JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
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2021
·
IF 5.279
Yingchao Li,Ran Zhang,Qi Zhang,Meiling Luo,Farong Lu,Zhonggui He,Qikun Jiang,Tianhong Zhang
Resveratrol (RES) suffers from poor water solubility and extensive metabolism, which lead to low bioavailability. A phospholipid complex (PC) containing RES and a UDP-glucuronosyltransferase (UGT) inhibitor was prepared to address these two limiting factors, thereby improving RES bioavailability. First, 11 natural active ingredients metabolized by similar enzyme subtypes to RES were screened in a glucuronidation assay in liver microsomes. Then, glycyrrhetinic acid (GA), the strongest inhibitor, was prepared with RES in a PC. RES-PC was prepared as a control. As expected, the water solubility and the cumulative dissolution of RES were significantly enhanced by RES-PC and RES/GA-PC. Compared with the RES group, the AUC0–10 of RES and resveratrol-3-glucuronide (R-3-G) in the RES/GA-PC group showed increases of 2.49- and 1.70-fold, respectively, with the proportion of RES absorption to total absorption increasing 1.45 times. These results demonstrated that RES/GA-PC could improve the bioavailability of RES by increasing its water solubility and inhibiting its glucuronidation.
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BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
·
2019
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IF 2.705
Conghui Fan,Fanhui Kong,Dattatrya Shetti,Bao Zhang,Yeguo Yang,Kun Wei
Currently, breast cancer has become the most commonly diagnosed malignancy among females and triple negative breast cancer (TNBC) is a highly aggressive and metastatic subtype. The natural polyphenolic compound, resveratrol (3, 4’, 5-trihydroxy-trans-stilbene, RES), has drawn great attention for its potential against TNBC. However, due to the poor aqueous solubility, the bioactivity of RES against TNBC is extremely hampered. In this study, oxidized mesoporous carbon nanoparticles (oMCNs) with size below 200 nm and excellent water dispersibility were synthesized using mild oxidation method and RES was successfully encapsulated into the pores of oMCNs with high drug loading efficiency (24.8% w/w). oMCNs exhibited good biocompatibility and excellent cellular uptake efficiency. Compared to pure RES, oMCNs-RES greatly improved the saturated solubility and in vitro release property. In vitro cytoxicity assay and apoptosis analysis showed that oMCNs-RES induced enhanced cytotoxic effect and pro-apoptosis effect mediated via the PARP and Caspase-3 protein cleavage in TNBC cell line, respectively. These results demonstrate oMCNs have the potential to deliver hydrophobic drugs and oMCNs-RES are promising in treating TNBC.
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JOURNAL OF MATERIALS SCIENCE
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2019
·Vol. 54
·期 11
·8591-8601
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IF 3.442
Huang Wenquan,Li Shaomin,Li Zhixian,Zhu Wei,Lu Shan,Jiang Yanbin
The development of multi-functional nanoparticles is important in overcoming the poor stability and low mucus permeation of traditional drug delivery systems. Hence, the encapsulation of a model drug, resveratrol (RES), into zein–polydopamine–lecithin (ZPLs) nanoparticles was investigated through a delicately controlled phase separation process. The surface of the nanoparticles obtained was successfully modified with lecithin, which endowed them with neutral and hydrophilic properties. Due to the strong charge repulsion of the particles, the fabricated ZPLs showed high stability under the conditions of a saline solution, various pH, long-term storage and high-speed centrifugation. In vitro study suggested that the RES exhibited remarkably sustained release performance after loading into ZPLs. The quantificational experiment of the Transwell system suggested that most of the ZPLs could pass through mucus and exhibited high mucus permeation. This study provides a new opportunity to prepare RES-ZPLs nanospheres as a smart drug nanocarrier, with enhanced stability and mucus permeation.
