NEW JOURNAL OF CHEMISTRY
·
2024
·
IF 2.7
Yuanbin Li,Wu Yi,Haowei Chen,Bao Han,Bo Ruan,Zhong Xiaoyu,Li ShanShan,Yifan Chen,Tao Peng,Jiaheng Zhang,Fang Wang
Betaine/ascorbyl glucoside (Bet/AA-2G) deep eutectic solvents (DES) composed of betaine and ascorbyl glucoside had been successfully used to improve the solubility of silymarin in this study. Under appropriate conditions, the solubility of silymarin in a 5 wt% Bet/AA-2G DES solution increased by 17.7% and 60.9% compared to a 50 wt% 1,3-butanediol solution and a 50 wt% ethanol solution, respectively. In addition, quantum chemical simulations showed that silymarin has a strong binding capacity to Bet/AA-2G DES and can remain stable after binding. The combination of Bet/AA-2G DES with silymarin enhanced the skin permeability and antioxidant capacity of silymarin. Moreover, SM-DES promoted the synthesis of type I collagen and significantly reduced the expression of MMP-1, indicating potential anti-wrinkle and firming properties. Overall, Bet/AA-2G DES showed great potential for improving the solubility and stabilizing the bioactivity of silymarin.
研究领域:
药学
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化学
·
化妆品科学
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材料科学
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产品关联
DOI
高影响因子
Small Science
·
2025
·
IF 8.3
Yong Li,Youdong Zhou,Yinqiu Tan,Gang Deng
Subarachnoid hemorrhage (SAH) is a common hemorrhagic cerebrovascular disease with high disability rate and high mortality. Early brain injury (EBI) is the main cause of high mortality and delayed neurological dysfunction in patients with SAH. Neuroinflammation is the important pathological processes of EBI.We prepared Silymarin nanoparticles (SIM NPs) through the solvent precipitation method and investigated their role in combating EBI following SAH in mice. We found that SIM NPs with a diameter of 150 nm have the strongest ability to cross the blood-brain barrier. SIM nanoparticles are spherical and contain irregular particles inside, which may be composed mainly of silibinin and assembled through hydrogen bonding. Further in vivo experiments showed that SIM NPs improved short-term neurological dysfunction in SAH mice, reduced cortical neural damage, and reduced EBI inflammation through the Nrf2/STING pathway. Finally, water maze experiments showed that SIM NPs can improve long-term memory and learning ability in SAH mice. Based on the above results, we conclude that silymarin nanoparticles can reduce EBI after SAH by inhibiting the Nrf2/STING pathway, inhibiting neuroinflammation and M1 polarization of microglia.
研究领域:
神经科学
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药理学
·
分子生物学
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产品关联
DOI
PubMed
高影响因子
PESTICIDE BIOCHEMISTRY AND PHYSIOLOGY
·
2024
·
IF 4.2
Xinyu Wu,Jiawei Chen,Kaixin Ping,Yan Xia,Mengxin Li,Yannan Xiang,Huimao Feng,Jingquan Dong
Long-term residue of difenoconazole (DFZ) in the environment caused multiple organ damage to aquatic organisms. Due to the potential hepatoprotective and neuroprotective properties of silybin (SIL), we hypothesized that SIL could alleviate growth inhibition, liver, and brain damage in carp induced by DFZ exposure. The in vivo experiments were divided into the Control group, the SIL group, the DFZ group and the DFZ + SIL group. The exposure concentration of DFZ was 0.39 mg/L, and the therapeutic dose of SIL was 400 mg/kg. The whole experiment lasted for 30 days. SIL was also found to reduce hepatic injury and lipid metabolism based on H&E staining, oil red O staining, and measurement of serum and liver tissue levels of ALT, AST, LDH, TG, and TC. Similarly, SIL reduced brain damage after DFZ exposure, according to H&E staining and detection transcription level of the ZO-1, ZO-2, occludin, and Claudin7 in carp brain. In terms of mechanism, the results showed that SIL inhibited the excessive production of ROS in liver and brain tissues, increased the activity of antioxidant enzymes (T-AOC, SOD, CAT) and resist oxidative stress. Also, SIL promoted the production of anti-inflammatory factors (TGF-β1 and IL-10) and inhibited the expression of pro-inflammatory factors (TNF-α and IL-6) to reduce the inflammatory response in liver and brain tissues caused by DFZ. ln terms of ferroptosis, by lowering iron levels, upregulating ferroptosis-related genes (GPX4, SIC7A11, GCLC), and downregulating the expression of NCOA4, STEAP3, COX2, and P53, SIL was able to inhibit ferroptosis of liver and brain tissues of carp. In addition, SIL restored the reduced mitochondrial membrane potential (MMP) level and inhibited apoptosis as measured by MMP level detection, TUNEL staining, and apoptosis gene transcript levels. In this study, we analyzed the interactions between genes and proteins associated with oxidative stress, inflammation, ferroptosis and apoptosis using the String database and ranked the nodes in the network using the Cytoscape plugin Cytohubba, and found that P53, Caspase3, TNF-α, IL-6 and Bcl-2 were the key hub genes. Our study not only revealed the multiple pharmacological activities of SIL, but also provided a reference for the prevention and reduction pesticide hazards to aquatic organisms.
