IRANIAN POLYMER JOURNAL
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2022
·Vol. 31
·期 10
·1225-1235
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IF 2.485
Mehmood Sahid,Uddin Md Alim,Yu Haojie,Wang Li,Amin Bilal Ul,Haq Fazal,Fahad Shah,Haroon Muhammad
Polymeric materials are used as ideal carriers for drug delivery applications due to their excellent physicochemical properties, however, the controlled preparation and drug release behavior of cross-linked polymeric microspheres are still open to discussion. Hexacyclotriphosphazene (HCCP), as one of the prominent members of polyphosphazene, can be easily treated with many monomers to produce micro/nanospheres. In this research work, cross-linked poly(cyclotriphosphazene- co -resveratrol) (PCTPRS) microspheres were prepared by the precipitation reaction of HCCP and resveratrol (RSV). The apparent peak at 961 cm −1 in FTIR spectra of the microspheres revealed that the polymerization between RSV and HCCP was successful. The TGA results showed that the increase in thermal properties was owing to the highly cross-linked structure of the microspheres. The XRD patterns showed the amorphous nature of the microspheres compared to the monomers. The obtained SEM micrographs dictated that the HCCP:RSV mole ratio had a significant impact on the size of the microspheres. The PCTPRS microspheres were used as carriers for the drug loading and release study of the anti-cancer model drug camptothecin (CPT). The drug loading efficiency of the PCTPRS microspheres was found to be 89.9 mg/g. Whereas the release study revealed that 53.0% of CPT was released at pH 4.0 and 37.5% at pH 7.4 from the drug-loaded microspheres after 11 days. Graphical abstract
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Gels
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2022
·Vol. 8
·期 9
·544
·
IF 4.432
Ningxin Cui,Zhen Xu,Xinyu Zhao,Meng Yuan,Leiyu Pan,Tianfeng Lu,Ai Du,Lili Qin
Resveratrol (Res) is a plant extract with strong anti-inflammatory, antioxidant and anti-aging biological activities. However, Res is limited by its disadvantages, such as poor solubility, rapid metabolism and low bioavailability. In this study, the Resveratrol-loaded TEMPO-oxidized cellulose aerogel (RLTA) drug delivery system was prepared by the method of “dissolution-freeze-drying” and characterized by a series of analysis. Then the blood biochemical indexes and HE staining were measured and analyzed in animal experiments. The in vivo results showed that RLTA can decrease the levels of TNF-α and IL-6 inflammatory factors in the synovial fluid. Furthermore, the molecular mechanism was investigated through the analysis of silent information regulator 2 homolog 1 (Sirt1) protein expression, which suggested that RLTA could upregulate the expression of Sirt1 and mediate the P38 signaling pathway, thereby inhibiting the expression of COX-2 and MMP13 which can suppress the levels of IL-6 and TNF-α inflammatory factor. These results reveal that cellulose aerogel is a promising candidate for drug delivery and RLTA has great potential application for the treatment of sports osteoarthritis.Keywords:osteoarthritis;cellulose aerogel;resveratrol;anti-inflammatory
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INDUSTRIAL CROPS AND PRODUCTS
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2022
·
IF 6.449
Chengjiang Lu,Shuai Bian,Ke Hu,Caicai Li,Kaiwen Zheng,Qingfeng Sun
Preparing biomass-based epoxy resin with high temperature resistance and flame retardancy is still an appealing yet challenging task. Now, a high-temperature resistant and flame-retardant resveratrol-based epoxy (RESEP) has been synthesized through a facile one-step method. The structure of RESEP was established using FTIR and NMR spectroscopy . RESEP and petroleum-based epoxy diglycidyl ether of bisphenol A (DGEBA) were each cured with 4,4-diaminodiphenyl methane (DDM) to prepare RESEP/DDM and DGEBA/DDM. Differential scanning calorimetry (DSC), dynamic mechanical analysis (DMA), tensile testing, thermogravimetric analysis (TGA), thermogravimetric analysis-infrared spectroscopy (TG-IR), scanning electron microscopy (SEM), limiting oxygen index (LOI) and the UL-94 vertical burning test were used to systematically evaluate the properties of RESEP and RESEP/DDM. The glass transition temperature (T g ) of RESEP/DDM is 335 ℃, which is significantly higher than that of DGEBA/DDM (168 ℃). In addition, RESEP/DDM displays good thermogravimetric performance and flame retardancy. Typically, it displays a UL-94 V-0 rating, an LOI value was as high as 31.8%, and a char yield as high as 38.6% (800 ℃). The results reported indicate the possibility of preparing biomass-based epoxy resin with high temperature resistance, flame retardancy and mechanical properties, which is potential to be utilized in the fields of electronics and aerospace.
