Materials
·
2020
·Vol. 13
·期 7
·1624
·
IF 3.057
Lili Qin,Xinyu Zhao,Yiwei He,Hongqiang Wang,Hanjing Wei,Qiong Zhu,Ting Zhang,Yao Qin,Ai Du
Resveratrol is a natural active ingredient found in plants, which is a polyphenolic compound and has a variety of pharmaceutical uses. Resveratrol-loaded TEMPO-oxidized cellulose aerogel (RLTA) was prepared using a freeze-drying method, employing high speed homogenization followed by rapid freezing with liquid nitrogen. RLTAs were designed at varying drug–cellulose aerogel ratios (1:2, 2:3, 3:2, and 2:1). It could be seen via scanning electron microscopy (SEM) that Res integrated into TEMPO-oxidized cellulose (TC) at different ratios, which changed its aggregation state and turned it into a short rod-like structure. Fourier transform infrared (FTIR) spectra confirmed that the RLTAs had the characteristic peaks of TC and Res. In addition, X-ray diffraction (XRD) demonstrated that the grain size of RLTA was obviously smaller than that of pure Res. RLTAs also had excellent stability in both simulated gastric fluid and phosphate buffer solution. The drug release rate was initially completed within 5 h under a loading rate of 30.7 wt%. The results of an MTT assay showed the low toxicity and good biocompatibility of the RLTAs. TC aerogel could be a promising drug carrier that may be widely used in designing and preparing novel biomedicine.Keywords:TEMPO-oxidized cellulose;aerogel;resveratrol;drug carrier
研究领域:
生物材料学
·
药剂学
✓ 已验证
DOI
PubMed
高影响因子
Gels
·
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
研究领域:
药理学
·
生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
MOLECULES
·
2023
·Vol. 28
·期 8
·3395
·
IF 4.6
Yi Ou,Zonglin You,Min Yao,Yingfan Cao,Xiu Xue,Min Chen,Rihui Wu,Lishe Gan,Dongli Li,Panpan Wu,Xuetao Xu,Wingleung Wong,Vincent Kam Wai Wong,Wenfeng Liu,Jiming Ye,Jingwei Jin
Naproxen is widely used for anti-inflammatory treatment but it can lead to serious side effects. To improve the anti-inflammatory activity and safety, a novel naproxen derivative containing cinnamic acid (NDC) was synthesized and used in combination with resveratrol. The results showed that the combination of NDC and resveratrol at different ratios have a synergistic anti-inflammatory efficacy in RAW264.7 macrophage cells. It was indicated that the combination of NDC and resveratrol at a ratio of 2:1 significantly inhibited the expression of carbon monoxide (NO), tumor necrosis factor α (TNF-α), interleukin 6 (IL-6), induced nitric oxide synthase (iNOS), cyclooxygenase 2 (COX-2) and reactive oxygen species (ROS) without detectable side effects on cell viability. Further studies revealed that these anti-inflammatory effects were mediated by the activation of nuclear factor kappa-B (NF-κB), mitogen-activated protein kinase (MAPK) and phosphoinositide-3 kinase (PI3K)/protein kinase B (Akt) signaling pathways, respectively. Taken together, these results highlighted the synergistic NDC and resveratrol anti-inflammatory activity that could be further explored as a strategy for the treatment of inflammatory disease with an improved safety profile.Keywords:naproxen derivative;resveratrol;synergistic;anti-inflammatory;mechanism
研究领域:
药理学
·
免疫学
·
细胞生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Food & Function
·
2021
·Vol. 13
·期 2
·846-856
·
IF 5.396
Weidong Wang,Zenggen Liu,Fan Kong,Lixia He,Linghao Fang,Qingyan Shu
Tree peonies are well-known horticultural and medicinal plants. The tree peony seeds, as emerging woody oil crops, recently have attracted great attention for their metabolites and bioactivities. In this study, the phytochemicals isolated from tree peony seed coats were systematically investigated. Seven polyphenolics were separated and prepared, mainly belonging to resveratrol derivatives. There was a great variation in the seed coat polyphenolic content among eight Paeonia species, and the contents of the resveratrol trimers and dimers were significantly higher in the seed coats of Paeonia ostii than other species. Based on the HPLC fingerprint characteristics and chemometric analysis, a clear discrimination among Paeonia plants was found, including the composition patterns and contents of the constituents. Moreover, the characteristic phytochemicals (vateriferol and trans-ε-viniferin) could significantly reduce the starch-mediated levels of postprandial blood glucose in diabetic/normal mice. In addition, in vitro enzyme tests showed that the two compounds could effectively and competitively inhibit α-glucosidase, with the IC50 values of 3.01 and 7.75 μM, respectively, indicating that vateriferol and trans-ε-viniferin could be therapeutic potential agents for hyperglycemia and diabetes mellitus.
