JOURNAL OF LIPOSOME RESEARCH
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2025
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IF 4.3
Qinyang Hua,Qilong Wang,Xue Wang,Xia Jiang,Mingjie Gong,Jiaying Li,Tingyuan Li,Xiaowen Wang,Xia Cao,Jiangnan Yu,Elmurat Toreniyazov,Bin Zong,Ximing Xu,Feng Shi,Michael Adu-Frimpong
The clinical application of Isoquercitrin (IQ) is limited by its low water solubility and short retention time in the body, despite its diverse pharmacological effects. To address these issues, we prepared polyethylene glycol (PEG)-modified IQ liposomes (IQ-L) using the thin film dispersion method and optimized the formulation through a combination of One Factor at a Time (OFAT) method and response surface experiments. Characterization of the IQ-L that was prepared using the optimal formulation revealed a particle size of 185.48 nm, a polydispersity index of 0.252, a zeta potential of −33.88 mV, and an impressive encapsulation efficiency of 97.84%. In vitro release studies showed a significantly higher cumulative release rate for IQ-L compared to free IQ. Pharmacokinetic evaluations in rats demonstrated a 4.54-fold increase in the area under the concentration-time curve, a 1.63-fold prolongation of the half-life, and a 2.07-fold increase in peak concentration for IQ-L compared to unmodified IQ. Moreover, assessments of renal function in a mouse model indicated promising therapeutic effects. In summary, the PEG-modified liposome system greatly improved the solubility and in vivo retention time of IQ, thus making it a potential clinical agent for the treatment of chronic kidney disease (CKD).
研究领域:
药剂学
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肾脏病学
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生物医学工程
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PubMed
高影响因子
BIOMEDICAL CHROMATOGRAPHY
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2012
·Vol. 27
·期 4
·509-514
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IF 1.966
Linling Lu,Dawei Qian,Jing Yang,Shu Jiang,Jianming Guo,Er-xin Shang,Jin-ao Duan
In this paper, ultraperformance liquid chromatography/quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF/MS) and the MetaboLynx™ software combined with mass defect filtering were applied to identity the metabolites of isoquercitrin using an intestinal mixture of bacteria and 96 isolated strains from human feces. The human incubated samples collected for 72 h in the anaerobic incubator and extracted with ethyl acetate were analyzed by UPLC-Q-TOF/MS within 10 min. The parent compound and five metabolites were identified by eight isolated strains, including Bacillus sp. 17, Veillonella sp. 23 and 32 and Bacteroides sp. 40, 41, 56, 75 and 88 in vitro . The results indicate that quercetin, acetylated isoquercitrin, dehydroxylated isoquercitrin, hydroxylated quercetin and hydroxymethylated quercetin are the major metabolites of isoquercitrin. Furthermore, a possible metabolic pathway for the biotransformation of isoquercitrin was established in intestinal flora. This study will be helpful for understanding the metabolic route of isoquercitrin and the role of different intestinal bacteria in the metabolism of natural compounds. Copyright © 2012 John Wiley & Sons, Ltd.
研究领域:
分析化学
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微生物学
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代谢组学
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PubMed
高影响因子
Biomedical Optics Express
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2025
·Vol. 16
·期 3
·1090-1103
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IF 3.2
Yong Wei,Yuye Xuan,Wenxiang Wang,Yonghui Zhang,Xiaoshan Li,Chunlan Liu,Chen Wang,Zhihai Liu
The existing screening methods for therapeutic targets of active ingredients in traditional Chinese medicine (TCM) have problems of long detection time and high instrument cost. This article proposes a new target screening method based on virtual screening and fiber surface plasmon resonance (SPR) sensing technology, which has the characteristics of flexibility, speed, and low cost. It also reveals the target mechanism of the active ingredient isoquercitrin in the treatment of insulin resistance (IR). The binding energies of isoquercitrin with target proteins PDPK1, INSR, and PTPN1 were calculated using computer virtual methods to be -8.9, -8.9, -8.8 kcal/mol, indicating strong binding activity with isoquercitrin and predicted as three key targets. Then a fiber optic SPR biosensor functionalized with isoquercitrin molecules was constructed to detect the binding affinity between isoquercitrin and the key targets. The experimental results showed that the binding affinities of isoquercitrin to the targets PDPK1, INSR, and PTPN1 were 1.45, 1.14, and 13.21, respectively, indicating that PTPN1 is the main target of isoquercitrin in the treatment of IR. The proposed sensor has a sensitivity of 0.699 nm/(μg/ml), LOD of 0.515μg/ml, and the experimental detection time of this method is as low as 45 minutes, without the need for large and expensive optical demodulation equipment, and the device volume is 5.50 dm3, providing new ideas for the screening of therapeutic targets of active ingredients in TCM.
