JOURNAL OF MOLECULAR RECOGNITION
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2016
·Vol. 30
·期 1
·e2566
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IF 2.091
Hua-jin Zeng,Min Miao,Ran Yang,Ling-bo Qu
In this study, the fibrillation of hen egg-white lysozyme (HEWL) in the absence and presence of different concentrations of silybin was studied by thioflavin T spectroscopy, Congo red binding assays, 8-anilino-1-naphthalenesulfonic acid (ANS) fluorescence assay, circular dichroism, and transmission electron microscopy. The experimental results indicated that not only the fibrillation of HEWL at high temperature (65°C) and low pH (pH = 2.0) could be inhibited effectively by silybin but also the inhibition of HEWL by silybin followed a dose-dependent manner. Molecular docking studies indicated that 2 possible binding modes could be found in the interaction between silybin and HEWL via van der Waals forces and electrostatic forces as well as hydrogen bonding. One of these 2 conformations was directly entered into the cavity of HEWL (binding site I); the other was bound to the surface of HEWL (binding site II). In this way, silybin could not only increase the hydrophobicity of the cavity or the surface of HEWL but also influence the microenvironment of the binding site, which was able to stabilize the structure of HEWL and delay the process of HEWL fibrosis.
研究领域:
生物化学
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分子生物学
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蛋白质科学
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药理学
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结构生物学
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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.
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JOURNAL OF LIPOSOME RESEARCH
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2025
·
IF 4.3
Xiaowen Wang,Xia Jiang,Jinjing Yang,Michael Adu-Frimpong,Mingjie Gong,Qinyang Hua,Tingyuan Li,Jiaying Li,Pengfei Pan,Elmurat Toreniyazov,Xia Cao,Jiangnan Yu,Qilong Wang,Ximing Xu
Moringa A (MA), the hepatoprotective components of Moringa oleifera Lam. seeds, are metabolized and eliminated quickly in the body. In this study, cholesterol-modified chitosan (CH-CS) was used as a polymer carrier to prepare chitosan-modified MA liposomes (MA-CLs) in order to slow down the release of MA, prolong its circulation time, and improve the oral bioavailability of MA in comparison with common MA liposomes (MA-Ls). The particle size (PS) of MA-CLs was 218.25 ± 1.07 nm, with a polydispersity index (PDI) of 0.143 ± 0.005 and a zeta potential (ZP) of 30.64 ± 0.29 mV. The encapsulation efficiency (EE) was 85.17 ± 1.70%, while the drug loading (DL) was 7.92 ± 0.16%. In contrast, the PS of MA-Ls was 232.06 ± 1.36 nm, with a PDI of 0.215 ± 0.009 and a ZP of −14.21 ± 0.33 mV. The EE and DL of MA-Ls were 71.34 ± 0.60% and 8.39 ± 0.07%, respectively. These results indicated that MA liposomes could effectively mitigate the burst release of MA, thereby enhancing its oral bioavailability. Furthermore, the performance of MA-CLs was superior to that of MA-Ls. ELISA kits demonstrated that, both MA and MA liposomes groups significantly reduced the levels of ach detection index in mice. Specifically, the therapeutic effect followed the order: MA-CLs > MA-Ls > MA, thus exhibiting a concentration-dependent manner. Histopathological analysis of liver sections revealed that MA and its formulations alleviated hepatocyte swelling and necrosis, thereby protecting the liver from alcohol-induced damage. This study found that MA has a protective effect on the liver, while MA-CLs hold promise as a therapeutic agent for prevention of acute alcoholic liver injury (ALI).
