Food & Function
·
2025
·
IF 5.4
Qi-Yuan Feng,Jiang-Tao Zhong,Hai-Ming Sun,Zheng Luo,Yu-Chen Jiang,Jian Song
Procyanidin B1 (PB1) is a natural polyphenol abundant in whole-grain highland barley as well as in many fruits, vegetables, and medicinal plants. The current study investigated the hepatoprotective effect and potential mechanism of PB1 against hepatic fibrosis. C57BL/6 mice with hepatic fibrosis were induced with thioacetamide (TAA), followed by the administration of PB1 or a positive control, silymarin, or followed by gene silencing of the thyroid hormone-responsive protein (THRSP). Hepatic stellate cells (HSCs) were stimulated with transforming growth factor β (TGF-β) or an isolated mouse peritoneal macrophage (MPM)-primed conditioned medium and cultured with PB1, silymarin or the THRSP agonist. MPMs were cultured in the presence of LPS/ATP and/or PB1. It was found that PB1 decreased the release of inflammatory factors, such as caspase-1 and IL-1β. Moreover, PB1 could activate THRSP and decrease P2X7r-modulated NLRP3 inflammasome activation in the TAA-induced mice. Additionally, PB1 inhibited the expressions of α-SMA, collagen I, the TIMP-1/MMP13 ratio, inflammatory factors, P2X7r, and NLRP3 and increased THRSP expression in activated HSCs and macrophages. THRSP deficiency attenuated the regulatory effect of PB1 on the reverse inflammation of activated HSCs, promoting hepatic fibrosis in vivo and in vitro. PB1 reversed the activation of HSCs by increasing the THRSP-mediated P2X7r/NLRP3 axis, similar in function to THRSP overexpression. PB1 could reverse the activation of HSCs and mitigate hepatic inflammation and fibrogenesis in TAA-induced hepatic fibrosis. Targeting THRSP-mediated P2X7r/NLRP3 is crucial for PB1's action against hepatic fibrosis, underscoring a promising approach and the utility of PB1 for the treatment of hepatic fibrosis.
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高影响因子
BIOMEDICINE & PHARMACOTHERAPY
·
2023
·
IF 7.5
Yao Shi,Haojie Zhang,Shuang Li,Danqing Xin,Shiyang Li,Bing Yan,Shuanglian Wang,Chuanyong Liu
Background Inflammatory bowel disease (IBD) is a chronic disease with an unclear pathogenesis for which successful treatments are still lacking. It has been reported that procyanidin, a natural antioxidant, relieves colitis, but the specific mechanism is elusive. Purpose Our present study was designed to investigate the effects of procyanidin on colitis and the regulation of the M1 macrophage phenotype and related signaling pathways. Methods In vivo, we used two classic colitis models to observe the effect of procyanidin on macrophage polarization. In vitro, we further validated the therapeutic effect of procyanidin in the RAW264.7 cell line and peritoneal macrophages. Results The current findings provide new evidence that procyanidin ameliorated dextran sulfate sodium (DSS)-induced colitis by preventing the polarization of macrophages to the M1 type and downregulating the levels of proinflammatory factors in cells. We also showed that procyanidin prevented lipopolysaccharide (LPS)-induced elevation of inflammatory cytokines and the activation of proinflammatory macrophages, which was achieved by activating the STAT3 and NF-κB pathways. Conclusions This is the first study to demonstrate that procyanidin alleviates experimental colitis by inhibiting the polarization of proinflammatory macrophages. These data reveal new ideas for the pathogenesis and treatment of inflammatory diseases.
