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- W4313655411 abstract "In the present study, a pharmacokinetics(PK)-pharmacodynamics(PD) model in the anti-inflammatory active components in Inula cappa extract was established based on the lipopolysaccharide(LPS)-induced in vitro inflammation model in order to clarify the relationship between the dynamic changes of anti-inflammatory active components in inflammatory cells and their efficacy. Firstly, the inflammation model in vitro was induced by 1 μg·mL~(-1) LPS in RAW264.7 cells for 24 h. After treatment with 400 μg·mL~(-1) I. cappa extract, the pharmacokinetics(PK) of five anti-inflammatory active components, including luteolin(LUT), chlorogenic acid(CA), cryptochlorogenic acid(CCA), 3,4-dicaffeoylquinic acid(3,4-DCQA), and 4,5-dicaffeoylquinic acid(4,5-DCQA), in normal cells and inflammatory cells was compared. Meanwhile, the PD study was carried out by measuring the inflammatory factors NO and TNF-α in the cell supernatant at each time point, which was fitted with PK by the Phoenix Model in the WinNonlin 8.2 to establish the PK-PD model for five components including LUT, CA, CCA, 3,4-DCQA, and 4,5-DCQA. The results showed that compared with normal cells, the model cells showed increased or decreased uptake of five components, advanced T_(max), faster absorption, prolonged MRT and t_(1/2), and increasing or decreasing trend of CL_(z/F) and V_(z/F). When NO was used as the efficacy index, the PK-PD model after the integration of the multi-effect components in I. cappa was E=7.45×[1-Ce~(5.74)/(78.24~(5.74)+Ce~(5.74))], while with TNF-α as the efficacy index, the PK-PD model after the integration of the multi-effect components in I. cappa was E=79.28×[1-Ce~(6.45)/(85.10~(6.45)+Ce~(6.45))]. The results of the study suggested that the inflammatory state could change the cellular PK of I. cappa. The anti-inflammatory effect of active components in I. cappa might be related to the down-regulation of the secretion of NO and TNF-α in inflammatory cells, and NO and TNF-α might serve as the anti-inflammatory targets of active components of I. cappa." @default.
- W4313655411 created "2023-01-07" @default.
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- W4313655411 date "2022-12-01" @default.
- W4313655411 modified "2023-09-29" @default.
- W4313655411 title "[Establishment of PK-PD model in anti-inflammatory active components in Inula cappa extract based on lipopolysaccharide-induced in vitro inflammation model]." @default.
- W4313655411 doi "https://doi.org/10.19540/j.cnki.cjcmm.20220914.201" @default.
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