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Foods
·
2023
·Vol. 12
·期 6
·1308
·
IF 5.2
Yanxia Liu,Minghuo Wu,Miaomiao Ren,Haijun Bao,Qing’an Wang,Nan Wang,Shibo Sun,Jianqiang Xu,Xiaojing Yang,Xu Zhao,Yongming Bao,Gaohong He,Weiping Xu
Milk thistle is a traditional medicinal herb. Silybin is a medicinal component found in the seed coat of milk thistle, which has liver-protective and anti-cancer properties. Conventional studies have focused on the extraction of silybin with organic reagents, which was inapplicable to the food industry. This study aims to develop a fermented milk containing silybin and protein from the milk thistle seeds. A three step procedure was developed, comprising homogenization of milk thistle seeds, NaHCO3heat treatment, and microbial fermentation. The silybin was characterized by high performance liquid chromatography, and the protein was quantified and electrophorized. It was found that the homogenization step was essential for the preparation of protein, and the NaHCO3heat treatment was the crucial step in obtaining silybin. The optimal NaHCO3treatment settings were 1% NaHCO3, 60°C, and 3 h, and the optimal strains for microbial fermentation were L131 (Rummeliibacillus stabekisii) and RS72 (Lactobacillus plantarum). The silybin yield in the fermented milk reached 11.24–12.14 mg/g seeds, accounting for 72.6–78.4% of the total silybin in the milk thistle seeds, and the protein yield reached 121.8–129.6 mg/g seeds. The fermented milk had a slightly sweet yoghurt-like flavor and could be used as a dietary supplement for silybin and protein.Keywords:milk thistle;silybin;protein;NaHCO3treatment;microbial fermentation;medical herb;functional foods
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FISH PHYSIOLOGY AND BIOCHEMISTRY
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2023
·
IF 2.9
Pan En-Zhuang,Xin Yue,Li Xue-Qing,Wu Xin-Yu,Tan Xue-Lian,Dong Jing-Quan
The aim of this study was to investigate the splenic tissue damage of environmental biological drug avermectin to freshwater cultured carp and to evaluate the effect of silybin on the splenic tissue damage of carp induced by avermectin. A total of 60 carp were divided into 4 groups with 15 carp in each group, including the control group fed with basic diet, experimental group fed with basal diet and exposed to avermectin (avermectin group), experimental group fed with basal diet supplement silybin (silybin group), and experimental group fed with basal diet supplement silybin and exposed to avermectin (silybin + avermectin group). The whole test period lasted for 30 days, and spleen tissue was collected for analysis. In this study, H&E staining, mitochondrial purification and membrane potential detection, ATP detection, DHE staining, biochemical tests, qPCR, immunohistochemistry, and apoptosis staining were used to evaluate the biological processes of spleen tissue injury, mitochondrial function, oxidative stress, apoptosis, and endoplasmic reticulum stress. The results show that silybin protected carp splenic tissue damage caused by chronic avermectin exposure, decreased mitochondrial membrane potential, decreased ATP content, ROS accumulation, oxidative stress, apoptosis, and endoplasmic reticulum stress. Silybin may ameliorate the splenic tissue damage of cultured freshwater carp caused by environmental biopesticide avermectin by alleviating mitochondrial dysfunction and inhibiting PERK-ATF4-CHOP-driven mitochondrial apoptosis. Adding silybin into the diet becomes a feasible strategy to resist the pollution of avermectin and provides a theoretical basis for creating a good living environment for freshwater carp. Graphical Abstract
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CHEMISTRY & BIODIVERSITY
·
2022
·Vol. 19
·期 8
·e202200471
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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.
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Frontiers in Pharmacology
·
2022
·
IF 5.988
Bai Yang,Chen Jiaqi,Hu Weijian,Wang Lei,Wu Yulian,Yu Shi’an
Background: Silibinin is widely utilized drug in various cancer treatments, though its application in cholangiocarcinoma has not yet been explored. For the first time, we evaluated the anticancer potential and underlying molecular mechanism of silibinin in treatment of cholangiocarcinoma treatment.Methods: HuCCT-1 and CCLP-1 cells were chosen to be an in vitro study model and were exposed to various concentrations of silibinin for indicated times. Cell viability was evaluated by the cell counting kit-8 (CCK-8) assay and half maximal inhibitory (IC50) concentrations were calculated. Cell proliferation capacity was determined through the use of colony formation and 5-Ethynyl-2′- deoxyuridine (EdU) assays. Cell apoptosis and cycle arrest were assessed by Live/Dead staining assay and flow cytometry (FCM). The protein levels of extracellular regulated protein kinases (ERK)/mitochondrial apoptotic pathway were evaluated through western blotting (WB). Mitochondrial membrane potential changes were determined via 5,5′,6,6′-Tetrachloro-1,1′,3,3′-tetraethyl-imidacarbocyanine iodide (JC-1). A cholangiocarcinoma cell line xenograft model was used to assess the anti-tumor activity of silibinin in vivo.Results: Inhibition of the ERK protein by silibinin led to a significant decrease in mitochondrial membrane potential, which, in turn, caused Cytochrome C to be released from the mitochondria. The activation of downstream apoptotic pathways led to apoptosis of cholangiocarcinoma cells. In general, silibinin inhibited the growth of cholangiocarcinoma cell line xenograft tumors.Conclusions: Silibinin is able to inhibit cholangiocarcinoma through the ERK/mitochondrial apoptotic pathway, which makes silibinin a potential anti-tumor drug candidate for cholangiocarcinoma treatment.
