PeerJ
·
2019
·
IF 2.353
Hongli Yin,Ji Ma,Jichun Han,Maoru Li,Jing Shang
Background Quercetin (Qr), isoquercitrin (IQ), and quercetin-3-O-β-D-glucuronide (QG) are powerful phytochemicals that have been shown to exhibit disease prevention and health promotion properties. However, there may exist transformations between Qr, IQ, and QG in vivo . And the pharmacokinetic profiles of Qr, IQ, and QG have not been systematically compared. The pharmacokinetics study would be helpful to better understand the pharmacological actions of them. Methods Herein, we developed a reliable HPLC-MS method to compare the pharmacokinetics of Qr, IQ, and QG after separate (50 mg/kg) oral administration of them in rats, using puerarin as internal standard. The detection was performed using negative selected ion monitoring. This method was validated in terms of selectivity, linearity, precision, accuracy, extraction recovery, matrix effect, and stability; and shows reliabilities in monitoring the pharmacokinetic behaviors of these three compounds. Results Our results showed that after separate oral administration of Qr, IQ, and QG, all of the compounds could be detected in plasma. In addition, QG could be detected in the Qr group; Qr and QG could be measured in the IQ group; and Qr could be found in rat plasma after 1.5 h of QG administration. Moreover, the AUC 0− t of Qr in the; Qr group (2,590.5 ± 987.9 mg/L*min), IQ group (2,212.7 ± 914.1 mg/L*min), and QG group (3,505.7 ± 1,565.0 mg/L*min) was larger than the AUC 0− t of QG in the; Qr group (1,550.0 ± 454.2 mg/L*min), IQ group (669.3 ± 188.3 mg/L*min), and QG group (962.7 ± 602.3 mg/L*min). The AUC 0− t of IQ was the lowest among all groups. Discussion Quercetin, IQ, and QG can all be absorbed into plasma. A mutual transformation exists between Qr and QG, and IQ can be metabolized into Qr and QG in SD rats. These results would provide a meaningful basis for understanding the pharmacological actions of these three compounds.
研究领域:
药理学
·
分析化学
✓ 已验证
DOI
PubMed
高影响因子
JOURNAL OF FOOD COMPOSITION AND ANALYSIS
·
2024
·
IF 4
Xu Ling,Yifan Hu,Yiming Hu,Jingwen Meng
Research about mulberry leaf with different producing area and harvest period will promote its quality control method and utilization in terms of active ingredient extraction and health products research. This study focused on the establishment of fingerprint of mulberry leaves from different harvest periods and different origins, the determination of chlorogenic acid , rutin as well as astragalin with ultrasound assisted liquid extraction. The extraction rate was optimized using response surface method . The optimized conditions were as follows: methanol for extraction, ultrasonic power of 240 W, extraction time of 77 min, methanol concentration of 59 % (v/v) and solid-to-liquid ratio of 1:48 (g/mL). Three ingredients in mulberry leaves were successfully extracted, and the HPLC fingerprint of mulberry leaves was established with 23 common peaks. Good similarity higher than 85.7 % was obtained among the 14 batch of samples from different harvest periods and different origins. The optimized extraction process was stable, reliable and suitable for extracting chlorogenic acid and two flavonoids from mulberry leaf. The established fingerprint exhibited good stability and repeatability, and provided comprehensive chromatographic peaks information. This method can be relied upon for the identification and comprehensive quality control of mulberry leaf.
