BIOMEDICAL CHROMATOGRAPHY
·
2025
·Vol. 39
·期 7
·e70107
·
IF 1.7
Jin-yao Liu,Ying-ying Pang,Piao-piao Wang,Wen-yan Li,Jing Dong
Linezolid is an oxazolidinone with potent antibacterial activity against multidrug resistant Gram-positive bacteria. This study aimed to develop and validate a sensitive, rapid and reliable high-performance liquid chromatography-photodiode array detector method for determining linezolid concentrations in the plasma and urine and to further characterize the pharmacokinetics of linezolid in rats. Chromatographic separation was performed using a SinoPak BEH C 18 column with isocratic elution (acetonitrile: water, 28:72, v/v). The retention times of linezolid and the internal standard are 3.30 and 5.20 min, respectively. The calibration curve for linezolid was linear over the concentration range of 0.25–50.0 μg/mL in rat plasma and 1.00–100.0 μg/mL in rat urine. Intra- and inter-assay precision values were below 9.00%, with accuracy ranging from 0.67% to 8.34%. Plasma samples were extracted using acetonitrile-mediated protein precipitation, and the recovery was > 93%. Following intragastric (63 mg/kg) and intravenous (25 mg/kg) administration of linezolid to rats, the area under the plasma concentration–time profile from time 0 to infinity were 224.5 and 86.4 μg·h/mL, total clearance were 0.29 and 0.30 L/h/kg, respectively. The cumulative urinary excretion rates of linezolid were 26.2%–27.5% for both administration routes. The presented method can certainly be used for routine analysis of linezolid in plasma and urine.
研究领域:
药理学
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分析化学
·
临床医学
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DOI
PubMed
高影响因子
BIOMEDICAL CHROMATOGRAPHY
·
2025
·Vol. 39
·期 6
·e70089
·
IF 1.7
Chunhua Liu,Changli Fu,Luping Tang,Jieqi Li,Jia Sun,Yuan Lu,Jie Pan,Ting Liu,Yongjun Li,Yonglin Wang,Yong Huang,Yueting Li,Meng Zhou
Polygonum orientale L. (PO) represents significant bioactivities in treating myocardial ischemia (MI); however, its underlying mechanisms remain unclear. This study aims to elucidate PO's potential mechanisms in MI using an integrated approach that combines UHPLC–Q-Exactive Orbitrap HRMS, network pharmacology, and RNA-sequencing (RNA-seq). Initially, the chemical constituents of PO were identified using UHPLC–Q-Exactive Orbitrap HRMS. Subsequently, network pharmacology, molecular docking, and RNA-seq were employed to screen potential active components of PO targeting MI and predict their molecular mechanisms. Then, the molecular mechanisms were verified using western blotting and ELISA in MI mice. A total of 45 components were identified from PO, with 14 potential active compounds interacting with 204 MI-related genes. The findings suggest that PO could alleviate heart damage. The RNA-seq results indicated 244 potential targets regulated by PO. Integrating RNA-seq and network pharmacology analyses revealed that the toll-like receptor signaling pathway plays an important role, alongside the PI3K-Akt. Notably, PO reduced the expression of TLR4 and TLR2 while increasing p-Akt and p-PI3K levels in MI mice, leading to decreased inflammatory cytokines and apoptosis-related proteins. This study provides initial evidence that PO inhibits the toll-like signaling pathway and activates PI3K–Akt signaling pathway to exert protective effects against MI.
