Matches in SemOpenAlex for { <https://semopenalex.org/work/W2011725503> ?p ?o ?g. }
- W2011725503 endingPage "e89752" @default.
- W2011725503 startingPage "e89752" @default.
- W2011725503 abstract "Baicalin has been used as mainly bioactive constituent of about 100 kinds of traditional Chinese medicines in Chinese pharmacopoeia. The effect of baicalin on cytochrome P450 should be paid more attention because baicalin was used widely. The aim of this study was to investigate whether baicalin could inhibit CYP1A2 in pooled human liver microsomes (HLMs) and in rats in vivo and the gene polymorphisms could affect inter-individual variation in IC50 in 28 human livers. Phenacetin was used as probe of CYP1A2. Kinetic parameter of CYP1A2 and IC50 of baicalin on CYP1A2 to each sample were measured and the common CYP1A2 polymorphisms (−3860G>A and −163C>A) were genotyped. The results showed that baicalin exhibited a mixed-type inhibition in pooled HLMs, with a Ki value of 25.4 µM. There was substantial variation in Km, Vmax, CLint of CYP1A2 and IC50 of baicalin on CYP1A2 (3∼10-fold). The range was from 26.6 to 114.8 µM for Km, from 333 to 1330 pmol·min−1·mg−1protein for Vmax and from 3.8 to 45.3 µL·min−1·mg−1 protein for CLint in HLMs (n = 28). The Mean (range) value of IC50 in 28 HLMs was 36.3 (18.9 to 56.1) µM. The genotypes of −3860G>A and −163C>A had no significant effect on the inhibition of baicalin on CYP1A2. The animal experiment results showed that baicalin (450 mg/kg, i.v.) significantly decreased the Cmax and CL of phenacetin, and increased C60 min, t1/2, Vd and AUC (P<0.05). There were significant correlations between percentage of control in C60 min, t1/2, CL, AUC of phenacetin and Cmax of baicalin in 11 rats (P<0.05). Protein binding experiments in vitro showed that baicalin (0–2000 mg/L) increased the unbound phenacetin from 14.5% to 28.3%. In conclusion, baicalin can inhibit the activity of CYP1A2 in HLMs and exhibit large inter-individual variation that has no relationship with gene polymorphism. Baicalin can change the pharmacokinetics of phenacetin in rats." @default.
- W2011725503 created "2016-06-24" @default.
- W2011725503 creator A5030128184 @default.
- W2011725503 creator A5039212509 @default.
- W2011725503 creator A5043886610 @default.
- W2011725503 creator A5046941513 @default.
- W2011725503 creator A5047986179 @default.
- W2011725503 creator A5066926559 @default.
- W2011725503 creator A5081194803 @default.
- W2011725503 date "2014-02-26" @default.
- W2011725503 modified "2023-10-01" @default.
- W2011725503 title "Inhibition of Baicalin on Metabolism of Phenacetin, a Probe of CYP1A2, in Human Liver Microsomes and in Rats" @default.
- W2011725503 cites W1586650121 @default.
- W2011725503 cites W1643324062 @default.
- W2011725503 cites W1734451748 @default.
- W2011725503 cites W1979637353 @default.
- W2011725503 cites W1982589515 @default.
- W2011725503 cites W1984552762 @default.
- W2011725503 cites W1985137752 @default.
- W2011725503 cites W2001003469 @default.
- W2011725503 cites W2024537358 @default.
- W2011725503 cites W2032967171 @default.
- W2011725503 cites W2045606394 @default.
- W2011725503 cites W2062764969 @default.
- W2011725503 cites W2070536631 @default.
- W2011725503 cites W2080767837 @default.
- W2011725503 cites W2084481978 @default.
- W2011725503 cites W2084485228 @default.
- W2011725503 cites W2088945339 @default.
- W2011725503 cites W2095166863 @default.
- W2011725503 cites W2097100227 @default.
- W2011725503 cites W2098965940 @default.
