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Anti-hyperlipidaemic effects of synthetic analogues of nordihydroguaiaretic acid in dyslipidaemic rats.

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  • معلومة اضافية
    • المصدر:
      Publisher: Wiley Country of Publication: England NLM ID: 7502536 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1476-5381 (Electronic) Linking ISSN: 00071188 NLM ISO Abbreviation: Br J Pharmacol Subsets: MEDLINE
    • بيانات النشر:
      Publication: London : Wiley
      Original Publication: London, Macmillian Journals Ltd.
    • الموضوع:
      Hyperlipidemias/*drug therapy ; Hypolipidemic Agents/*pharmacology ; Masoprocol/*pharmacology; Animals ; Hypolipidemic Agents/chemistry ; Male ; Masoprocol/analogs & derivatives ; Masoprocol/chemistry ; Molecular Docking Simulation ; Molecular Structure ; Rats ; Rats, Sprague-Dawley
    • نبذة مختصرة :
      Background and Purpose: Previous studies have shown that Creosote bush-derived nordihydroguaiaretic acid (NDGA) exerts beneficial actions on the key components of metabolic syndrome including dyslipidaemia, insulin resistance and hypertension in several relevant rodent models. Here, we synthesized and screened a total of 6 anti-hyperlipidaemic analogues of NDGA and tested their efficacy against hepatic lipid metabolism in a high-fructose diet (HFrD) fed dyslipidaemic rat model.
      Experimental Approach: HFrD fed Sprague-Dawley rats treated with NDGA or one of the six analogues were used. Serum samples were analysed for blood metabolites, whereas liver samples were quantified for changes in various mRNA levels by real-time RT-PCR.
      Key Results: Oral gavage of HFrD-fed rats for 4 days with NDGA analogues 1 and 2 (100 mg·kg -1 ·day -1 ) suppressed the hepatic triglyceride content, whereas the NDGA analogues 2, 3 and 4, like NDGA, decreased the plasma triglyceride levels by 70-75%. qRT-PCR measurements demonstrated that among NDGA analogues 1, 2, 4 and 5, analogue 4 was the most effective at inhibiting the mRNA levels of some key enzymes and transcription factors involved in lipogenesis. All four analogues almost equally inhibited the key genes involved in triglyceride synthesis and fatty acid elongation. Unlike NDGA, none of the analogues affected the genes of hepatic fatty acid oxidation or transport.
      Conclusions and Implications: Our data suggest that NDGA analogues 1, 2, 4 and 5, particularly analogue 4, exert their anti-hyperlipidaemic actions by negatively targeting genes of key enzymes and transcription factors involved in lipogenesis, triglyceride synthesis and fatty acid elongation. These analogues have therapeutic potential.
      (© 2018 The British Pharmacological Society.)
    • References:
      Br J Pharmacol. 2019 Feb;176(3):369-385. (PMID: 30374952)
      Semin Liver Dis. 2013 Nov;33(4):380-8. (PMID: 24222095)
      Metabolism. 2016 Aug;65(8):1183-95. (PMID: 27301803)
      Am J Physiol Endocrinol Metab. 2000 Sep;279(3):E593-600. (PMID: 10950827)
      Nucleic Acids Res. 2018 Jan 4;46(D1):D1091-D1106. (PMID: 29149325)
      J Biol Chem. 1957 May;226(1):497-509. (PMID: 13428781)
      J Biol Chem. 2007 Aug 3;282(31):22678-88. (PMID: 17526931)
      Am J Physiol Endocrinol Metab. 2009 Jun;296(6):E1195-209. (PMID: 19336658)
      J Med Chem. 2015 Sep 24;58(18):7173-85. (PMID: 26349027)
      J Biol Chem. 1991 Mar 5;266(7):4214-9. (PMID: 1999415)
      Nat Rev Endocrinol. 2011 May 10;7(8):456-65. (PMID: 21556019)
      Nat Rev Mol Cell Biol. 2015 Nov;16(11):678-89. (PMID: 26490400)
      Br J Pharmacol. 2017 Dec;174 Suppl 1:S208-S224. (PMID: 29055032)
      J Ethnopharmacol. 2005 Apr 26;98(3):231-9. (PMID: 15814253)
      Proc Natl Acad Sci U S A. 2002 Aug 20;99(17):11482-6. (PMID: 12177411)
