JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES
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2014
·
IF 2.694
Wei-min Zhang,Rui-fang Li,Ming Sun,Da-ming Hu,Jian-fei Qiu,Yun-hao Yan
A rapid, sensitive and selective ultra-performance liquid chromatography tandem mass spectrometry (UPLC–MS/MS) was developed and validated for the determination and pharmacokinetic investigation of avicularin in rat plasma. Sample preparation was accomplished through a simple one-step deproteinization procedure with 0.2 mL of acetonitrile–methanol (9:1, v/v) to a 0.1 mL plasma sample. Plasma samples were separated by UPLC on an Acquity UPLC BEH C18 column using a mobile phase consisting of acetonitrile–0.1% formic acid in water with gradient elution. The total run time was 1.60 min and the elution of avicularin was at 1.20 min. The detection was performed on a triple quadrupole tandem mass spectrometer in the multiple reaction-monitoring (MRM) mode using the respective transitions m / z 434.1 → 301.3 for avicularin and m / z 237.2 → 194.3 for carbamazepine (IS), respectively. The calibration curve was linear over the range of 10–3000 ng/mL with a lower limit of quantitation (LLOQ) of 10 ng/mL. Mean recovery of avicularin in plasma was in the range of 84.2–89.5%. Intra-day and inter-day precision were both <12%. This method was successfully applied in pharmacokinetic study after intravenous administration of 5.0 mg/kg avicularin in rats.
研究领域:
分析化学
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药理学
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DOI
PubMed
高影响因子
IET Nanobiotechnology
·
2020
·Vol. 14
·期 3
·239-244
·
IF 1.859
Hui Guo,Yun Fei Chen,Yi Tang,Jun Qing Qian
In order to expand the application in the medical field and enhance pharmacological effects, casein–myricetin nanomicelles were prepared by the self-assembly method and characterised by ultraviolet–visible spectroscopy and Fourier transform infrared spectroscopy. The parameters in self-assembly were optimised according to the factors of particle size, encapsulation yield, and drug loading. The result showed a pH of 5.5, a casein concentration of 2 mg/ml, a mass ratio of casein to myricetin of 8:1, ultrasonic power of 300 W, ultrasonic time of 5 min and ethanol volume of 7 ml were the optimal conditions. The situ cycle intestinal perfusion methods indicated that casein–myricetin nanomicelles can be more easily absorbed by small intestine than myricetin standard sample. Therefore, casein micelles are effective for improving the water solubility of myricetin.
研究领域:
食品科学
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药理学
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医学
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DOI
PubMed
高影响因子
JOURNAL OF NANOPARTICLE RESEARCH
·
2024
·Vol. 27
·期 1
·1-14
·
IF 2.1
Li Tingyuan,Li Jiaying,Wang Qilong,Gong Mingjie,Wang Xiaowen,Jiang Xia,Hua Qinyang,Ji Hao,Toreniyazov Elmurat,Yu Jiangnan,Cao Xia,Adu-Frimpong Michael,Xu Ximing
Isorhamnetin (ISO) is a kind of flavonoid widely found in sea buckthorn, ginkgo biloba, and other plants. It has many pharmacological activities, but poor solubility in aqueous media has limited its clinical application. In order to increase the bioavailability of ISO, we employed a thin film dispersion method to prepare ISO-loaded Soluplus-TPGS mixed polymer micelle (ISO-STM) and subsequently conducted appropriate characterizations. The micelles prepared in this work were spherical nanoparticles with uniform distribution with respective particle size (PS) and dispersion coefficient (PDI) of 81.62 ± 1.23 nm and 0.115 ± 0.020. Meanwhile, the encapsulation rate (EE) was 91.37% ± 0.82%, whereas the drug loading (DL) was 5.91% ± 0.06%. Compared to free ISO, the dissolution rate of mixed micelles (MM) significantly increased in three media. After oral administration, the oral bioavailability of MM was nearly 3 times higher than free ISO’s. In addition, the results of the zebrafish experiment showed that the anti-aging of zebrafish in the administration group was significantly better than that in the model control group. In summary, ISO-STM is a promising method with the potential to improve the solubility, and bioavailability and enhance the clinical application value of ISO.