研究领域:
植物化学
·
药用植物研究
·
分析化学
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2025
·
IF 4.9
Fan Yang,Jie Wang,Jingjing Wang,Xinyue Yang,Hongyan Zhang
Quercetin (Qc) is a natural flavonoid recognized for its diverse biological activities but is poorly soluble in water. Hydroxypropyl beta-cyclodextrin (HP-β-CD), a cyclodextrin analog, serves as a safe and efficient drug carrier by forming clathrates with therapeutic agents, enhancing their physicochemical and pharmacokinetic properties. This study reports the synthesis of inclusion complexes of HP-β-CD and Qc using ultrasonic magnetic stirring followed by lyophilization. These complexes were analyzed using X-ray Diffraction (XRD), Scanning Electron Microscopy (SEM) and UV–Vis spectroscopy (UV), Fourier-Transform Infrared spectroscopy (FTIR), and Nuclear Magnetic Resonance (NMR) to elucidate their structural and physicochemical properties. The findings validated the successful formation of clathrates between Qc and HP-β-CD, with the resulting inclusion complexes comprising Qc/HP-β-CD demonstrating markedly distinct spectral characteristics compared to unmodified Qc. Moreover, studies revealed a substantial enhancement in the anti-inflammatory and osteogenic activities of Qc upon encapsulation. These findings demonstrate that the Qc/HP-β-CD inclusion complexes markedly enhanced Qc bioavailability while amplifying its therapeutic efficacy in inflammation and bone regeneration.
研究领域:
药理学
·
材料科学
·
骨生物学
✓ 已验证
产品关联
DOI
高影响因子
MOLECULES
·
2016
·Vol. 21
·期 9
·1246
·
IF 2.465
Xican Li,Qian Jiang,Tingting Wang,Jingjing Liu,Dongfeng Chen
The role of the 6″-OH (ω-OH) group in the antioxidant activity of flavonoid glycosides has been largely overlooked. Herein, we selected quercitrin (quercetin-3-O-rhamnoside) and isoquercitrin (quercetin-3-O-glucoside) as model compounds to investigate the role of the 6″-OH group in several antioxidant pathways, including Fe2+-binding, hydrogen-donating (H-donating), and electron-transfer (ET). The results revealed that quercitrin and isoquercitrin both exhibited dose-dependent antioxidant activities. However, isoquercitrin showed higher levels of activity than quercitrin in the Fe2+-binding, ET-based ferric ion reducing antioxidant power, and multi-pathways-based superoxide anion-scavenging assays. In contrast, quercitrin exhibited greater activity than isoquercitrin in an H-donating-based 1,1-diphenyl-2-picrylhydrazyl radical-scavenging assay. Finally, in a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl assay based on an oxidatively damaged mesenchymal stem cell (MSC) model, isoquercitrin performed more effectively as a cytoprotector than quercitrin. Based on these results, we concluded that (1) quercitrin and isoquercitrin can both indirectly (i.e., Fe2+-chelating or Fe2+-binding) and directly participate in the scavenging of reactive oxygen species (ROS) to protect MSCs against ROS-induced oxidative damage; (2) the 6″-OH group in isoquercitrin enhanced its ET and Fe2+-chelating abilities and lowered its H-donating abilities via steric hindrance or H-bonding compared with quercitrin; and (3) isoquercitrin exhibited higher ROS scavenging activity than quercitrin, allowing it to improve protect MSCs against ROS-induced oxidative damage.Keywords:quercitrin;isoquercitrin;Q3G;6″-OH;ω-OH;flavonoid glycoside;antioxidant mechanisms;mesenchymal stem cells
研究领域:
药理学
·
生物化学
·
细胞生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF MOLECULAR AND CELLULAR CARDIOLOGY
·
2025
·
IF 4.7
Long Li,Quanyou Chai,Chunling Guo,Junyi Wei,Yuqiao Qin,Huimin Liu,Zhaoyang Lu
Aim Vascular calcification (VC) is a major adverse cardiovascular event in chronic kidney disease (CKD) patients. N6-methyladenosine (m6A) modification is vital for many biological processes, but its function and possible molecular mechanisms in VC are poorly understood. This study aimed to clarify the function and molecular mechanisms of N6-adenosine-methyltransferase-like 3 (METTL3) in VC. Methods and results The results of the bioinformatic analysis showed that METTL3 expression was significantly upregulated in calcified VSMCs. This finding was corroborated by phosphate-induced VSMCs calcification models and 5/6 nephrectomy-induced CKD mouse VC models. Afterward, Alizarin Red S staining and m6A dot blot analysis demonstrated METTL3 overexpression elevated m6A levels and encouraged calcification in VSMCs and mouse aortic rings, while METTL3 knockdown decreased m6A levels and inhibited calcium deposition in these experimental models. Furthermore, METTL3 promoted VC via the PTEN/AKT pathway, and MeRIP verified that METTL3 induced PTEN mRNA degradation by modifying it with m6A. In addition, molecular docking simulations and DARTS assays revealed that quercetin is a natural small-molecule inhibitor of METTL3. The current investigation demonstrated that quercetin mitigated VC by reducing METTL3-dependent m6A levels in vivo and in vitro. Conclusion In conclusion, this study unraveled the pathogenic mechanism of METTL3-mediated m6A modification in VC and provided new insights to establish METTL3 as a therapeutic target for VC.