研究领域:
毒理学
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药理学
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环境科学
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神经科学
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肝病学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
·
2025
·
IF 3.1
Jianying Liu,Yan Chen,Zhifeng Cen,Meiqi Hong,Binzhi Zhang,Xia Luo,Leqi Wang,Shasha Li,Xue Xiao,Qinqiang Long
The incidence of acute liver injury is increasing and poses a significant threat to human health. Ganoderma lucidum spore oil (GLSO), a lipid substance extracted from Ganoderma lucidum spore powder using supercritical CO 2 technology, has been investigated for its potential to prevent acute liver injury. However, the specific mechanism underlying the protective effects of GLSO remains incompletely understood. In this study, we investigated the preventive effect of GLSO on acute liver injury in rats, focusing on the gut microbiome and serum metabolomics. GLSO effectively alleviated liver dysfunction and reduced inflammation, leading to the prevention of acute liver injury in rats. Serum metabolomics analysis revealed that GLSO primarily modulated lipid metabolic pathways related to glycerophospholipid metabolism and sphingolipid metabolism. Specifically, GLSO decreased the levels of metabolites such as lysophosphatidylcholine (LPC), glycerophosphatidylcholine (GPC), and sphinganine 1-phosphate (SA1P), while increasing the levels of phosphatidylglycerol (PG) and digalactosylceramide (DGC). Gut microbiomics data indicated that GLSO effectively regulated the composition of the gut microbiota in rats with acute liver injury. Specifically, it increased the abundance of Firmicutes and decreased the abundance of Proteobacteria . Mantel test correlation analysis revealed a close relationship between gut microbial Burkholderiales and lipid metabolites in GLSO-mediated prevention of acute liver injury. GLSO exerts its preventive effects on acute liver injury by remodeling the gut microbiota and regulating lipid metabolism. These findings provide novel insights and potential directions for the development of new drugs targeting acute liver injury.
研究领域:
药理学
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肝病学
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微生物组研究
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代谢组学
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产品关联
DOI
PubMed
高影响因子
Frontiers in Pharmacology
·
2025
·
IF 4.8
Jie Li,Xiujuan Yang,Xiaolong Lian,Baojian Li,Quhuan Ma,Lingling Yang,Guangmiao Gao,Yi Deng,Zhijun Yang
Cisplatin (CP), a widely used antineoplastic drug, could induce hepatotoxicity and is also one of the most common reasons for drug-induced liver injury (DILI). Licorice (Chinese name GanCao, GC) is a commonly used herbal drug in traditional Chinese medicine (TCM) that has been shown to treat liver diseases and DILI. CP has been documented to induce apoptosis through the promotion of endoplasmic reticulum (ER) stress. However, the exact role of ER stress in the pathogenesis of CP-induced hepatotoxicity remains unclear. A rat DILI model was constructed through intraperitoneal injection of CP, and the anti-DILI effect of GC was detected by liver coefficients, liver function tests, pathological staining, and oxidative stress indices. Additionally, the ER stress and apoptosis indices were investigated by quantitative real-time PCR (qRT-PCR), Western blotting, and immunofluorescence (IF) on CP-induced toxicity in rat liver tissues and LO2 cells. In the model group, liver function indicators significantly elevated, liver lesions more pronounced, and the reactive oxygen species (ROS) level in the liver increased, the expression of ER stress markers, apoptosis factors, and indicators related to the protein kinase RNA-like ER kinase/activating transcription factor 4/C/EBP homologous protein (PERK/ATF4/CHOP) pathway significantly elevated. Treatment of the CP-induced toxicity in the rat model with GC significantly improved liver function, reduced liver lesions, decreased liver ROS. In addition, GC significantly inhibited the expression of ER stress markers, apoptosis factors, and indicators related to PERK/ATF4/CHOP pathway, demonstrating the anti-CP-induced hepatotoxicity effect of GC. In this study, we verified the protective effect of GC in CP-induced hepatotoxicity in rats and clarified its mechanisms related to ER stress and apoptosis.
