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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产品关联
DOI
PubMed
高影响因子
BIOMEDICAL CHROMATOGRAPHY
·
2025
·Vol. 39
·期 2
·e6065
·
IF 1.7
Yong Jiang,Wenjun Ji,Ying Lu,Qin Wang,Linwei Chen
The high mortality rate of chronic heart failure (CHF) makes it a primary battlefield in the field of cardiovascular diseases. Qiangxin Lishui Prescription (QLP) is a traditional Chinese medicine (TCM) prescription used clinically for treating CHF, but its underlying mechanism remains unclear. This study integrated plasma metabolomics, network pharmacology, and experimental validation to reveal the pharmacological effects of QLP and its potential mechanism of anti-CHF. Using ultra-high-performance liquid chromatography combined with quadrupole time-of-flight mass spectrometry (UPLC-Q/TOF-MS/MS), 119 absorbed prototype compounds of QLP were identified from rat plasma. By applying network pharmacology and molecular docking techniques, a QLP absorption components–target–CHF network was constructed. The IL6/JAK/STAT3 signaling pathway is likely critical to QLP's therapeutic effect on CHF. A CHF mouse model was established using aortic ligation surgery to investigate the regulation of the IL6/JAK/STAT3 pathway by QLP in CHF mice. Network pharmacology analysis and in vivo experimental data indicate that QLP alleviates myocardial injury and inflammatory response in CHF mice by modulating the IL6/JAK/STAT3 pathway, significantly improving cardiac function. This presents a promising therapeutic strategy for CHF treatment.
研究领域:
中医药学
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心血管疾病
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药理学
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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
·
2024
·
IF 1.8
Xiaomin Xu,Donghua Yu,Yu Wang,Peng Xu,Xin Jiang,Fang Lu,Shumin Liu
Resveratrol (Res) has been demonstrated to have beneficial effects on gouty nephropathy (GN). However, the mechanisms of Res on GN remain unclear. This study aimed to investigate the mechanisms of Res on GN. In this study, network pharmacology technology was used to predict the Res targets in the prevention and treatment of GN. Renal metabonomics was used to identify differential metabolites in kidney tissue of GN model rats. Finally, molecular docking technology was used to verify the binding ability of Res to key targets. Metabonomics analysis showed that 24 potentially important metabolites were involved in the prevention and treatment of GN with Res. After exposure to Res, metabolite levels normalized. The network pharmacology analysis showed that 24 key targets were involved in the prevention and treatment of GN disease. According to the metabolite–gene network diagram, we identified two core genes, PTGS1 and PTGS2, and found that both were involved in the arachidonic acid metabolism pathway. Molecular docking further verified the affinity of Res binding to PTGS1 and PTGS2. In conclusion, the mechanism of Res against GN may be the regulation of arachidonic acid metabolism through the regulation of PTGS 1 and PTGS 2.
研究领域:
药理学
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代谢组学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
BIOMEDICAL CHROMATOGRAPHY
·
2025
·Vol. 39
·期 2
·e6074
·
IF 1.7
Qinghai Dong,Fei Shi,Fang Lin,Yaqi Wang,Yang An,Hongliu Xie,Jihua Liu
Previous studies have suggested that ginsenoside Rg 2 glycine ester derivative (RG) exhibits therapeutic potential in mitigating hypoxia. This study aimed to elucidate the potential mechanism of RG in hypoxia injury through a combined approach of metabolomics and network pharmacology. Initially, a CoCl 2 -induced cell hypoxia model was established, and the therapeutic impact of RG on biochemical indices was evaluated. Subsequently, metabolomics analysis of cell samples was conducted to identify biomarkers, and network pharmacology was employed to identify potential targets of RG for hypoxia treatment. Finally, the key target and pathway were verified. The study revealed that RG could reverse CoCl 2 -induced abnormalities in biochemical indicators. Metabolomics analysis identified 13 biomarkers and seven metabolic pathways associated with RG treatment. Utilizing network pharmacology, five key targets and five metabolic pathways were identified, partially aligning with the metabolomics results. Molecular docking results demonstrated the effective binding of RG to the key targets. Enzyme linked immunosorbent assay verified that RG could exert antihypoxia effect by activated PI3K/Akt pathway. In conclusion, this integrated strategy, combining metabolomics with network pharmacology, sheds light on the protective mechanism of RG against hypoxia-induced cellular damage. The findings offer valuable insights for future research and potential applications of RG in the field.