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FOOD CHEMISTRY
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2018
·
IF 4.946
Xiaofeng Ren,Ting Hou,Qiufang Liang,Xi Zhang,Di Hu,Baoguo Xu,Xinxiang Chen,Meram Chalamaiah,Haile Ma
In this study, resveratrol was successfully encapsulated using zein-chitosan complex coacervation. The encapsulation efficiency was markedly improved (51.4%) after chitosan coating at 1:2.5 zein/chitosan ratio, compared with 38.6% using native zein . Analysis of multi-model frequency ultrasound treatment effects on resveratrol encapsulation using zein-chitosan complex coacervation showed that 28/40 kHz dual-frequency ultrasound led to the highest encapsulation efficiency (65.2%; 31.9% increase) and loading capacity (5.9%; 31.1% increase) of resveratrol, followed by multi-frequency ultrasound at 20/28/40 kHz (17.8% encapsulation efficiency increase; 17.8% loading capacity increase). Dual-frequency ultrasound treatment significantly reduced the zein-chitosan complex coacervation particle size and reduced their distribution, however, did not change the zeta potential. Fourier transform infrared spectroscopy and fluorescence spectroscopy analysis demonstrated that ultrasound treatment had no effect on secondary structure of zein-chitosan complex but markedly decreased the fluorescence emission intensity. Differential scanning calorimetry and X-ray diffraction results indicated that Dual-frequency ultrasound treatment improved the thermal stability of zein-chitosan complex coacervation but had no effect on the crystal structure. Atomic force microscopy and scanning electron microscopy images revealed uniform distribution of zein-chitosan complex coacervation followed by ultrasonic treatment.
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Food Bioscience
·
2024
·
IF 4.8
Xiaoyue Yang,Dequan Zhang,Christophe Blecker,Chunjiang Zhang,Xiangxiang Sun,Zhenyu Wang
To elucidate the pathways and mechanisms by which polyphenols inhibit protein-bound heterocyclic amines (HAs), the influence of resveratrol on bound/free HAs and the structure changes of myofibrillar proteins (MP) in the system of creatinine/MP/glucose model was studied. The results demonstrate that resveratrol significantly reduced bound and free HAs in the reaction systems ( P < 0.05), and facilitates the transition from bound to free HAs. In addition, resveratrol altered the secondary structure of MP and had a static quenching effect on MP fluorescence. The strong interactions between resveratrol and MP are mainly hydrogen bonding and hydrophobic interactions. Furthermore, the results of molecular docking demonstrated that resveratrol exposed more hydrophobic amino acids (Ala, Lys and Pro) at the 556–578 amino acid sites of myosin. These results indicate that resveratrol controls the formation of bound HAs by reducing exposure to amino acids involved in the HAs reaction and promoting exposure to non-precursor amino acids.
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BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
·
2024
·
IF 2.5
Yuan Ning,Ping Chen,Zhengnan Shen,Xing Liu,Huan Gu
Cisplatin (CDDP) is commonly used as an anticancer drug in clinical practice, but severe nephrotoxicity restricts it from exerting anticancer effects. Natural drugs, such as resveratrol, can alleviate the side effects of cisplatin, but their low solubility and gastrointestinal effects prevent them from working. Herein, we developed nanoparticles for kidney injury consisting of a biocompatible material, zein, as a carrier. HA-Zein/Res NPs were fabricated using low-molecular-weight hyaluronic acid coatings. This preparation is non-cytotoxic to renal tubular epithelial cells and can be used with confidence. Low-molecular-weight hyaluronic acid has inflammation-targeting properties and CDDP damage causes renal inflammation. Owing to this property of the low-molecular-weight hyaluronic acid coating, in vivo imaging experiments in mice demonstrated that the HA-Zein/Res NPs enabled more nanoparticles to accumulate in the renal sites affected by inflammation. Efficient resveratrol delivery alleviated kidney injury, and experiments demonstrated that HA-Zein/Res NPs could treat kidney injury while reducing the serum creatinine and urea nitrogen levels in mice. Collectively, these results indicated that this nanomaterial is a promising agent for reducing the clinical nephrotoxicity of cisplatin.
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FOOD HYDROCOLLOIDS
·
2018
·
IF 5.089
Hao Cheng,Zheng Fang,Wusigale,Amr M. Bakry,Yantao Chen,Li Liang
Clarification of the mechanism of protein-ligand interaction is important for the encapsulation of bioactive components. Trans -resveratrol is labile to convert to cis -isomer during fermentation and storage, but the cis -isomer interaction with proteins has not yet gained as much attention as that of trans -isomer. The influence of resveratrol's isomerization on interaction with ligand-binding proteins was investigated here. Cis -resveratrol exhibited higher affinity for bovine serum albumin than trans -isomer, but the isomerization to cis -isomer decreased the polyphenol affinity for α-lactalbumin and β-lactoglobulin. For each protein, trans - and cis -resveratrol shared the same optimal docking site but showed clear diversity in the second best site. Protein ternary complex could be formed when trans -/ cis -resveratrol were added in the sequence. Moreover, photostability of resveratrol and antioxidant activity of the polyphenol-protein mixtures were also discussed. The results gathered here should provide further insight into protein-polyphenol interactions and be useful for the development of protein-based carriers for the polyphenols.
