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NDT Advance Access originally published online on May 27, 2009
Nephrology Dialysis Transplantation 2009 24(10):3033-3041; doi:10.1093/ndt/gfp245
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© The Author [2009]. Published by Oxford University Press on behalf of ERA-EDTA. All rights reserved. For Permissions, please e-mail: journals.permissions@oxfordjournals.org



In vitro anti-fibrotic activities of herbal compounds and herbs

Qin Hu1,2, Mazhar Noor1, Yuen Fei Wong1, Peter J. Hylands3, Monique S. J. Simmonds4, Qing Xu5, Dan Jiang1,3, Bruce M. Hendry1 and Qihe Xu1

1 Department of Renal Medicine, King's College London, London, UK 2 Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences, Beijing, China 3 Department of Pharmacy, King's College London, London, UK 4 Royal Botanic Gardens, Kew, Richmond, Surrey, UK 5 Dalian Institute of Chemical Physics, Chinese Academy of Sciences, Dalian, China

Correspondence and offprint requests to: Qihe Xu; E-mail: qihe.xu{at}kcl.ac.uk



  Abstract

Background. We recently developed high-throughput assays of inflammation-independent anti-fibrotic activities based on TGF-β1-induced total collagen accumulation and nodule formation in normal rat kidney fibroblasts.

Methods. These assays were applied to examine the anti-fibrotic activities of 21 compounds isolated from plants used in Chinese medicine and methanol extracts of 12 Chinese herbs. Lactate dehydrogenase release assay and cell detachment index were used to monitor cytotoxicity. Changes in fibrogenic molecular markers were observed by reverse transcriptase quantitative polymerase chain reaction and high-content imaging analysis of immunofluorescence.

Results. Three flavonoids (quercetin, baicalein and baicalin) and two non-flavonoids (salvianolic acid B and emodin) demonstrated anti-fibrotic activities in both total collagen accumulation and nodule formation assays. The remaining 16 compounds had little anti-fibrotic effect or were cytotoxic. The anti-fibrotic compounds suppressed collagen I expression at both mRNA and protein levels and also variably suppressed {alpha}-smooth muscle actin expression and bromodeoxyuridine incorporation. Methanol extracts of Scutellaria baicalensis Georgi, Salvia miltiorrhiza Bunge and Rheum palmatum L., which are rich sources of baicalein, baicalin, salvianolic acid B and emodin, respectively, also showed in vitro anti-fibrotic activities.

Conclusions. Five herbal compounds and three herbal extracts have in vitro anti-fibrotic activities. These data warrant further studies on these anti-fibrotic entities and suggest it a promising strategy to discover new anti-fibrotic drugs by screening more plant materials.

Keywords: fibroblasts; herbal compounds; renal fibrosis; TGF-β1

Received for publication: 24.10.08
Accepted in revised form: 30. 4.09


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