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1.
Molecules ; 27(21)2022 Nov 03.
Artículo en Inglés | MEDLINE | ID: mdl-36364367

RESUMEN

Iphiona mucronata (Family Asteraceae) is widely distributed in the Eastern desert of Egypt. It is a promising plant material for phytochemical analysis and pharmacologic studies, and so far, its specific metabolites and biological activity have not yet been thoroughly investigated. Herein, we report on the detailed phytochemical study using UPLC-Q-TOF-MS approach. This analysis allowed the putative annotation of 48 metabolites belonging to various phytochemical classes, including mostly sesquiterpenes, flavonoids, and phenolic acids. Further, zebrafish embryotoxicity has been carried out, where 100 µg/mL extract incubated for 72 h resulted in a slow touch response of the 10 examined larvae, which might be taken as a sign of a disturbed peripheral nervous system. Results of in vitro testing indicate moderate cytotoxicity towards VERO, FaDu, and HeLa cells with CC50 values between 91.6 and 101.7 µg/mL. However, selective antineoplastic activity in RKO cells with CC50 of 54.5 µg/mL was observed. To the best of our knowledge, this is the first comprehensive profile of I. mucronata secondary metabolites that provides chemical-based evidence for its biological effects. A further investigation should be carried out to precisely define the underlying mechanisms of toxicity.


Asunto(s)
Asteraceae , Pez Cebra , Humanos , Animales , Células HeLa , Extractos Vegetales/farmacología , Fitoquímicos/farmacología , Fitoquímicos/análisis , Cromatografía Líquida de Alta Presión/métodos
2.
Molecules ; 27(20)2022 Oct 21.
Artículo en Inglés | MEDLINE | ID: mdl-36296710

RESUMEN

The aim of the present study is to investigate the phytochemical composition of tiger nut (TN) (Cyperus esculentus L.) and its neuroprotective potential in scopolamine (Scop)-induced cognitive impairment in rats. The UHPLC-ESI-QTOF-MS analysis enabled the putative annotation of 88 metabolites, such as saccharides, amino acids, organic acids, fatty acids, phenolic compounds and flavonoids. Treatment with TN extract restored Scop-induced learning and memory impairments. In parallel, TN extract succeeded in lowering amyloid beta, ß-secretase protein expression and acetylcholine esterase (AChE) activity in the hippocampus of rats. TN extract decreased malondialdehyde levels, restored antioxidant levels and reduced proinflammatory cytokines as well as the Bax/Bcl2 ratio. Histopathological analysis demonstrated marked neuroprotection in TN-treated groups. In conclusion, the present study reveals that TN extract attenuates Scop-induced memory impairments by diminishing amyloid beta aggregates, as well as its anti-inflammatory, antioxidant, anti-apoptotic and anti-AChE activities.


Asunto(s)
Disfunción Cognitiva , Cyperus , Fármacos Neuroprotectores , Animales , Ratas , Escopolamina/efectos adversos , Cyperus/química , Fármacos Neuroprotectores/uso terapéutico , Antioxidantes/metabolismo , Acetilcolina/metabolismo , Péptidos beta-Amiloides/metabolismo , Secretasas de la Proteína Precursora del Amiloide/metabolismo , Proteína X Asociada a bcl-2/metabolismo , Trastornos de la Memoria/inducido químicamente , Trastornos de la Memoria/tratamiento farmacológico , Trastornos de la Memoria/metabolismo , Malondialdehído/metabolismo , Disfunción Cognitiva/inducido químicamente , Disfunción Cognitiva/tratamiento farmacológico , Extractos Vegetales/metabolismo , Flavonoides/metabolismo , Aminoácidos/metabolismo , Ácidos Grasos/metabolismo , Citocinas/metabolismo , Esterasas/metabolismo
3.
J Ethnopharmacol ; 289: 115062, 2022 May 10.
Artículo en Inglés | MEDLINE | ID: mdl-35114339