研究领域:
药理学
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毒理学
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肝脏病学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
FITOTERAPIA
·
2024
·
IF 2.5
Ling Jiang,Cai-Bo Tian,Rui-Han Ye,Nian Shi,Xing-Chao He,Yun-Li Zhao,Xiao-Dong Luo
Drug-induced liver injury caused acute hepatic failure and hepatitis frequently. In this investigation, kakuol and asarinin reduced the levels of serum alanine transaminase (ALT), aspartate transaminase (AST) and malondialdehyde (MDA) dramatically, and ameliorated the pathological damage of liver tissues in APAP-induced mice. Furthermore, both compounds increased the viabilities of APAP-induced L-O2 cells and extracellular glutathione (GSH) levels accompanied significantly by reducing the level of intracellular ROS in vitro . In addition, HSP90AA1/CDK2/mTOR signaling pathway and five target proteins (CDK2, HSP90AA1, HRAS, MMP1, mTOR) were proposed from network pharmacology and molecular docking prediction, and then the up-regulation of protein expression of CDK2, mTOR and down-regulation of HSP90AA1, HRAS, MMP1 by kakuol and asarinin in western blotting supported their mechanism.
研究领域:
药理学
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分子生物学
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毒理学
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肝病学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Journal of Future Foods
·
2026
·
IF 10.6
Bailin Li,Fen Liu,Yaoguang Huang,Sui Kiat Chang,Chenqi Niu,Pu Liu,Xiancai Li,Liyuan Yao,Sheng-Xiang Qiu
Pigeon pea ( Cajanus cajan (L.) Millsp.), a plant with documented safety and dual use in food and traditional medicine, holds promise for developing hepatoprotective agents. This study aimed to evaluate its potential to mitigate high-fat diet (HFD)-induced hepatic steatosis. We investigated a stilbene-enriched extract (EX) from pigeon pea leaves and its major constituent, cajanstilbenoid A (CSA). In HFD-fed mice, both EX and CSA significantly reduced body weight, liver index, lipid accumulation and serum cholesterol/triglyceride levels. CSA also ameliorated oxidative stress and improved liver function markers. Mechanistic studies revealed that CSA acted as a selective agonist of peroxisome proliferator-activated receptor alpha (PPARα): Network pharmacology, transcriptomics, and molecular docking predicted PPARα as a target; this was confirmed by cellular thermal shift assay (CETSA), drug affinity responsive target stability assays (DARTS) and surface plasmon resonance (SPR), which demonstrated direct binding. Crucially, siRNA-mediated knockdown of PPARα in HepG2 cells abolished the lipid-lowering effects of CSA. Our findings demonstrated that CSA alleviated HFD-induced hepatic steatosis primarily by activating the PPARα pathway, reducing oxidative stress and promoting lipid metabolism. This study highlighted the therapeutic potential of CSA for non-alcoholic fatty liver disease and underscored pigeon pea as a valuable medicinal and edible resource.
