Traversal of the Blood–Brain Barrier by Cleavable l‑Lysine Conjugates of Apigenin
Version 2 2018-07-20, 18:24
Version 1 2018-07-20, 18:23
Posted on 2018-07-20 - 18:24
Apigenin,
a flavone abundant in parsley and celery, is known to
act on several CNS receptors, but its very poor water solubility (<0.001
mg/mL) impedes its absorption in vivo and prevents clinical use. Herein,
apigenin was directly conjugated with glycine, l-phenylalanine,
and l-lysine to give the corresponding carbamate derivatives,
all of which were much more soluble than apigenin itself (0.017, 0.018,
and 0.13 mg/mL, respectively). The Lys-apigenin carbamate 10 had a temporary sedative effect on the mice within 5 min of intraperitoneal
administration (single dose of 0.4 mg/g) and could be detected in
the mice brain tissues at a concentration of 0.82 μg/g of intact
Lys-apigenin carbamate 10 and 0.42 ug/g of apigenin at
1.5 h. This study accomplished the delivery of apigenin across the
BBB in a manner that might be applicable to other congeners, which
should inform the future development of BBB-crossing flavonoids.
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Wong, Tsung-Yun; Tsai, Ming-Shian; Hsu, Lih-Ching; Lin, Shu-Wha; Liang, Pi-Hui (2018). Traversal of the Blood–Brain Barrier by Cleavable l‑Lysine Conjugates of Apigenin. ACS Publications. Collection. https://doi.org/10.1021/acs.jafc.8b01187
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AUTHORS (5)
TW
Tsung-Yun Wong
MT
Ming-Shian Tsai
LH
Lih-Ching Hsu
SL
Shu-Wha Lin
PL
Pi-Hui Liang