Immunostimulatory lipid nanoparticles from herbal medicine

Tal H. Hasson, Anna Takaoka, Roberto De La Rica, Hiroshi Matsui, Gabriela Smeureanu, Charles Michael Drain, Akira Kawamura

Research output: Contribution to journalLetterpeer-review

1 Citation (Scopus)


Reproducibility is an important issue in biological characterization of drug candidates and natural products. It is not uncommon to encounter cases in which supposedly the same sample exhibits very different biological activities. During our characterization of macrophage-stimulatory lipids from herbal medicine, it was found that the potency of these lipids could vary substantially from experiment to experiment. Further analysis of this reproducibility issue led to the discovery of solvent-dependent nanoparticle formation by these lipids. While larger nanoparticles (approximately 100 nm) of these lipids showed modest macrophage-stimulatory activity, smaller nanoparticles (<10 nm) of the same lipids exhibited substantially higher potency. Thus, the study revealed an unexpected link between nanoparticle formation and macrophage-stimulatory activity of plant lipids. Although nanoparticles have been extensively studied in the context of vehicles for drug delivery, our finding indicates that drugs themselves can form nanoassemblies, and their biological properties may be altered by the way they assemble.
Original languageEnglish
Pages (from-to)493–497
Number of pages5
JournalChemical Biology and Drug Design
Issue number4
Early online date5 Feb 2014
Publication statusPublished - Apr 2014


  • atomic force microscopy
  • dynamic light scattering
  • Juzen-taiho-to
  • macrophages
  • nanoparticles
  • β-sitosteryl β-d-glucoside


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