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CHEMICAL ENGINEERING JOURNAL
·
2022
·
IF 16.744
Shanshan Tie,Wentao Su,Yannan Chen,Shida Wu,Hao Wu,Yukun Song,Siyuan Fei,Mingqian Tan
The purpose of this study is to design a cell membrane and mitochondrial targeting nanoparticle with glutathione stimulus response to deliver procyanidin for effective treatment of inflammatory bowel disease (IBD). The dual targeting procyanidin nanoparticles were prepared with amphiphilic stearic acid modified hyaluronic acid using cystamine dihydrochloride as a linker for encapsulation of (5-carboxypentyl) (triphenyl) phosphonium bromide conjugated procyanidins. As expected, the procyanidin nanoparticles showed good mitochondrial targeting ability, with a Pearson’s correlation coefficient of 0.91 at 4 h. In vivo imaging of IBD mice model demonstrated a remarkable colon accumulation of the targeting procyanidin nanoparticles. Significant glutathione stimulus release of procyanidin was found in the presence of 10 mM of glutathione at pH 7.4. In vivo experiments showed that the colon length of targeting procyanidin nanoparticle-treated IBD mice increased by 20.84% compared with the IBD mice. The weight loss, disease activity index score, oxidative stress level and the release of proinflammatory cytokines were significantly ameliorated. The composition and relative abundance of gut microbiota, and the number of short chain fatty acids were improved upon the uptake of targeting procyanidin nanoparticles. This study provided a dual targeting and glutathione response strategy to improve the bioavailability of procyanidin in IBD treatment.
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Drug Design Development and Therapy
·
2025
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IF 5.1
Yudong Su,Jinman Shui,Danshi Qi,Jie Bai,Xiaoxia Xu,Yongchun Huang,Ruilian Li,Qiong Wu,Haiyan Wang,Chengzhu Cao,Zhanhai Su,Shoude Zhang
Purpose Erectile dysfunction (ED), a prevalent form of male sexual dysfunction, is predominantly treated with Phosphodiesterase type 5 inhibitors (PDE5Is). Our previous research highlighted procyanidin, a natural compound, as a notably effective PDE5I. In the current study, we intend to further validate the inhibitory activity of procyanidin on PDE5A through in vitro and in vivo assessments. This study aims to validate the efficacy of procyanidin as a treatment for ED.Methods The binding affinity of procyanidin for PDE5A was assessed by molecular docking, molecular dynamics (MD) simulations, and microscale thermophoresis (MST) assay. The toxicity of procyanidin on penile corpus cavernosum smooth muscle (CCSM) cells (n=5) was evaluated. Additionally, its effects on intracellular cyclic guanosine monophosphate (cGMP) levels in CCSM cells (n=5) were evaluated. The absorption of procyanidin was evaluated by measuring plasma levels at various times after oral gavage to Sprague-Dawley (SD) rats (n=6). Subsequently, the effects of procyanidin on intracavernous pressure (ICP) and cGMP levels in penile cavernous tissue were evaluated in SD rats (n=6).Results Procyanidin forms three hydrogen bonds with PDE5A and stabilizes the complex structure, exhibiting equilibrium dissociation constants (KD) value of 7.77 ± 2.39 µmol/L. Additionally, procyanidin exhibits minimal cytotoxicity toward CCSM cells and significantly elevates intracellular cGMP levels compared to the control group. In vivo studies demonstrate that procyanidin is rapidly absorbed, achieving peak blood concentrations within one hour. Simultaneously, procyanidin significantly increases ICP and cGMP levels in rats compared to the control group.Conclusion These findings indicate that procyanidin sustains elevated cGMP levels within cells by targeting PDE5A, thereby exhibiting therapeutic efficacy in improving ICP. Procyanidin emerges as a promising PDE5I for treating ED and potentially other related conditions.
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高影响因子
JOURNAL OF FOOD AND DRUG ANALYSIS
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2022
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IF 6.157
Shuai Quan,Kaixiang Ji,Fangshuo Liu,Tesfaye Hailemariam Barkae,Mohamed Ibrahim Halawa,Saima Hanif,Baohua Lou,Jianping Li,Guobao Xu
Tetracycline was reported to trigger intense lucigenin chemiluminescence (CL). Based on its significant quenching to lucigenin-tetracycline CL, procyanidin was detected. The mechanism of the lucigenin-tetracycline CL and its quenching by procyanidin were proposed. Under the optimum conditions, the calibration curve is linear in the range of 10–1000 nM for procyanidin with a detection limit of 4.4 nM. The RSD for nine replicate determinations of procyanidin was less than 1.7%. Moreover, this method was satisfactorily applied to the determination of procyanidin in human urine samples and health food capsule of grape seed.
