INTERNATIONAL JOURNAL OF FOOD SCIENCE AND TECHNOLOGY
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2025
·
IF 3.1
Zhang Qiong,Yu Ying,Cheng Keyun,Deng Dan,He Shunv,Chen Chao,Wang Yingqian,Jin Danping,Shen Qing
Resveratrol (Res) has many potential benefits for human health. This investigation employed a complex protein system comprising pea protein isolate (PPI) and whey protein isolate (WPI) as an innovative carrier for Res delivery. The effect of PPI and WPI binding on protein conformation was investigated and differences in Res delivery by PW (pea protein isolate-whey protein isolate) complex protein and single PPI and WPI proteins were compared. The secondary structure and surface hydrophobicity results showed that the formation of PW complex protein increased the flexibility and surface hydrophobicity. Fluorescence spectroscopy results indicated that compared to single proteins, PW complex protein could bind more efficiently to Res through hydrophobic interactions. The PW-Res complex achieved higher encapsulation efficiency (EE), improving by 59.17% and 25.80% over PPI and WPI, respectively, and more significantly increased the antioxidant activity of Res by 36.89%. Furthermore, the smaller average particle size (173.95 ± 10.94 nm) and larger absolute value of ζ-potential (27.07 ± 0.49 mV) of the PW-Res complex resulted in better stability compared to the PPI-Res and WPI-Res complexes. This study has significant implication for encapsulation of hydrophobic active ingredients such as Res using complex protein systems.
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JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY
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2022
·Vol. 36
·期 9
·e23120
·
IF 3.568
Jun-Heng Jiao,Lei Gao,Wen-Long Yong,Zhong-Yun Kou,Zhi-Qiang Ren,Rui Cai,Gui-Yan Chu,Wei-Jun Pang
Bisphenol A (BPA), as a widely used plasticizer, is easily absorbed by animals and humans. It has certain toxic effects on various tissues, including liver, heart, kidney, testis, and ovary. The toxic effects of BPA on animal reproduction have aroused widespread concern, but its regulatory mechanism and antidote in female animals estrus cycle remain unclear. In this study, the results displayed that BPA destroyed the normal estrus cycle of mice through decreasing the levels of progesterone and estradiol. Furthermore, BPA significantly increased the levels of oxidative stress, autophagy, and apoptosis in ovaries and granulosa cells. Interestingly, we found that the natural antioxidant resveratrol rescued estrus disorder and impaired estradiol secretion, reduced the abnormal reactive oxygen species accumulation, autophagy, and apoptosis in BPA exposed ovarian tissues. Moreover, transmission electron microscopy showed that resveratrol reduced BPA-induced autophagic vesicles formation and flow cytometry showed that resveratrol inhibited the increase of apoptotic cells induced by BPA on granulosa cells. Therefore, the supplement of resveratrol could restore BPA-induced estrus disorder by protecting ovarian granulosa cells. Overall, resveratrol is a potential drug to alleviate BPA-induced estrous cycle disorders and ovarian damage.
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Pharmaceutics
·
2022
·Vol. 14
·期 3
·603
·
IF 6.525
Dandan Hu,Xin Chen,Duanxiu Li,Hailu Zhang,Yanwen Duan,Yong Huang
Matrine (MAR), oxymatrine (OMAR), and sophoridine (SPD) are natural alkaloids with varying biological activities; matrine was recently used for the treatment of coronavirus disease 2019 (COVID-19). However, the short half-lives and rapid elimination of these matrine-type alkaloids would lead to low oral bioavailability and serious side effects. Herein, resveratrol (RES) was selected as a co-former to prepare their co-amorphous systems to improve the therapeutic index. The formation of co-amorphous MAR-RES, OMAR-RES, and SPD-RES was established through powder X-ray diffraction and modulated temperature differential scanning calorimetry. Furthermore, Fourier transform infrared spectroscopy and NMR studies revealed the strong molecular interactions between resveratrol and these alkaloids, especially OMAR-RES. Matrine, oxymatrine, and sophoridine in the co-amorphous systems showed sustained release behaviors in the dissolution experiments, due to the recrystallization of resveratrol on the surface of co-amorphous drugs. The three co-amorphous systems exhibited excellent physicochemical stability under high relative humidity conditions. Our study not only showed that minor structural changes of active pharmaceutical ingredients may have distinct molecular interactions with the co-former, but also discovered a new type of sustained release mechanism for co-amorphous drugs. This promising co-amorphous drug approach may present a unique opportunity for repurposing these very promising drugs against COVID-19.Keywords:co-amorphous systems;sustained-release;COVID-19;matrine-type alkaloids;resveratrol
