npj Biofilms and Microbiomes
·
2025
·Vol. 11
·期 1
·1-14
·
IF 9.2
Zhang Song-xia,Hu Fang-fang,Chen Huan,Guo Jing,Xiang Zhong-wen,Ding Xin,Ye Meng-ling,Ye Wen-li,Chen Jun-hong,Wang Xin,Han Wen-jing,Zhou Hong-hao,Zhang Wei,Huang Yun,Wu Lie-lin,Lian Guang-hui,Chen Yao
Drug tolerance is clinically common but its mechanism is unclear. Previous studies found RSV tolerance in ALD treatment. This study explores mechanisms involving gut bacteria and host factors. Male C57BL/6J mice were induced into ALD with the Lieber-DeCarli alcohol diet, then ALD-RSV group mice were gavaged RSV (150 mg/kg/day) for 5 weeks. Throughout the experiment, ALD and ALD-RSV mice were on the Lieber-DeCarli alcohol diet, while the Vehicle group received a control diet. By week 5, tolerance to RSV efficacy emerged, with markedly reduced RSV exposure at the final dose. ALD-RSV group exhibited increased levels of Eggerthella lenta ( E.lent ), which metabolizes RSV into dihydroresveratrol (DHR). Chronic RSV treatment upregulated UGT1A1, the enzyme converting RSV into its primary metabolite, trans-resveratrol-3-O-β-D-glucuronide (R3G). The synergy between gut bacteria and host factors enhances RSV metabolism in ALD mice, driving tolerance and offering insights into other clinical drugs tolerance mechanisms.
研究领域:
微生物学
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药理学
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代谢生物学
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胃肠病学
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肝病学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
AUSTRALIAN JOURNAL OF GRAPE AND WINE RESEARCH
·
2019
·Vol. 25
·期 3
·307-315
·
IF 2.343
Y. Yang,X. Wang,F. Tan,M. Fu,F. Sun
Background and Aims Burdock fructooligosaccharides (BFO) is an elicitor that induces biotic resistance and delays colour development in grapes postharvest. The mechanism of the delayed colour development requires further study. Methods and Results Colour development index; anthocyanin, tannin, flavonol, flavanol, trans -resveratrol and lignin; the trans -resveratrol, lignin and anthocyanin biosynthesis-related transcription factors; and functional gene expression were investigated. In response to BFO induction, upregulation of the v-myb avian myeloblastosis viral oncogene homologue 14 ( MYB14 )-mediated stilbene synthase ( STS ) altered the phenylpropanoid fluxes from anthocyanin to trans -resveratrol; MYBA1 and MYBA2- mediated the downregulation of dihydroflavonol 4-reductase ( DFR ), and flavonoid-3-O-glycosyltransferase ( UFGT ) limited anthocyanin biosynthesis. Downregulation of MYB4- mediated chalcone synthase ( CHS ) and upregulation of cinnamoyl CoA reductase ( CCR ) and cinnamyl alcohol dehydrogenase ( CAD ) altered the phenylpropanoid fluxes from anthocyanin to lignin. Conclusions Burdock fructooligosaccharides inhibits postharvest colour development in grapes by altering the phenylpropanoid fluxes from anthocyanin to resistance-related phenolic substances. Significance of the Study Understanding the mechanism of the effect of BFO on grape colour development may improve our understanding of colour development in grape berries.
研究领域:
植物学
·
分子生物学
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DOI
高影响因子
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
研究领域:
分子生物学
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细胞生物学
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药理学
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产品关联
DOI
PubMed
高影响因子
SOUTH AFRICAN JOURNAL OF BOTANY
·
2023
·
IF 3.1
Wanying Hu,Mengdan Jiang,Zongsuo Liang,Pengguo Xia
Tetrastigma hemsleyanum Diels et Gilg, a plant of the Vitaceae family, is often used as a medicine. Modern pharmacological studies have found that its root tubers have a particular anticancer effect. Polydatin, piceatannol, resveratrol, and kaempferol could be detected stably in this herbal plant, which are vital indicators for controlling and evaluating its quality. At present, its planting mode is chaotic and complicated. In order to explore the optimal cultivation mode with excellent quality and yield, the agronomic indicators, the indicators of conventional medical materials and the content of active ingredients were determined in this study. Then, their discrepancy under different planting bases and various planting modes was analyzed. The T. hemsleyanum cultivated in the greenhouse had the thickest stems and the longest leaves, as well as the largest aerial and underground biomass. Compared with understory planting, the root tubers have higher total flavonoid content in the greenhouse planting mode. In addition, the index component content of the stereoscopic planting was higher than that of the crawl planting. In summary, greenhouse planting combined with stereoscopic planting mode was conducive to improving the yield and quality of T. hemsleyanum simultaneously. These results provided a more comprehensive reference basis for the artificial planting of T. hemsleyanum . Simultaneously, it provided a theoretical basis for strengthening the sustainable development and utilization of medicinal materials from T. hemsleyanum and protection of resources.
