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1.
J Enzyme Inhib Med Chem ; 38(1): 2224944, 2023 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-37369580

RESUMEN

Callistemon is an aromatic genus of flowering plants belonging to family Myrtaceae. The essential oils of C. subulatus leaves were collected in four seasons and analyzed using GC/MS. The oils demonstrated monoterpenes as the predominant class. Eucalyptol was the main component in all seasons; summer (66.87%), autumn (58.33%), winter (46.74%) and spring (44.63%), followed by α-pinene; spring (31.41%), winter (28.69%), summer (26.34%) and autumn (24.68%). Winter oil, the highest yield (0.53 mL/100g), was further investigated for its inhibitory activity against enzymes associated with ageing; elastase and acetylcholinesterase. It remarkably inhibited elastase and acetylcholinesterase with IC50 values of 1.05 and 0.20 µg/ml, respectively. A molecular docking study was conducted for the major oil components on the active sites of target enzymes. Eucalyptol revealed the best binding affinity for both enzymes. C. subualtus oil could be used as supplement for management of ageing disorders like skin wrinkles and dementia.


Asunto(s)
Myrtaceae , Aceites Volátiles , Aceites Volátiles/farmacología , Aceites Volátiles/análisis , Aceites Volátiles/química , Estaciones del Año , Acetilcolinesterasa , Eucaliptol/farmacología , Eucaliptol/análisis , Egipto , Simulación del Acoplamiento Molecular , Hojas de la Planta/química , Myrtaceae/química , Elastasa Pancreática
2.
Mar Drugs ; 18(7)2020 Jul 08.
Artículo en Inglés | MEDLINE | ID: mdl-32650455

RESUMEN

Thalassodendron ciliatum (Forssk.) Den Hartog is a seagrass belonging to the plant family Cymodoceaceae with ubiquitous phytoconstituents and important pharmacological potential, including antioxidant, antiviral, and cytotoxic activities. In this work, a new ergosterol derivative named thalassosterol (1) was isolated from the methanolic extract of T. ciliatum growing in the Red Sea, along with two known first-reported sterols, namely ergosterol (2) and stigmasterol (3), using different chromatographic techniques. The structure of the new compound was established based on 1D and 2D NMR spectroscopy and high-resolution mass spectrometry (HR-MS) and by comparison with the literature data. The new ergosterol derivative showed significant in vitro antiproliferative potential against the human cervical cancer cell line (HeLa) and human breast cancer (MCF-7) cell lines, with IC50 values of 8.12 and 14.24 µM, respectively. In addition, docking studies on the new sterol 1 explained the possible binding interactions with an aromatase enzyme; this inhibition is beneficial in both cervical and breast cancer therapy. A metabolic analysis of the crude extract of T. ciliatum using liquid chromatography combined with high-resolution electrospray ionization mass spectrometry (LC-ESI-HR-MS) revealed the presence of an array of phenolic compounds, sterols and ceramides, as well as di- and triglycerides.


Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Inhibidores de la Aromatasa/farmacología , Ergosterol/farmacología , Magnoliopsida , Extractos Vegetales/farmacología , Antineoplásicos Fitogénicos/química , Inhibidores de la Aromatasa/química , Ergosterol/química , Humanos , Océano Índico , Células MCF-7/efectos de los fármacos , Espectroscopía de Resonancia Magnética , Extractos Vegetales/química , Relación Estructura-Actividad
3.
Artículo en Inglés | MEDLINE | ID: mdl-29317894

RESUMEN

Convolvulus austroaegyptiacus Abdallah & Sa'ad (CA) and Convolvulus pilosellifolius Desr. (CP) are commonly used in the Saudi Arabia folk medicine. They are potent in treating the ulcers and skin diseases. The lack of information about their biological activities led us to investigate the possible biological activities by determination of antibacterial and antioxidant activities of total ethanolic extracts and various fractions. Total flavonoid contents of the plants were determined by colorimetric method while total phenols were determined by using Folin-Ciocalteu method. In vitro antibacterial activity was studied against E. coli, P. aeruginosa, and B. subtilis, and the total antioxidant capacity was evaluated by radical scavenging method. IC50 were found to be 21.81, 17.62, and 3.31 µg/mL for CA, CP, and vitamin C, respectively, while the lowest MIC value of 0.25 mg/mL was recorded with CP extract against B. subtilis. Around 21 compounds are tentatively elucidated from both plants using rapid, simple, and high-resolution analytical technique for chemical profiling of natural compounds by direct analysis in real-time of flight-mass spectrometry, of which 17 were not isolated or reported previously.

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