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2024
·
IF 7.7
Long Chen,Wen Xu,Zhongyu Yang,David Julian McClements,Xinwen Peng,Zhenlin Xu,Man Meng,Yidong Zou,Guanxiong Chen,Zhengyu Jin
Three nanoparticles were fabricated for the co-delivery of quercetin and resveratrol. Nanoparticles consisted of a zein and carboxymethyl cellulose assembled using antisolvent precipitation/layer-by-layer deposition method. Nanoparticles contained quercetin in the core and resveratrol in the shell, resveratrol in the core and quercetin in the shell or both quercetin and resveratrol in the core. The particle sizes of nanoparticles were 280.4, 214.8, and 181.8 nm, respectively. Zeta-potential was about −50 mV and PDI was about 0.3. The different positions of polyphenol distribution nanoparticles could reduce the competition between the two polyphenols, the encapsulation rate, loading rate and storage stability reached up to 91.7 %, 5.37 % and 97.1 %, respectively. FT-IR showed that hydrophobic and electrostatic interactions were the main driving forces of nanoparticle assembly. XRD showed that two polyphenols were successfully encapsulated in nanoparticles. TGA showed that distributing the nanoparticles in different layers would enhance thermal stability. TEM and SEM showed that polysaccharides attached to the surface of nanoparticles formed a core-shell structure with uniform particle size. All three nanoparticles could release two polyphenols slowly in simulated gastrointestinal digestion, Korsmeyer-Peppas was the most suitable kinetic release model. Therefore, biopolymer-based nanocarriers can be created to enhance the loading, stability, and bioaccessibility of co-encapsulated nutraceuticals.
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JOURNAL OF CONTROLLED RELEASE
·
2025
·
IF 11.5
Anning Yang,Hongwen Zhang,Huiping Zhang,Nan Li,Cong Chen,Xiaoling Yang,Jue Tian,Jianmin Sun,Guizhong Li,Yue Sun,Bin Liu,Yideng Jiang
Atherosclerosis (AS) therapy has been commonly based on lipid-lowering agents ( e.g. , statins), supplemented by other therapies, such as anti-inflammatory agents and antioxidants, through traditional Chinese herbs. Ferroptosis, a form of regulated cell death characterized by iron-dependent lipid peroxidation, has been implicated in the progression of AS, particularly in macrophages. In the study, we constructed a macrophage targeted hybridization nanodrug of HMLRPP NPs, which used Pit-loaded Poly(lactic- co -glycolic) acid (PLGA) nanoparticles and Res-loaded liposomes (Lipo) as nano-core, then, coated with a macrophage membrane hybridized by hyaluronic acid (HA). The nanodrug prolonged blood circulation time and achieved optimal Res and Pit accumulation in the atherosclerotic plaques by effectively evading immune system clearance. In vivo studies demonstrated that HMLRPP NPs significantly attenuated plaque progression, characterized by decreased plaque area, less lipid deposition, and increased collagen. Meanwhile, HMLRPP NPs inhibited macrophage ferroptosis by decreasing the expression of β-Hydroxybutyrate dehydrogenase 1 (BDH1), Orosomucoid 1 (ORM1) and enhancing the expression of Ribosomal protein S27-like (RPS27L), which resulted in the alleviation of lipid accumulation and inflammation. Our data suggest that the HMLRPP nanodrug delivery system with ferroptosis-regulating capability provides a feasible therapeutic strategy for atherosclerosis.