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DRUG DELIVERY
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2022
·
IF 6.819
Yingqiao Li,Zhiru Zou,Jinyu An,Qian Wu,Le Tong,Xifan Mei,He Tian,Chao Wu
Spinal cord injury (SCI) is a serious central nervous system disease, and secondary injury, including oxidative stress, the inflammatory response and accompanying neuronal apoptosis, will aggravate the condition. Due to the existence of the blood–spinal cord barrier (BSCB), the existing drugs for SCI treatment are difficulty to reach the injury site and thus their efficacy is limited. In this study, we designed chitosan-modified hollow manganese dioxide nanoparticles (CM) for the delivery of resveratrol to help it pass through the BSCB. Resveratrol (Res), a poorly soluble drug, was adsorbed into CM with a particle size of approximately 130 nm via the adsorption method, and the drug loading reached 21.39 ± 2.53%. In vitro dissolution experiment, the Res release of the loaded sample (CMR) showed slowly release behavior and reached about 87% at 36 h. In vitro at the cellular level and in vivo at the animal level experiments demonstrated that CMR could alleviate significantly oxidative stress by reducing level of reactive oxygen species (ROS), malondialdehyde (MDA), superoxide dismutase (SOD), and increasing glutathione peroxidase (GSH) level. Additionally, immunofluorescence (iNOS, IL-1β, and Cl caspase-3) and western blot (iNOS, cox-2, IL-1β, IL-10, Cl caspase-3, bax, and bcl-2) were used to detect the expression of related factors, which verified that CMR could also reduce inflammation and neuronal apoptosis. These results indicated that CM, as a potential central nervous system drug delivery material, was suitable for SCI treatment.
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Asian Journal of Pharmaceutical Sciences
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2022
·
IF 9.273
Ziting Zhang,You Ji,Nan Hu,Qinqi Yu,Xinrui Zhang,Jie Li,Fenglei Wu,Huae Xu,Qiyun Tang,Xiaolin Li
Ferroptosis is a novel form of programmed cell death impelled by iron-dependent lipid peroxidation, which may be a potential strategy for cancer therapy. Here we demonstrated for the first time that Resveratrol (RSV), a traditional Chinese medicine (TCM) chemical monomer, could effectually inhibit the growth of colon cancer cells through the ROS-dependent ferroptosis pathway. Mechanistically, RSV evoked the increase of reactive oxygen species and lipid peroxidation in colorectal cancer cells, and eventually lead to ferroptosis. Furthermore, RSV could promote ferroptosis by downregulating the expression of the channel protein solute carrier family 7 member 11 (SLC7A11) and glutathione peroxidase 4 (GPX4). To improve the delivery efficiency of RSV, a biomimetic nanocarrier was developed by coating RSV-loaded poly(ε-caprolactone)–poly(ethylene glycol) (PCL-PEG) nanoparticles with erythrocyte membrane ( [email protected] ). The [email protected] provide the possibility to escape macrophage phagocytosis and have a long circulation effect. In addition, when coupled with a tumor-penetrating peptide iRGD, which could trigger enhanced tissue penetration tumor-specifically, the delivery of [email protected] into tumors would be significantly improved results from the in vivo study demonstrated an excellent treatment efficacy for CRC. Altogether, our study highlighted the therapeutic potential of RSV as a ferroptosis-inducing anticancer agent and when loaded into a biomimetic nanoplatform, it might pave the way for the application of RSV loaded nanosystems for colorectal cancer treatment.
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INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2021
·
IF 5.875
Huanyue Zhou,Yu Wang,Shuting Li,Ming Lu
Hot melt extrusion (HME) is a technique applied in the preparation of pharmaceutical amorphous solid dispersions (ASD). Notably it is important to prevent thermal degradation of heat-sensitive drugs during HME. In this study, we present a new strategy to improve chemical stability of pharmaceutical compounds during HME through the formation of eutectics with small molecules. Resveratrol (RES) was selected as the model compound because it is a heat-liable natural product with a very high melting point of 267 °C. When heated at its melting point for 3 min, it degrades by 40%. RES can co-crystallize with nicotinamide (NIC) in solution, however, it can only form a eutectic with NIC during heating. HPMCAS was selected as the polymer matrix and the drug loading of RES was fixed as 20% (weight ratio). The lowest extrusion temperature that can result to RES-HPMCAS ASD is 215 °C. At this temperature, RES shows 7.36% degradation during extrusion. Replacement of 21.4% HPMCAS with NIC decreased the melting temperature of NIC and thus lowered the minimal extrusion temperature to 155 °C. This effectively prevented thermal degradation of RES without negatively affecting non-sink dissolution. The only extra cost for this method is stricter storage conditions (low temperature and low humidity) due to the low glass transition temperature of NIC. Similar strategy may be applied to other heat-liable drugs in similar ways. This study demonstrates the use of eutectic formation for preventing thermal degradation of drug during extrusion of ASD.