研究领域:
药理学
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生物医学工程
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中药学
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PubMed
高影响因子
PREPARATIVE BIOCHEMISTRY & BIOTECHNOLOGY
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2020
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IF 1.415
Li Jun Li,Xiao Qing Liu,Xi Ping Du,Ling Wu,Ze Dong Jiang,Hui Ni,Qing Biao Li,Feng Chen
Isoquercitrin is a flavonoid with important applications in the pharmaceutical and nutraceutical industries. However, a low yield and high production cost hinders the industrial preparation of isoquercitrin. In the present study, isoquercitrin was prepared by biotransformation of rutin using α-L-rhamnosidase from Aspergillus niger JMU-TS528 combined with high-speed countercurrent chromatography (HSCCC) purification. As a result, the optimum transformation pH, temperature, and time were pH 4.0, 60 °C, and 60 min, respectively. The Km and Vmax were 0.36 mM and 0.460 mmol/min, respectively. For isoquercitrin production, the optimal rutin concentration and transformation time were approximately 1000 mg/L and 60 min. The rutin transformation rate reached 96.44%. The isoquercitrin was purified to a purity of 97.83% using one-step purification with HSCCC. The isoquercitrin was identified using UPLC-Q-TOF-MS. The comprehensive results indicated that the biotransformation procedure using the α-L-rhamnosidase from A. niger JMU-TS528 combined with HSCCC was a simple and effective process to prepare isoquercitrin, which might facilitate the production of isoquercitrin for industrial use.
研究领域:
生物化学
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制药工程
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食品科学
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PubMed
高影响因子
ANALYST
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2012
·Vol. 137
·期 17
·4076-4085
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IF 4.23
Xiao Lin,Yuzhi Wang,Xiaojie Liu,Songyun Huang,Qun Zeng
Ionic liquids-based microwave-assisted extraction (ILs-MAE) of medicinal or useful compounds from plants was investigated as an alternative to conventional organic solvent extractions. The extraction and the preconcentration of aqueous two-phase (ATP) systems have been integrated. Various operating parameters were systematically considered by single-factor and L9 (34) orthogonal array experiments. 1-Butyl-3-methylimidazolium tetrafluoroborate ([bmim][BF4]) has been selected to extract Apocynum venetum. The extract was then converted to the top phase by [bmim][BF4]/NaH2PO4 system which was suitable for the preconcentration. Reversed phase high performance liquid chromatography (RP-HPLC) with ultraviolet detection was employed for the analysis of hyperin and isoquercitrin in Apocynum venetum. The optimal experiment approach could provide higher detection limit of hyperin and isoquercitrin which were 3.82 μg L−1 and 3.00 μg L−1 in Apocynum venetum. The recoveries of hyperin and isoquercitrin were 97.29% (RSD = 1.02%) and 99.40% (RSD = 1.13%), respectively, from aqueous samples of Apocynum venetum by the proposed method. Moreover, the extraction mechanism of ILs-MAE and the microstructures and chemical structures of the herb before and after extraction were also investigated. The method exhibited potential applicability with other complicated samples.
