Comparative Pharmacokinetic Study of Taxifolin after Oral Administration of Fructus Polygoni Orientalis Extract in Normal and Fibrotic Rats by UPLC-MS/MS

Wei, Feili; Xu, Yuqian; Chen, Dexi; Gong, Muxin

doi:10.1155/2019/9348075

Cited by 11 publications

(3 citation statements)

References 42 publications

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“…This made it possible to use the compound in the form of a dietary additive as an antioxidant, an immunostimulatory agent, and a cardioprotector for athletes [11]. It was shown that the concentration of TAX in the nervous tissue was maintained for 24 h, whereas its intracellular level was maintained over a longer time in the epithelium [28,[45][46][47]. Therefore, an optimal condition providing a chronic action on a monolayer culture of the cerebral cortex was preliminary incubation for 24 h.…”

Section: Discussionmentioning

confidence: 99%

A Comparative Analysis of Neuroprotective Properties of Taxifolin and Its Water-Soluble Form in Ischemia of Cerebral Cortical Cells of the Mouse

Varlamova,

Uspalenko,

Khmil

et al. 2023

IJMS

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Cerebral ischemia, and, as a result, insult, attacks up to 15 million people yearly in the world. In this connection, the development of effective preventive programs and methods of therapy has become one of the most urgent problems in modern angiology and pharmacology. The cytoprotective action of taxifolin (TAX) in ischemia is well known, but its limitations are also known due to its poor solubility and low capacity to pass through the hematoencephalic barrier. Molecular mechanisms underlying the protective effect of TAX in complex systems such as the brain remain poorly understood. It is known that the main cell types of the brain are neurons, astrocytes, and microglia, which regulate the activity of each other through neuroglial interactions. In this work, a comparative study of cytoprotective mechanisms of the effect of TAX and its new water-soluble form aqua taxifolin (aqTAX) was performed on cultured brain cells under ischemia-like conditions (oxygen–glucose deprivation (OGD)) followed by the reoxygenation of the culture medium. The concentration dependences of the protective effects of both taxifolin forms were determined using fluorescence microscopy, PCR analysis, and vitality tests. It was found that TAX began to effectively inhibit necrosis and the late stages of apoptosis in the concentration range of 30–100 µg/mL, with aqTAX in the range of 10–30 µg/mL. At the level of gene expression, aqTAX affected a larger number of genes than TAX; enhanced the basic and OGD/R-induced expression of genes encoding ROS-scavenging proteins with a higher efficiency, as well as anti-inflammatory and antiapoptotic proteins; and lowered the level of excitatory glutamate receptors. As a result, aqTAX significantly inhibited the OGD-induced increase in the Ca2+ levels in the cytosol ([Ca2+]i) in neurons and astrocytes under ischemic conditions. After a 40 min preincubation of cells with aqTAX under hypoxic conditions, these Ca2+ signals were completely inhibited, resulting in an almost complete suppression of necrotic death of cerebral cortical cells, which was not observed with the use of classical TAX.

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Section: Discussionmentioning

confidence: 99%

A Comparative Analysis of Neuroprotective Properties of Taxifolin and Its Water-Soluble Form in Ischemia of Cerebral Cortical Cells of the Mouse

Varlamova,

Uspalenko,

Khmil

et al. 2023

IJMS

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“…Then, the mixture was centrifuged twice at 13,000 r/min for 5 min at 4°C. A 2 μl aliquot of the supernatant was injected into the LC–MS/MS system for analysis (Wei, Guo, Xu, Chen, & Gong, 2019).…”

Section: Methodsmentioning

confidence: 99%

Quantification of 10 bioactive components of Yazhangsan in rat plasma by LC–MS/MS and its application

Zhang

Chen

Liu

et al. 2020

Biomedical Chromatography

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Yazhangsan (YZS) is a common prescription for the treatment of cough and asthma caused by wind‐cold. The purpose of this study was to investigate the pharmacokinetic profiles of 10 bioactive components in YZS. A simple, sensitive and reliable high‐performance liquid chromatography coupled with a triple‐quadruple mass spectrometry method (LC–MS/MS) was developed and fully validated in this study for the measurement of these 10 bioactive compounds in rat plasma. One‐step protein precipitation method using methanol was applied to the treatment of rat plasma samples. Chromatographic separation was conducted on a C18 column by gradient elution, and water (containing 0.1% formic acid) and acetonitrile were chosen as the mobile phase. The analytes were quantified by using a mass spectrometer in multiple reaction monitoring scanning mode, and electrospray ionization was performed in positive and negative ion modes. The established method met the requirements for the quantification of these 10 bioactive compounds in biological samples, and it was successfully applied to the pharmacokinetic study of 10 components in rats after the intragastrical administration of YZS. This study will lay a foundation for the investigation of the mechanism of action of YZS and provide useful data for the rational use of YZS in clinical.

