Telmisartan plus propranolol improves liver fibrosis and bile duct proliferation in the PSC-like Abcb4-/- mouse model

Dig Dis Sci. 2013 May;58(5):1271-81. doi: 10.1007/s10620-012-2499-3. Epub 2012 Dec 18.

Abstract

Background: Primary sclerosing cholangitis (PSC) is a chronic cholestatic liver disease leading to cirrhosis and cholangiocellular carcinoma. Inhibitors of the renin-angiotensin system or the sympathetic nervous system delay liver fibrogenesis in animal models.

Aims: We investigated the antifibrotic potential of telmisartan, an angiotensin II type 1 receptor antagonist, and the β-adrenoceptor blocker propranolol in the PSC-like Abcb4 knockout mouse model.

Methods: Sixty-five Abcb4 (-/-) mice were treated with telmisartan for 3 or 5 months (T) and with telmisartan plus propranolol for 3, 5, or 8 months (TP), or for 2 or 5 months starting with a delay of 3 months (TP delayed). Liver hydroxyproline content, inflammation, fibrosis, and bile duct proliferation were assessed; fibrosis-related molecules were analyzed by real-time polymerase chain reaction and Western blotting.

Results: Compared to controls, telmisartan monotherapy had no significant influence on hydroxyproline; however, telmisartan plus propranolol reduced hydroxyproline (TP 3 months, p = 0.008), fibrosis score (TP 3 months and TP 8 months, p = 0.043 and p = 0.008, respectively; TP delayed 8 months, p < 0.0005), bile duct proliferation (TP 8 months and TP delayed 8 months, p = 0.006 and p < 0.0005, respectively), and procollagen α1(I), endothelin-1, TIMP-1 and MMP3 mRNA as well as α-SMA, CK-19, and TIMP-1 protein.

Conclusions: Telmisartan plus propranolol reduces liver fibrosis and bile duct proliferation in the PSC-like Abcb4 (-/-) mouse model, even when started at late stages of fibrosis, and may thus represent a novel therapeutic option for cholestatic liver diseases such as PSC.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • ATP Binding Cassette Transporter, Subfamily B / genetics
  • ATP-Binding Cassette Sub-Family B Member 4
  • Adrenergic beta-Antagonists / pharmacology
  • Adrenergic beta-Antagonists / therapeutic use*
  • Animals
  • Benzimidazoles / pharmacology
  • Benzimidazoles / therapeutic use*
  • Benzoates / pharmacology
  • Benzoates / therapeutic use*
  • Bile Ducts / drug effects
  • Bile Ducts / pathology
  • Cholangitis, Sclerosing / drug therapy*
  • Cholangitis, Sclerosing / metabolism
  • Collagen Type I / metabolism
  • Collagen Type I, alpha 1 Chain
  • Cytokines / metabolism
  • Disease Models, Animal
  • Drug Evaluation, Preclinical
  • Drug Therapy, Combination
  • Liver / drug effects
  • Liver / pathology
  • Mice
  • Mice, Inbred BALB C
  • Mice, Knockout
  • Myofibroblasts / metabolism
  • Propranolol / pharmacology
  • Propranolol / therapeutic use*
  • RNA, Messenger / metabolism
  • Receptor, Angiotensin, Type 1 / therapeutic use*
  • Telmisartan

Substances

  • ATP Binding Cassette Transporter, Subfamily B
  • Adrenergic beta-Antagonists
  • Benzimidazoles
  • Benzoates
  • Collagen Type I
  • Collagen Type I, alpha 1 Chain
  • Cytokines
  • RNA, Messenger
  • Receptor, Angiotensin, Type 1
  • Propranolol
  • Telmisartan