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SENSORS AND ACTUATORS B-CHEMICAL
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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.
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Drug Design Development and Therapy
·
2022
·
IF 4.319
Rong Xu,Siyan Qiu,Jie Zhang,Xiaoli Liu,Ling Zhang,Haizhu Xing,Min You,Man Wang,Yuting Lu,Peng Zhang,Jing Zhu
Background: Silibinin (Sil), a flavonoid lignan-like natural compound derived from milk thistle seeds, has been used to treat hepatic diseases, including early-phase hepatocirrhosis and fatty liver, for many years. However, its poor water solubility limits its gastrointestinal absorption and bioavailability. It clinical use has been limited due to its slow onset of action. Faced with this problem, research on the derivatives of silibinin has been receiving much attention. Purpose: A series of silibinin derivatives with good biosafety and higher hepatoprotective activity were obtained by a safe, efficient and green chemical synthesis method. Patients and methods: First, the carbonyl group in the structure of silibinin was used to obtain silibinin Schiff base derivatives by dehydration condensation with the carboxyl group in the sulfur-containing amino acid. Next, relevant experiments were performed to characterize the structure, physical form and solubility of the derivatives. Then, toxicity tests of the derivatives were performed in LO-2 cells and SD rats to evaluate their biosafety. Finally, the anti-inflammatory and antiapoptotic activities were observed using a carbon tetrachloride (CCl 4 )-induced acute liver injury model in C57BL/6J mice using silibinin as a control. Results: The studies showed that SS and ST behaved as amorphous substances and showed a significant increase in solubility compared to silibinin. These two derivatives showed low toxicity in biosafety tests and higher bioactivity (anti-inflammatory and anti-apoptotic) than silibinin against acute liver injury induced by CCl 4 . Conclusion: Two silibinin derivatives (SS and ST) obtained by the Schiff base reaction improved the solubility of the silibinin parent nucleus in biological media with the help of the hydrophilic and amorphous morphology of the ligand. The low toxicity in vivo and in vitro ensures the biosafety of the derivatives. The hepatoprotective activity (anti-inflammatory and anti-apoptotic) was significantly improved compared to silibinin.
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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
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CHEMICAL ENGINEERING JOURNAL
·
2023
·
IF 15.1
Yanan Wang,Huichao Wei,Keyang Li,Liru Liu,Yingfei Zhu,Xinyuan Wang,Jiahui Yan,Liangmin Yu,Xuefeng Yan,Zhiyu He
Calcium overload in hepatocytes mediates the crosstalk and amplification loop with oxidative stress and severe inflammation that initiate pro-apoptotic and necrotic signaling pathways in acute liver injury (ALI). In this study, an N-acetylgalactosamine-modified amphiphilic dextran-silibinin conjugate (GalNAc-Dex-Sil) with ROS-sensitive phenylboronic acid (PBA) linkage was synthesized. The as-prepared amphiphilic polymer was self-assembled into GalNAc-Dex-Sil nanoparticles, which efficiently encapsulated the membrane-permeable calcium chelator BAPTA-AM (BA), achieving GalNAc-mediated hepatocyte-specific targeting and ROS-responsive release in injured hepatocytes through PBA cleavage. Accordingly, a single low-dose injection of formulation (BA: 150 μg·kg −1 ) significantly alleviated hepatocyte oxidative stress and inflammation, rescued dying hepatocytes, prevented further hepatocyte damage, and ultimately restored liver function in the ALI mouse model by 1) rapidly and effectively eliminating the overloaded calcium and scavenging excessive ROS via released BA to block the feed-forward vicious cycles of the cell damage, 2) inhibiting the inflammatory cascade by decreasing the expression of the key factor of the NF-κB/NLPR3 axis, 3) inhibiting the key branch of the mitochondrial apoptotic pathway (Cyt C/Bcl-2 family/caspase-3 axis) and death receptor pathway (TNFα/Caspase-8 axis), and 4) stabilizing hepatocyte membranes through the synergistic hepatoprotective effect of silibinin. Taken together, this formulation exhibited great potential as a potent and effective ALI treatment strategy.
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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.
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