Journal of Food Measurement and Characterization
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2024
·Vol. 18
·期 9
·7388-7401
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IF 2.9
Ge Zhiwen,Wang Dan,Zhao Wenting,Wang Pan,Dong Mingsheng,Zhao Xiaoyan
Resveratrol (RES) is a lipophilic polyphenol susceptible to photo- and thermal-degradation. The strategies to enable its distribution in food matrices, prevent its degradation during storage and improve its bioaccessibility during digestion have obtained much attention and studies. In the present study, natural porous matrix in the form of freeze-dried yogurt cubes (FDYC) was investigated as an absorbent for loading RES. The sodium caseinate (NaCas)-coconut oil lotion was used as a carrier for delivering RES and was added to milk medium for L. helveticus MB2-1 fermentation to obtain freeze-dried Sayram ketteki yogurt cubes (SKYC) with fortified RES. The results showed that the loading capacity of RES in SKYC was 28.08 ± 0.31% in freshly prepared samples and was 26.34 ± 0.13% (93.80 ± 0.17% retention) after 90 d of ambient storage in amber vials. The photothermal stability of RES encapsulated in SKYC was significantly higher than that of the original RES due to the protective effect of SKYC ( p < 0.05). During in vitro simulated gastrointestinal digestion, the RES release rate of the three treatments were in the following order: original RES < physical mixture of RES < encapsulated RES. Besides, the flavor of SKYC was enriched by the addition of NaCas-coconut oil lotion. Taken together, it can be demonstrated the SKYC has the potential to be loaded with lipophilic bioactive compounds for application in functional food. Graphical Abstract
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Food Bioscience
·
2024
·
IF 4.8
Dami Li,Yaoyao Zhang,Xing Qiao,Hira Ijaz,Shangde Sun
Resveratrol (RES) is a natural non-flavonoid polyphenolic antioxidant. The low solubility of RES in water (26 mg/L) and oil (175.51 mg/kg) limited its antioxidant activity and bioavailability. In order to overcome these issues, in this work, a lipophilic resveratrol laurate was efficiently synthesized using RES as starting material in the presence of enzymes. The catalytic activities of enzymes (Lipase CALA, Lipozyme TL 100L, Lipase CALB, Novozym 435, Lipozyme TLIM, and Lipozyme RMIM) were investigated and screened. Moreover, reaction conditions were optimized using response surface methodology. Meanwhile, thermodynamic and kinetic analyses were also conducted to investigate the enzymatic mechanism. Results showed that, Lipozyme RMIM showed the best performance for resveratrol monolaurates regioselective synthesis. Two products, 3-resveratrol monolaurate (3-RC12) and 4′-RC12, were prepared and purified. The optimal reaction conditions for the preparation of 3-RC12, and 4′-RC12 were 1:65 substrate ratio and 11.7 wt% lipase dosage at 75 °C for 33.2 h. Under these conditions, the RES conversion reached a maximum of 98.04 ± 1.76%. The regioselective products were analyzed for antioxidant activity. Notably, the esterification site significantly impacts resveratrol monoesters' antioxidant activity. And 3-RC12 demonstrates superior ABTS and DPPH radical cation scavenging activity, surpassing RES and 4′-RC12. Notably, in yield and antioxidant activity, 3-RC12 is better than 4′-RC12, which make it a potential antioxidant for industrial application.
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CRYSTENGCOMM
·
2017
·Vol. 19
·期 41
·6154-6163
·
IF 3.474
Hongyan He,Qi Zhang,Jian-Rong Wang,Xuefeng Mei
It was reported that the alkaloid component piperine (Pip) can drastically improve the bioavailability of the compound resveratrol (RSV) when co-administered. Therefore, cocrystallization experiments of RSV and Pip were attempted, and four cocrystals are successfully obtained from solution evaporation experiments. Their single crystals are acquired and the structural determination reveals that all the cocrystals contain solvent molecules within the crystals. Confirmed by VT-PXRD, the cocrystals transformed into the amorphous state after desolvation. Considering the toxicity of the solvent molecule, only RSV–Pip co-1 was utilized for further dissolution and pharmacokinetic experiments. The dissolution results demonstrate that RSV–Pip co-1 shows lower dissolution and apparent solubility than the RSV constituent under different buffers in the presence of different surfactants. The reduced dissolution and apparent solubility have a strong diminishing impact on the absorption of RSV, thus leading to unfavorable bioavailability, even though the coformer Pip possesses bioenhancer properties.