研究领域:
药剂学
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药理学
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DOI
高影响因子
Biomed Research International
·
2018
·
IF 2.583
Zhihua Liao,Fei Qiu,Junlan Zeng,Li Gu,Bangjun Wang,Xiaozhong Lan,Min Chen
Rhodiola crenulata is a Tibetan native herbal plant belonging to the family of Crassulaceae, which produces the pharmaceutical icariside D2 with the activities of inhibiting angiotensin-converting enzyme and killing leukemia cancer cells. In this study, we functionally characterized a novel UDP-glycosyltransferase (RcUGT1) that converted tyrosol to specifically produce icariside D2 from R. crenulata at molecular and biochemical levels. RcUGT1 was highly expressed in flowers and roots, while the icariside D2 content was much higher in stems than that in other organs, suggesting the potential translocation of icariside D2 from flowers and roots to stems. The high production of icariside D2 in stems provided a reasonable suggestion to farmers to harvest stems instead of roots for icariside D2 production. Enzymatic assays of recombinant RcUGT1 indicated that it converted tyrosol to specifically form icariside D2, with the values of Km 0.97±0.10 mM, Vmax 286±8.26 pKat/mg, Kcat 0.01552 s−1, and Kcat/Km 159.55 s−1 M−1. Functional identification of RcUGT1 facilitated the icariside D2 production through metabolic engineering in plants or synthetic biology in microbes.
研究领域:
植物学
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药理学
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生物化学
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PubMed
高影响因子
BIOSCIENCE BIOTECHNOLOGY AND BIOCHEMISTRY
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2012
·Vol. 76
·期 6
·1091-1097
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IF 1.276
Yue-Xiu SI,Zhi-Jiang WANG,Daeui PARK,Hyoung Oh JEONG,Sen YE,Hae Young CHUNG,Jun-Mo YANG,Shang-Jun YIN,Guo-Ying QIAN
We studied the inhibitory effects of isorhamnetin on mushroom tyrosinase by inhibition kinetics and computational simulation. Isorhamnetin reversibly inhibited tyrosinase in a mixed-type manner at Ki=0.235 ± 0.013 mM. Measurements of intrinsic and 1-anilinonaphthalene-8-sulfonate(ANS)-binding fluorescence showed that isorhamnetin did not induce significant changes in the tertiary structure of tyrosinase. To gain insight into the inactivation process, the kinetics were computed via time-interval measurements and continuous substrate reactions. The results indicated that inactivation induced by isorhamnetin was a first-order reaction with biphasic processes. To gain further insight, we simulated docking between tyrosinase and isorhamnetin. Simulation was successful (binding energies for Dock6.3: −32.58 kcal/mol, for AutoDock4.2: −5.66 kcal/mol, and for Fred2.2: −48.86 kcal/mol), suggesting that isorhamnetin interacts with several residues, such as HIS244 and MET280. This strategy of predicting tyrosinase interaction in combination with kinetics based on a flavanone compound might prove useful in screening for potential natural tyrosinase inhibitors.
研究领域:
生物化学
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药理学
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DOI
PubMed
高影响因子
International Journal of Electrochemical Science
·
2023
·
IF 1.5
Li Sun,Buhong Gao,Weina Jiang,Li Xu,Wen Lu,Shilong Yang,Dong Jiang,Jichao Chen,Huayu Xue,Jiuzhou Shi
Isorhamnetin as a natural product has excellent biological activity, but there are few reports of it in electrochemical applications. In this paper, we developed a neoteric electrochemical sensor for sensitive detection of mercury ions (Hg 2+ ) for the first time using glassy carbon (GC) electrode which was modified with isorhamnetin (ISO) and graphene oxide (GO). The electrochemical behaviors of the fabricated GC electrode were characterized by cyclic voltammetry (CV) and differential pulse voltammetry (DPV). Under optimal conditions, the linear range to detect Hg 2+ with DPV was from 1.0×10 -6 to 1.0×10 -4 M with limit detection of 2.3×10 -8 M (S/N=3). In addition, it also showed excellent selectivity of Hg 2+ with comparison to several inorganic salt ions and other metal ions. We also report the application for Hg 2+ detection in real water samples with a good recovery (92.1-104.7%). In conclusion, isorhamnetin can be applied in the electrochemical field successfully with extraordinary results.
