2. Academic Validation
  3. PG490-88, a derivative of triptolide, blocks bleomycin-induced lung fibrosis

PG490-88, a derivative of triptolide, blocks bleomycin-induced lung fibrosis

  • Am J Pathol. 2001 Mar;158(3):997-1004. doi: 10.1016/S0002-9440(10)64046-1.
G Krishna 1,  K Liu,  H Shigemitsu,  M Gao,  T A Raffin,  G D Rosen
Affiliations

Affiliation

  • 1 Division of Pulmonary and Critical Care Medicine, Stanford University School of Medicine, 300 Pasteur Dr., Stanford, CA 94305-5236, USA.
PMID: 11238047 DOI: 10.1016/S0002-9440(10)64046-1
Abstract

In this study we evaluate the antifibrotic properties of PG-490-88, a water-soluble derivative of triptolide. Triptolide is an oxygenated diterpene that is derived from a traditional Chinese herb that has potent immunosuppressive and antitumor activity. We used the intratracheal bleomycin mouse model and found that PG490-88 inhibits fibrosis in the bleomycin group when given the same day or 5 days after bleomycin. PG490-88 also markedly reduced the number of myofibroblasts in the bleomycin treatment group. An enzyme-linked immunosorbent assay of transforming growth factor (TGF)-beta in the bronchoalveolar lavage fluid showed a significant decrease in TGF-beta in the PG490-88-treated groups compared to the bleomycin-treated group. Additionally, triptolide blocked bleomycin-induced increase in TGF-beta mRNA in cultured normal human lung fibroblasts. The efficacy of PG490-88 when administered late after bleomycin installation suggests a potential role in the treatment of idiopathic pulmonary fibrosis.

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