研究领域:
中药学
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分子生物学
·
心血管病学
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DOI
PubMed
高影响因子
BIOMEDICAL CHROMATOGRAPHY
·
2025
·Vol. 39
·期 5
·e70060
·
IF 1.7
Weijie Pan,Qianru Chen,Menghua Wu,Yue Sun,Ming Li,Shumei Wang,Xingyang Xue,Jiang Meng
Moutan Cortex (MC) is a renowned Chinese medicine used for promoting blood circulation and removing blood stasis. However, the active ingredients are unclear. This study aimed to identify and validate the active ingredients of MC. UPLC fingerprints of 23 batches of MC from various origins were analyzed. The activating blood efficacy of MC was assessed by evaluating the inhibitory effects on thrombin and factor Xa (FXa) using the chromogenic substrate method. Active ingredients were identified through spectrum-effect relationship analysis using gray relation analysis (GRA), partial least squares (PLS), and support vector machine (SVM) algorithms. Consequently, five components were identified as potential active ingredients: mudanpioside H, oxypaeoniflorin, 1,2,3,4,6-penta-O-galloyl-β-d-glucose (PGG), benzoyloxypaeoniflorin, and suffruticoside A/B/C/D. The pharmacological activities of these five active ingredients were further confirmed by measuring their thrombin inhibition ability and antithrombotic effects in zebrafish, and their interactions with thrombin and FXa were examined using molecular docking technology. Oxypaeoniflorin, benzoyloxypaeoniflorin, and PGG demonstrated significant efficacy in promoting blood circulation and resolving blood stasis, as well as strong binding affinities. This study provides a biochemical foundation for the anticoagulant effects of MC and offers valuable insights for quality control and the development of novel anticoagulant ingredients drugs.
研究领域:
中药学
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生物信息学
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药理学
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DOI
PubMed
高影响因子
BIOMEDICAL CHROMATOGRAPHY
·
2025
·Vol. 39
·期 6
·e70093
·
IF 1.7
Longxin Guo,Li Lin,Jun Ling,Shengkai Zhu,Xinyu Li,Minjuan Long,Yingjie Xu,Zhanjiang Hu,Ming Niu,Xu Zhao,Xiaohe Xiao
Corydalis yanhusuo W.T.Wang (YHS) is a commonly used traditional Chinese medicine, often prescribed for treating a variety of pains. In recent years, there has been a gradual increase in the number of reports to liver injury caused by YHS and its preparations, but the exact type and mechanism of hepatotoxicity are still unclear. In the present study, we demonstrated that YHS could induce idiosyncratic drug-induced liver injury (IDILI) in the inflammatory activation models. A total of 459 differential genes and 25 differential metabolites were identified by transcriptomics and metabolomics, which were significantly enriched in the TNF and NF-κB signaling pathways as well as glycerophospholipid metabolism, sphingolipid metabolism, and arachidonic acid metabolism. In addition, YHS significantly increased the levels of TNF-α, IL-1β, and IL-6. Therefore, we believe that the mechanism of toxicity may be related to the TNF and NF-κB signaling pathways, with glycerophospholipid metabolism, sphingolipid metabolism, and arachidonic acid metabolism also playing important roles. It provides a reference for the safe and rational use of YHS in clinical practice and contributes to the precise prevention and control of the risk of liver toxicity associated with YHS.
研究领域:
中药学
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毒理学
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分子生物学
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DOI
PubMed
高影响因子
BIOMEDICAL CHROMATOGRAPHY
·
2025
·Vol. 39
·期 4
·e70038
·
IF 1.7
Mengjiao Li,Fuqiang Liu,Lulu Guo,Wu Fan,Jiazhong Wang,Binbin Lu,Guangfeng Hong,Wenjuan Zhang,Shu Tian,Jian Mao,Jianping Xie
Cordycepin, a natural adenosine derivative, exhibits multiple pharmacological effects on organisms. However, its distribution and metabolic characteristics have not been fully elucidated in vivo. In this study, ultra-high liquid chromatography tandem high-resolution mass spectrometry (UHPLC-HRMS/MS) was used to investigate the pharmacokinetic characteristics and effects of cordycepin on endogenous adenosine and inosine. Microdialysis was used for real-time monitoring of unbound drug in brain and blood, whereas conventional tissue homogenate methods assessed distribution in various tissues. Results showed that the distribution pattern of cordycepin was as follows: kidney > liver > heart > lung > spleen > brain. Cordycepin administration significantly altered the levels of adenosine and inosine in heart and liver. Synchronous microdialysis sampling for the pharmacokinetic profile indicated that cordycepin was rapidly consumed and 3′-deoxyinosine was generated as the main metabolite. The C max values of cordycepin in the rat blood and brain after exposure (10 mg/kg, i.p.) were 7.8 and 5.4 ng/mL, respectively. Mean residence time in blood and brain was 102.2 and 137.0 min, respectively. Inhibition of adenosine deaminase by racemic 9-(2-hydroxy-3-nonyl) adenine hydrochloride (EHNA) enhanced cordycepin levels in the blood. This work provides a solid basis for understanding the metabolism of cordycepin and its pharmacological effects.