研究领域:
药学
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分析化学
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PubMed
高影响因子
EXPERIMENTAL NEUROLOGY
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2024
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IF 4.6
Tingwang Guo,Gang Chen,Lin Yang,Jia Deng,Yun Pan
In intracerebral hemorrhage (ICH), the mechanical brain injury is a considerable and indispensable factor determining the neurological functions and poor outcomes. Previous studies indicate the mechanically gated ion channel-Piezo1 can transduce mechanical effects following ICH. Isoquercitrin (ISQ) is a well-studied ion channel inhibitor. Furthermore, whether the following Piezo1-mediated neurological impairment can be ameliorated by ISQ remains unclear. Herein, we constructed the hydrostatic pressure model and ICH rat model. Firstly, we found that Piezo1 agonists Yoda1 and Jedi1 facilitated extracellular calcium influx dramatically, but ISQ could depress intracellular Ca 2+ overload under hydrostatic pressure in primary neurons. Then we detected the expression profile of Piezo1, NLRP3 and NF-κB p-p65 after ICH, and found that the expression of Piezo1 was much earlier than NLRP3 and NF-κB p-p65. Furthermore, by western blot and immunofluorescence, ISQ decreased the expression of Piezo1 and NLRP3 dramatically like GsMTx4, but Nigericin as a NLRP3 agonist failed to affect Piezo1. Besides, both ISQ and interfering Piezo1 suppressed the upregulated caspase-1, NF-κB p-p65, p-IκBα, Tunel-positive cells and inflammatory factors (IL-1β, IL-6 and TNF-α) in ICH. At last, the hydrostatic pressure or hematoma induced disturbed neural viability, disordered neural cytomorphology, and increased neurobehavioral and cognitive deficits, but they were improved by ISQ and GsMTx4 strongly. Therefore, ISQ could alleviate neurological injuries induced by Piezo1 via NLRP3 pathway. These observations indicated that Piezos might be the new therapeutic targets, and blocking Piezos/NLRP3 pathway by ISQ could be an auspicious strategy for the treatment of ICH.
研究领域:
神经科学
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药理学
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分子生物学
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PubMed
高影响因子
ARCHIVES OF MICROBIOLOGY
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2025
·Vol. 207
·期 4
·1-12
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IF 2.6
Byambaakhuu Narantsetseg,Duan Shen,Sa Ren,Yang Qing-lan,Xu Hai-Yan,Shan Cheng-Bin,Xu Ri-hua,Ma Chao-Mei
This study was to evaluate the potential of human intestinal bacterial species in the biotransformation of rutin to quercetin and isoquercitrin which is rarer than rutin in nature and could more potently inhibit the growth of some cancer cell lines. Bacterial strains isolated from healthy human fecal samples were identified through 16S rDNA gene sequence analysis and genome analysis. Isoquercitrin and quercetin were identified and quantified by UHPLC-QQQ-MS in multiple reaction monitoring mode. As results, the intestinal bacterial strains, comprising nine Gram-positive rods and one Gram-negative rod, were classified into Enterococcus , Lactococcus , and Escherichia genera. Among the ten isolates , Lactococcus garvieae Y3-2 and Lactococcus petauri Y5-4 produced higher amounts of quercetin compared to other bacteria. Interestingly, all strains of Enterococcus faecium species (Y4-1, Y4-2, Y5-1, and Y5-2) exhibited a relatively strong ability to convert rutin to isoquercitrin, with Y4-2 being particularly efficient. The higher L-rhamnosidase activity observed in E. faecium Y4-1 and E. faecium Y4-2 correlated with their significant yield of isoquercitrin. Four or three genes were probably involved in rutin metabolism according to the analysis of flavonoid pathway based on genome sequences. The results provided information for selecting bacterial species to convert rutin into target bioactive compounds, and for purification of pure enzymes to biosynthesize isoquercitrin.
研究领域:
食品科学
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微生物学
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药理学
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PubMed
高影响因子
Food Chemistry-X
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2025
·
IF 8.2
Xiangyang Zhang,Yupei Sun,Zongwei Yu,Guoqiang Cai,Jianzeng Xin,Sheng Liu
Meat color is the most intuitive indicator for consumers to judge meat freshness, which mainly depends on myoglobin (Mb). In order to explore the effect of isoquercetin on meat color preservation and its mechanism, this study mainly carried out systematic research through in vitro experiments, multi-spectral technology, molecular docking and molecular dynamics simulation. This study found that isoquercetin has a good protective effect on meat color. And isoquercetin has a static quenching effect on Mb. In addition, after forming a stable complex through hydrogen bonds and van der Waals forces, isoquercetin changed the secondary structure of Mb, resulting in a decrease in surface hydrophobicity by 9.67 % and a decrease in solubility by 27 %. Molecular dynamics and molecular docking experiments further confirmed the interaction between the two. This study confirmed that isoquercitrin can stabilize meat color through a variety of mechanisms, providing a theoretical basis for its application in meat processing.