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COLLOIDS AND SURFACES B-BIOINTERFACES
·
2022
·
IF 5.999
Bowen Li,Mei Wang,Yuhua Liu,Yongsheng Zhou,Lin Tang,Pengyue You,Yi Deng
Due to their natural biological activity and low immunogenicity , decellularized extracellular matrix (ECM) materials have aroused interest as potential scaffold materials in tissue engineering. Decellularized small intestinal submucosa (SIS) is one ECM biomaterial that can be easily sourced. In the present study, we tested whether the osteogenesis of SIS scaffolds was enhanced via structural optimization and resveratrol (RSV) functionalization and explored the independent effects of these modifications. We obtained SIS scaffolds with different pore structures by controlling the preparation concentration. The group with superior osteogenic properties was further RSV-functionalized via covalent immobilization. We conducted a series of in vitro and in vivo studies to explore the effects of these two optimization strategies on the osteogenic properties of SIS scaffolds. The results showed that pore structure and RSV functionalization significantly affected the osteogenic properties of SIS scaffolds. With a fabrication concentration of 1%, the SIS scaffolds had superior osteogenic properties. Through covalent coupling, RSV was successfully grafted onto SIS scaffolds, where it was slowly released. The most significant improvements in osteogenic properties were obtained with a coupling concentration of 1%. Furthermore, in in vivo experiments, vascular and new bone tissue formation was enhanced with RSV/SIS scaffolds compared with SIS scaffolds and the blank control group at 4 weeks after implantation. These findings indicate that the RSV/SIS scaffolds obtained via dual optimization strategies show promise as biomaterials in bone tissue engineering.
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Nanomaterials
·
2021
·Vol. 11
·期 11
·3060
·
IF 5.076
Jinxing Zhang,Qi Ouyang,Qilin Gui,Xiaonong Chen
Scalable preparation of graphene with high adsorption capacity is an important prerequisite for fully realizing its commercial application. Herein, we propose an environmentally friendly route for exfoliation of graphene, which is established based on the Diels–Alder reaction. In our route,N-(4-hydroxyl phenyl) maleimide enters between the flakes as an intercalating agent and participates in the Diels–Alder reaction as a dienophile to increase the interlayer spacing of graphite. Then, graphite is exfoliated into graphene with the aid of ultrasound. The exfoliated product is hydroxyl phenyl functionalized graphene with a thickness of 0.5–1.5 nm and an average lateral size of about 500–800 nm. The exfoliation process does not involve any acid or catalyst and would be a safe and environmentally friendly approach. In addition, the exfoliated graphite shows high resveratrol adsorption capacity, which is ten times that of macroporous resins reported in the literature. Thus, the method proposed herein yields exfoliated graphite with high resveratrol adsorption capacity and is of great significance for the mass production of graphene for practical applications.Keywords:graphene;Diels–Alder reaction;exfoliation;resveratrol;adsorption
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EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
·
2019
·
IF 4.833
Liu Zeng Chen,Li Yao,Ming Ming Jiao,Jing Bo Shi,Yue Tan,Ban Feng Ruan,Xin Hua Liu
In order to discover novel anti-inflammatory agents, total thirty-seven new resveratrol-based flavonol derivatives were designed and synthesized. All compounds have been screened for their anti-inflammatory activity by evaluating their inhibition effect of LPS-induced NO production in RAW 264.7 macrophages. Their toxicity was also assessed in vitro . Structure-activity relationships (SARs) have been concluded, and finally 2-(2,4-dimethoxy-6-(4-methoxystyryl)phenyl)-3-hydroxy-4H-chromen-4-one was found to be the most active scaffold with low toxicity. This compound could significantly decrease productions of NO, IL-6 and TNF-α with IC 50 values of 1.35, 1.12 and 1.92 μM, respectively in RAW 264.7 macrophages. Preliminary mechanism studies indicated that it could inhibit the expression of TLR4 protein, resulting in activation of the NF-ĸB cell signaling pathway. The in vivo anti-inflammatory activity of this compound could reduce pulmonary inflammation by mouse model of LPS-induced acute lung injury (ALI). We believe these findings would further support studies of rational design of more efficient acute lung injury regulatory inhibitors.