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International Journal of Nanomedicine
·
2022
·
IF 7.033
Meiyi Liang,Mingyan Guo,Phei Er Saw,Yandan Yao
Introduction Chemotherapeutics are known to have undesirable side effects (i.e. nausea, weight loss, hair loss, weakened immune system, etc.) due to the non-specificity of the drugs. Encapsulation of these chemotherapeutics inside nanoparticles significantly improves the bioavailability and half-life of drugs, while increasing their tumor penetration and localization. However, most, if not all, nanoparticles in clinics or research are synthetic, with no long-term studies on the effect of these nanoparticles in vivo. Herein, we developed a synergistic resveratrol nanoparticle system by using lecithin encapsulation. Lecithin, being a fully natural phospholipid derived from soybean, possesses inherent anti-tumor activity.Methods Lec(RSV) was successfully prepared using the nanoprecipitation method, and characterized by particle size and zeta potential analysis, and transmission electron microscopy (TEM). The in vitro cellular uptake and cytotoxic effects of Lec(RSV) were investigated in human breast cancer cell line BT474. Finally, the in vivo tumoral uptake of Lec(RSV) was carried out in the BT474 orthotopic model.Results Lec(RSV) showed a uniform distribution of ~120 nm, with prolonged stability. Lec(RSV) showed high cellular uptake and anti-cancer properties in vitro. Time-dependent uptake in the BT474 xenograft model indicated an increased tumoral uptake and apoptosis rate at 4 hours after tail vein injection of Lec(RSV).Conclusion Taken together, we successfully developed a fully natural Lec(RSV) that possesses potent anti-cancer activity in vitro, with good tumoral uptake in vivo. We hypothesize that Lec(RSV) could be a safe anti-cancer therapeutic that could be easily translated into clinical application.
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CRYSTAL GROWTH & DESIGN
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2017
·
IF 4.055
Hongyan He,Qi Zhang,Meiqi Li,Jian-Rong Wang,Xuefeng Mei
Resveratrol (RSV), a dietary polyphenol found in red wine, has renewed interest in recent years due to a broad range of in vitro evidence that indicate cardioprotective effects. Herein, we have synthesized four RSV cocrystals with the objective to improve the physicochemical and mechanical properties. Single crystal structures were illustrated and comprehensive characterization of the cocrystals were performed. In addition, powder dissolution of RSV cocrystals in different buffer medium containing different surfactants were conducted, and the result revealed that PVP K30 is an effective surfactant to maintain the supersaturation. Then pharmacokinetic experiments suggested that RSV cocrystals showed shorter Tmax, and RSV–NA exhibited higher Cmax and AUC0–24 values. Furthermore, RSV cocrystals exhibited superior mechanical properties compared to RSV pure component. These results may provide an alternative formulation for RSV.
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JOURNAL OF PHARMACEUTICAL SCIENCES
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2022
·
IF 3.784
Lihai Zhai,Zhaohua Zhang,Lihong Guo,Huaimin Dong,Junhou Yu,Guimin Zhang
Gefitinib (GEF) is an anti-tumor oral solid formulation with a superior advantage for lung tumors. However, it has poor aqueous solubility which limits its utility in vivo . Herein, a novel cocrystal (GEF-RES) assembled by GEF and RES (Resveratrol) has been successfully prepared and comprehensively characterized by differential scanning calorimetry , thermogravimetric analysis, Raman spectroscopy and powder X-ray diffraction. A single-crystal structure of the GEF-RES cocrystal was solved and illustrated in detail. In aqueous hydrochloric acid , the GEF-RES cocrystal showed that the maximum concentration of GEF was slightly higher than that of raw GEF. Furthermore, the thermal and physical stability of the GEF-RES cocrystal were also evaluated in this paper. The enhanced solubility and excellent solid-state stability results may provide new potential to the application of key GEF in clinical.
