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1.
SAR QSAR Environ Res ; 35(5): 391-410, 2024 May.
Artículo en Inglés | MEDLINE | ID: mdl-38769919

RESUMEN

Alpinia officinarum is a commonly used spice with proven folk uses in various traditional medicines. In the current study, six compounds were isolated from its rhizomes, compounds 1-3 were identified as diarylheptanoids, while 4-6 were identified as flavonoids and phenolic acids. The isolated compounds were subjected to virtual screening against α-glucosidase, butyrylcholinesterase (BChE), and acetylcholinesterase (AChE) enzymes to evaluate their potential antidiabetic and anti-Alzheimer's activities. Molecular docking and dynamics studies revealed that 3 exhibited a strong binding affinity to human a α- glucosidase crystal structure compared to acarbose. Furthermore, 2 and 5 demonstrated high potency against AChE. The virtual screening results were further supported by in vitro assays, which assessed the compounds' effects on α-glucosidase, cholinesterases, and their antioxidant activities. 5-Hydroxy-7-(4-hydroxy-3-methoxyphenyl)-1-phenylheptan-3-one (2) showed potent antioxidant effect in both ABTs and ORAC assays, while p-hydroxy cinnamic acid (6) was the most potent in the ORAC assay. In contrary, kaempferide (4) and galangin (5) showed the most potent effect in metal chelation assay. 5-Hydroxy-1,7-diphenylhepta-4,6-dien-3-one (3) and 6 revealed the most potent effect as α-glucosidase inhibitors where compound 3 showed more potent effect compared to acarbose. Galangin (5) revealed a higher selectivity to BChE, while 2 showed the most potent activity to (AChE).


Asunto(s)
Acetilcolinesterasa , Alpinia , Antioxidantes , Butirilcolinesterasa , Inhibidores de la Colinesterasa , Inhibidores de Glicósido Hidrolasas , Simulación del Acoplamiento Molecular , Rizoma , Alpinia/química , Inhibidores de la Colinesterasa/farmacología , Inhibidores de la Colinesterasa/química , Inhibidores de la Colinesterasa/aislamiento & purificación , Inhibidores de Glicósido Hidrolasas/farmacología , Inhibidores de Glicósido Hidrolasas/química , Inhibidores de Glicósido Hidrolasas/aislamiento & purificación , Antioxidantes/farmacología , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Rizoma/química , Butirilcolinesterasa/metabolismo , Acetilcolinesterasa/metabolismo , alfa-Glucosidasas/metabolismo , Relación Estructura-Actividad Cuantitativa , Flavonoides/química , Flavonoides/farmacología , Flavonoides/aislamiento & purificación , Hidroxibenzoatos/farmacología , Hidroxibenzoatos/química , Hidroxibenzoatos/aislamiento & purificación , Humanos
2.
Opt Express ; 26(6): 7313-7323, 2018 Mar 19.
Artículo en Inglés | MEDLINE | ID: mdl-29609288

RESUMEN

Mechanically robust and low loss single-mode arsenic sulfide fibers are used to deliver high power mid-infrared sources. Anti-reflection coatings were deposited on the fiber facets, enabling 90% transmission through 20 cm length fibers. 10.3 W was transmitted through an anti-reflection coated fiber at 2053 nm, and uncoated fibers sustained 12 MW/cm2 intensities on the facet without failure. A Cr:ZnSe laser transmitted >1 W at 2520 nm, and a Fe:ZnSe laser transmitted 0.5 W at 4102 nm. These results indicate that by improving the anti-reflection coatings and using a high beam quality mid-infrared source, chalcogenide fibers can reliably deliver ≥10 W in a single mode, potentially out to 6.5 µm.

3.
Phytother Res ; 30(5): 768-73, 2016 May.
Artículo en Inglés | MEDLINE | ID: mdl-27145225

RESUMEN

Luteolin-7-O-glycoside (LG), an abundant component in many edible plants, was found to be one of the major constituents of the aqueous methanol extract of Trifolium alexandrinum L. family Fabaceae, a fodder plant widely cultivated in Egypt. The estrogenic activity of LG concerning the effect on uterotrophy, lipid profile, weight gain and bone enhancement activity was determined in ovariectomized rat model at a dose of 5 mg/kg. Luteolin-7-O-glycoside showed significant estrogenic effect through the preservation of normal uterine weight and plasma estradiol level. It also significantly inhibited the bone turnover markers plasma bone-specific alkaline phosphatase, plasma osteocalsin, type I procollagen N-terminal, and C-telopeptide of type II collagen levels. It induced a significant improvement in plasma lipid profile. The effect of LG was comparable with estradiol with lower effect on uterine weight. Liver and kidney functions revealed a wide safety of LG at this dose level. The present study revealed that LG may be a promising hormone replacement therapy after being examined thoroughly on human. Copyright © 2016 John Wiley & Sons, Ltd.


Asunto(s)
Flavonas/química , Glucósidos/química , Lípidos/química , Extractos Vegetales/química , Trifolium/química , Animales , Estrógenos/farmacología , Femenino , Humanos , Extractos Vegetales/farmacología , Ratas
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