研究领域:
分析化学
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环境科学
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生物医学工程
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DOI
高影响因子
Journal of Biomedical Nanotechnology
·
2024
·Vol. 20
·期 9
·1457-1466
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IF 2.9
Shi Feng,Sun Weigang,Yin Wenxiong,Xia Xiaoli,Adu-Frimpong Michael,Cao Xia,Ji Hao,Wang Qilong,Xu Ximing,Yu Jiangnan
In this study, Esculin (ES)-loaded liposomes modified with TPGS (ES-TPGS-Ls) were successfully prepared to enhance bioavailability and hepatoprotective activity of this coumarin glucoside. We utilize thin-film dispersion to fabricate ES-TPGS-Ls. The size, polydispersed index (PDI),
Zeta potential (Z-potential), morphology, and encapsulation effectiveness of the liposomes were all evaluated afterwards. The storage stability of ES-TPGS-Ls at 4 °C was investigated. The findings showed that ES-TPGS-Ls had spherical nanoparticles with 194.47±8.54 nm as the mean
size, 0.239±0.011 as PDI, and −21.16±0.97) mV as Z-potential coupled with encapsulation efficiency (EE) of 91.85±0.44%. Storage stability of liposomes at 4 °C was maintained within one week. Pharmacokinetic study showed that the relative oral bioavailability
of ES-TPGS-Ls increased by 2.38 times. Pharmacodynamic studies showed that the developed liposomes could enhance the hepatoprotective activity of ES. Overall, the ES-TPGS-Ls significantly enhanced the bioavailability of esculin, thereby enhancing the in vivo hepatoprotective effect
of ES.
研究领域:
药剂学
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药物代谢动力学
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肝脏保护研究
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DOI
高影响因子
BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE
·
2024
·
IF 4.2
Huiyan Zha,Shuying Lv,Yuming Hu,Yaochen Xie,Lingkun Wang,Chen Yang,Guilin Li,Shuchen Gong,Li Ping,Difeng Zhu,Jiajia Wang,Qinjie Weng,Qiaojun He,Jincheng Wang
Acetaminophen (APAP) is a widely used analgesic and antipyretic medicine. It is frequently employed to alleviate pain and mitigate fever-related symptoms, but it can cause liver injury or even liver failure when overdosed. Isorhapontigenin, a compound derived from Chinese herbs and grapes, has been demonstrated to exhibit antioxidant and anti-inflammatory effects. This study focused on evaluating the effect of isorhapontigenin in alleviating APAP-induced liver injury. In the study, a single intraperitoneal administration of APAP was employed to induce liver injury, and isorhapontigenin was given orally 3 days before or 1 h after APAP administration. The results revealed that isorhapontigenin significantly mitigated liver injury by effectively inhibiting APAP-induced apoptosis, oxidative stress, and inflammation. Furthermore, transcriptomic RNA sequencing of liver tissues indicated that isorhapontigenin probably protected against APAP-induced liver injury by promoting fatty acid oxidation. Pharmacological experiments also demonstrated that isorhapontigenin treatment led to a significant reduction in triglyceride accumulation, increased ATP levels and direct fatty acid oxidation activity, as well as enhanced expression of proteins associated with fatty acid oxidation, including PPAR-α, PGC-1α, and CPT-1A. Moreover, the protective effects of isorhapontigenin against APAP-induced liver injury were abolished by a CPT-1A inhibitor, etomoxir. Notably, we found that combining isorhapontigenin with NAC ( N -acetyl-L-cysteine) resulted in a more significant alleviation of APAP-induced liver injury compared to NAC alone. In conclusion, our study indicates that isorhapontigenin is a potential therapeutic strategy that works by regulating fatty acid oxidation to alleviate APAP-induced liver injury.
