4th EucheMs chemistry congress

Poster Session 2
s1238
chem. Listy 106, s257–s1425 (2012)
Poster session 2 - Nanochemistry, Nanotechnology
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orGAniC nAnotuBeS for druG LoAdinG And
CeLLuLAr deLivery
y. MAitAni 1 , A. wAKASuGi 1 , M. ASAKAwA 2 ,
M. KoGiSo 2 , t. ShiMizu 2
1 Hoshi University, Medicinal Chemistry, Tokyo, Japan
2 National Institute of Advanced Industrial Science and
Technology, Nanotube Research Center, Tsukuba, Japan
Background: Organic nanotubes made of synthetic
amphiphilic molecules are novel materials that form by selfassembly.
objectives: Organic nanotubes were expected to apply a
drug carrier in drug delivery system.
Methods: Organic nanotubes with a carboxyl group (ONTs)
at the surface were used as a carrier for the anticancer drug
doxorubicin, which has a weak amine group. Drug loading into
ONT and cellular delivery of them was investigated, using
cytotoxicity and transmission electron microscope.
results: The IC(50) values of ONT for cells were higher
than that of conventional liposomes, suggesting that ONTs are
safe. The results showed that the drug loading of ONTs was
susceptible to the effect of ionic strength and H(+) concentration
in the medium, and drug release from ONTs was promoted at
lower pH, which is favorable for the release of drugs in the
endosome after cellular uptake. ONTs loaded with the drug were
internalized, and the drug was released quickly in the cells, as
demonstrated on transmission electron microscopy images of
ONTs and the detection of a 0.05% dose of ONT chelating
gadolinium in the cells. Moreover, ONT could be modified
chemically with folate by simply mixing with a folate-conjugate
lipid.
Conclusion: These novel, biodegradable organic nanotubes
have the potential to be used as drug carriers for controlled and
targeting drug delivery.
Keywords: nanotube; cellular uptake; drug load; doxorubicin;
4 th EucheMs chemistry congress
P - 0 7 5 2
dnA-nAnoCuBeS hyBridS for BioMoLeCuLAr
reCoGnition
C. MArtini 1 , C. AiMe 1 , t. CorAdin 1
1 University Pierre and Marie Curie, Laboratoire de Chimie de
la Matiere Condensée, Paris, France
Biomolecules recognition is a very important area of
research for medical diagnostic improvement. Among existing
methods, the specific disassembling of network based on
“aptamer” – DNA interactions appears to be one of the most
promising strategy. Aptamers are oligonucleic acids or peptides
selected through repeated rounds of in vitro selection (SELEX:
systematic evolution of ligands by exponential enrichment) to
bind strongly to various molecular targets such as proteins, nucleic
acids and even whole cells. Combined with a complementary
sequence, oligonucleotide aptamers are able to assemble owing
to Watson-Crick DNA base pairing. The obtained double strands
disassemble as the target molecule is introduced, aptamer-target
interactions being higher than that of aptamer-complementary
sequence. While aptamers are bonded to nanoparticles,
self-assembled networks of nanoobjects can be obtained. Their
disassembling in the presence of the target molecule can strongly
disturb the physical properties such as plasmonic or magnetism,
depending on the chemical nature and the organization of
nanoparticles. Such physical disturbing can be easily exploited
for biomolecular detection. In this context, we develop
nanohybrids composed of DNA associated with platinum,
iron-platinum or iron oxide nanocubes. Since they own planar
faces, nanocubes represent unique shapes for self-assembly. The
poster will present all aspects of this work: the chemical synthesis
of nanocubes, the ligands exchange to confer water solubility and
to further introduce specific functions, and the peptidic coupling
between DNA and functionalized nanocubes.
AUGUst 26–30, 2012, PrAGUE, cZEcH rEPUbLIc