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@ARTICLE{Falckenhayn:289032,
author = {C. Falckenhayn and A. Bienkowska and J. Söhle and K.
Wegner and G. Raddatz$^*$ and B. Kristof and D. Kuck and R.
Siegner and R. Kaufmann and J. Korn and S. Baumann and D.
Lange and A. Schepky and H. Völzke and L. Kaderali and M.
Winnefeld and F. Lyko$^*$ and E. Grönniger},
title = {{I}dentification of dihydromyricetin as a natural {DNA}
methylation inhibitor with rejuvenating activity in human
skin.},
journal = {Frontiers in aging},
volume = {4},
issn = {2673-6217},
address = {Lausanne},
publisher = {Frontiers Media S.A.},
reportid = {DKFZ-2024-00564},
pages = {1258184},
year = {2023},
note = {DKFZ-ZMBH Alliance},
abstract = {Changes in DNA methylation patterning have been reported to
be a key hallmark of aged human skin. The altered DNA
methylation patterns are correlated with deregulated gene
expression and impaired tissue functionality, leading to the
well-known skin aging phenotype. Searching for small
molecules, which correct the aged methylation pattern
therefore represents a novel and attractive strategy for the
identification of anti-aging compounds. DNMT1 maintains
epigenetic information by copying methylation patterns from
the parental (methylated) strand to the newly synthesized
strand after DNA replication. We hypothesized that a modest
inhibition of this process promotes the restoration of the
ground-state epigenetic pattern, thereby inducing
rejuvenating effects. In this study, we screened a library
of 1800 natural substances and 640 FDA-approved drugs and
identified the well-known antioxidant and anti-inflammatory
molecule dihydromyricetin (DHM) as an inhibitor of the DNA
methyltransferase DNMT1. DHM is the active ingredient of
several plants with medicinal use and showed robust
inhibition of DNMT1 in biochemical assays. We also analyzed
the effect of DHM in cultivated keratinocytes by array-based
methylation profiling and observed a moderate, but
significant global hypomethylation effect upon treatment. To
further characterize DHM-induced methylation changes, we
used published DNA methylation clocks and newly established
age predictors to demonstrate that the DHM-induced
methylation change is associated with a reduction in the
biological age of the cells. Further studies also revealed
re-activation of age-dependently hypermethylated and
silenced genes in vivo and a reduction in age-dependent
epidermal thinning in a 3-dimensional skin model. Our
findings thus establish DHM as an epigenetic inhibitor with
rejuvenating effects for aged human skin.},
keywords = {DNA methylation (Other) / DNAm age clock (Other) / DNMT1
inhibition (Other) / dihydromyricetin (Other) / rejuvenation
(Other) / skin (Other)},
cin = {A130},
ddc = {610},
cid = {I:(DE-He78)A130-20160331},
pnm = {311 - Zellbiologie und Tumorbiologie (POF4-311)},
pid = {G:(DE-HGF)POF4-311},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:38500495},
pmc = {pmc:PMC10944877},
doi = {10.3389/fragi.2023.1258184},
url = {https://inrepo02.dkfz.de/record/289032},
}