Screening active components in compound danshen based on PXR-CYP3A4: an experimental study / 中国中西医结合杂志
Chinese Journal of Integrated Traditional and Western Medicine
; (12): 606-610, 2014.
Article
in Zh
| WPRIM
| ID: wpr-312768
Responsible library:
WPRO
ABSTRACT
<p><b>OBJECTIVE</b>To screen active components in Compound Danshen (CD) based on pregnane X receptor-cytochrome P450 3A4 (PXR-CYP3A4).</p><p><b>METHODS</b>By using PXR-CYP3A stable transfection human hepatoblastoma G2 (HepG2) cell lines engineering cell strain combined reporter genes technology, active components that induce or inhibit PXR-CYP3A4 paths in CD were screened, and confirmed at the level of enzymic activities. The experiment was divided into the positive control group (RIF 10 micro mol/L), the DMSO group (DMSO 0.1%), each dose of treatment groups (ginsenoside Rc, Rf, Rb2, Rg2, F2, F1, tanshinone I , isoborneol 5, 10, 25, 50, 100, and 200 micro mol/L; each with six duplicates). Cells medium was removed 36, 48, and 60 h after treatment. The activity of CYP3A4 was then determined in the supernant and the fold induction was calculated.</p><p><b>RESULTS</b>Compared with the DMSO group, the fold induction increased when ginsenoside Rc, Rf, Rb2, Rg2, F2, F1, tanshinone I , and isoborneol 50 and 100 micro mol/L was respectively intervened for 36, 48, and 60 h (P <0.05). When cells were treated with isoborneol 200 micro mol/L for 48 and 60 h,the fold induction of ginsenoside Rb2, Rg2, and F1 was significantly higher than that of the RIF group (P <0.05). Enzymic activity results showed that ginsenoside Rc, Rf, Rb2, F2, and F1 could increase the enzyme activity of CYP3A4 at 48 h (P <0.05).</p><p><b>CONCLUSION</b>Ginsenoside Rc, Rf, Rb2, F2, F1, tanshinone I, and isoborneol in DC could induce CYP3A4 enzymes.</p>
Full text:
1
Index:
WPRIM
Main subject:
Drugs, Chinese Herbal
/
Transfection
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Receptors, Steroid
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Chemistry
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Genes, Reporter
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Salvia miltiorrhiza
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Ginsenosides
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Abietanes
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Cytochrome P-450 CYP3A
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Hep G2 Cells
Type of study:
Diagnostic_studies
/
Screening_studies
Limits:
Humans
Language:
Zh
Journal:
Chinese Journal of Integrated Traditional and Western Medicine
Year:
2014
Type:
Article