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ACS Omega
·
2026
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IF 5.2
Cheng Wang,Shaoyin Wei,Qingtian Tang,Kaixian Deng,Hongjun Jin,Huali Weng,Xingjie Zan,Qiangqiang Li
Hypertriglyceridemic acute pancreatitis (HAP) is characterized by mitochondrial oxidative phosphorylation (OXPHOS) impairment and excessive reactive oxygen species (ROS), leading to severe inflammation and organ damage. Existing therapies often lack targeted antioxidant efficacy and long-term stability. In this study, we innovatively designed and synthesized procyanidin capsules using a one-step calcium carbonate template method, which enables sustained release of procyanidin for over one month and exhibits exceptional scavenging capacity for both ROS and RNS. The capsules demonstrated high biocompatibility in macrophage and dendritic cell lines and significantly reduced inflammatory cytokines and pancreatic damage in a HAP mouse model. Proteomic analysis revealed that the therapeutic effect is mediated through the restoration of the aqueous OXPHOS function. This work provides a novel, biocompatible, and potent antioxidant strategy for the targeted treatment of HAP.
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CHEMICAL ENGINEERING SCIENCE
·
2019
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IF 3.372
Mingyue Liu,Renliang Huang,Chuanxi Li,Mingda Che,Rongxin Su,Shuzhou Li,Jing Yu,Wei Qi,Zhimin He
Nanoscale zero-valent iron has been widely applied in environmental remediation and toxic waste treatment, especially for the degradation of persistent organic pollutants (POPs). However, the dechlorination activity of Fe nanoparticles (Fe NPs) can be suppressed by the precipitation of iron oxides generated from the corrosion of Fe-Pd NPs under alkaline conditions, leading to a decreased dechlorination efficiency. Faced with this challenge, we report a highly effective dechlorination system that functions over a broad pH range and especially well under alkaline conditions in this work. Procyanidin (PROC), a natural polyphenol, was utilized as a stabilizer to manipulate the size distribution of Fe-Pd NPs and, more importantly, as a scavenger of Fe ions to prevent iron oxide precipitation. Experiments and theoretical calculations reveal that the generated Fe ions was mainly present in the form of bis- and tris-PROC-Fe complexes in the reaction solution. Compared with pristine Fe-Pd NPs, the PROC-modified Fe-Pd NPs had a dechlorination efficiency that was increased 20-fold (pH 9.0). Notably, a normalized rate constant was enhanced by more than 2 orders of magnitude compared to the previously reported dechlorination systems. The PROC-modified Fe-Pd NPs showed excellent dechlorination efficiency over a wide pH range (2.3–13.0).
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高影响因子
ENVIRONMENTAL TOXICOLOGY
·
2021
·Vol. 37
·期 2
·201-211
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IF 4.119
Rong Li,Hongsong Li,Qian Zhang
Purpose The damage of hyperglycemia to the retinal pigment epithelial (RPE) cells is a critical event in diabetic retinopathy (DR). Procyanidin (PC), a kind of polyphenol compounds, has shown to be effective in preventing and treating diabetes as well as its complications, in which autophagy disorder is involved in the pathological mechanism. However, it remains unclear whether PC can play a protective role in DR by regulating the autophagy of RPE. Here, the effect of PC on RPE under high glucose conditions and the role of autophagy were investigated. Materials and Methods The cell viability of ARPE-19, a human RPE cell line, was detected by cell counting kit-8 (CCK-8) and the apoptosis rate was measured by flow cytometry. The protein expressions of apoptosis markers, including Bax, Bcl-2, and Caspase-3, as well as autophagy markers including LC3, p62, p53, and mTOR were detected by Western blotting. Autophagic flux in ARPE-19 cells was detected by transfection with Ad-mCherry-GFP-LC3B. Results Under high glucose conditions, the viability of ARPE-19 was decreased and the apoptosis rate increased, the protein expressions of Bax, Caspase-3, LC3-II/LC3-I, and p-p53 were all increased and the expressions of Bcl-2, p62, and p-mTOR decreased, and autophagic flux was increased compared with that of the controls. Treatment with PC weakened all these changes caused by high glucose. When rapamycin (RPM), an autophagy agonist was added, the cell viability of ARPE-19 by PC treatment was decreased while the apoptosis was increased. Conclusions Our findings indicate that through the p53/mTOR autophagy pathway, PC may protect RPE cells from high glucose-induced injury.