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF CONTROLLED RELEASE
·
2020
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IF 7.727
Meirong Huo,Honglan Wang,Ying Zhang,Han Cai,Pan Zhang,Lingchao Li,Jianping Zhou,Tingjie Yin
Modulation of tumor microenvironment (TME) has been indicated as an approach to improve efficacy of cancer therapy. Here, we proposed a nano co-delivery based combination therapy of paclitaxel (PTX) and silybin (SB) which can employ the synergistic effects through chemotherapy sensitization and microenvironment modulation. A dextran-based amphiphilic polymer (Dex-DOCA) was successfully developed for in vivo co-delivery and thus “synchronizing” the biodistribution , transport and release of PTX and SB. Resultantly, Dex-DOCA exhibited an excellent encapsulating efficiency for both PTX and SB with adjustable loading ratio for an optimal synergistic antitumor activity . Moreover, the co-loaded nanoparticles efficiently discharged the two drugs at the prospective dosage ratio specifically in acid endo/lysosome mimic environments. The results of in vitro cytotoxicity and cell apoptosis assays further confirmed the SB sensitized PTX potency. Finally, in vivo investigation demonstrated that the co-loaded nanoparticles could effectively accumulate in tumor sites by passive targeting, and inhibit tumor growth through an enhanced intratumoral penetration (resulted from stromal components eradication and tumor vessels normalization associated TME modulation), as well as a sensitization effect of SB on PTX cytotoxic chemotherapy .
研究领域:
药学
·
肿瘤学
·
纳米技术
·
生物医学工程
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产品关联
DOI
PubMed
高影响因子
Foods
·
2021
·Vol. 10
·期 11
·2709
·
IF 4.35
Yan Huang,Dandan Pu,Zhilin Hao,Xiao Yang,Yuyu Zhang
This work aims to explore the contribution of prickly ash (Zanthoxylum bungeanumMaxim) on the taste perception of stewed sheep tail fat. Liquid chromatography-tandem quadrupole time of flight mass spectrometry (LC-QTOF-MS) was applied to analyze the taste-related compounds. A total of 99 compounds in different sheep tail fat samples were identified. The semi-quantitative results showed that there were differences between the samples. The partial least squares discriminant analysis (PLS-DA) model without overfitting was used to investigate the effect of prickly ash. Eleven marker compounds were predicted with a variable importance for projection > 1, fold change > 2 andp< 0.05. An additional experiment showed that guanosine 5′-monophosphate, malic acid, inosine and adenosine 5′-monophosphate could improve the umami and saltiness taste of stewed sheep tail fat.Keywords:sheep tail fat;taste compounds;LC-QTOF-MS;PLS-DA;sensory analysis;additional experiment
研究领域:
食品科学
·
化学计量学
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植物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
CHEMISTRY & BIODIVERSITY
·
2022
·Vol. 19
·期 8
·e202200471
·
IF 2.745
Qiang-Ming Li,Xiu-Rong Yang,Xue-Qiang Zha,Li-Hua Pan,Dan-Dan Zang,Feng-Yun Zhang,Jian-Ping Luo
Dendrobium huoshanense flowers have been widely used for liver protection in China. This work was aimed to discover the natural products with activity of mitigating alcoholic hepatocyte injury from Dendrobium huoshanense flowers via bioactivity-guided isolation, and to clarify the underlying mechanisms of these natural products. As a result, three flavonoids, 3′- O- methylquercetin-3- O-β -D-galactopyranoside ( 1 ), 3′- O- methylquercetin-3- O-β -D-glucopyranoside ( 2 ) and quercetin-3- O-β -D-glucopyranoside ( 3 ), were firstly isolated from D. huoshanense flowers. Results exhibited that flavonoids 1 – 3 could enhance the cell viability, decrease the expression of ALT and AST, inhibit the cell apoptosis, alleviate the oxidative stress, and mitigate the inflammatory response of alcohol-induced L02 cells. Mechanism study exhibited that flavonoids 1 – 3 could increase the expression of Nrf2 as well as its downstream antioxidation genes of alcohol-induced L02 cells, while ML-385 (Nrf2 inhibitor) could abolish the inhibitory effects of 1 – 3 on alcohol-induced hepatocyte injury. Flavonoids 1 – 3 could also reduce the phosphorylation levels of I κ B α and NF- κ B p65 of alcohol-induced L02 cells, while SC75741 (NF- κ B inhibitor) could not enhance the inhibitory effects of 1 – 3 on alcohol-induced L02 cells injury. The data above indicated that flavonoids 1 – 3 could inhibit alcohol-induced hepatocyte injury, which might be attributed to alleviating oxidative stress and mitigating inflammatory response by activating Nrf2 and inhibiting NF- κ B pathways.