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“…or subacute i.p. injection [ 12 – 16 ]. Considering the major application of Bai-Tou-Weng-Tang for the treatment of UC and the high content of anemoside B4 in Bai-Tou-Weng-Tang together with its better distribution and ease of study in the intestine of colitis animals [ 17 ], it may be a more potent anti-UC agent than berberine as discovered in previous studies [ 14 ].…”

Section: Introductionmentioning

confidence: 99%

Anemoside B4 ameliorates TNBS-induced colitis through S100A9/MAPK/NF-κB signaling pathway

et al. 2021

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Background Despite the increased morbidity of ulcerative colitis (UC) in the developing countries, available treatments remain unsatisfactory. Therefore, it is urgent to discover more effective therapeutic strategies. Pulsatilla chinensis was widely used for the treatment of inflamed intestinal diseases including UC for thousands of years in China. Anemoside B4, the most abundant triterpenoid saponin isolated from P. chinensis, exerts anti-inflammatory and antioxidant effects and may be the most active compounds, which is responsible for the therapeutic effects. However, the mechanism how anemoside B4 executes its biological functions is still elusive. Methods Here, we used the 2, 4, 6-trinitrobenzene sulfonic acid (TNBS)-induced colitis rat model to evaluate the therapeutic effect of anemoside B4. Blood samples of colitis rats were collected for hematology analysis. The inflammation-associated factors were investigated by enzyme-linked immunosorbent assay (ELISA). Cell proliferation and apoptosis was determined with EdU cell proliferation assay and TUNEL assay. The proteins regulated by anemoside B4 were identified by label-free quantitative proteomics. The significantly down-regulated proteins were verified by Western blotting analysis. mRNA expression was analyzed by quantitative real-time RT-PCR. Results The results showed that anemoside B4 ameliorated TNBS-induced colitis symptoms, including tissue damage, inflammatory cell infiltration, and pro-inflammatory cytokine production, apoptosis and slowed proliferation in colon. Quantitative proteomic analyses discovered that 56 proteins were significantly altered by anemoside B4 in the TNBS-induced rats. These proteins mainly clustered in tricarboxylic acid (TCA) cycle and respiratory electron transport chain. Among the altered proteins, S100A9 is one of the most significantly down-regulated proteins and associated with NF-κB and MAPK signaling pathways in the pathogenesis of UC. Further experiments revealed that anemoside B4 suppressed the expression of S100A9 and its downstream genes including TLR4 and NF-κB in colon. In vitro, anemoside B4 could inhibit the NF-κB signaling pathway induced by recombinant S100A9 protein in human intestinal epithelial Caco-2 cells. Moreover, anemoside B4 inhibits neutrophils recruitment and activation in colon induced by TNBS. Conclusions Our results demonstrate that anemoside B4 prevents TNBS-induced colitis by inhibiting the NF-κB signaling pathway through deactivating S100A9, suggesting that anemoside B4 is a promising therapeutic candidate for colitis.

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Comparative Pharmacokinetic Study of Taxifolin after Oral Administration of Fructus Polygoni Orientalis Extract in Normal and Fibrotic Rats by UPLC-MS/MS

Cited by 11 publications

References 42 publications

A Comparative Analysis of Neuroprotective Properties of Taxifolin and Its Water-Soluble Form in Ischemia of Cerebral Cortical Cells of the Mouse

A Comparative Analysis of Neuroprotective Properties of Taxifolin and Its Water-Soluble Form in Ischemia of Cerebral Cortical Cells of the Mouse

Quantification of 10 bioactive components of Yazhangsan in rat plasma by LC–MS/MS and its application

Anemoside B4 ameliorates TNBS-induced colitis through S100A9/MAPK/NF-κB signaling pathway

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