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Frontiers in Pharmacology
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2021
·
IF 5.811
Hao Xincai,Sun Xiaodong,Zhu Haizhen,Xie Lixia,Wang Xuanbin,Jiang Nan,Fu Pan,Sang Ming
Trans-resveratrol (RES) exhibits a wide range of biological activities. Various methodological approaches have been established to improve the pharmacokinetic properties of RES. Moreover, additional in vivo studies are required to support clinical application. In this study, RES/HP-β-CD (RHSD) inclusion complex was prepared and characterized by FTIR, PXRD, DSC and NMR data. The effect and potential mechanism of RHSD against cervical cancer were investigated in a mouse xenograft tumor model by qPCR assay, Western blot assay, and immunohistochemical assay. Results showed that RHSD significantly decreased tumor growth compared with free RES, while the effect of preventing tumor growth was more prominent in vivo. Notably, RHSD could inhibit tumor development by suppressing the expression of HPV E6 and E7 oncogenes and upregulating P53 and Rb1 protein in cervical cancer. These findings demonstrated that RHSD was safe and potential for development of a new oral administration drug to treat cervical cancer.
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FREE RADICAL RESEARCH
·
2020
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IF 2.839
Bo Yin,Rui Rui Liu,Ya Jie Meng,Hong Lin Zhai,Sha Sha Li,Jules Muhire
Found in various natural food products, many in vitro evidence indicated that resveratrol (RES) has been linked to neuroprotective and cardioprotective effects and prevent cancer development. However, human clinical trials have been conducted with varying results, making the usage of RES controversial. In this paper, we demonstrated that the drug RES could be conjugated with the high levels of endogenous GSin cancer cells. 5,5-Dimethyl-1-Pyrroline-N-Oxide (DMPO) was employed to capture the GS•. The molecular mechanism of the reaction between RES and GSwas further studied by UV-Vis spectrometry, mass spectrometry and Density Functional Theory (DFT) calculations. Besides, the formation of the adduct GS-RES in cancer cell was obtained when RES was added during incubation. Further study indicated that over 77.6% of the RES was consumed in cancer cells. This study suggested that endogenous GSmay be one of the important factors to cause the depletion of anti-tumour drugs during chemotherapy, which should be paid special attention in clinical therapeutics and drug development.
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Polymers
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2020
·Vol. 12
·期 12
·2794
·
IF 3.426
Yunliang Xing,Xianru He,Rui Yang,Kan Zhang,Shengfu Yang
A novel resveratrol-based bio-benzoxazine monomer (RES-al) containing an allyl group has been synthesized using resveratrol, allylamine, and paraformaldehyde via Mannich condensation reaction, and its chemical structures have been characterized by FT-IR spectroscopy and NMR techniques. The polymerization behavior of this benzoxazine resin has been investigated using in situ FT-IR and differential scanning calorimeter (DSC) measurements, and the thermal-mechanical properties of its corresponding polybenzoxazines are evaluated by DMA and TGA. We show that by controlling the curing process of the oxazine ring, the C=C bond in resveratrol, and the allyl group in RES-al, the cross-linking network of the polybenzoxazine can be manipulated, giving rise to tunable performance of thermosets. As all curable functionalities in RES-al are polymerized, the resulted polybenzoxazine exhibits a good thermal stability with aTgtemperature of 313 °C, a Td5value of 352 °C, and char yield of 53% at 800 °C under N2.Keywords:benzoxazine;resveratrol;polybenzoxazine;allyl;high-performance
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MOLECULES
·
2022
·Vol. 27
·期 23
·8475
·
IF 4.927
Lanxin Bao,Jing Ye,Nannan Liu,Yubao Shao,Wenhao Li,Xuefei Fan,Dahai Zhao,Hongzhi Wang,Xiaoyu Chen
