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1.
Int J Mol Sci ; 24(21)2023 Oct 25.
Article in English | MEDLINE | ID: mdl-37958552

ABSTRACT

Women are at a higher risk of cognitive impairments and Alzheimer's disease (AD), particularly after the menopause, when the estrous cycle becomes irregular and diminishes. Numerous studies have shown that estrogen deficiency, especially estradiol (E2) deficiency, plays a key role in this phenomenon. Recently, a novel polymeric drug, hyaluronic acid-17ß-estradiol conjugate (HA-E2), has been introduced for the delivery of E2 to brain tissues. Studies have indicated that HA-E2 crosses the blood-brain barrier (BBB) and facilitates a prolonged E2 release profile while lowering the risk of estrogen-supplement-related side effects. In this study, we used ovariohysterectomy (OHE) rats, a postmenopausal cognitive deficit model, to explore the effect of a 2-week HA-E2 treatment (210 ng/kg body weight, twice a week) on the cholinergic septo-hippocampal innervation system, synaptic transmission in hippocampal pyramidal neurons and cognitive improvements. Our study revealed an 11% rise in choline acetyltransferase (ChAT) expression in both the medial septal nucleus (MS nucleus) and the hippocampus, along with a 14-18% increase in dendritic spine density in hippocampal pyramidal neurons, following HA-E2 treatment in OHE rats. These enhancements prompted the recovery of cognitive functions such as spatial learning and memory. These findings suggest that HA-E2 may prevent and improve estrogen-deficiency-induced cognitive impairment and AD.


Subject(s)
Alzheimer Disease , Cognitive Dysfunction , Humans , Rats , Female , Animals , Hyaluronic Acid/pharmacology , Estradiol/pharmacology , Estradiol/metabolism , Estrogens/pharmacology , Cognitive Dysfunction/drug therapy , Cognitive Dysfunction/etiology , Cognition
2.
Chem Pharm Bull (Tokyo) ; 56(6): 851-3, 2008 Jun.
Article in English | MEDLINE | ID: mdl-18520094

ABSTRACT

Two major acylated flavonoid tetraglycosides were isolated from the methanol extract of oolong tea. Their structures were elucidated by spectroscopic methods as quercetin 3-O-[2(G)-(E)-coumaroyl-3(G)-O-beta-D-glucosyl-3(R)-O-beta-D-glucosylrutinoside] (1) and kaempferol 3-O-[2(G)-(E)-coumaroyl-3(G)-O-beta-D-glucosyl-3(R)-O-beta-D-glucosylrutinoside] (2). Compounds 1 and 2 exhibited scavenging activity against DPPH radical with EC(50) values of 30.5 and 487.2 microM, respectively.


Subject(s)
Camellia/chemistry , Flavonoids/chemistry , Free Radical Scavengers/chemistry , Glucosides/chemistry , Kaempferols/chemistry , Picrates/chemistry , Quercetin/analogs & derivatives , Acylation , Biphenyl Compounds , Carbohydrate Conformation , Flavonoids/isolation & purification , Glucosides/isolation & purification , Glycosides/chemistry , Glycosides/isolation & purification , Hydrolysis , Kaempferols/isolation & purification , Magnetic Resonance Spectroscopy , Quercetin/chemistry , Quercetin/isolation & purification , Saponins/chemistry , Spectrophotometry, Infrared , Spectrophotometry, Ultraviolet
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