研究领域:
分子生物学
·
心血管疾病
·
表观遗传学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Journal of Environmental Chemical Engineering
·
2024
·
IF 7.4
Fan Feng,Siqing Liu,Shuming Wen,Guang Han,Qicheng Feng
In flotation, the separation and concentration of copper-iron sulfide ores are usually carried out at high alkalinity to depress pyrite, and plenty of lime could block the flotation pipeline and affect the recovery of precious metals during practical operation. Herein, the current research hotspot to achieve the separation of copper-iron sulfide ores under low alkalinity. This paper presented an eco-friendly reagent, quercetin, for the flotation separation of chalcopyrite and pyrite, and investigated the effect on the flotation performance of the two minerals. The interaction mechanism of quercetin with mineral was demonstrated using zeta potential measurements, atomic force microscopy (AFM), surface adsorption measurements, Fourier-transform infrared spectroscopy (FT-IR), and X-ray Photoelectron Spectroscopy (XPS). The flotation results showed that the depressive effect of quercetin on pyrite was more pronounced in comparison to its impact on chalcopyrite at pH 8.0, and the chalcopyrite recovery reached 90 %, whereas that of pyrite was under 10 %. The surface analysis revealed quercetin chemisorption on the mineral surface through interaction with metal sites. In the presence of quercetin, the quercetin significantly diminished the ability of pyrite to adsorb xanthan but had minor effects on the adsorption of chalcopyrite.
研究领域:
矿物加工工程
·
表面化学
·
环境科学
✓ 已验证
产品关联
DOI
高影响因子
MICROCHIMICA ACTA
·
2024
·Vol. 191
·期 10
·1-13
·
IF 5.3
Zhong Yu,Liao Ran,He Guowen,Liu Saiwen,Zhang Jin,Chen Chao
Cubic hollow-structured NiCo-LDH was synthesized using a solvothermal method. Subsequently, clay-like Ti 3 C 2 T x MXenes were electrostatically self-assembled with NiCo layered double hydroxides (NiCo-LDH) to form composites featuring three-dimensional porous heterostructures. The composites were characterized using SEM, TEM, XRD, XPS, and FT-IR spectroscopy. Ti 3 C 2 T x MXenes exhibit excellent electrical conductivity and hydrophilicity, providing abundant binding sites for NiCo-LDH, thereby promoting an increase in ion diffusion channels. The formation of three-dimensional porous heterostructural composites enhances charge transport, significantly improving sensor sensitivity and response speed. Consequently, the sensor demonstrates excellent electrochemical detection capability for quercetin (Qu), with a detection range of 0.1–20 µM and a detection limit of 23 nM. Additionally, it has been applied to the detection of Qu in natural plants such as onion, golden cypress, and chrysanthemum. The recovery ranged from 97.6 to 102.28%. Graphical Abstract
研究领域:
材料科学
·
分析化学
·
植物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
HOLZFORSCHUNG
·
2022
·
IF 2.493
Li Yan,Xiaodi Ji,Feiyang Zeng,Zhangjing Chen,Yafang Lei
As a renewable biomass material, wood is often deteriorated by decay fungi. Quercetin was here grafted onto poplar ( Populus nigra ) using oxalic acid as a linker through vacuum-pressure treatment and esterification with various molar ratios of quercetin to oxalic acid (Q/O) to enhance the wood decay resistance. Decay resistance, flexural strength, graft mechanism, and microscopic structure of the quercetin-grafted wood were analyzed. Results indicated that the decay resistance of quercetin-grafted wood to white-rot fungi ( Trametes versicolor ) and brown-rot fungi ( Gloephyllum trabeum ) was significantly improved. The modulus of rupture (MOR) of the quercetin-grafted wood was reduced while the modulus of elasticity (MOE) was improved. Quercetin was grafted onto wood through formation of ester groups among oxalic acid, wood, and quercetin. The highest amount of ester groups in the grafted wood was achieved when Q/O was 1:2 and Q/O lower than 1:2 would severely degrade the wood. The thickness of cell walls of the quercetin-grafted wood increased and reached a maximum of 2.2 μm with Q/O of 1:2. Quercetin can be grafted on wood cell wall by oxalic acid as an environment-friendly preservative to enhance the decay resistance of wood.