Interstitial lung disease associated with rheumatoid arthritis (RA-ILD) can lead to interstitial fibrosis and even lung failure as a complication of rheumatoid arthritis (RA), and there is currently no effective treatment and related basic research. Studies have found that resveratrol (Res) can improve the progression of RA by regulating autophagy, and increasing evidence supports the connection between autophagy and common interstitial lung disease (ILD). We explored changes in autophagy levels in fibrotic lungs in RA-ILD and found that the level of autophagy is enhanced in the early stage but inhibited in the late stage. However, resveratrol treatment improved the level of autophagy and reversed the inhibition of autophagy, and attenuated fibrosis. We created corresponding cell models that exhibited the same phenotypic changes as animal models; under the effect of resveratrol, the level of fibrosis changed accordingly, and the fusion process of lysosomes and autophagosomes in autophagy was liberated from the inhibition state. Resveratrol effects were reversed by the addition of the late autophagy inhibitor chloroquine. These results suggest that resveratrol attenuates pulmonary fibrosis, increases autophagic flux, and modulates the autophagy–lysosome pathway, and particularly it may work by improving the formation of autophagic lysosomes, which may be an effective treatment for induced RA-ILD.Keywords:RA-ILD;resveratrol;autophagy;fibrosis;P62/SQSTM1
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PROGRESS IN ORGANIC COATINGS
·
2023
·
IF 6.6
Zhixi Zhao,Xiang Wang,Jizhen Tian,Yunfei Gao,Fei Chen,Shuai Li,Huawei Zou,Pengbo Liu
The production of epoxy resins with low dissipation factor ( D f ) remains an alluring yet challenging task. In this work, we successfully synthesized a novel resveratrol based active ester (ResE) by a one-step method using the renewable resveratrol as raw material. The structure of ResE was characterized using FTIR and NMR techniques. The phenol biphenyl epoxy (SQXN-324) was cured with ResE, the SQXN/ResE system boasted a favorable dielectric constant ( D k ) of 2.78 and dissipation factor ( D f ) of 3.5 × 10 −3 at a high frequency of 10 GHz. Additionally, the SQXN/ResE system exhibited impressive thermal performances, with a 5 % weight loss temperature ( T 5% ) of 368 °C, a residual carbon of 34 wt% at 800 °C in N 2 atmosphere, a glass transition temperature ( T g ) of 154 °C, a coefficient of thermal expansion (CTE) of 61.9 ppm/°C from 25 °C to T g and the CTE of 130 ppm/°C from T g to 250 °C. These findings suggested that a biomass curing agent for epoxy with low D f and high thermal performances were successfully developed, it had potential applications in the high frequency communication field and microelectronics industry.
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Food Bioscience
·
2023
·
IF 5.2
Wenya Ke,Juan Huang,Yi Zhong,Yuhong Shi,Fen Yan,Da Huang,Yuanzi Wu,Houbing Zheng,Zuquan Weng
Non-alcoholic fatty liver disease (NAFLD) has become a globally rising issue that can cause liver-related morbidity and mortality. Recent studies have revealed that a high-fat diet (HFD) highly contributes to the prevalence and progression of NAFLD via impacting gut microbiota and lipid metabolism signal pathways. Resveratrol (RSV), a natural bioactive compound , has exhibited potential for preventing and alleviating NAFLD. However, due to the poor bioavailability of RSV, its strengths and underlying mechanisms for NAFLD therapeutic potential are poorly understood. To address this, we utilized Hydroxypropyl-beta-Cyclodextrin (HBC) to encapsulate RSV to enhance its water solubility and conducted prevention and intervention experiments in HFD-fed mice. The results showed that the HBC has significantly enhanced the water solubility of RSV by 250-fold and the HBC-RSV better prevented and alleviated the liver steatosis, obesity and abnormal lipid metabolism induced by HFD than RSV alone. Meanwhile, combining HFD and HBC-RSV or RSV prevented HFD mice progressing to NAFLD. Besides, further investigation indicated that RSV could resist liver injury and obesity by modulating gut microbiota, raising the levels of short-chain fatty acids (SCFAs) and activating AMP-activated protein kinase (AMPK) signaling pathway . The activated pathway down-regulated sterol receptor element binding protein 1c (SREBP1c) and acetyl-coenzyme A carboxylase (ACC) to decrease lipid synthesis and up-regulated peroxisome proliferators-activated receptorα (PPARα) to promote the fatty acid oxidation , thus preventing NAFLD. Our findings suggested that water solubility-enhanced RSV beneficially modulated gut microbiota, altered gut microbiota-derived SCFAs, and activated lipid metabolism regulatory pathways, providing potential for NAFLD prevention and alleviation.
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