研究领域:
药理学
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代谢组学
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细胞生物学
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产品关联
DOI
PubMed
高影响因子
BIOMEDICAL CHROMATOGRAPHY
·
2025
·Vol. 39
·期 2
·e6068
·
IF 1.7
Wenbin Huang,Hongjian Zhang,Yayun Zhou,Xuechao Liu,Qilei Zhang,Xiaopeng Ma
Proteolysis targeting chimera (PROTAC) is emerging as a promising medicinal modality, which has aroused widespread interest among the field of pharmaceutical manufacturing in the recent years. ARV-471 is an orally active PROTAC estrogen receptor degrader against breast cancer, which leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. In this study, we developed a highly sensitive liquid chromatography tandem mass spectrometry method (LLOQ = 0.5 ng/mL) for the measurement of ARV-471 in rat plasma. The acetonitrile precipitated sample was separated on ACQUITY BEH C 18 column using acetonitrile-0.1% formic acid as mobile phased with gradient elution. Multiple reactions monitoring in positive ESI mode was employed for the quantification of ARV-471 ( m/z 724.4 → 396.2). The assay showed good linearity over the concentration range of 0.5–1000 ng/mL with correlation coefficient > 0.996. The assay was validated according to FDA guidance, and all the validation parameters were within the predefined acceptance criteria. After validation, the assay was applied to the pharmacokinetic study of ARV-471 in rats. Additionally, the metabolites in rat plasma were identified using liquid chromatography–high resolution mass spectrometry. Four metabolites were identified and characterized. Hydrolysis, glucuronidation and deamination were the main metabolic pathways of ARV-471 in rats.
研究领域:
药理学
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分析化学
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肿瘤学
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产品关联
DOI
PubMed
高影响因子
BIOMEDICAL CHROMATOGRAPHY
·
2025
·Vol. 39
·期 12
·e70245
·
IF 1.7
Shulu Zhang,Enlin Zhu,Zhibin Wang,Shuang Jiang,Xiaotian Wu,Li Zhang,Xuepeng Shi,Lin Wei,Yuanqiu Mu,Zheng Feng,Yinze Zhong,Xinhui Huang,Yeqing Xu,Chunjuan Yang,Chunli Gan
Syringa oblata Lindl. leaf extract has a long history of use with pharmacological properties such as heat-clearing, detoxifying, and anti-inflammatory effects. In this study, an ulcerative colitis (UC) animal model was established and compared with a normal group. The study simultaneously determined 6 components of S. oblata Lindl. leaf extract (protocatechuic acid, caffeic acid, quercetin 3-O-β-D-glucopyranoside, (8E)-ligstroside, oleuropein, and oleacein) in the plasma of rats. The results showed that the extract exhibited good biological utilization in both groups, with stable metabolism of the six components, maintaining effective plasma concentrations. Pharmacokinetic analysis suggested the extract's potential for UC treatment. The relative standard deviation (RSD) of precision and accuracy for the six components was below 13%, and the lower limits of quantification (LLOQ) were 5.10, 5.10, 10.2, 10.1, 3.39, and 3.18 ng/mL, respectively. The method met FDA bioanalytical validation criteria for stability, matrix effects, and extraction recovery. Significant pharmacokinetic differences between UC and normal rats were observed, highlighting the extract's potential for clinical application and health product development, offering a promising therapeutic option for UC.
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DOI
PubMed
高影响因子
BIOMEDICAL CHROMATOGRAPHY
·
2021
·Vol. 35
·期 12
·e5177
·
IF 1.902
Qian-qian Pang,Ting Li,Ling-xian Liu,Dan-feng Shi,Xin-sheng Yao,Hai-bo Li,Yang Yu
Cimicifuga dahurica (Turcz.) Maxim, which is also regarded as the main origin of “Shengma” in the Chinese Pharmacopoeia , has been used as a cooling and detoxification agent for thousands of years. Our previous phytochemical investigations of C. dahurica extracts (CDEs) led to the isolation of a series of 9,19-cycloalkane triterpenoids and phenolic acids showing a potential anti-inflammatory activity. However, the chemical profiling of CDEs and the material basis of its anti-inflammatory effect in vivo has not been clarified. In the present study, the CDE chemical profile and prototype components in rat plasma were identified via ultra-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry. As a result, a total of 106 components were identified or tentatively characterized in CDEs, including 54 triterpenoids, 35 phenolic acids, eight amides and nine other type constituents (39 compounds were confirmed with the reference standards). In addition, 20 prototype components (15 triterpenoids and five phenolic acids) were identified in rat plasma, which potentially related to the anti-inflammatory effects of CDEs. Moreover, the anti-inflammatory activities of the main prototype components were further evaluated by their inhibitory effects on the production of NO, as well as the expressions of iNOS and COX-2 in lipopolysaccharide-stimulated RAW264.7 cells, which indicated that 9,19-cycloalkane triterpenoids may play an anti-inflammatory role by down-regulating the expression of iNOS.
