In vitro: Miquelianin shows an antioxidant effect in human plasma. At 50 μM, miquelianin suppresses the consumption of the three antioxidants lycopene, β-carotene and α-tocopherol significantly. In vitro studies indicate that miquelianin is able to reach the central nervous system from the small intestine. Miquelianin significantly reduces the generation of β-amyloid (Aβ) peptides by primary neuron cultures generated from the Tg2576 AD mouse model. It is also capable of interfering with the initial protein-protein interaction of Aβ1–40 and Aβ1–42 that is necessary for the formation of neurotoxic oligomeric Aβ species. Treatment with 0.1 μM miquelianin suppresses ROS generation, cAMP and RAS activation, phosphorylation of ERK1/2 and the expression of HMOX1, MMP2, and MMP9 genes. Miquelianin suppresses invasion of MDA-MB-231 breast cancer cells and MMP-9 induction, and inhibits the binding of [3H]-NA to b2-AR. Miquelianin may function to suppress invasion of breast cancer cells by controlling b2-adrenergic signaling, and may be a dietary chemopreventive factor for stress-related breast cancer. In vivo: Miquelianin treatment, compared to vehicle-control treatment, significantly improves AD-type deficits in hippocampal formation basal synaptic transmission and long-term potentiation. A flavonoid fraction obtained from a crude extract of Hypericum perforatum (St. John's wort) is remarkably active in the forced swimming test. Miquelianin is one of the compound separated from the fraction.
|Cell lines||14–16 corticohippocampal neuronal|
|Preparation method||Freshly isolated low-molecular-weight Aβ1–42 (25 μM) or Aβ1–40 (25 μM) peptide (18 μl) was mixed with 1 μl of 1 mm tris-(2,2′-bipyridyl)dichlororuthenium(II) [Ru(Bpy)] and 1 μl of 20 mM ammonium persulfate in the presence or absence of 25 μM quercetin-3-O-glucuronide in 10 mM phosphate.|
|Animal models||Tg2576 mice|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||30 mg/mL in DMSO|
Quercetin-3-O-β-D-glucuronide isolated from Polygonum aviculare inhibits cellular senescence in human primary cells.
Yang HH, et al. Arch Pharm Res. 2014;37(9):1219-33. PMID: 24638927.
Identification of brain-targeted bioactive dietary quercetin-3-O-glucuronide as a novel intervention for Alzheimer's disease.
Ho L, et al. FASEB J. 2013 Feb;27(2):769-81. PMID: 23097297.
Ceforanide is a new cephalosporin with antibacterial activity and has a longer elimination half-life than any currently available cephalosporin.
Inositol Nicotinate is a formulation of niacin, which is also called vitamin B3, an essential human nutrient.
ND-630 is an ACC inhibitor of human ACC1 and ACC2 with IC50 values of 2.1 and 6.1 nM, respectively.
|D-Luciferin potassium salt
D-Luciferin potassium salt is the substrate of luciferases that catalyze the production of light in bioluminescent insects.
|ZD 7114 hydrochloride
ZD 7114 is a selective β3 adrenergic receptor agonist.
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