研究领域:
药理学
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农业
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植物科学
✓ 已验证
产品关联
DOI
高影响因子
Arabian Journal of Chemistry
·
2024
·
IF 5.3
Xiaohai Chen,Fengsheng Hong,Hualu Wu,Yuxin Shen,Hailun Xia,Ren-ai Xu,Lu Shi
The primary objective of this study was to investigate the effects of baicalein and fangchinoline on the metabolism of abemaciclib. We hypothesized that these two natural compounds could significantly affect the metabolism of abemaciclib by inhibiting the activity of the CYP3A4 enzyme, thus potentially increasing its concentration in the body. In vitro , rat liver microsomes (RLM) and human liver microsomes (HLM) were employed to explore the inhibitory effects and mechanisms of baicalein and fangchinoline on abemaciclib. In vivo , twelve healthy male Sprague-Dawley (SD) rats were randomly assigned to three groups: Group A (control group), Group B (baicalein), and Group C (fangchinoline). The concentrations of abemaciclib and its metabolite N-desethylabemaciclib (M2) were evaluated using ultra performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS). Finally, molecular docking method was employed to understand the interaction between abemaciclib and baicalein. It was indicated by the in vitro findings that both baicalein and fangchinoline inhibited abemaciclib metabolism in RLM through a mixed mechanism of competitive and non-competitive inhibition pathway. In HLM, baicalein inhibited abemaciclib metabolism by employing a hybrid mechanism of uncompetitive and non-competitive inhibition, while fangchinoline exhibited its inhibition in a competitive manner. In vivo , pharmacokinetic experiments revealed significant increases for AUC (0-t) and AUC (0-∞) of abemaciclib in Group B and Group C when compared to Group A, while the plasma clearance (CLz/F) of abemaciclib exhibited significant reductions. Moreover, molecular docking studies showed that both abemaciclib and baicalein docked to the active pocket of CYP3A4. This study demonstrated that the co-administration of baicalein or fangchinoline significantly affected the metabolism of abemaciclib, providing valuable insights for its clinical application.
研究领域:
药理学
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分子生物学
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临床医学
✓ 已验证
产品关联
DOI
高影响因子
Advances in Experimental Medicine and Biology
·
2016
·
IF 1.953
Jin Ju,Li Yan,Zhang Xiuli,Chen Tongsheng,Wang Yifei,Wang Zhiping
Cellular damage such as oxidation and lipid peroxidation, and DNA damage induced by free-radicals like reactive oxygen species, has been implicated in several diseases. Radicals generated by 2,2-azobis (2-amidino-propane) dihydrochloride (AAPH) are similar to physiologically active ones. In this study we found that polydatin, a resveratrol natural precursor derived from many sources, has the capacity of free radical scavenging and antioxidative damage. Using free radical scavenging assays, the IC 50 values of polydatin were 19.25 and 5.29 μg/ml with the DPPH and the ABTS assay, respectively, and 0.125 mg ferrous sulfate/1 mg polydatin with the FRAP assay. With the AAPH-induced oxidative injury cell model assay, polydatin showed a strong protective effect against the human liver tumor HepG2 cell oxidative stress damage. These results indicate that the antioxidant properties of polydatin have great potential for use as an alternative to more toxic synthetic antioxidants as an additive in food, cosmetics and pharmaceutical preparations for the treatment of oxidative diseases. Keywords Free radical scavenging Polydatin Antioxidation AAPH
研究领域:
药理学
·
生物化学
✓ 已验证
DOI
PubMed
高影响因子
Toxics
·
2024
·Vol. 12
·期 11
·810
·
IF 3.9
Xiangsheng Tian,Yiquan Ou,Shengyuan Shi,Qiuhua Zhou,Sihong Long,Yao Xiang,Weichao Zhao,Dingxin Long
This study explores the neuroprotective effects of resveratrol (Resv) against tri-o-cresyl phosphate (TOCP)-induced neurotoxicity in the spinal cord of adult hens. It is well documented that TOCP exposure causes significant neurodegeneration via mechanisms that involve endoplasmic reticulum (ER) stress and impaired autophagy. In this experiment, adult hens were assigned to one of four groups: Control, Resv, TOCP, and TOCP + Resv. The spinal cord tissues were examined through transmission electron microscopy, hematoxylin and eosin (HE) staining, Nissl staining, and Western blotting to evaluate key proteins associated with ER stress and autophagy. Additionally, RT-qPCR and immunofluorescence were employed to measure sirtuin1 (SIRT1) expression. The findings revealed that TOCP induced severe ultrastructural damage, including disrupted myelin sheaths, dilated ER, and extensive neurodegeneration, as confirmed by histological evaluations. The expression levels of GRP78, p-PERK, p-eIF2α, ATF4, CHOP, Beclin-1, P62, and LC3-II were also significantly elevated by TOCP. However, Resv treatment markedly attenuated these pathological changes by reducing ER stress, restoring autophagic flux, and upregulating SIRT1 expression, preserving spinal cord integrity. These results indicate that Resv can effectively counteract TOCP-induced neurotoxicity by modulating ER stress and autophagy, underscoring its potential as a therapeutic agent for neuroprotection.