研究领域:
林学
·
材料科学
✓ 已验证
DOI
高影响因子
Journal of Toxicologic Pathology
·
2016
·
IF 0.848
Yuan Yuan,Shixun Ma,Yongmei Qi,Xue Wei,Hui Cai,Li Dong,Yufeng Lu,Yupeng Zhang,Qingjin Guo
The objective of the current study was to explore the inhibitory effects of quercetin on cadmium-induced autophagy in mouse kidneys. Mice were intraperitoneally injected with cadmium and quercetin once daily for 3 days. The LC3-II/β-actin ratio was used as the autophagy marker, and autophagy was observed by transmission electron microscopy. Oxidative stress was investigated in terms of reactive oxygen species, total antioxidant capacity, and malondialdehyde. Cadmium significantly induced typical autophagosome formation, increased the LC3-II/β-actin ratio, reactive oxygen species level, and malondialdehyde content, and decreased total antioxidant capacity. Interestingly, quercetin markedly decreased the cadmium-induced LC3-II/β-actin ratio, reactive oxygen species levels, and malondialdehyde content, and simultaneously increased total antioxidant capacity. Cadmium can inhibit total antioxidant capacity, produce a large amount of reactive oxygen species, lead to oxidative stress, and promote lipid peroxidation, eventually inducing autophagy in mouse kidneys. Quercetin could inhibit cadmium-induced autophagy via inhibition of oxidative stress. This study may provide a theoretical basis for the treatment of cadmium injury.
研究领域:
毒理学
·
药理学
·
分子生物学
✓ 已验证
DOI
PubMed
高影响因子
CLAYS AND CLAY MINERALS
·
2024
·Vol. 69
·期 1
·94-104
·
IF 2
Shu-Ting Liu,Xue-Gang Chen,Shi-Long Zhang,Xue-Min Liu,Jun-Ji Zhang
Halloysite nanotubes (HNTs) have attracted much attention as delivery carriers for various drugs, but the loading of one such drug, quercetin, on HNTs has been investigated only rarely and usually involved cyclic vacuum pumping. The main objective of the present study was to develop a novel carrier system based on HNTs for quercetin delivery without a vacuum process and to investigate the effect of chemical modification of HNTs on the loading and release of quercetin. For this purpose, comparative studies of five chemical modification reagents (sodium lauroamphoacetate, cocoamidopropyl betaine, 1-hydroxyethyl 2-nonyl imidazoline betaine, triethanolamine, and dipicolinic acid) functionalized on HNTs were investigated for quercetin loading and in vitro release. Characterization of raw halloysite, modified halloysite, and quercetin-loaded halloysite were done by X-ray diffraction (XRD), Fourier-transform infrared spectrometry (FTIR), thermogravimetric analysis (TGA), and transmission electron microscopy (TEM). The results indicated that chemical modification could improve the interactions between HNTs and quercetin. After chemical modification, quercetin was anchored to both the inner and outer surfaces of HNTs by electrostatic attraction, hydrogen bonding, and van der Waals forces. Sodium lauroamphoacetate-modified HNTs were given the highest loading of 1.96 wt.% among the five reagents. Cocamidopropyl betaine-modified HNTs exhibited the best sustained-release profile with only 29.07% for initial burst release and 480 h of consecutive release. Carboxyl groups of the modification reagent improved the loading capacity of quercetin. Amide groups prolonged drug release due to the strong affinity between amine and phenolic hydroxyl groups of quercetin. The release of quercetin from the cocamidopropyl betaine-modified HNTs fitted a first-order kinetics model well. The present study suggested that cocamidopropyl betaine-modified HNTs offer promise as vehicles for delivery of quercetin and for extending the application of quercetin.