研究领域:
食品科学
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生物化学
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分子生物学
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光谱学
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计算生物学
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PubMed
高影响因子
AAPS PHARMSCITECH
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2024
·Vol. 26
·期 1
·1-13
·
IF 3.4
Sheng Liangju,Gao Fuping,Lan Zhe,Zong Bin,Wang Qilong
Osteoporosis has increasingly become a major public health concern because of its associated heightened risk of bone fragility and fractures. In order to avoid the adverse risk of hormone therapy, scientists have considered isoquercitrin (IQ) as a natural phytoestrogen to potentially prevent osteoporosis. However, IQ has poor solubility and bioavailability which culminates in rapid elimination of phytoestrogen. Herein, this study sought to solve limited applications of IQ by preparing IQ-loaded PEGylated long circulating liposomes (IQ-Lips) via thin-film hydration method. After appropriate characterization using zeta-potential, polydispersed index (PDI), particle size and entrapment efficiency (EE), IQ-Lips were applied to ovariectomized rat models to evaluate their effect on osteoporosis. The results showed that the prepared IQ-Lips exhibited smaller sized nanoparticles (125.35 ± 4.50 nm), excellent PDI (0.244 ± 0.001) and zeta-potential (-28.64 ± 0.71 mV) with stable property and higher EE (92.10 ± 0.32%). Importantly, administration of IQ-Lips through oral route increased aqueous solvability, bioavailability and circulation time of IQ. Moreover, the IQ-Lips could increase bone microstructural densities and bone mass, as well as reduce oxidative stress in ovariectomized rat models. Altogether, the IQ-Lips may serve as a novel avenue to potentially prolong the circulation of IQ in the body and improve the bioavailability of IQ for treatment of osteoporosis. Graphical
研究领域:
药剂学
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骨科医学
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分子生物学
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DOI
PubMed
高影响因子
ACS Sustainable Chemistry & Engineering
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2020
·
IF 7.632
Deqing Wang,Pu Zheng,Pengcheng Chen,Dan Wu
Deep eutectic solvents (DESs), considered to be “green media”, have recently been employed in multiple applications including biotransformations. Here, a DES was used in the production of isoquercitrin and l-rhamnose from rutin by enzymatic transformation with recombinant α-l-rhamnosidase from Aspergillus niger. A solution synthesized from choline chloride and urea (ChCl-U) performed best in the conversion of rutin among 24 kinds of DESs. When 130 g/L rutin was used as the substrate, the conversion rate was 100% and the productivity of l-rhamnose and isoquercitrin was 208.68 mM/h under optimized conditions in ChCl-U solution, which was 1.12 times higher than that in buffer (186.92 mM/h). The recycling of ChCl-U solution was also investigated by aqueous two-phase system extraction of l-rhamnose, and ChCl-U/K2HPO4 was screened as the suitable extraction solvent. When the ChCl-U content was 34%, the extraction efficiency of l-rhamnose was 79.06% with a purity and primary crystallization yield of 96.28 and 66.49%, respectively. After five cycles of ChCl-U solution, the average enzymatic conversion rate of recycling was 95.63% with an average purity of 94.22% of the isoquercitrin prepared. After 10 cycles of reuse, the residual conversion rate was 61.14%. The results indicate that the DES has obvious advantages in biocatalytic processes involving flavonoid conversion.