研究领域:
药理学
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分析化学
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生物化学
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DOI
PubMed
高影响因子
BIOMEDICAL CHROMATOGRAPHY
·
2025
·Vol. 39
·期 5
·e70083
·
IF 1.7
Yonghua Hu,Xujin Yang,Chenmei Ma,Zhen Wang,Xin Yuan,Man He,Penghai Zhang,Yi Tao
Da-Huang-Zhe-Chong Pills (DHZCPs) have demonstrated efficacy in treating uterine fibroids (UFs), but the mechanisms underlying their action remain unclear. In this study, untargeted serum metabolomic analysis was employed to investigate the therapeutic effects of DHZCP in a rat model of UFs utilizing advanced ultra-performance liquid chromatography tandem quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF/MS) and pattern recognition. Histopathological examination through H&E staining revealed significant improvements in uterine morphology following DHZCP administration. The levels of four serum hormones, that is, estradiol (E 2 ), follicle-stimulating hormone (FSH), luteinizing hormone (LH), and progesterone (PROG), tended to shift toward normal in the DHZCP-treated group compared with the model group. Our metabolomic profiling identified 20 distinct endogenous metabolites that were differentially expressed between UF and normal rats, with DHZCP treatment significantly normalizing 16 of these metabolic markers. Comprehensive pathway analysis highlighted three major metabolic pathways affected by DHZCP intervention: tryptophan metabolism, riboflavin metabolism, and arginine-proline metabolism. Notably, spearman correlation analysis indicated that tryptophan, lysoPC (18:1/0:0), uric acid, and serotonin were strongly positively correlated with serum levels of both E 2 and PROG. Additionally, riboflavin, indoleacetic acid, and indole-3-propionic acid were positively correlated with E 2 levels. Our findings suggest that DHZCP may exert therapeutic effects primarily through the modulation of tryptophan and riboflavin metabolism, providing a solid foundation for its clinical application.
研究领域:
药理学
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妇产科学
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代谢组学
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产品关联
DOI
PubMed
高影响因子
BIOMEDICAL CHROMATOGRAPHY
·
2025
·Vol. 39
·期 5
·e70055
·
IF 1.7
Nan Guo,Sheng Hu,Yahui Zhang,Wen Zhang,Dejun Li,Yue Tang,Zijian Tai,Xin Guo,Bing Leng
Tigecycline has been widely used for treating infections caused by multidrug resistant bacteria, but the dosage and intrapulmonary distribution were still controversial. In this study, a UPLC–MS/MS method was established and fully validated to quantify tigecycline in human plasma and BALF. A simple and rapid protein precipitation was used to extract the analytes from plasma and BALF samples. Then, tigecycline and IS were separated on a SHIMADZU AQ-C18 column and detected using electrospray ionization positive ion mode using the transitions of m / z 586.3 → 513.2 m / z for TGC and 458.0 → 441.0 m / z for minocycline (IS). The linearity of the calibration was in the range of 20–2000 ng/mL in plasma and BALF. The validated method was successfully applied to investigate pharmacokinetic characteristics of tigecycline in critically ill patients. The results suggested that after intravenous administration of 100-mg q12h tigecycline, the AUC 0–12 was 3663.02 ± 2075.84 ng × h/mL and C ss,av was 305.25 ± 172.99 ng/mL; the average plasma concentration/ELF concentration ratio was 3.66. Significant individual differences and highly variable pharmacokinetic properties were observed, indicating that adjustment of dosing regimens according to therapeutic drug monitoring is effective and efficient to guarantee the drug efficacy and safety especially for critically ill patients.