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Antioxidants
·
2022
·Vol. 11
·期 12
·2330
·
IF 7.675
Tian Su,Zhengyi Zhang,Xiao Han,Fei Yang,Zhen Wang,Ying Cheng,Huadong Liu
SIRT1 functions by regulating the modification of proteins or interacting with other proteins to form complexes. It has been widely studied and found to play significant roles in various biological processes and diseases. However, systematic studies on activated-SIRT1 interactions remain limited. Here, we present a comprehensive SIRT1 interactome under resveratrol stimulation through proximity labeling methods. Our results demonstrated that RanGap1 interacted with SIRT1 in HEK 293T cells and MCF-7 cells. SIRT1 regulated the protein level of RanGap1 and had no obvious effect on RanGap1 transcription. Moreover, the overexpression of Rangap1 increased the ROS level in MCF-7 cells, which sensitized cells to resveratrol and reduced the cell viability. These findings provide evidence that RanGap1 interacts with SIRT1 and influences intracellular ROS, critical signals for mitochondrial functions, cell proliferation and transcription. Additionally, we identified that the SIRT1-RanGap1 interaction affects downstream signals induced by ROS. Overall, our study provides an essential resource for future studies on the interactions of resveratrol-activated SIRT1. There are conflicts about the relationship between resveratrol and ROS in previous reports. However, our data identified the impact of the resveratrol-SIRT1-RanGap1 axis on intracellular ROS.Keywords:SIRT1;resveratrol;proximity labeling;RanGap1;ROS
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Food & Function
·
2020
·Vol. 11
·期 5
·4014-4025
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IF 4.171
Ye Liu,Xiao Liang,Yan Zou,Yaqi Peng,David Julian McClements,Kun Hu
The cellular uptake and simulated intestinal wall transportation of resveratrol-loaded zein/pectin nanoparticles were assessed using Caco-2 cells and monolayers, respectively. The oral bioavailabilities of encapsulated (En-RES) and free (RES) resveratrol were evaluated by monitoring the resveratrol concentration in rat plasma after oral administration. The impact of encapsulation on the anti-inflammatory activity of the resveratrol was determined using lipopolysaccharide (LPS)-treated RAW 264.7 macrophages. The cellular uptake of encapsulated resveratrol increased appreciably with observation time (1–4 h), reaching a maximum value (≈1.06 μg mL−1) after 2 h, whereas that of free resveratrol (in DMSO) only increased slightly, reaching 0.62 μg mL−1 after 4 h. The transmembrane transport of En-RES was significantly higher than that of RES (p < 0.05): the resveratrol concentration in the receiving compartment of Costar trans-wells was 4.7-fold higher for the encapsulated resveratrol. The resveratrol concentration in the plasma of rats was measured after they were fed formulations containing a resveratrol equivalent of 20 mg per kg bodyweight. The plasma level reached a maximum value of 1.35 ± 0.26 μg mL−1 at 4 h after feeding the En-RES formulation, and then decreased to 0.19 ± 0.04 μg mL−1 after 48 h. Conversely, the plasma level only reached a maximum value of 0.31 ± 0.05 μg mL−1 at 0.5 h after feeding the free resveratrol formulation (an aqueous PEG 400 solution), and was totally cleared after 8 h. Cell culture studies suggested that En-RES exhibited a strong anti-inflammatory activity by inhibiting the production of NO, PGE2, IL-1β, IL-6, TNF-α, promoting IL-10 release, inhibiting expression of TLR4, and inhibiting phosphorylation of JNK, ERK1/2, p38 and MAPK. Overall, this research suggests that zein-pectin core/shell nanoparticles are a highly effective delivery system for resveratrol, significantly increasing its bioavailability and anti-inflammation activity. These oral delivery systems may be particularly suitable for applications in functional foods or pharmaceuticals.
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EUROPEAN POLYMER JOURNAL
·
2021
·
IF 4.598
Yazhou Tian,Meng Ke,Xiuli Wang,Guangdong Wu,Junying Zhang,Jue Cheng
Preparing and designing an epoxy system with ultrahigh glass transition temperature (T g > 300 °C) is always a big challenge, which restrict its applications in some cutting-edge areas such as aerospace engineering and electrical electronics. Herein, a biomass-based epoxy resin (REEP) was prepared from resveratrol, and then curing behavior, thermal–mechanical properties, mechanical performance, thermal stability, dielectric properties and optical properties of REEP/HDDM, REEP/DGEBA/HDDM and DGEBA/HDDM were respectively studied systematically. Results suggested that the T g of REEP/HDDM was above 320 °C, higher than those of most reported epoxy systems, both derived from biomass-based and petroleum-based materials. Moreover, the tensile strength of REEP/HDDM, REEP/DGEBA/HDDM and DGEBA/HDDM were 77.8 MPa, 70.8 MPa and 63.6 MPa, respectively, and the T d5% of REEP/HDDM, REEP/DGEBA/HDDM and DGEBA/HDDM were 319.9 °C, 335.1 °C and 348.1 °C, respectively, indicating excellent mechanical performance and thermal stability of the cured epoxy system. Interestingly, the REEP/HDDM exhibited outstanding blocking properties in the range of 220–400 nm (UV-light) and low flammability with compact and continuous char residues. In short, REEP, with a well-defined chemical structure, has a stiffness conjugated stilbene structure to prevent the molecular from motioning in the crosslinked network structure and three epoxy groups, thereby increasing the crosslinked density dramatically, which endows REEP/HDDM network with outstanding comprehensive properties.