研究领域:
中药学
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药理学
·
分析化学
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DOI
PubMed
高影响因子
BIOMEDICAL CHROMATOGRAPHY
·
2019
·Vol. 34
·期 3
·e4769
·
IF 1.748
Lianguo Chen,Chao-Wei Wen,Ming-Jie Deng,Ping-Li,Zhi-Da Zhang,Zhuo-Hua Zhou,Xianqin Wang
This study was designed to investigate the metabolic and transcriptional alterations in seminal fluid caused by asthenozoospermia (AS). To address these issues, a method of metabonomics based on ultra-performance liquid chromatography–tandem mass spectrometry (UPLC–MS/MS) and real-time quantitative PCR (RT-qPCR) was performed to identify some crucial biomarkers and transcription levels of the enzymes in seminal fluid. Seminal fluid samples were collected from 87 AS patients and 73 healthy males with normozoospermia. The quantitative analysis by UPLC–MS/MS showed that 19 metabolites in seminal plasma were associated with AS, and they were involved in several metabolic pathways, such as energy metabolism, purine metabolism, methionine cycle, and branched chain amino acid metabolism. Among these metabolites, the levels of citric acid, malic acid, succinic acid, and pyruvic acid, which are related to energy metabolism, were collectively reduced in the AS group, whereas the lactic acid level was enhanced. These results indicated that lesser energy source (adenosine triphosphate) was produced through the anaerobic glycolysis pathway rather than via aerobic catabolism of suger and tricarboxylic acid cycle, resulting in reduced power of sperms. Meanwhile, partial least squares discriminant analysis showed significant differences in metabolic profiles between the AS and control groups. In addition, RT-qPCR results revealed that the expression levels of four genes encoding fructokinase citrate synthase , succinate dehydrogenase , and spermine synthase , which were related to energy metabolism, were decreased in the AS group. The 23 descriptors with differential expression in AS may be valuable for the diagnosis and sequential study on AS. These results will help highlight the role of sperm inactivity in AS pathogenesis.
研究领域:
生殖生物学
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分子生物学
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临床生物化学
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DOI
PubMed
高影响因子
BIOMEDICAL CHROMATOGRAPHY
·
2021
·Vol. 35
·期 10
·e5174
·
IF 1.902
Yuan Lu,Na Li,Xiaoqin Zhu,Jie Pan,Yonglin Wang,Yanyu Lan,Yongjun Li,Aimin Wang,Jia Sun,Chunhua Liu
Polygonum orientale L . is a traditional Chinese medicine having extensive pharmacological activities including antimyocardial ischemia (MI) injury properties. Isoorientin, orientin, vitexin, quercitrin, astragalin and protocatechuic acid are the main compounds in P. orientale extract. The aim of this study was to establish an ultra-performance liquid chromatography–tandem mass spectrometry method for the determination of the content of these compounds in urine, feces and bile samples simultaneously and application of the method in a comparative excretion study in normal and MI model rats after oral administration of P. orientale extract. Chromatographic seperation was conducted on an Agilent Eclipse Plus C 18 column with the mobile phase consisting of 0.1% formic acid–acetonitrile and 0.1% formic acid–water. Negative ion multiple reaction monitoring mode was used for quantification. The six compounds had good linearity ( r ≥ 0.9921) and acceptable accuracy ranging from 10.10 to −5.82% The relative standard deviations of within-day precision and inter-day precision were <10.45 and 13.44%, respectively. The extraction recovery of the six analytes ranged from 80.31 to 101.47% and the matrix effect was 82.56–102.88%, indicating that the preparations of sample collected form urine, feces and bile were stable throughout analysis. The excretion amount of the six analytes increased in both normal and MI model rats’ urine, feces and bile in a 24 h period and became stable between 36 and 48 h after administration. The total excretion rate of six compounds was <5% in urine, feces and bile of normal and MI model rats. The excretion peak period for all compounds in MI rats was slower than that in normal rats. This excretion study provides insights for further application and research on P. orientale .
