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A comprehensive study on phytochemical characterization of Haplophyllum myrtifolium Boiss. endemic to Turkey and its inhibitory potential against key enzymes involved in Alzheimer, skin diseases and type II diabetes
Scopus
Toplam 222 atıf DOI
The interest of medicinal plants as therapeutic agents against diseases such as Alzheimer, skin disorders and diabetes mellitus is growing. In order to investigate the influence of Haplophyllum myrtifolium, four solvent extracts (petroleum ether, ethyl acetate, methanol and water) were screened for antioxidant potentials, anti-cholinesterase, anti-tyrosinase, anti-amylase and anti-glycosidase activity. Antioxidant effects were elucidated by different assays including free radical scavenging (ABTS, DPPH and NO assay), reducing power (FRAP and CUPRAC), phosphomolybdenum, β-carotene/linoleic acid system and metal chelating. Total phenolic, flavonoid, flavanol, tannin and saponin contents in these extracts were also calculated. Generally, ethyl acetate extract showed the strongest antioxidant activity in these extracts. This activity may be related to a good total phenolic content. The total phenolic contents of these extracts ranged from 32.32 to 52.50. mg GAEs/g extract. Except for water extract, all extracts showed good inhibitory activities on cholinesterase, tyrosinase, amylase and glycosidase. Apolar extracts (petroleum ether and ethyl acetate) were more potent as enzyme inhibitors in comparison to polar extracts (methanol and water). These findings reveal that H. myrtifolium could be used a source of natural compounds for the management of oxidative damage, Alzheimer, skin disorders and diabetes mellitus. © 2014 Elsevier B.V.
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Validation of the antioxidant and enzyme inhibitory potential of selected triterpenes using in vitro and in silico studies, and the evaluation of their admet properties
Scopus
Havuzumuzda Open Access 40 atıf almış
The antioxidant and enzyme inhibitory potential of fifteen cycloartane-type triterpenes’ potentials were investigated using different assays. In the phosphomolybdenum method, cycloalpio-side D (6) (4.05 mmol TEs/g) showed the highest activity. In 1,1-diphenyl-2-picrylhydrazyl (DPPH*) radical and 2,2′-azino-bis(3-ethylbenzothiazoline)-6-sulfonic acid (ABTS) cation radical scavenging as-says, cycloorbicoside A-7-monoacetate (2) (5.03 mg TE/g) and cycloorbicoside B (10) (10.60 mg TE/g) displayed the highest activities, respectively. Oleanolic acid (14) (51.45 mg TE/g) and 3-O-β-D-xylopyranoside-(23R,24S)-16β,23;16α,24-diepoxycycloart-25(26)-en-3β,7β-diol 7-monoacetate (4) (13.25 mg TE/g) revealed the highest reducing power in cupric ion-reducing activity (CUPRAC) and ferric-reducing antioxidant power (FRAP) assays, respectively. In metal-chelating activity on ferrous ions, compound 2 displayed the highest activity estimated by 41.00 mg EDTAE/g (EDTA equiva-lents/g). The tested triterpenes showed promising AChE and BChE inhibitory potential with 3-O-β-D-xylopyranoside-(23R,24S)-16β,23;16α,24-diepoxycycloart-25(26)-en-3β,7β-diol 2′,3′,4′,7-tetraacetate (3), exhibiting the highest inhibitory activity as estimated from 5.64 and 5.19 mg GALAE/g (galan-tamine equivalent/g), respectively. Compound 2 displayed the most potent tyrosinase inhibitory activity (113.24 mg KAE/g (mg kojic acid equivalent/g)). Regarding α-amylase and α-glucosidase inhibition, 3-O-β-D-xylopyranoside-(23R,24S)-16β,23;16α,24-diepoxycycloart-25(26)-en-3β,7β-diol (5) (0.55 mmol ACAE/g) and compound 3 (25.18 mmol ACAE/g) exerted the highest activities, respectively. In silico studies focused on compounds 2, 6, and 7 as inhibitors of tyrosinase revealed that compound 2 displayed a good ranking score (−7.069 kcal/mole) and also that the ∆G free-binding energy was the highest among the three selected compounds. From the ADMET/TOPKAT prediction, it can be concluded that compounds 4 and 5 displayed the best pharmacokinetic and pharmacodynamic behavior, with considerable activity in most of the examined assays.
Atıf Yapan Makale Bilgileri
Kurumlar (6)
Academy of Sciences of the Republic of Uzbekistan
Tashkent, Uzbekistan
College of Pharmacy
Riyadh, Saudi Arabia
Faculty of Pharmacy, Ain Shams University
Cairo, Egypt
Leibniz Institut fur Pflanzenbiochemie
Halle, Germany
Selçuk Üniversitesi
Selçuklu, Turkey
University of G. d'Annunzio Chieti and Pescara
Chieti, Italy