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
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2020
·
IF 4.192
Ping-Ping Wang,Zhi-Gang Luo,Tamer Mahmoud Tamer
In this work, spiral dextrin/resveratrol (SD/Res) crystal, a new colon-specific drug-delivery system, was established by a novel method of encapsulation and cocrystallization to improve the antidigestion ability compared with the SD/Res inclusion complex (SD/Res IC) prepared by encapsulation and coprecipitation. X-ray diffraction (XRD) and scanning electron microscopy (SEM) revealed that the SD/Res crystal formed a more regular and perfect crystallite than SD/Res IC. Moreover, the encapsulation ability and thermostability of the SD/Res crystal were enhanced as the chain length of SD was increased. In vitro digestion indicated that SD/Res IC merely achieved small intestine-targeted release of resveratrol, while the SD/Res crystal could act as a colon-specific delivery system to protect resveratrol from degradation by gastric acid and pancreatic enzymes. The SD-1/Res crystal presented much higher thermal stability and stronger gastrointestinal stability than other SD/Res crystals and SD/Res ICs, which facilitated its application as a novel colon-target delivery system for resveratrol.
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BMC Complementary and Alternative Medicine
·
2017
·Vol. 17
·期 1
·1-10
·
IF 2.288
Chen Long,Liu Tianjun,Wang Qiangsong,Liu Juan
Background Resveratrol and curcumin, as natural flavones products, have good therapeutic effect in acute and chronic inflammation; on the other hand, tetramethylpyrazine (TMP) has angiogenesis and vessel protection effect as well as anti-inflammatory function. In this paper, the anti-inflammatory effect of the tetramethylpyrazine, resveratrol and curcumin (TRC) combination in acute and chronic inflammation was reported in vivo.Methods The dose of the combined three natural products was optimized based on the acute paw swelling mouse model with a Uniform Design methodology. The therapeutic effect of TRC combination on chronic inflammation was investigated by using the collagen-induced arthritis (CIA) rat model based upon the following indexes: the volume of paw swelling, arthritis score, serum mediators and histological examination as well as immunohistochemical staining. The levels of alanine aminotransferase (ALT) and aspartate transaminase (AST) in serum were measured and the pathological sections of liver and kidney were analysed. LD50 was measured based on the acute oral toxicity (AOT) standard method.Results The best formulation was the three components combined at the same mass proportion revealed by the Uniform Design methodology. This combination could significantly reduce the paw swelling in acute paw swelling mouse model, could reduce paw swelling and alleviate the damage in joint structural of ankle, cartilages and fibrous tissue in CIA rat model. The dose relationship was clear in both cases. Immunohistochemical staining of ankle tissue revealed that TRC combination was able to inhibit the expression of NF-κB p65 and TNF-α which were closely related to the inflammatory process. Analysis of serum mediators revealed TRC combination could inhibit the production of TNF-α, IL-1β, and IL-6 in the serum. Toxic study revealed this formulation was low toxic, LD50 was larger than 5 g/kg, both the level of ALT and AST and histopathology in the liver and kidney exhibited no distinctions between the TRC combination and the blank group, no mortality occurred at the administered doses of 5 g/kg.Conclusion sThe results showed this formulation could provide a novel potent treatment for acute and chronic inflammation (RA) without side effect like gastric injury occurring in NSAIDs.
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Scientific Reports
·
2016
·Vol. 6
·期 1
·1-10
·
IF 5.228
Zhang Junqiang,Song Xianbin,Cao Wei,Lu Jinseng,Wang Xiaoqing,Wang Gaoyuan,Wang Zhicheng,Chen Xiaoyu
Resveratrol is a polyphenol derivatives which exhibits a pro-apoptotic effect in a variety of human cancers by triggering mitochondria apoptosis pathway and autophagy. However, there are scarcely reports on its apoptosis-promoting effect in abnormal proliferation fibroblast-like synoviocytes (FLSs). In this study, we investigated the underlying mechanism and apoptosis-inducing effects of resveratrol on the abnormal proliferation of FLSs in adjuvant-arthritis (AA) rats. Since using resveratrol for 12 days resulted in a significant decreasing the swelling degree of the paw, reducing malondialdehyde (MDA) content and enhancing superoxide dismutase (SOD) activity, antioxidant capacity, glutathione peroxidase and glutathione reductase ratio in AA rats. Moreover, we found that 5 μMH 2 O 2 could increase cells viability, Beclin1, LC3A/B, MnSOD, SIRT3 protein expression in FLSs. But, resveratrol could reverse these effects by changing mitochondrial membrane potential (Δψm) to promote mitochondrial reactive oxygen species (mtROS) generation in 5 μMH 2 O 2 -treatment FLSs. These results suggest that oxidative stress existed in AA rats. Resveratrol could suppress oxidative stress in AA rats and increase mtROS production by reducing autophagy protein Beclin1, LC3A/B and oxidative stress protein MnSOD to promoted the apoptosis of FLSs. Thus, targeting of mtROS may be a crucial mechanism of resveratrol confers patients with rheumatoid arthritis.
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