研究领域:
药理学
·
植物科学
·
生物化学
·
药物化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INDUSTRIAL CROPS AND PRODUCTS
·
2023
·
IF 5.9
Xiao-Jia He,Jin-Xian Fu,Jiao Jiao,Qing-Yan Gai,Yu-Jie Fu,Xue Feng,Yuan Wang
Resveratrol (a high-value natural polyphenolic compound with numerous pharmacological activities) is predominantly present in the form of the glycoside polydatin in Polygonum cuspidatum roots. In this study, a novel endophytic fungus, Penicillium rubens , capable of producing both cellulase (0.71 ± 0.09 U/mL) and β-glucosidase (4.35 ± 0.38 U/mL) for cell wall hydrolysis and polydatin deglycosylation, was used to ferment P. cuspidatum roots to improve the yield of valuable resveratrol. Results showed that the semi-solid-state fermentation (SSSF) using the homogeneous cultures of P. rubens was the appropriate strategy to obtain a higher yield of resveratrol from P. cuspidatum roots. Under the optimal fermentation conditions (temperature 30 °C, inoculation dose 4.0 mL/g, and time 72 h), the yield of resveratrol (19.95 ± 0.83 mg/g DW) in P. cuspidatum roots fermented by P. rubens was 19.18-fold higher than that in the unfermented control (1.04 ± 0.47 mg/g DW). Moreover, the digestibility of P. cuspidatum roots by P. rubens in terms of dry matter weight and cellulose content was 40.04% and 21.91%, respectively. Scanning electron microscope observation indicated that P. rubens fermentation could effectively disrupt the cell walls of P. cuspidatum roots, thus contributing to the release of more polydatin for deglycosylation. In addition, the extracts of P. cuspidatum roots fermented by P. rubens exhibited higher antioxidant and antibacterial activities compared with those of the unfermented control. The economic analysis showed that the benefit of SSSF approach for resveratrol production was much greater than that of the unfermented control. Overall, this study proposed a cost-effective SSSF method using the novel P. rubens to obtain bioactive resveratrol from P. cuspidatum roots, which had promising potential in the pharmaceutical, nutraceutical , and cosmetic industries.
研究领域:
药理学
·
生物技术
·
发酵科学
·
植物科学
·
生物化学
✓ 已验证
产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
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.
研究领域:
食品科学
·
药物递送
·
材料科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF CANCER RESEARCH AND CLINICAL ONCOLOGY
·
2014
·Vol. 140
·期 12
·2065-2075
·
IF 3.009
Li Peichun,Yang Sen,Dou Mengmeng,Chen Youran,Zhang Jie,Zhao Xiaoyan
Purpose The aim of this study was to investigate whether resveratrol (Res) combined with artemisinin (ART) possess synergistic effect on different cancer cells. Materials and methods The viability of HepG2 and HeLa cells treated with ART and Res was detected by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Combination index (CI) analysis and isobologram were used to assess the synergistic effect of ART and Res in different ratios. Wound-healing assay was used to investigate the migration rate. AO staining and fluorescent microscopy measurements were performed to detect the cell apoptosis. Reactive oxygen species (ROS) was measured with 2′7′-dichlorofluorescein diacetate (DCFH-DA). Results MTT assay indicated that ART and Res inhibited the growth of HeLa and HepG2 cells in a dose-dependent manner. The combination of ART and Res exhibited the strongest anticancer effect at the ratio of 1:2 (ART to Res). The combination of the two drugs also markedly reduced the ability of cell migration. Apoptosis analysis showed that combination of ART and Res significantly increased the apoptosis and necrosis rather than use singly. Additionally, ROS levels were elevated by combining ART with Res. Conclusions Taken together, the present study suggested that ART and Res possessed the synergistic anti-tumor effect. ART in combination with Res could be an effective therapeutic strategy for cancer.