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INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2023
·
IF 5.8
Tao Chen,Lihang Chen,Fengxian Luo,Yu Xu,Di Wu,Yanfei Li,Runan Zhao,Ziqi Hua,Jiangning Hu
Developing innovative strategies for the oral administration of phytochemicals presents a promising approach to addressing intestinal diseases. However, numerous challenges persist, including limited therapeutic efficacy, poor bioavailability, and inadequate biocompatibility. In this study, we employed a cross-linked cyclodextrin-metal organic framework (CDF) to encapsulate resveratrol (Res), generating Res-CDF, which was subsequently incorporated into natural polysaccharide hydrogel microspheres (Res-CDF in MPs) for targeted oral delivery to alleviate ulcerative colitis (UC). The underlying adsorption mechanism of Res by γ-CD elucidated by molecular dynamics simulations. Importantly, the Res-CDF in MPs formulation protected against gastric acid degradation while preserving the bioactivity of Res. Moreover, the design enabled specific release of Res-CDF in response to the mildly alkaline environment of the intestinal tract, followed by sustained Res release. In UC mice model, Res-CDF in MPs demonstrated potent anti-inflammatory effects by attenuating pro-inflammatory cytokine production and exhibited antioxidant properties. Additionally, Res-CDF in MPs enhanced the expression of tight junction proteins ZO-1, Occludin, and mucin-2 (Muc-2), thereby maintaining normal intestinal barrier function. This innovative oral delivery strategy capitalizes on the advantageous properties of polysaccharide hydrogel and CDF to augment bioavailability of phytochemicals, laying the groundwork for developing novel oral interventions employing natural phytochemicals to address intestinal-related diseases.
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Biomolecules & Therapeutics
·
2023
·
IF 3.7
Nayun Kim,Junhye Kwon,Ui Sup Shin,Joohee Jung
Colorectal cancer (CRC) is one of the most high-risk cancers; however, it has been suggested that estrogen signaling in CRC could have a protective effect. Therefore, we focused on the function of the G protein-coupled estrogen receptor (GPER) among the estrogen receptors in CRC. In this study, we investigated the therapeutic effect of resveratrol via GPER in CRC (RKO and WiDr) cells, CRC cell-derived xenograft models, and organoids (30T and 33T). Resveratrol significantly suppressed cell viability and proliferation in highly GPER-expressing RKO cells compared to that in low GPER-expressing WiDr cells. In xenograft models, resveratrol also delayed tumor growth and exhibited a high survival rate depending on GPER expression in RKO-derived tumors. Furthermore, resveratrol significantly inhibited the viability of organoids with high GPER expression. Additionally, the anticancer effect of resveratrol on CRC showed that resveratrol rapidly responded to GPER, while increasing the expression of p-ERK and Bax and cleaving PARP proteins.
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Archives of Medical Science
·
2020
·
IF 2.807
Ning Xu,Lili Wang,Shiping Fu,Bin Jiang
Introduction Osteosarcoma is the most common primary malignancy of the bone. The existing adjuvant chemotherapy regimens, while improving the overall survival, have been limited by the significant systemic toxicity. Substantial clinical and research efforts are being invested to develop novel pharmaceutical agents. Resveratrol (Res) has been suggested to have a chemopreventive effect. However, the mechanism of Res in osteosarcoma remains to be elucidated. Material and methods The MG-63 osteosarcoma cell culture model was used to investigate the chemotherapeutic effect of Res. MTT assay, wound healing assay, and Transwell migration assay were used to document the effect of Res on cell proliferation, migration, and invasion, respectively. Apoptosis in MG-63 cells was quantified with the TUNEL assay. Western blotting analysis was used to examine the molecular changes following Res treatment. Data processing and analysis were conducted using GraphPad Prism 5.0. P < 0.05 was considered statistically significant. Results Our data suggested that Res blocks cell proliferation, migration, and invasion, and activates apoptotic cell death in osteosarcoma MG-63 cells. We found that Res potentially down-regulates nuclear factor κB (NF-κB) and Akt intracellular signaling transduction. Moreover, the combination of Res and pyrrolidine dithiocarbamate (PDTC), an NF-κB inhibitor, resulted in synergistic growth inhibition of osteosarcoma. Conclusions Our in vitro preclinical study in the MG-63 cell line model supports the translation of Res to the clinical management of patients with osteosarcoma.
