Despite the fact that Echium angustifolium growing in Egypt is used for grazing and medicinal uses, as well as a previous work showed that some isolated lignans revealed strong cytotoxic activity, there is rarity of scientific data concerning the chemical and biological profiles of the plant. Accordingly, our study was conducted to complementarily investigate in vitro anticancer activity of the plant's aerial parts supported by bioguided chromatographic fractionation of the total extract along with tentative identification of the bioactive fractions. Our results represented that the total extract inhibited the growth of HEPG2 and HCT116 cancer cell lines with IC 50 = 22 ± 0.6 and 15 ± 1.1 µg/ml, respectively. Two promising subfractions (Ea-DfD and Ea-DfE) resulting from extensive fractionation possessed remarkable anticancer activities with IC 50 10 ± 0.2 and 4 ± 0.5 µg/ml against HEPG2 and IC 50 4 ± 0.8 and 11 ± 0.7 µg/ ml toward HCT116, respectively. Additionally, the antioxidant activity of these two active subfractions was evaluated in vitro using the 2,2′-diphenyl-1-picryl-hydrazyl hydrate, 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonate), ferricreducing ability power, and oxygen radical absorbance capacity assays which confirmed their antioxidant potential compared to Trolox (reference drug). Furthermore, these activities could be attributed to the presence of phenolic acid derivatives and lignans in Ea-DfD and Ea-DfE that were tentatively identified using LC-ESI-MS analysis.
Background: In traditional North Africa, medicine decoctions of the leaves of Periploca angustifolia are used to treat diarrhea, inflammation, ulcers, edema and diabetes. The aim of the study was to evaluate the phytochemical, antiinflammatory, anti-ulcerogenic, and hypoglycemic activities of an ethanolic extract of P. angustifolia L. in rats. Methods: An extract of air-dried powdered P. angustifolia plant was obtained using 96% ethanol. The extract was concentrated and the total phenolic and flavonoids contents were estimated colorimetrically. The phenolic and flavonoid compounds were quantified and identified using high performance liquid chromatography (HPLC). The anti-inflammatory, anti-ulcerogenic and hypoglycemic activities of the extract were evaluated in three rat models respectively: formaldehyde-induced paw edema, ethanol induced gastric damage and alloxan induced hyperglycemia. Results: The total flavonoids and total phenolics constituted 15% and 2.69% of the extract, respectively and are expressed as quercetin equivalent and μg/mg gallic acid equivalent (GAE). Coumarin, resorcinol, isorhamnetin, quercetin, and naphthalene were isolated from the ethanolic extract of P. angustifolia. Oral administration of the ethanolic extract at 500 mg/kg body weight (b.wt.) significantly reduced paw inflammation, gastric lesions, ulcer index scores and blood glucose levels in normal and diabetic rats. Conclusion:The crude ethanolic extract of P. angustifolia exhibited promising anti-inflammatory, anti-ulcerogenic, and hypoglycemic activities in accordance with the plant's uses in folk medicine suggesting that P. angustifolia may be a safe alternative to chemical drugs.
Our previous findings elucidated that the hydroethanolic extract of Echium angustifolium M ill. aerial parts and its defatted (polar) fraction supported by bio-guided fractionation possessed potential anticancer and antioxidant activities, as well as other documented plant therapeutic uses. Consequently, the present study aimed to evaluate the hexane (non-polar) extract of E. angustifolium aerial parts for in vitro anticancer, antioxidant, and anti-inflammatory activities accompanied by characterization of its bioactive constituents using GC-M S and LC-ESI-M S techniques in order to gain a deeper understanding of this medicinal plant that could be developed as a phytomedicine. This extract exhibited high inhibition against HCT116 (IC 50 = 12 µg/mL) & HEPG2 (IC 50 = 18 µg/mL) cancer cell lines, with antioxidant and anti-inflammatory potentials. GC-M S of the analyzed extract led to identifying 24 volatile constituents, among them, ethyl esters of palmitic acid and linoleic acid were the most abundant oxygenated compounds. M eanwhile, 10 nonvolatile components were annotated by LC-ESI-M S comprising five phenolic acid derivatives, two lignans, echimidine, acetylshikonin, and quinic acid. M oreover, some of these phytoconstituents were identified in this plant species for the first time. These results justify using non-polar E. angustifolium extract as a possible source of anticancer, antioxidant, and anti-inflammatory agents, which can be better confirmed by further in vivo studies.
(1) Background: SARS-CoV-2 Omicron BA.1 is the most common variation found in most countries and is responsible for 99% of cases in the United States. To overcome this challenge, there is an urgent need to discover effective inhibitors to prevent the emerging BA.1 variant. Natural products, particularly flavonoids, have had widespread success in reducing COVID-19 prevalence. (2) Methods: In the ongoing study, fifteen compounds were annotated from Echium angustifolium and peach (Prunus persica), which were computationally analyzed using various in silico techniques. Molecular docking calculations were performed for the identified phytochemicals to investigate their efficacy. Molecular dynamics (MD) simulations over 200 ns followed by molecular mechanics Poisson–Boltzmann surface area calculations (MM/PBSA) were performed to estimate the binding energy. Bioactivity was also calculated for the best components in terms of drug likeness and drug score. (3) Results: The data obtained from the molecular docking study demonstrated that five compounds exhibited remarkable potency, with docking scores greater than −9.0 kcal/mol. Among them, compounds 1, 2 and 4 showed higher stability within the active site of Omicron BA.1, with ΔGbinding values of −49.02, −48.07, and −67.47 KJ/mol, respectively. These findings imply that the discovered phytoconstituents are promising in the search for anti-Omicron BA.1 drugs and should be investigated in future in vitro and in vivo research.
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