研究领域:
肿瘤学
·
药理学
·
细胞生物学
✓ 已验证
DOI
PubMed
高影响因子
JOURNAL OF DRUG TARGETING
·
2024
·
IF 4.3
Jiaxin Liu,Liuqi Zhou,Huijing Cong,Jing Hu,Jingling Tang
Background Vaginal inflammation is a prevalent gynecological condition. If left untreated, it can potentially spread to the urinary and reproductive systems.Methods In this study, we propose a resveratrol-loaded microemulsion-based thermosensitive hydrogel (Res-Me-Tsgel) and compare it with a chitosan hydrogel-based Res-Me-Cogel. We characterized the different characters of Res-Me-Tsgel. The safety of Res-Me-Tsgel was also evaluated in vitro and in vivo. Finally, we measured the retention of Res in the vagina after drug administration.Results The Res-Me-Tsgel we prepared is a transparent liquid solution at room temperature that rapidly forms a gel at 37oC. Compared to Res solution and Res-Me, both Res-Me-Cogel and Res-Me-Tsgel demonstrate superior sustained release properties. Both in vitro and in vivo studies confirm the excellent biosafety profile of Res-Me-Cogel and Res-Me-Tsgel. Vaginal administration of these formulations in rats results in prolonged retention of resveratrol within the vagina. Notably, due to its improved flow into vaginal folds after administration, the retention of Resveratrol was approximately three times higher for the Res-Me-Tsgel group compared to the Res-Me-Cogel group at 24 h post-administration. Overall, these findings highlight the potential application of Res-Me-Tsgel as an effective means for vaginal inflammation.Conclusions We developed a novel micromulsion based thermosensitive hydrogel for the delivery of Res. The sustained release of Res and favorable vaginal retention from Res-Me-Tsgel make them promise as a potential candidate for local intravaginal therapy.
研究领域:
药剂学
·
妇科学
·
生物材料学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
RUSSIAN JOURNAL OF GENERAL CHEMISTRY
·
2024
·Vol. 94
·期 7
·1710-1719
·
IF 0.9
Han D.,Wang J.,Yang H.,Ran T.,Lu H.,Wang L.,Yan Z.
Abstract In the present study, carbon dots (CDs) were synthesized by solvothermal method using 1,4-diethynylbenzene as carbon source. The CDs exhibited the spherical particles as observed from transmission electron microscopy (TEM) image with the average particle size of 2.25±0.51 nm. The fluorescence quantum yield of the final CDs was 13% under excitation at 460 nm. The fluorescence intensity of CDs is diminished at both acidic and basic conditions, while a good linear relationship was realized at pH = 2–7 with the coefficient of determination ( R 2 ) of 0.9984 and the minimum detection limit (LOD) of 0.6 with good reversibility and cyclicity for pH detection. trans -resveratrol (t-res) was found to enhance the fluorescence of CDs well and the fluorescence intensity showed a good linear relationship to t-res within the concentration range of 10–100 μM with the coefficient of determination R 2 of 0.9993 and the LOD of 3 μM. The recoveries of the wines ranged from 100.36–102.40% with the relative standard deviations (RSD) of 2.56–3.48%. Thus, the CDs are extremely sensitive to t-res. Alkynyl ligand is used to prepare CDs, which illustrate the potential application for pH and t-res detection.
研究领域:
化学
·
分析化学
✓ 已验证
产品关联
DOI
高影响因子
Carbohydrate Polymer Technologies and Applications
·
2025
·
IF 6.5
Hurong Ge,Peipei Ma,Qing Huang,Shijie Wei,Zhizhong Wang
Objectives: To study the encapsulation of resveratrol by three cyclodextrin derivatives, investigate the impact of encapsulation technology on its anti-fatigue effect, and explore the anti-fatigue mechanism of the encapsulated resveratrol via transcriptomics analysis of exosomal miRNAs. Methods (1) UV spectroscopy and nuclear magnetic resonance (NMR) were used to investigate the encapsulation and encapsulation modes of resveratrol by β -CD, HP- β -CD and CM- β -CD; and the phase solubility method was used to calculate the solubilisation multiplicity of resveratrol by the three cyclodextrin derivatives. (2) Male C57BL/6 J mice were randomly divided into: fatigue model group (FM), FM+resveratrol group (SF+Res), FM+ β -CD, FM+HP- β -CD, FM+CM- β -CD, FM+ β -CD+Res, FM+HP- β -CD+Res, FM+CM- β -CD +Res, and after 30 days of rearing, the mice were subjected to exhaustion swimming experiment to detect fatigue-related indexes and observe the effects of the three cyclodextrin derivatives on the anti-fatigue effects of resveratrol. (3) Male C57BL/6 J mice were randomly divided into Control, FM, and FM+HP- β -CD+Res. After 30 days of rearing, except for the Control group, the remaining mice were subjected to exhaustion swimming experiments, and