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Bioactive Materials
·
2020
·
IF 8.724
Limei Li,Mali Yu,Yao Li,Qing Li,Hongcai Yang,Meng Zheng,Yi Han,Di Lu,Sheng Lu,Li Gui
The development of functional materials for osteoporosis is ultimately required for bone remodeling. However, grafts were accompanied by increasing pro-inflammatory cytokines that impaired bone formation. In this work, nano-hydroxyapatite (n-HA)/resveratrol (Res)/chitosan (CS) composite microspheres were designed to create a beneficial microenvironment and help improve the osteogenesis by local sustained release of Res. Study of in vitro release confirmed the feasibility of n-HA/Res/CS microspheres for controlled Res release. Notably, microspheres had anti-inflammatory activity evidenced by the decreased expression of pro-inflammatory cytokines TNF-α, IL-1β and iNOS in RAW264.7 cells in a dose dependent manner. Further, enhanced adhesion and proliferation of BMSCs seeded onto microspheres demonstrated that composite microspheres were conducive to cell growth. The ability to enhance osteo-differentiation was supported by up-regulation of Runx2, ALP, Col-1 and OCN, and substantial mineralization in osteogenic medium. When implanted into bone defects in the osteoporotic rat femoral condyles, enhanced entochondrostosis and bone regeneration suggested that the n-HA/Res/CS composite microspheres were more favorable for impaired fracture healing. The results indicated that optimized n-HA/Res/CS composite microspheres could serve as promising multifunctional fillers for osteoporotic bone defect/fracture treatment.
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MOLECULAR NUTRITION & FOOD RESEARCH
·
2020
·Vol. 64
·期 14
·2000105
·
IF 5.309
Yanan Chen,Hao Zhang,Yueping Chen,Yuying Zhang,Mingming Shen,Peilu Jia,Shuli Ji,Tian Wang
Scope Endoplasmic reticulum (ER) stress is widely recognized as a critical factor linked to lipid metabolic disorders in nonalcoholic fatty liver disease. However, its pathogenesis remains elusive, and therapeutic options are limited. This study investigates the potential of resveratrol (RSV) to alleviate hepatic steatosis and injury in a tunicamycin (TM)-induced murine ER stress model and provides detailed evidence. Methods and Results Male C57BL/6J mice were orally administered either RSV or vehicle for 2 weeks before the TM challenge. Results indicated that TM induced ER morphological damage and severe unfolded protein reaction (UPR), accompanied by increases in lipid accumulation, oxidative damage, and inflammatory response. Administering RSV decreased the expression of ER stress markers, partially normalized the active levels of UPR sensors, and facilitated sirtuin 1 activity in the liver under ER stress. Notably, the TM-induced hepatic steatosis was also alleviated by RSV, possibly by regulating the expression pattern of genes involving lipid oxidation and delivery. Consistently, RSV attenuated the TM-induced increases in lipid peroxidation, hepatocyte apoptosis, and the overactivation of inflammatory signals. Conclusion RSV may have an auxiliary therapeutic potential to prevent the development of steatosis and its progression to steatohepatitis in the liver by alleviating severe ER stress.
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ACTA PHARMACOLOGICA SINICA
·
2021
·Vol. 43
·期 5
·1264-1273
·
IF 6.15
Ren Zheng-nan,Yang Jun,Zhang Meng-ya,Huang Yi-wen,Song Dong-xiao,Sun Xun,Pan Li-long,Sun Jia
Acute pancreatitis (AP), an inflammatory disorder of the pancreas, is a complicated disease without specific drug therapy. ( R )-4,6-dimethoxy-3-(4-methoxy phenyl)-2,3-dihydro-1H-indanone [( R )-TML104] is a synthesized analog of the natural product resveratrol sesquiterpenes (±) -isopaucifloral F. This study aimed to investigate the effect and underlying mechanism of ( R )-TML104 on AP. The experimental AP model was induced by caerulein hyperstimulation in BALB/c mice. ( R )-TML104 markedly attenuated caerulein-induced AP, as evidenced by decreased pancreatic edema, serum amylase levels, serum lipase levels, and pancreatic myeloperoxidase activity. In addition, ( R )-TML104 significantly inhibited the expression of pancreatic chemokines C–C motif chemokine ligand 2 and macrophage inflammatory protein-2 and the infiltration of neutrophils and macrophages. Mechanistically, ( R )-TML104 activated AMP-activated protein kinase and induced sirtuin 1 (SIRT1) expression. ( R )-TML104 treatment markedly induced the SIRT1-signal transducer and activator of transcription 3 (STAT3) interaction and reduced acetylation of STAT3, thus inhibiting the inflammatory response mediated by the interleukin 6-STAT3 pathway. The effect of ( R )-TML104 on SIRT1-STAT3 interaction was reversed by treatment with a SIRT1 inhibitor selisistat (EX527). Together, our findings indicate that ( R )-TML104 alleviates experimental pancreatitis by reducing the infiltration of inflammatory cells through modulating SIRT1.
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