研究领域:
生物化学
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绿色化学
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酶工程
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DOI
高影响因子
CHEMICO-BIOLOGICAL INTERACTIONS
·
2023
·
IF 5.1
Jie Liu,Ailing Hui,Jinghe Wang,Qingfeng Hu,Shengnan Li,Yuanli Chen,Zeyu Wu,Wencheng Zhang
Neuroinflammation is considered as an important pathological mechanism in neurodegenerative diseases. The natural isoquercitrin (IQ) was reported to have potential anti-neuroinflammatory activity. The acylation of glycoside in IQ enhanced its hydrophobicity, which was expected to enhance the protective effect against inflammation. In this study, three carboxylic acids with anti-neuroinflammatory effects including cinnamic acid, ibuprofen (IBU) and acetylsalicylic acid were introduced into the 6''-OH of IQ through the corresponding vinyl esters intermediates ( 8a-8c ). Ultimately, the acylated IQ derivatives (Compound 9a-9c ) were obtained with 35–42% yields using immobilized lipase Novozym 435 as catalyst. Subsequently, their anti-neuroinflammatory activities were evaluated in lipopolysaccharide (LPS)-induced BV2 cells. Compound 9b improved cell viability in the range of ≤50 μM and significantly decreased NO, PGE 2 production and TNF-α, IL-1β release and oxidative stress level with a concentration-dependent manner. Also, it could downregulate iNOS, COX-2, TNF-α and IL-1β expression levels, approximately 40% reduction were achieved when 15 μM compound 9b was employed. In addition, compound 9b resisted phosphorylation and degradation of IkBαs, suppressing the activation of NF-κB signaling pathway, exhibiting excellent neuroinflammatory inhibition. Moreover, the administration of compound 9b (30, 60 mg/kg) alleviated behavioral disorders and neuronal damages in LPS-induced neuroinflammatory mice. Meanwhile, the decreased TNF-α, IL-1β release, expression and the inhibited glial cells activation were obtained in compound 9b -treated group, which was superior to that of IQ or IBU. Overall, these findings demonstrated that compound 9b , formed by the introduction of ibuprofen into IQ, can serve as a novel promising therapeutic agent for anti-neuroinflammation.
研究领域:
药理学
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神经科学
·
炎症
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PubMed
高影响因子
PHYTOMEDICINE
·
2024
·
IF 6.7
Majid Manzoor,Danni Chen,Jiahui Lin,Ying Wang,Lan Xiang,Jianhua Qi
Background Hair follicles play a crucial role in hair growth, wound healing, thermoregulation, and sebum production. Hair loss affects millions of people worldwide, yet therapeutic options for managing hair loss and pattern baldness are limited. Isoquercitrin (IQ), a natural small molecule from drinkable Chinese tea, is famous for anti-aging properties. Purpose This study aimed to explore the potential of IQ in treating and preventing hair loss, along with its underlying mechanisms. Methods The adult male and female, as well as middle-aged female sprague dawley (SD) rats were used to conduct hair growth experiments in vivo . Signaling pathways and target protein identification were analyzed through western blotting, drug affinity responsive target stability (DARTS), cellular thermal shift assay (CETSA) and surface plasmon resonance (SPR) analyses. Further, the targets were confirmed through in vivo inhibition experiments. Results IQ is reported here to stimulate anagen phase initiation and hair regrowth by directly interacting with adenosine 5′-monophosphate-activated protein kinase (AMPK) and insulin-like growth factor 1 receptor (IGF-1R). This process involves the AMPK/mammalian target of rapamycin (mTOR)/ unc-51-like autophagy-activating kinase 1 (ULK1) signalling pathway to trigger autophagy and the IGF-1R/phosphatidylinositol 3-kinase (PI3 K)/protein Kinase B (AKT), vascular endothelial growth factor (VEGF)/ vascular endothelial growth factor receptor (VEGFR)/ angiotensin (ANG) pathways to promote angiogenesis in female rats. Furthermore, the hair regrowth efficacy of IQ in adult male rats and middle-aged female rats was verified and shown. Similarly, our findings indicate that IQ promotes hair regrowth in middle-aged rats through autophagy and angiogenesis, akin to its effects in adult rats. Conclusion AMPK and IGF-1R proteins are identified as the target proteins of IQ and the AMPK/mTOR/ULK1, IGF-1R/PI3K/AKT and VEGF/VEGFR/ANG signalling pathways take important roles in hair growth effect of IQ. Thus, these signaling pathways are crucial for developing future treatments and clinical strategies for hair regeneration.
研究领域:
药理学
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皮肤病学
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分子生物学
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DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）