
LWT-FOOD SCIENCE AND TECHNOLOGY
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2024
·
IF 6
Qian Zhang,Lin Li,Yu-Qiao Wang,Hai-Tao Wu,Bei-Wei Zhu
A water-in-oil-in-water (W/O/W) emulsion for the encapsulation of salidroside (Sal) was constructed. This study aimed to detect the impact of whey protein isolate (WPI) on the microstructure and stability of Sal W/O/W emulsion, which was prepared by two-step emulsification. First , Sal and sodium alginate (SA) were added to the inner water phase, and polyglycerol polyricinoleate (PGPR) was added to the oil phase to prepare a water-in-oil (W/O) emulsion. Second , different concentrations of WPI were added to the outer water phase containing SA to prepare a Sal W/O/W emulsion. The microstructure, stability, moisture distribution, rheological properties, and encapsulation efficiency of Sal were detected. The results showed that the particle size and the size distribution range became smaller and narrower with increasing WPI concentration . When the concentration of WPI was greater than 2%, the double-layer structure remained stable over 28 days of storage at 4 °C. Moreover, when the WPI concentration reached 4%, the entrapment efficiency of Sal was the highest. These results indicated that the optimum concentration of WPI was 4%.
研究领域:
食品科学
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药学
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材料科学
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产品关联
DOI
高影响因子
Arabian Journal of Chemistry
·
2023
·
IF 6
Zijie Liu,Xingbin Ma,Shuyu Li,Jiajie Qiu,Siyu Liu,Zhifeng Huang,Hongling Lin,A.M. Abd El-Aty
This study focuses on creating a green drug release system using a food-grade titanium dioxide (TiO 2 ) material through surface molecular imprinting. Salidroside (SD) was chosen as the template molecule to synthesize molecularly imprinted polymers (SDT-MIP) utilizing TiO 2 -doped chitosan oligosaccharides as the functional monomer. The SDT-MIPs were characterized using multiple techniques, and their effectiveness was evaluated through an in vitro release study. Additionally, the affinity of SDT-MIPs toward the template molecule was examined using Langmuir and Freundlich adsorption models. The Langmuir model revealed a maximum capacity of 170.41 mg/g and an imprinted factor of 3.4. The study demonstrated that drug release from the SDT-MIPs in simulated gastrointestinal fluid primarily occurred through pure Fick diffusion. The release kinetics exhibited diffusion coefficients ranging from 3.38 × 10 -3 cm 2 /s to 2.78 × 10 -2 cm 2 /s, indicating their biocompatibility and potential application in drug delivery. Furthermore, the SDT-MIP demonstrated no adverse impact on cell viability even at concentrations as high as 1000 μg/mL. The survival rate of cells cultivated in the presence of SDT-MIP solution exceeded 120 ± 12.46%, providing evidence of the excellent biocompatibility and absence of cytotoxicity associated with SDT-MIP. The SDT-MIP possesses favorable sustained-release properties and lacks toxicity, allowing novel drug delivery systems to be created.
研究领域:
药学
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材料科学
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生物技术
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纳米技术
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药物递送系统
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产品关联
DOI
高影响因子
Diabetes Metabolic Syndrome and Obesity-Targets and Therapy
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2019
·
IF 3.319
Qi Feng,Chen Liu,Wei Gao,Xiao-ling Geng,Ning Dai
Purpose Oxidative stress plays an important role in the pathogenesis of non-alcoholic fatty liver disease (NAFLD). TRPM2 ion channel functions as a molecular sensor for oxidative stress. The aim of this study was to examine the protective effects of Salidroside, a powerful antioxidative plant, on TRPM2 in an established in vitro model of NAFLD. Methods NAFLD model was established by palmitic acid (PA) in hepatic L02 cell lines and was added to the media at a final concentration of 400 μM. Cells were used as normal group, PA group and PA receiving varied concentrations of Salidroside (75μg/mL, 150μg/mL, 300μg/mL). After treating 24 hrs, MTT assay was used to detect cell viability, and ALT level was measured using an appropriate kit assay. Intracellular lipid accumulation was observed by Oil red O staining. Cytosolic Ca 2+ concentrations were evaluated by flow cytometer with Fluo-3/AM. Quantitative RT-PCR was used to measure the mRNA expression of TRPM2, IL-1β and IL-6, and the protein expressions of TRPM2, p-CaMKII and autophagy (LC3B, p62) were determined using Western blot. Results Treatment with Salidroside effectively restored liver injury and alleviated lipid droplet deposition in a dose-dependent manner, which was associated with inhibition of TRPM2/Ca 2+ /CaMKII pathway. Additionally, autophagic clearance was enhanced by intervention with Salidroside in a dose-dependent manner. Further investigation indicated that Salidroside down-regulated the mRNA expression of IL-1β and IL-6-pro-inflammatory cytokines. Conclusion These results suggest that Salidroside could alleviate inflammatory injury and steatosis via autophagy activation mediated by downregulation of the TRPM2/Ca 2+ /CaMKII pathway. Targeting the TRPM2 ion channel is a novel treatment strategy for oxidative stress-induced liver in NAFLD.
研究领域:
药理学
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细胞生物学
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分子生物学
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肝病学
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DOI
PubMed
高影响因子
PHYTOTHERAPY RESEARCH
·
2021
·Vol. 35
·期 10
·5767-5780
·
IF 5.882
Lin Zhu,Zhenchao Liu,Yuqian Ren,Xiaolin Wu,Yingjuan Liu,Tingting Wang,Yizhao Li,Yusheng Cong,Yunliang Guo
Studies have found that salidroside, isolated from Rhodiola rosea L , has various pharmacological activities, but there have been no studies on the effects of salidroside on brain hippocampal senescence. The purpose of this study was to investigate the mechanistic role of salidroside in hippocampal neuron senescence and injury. In this study, long-term cultured primary rat hippocampal neurons and naturally aged C57 mice were treated with salidroside. The results showed that salidroside increased the viability and MAP2 expression, reduced β-galactosidase (β-gal) levels of rat primary hippocampal neurons. Salidroside also improved cognition dysfunction in ageing mice and alleviated neuronal degeneration in the ageing mice CA1 region. Moreover, salidroside decreased the levels of oxidative stress and p21, p16 protein expressions of hippocampal neurons and ageing mice. Salidroside promoted telomerase reverse transcriptase (TERT) protein expression via the phosphatidylinositol-3-kinase (PI3K)/protein kinase B (Akt) pathway. In conclusion, our findings suggest that salidroside has the potential to be used as a therapeutic strategy for anti-ageing and ageing-related disease treatment.
研究领域:
神经科学
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药理学
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衰老研究
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分子生物学
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DOI
PubMed
高影响因子
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