研究领域:
临床医学
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药理学
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产品关联
DOI
PubMed
高影响因子
BIOMEDICAL CHROMATOGRAPHY
·
2025
·Vol. 39
·期 5
·e70066
·
IF 1.7
Jiemei Liang,Hua Zhu,Qiyuan Yang,Zhouwei Li,Xiang Meng,Lanlan Fan,Li Li
Taxillus chinensis (DC) Danser ( T. chinensis ) is broadly used in traditional Chinese medicine. Although pharmacological research shows that the ethyl acetate extract of T. chinensis (JEA) has beneficial effects in treating hyperuricemic nephropathy (HN), the active components and potential mechanisms for these effects remain unclear. This study aims to predict the effective components and mechanism of JEA for HN. Firstly, we adopted UHPLC-Q-Exactive HFXMS technology to analyze the chemical profile of JEA and the absorbed prototype ingredients in rat plasma. In addition, network pharmacology methods were utilized by us to elaborate on the active compounds, signaling pathways, and potential mechanisms of JEA in treating HN. Finally, a UPLC method was established to screen potential chemicals that can effectively inhibit the activity of xanthine oxidase (XOD). A total of 92 components were systematically characterized in JEA. Of those, 46 compounds were identified in the plasma of rats administered with JEA extract. Through network pharmacology, 10 potential active components, 10 crucial target genes, and 20 pathways were predicted to be involved in the JEA-mediated treatment of HN. The molecular docking results indicated that oxyresveratrol, isorhammeiol, and robinetwere exhibited strong binding affinities for GAPDH, PPARG, and ALB. The analysis of the XOD inhibition experiment suggested that dihydromyricetin and oxyresveratrol exhibited potent inhibitory effects on XOD, with IC 50 values of 0.48 and 0.68 mg·mL −1 . This study preliminarily identified the potential effective components of JEA and revealed its underlying molecular mechanisms of action in preventing HN, which will improve our further studies on JEA to treat HN.
研究领域:
中药学
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药理学
·
代谢组学
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产品关联
DOI
PubMed
高影响因子
BIOMEDICAL CHROMATOGRAPHY
·
2025
·Vol. 39
·期 2
·e6060
·
IF 1.7
Chen Wang,Xueying Qin,Ying Wang,Weiping Wang,Shuai Sun,Hongsen Wang,Shiyu Li,Xiao Dai,Xianhong Zhu,Xun Gao,Kunming Qin,Qing Zhang
Choerospondias axillaris is a medicinal plant used for treating coronary heart disease (CHD) due to its broad spectrum of anti-inflammatory activities. Cyclooxygenase 2 (COX-2) and lipoxygenase 5 (5-LOX) were immobilized on magnetic nanoparticles for selective ligand-extraction of these two enzymes present in C. axillaris . Sixteen extracted components were identified and analyzed using ultraperformance liquid chromatography plus Q-Exactive Orbitrap tandem mass spectrometry (UHPLC-Q-ExactiveOrbitrap-MS/MS), including flavonoids Curcumin and Epicatechin. The metabolization of the aforementioned 16 components in rats with acute blood stasis indicated a solid pharmacodynamic foundation. This method offers an effective approach for conducting basic research on the enrichment, analysis, and efficacy evaluation of active components in complex natural products.