研究领域:
药理学
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肝脏病学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
Food & Function
·
2025
·
IF 5.4
Xiaoran Kong,Li Zhao,He Huang,Qiaozhen Kang,Jike Lu,Jia-Qing Zhu
Hyperuricemia is chronic metabolic disease with a high incidence, and it has become the “fourth highest” health risk in modern times. Isorhamnetin is a natural flavonoid found in a variety of plants, especially fruits such as buckthorn. In vivo hyperuricemia ameliorating effect of isorhamnetin and the specific molecular mechanism were profoundly investigated through a hyperuricemia mice model in the present study. The results demonstrated that isorhamnetin showed a significant uric acid-lowering effect in mice. Isorhamnetin was able to reduce uric acid production by inhibiting XOD activity. On the other hand, it reduced the expression of GLUT9 to inhibit uric acid reabsorption and enhanced the expression of ABCG2, OAT1, and OAT3 to promote uric acid excretion. Metabolomics analysis revealed that isorhamnetin gavage restored the purine metabolism and riboflavin metabolism disorders, and thus significantly alleviated the hyperuricemia in mice. Further, the alleviating effect of isorhamnetin on hyperuricemia-induced renal inflammation and its specific mechanism were explored through network pharmacology and molecular validation experiments. Network pharmacology predicted that seven targets were enriched in the PI3K/AKT pathway (CDK6, SYK, KDR, RELA, PIK3CG, IGF1R, MCL1) and four targets were enriched in the NF-κB pathway (SYK, PARP1, PTGS2, RELA). Western blot validated that isorhamnetin inhibited the phosphorylation of PI3K and AKT and down-regulated the expression of NF-κB p65. It indicated that isorhamnetin could inhibit the PI3K/AKT/NF-κB signaling pathway to reduce the levels of renal inflammatory factors (TNF-α, IL-β and IL-6) and ultimately ameliorate the hyperuricemia-induced renal inflammation in mice. This study will provide comprehensive and penetrating theoretical basis for the application of isorhamnetin in the field of functional foods or dietary supplements to improve hyperuricemia.
研究领域:
药理学
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代谢生物学
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分子生物学
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DOI
PubMed
高影响因子
BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS
·
2025
·
IF 3.3
Zhixin Zhang,Linli Zhao,Jiahui Wang,Hao Chen,Yan Lin,Fangbin Wang,Lu Wang,Juan Chen,Jian Liu,Xian Zhang
In beige adipocytes, UCP1-dependent thermogenesis can be driven by intracellular reactive oxygen species (ROS) generation. While ROS elevation also induces mast cell activation, serotonin synthesis and release from mast cells inhibits beige progenitor cell proliferation and browning. As a natural antioxidant and mast cell stabilizer, luteolin promotes adipocyte thermogenesis and inhibits mast cell activation. Thus, to activate adipocyte thermogenesis, how luteolin regulates ROS level in beige adipocytes and mast cells needs to be further investigated. In this study, mouse subcutaneous stromal vascular fraction (SVF) cells are induced to differentiate into beige adipocytes, and mouse bone marrow-derived mast cells (BMMCs) are activated with hydrogen peroxide (H 2 O 2 ). Intracellular ROS level is augmented in differentiated beige adipocytes and H 2 O 2 -activated BMMCs, and H 2 O 2 -activated BMMCs inhibited brown differentiation of SVF cells and thermogenesis of beige adipocytes. In beige adipocytes, unlike synthetic antioxidant N -acetylcysteine (NAC), luteolin elevates the expression of thermogenic and beige-selective marker genes and intracellular ROS generation. Contrarily, luteolin inhibits H 2 O 2 -induced mast cell activation and ROS generation. Further, luteolin partially reverses the inhibitory effects of H 2 O 2 -activated BMMCs on the brown differentiation of SVF cells and the thermogenesis of beige adipocytes. Molecular mechanistic studies demonstrate that luteolin regulates intracellular ROS level in beige adipocytes and mast cells via the nuclear factor erythroid 2-related factor 2 (Nrf2)/Catalase pathway. Altogether, as a ROS regulator, luteolin contrarily affects intracellular ROS generation in beige adipocytes and mast cells, and hence elevates adipocyte browning.