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NEW JOURNAL OF CHEMISTRY
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2023
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IF 3.3
Tian-Xiao Yang,Hang Li,Yuan Zhu,Yu Gao,Hong-Ning Lv,Sheng-Hua Zha,Xiao-Li Sun,Qing-Sheng Zhao
Procyanidins (PC) are formed by the polymerisation of flavan-3-ol monomers, which have excellent bioactivity and present great health benefits. However, the application range of the PC is greatly limited due to their poor stability. Therefore, in this study, starch aerogels were used as carriers to encapsulate PC. After screening, wheat starch aerogel (WSA) was finally chosen to encapsulate PC. Afterward, characterization (SEM, XRD, FT-IR, TGA and BET), stability testing, investigations on antioxidant activity, and in vitro tests simulating digestion were carried out. The results of relevant characterization showed that the micro surface structure of the procyanidin wheat starch aerogel (PC-WSA) presented a network structure, and PC were encapsulated in WSA. In addition, PC-WSA allows PC to be released in the final stage of simulated digestion. Meanwhile, the results of antioxidant experiments indicate that PC-WSA exhibits antioxidant activity after encapsulating PC. Moreover, the retention of PC in PC-WSA was still 53.63 ± 3.23% when stored at 70 °C for 20 days. After 6 days of light exposure, the retention of PC in PC-WSA under different light sources was all above 85%, which was higher than that of PC. In conclusion, the wheat starch aerogel could improve the stability of PC and has great potential for application.
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JOURNAL OF PHYSIOLOGY AND BIOCHEMISTRY
·
2022
·Vol. 78
·期 1
·213-227
·
IF 5.08
Zhang Haihua,Lang Wuying,Liu Xin,Bai Jiangsong,Jia Qinghui,Shi Qiumei
Ulcerative colitis (UC) is a recurrent chronic inflammatory disease. The symptom of UC is mainly diarrhea including bloody stools. Increasing evidence has suggested that procyanidin A1 (PCA1) exerts an anti-inflammatory effect in several diseases. However, the role of PCA1 in UC is still a mystery. In our study, we explored the effect of PCA1 in dextran sulfate sodium (DSS)–induced UC mice and lipopolysaccharide (LPS)-stimulated HT-29 and IEC-6 cells. Then, cell proliferation, apoptosis, the production of proinflammatory cytokines, and autophagy-related markers were determined. Furthermore, the AMPK/mTOR/p70S6K signaling pathway was assayed by Western blot assay. In in vivo study, we found that PCA1 administration alleviated DSS-induced UC, as evidenced by reducing weight loss, clinical scores, colon weight/length ratio, histological damage, proinflammatory cytokines, and apoptosis. Moreover, we showed that the expression of Beclin-1 and LC3II/I ratio was increased, whereas the level of p62 was decreased after PCA1 treatment in vivo . Meanwhile, the reduced AMP/ATP ratio, enhanced expression of p-AMPK, and decreased p-p70S6K and p-mTOR levels indicate the activation of AMPK/mTOR/p70S6K signaling pathway. In in vitro study, PCA1 promoted cell proliferation and inhibited cell apoptosis in LPS-stimulated HT-29 and IEC-6 cells. Pro-inflammatory cytokines and autophagy-related factors exhibited the same trend as in in vivo results. Mechanically, PCA1 activated the AMPK/mTOR/p70S6K signaling pathway. The treatment with an AMPK inhibitor compound C significantly reversed the anti-inflammatory effect of PCA1 in LPS-stimulated cells. Taken together, these data indicated that PCA1 alleviated UC through induction of AMPK/mTOR/p70S6K-mediated autophagy.