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BRAZILIAN JOURNAL OF MEDICAL AND BIOLOGICAL RESEARCH
·
2024
·
IF 1.9
Liu Lilong,Wang Yexin,Dong Yanyan,Lin Shan,Guan Wenhui,Song Jia
The clinical application of 5-fluorouracil (5-Fu), a potent chemotherapeutic agent, is often hindered by its well-documented cardiotoxic effects. Nevertheless, natural polyphenolic compounds like resveratrol (RES), known for their dual anti-tumor and cardioprotective properties, are potential adjunct therapeutic agents. In this investigation, we examined the combined utilization of RES and 5-Fu for the inhibition of gastric cancer using both in vitro and in vivo models, as well as their combined impact on cardiac cytotoxicity. Our study revealed that the co-administration of RES and 5-Fu effectively suppressed MFC cell viability, migration, and invasion, while also reducing tumor weight and volume. Mechanistically, the combined treatment prompted p53-mediated apoptosis and autophagy, leading to a considerable anti-tumor effect. Notably, RES mitigated the heightened oxidative stress induced by 5-Fu in cardiomyocytes, suppressed p53 and Bax expression, and elevated Bcl-2 levels. This favorable influence enhanced primary cardiomyocyte viability, decreased apoptosis and autophagy, and mitigated 5-Fu-induced cardiotoxicity. In summary, our findings suggested that RES holds promise as an adjunct therapy to enhance the efficacy of gastric cancer treatment in combination with 5-Fu, while simultaneously mitigating cardiotoxicity.
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JOURNAL OF THE SCIENCE OF FOOD AND AGRICULTURE
·
2024
·
IF 3.3
Jun Yang,Jieqiong Lin,Weidong Zhang,Mingyue Shen,Yuanxing Wang,Jianhua Xie
BACKGROUND Resveratrol (Res) is promising food functional factor with favorable antioxidant and anti-inflammatory properties, although its poor water solubility and low bioavailability limit extensive application. Therefore, in combination with another promising polysaccharide ( Mesona chinensis polysaccharides, MCP), Res-loaded food nanocarriers (ResNPs) were developed to increase its water solubility, bioactivity and targeting properties. ResNPs were then applied to alleviate dextran sulfate sodium (DSS)-induced ulcerative colitis. RESULTS Resveratrol can be well encapsulated in MCP-based nanoparticles in an amorphous state, improving its water solubility. ResNPs showed pH-response controlled release behavior in the gastrointestinal tract and increased the enrichment of Res in the colon. In vivo experiments of ResNPs against DSS-induced ulcerative colitis (UC) revealed that ResNPs significantly improved UC symptoms, modulated intestinal inflammation and down-regulated oxidative stress levels compared to free Res. ResNPs also play an positive role with respect to inhibiting the mitogen-activated protein kinase pathway and promoting the expression of tight junction proteins. In addition, ResNPs improved the species composition and relative abundance of intestinal flora in UC mice, which effectively regulated the balance of intestinal flora and promoted the production of short-chain fatty acids. CONCLUSION These results suggest that MCP-based nanoparticles can effectively improve the solubility of resveratrol and enhance its in vivo bioactivity. Moreover, the present study also provides a new strategy for the prevention and treatment of UC with food polyphenol. © 2024 Society of Chemical Industry.
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Scientific Reports
·
2025
·Vol. 15
·期 1
·1-16
·
IF 3.9
Chen Chunxia,Huang Huan,Zhang Haofeng,Huang Junli,Zhou Xing,Xie Xixiang,Liao Xiaoling,Zhou Yao,Cai Fangqi,Chen Guirong,Xie Yuping,Huang Luying
The TLR4/NLRP3 inflammasome pathway drives lung cancer cell proliferation, migration, and invasiveness. However, no in vivo treatments targeting this pathway in lung cancer exist. Resveratrol, an anti-inflammatory compound, inhibits the NLRP3 inflammasome but requires high doses due to its hydrophobicity and instability. This study aimed to enhance the therapeutic efficacy of resveratrol by encapsulating it in liposomes to effectively target the TLR4/NLRP3 inflammasome pathway in lung cancer. In this study, the efficacy of resveratrol liposome was tested in vitro through cell proliferation and migration assays and gene expression analysis. In vivo effects were evaluated in a lung cancer mouse model using histological and molecular techniques. Resveratrol liposome significantly inhibited lung cancer cell proliferation and migration, and induced apoptosis in orthotopic lung cancer models. Additionally, by suppressing TLR4/NLRP3 inflammasome-related genes, resveratrol liposomes diminished levels of IL-1β and IL-18 both locally at tumor sites and systemically, thus modulating the tumor immune microenvironment by decreasing MDSCs and increasing CD4 + and CD8 + T cells. In conclusion, resveratrol liposome alleviates lung cancer progression by targeting the TLR4/NLRP3 inflammasome pathway and enhancing anti-tumor immune responses, highlighting its potential as a promising therapeutic strategy for lung cancer treatment.
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