研究领域:
分子生物学
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代谢研究
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药理学
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DOI
PubMed
高影响因子
MOLECULAR NUTRITION & FOOD RESEARCH
·
2025
·
IF 4.2
Bin Xu,Yan Zhuang,Ying Zhang,Suoning Liu,Rongjun Fan,Weiru Jiang
Epithelial barrier dysfunction, critically involved in intestinal ischemia/reperfusion (I/R) injury, is significantly regulated by Nrf2-mediated oxidative stress. Apigenin, a flavonoid commonly found in fruits and vegetables with diverse biological properties, has an unclear impact on intestinal I/R injury. We hypothesize that apigenin improves intestinal barrier dysfunction by activating Nrf2 signaling. Thirty rats were randomly divided into five groups to establish an I/R model using superior mesenteric artery occlusion. Hypoxia and re-oxygenation (H/R) model was developed utilizing Caco-2 and IEC-6 cells, which were exposed to hypoxic conditions followed by re-oxygenation. Apigenin protected against intestinal mucosal damage by suppressing inflammatory cytokines release (TNF-α, IL-1β, IL-6, MPO, p < 0.01), ameliorating oxidative stress (MDA, SOD, GSH, GSH-Px, p < 0.01), and improving barrier dysfunction (DAO and TEER, p < 0.01) both in vivo and in vitro, without causing significant changes in the corresponding normal controls ( p > 0.05). Apigenin up-regulated the protein expression of Nrf2, HO-1, and tight junction (TJ) proteins ( p < 0.01). Furthermore, the knockdown of Nrf2 significantly abrogated apigenin-enhanced the TJ expression. Apigenin pretreatment alleviates intestinal I/R-induced barrier damage through Nrf2 activation and TJ upregulation, offering new strategies for preventing or treating I/R-associated intestinal diseases.
研究领域:
药理学
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分子生物学
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消化系统疾病
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DOI
PubMed
高影响因子
Molecular Medicine Reports
·
2020
·Vol. 22
·期 4
·3151-3160
·
IF 2.1
Bing‑Feng Guan,Xiao‑Feng Dai,Qi‑Bin Huang,Di Zhao,Jin‑Long Shi,Cheng Chen,Yan Zhu,Fen Ai
Icariside II (ICAII) is a bioflavonoid compound which has demonstrated anti‑oxidative, anti‑inflammatory and anti‑apoptotic biological activities. However, to the best of our knowledge, whether ICAII can alleviate myocardial ischemia and reperfusion injury (MIRI) remains unknown. The aim of the present study was to determine whether ICAII exerted a protective effect on MIRI and to investigate the potential underlying mechanism of action. A rat MIRI model was established by ligation of the left anterior descending coronary artery for 30 min, followed by a 24 h reperfusion. Pretreatment with ICAII with or without a PI3K/AKT inhibitor was administered at the beginning of reperfusion. Morphological and histological analyses were detected using hematoxylin and eosin staining; the infarct size was measured using Evans blue and 2,3,5‑triphenyltetrazolium chloride staining; and plasma levels of lactate dehydrogenase (LDH) and creatine kinase‑myocardial band (CK‑MB) were analyzed using commercialized assay kits. In addition, the cardiac function was evaluated by echocardiography and the levels of cardiomyocyte apoptosis were determined using a TUNEL staining. The protein expression levels of Bax, Bcl‑2, cleaved caspase‑3, interleukin‑6, tumor necrosis factor‑α, PI3K, phosphorylated (p)‑PI3K, AKT and p‑AKT were analyzed using western blotting analysis. ICAII significantly reduced the infarct size, decreased the release of LDH and CK‑MB and improved the cardiac function induced by IR injury. Moreover, ICAII pretreatment significantly inhibited myocardial apoptosis and the inflammatory response. ICAII also upregulated the expression levels of p‑PI3K and p‑AKT. However, the protective effects of ICAII were abolished by an inhibitor (LY294002) of the PI3K/AKT signaling pathway. In conclusion, the findings of the present study suggested that ICAII may mitigate MIRI by activating the PI3K/AKT signaling pathway.
研究领域:
药理学
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心脏病学
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分子生物学
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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）