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FOOD RESEARCH INTERNATIONAL
·
2025
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IF 8
Min Li,Jia-Yao Si,Peng-Fei Xie,Zhen-Jie Feng,Sheng-Jie Li,Feng Zhou,Jian-Mei Li
The global aging crisis has increased the risk of atherosclerosis (AS), positioning vascular senescence as a critical therapeutic target. Procyanidin C1 (PCC1), a bioactive polyphenol from hawthorn, demonstrates dual senolytic and longevity-enhancing effects. This study explored the regulatory role and mechanisms of PCC1 in AS using an ApoE −/− mouse model fed a high-fat diet (HFD) and a D-galactose (D-Gal)-induced cellular senescence model. Hawthorn oligomeric proanthocyanidins (HOPCs), as well as PCC1, showed potent anti-atherosclerotic and anti-aging effects by improving serum lipid metabolism and reducing aortic root plaque, vascular senescence markers and inflammatory adhesion molecules. Metabolomic analysis demonstrated that PCC1 significantly suppresses key enzymes in arachidonic acid (AA) metabolism, thereby decreasing downstream pro-inflammatory mediators. Target identification studies, including drug affinity responsive target stability (DARTS) assay, liquid chromatography-tandem mass spectrometry (LC-MS/MS), cellular thermal shift assay (CETSA), and molecular docking, identified heat shock protein 90 (HSP90) as a direct target of PCC1, leading to inhibition of its downstream signaling. In vitro, PCC1 selectively cleared senescent cells, suppressed the senescence-associated secretory phenotype (SASP), enhanced endothelial nitric oxide synthase (eNOS) phosphorylation, and inhibited the toll-like receptor 2 (TLR2)/nuclear factor kappa-B (NF-κB) pathway, demonstrating multimodal anti-aging and anti-inflammatory effects. Together, these findings indicate that PCC1 mitigates atherosclerosis by targeting both metabolic and inflammatory pathways through senescent cell clearance and HSP90-mediated blockade of the TLR2/NF-κB signaling axis. This dual mechanism highlights PCC1 as a promising vasoprotective agent and supports the potential application of hawthorn extracts in functional foods aimed at preventing aging-related cardiovascular diseases.
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2023
·
IF 8.2
Qin Geng,David Julian McClements,Zhihua Wu,Ti Li,Xuemei He,Xixiang Shuai,Chengmei Liu,Taotao Dai
Procyanidins are bioactive polyphenols that have a strong affinity to proteins. Beta-lactoglobulin (BLG) is widely used as an emulsifier in the food and other industries. This study evaluated the interaction between BLG and A-type procyanidin dimer (PA2) using the spectroscopic, thermodynamic, and molecular simulation. PA2 decreased the transmissivity and quenched the intrinsic fluorescence of BLG, suggesting that the two molecules formed a complex. The binding of PA2 reduced the surface hydrophobicity and altered the conformation of BLG with increasing the random coil regions. Thermodynamic and isothermal titration calorimetry analyses suggested that the main driving force of PA2-BLG interaction was hydrophobic attraction. Molecular docking simulations were used to identify the main interaction sites and forces in the BLG-PA2 complexes, which again indicated that hydrophobic interactions dominated. In addition, the influence of PA2 on the ability of BLG to form and stabilize O/W emulsions was analyzed. Emulsions formulated using BLG-PA2 complexes contained relatively small droplets (D 4,3 ≈ 0.7 μm) and high surface potentials (absolute value >50 mV). Compared to BLG alone, BLG-PA2 complexes improved the storage stability of the emulsions. This study provides valuable new insights into the formation, properties, and application of protein-polyphenol complexes as functional ingredients in foods.
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