      Obesity (Silver Spring). 2009 Oct;17(10):1872-7. (PMID: 19629053)
      Biochem J. 2013 Apr 1;451(1):1-12. (PMID: 23489367)
      Prog Lipid Res. 2009 Jan;48(1):1-26. (PMID: 18824034)
      PLoS One. 2015 Sep 22;10(9):e0138203. (PMID: 26394137)
      J Lipid Res. 2006 Sep;47(9):1928-39. (PMID: 16751624)
      Aging Cell. 2016 Oct;15(5):872-84. (PMID: 27312235)
      Arterioscler Thromb Vasc Biol. 2015 May;35(5):1080-91. (PMID: 25792450)
      Gastroenterology. 2008 Feb;134(2):424-31. (PMID: 18242210)
      Drug Discov Today. 2008 Apr;13(7-8):285-94. (PMID: 18405840)
      J Hepatol. 2015 Apr;62(1 Suppl):S47-64. (PMID: 25920090)
      Prog Lipid Res. 2012 Oct;51(4):350-77. (PMID: 22705711)
      Prog Lipid Res. 2006 May;45(3):237-49. (PMID: 16564093)
      Adv Drug Deliv Rev. 2001 Mar 1;46(1-3):3-26. (PMID: 11259830)
      Br J Pharmacol. 2017 Dec;174 Suppl 1:S272-S359. (PMID: 29055034)
      Metabolism. 2000 Sep;49(9):1106-10. (PMID: 11016888)
      J Gastroenterol. 2013 Apr;48(4):434-41. (PMID: 23397118)
      Am J Physiol Gastrointest Liver Physiol. 2013 Jan 1;304(1):G72-86. (PMID: 23104557)
      Br J Pharmacol. 2010 Aug;160(7):1577-9. (PMID: 20649561)
      J Comput Chem. 2010 Jan 30;31(2):455-61. (PMID: 19499576)
      Prog Lipid Res. 2010 Apr;49(2):186-99. (PMID: 20018209)
      Crit Rev Biochem Mol Biol. 2010 Jun;45(3):199-214. (PMID: 20218765)
      Diabetologia. 2006 Jan;49(1):141-8. (PMID: 16323001)
      Nat Rev Gastroenterol Hepatol. 2013 Jun;10(6):330-44. (PMID: 23507799)
      Semin Liver Dis. 2013 Nov;33(4):301-11. (PMID: 24222088)
      Nutr Metab (Lond). 2016 Sep 29;13:63. (PMID: 27708683)
      Gastroenterology. 2014 Mar;146(3):726-35. (PMID: 24316260)
      J Biol Chem. 2015 Aug 14;290(33):20023-31. (PMID: 26124277)
      J Clin Invest. 2002 May;109(9):1125-31. (PMID: 11994399)
      Annu Rev Pathol. 2016 May 23;11:451-96. (PMID: 26980160)
      Nat Struct Mol Biol. 2015 Jul;22(7):581-5. (PMID: 26098317)
      Metabolism. 1999 Apr;48(4):411-4. (PMID: 10206430)
      Am J Hypertens. 1999 Jul;12(7):744-6. (PMID: 10411373)
      Curr Opin Cardiol. 2012 Jul;27(4):420-8. (PMID: 22596186)
      Nat Rev Dis Primers. 2015 Dec 17;1:15080. (PMID: 27188459)
      Curr Opin Clin Nutr Metab Care. 2011 Mar;14(2):115-20. (PMID: 21178610)
      Med Sci Monit. 2010 May;16(5):RA93-100. (PMID: 20424564)
      Nat Rev Gastroenterol Hepatol. 2013 Nov;10(11):686-90. (PMID: 24042449)
      Environ Microbiol. 2001 Feb;3(2):81-91. (PMID: 11321547)
      Nat Rev Gastroenterol Hepatol. 2013 Nov;10(11):656-65. (PMID: 24080776)
      Lancet Diabetes Endocrinol. 2014 Nov;2(11):901-10. (PMID: 24731669)
      Mol Metab. 2014 Mar 06;3(4):354-71. (PMID: 24944896)
      J Biol Chem. 2006 Sep 29;281(39):28721-30. (PMID: 16885160)
      J Clin Invest. 2005 May;115(5):1343-51. (PMID: 15864352)
      Chem Rev. 2011 Oct 12;111(10):6359-86. (PMID: 21627334)
      Endocr Rev. 2002 Apr;23(2):201-29. (PMID: 11943743)
      J Lipid Res. 2008 Nov;49(11):2283-301. (PMID: 18757836)
      Am J Physiol. 1998 Feb;274(2):E321-7. (PMID: 9486165)
      Microbiol Mol Biol Rev. 2003 Sep;67(3):454-72, table of contents. (PMID: 12966144)
      Diabetes Metab. 2003 Nov;29(5):478-85. (PMID: 14631324)
      Annu Rev Nutr. 2014;34:281-303. (PMID: 24850384)
    • Grant Information:
      I01 BX000398 United States BX BLRD VA; I01 BX001923 United States BX BLRD VA; P30 DK116074 United States DK NIDDK NIH HHS; R01 HL092473 United States HL NHLBI NIH HHS
    • الرقم المعرف:
      0 (Hypolipidemic Agents)
      7BO8G1BYQU (Masoprocol)
    • الموضوع:
      Date Created: 20181031 Date Completed: 20200224 Latest Revision: 20210109
    • الموضوع:
      20250114
    • الرقم المعرف:
      PMC6329620
    • الرقم المعرف:
      10.1111/bph.14528
    • الرقم المعرف:
      30374952