HE 3286 is a synthetic derivative of a natural anti-inflammatory steroid, β-AET. HE 3286 is an orally active partial Attenuated NF-κB phosphorylation.
Blocked the activation of IKK, JNK, p38, and ERK partially.
HE 3286 (25-50 mg/kg; oral gavage; daily for 22-49 days) reduces joint inflammation, synovial proliferation, and erosion of DBA/1 Lac male collagen-induced arthritis mice [1].
HE 3286 (40 mg/kg; intraperitoneal injection; daily for 40 days) suppresses inflammation, reduces demyelination and axonal loss, and promotes RGC survival during experimental optic neuritis of experimental autoimmune encephalomyelitis mice[2].
HE 3286 (80 mg/kg; 0-24h) freely penetrates the BBB in male CD-1 mice[4].
HE 3286 (40 mg/kg; gavage; twice-daily for 4 days) increases the numbers of tyrosine droxylase-positive cells and decreases the numbers of damaged neurons in Parkinson's disease mice[4].
[1]. Auci D, et al. A new orally bioavailable synthetic androstene inhibits collagen-induced arthritis in the mouse: androstene hormones as regulators of regulatory T cells. Ann N Y Acad Sci. 2007;1110:630-640.
[2]. Khan RS, et al. HE3286 reduces axonal loss and preserves retinal ganglion cell function in experimental optic neuritis. Invest Ophthalmol Vis Sci. 2014;55(9):5744-5751. Published 2014 Aug 19.
[3]. Lu M,et al. A new antidiabetic compound attenuates inflammation and insulin resistance in Zucker diabetic fatty rats. Am J Psiol Endocrinol Metab. 2010;298(5):E1036-E1048.
[4]. Nicoletti F, et al. 17α-Etnyl-androst-5-ene-3β,7β,17β-triol (HE3286) Is Neuroprotective and Reduces Motor Impairment and Neuroinflammation in a Murine MPTP Model of Parkinson's Disease. Parkinsons Dis. 2012;2012:969418.