Immunostimulatory lipid nanoparticles from herbal medicine.
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.
Department of Chemistry, Hunter College of CUNY, New York, NY, 10065, USA.
Tal H
TH
Hasson
Anna
A
Takaoka
Roberto
R
de la Rica
Hiroshi
H
Matsui
Gabriela
G
Smeureanu
Charles M
CM
Drain
Akira
A
Kawamura
D000276:Adjuvants, Immunologic / Q000494:pharmacology*; D000818:Animals; D001688:Biological Products / Q000737:chemistry*; D002478:Cells, Cultured; D029001:Herbal Medicine; D006801:Humans; D008055:Lipids / Q000737:chemistry* / Q000494:pharmacology*; D008264:Macrophages / Q000187:drug effects*; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D015203:Reproducibility of Results
D000276:Adjuvants, Immunologic; D001688:Biological Products; D008055:Lipids
Juzen-taiho-to; atomic force microscopy; dynamic light scattering; macrophages; nanoparticles; β-sitosteryl β-d-glucoside