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Avasimibe encapsulated in human serum albumin blocks cholesterol esterification for selective cancer treatment

Steve Seung-Young Lee1, Junjie Li1, Jien Nee Tai1

  • 1†Weldon School of Biomedical Engineering, ‡Department of Biological Sciences, §Department of Chemistry, ⊥Center for Cancer Research, ∥Department of Comparative Pathobiology, #Department of Industrial and Physical Pharmacy, Purdue University, West Lafayette, Indiana 47907, United States.

ACS Nano
|February 10, 2015
PubMed

Insights

Targeting cholesterol metabolism with avasimin (avasimin) offers a novel cancer chemotherapy strategy. This approach selectively induces cancer cell death and suppresses tumor growth without harming healthy tissues.

Area of Science:

  • Oncology
  • Biochemistry
  • Nanotechnology

Background:

  • Cancer chemotherapy often causes undesirable side effects.
  • Altered cholesterol metabolism is a hallmark of cancer cells.
  • Acyl-CoA:cholesterol acyltransferase-1 (ACAT-1) plays a role in cancer cell cholesterol homeostasis.

Purpose of the Study:

  • To develop a cancer-selective chemotherapy strategy by inhibiting ACAT-1.
  • To create a nanoformulation of avasimibe for targeted delivery to tumors.

Main Methods:

  • Developed a nanoformulation of avasimibe (avasimin) for systemic injection.
  • Tested avasimin in human cancer cell lines (prostate, pancreatic, lung, colon).
  • Evaluated avasimin efficacy and safety in prostate and colon cancer xenograft mouse models.

Main Results:

  • Avasimin reduced cholesteryl ester storage and increased free cholesterol in cancer cells, inducing apoptosis and inhibiting proliferation.
  • Intravenous avasimin administration achieved high drug concentrations in tumors.
  • Avasimin suppressed tumor growth and extended survival time in mice.
  • No adverse effects were observed in normal cells or organs.

Conclusions:

  • Targeting ACAT-1-mediated cholesterol esterification is a viable strategy for selective cancer chemotherapy.
  • Avasimin nanoformulation demonstrates potent anti-cancer effects with minimal toxicity.
  • This approach offers a promising new avenue for cancer treatment by exploiting cancer cell metabolic vulnerabilities.
Keywords:
ACAT-1 inhibitoravasimibecancercholesterolcholesteryl esterhuman serum albumin

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