研究领域:
药剂学
·
材料科学
✓ 已验证
产品关联
DOI
高影响因子
Journal of Food Measurement and Characterization
·
2024
·
IF 2.9
Zhang Tong,Wang Hongyue,Pan Xiaoya,Zhang Xindi,Shi Caihong,Zhang Xiangrong
In this study, quercetin in cellulose porous microspheres were prepared by quasi-emulsion solution diffusion method. The formulation of microspheres was optimized by Box-Behnken Design and their antioxidant activity was evaluated. Morphological structures and physicochemical properties of the microspheres were investigated. The findings of porous microspheres particle size ranged from 150 to 200 μm. The encapsulation efficiency and loading capacity were of 90.32% and 20.54%. Respectively, prepared using polyvinyl alcohol (0.16%), ethyl cellulose and quercetin (41:19, w/w), stirred in dichloromethane/ethanol solution (4:1, v/v). The scanning electron microscopy confirmed porous structure of the microsphere surface. Fourier transform infrared spectroscopy revealed structural changes between quercetin and ethyl cellulose. X-ray diffraction and thermal analysis showed that the encapsulated quercetin was amorphous. Compared with free quercetin, the antioxidant capacity and stability of quercetin in porous microspheres were significantly improved. This research reveals the development of porous microsphere carrier that facilitated improved antioxidant activity and stability of quercetin.
研究领域:
食品科学
·
材料科学
·
药学
✓ 已验证
产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2025
·
IF 8.5
Chunpeng Yang,Huiling Ma,Ze Liang,Ying Zhuang,Litao Hu,Kexin Zhang,Leixiao Huang,Min Li,Shubiao Zhang,Yuhong Zhen
Quercetin is a natural flavonoid found in many plants which has various pharmacological activities including antitumor effect. However, the poor water solubility and bioavailability limit the potential benefits of quercetin for patients. Thus, modifying quercetin structure and developing actively targeted drug delivery systems are extremely important for tumor precision therapy. Herein, polymer-drug conjugates dextran-quercetin (D-Q) and cRGD-dextran (R-D) were synthesized by grafting quercetin and polypeptide cRGDfk (Arg-Gly-Asp-(D-Phe)-Lys) to dextran. Then cRGD-modified dextran-quercetin polymer micelles (R-D-Q) were constructed by self-assembling of D-Q and R-D. R-D-Q micelles possessed appropriate particle size (133.4 nm), nearly neutral potential (8.14 mV) and excellent drug-loading efficiency (13.1 %) and achieved higher cytotoxicity, apoptosis induction and penetration to human breast cancer MCF-7 cells than the micelles unmodified with cRGD, which were ascribed to cRGD-integrin mediated transcytosis. R-D-Q micelles effectively suppressed tumor growth in tumor-bearing mice by delivering more quercetin throughout the tumor tissue. And R-D-Q micelles could promote the apoptosis of tumor cells by activating p38 and JNK signal pathways and suppressing ERK signal pathway. In addition, R-D-Q micelles had no damage to normal tissues of mice at therapeutic dose. These results indicate promising prospects for R-D-Q micelles as an effective drug delivery system against tumor.
研究领域:
药学
·
肿瘤学
·
生物材料学
✓ 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）