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2017 ; 95
(4
): 417-429
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The HIF-1 antagonist acriflavine: visualization in retina and suppression of
ocular neovascularization
#MMPMID28004126
Zeng M
; Shen J
; Liu Y
; Lu LY
; Ding K
; Fortmann SD
; Khan M
; Wang J
; Hackett SF
; Semenza GL
; Campochiaro PA
J Mol Med (Berl)
2017[Apr]; 95
(4
): 417-429
PMID28004126
show ga
Acriflavine, a fluorescent drug previously used for bacterial and trypanosomal
infections, reduces hypoxia-inducible factor-1 (HIF-1) and HIF-2 transcriptional
activity. In mice with oxygen-induced ischemic retinopathy, intraocular or
intraperitoneal injections of acriflavine caused dose-dependent suppression of
retinal neovascularization (NV) and significantly reduced expression of
HIF-1-responsive genes. Intraocular injection of 100 ng caused inner retina
fluorescence within 1 h that was seen throughout the entire retina between 1 and
5 days, and at 7 days after injection, strongly suppressed choroidal NV at
Bruch's membrane rupture sites. After suprachoroidal injection of 300 ng in rats,
there was retinal fluorescence in the quadrant of the injection at 1 h that
spread throughout the entire retina and choroid by 1 day, was detectable for
5 days, and dramatically reduced choroidal NV 14 days after rupture of Bruch's
membrane. After topical administration of acriflavine in mice, fluorescence was
seen in the retina and retinal pigmented epithelium within 5 min and was
detectable for 6-12 h. Administration of 0.5% drops to the cornea twice a day
significantly reduced choroidal NV in mice. Electroretinographic b-wave
amplitudes were normal 7 days after intravitreous injection of 100 ng of
acriflavine in mice, showed mild threshold reductions at highest stimulus
intensities after injection of 250 ng, and more extensive changes after injection
of 500 ng. These data provide additional evidence for an important role for HIF-1
in retinal and choroidal NV and suggest that acriflavine can target HIF-1 through
a variety of modes of administration and has good potential to provide a novel
therapy for retinal and choroidal vascular diseases. KEY MESSAGE: Acriflavine, an
inhibitor of HIF-1, suppresses retinal and choroidal neovascularization. HIF-1
plays a critical role in ocular neovascularization. Acriflavine's fluorescence
provides a mean to track its entry and exit from the retina. Acriflavine has
therapeutic potential for the treatment of ocular neovascularization.
|Acriflavine/administration & dosage/pharmacokinetics/*therapeutic use
[MESH]
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