| Cell Research: |
| Yao Xue Xue Bao. 1993;28(10):728-31. | | Effects of praeruptorin-C on cytosolic free calcium in cultured rat heart cells[Pubmed: 7516604] | The negative inotropic effect of Praeruptorin C(Pra-C) was supposed to be related to the blocking of extracellular calcium influx but direct evidence is not known.
METHODS AND RESULTS:
We, therefore, examined the effects of Pra-C on [Ca2+]i in isolated rat ventricular myocytes using the fluorescent Ca(2+)-indicator Fura-2/AM. It was found that Pra-C inhibited the elevation of [Ca2+]i induced by potassium-depolarization, high extracellular calcium and calcium agonist Bay K 8644 in a dose-dependent manner. At 1.0 mumol.L-1, it decreased the [Ca2+]i at the presence of 75 mmol.L-1 KCl, 10 mol.L-1 CaCl and 3 mumol.L-1 Bay K 8644 by 50, 31 and 42% respectively. No significant effect on ouabain evoked [Ca2+]i increase was found, showing that it does not affect sarcolemmal Na(+)-Ca2+ exchange.
CONCLUSIONS:
These results further indicate that Pra-C may decrease the [Ca2+]i of myocyte by blocking voltage-dependent calcium channels. | | Evid Based Complement Alternat Med. 2013;2013:156574. | | PXR-Mediated Upregulation of CYP3A Expression by Herb Compound Praeruptorin C from Peucedanum praeruptorum Dunn.[Pubmed: 24379885] | We recently reported that Praeruptorin C effectively transactivated the mRNA, protein expression, and catalytic activity of CYP3A4 via the CAR-mediated pathway, but whether and how PC could affect the expression and catalytic activity of CYP3A4 via PXR pathway remains unknown.
METHODS AND RESULTS:
Therefore, in this study, the effect of PC on the CYP3A gene expression was investigated in mice primary hepatocytes after knockdown of PXR by transient transfection of PXR siRNA, and the gene expression, protein expression, and catalytic activity of CYP3A4 in the LS174T cells with PXR overexpression were determined by real-time PCR, western blot analysis, and LC-MS/MS-based CYP3A4 substrate assay, respectively. We found that the level of CYP3a11 gene expression in mouse primary hepatocytes was significantly increased by Praeruptorin C, but such an induction was suppressed after knockdown of pregnane X receptor by its siRNA. In PXR-overexpressed LS174T cells, PC significantly enhanced CYP3A4 mRNA, protein expression, and functional activity through PXR-mediated pathway; conversely, no such increase was found in the untransfected cells.
CONCLUSIONS:
These findings suggest that PC can significantly upregulate CYP3A level via the PXR-mediated pathway, and this should be taken into consideration to predict any potential herb-drug interactions between PC, Qianhu, and the other coadministered drugs. |
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