研究领域:
药理学
·
分子生物学
·
肝病学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
SENSORS AND ACTUATORS B-CHEMICAL
·
2022
·
IF 9.221
Xinran Shi,Liang Ji,Yuanyuan Hu,Jinyu Gu,Liming Wang,Wenwen Lu,Jiali Meng,Yan Du,Lingzhong Huang,Dongxia Nie,Yanyan Yu
Since adenosine triphosphate (ATP) and reactive oxygen species (ROS) are closely related to neuron functions and the pathogenesis of Alzheimer's disease , herein, the first example of using a dual-responsive zeolitic imidazolate framework-90 (ZIF-90) to fabricate a single fluorescent probe , CuNCs/ [email protected] /ZIF, was reported, which specifically and sensitively responded to intracellular level fluctuations of ATP and ROS both in neuronal and tumor cells without obvious cross-talking. Through a stepwise in situ growth method, ROS-responsive glutathione-stabilized copper nanoclusters (GSH-CuNCs) and double tagged ATP aptamer hybrid chain (P1-P2) were prepared and respectively encapsulated into the inner and outer ZIF-90. The obtained CuNCs/ [email protected] /ZIF probe as a tandem system could firstly respond to ATP in an “off-to-on” mode, in which, the quenched fluorescence of FAM by BHQ1 attached on P2 was recovered through the competitive displacement between ATP and ZIF-90, leading to the release of FAM from ZIF-90. Upon collapse of the outer ZIF-90, the strong emission of CuNCs enclosed in the inner ZIF-90 was subsequently quenched in the presence of ROS. Accompanied with high sensitivity, selectivity and accuracy, the resultant fluorescent probe exhibited good performance and properties for tracking the level variations of ATP and ROS in SH-SY5Y and Hela cells under different stimulations. This strategy highlighted the potential of the ZIF-90 based nanocomposite for multi-targets detection, and also provided a value tool for the early diagnosis of diseases.
研究领域:
生物化学
·
医学诊断
·
材料科学
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产品关联
DOI
高影响因子
ENVIRONMENTAL TOXICOLOGY AND PHARMACOLOGY
·
2023
·
IF 4.3
Guanglu Wang,Yue Xin,Kaixin Ping,Xuhui Xu,Ying Sun,Xing Li,Xinying Guan,Jingquan Dong
Avermectins, as a new type of environmental pollutant, have received significant attention in recent years. Previous research has shown that acute exposure to avermectins can induce oxidative stress and inflammation in non-target fish species, such as carp. Flavonoid lignans, particularly Silybin, have demonstrated promising biological activities, including regulation of non-alcoholic fatty liver and cerebral ischemia-reperfusion injury. This study aims to investigate the impact of dietary supplementation with Silybin on the intestinal damage in carp caused by chronic exposure to avermectins and to improve the health status and production of carp in aquaculture. Silybin was used as a dietary supplement by adding it to the experimental feed, and an animal experimental model was utilized to assess its effects on oxidative stress, inflammation, and cell apoptosis in carp intestine. Additionally, intestinal barrier integrity, digestive capacity, and fish growth were evaluated. The results indicated that dietary supplementation with Silybin effectively alleviated the oxidative stress induced by chronic exposure to avermectins in carp intestine. Furthermore, Silybin improved intestinal barrier integrity and digestive capacity by modulating the Nrf2/Keap1 pathway. This study demonstrates that dietary supplementation with Silybin can effectively mitigate the intestinal damage caused by chronic exposure to avermectins in carp, providing a sustainable solution for the aquaculture industry to enhance the overall health and production of cultured fish. The research expands our understanding of avermectin environmental pollution and offers a potential remediation approach.
研究领域:
水产养殖
·
环境毒理学
·
药理学
·
鱼类生理学
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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）