研究领域:
药理学
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分析化学
·
中药学
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DOI
PubMed
高影响因子
BIOMEDICAL CHROMATOGRAPHY
·
2013
·Vol. 27
·期 12
·1759-1766
·
IF 1.945
Zhang-xiao Peng,Yan Wang,Xue Gu,Yuan-yuan Wen,Chao Yan
Several Chinese herbs, namely, Pu-Gong-Ying, Gan-Cao, Chai-Hu, Mu-Xiang, Gua-Lou and Huang-Yao-Zi, are frequently used in complex traditional Chinese medicing formulas for breast hyperplasia and breast tumor therapy. The pharmacological effects of these Chinese herbs are all described as ‘clearing heat-toxin and resolving masses’ in traditional use. However, the chemical profiles of anti-breast cancer constituents in these herbs has not been investigated so far. In this study, a bioactivity-oriented screening platform, which was based on a human breast cancer MCF-7 cellular model, semi-preparative high performance liquid chromatography coupled with ultraviolet spectrophotometry and ultraperformance liquid chromatography coupled to quadrupole-time-of-flight mass spectrometer, was developed to rapidly screen the six Chinese herbs. Two potential anti-breast cancer compounds, which were costunolide (Cos) and dehydrocostus lactone (Dehy), were identified in Mu-Xiang. Combination of the two compounds showed a synergism on inhibiting the proliferation of MCF-7 cells in vitro , which exhibits a potential application prospect for breast cancer therapy. This bioactivity-oriented screening strategy is rapid, economical, reliable and specific for screening potential anti-breast cancer compounds in traditional Chinese medicines. Copyright © 2013 John Wiley & Sons, Ltd.
研究领域:
药理学
·
肿瘤学
·
传统医学
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分析化学
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DOI
PubMed
高影响因子
BIOMEDICAL CHROMATOGRAPHY
·
2023
·Vol. 37
·期 5
·e5594
·
IF 1.8
Yunqian Feng,Pan Zhang,Yaxin Yang,Zhiwei Wang,Guoyong Luo,Wude Yang
Itea ilicifolia Oliv is a folk medicine with antioxidant potential. In this study, the fingerprints of 14 batches of I. ilicifolia were established by HPLC with 17 common peaks. The similarities evaluated by Similarity Evaluation System for Chromatographic Fingerprint of Chinese Materia (version 2012) were >0.89. Ten compounds were identified with definite structures by comparing the retention time and characteristic UV spectral pattern with those of reference substances. The antioxidant capacities of 14 batches of I. ilicifolia were evaluated based on O 2 · − , DPPH and ABTS · + radical scavenging assays in combination with ferric reducing antioxidant power assay. Via multivariate statistical analyses of gray relation analysis, bivariate correlation analysis and partial least squares regression analysis, a study on the spectrum–effect relationship was then performed to screen eight peaks as the antioxidant Q-markers of I. ilicifolia . The contents of representative antioxidant Q-markers (isoorientin, orientin, vitexin, isovitexin and iteafuranal A) in samples were accurately determined to be 0.054–0.118%, 0.034–0.080%, 0.018–0.055%, 0.031–0.091% and 0.033–0.140%, respectively. The qualitative and quantitative analytical method based on Q-markers helps to control the antioxidant quality of I. ilicifolia , which will lay the foundation to promote the rational utilization of I. ilicifolia in curing diseases related to oxidative stress.
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DOI
高影响因子
BIOMEDICAL CHROMATOGRAPHY
·
2015
·Vol. 29
·期 8
·1280-1289
·
IF 1.723
Xiang Ji,Dan Li,Hua Li
A novel molecularly imprinted polymer (MIP) monolith for highly selective extraction of cholecystokinin (CCK) neuropeptides was prepared in a micropipette tip. The MIPs were synthesized by epitope imprinting technique and the polymerization conditions were investigated and optimized. The synthesized MIPs were characterized by infrared spectroscopy, elemental analyzer and scanning electron microscope. A molecularly imprinted solid-phase microextraction (MI- μ -SPE) method was developed for the extraction of CCK neuropeptides in aqueous solutions. The parameters affecting MI- μ -SPE were optimized. The results indicated that this MIP monolith exhibited specific recognition capability and high enrichment efficiency for CCK neuropeptides. In addition, it showed excellent reusability. This MIP monolith was used for desalting and enrichment of CCK4, CCK5 and CCK8 from human cerebrospinal fluid prior to matrix-assisted laser desorption/ionization time-of-flight mass spectrometry analysis, and the results show that this MIP monolith can be a useful tool for effective purification and highly selective enrichment of multiple homologous CCK neuropeptides in cerebrospinal fluid simultaneously. By employing MI- μ -SPE combined with HPLC-ESI-MS/MS analysis, endogenous CCK4 in human cerebrospinal fluid was quantified. Copyright © 2015 John Wiley & Sons, Ltd.
研究领域:
分析化学
·
神经生物学
·
医学
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DOI
高影响因子
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