exosomes were extracted from cardiac tissue, skeletal muscle tissue, and liver tissue of the three groups of mice, and the transcriptomics technology was applied to sequence the exosomal miRNAs and to explore the mechanism of the effect of the HP- β -CD+Res envelope on fatigue. Results (1) The inclusion ratios of β -CD, HP- β -CD, and CM- β -CD encapsulated resveratrol were 1:1, 1:2, and 1:1, and the solubilisation multiplicities of resveratrol were 23, 39, and 21 fold, respectively; β -CD and CM- β -CD encapsulated Res, which was the benzene ring with two hydroxyl‑terminal ends of Res entered the cavity from the small-ported end of the cyclodextrins; HP- β -CD encapsulated Res, which was the Res containing one hydroxyl‑terminated benzene ring enters the cavity from the wide-mouth end of HP-β-CD. (2) Compared with the FM+Res group, all three inclusions were able to prolong the exhaustion swimming time of mice, with HP- β -CD+Res being the most effective. (3) After HP- β -CD+Res acted on the fatigued mouse model, cardiac tissue showed 1726 differentially expressed exosomal miRNAs, of which 840 were up-regulated and 886 were down-regulated, reversing the fatigue-induced changes in 64.96 % of the exosomal miRNAs (1170 shared differential exosomal miRNAs); Skeletal muscle tissue showed 1948 differentially expressed exosomal miRNAs, of which 718 were up-regulated and 1230 were down-regulated, reversing 80.57 % of the fatigue-induced changes in exosomal miRNAs (1576 shared differential exosomal miRNAs); Liver tissue showed 1442 differentially expressed exosomal miRNAs, of which 451 were up-regulated and 991 were down-regulated, reversing 84.31 % of fatigue-induced changes in exosomal miRNAs (1214 shared differential exosomal miRNAs). Target gene enrichment analysis of differentially expressed exosomal miRNAs in cardiac tissue, skeletal muscle tissue, and liver tissue had similar results, and the biological processes involved in HP- β -CD+Res were related to biological_process, signal transduction, G protein-coupled receptor signaling pathway, etc., and cellular components such as membrane, cytoplasm, integral component of membrane, etc., and molecular functions are closely related to protein binding, metal ion binding, molecular_function, etc.; mainly enriched in Axon guidance, MicroRNAs in cancer, Apoptosis and other signalling pathways. Conclusions (1) All three cyclodextrin derivatives encapsulated increased the solubility of resveratrol, with HP- β -CD having the best effect. (2) All three cyclodextrin derivative encapsulation techniques improved the anti-fatigue effect of resveratrol, with HP- β -CD being the most effective. (3) HP- β -CD+Res was able to induce differential expression of exosomal miRNAs in cardiac tissue, skeletal muscle tissue and liver tissue of fatigued mice.
研究领域:
药理学
·
分子生物学
·
生物信息学
✓ 已验证
产品关联
DOI
高影响因子
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.
研究领域:
药物化学
·
药理学
·
生物化学
✓ 已验证
产品关联
DOI
高影响因子
Nutrients
·
2022
·Vol. 14
·期 22
·4752
·
IF 6.706
Songxia Zhang,Ying Xu,Mengling Ye,Wenli Ye,Jian Xiao,Honghao Zhou,Wei Zhang,Yan Shu,Yun Huang,Yao Chen
People in Eastern countries hold a tradition of soaking herbal medicine in wine; however, the efficacy and safety of herbal wine have not been rigorously assessed. By assessing the efficacy of resveratrol (RSV) in ethanol against alcoholic liver disease (ALD) in mice, we aimed to offer a perspective on the use of herbal wine. To simulate the behaviour of herbal wine users, RSV (15 mg/kg) soaked in ethanol (RSV-alcohol) was administrated via gavage to the mice, here with alcohol consumption-induced ALD. RSV soaked in water (RSV-water) was the treatment control. The efficacy and safety of RSV on ALD were evaluated. Compared with the RSV-water group, a higher rate of mortality was found in the RSV-alcohol group (50.0% vs. 20.0%), which also exhibited more severe liver injury. RSV significantly increased the exposure of alcohol by 126.0%, which was accompanied by a significant inhibition of the ethanol metabolic pathway. In contrast, alcohol consumption significantly reduced exposure to RSV by 95.0%. Alcohol consumption had little effect on the expression of drug-metabolizing enzymes in RSV; however, alcohol seemed to reduce the absorption of RSV. RSV in liquor exacerbates alcoholic liver injury and has a reduced therapeutic effect, suggesting that the habit of herbal wine use without supervision is risky.Keywords:herbal wine use;resveratrol;ethanol;concomitant administration;liver injury
研究领域:
药理学
·
肝病学
·
毒理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）