研究领域:
药理学
·
分析化学
·
天然产物研究
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DOI
PubMed
高影响因子
BIOMEDICAL CHROMATOGRAPHY
·
2026
·Vol. 40
·期 3
·e70366
·
IF 1.7
Zhiyuan Li,Qing Shao,Hongqun Qiao
A sensitive and robust HPLC-MS/MS method was developed and validated for the simultaneous determination of YWS22026 and its major metabolite M3 in rat plasma using protein precipitation. Chromatographic separation was achieved on a Shim-pack Scepter C18 column (4.6 × 50 mm, 3 μm) with a gradient elution program (mobile phase A: 0.2% formic acid in water; mobile phase B: methanol) at a flow rate of 0.9 mL/min. Detection was performed via positive electrospray ionization (ESI+) in multiple reaction monitoring (MRM) mode. The method demonstrated excellent specificity, accuracy (relative error, %RE < 9.1%), precision (relative standard deviation, %RSD < 9.9%), and linearity (5–2000 ng/mL for both analytes). The lower limit of quantification (LLOQ) was 5 ng/mL. Stability studies confirmed that plasma samples remained stable under various storage conditions (at room temperature for 10 h, −20°C for 22 days, three freeze–thaw cycles, and 4°C autosampler storage for 73 h). This validated method was successfully applied to a 26-week concomitant toxicokinetic study in Sprague–Dawley rats, which revealed significant sex-related differences in exposure for both YWS22026 and M3. These findings provide valuable insights for informing the safety assessment of YWS22026 in subsequent clinical trials.
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DOI
PubMed
高影响因子
BIOMEDICAL CHROMATOGRAPHY
·
2015
·Vol. 29
·期 8
·1133-1136
·
IF 1.723
Li Zhang,Chaozhan Wang,Yinmao Wei
Boronate affinity has attracted much attention in recent years. It has been broadly used for selective isolation and enrichment of cis -diol-containing molecules. Conventionally, the cis -diols are adsorbed in mild alkaline aqueous solutions. In this work, for the first time, we found that boronate affinity adsorption could also be performed in nonaqueous solvent at nonbasic pH. Cis -diol-containing compounds present in herbal medicines were used for the adsorption test. The results indicated that all compounds obtained higher recoveries in the organic solvents (methanol, acetonitrile, ethyl acetate) compared with alkaline buffer. The adsorption of vicinal cis -diol-containing molecules in organic solvents could be accomplished rapidly, with high selectivity and high recoveries (>80%). These results shed light on the possibility of boronate affinity adsorption in nonaqueous solvents. The results are very important for the isolation and enrichment of cis -diols, which have poor solubility in water, especially for those in herbal medicines. Copyright © 2015 John Wiley & Sons, Ltd.
研究领域:
生物化学
·
药物化学
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DOI
高影响因子
BIOMEDICAL CHROMATOGRAPHY
·
2017
·Vol. 31
·期 8
·e3937
·
IF 1.613
Ting Cui,Hong-Mei Qiu,Dan Huang,Qi-Xin Zhou,Xiao-Yan Fu,Hai-Yan Li,Xin-Hui Jiang
The determination of amino acids with actions like neurotransmitters or modulators has been increasingly important for diagnosis in many neuropsychiatric diseases. A rapid and simple high-performance liquid chromatography with fluorescence detection method was developed for simultaneous determination of seven amino acids: aspartate (Asp), glutamate (Glu), serine (Ser), glutamine (Gln), glycine (Gly), taurine (Tau) and γ-aminobutyric` acid (GABA). Homoserine was used as an internal standard. The analysis was performed on a BDS column with methanol and 50 m m sodium acetate solution (pH 6.5) using a simple gradient elution. Several parameters of the developed method were validated including linearity, accuracy, precision, extraction recovery and stability, which were within the acceptable range. The method was successfully applied to determination of real samples: hippocampus and cortex in depressed rats exposed to chronically unpredictable stress in order to study if there existed differences in the seven amino acids levels between depressed rats and control. The results showed that Asp, Gly, Tau and GABA significantly decreased with increasing Gln in the hippocampus of depressed rats, compared with that of the control group, among which obviously lower level of Asp and higher level of Gln in cortex were observed. The analytical method and the results could be useful for clinical diagnosis and further insight into pathophysiological mechanism of depression.
研究领域:
神经科学
·
分析化学
·
精神病学
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DOI
高影响因子
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