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Ferula hermonis is a small shrub renowned for its aphrodisiac abilities. Middle East herbalists have utilized Ferula hermonis seed and root as an aphrodisiac folk medicine to treat women's frigidity and male erectile and sexual dysfunction. AIM OF THE STUDY: Assessment of follicle-stimulating hormone-like (FSH), luteinizing hormone-like (LH), and estrogenic activities of the methanolic extract (ME) of the roots of Ferula hermonis on female reproductive function. MATERIALS AND METHODS: The methanolic extract was prepared from the root of F. hermonis and studied at dose level 6 mg/kg in immature female rats for FSH-like, LH-like, and estrogenic activities. These activities were determined by analyzing gross anatomical features, relative organ weight, and serum level of FSH, LH, progesterone and estrogen hormones, and histopathological characteristics. Quantification of the main phytoestrogenic component ferutinin carried out by HPLC. In addition, molecular docking for the binding affinity of ferutinin inside active sites of both estrogen receptor alpha (ERα) and FSH receptor (FSHR) was performed to predict the potential role of ferutinin in regulating the female reproductive process. RESULTS: Ferula hermonis (ME) showed potent FSH-like, LH-like activities and moderate estrogenic effect at the dose of 6 mg/kg. The content of ferutinin in F. hermonis was estimated to be 92 ± 1.33 mg/g of the methanolic extract. Molecular docking of ferutinin with ERα and FSHR displayed strong interaction with target proteins. CONCLUSIONS: Based on results, it can be concluded that Ferula hermonis can be considered as a suitable female fertility improving agent.


Asunto(s)
Benzoatos/farmacología , Cicloheptanos/farmacología , Fármacos para la Fertilidad/farmacología , Ferula/química , Extractos Vegetales/farmacología , Sesquiterpenos/farmacología , Animales , Benzoatos/aislamiento & purificación , Compuestos Bicíclicos con Puentes/aislamiento & purificación , Compuestos Bicíclicos con Puentes/farmacología , Cromatografía Líquida de Alta Presión , Cicloheptanos/aislamiento & purificación , Femenino , Fertilidad , Fármacos para la Fertilidad/aislamiento & purificación , Hormona Folículo Estimulante/metabolismo , Hormona Luteinizante/metabolismo , Simulación del Acoplamiento Molecular , Ratas , Sesquiterpenos/aislamiento & purificación
4.
Nat Prod Res ; 36(4): 1115-1117, 2022 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-33342292

RESUMEN

The present study aims at evaluating potential of the ethanol extracts of L. camara leaves (LE), flowers (FlE) and roots (RE) in the treatment of renal calculi and characterising the secondary metabolites in the active extract. The results revealed that the FlE had significantly reduced the levels of kidney parameters (calcium, creatinine, urea, and uric acid) against ethylene glycol (EG) injuries, and restored the activity of glutathione peroxidase (GPx), superoxide dismutase and lipid peroxide malondialdehyde to the normal level. In addition, FlE significantly attenuated iNOS tissue expression caused by EG. The results obtained in this study suggest the potential value of the L. camara L. flowers as an antiurolithiatic agent.


Asunto(s)
Lantana , Animales , Flores , Extractos Vegetales/farmacología , Hojas de la Planta , Ratas , Ratas Wistar
5.
Artículo en Inglés | MEDLINE | ID: mdl-34052752

RESUMEN

Detailed metabolic profiling of needles of five Pinus species was investigated using complementary HPLC-MS/MS techniques together with supervised and unsupervised chemometric tools. This resulted in putative identification of 44 compounds belonging to flavonoids, phenolics, lignans, diterpenes and fatty acids. Unsupervised principal component analysis showed that differences were maintained across the metabolites characteristic of each Pinus species, are mainly related to di-O-p-coumaroyltrifolin, p-coumaroyl quinic acid derivative, arachidonic acid, hydroxypalmitic acid, isopimaric acid and its derivative. A supervised Partial Least Squares regression analysis was performed to correlate HPLC-MS/MS profiles with the variation observed in the in vitro anticholinesterase, antiaging and anti-diabetic potential. All investigated Pinus extracts exerted their antiaging activity via increasing telomerase and TERT levels in normal human melanocytes cells compared to the control (untreated cells). Profound inhibition activities of acetylcholinesterase and dipeptidyl peptidase-4 were also observed with P. pinea and P. canariensis extracts having comparable antidiabetic activities to sitagliptin as a standard antidiabetic drug. Our findings suggested that pine needles are a good source of phenolics and diterpenoids that have possible health promoting activities in management and alleviation of diabetic conditions and Alzheimer disease.


Asunto(s)
Cromatografía Líquida de Alta Presión/métodos , Metaboloma/fisiología , Pinus , Espectrometría de Masas en Tándem/métodos , Inhibidores de la Colinesterasa/análisis , Inhibidores de la Colinesterasa/química , Inhibidores de la Colinesterasa/metabolismo , Diterpenos/análisis , Diterpenos/química , Diterpenos/metabolismo , Flavonoides/análisis , Flavonoides/química , Flavonoides/metabolismo , Hipoglucemiantes/análisis , Hipoglucemiantes/química , Hipoglucemiantes/metabolismo , Metabolómica , Pinus/química , Pinus/metabolismo , Extractos Vegetales/química , Sustancias Protectoras/análisis , Sustancias Protectoras/química , Sustancias Protectoras/metabolismo , Extracción en Fase Sólida/métodos
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