研究领域:
神经科学
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毒理学
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药理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
BIOLOGICAL & PHARMACEUTICAL BULLETIN
·
2015
·Vol. 38
·期 10
·1658-1662
·
IF 1.828
Lu-yang Lu,Yuan Liu,Zhi-feng Zhang,Xiao-jun Gou,Jun-hao Jiang,Ji-zhong Zhang,Qian Yao
Pomegranate seed oil (PSO) has diverse bioactivities. It was hyphothesized that if PSO were employed to construct a trans-resveratrol-loaded self-nanoemulsifying drug delivery system (RES SNEDDS-PSO), not only could PSO serve as an oil phase but also exert synergistic effects with resveratrol to yield better therapeutic outcomes. In this study, we prepared RES SNEDDS-PSO for the first time to validate that hypothesis. The anti-inflammatory and anticancer activities of RES SNEDDS-PSO were compared with another SNEDDS composed of oil phase isopropyl palmitate (RES SNEDDS-IP). The results showed that upon exposure to a 10-fold amount of water, RES SNEDDS-PSO was converted into nanoemulsions with a mean size of 44 nm. Nanoemulsions enhanced the water solubility of resveratrol by 20-fold, significantly improved resveratrol stability in intestinal fluid, and slowed the decomposition of resveratrol in water by 1-fold. An in vivo anti-infection test showed that the degree of inflammatory swelling in mice given RES SNEDDS-PSO was only 60 and 76% that of the group fed with RES SNEDDS-IP at doses of 10 and 20 mg/kg, respectively. An in vitro anticancer study showed that the inhibitory rate of RES SNEDDS-PSO against MCF-7 breast cancer cells was 2.03- and 1.24-fold that of RES SNEDDS-IP at a concentration of 12.5 and 25 µg/mL, respectively. This study demonstrated that the newly developed SNEDDS may be a prospective formulation in the functional food and clinical fields.
研究领域:
药剂学
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生物医学
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食品科学
✓ 已验证
DOI
PubMed
高影响因子
PHYTOTHERAPY RESEARCH
·
2024
·Vol. 38
·期 6
·3218-3239
·
IF 6.1
MinFeng Zhou,HuiFang Niu,DanDan Cui,GuoQuan Huang,JinXiao Li,HaoRan Tian,XiaoJuan Xu,FengXia Liang,Rui Chen
Colorectal cancer (CRC) is a significant health problem with elevated mortality rates, prompting intense exploration of its complex molecular mechanisms and innovative therapeutic avenues. Resveratrol (RSV), recognised for its anticancer effects through SIRT1 activation, is a promising candidate for CRC treatment. This study focuses on elucidating RSV's role in CRC progression, particularly its effect on autophagy-related apoptosis. Using bioinformatics, protein imprinting and immunohistochemistry, we established a direct correlation between FOXQ1 and adverse CRC prognosis. Comprehensive in vitro experiments confirmed RSV's ability to promote autophagy-related apoptosis in CRC cells. Plasmids for SIRT1 modulation were used to investigate underlying mechanisms. Molecular docking, glutathione-S-transferase pull-down experiments and immunoprecipitation highlighted RSV's direct activation of SIRT1, resulting in the inhibition of FOXQ1 expression. Downstream interventions identified ATG16L as a crucial autophagic target. In vivo and in vitro studies validated RSV's potential for CRC therapy through the SIRT1/FOXQ1/ATG16L pathway. This study establishes RSV's capacity to enhance autophagy-related cell apoptosis in CRC, positioning RSV as a prospective therapeutic agent for CRC within the SIRT1/FOXQ1/ATG16L pathway.
研究领域:
肿瘤学
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分子生物学
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药理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF PHARMACEUTICAL SCIENCES
·
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.
研究领域:
药学
·
材料科学
✓ 已验证
DOI
PubMed
高影响因子
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
危险品化学品经营许可证（带存储）