- W2011725503 cites W2128161188 @default.
- W2011725503 cites W2145696691 @default.
- W2011725503 cites W2148368238 @default.
- W2011725503 cites W2152964734 @default.
- W2011725503 cites W2169188579 @default.
- W2011725503 cites W28666504 @default.
- W2011725503 cites W4293247451 @default.
- W2011725503 doi "https://doi.org/10.1371/journal.pone.0089752" @default.
- W2011725503 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/3935934" @default.
- W2011725503 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/24587011" @default.
- W2011725503 hasPublicationYear "2014" @default.
- W2011725503 type Work @default.
- W2011725503 sameAs 2011725503 @default.
- W2011725503 citedByCount "19" @default.
- W2011725503 countsByYear W20117255032014 @default.
- W2011725503 countsByYear W20117255032015 @default.
- W2011725503 countsByYear W20117255032016 @default.
- W2011725503 countsByYear W20117255032017 @default.
- W2011725503 countsByYear W20117255032018 @default.
- W2011725503 countsByYear W20117255032019 @default.
- W2011725503 countsByYear W20117255032020 @default.
- W2011725503 countsByYear W20117255032021 @default.
- W2011725503 countsByYear W20117255032022 @default.
- W2011725503 countsByYear W20117255032023 @default.
- W2011725503 crossrefType "journal-article" @default.
- W2011725503 hasAuthorship W2011725503A5030128184 @default.
- W2011725503 hasAuthorship W2011725503A5039212509 @default.
- W2011725503 hasAuthorship W2011725503A5043886610 @default.
- W2011725503 hasAuthorship W2011725503A5046941513 @default.
- W2011725503 hasAuthorship W2011725503A5047986179 @default.
- W2011725503 hasAuthorship W2011725503A5066926559 @default.
- W2011725503 hasAuthorship W2011725503A5081194803 @default.
- W2011725503 hasBestOaLocation W20117255031 @default.
- W2011725503 hasConcept C112705442 @default.
- W2011725503 hasConcept C134018914 @default.
- W2011725503 hasConcept C179998833 @default.
- W2011725503 hasConcept C185592680 @default.
- W2011725503 hasConcept C202751555 @default.
- W2011725503 hasConcept C22979827 @default.
- W2011725503 hasConcept C2775922563 @default.
- W2011725503 hasConcept C2777752497 @default.
- W2011725503 hasConcept C2778500429 @default.
- W2011725503 hasConcept C2780113650 @default.
- W2011725503 hasConcept C43617362 @default.
- W2011725503 hasConcept C55493867 @default.
- W2011725503 hasConcept C71924100 @default.
- W2011725503 hasConcept C86745063 @default.
- W2011725503 hasConcept C87644729 @default.
- W2011725503 hasConcept C98274493 @default.
- W2011725503 hasConceptScore W2011725503C112705442 @default.
- W2011725503 hasConceptScore W2011725503C134018914 @default.
- W2011725503 hasConceptScore W2011725503C179998833 @default.
- W2011725503 hasConceptScore W2011725503C185592680 @default.
- W2011725503 hasConceptScore W2011725503C202751555 @default.
- W2011725503 hasConceptScore W2011725503C22979827 @default.
- W2011725503 hasConceptScore W2011725503C2775922563 @default.
- W2011725503 hasConceptScore W2011725503C2777752497 @default.
- W2011725503 hasConceptScore W2011725503C2778500429 @default.
- W2011725503 hasConceptScore W2011725503C2780113650 @default.
- W2011725503 hasConceptScore W2011725503C43617362 @default.
- W2011725503 hasConceptScore W2011725503C55493867 @default.
- W2011725503 hasConceptScore W2011725503C71924100 @default.
- W2011725503 hasConceptScore W2011725503C86745063 @default.
- W2011725503 hasConceptScore W2011725503C87644729 @default.
- W2011725503 hasConceptScore W2011725503C98274493 @default.
- W2011725503 hasIssue "2" @default.