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Antiglycation Activity and HT-29 Cellular Uptake of Aloe-Emodin, Aloin, and Aloe arborescens Leaf Extracts.

ABSTRACT: Aloe arborescens is a relevant species largely used in traditional medicine of several countries. In particular, the decoction of leaves is prepared for various medicinal purposes including antidiabetic care. The aim of this research was the study of the antiglycation activity of two A. arborescens leaf extracts and isolated compounds: aloin and aloe-emodin. These phytoconstituents were quantitatively assessed in methanolic and hydroalcoholic extracts using high performance liquid chromatography (HPLC) analysis. In addition, the total phenolic and flavonoid contents were detected. In order to study their potential use in diabetic conditions, the antiglycation and antiradical properties of the two extracts and aloin and aloe-emodin were investigated by means of bovine serum albumin (BSA) and 1,1-diphenyl-2-picryl-hydrazil (DPPH) assays; further, their cytotoxicity in HT-29 human colon adenocarcinoma cells was evaluated by 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl tetrazolium bromide (MTT) assay. Furthermore, the ability of aloin and aloe-emodin to permeate the cellular membranes of HT-29 cells was determined in order to estimate their potential in vivo absorption. This assessment indicated that aloe-emodin can substantially pass through cell membranes (~20%), whereas aloin did not permeate into HT-29 cells. Overall, the data show that both the methanolic and the hydroalcoholic A. arborescens extracts determine significant inhibition of glycation and free-radical persistence, without any cytotoxic activity. The data also show that the antiglycation and the antiradical activities of aloin and aloe-emodin are lower than those of the two extracts. In relation to the permeability study, only aloe-emodin is able to cross HT-29 cellular membranes, showing the attitude to pass through the intestinal layer. Overall, the present data surely support the traditional use of A. arborescens leaf extracts against hyperglycemic conditions, while aloin and aloe-emodin as potential drugs need further study.

SUBMITTER: Froldi G

PROVIDER: S-EPMC6600357 | biostudies-literature | 2019 Jun

REPOSITORIES: biostudies-literature

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Antiglycation Activity and HT-29 Cellular Uptake of Aloe-Emodin, Aloin, and Aloe arborescens Leaf Extracts.

Froldi Guglielmina G Baronchelli Federica F Marin Elisa E Grison Margherita M

Molecules (Basel, Switzerland) 20190605 11

Aloe arborescens is a relevant species largely used in traditional medicine of several countries. In particular, the decoction of leaves is prepared for various medicinal purposes including antidiabetic care. The aim of this research was the study of the antiglycation activity of two A. arborescens leaf extracts and isolated compounds: aloin and aloe-emodin. These phytoconstituents were quantitatively assessed in methanolic and hydroalcoholic extracts using high performance liquid ...[more]

PMID: 31195732

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Project description:IntroductionIsolated bioactive components of plants or their raw extract are utilized as complementary or alternate remedy in copious illnesses. The current research was aimed at assessing the activity of aloin A isolated from Aloe barbadensis Miller and its formulated ointment against six (6) selected clinical isolates.MethodsThe column chromatography was utilized in isolating aloin A from chloroform/methanol solvent polarity. The characterization of the isolated compound was performed by spectroscopy techniques corresponding to UV, IR, 1H- and 13C-NMR spectroscopy. It was formulated as ointment using polyethylene glycol (PEG) and both the ointment and the isolated compound were probed for in vitro antimicrobial activity.ResultsAloin A has been isolated from chloroform/methanol solvent mixture. The structure has been explicated as (10S)-10-β-d-glucopyranosyl-1,8-dihydroxy-3-(hydroxymethyl)-9(10H)-anthracenone(1S)-1,5-anhydro-1-[(9S)-4,5-dihydroxy-2-(hydroxymethyl)-10-oxo-9,10-dihydro-9-anthracenyl]-d-glucitol. The minimum inhibitory concentration (MIC) of the isolated aloin A on the pathogens ranged from 2.5 to 5.0 mg/ml and 0.32 to 5.0 mg/ml for both aloin A and the formulated ointment respectively. It was further revealed that the activity of aloin A showed dose dependence against all the test microorganisms. There was no significant difference in the activity of the drug against K. pneumoniae, S. aureus, E. coli, C. albicans and T. flavus (P > 0.05) when the concentration was raised from 2.5 to 5 mg/ml, however, there was significant difference (P ˂ 0.05) in activity against P. aeruginosa. The formulated ointment exhibited dose dependent activity against all test microorganisms. At low concentrations, the ointment showed no significant difference in diameter zone of inhibition against all test microorganisms (P > 0.05) except P. aeruginosa which exhibited a highly significant difference (P < 0.05).ConclusionBoth the isolated aloin A and its formulated ointment demonstrated substantial inhibition of growth of the pathogenic strains. These findings sturdily suggest that aloin A is a nascent drug that could be explored as skin and wound transmittable agent.

Project description:Background: Heteromorpha arborescens (Spreng.) Cham. and Schltdl (Apiaceae) is widely used traditionally for the treatment of a wide range of diseases in Southern and Eastern Africa. Although previous studies have reported the biological activities of hexane, ethyl acetate and methanol extracts of H. arborescens leaves, there is no scientific information on the phytochemical contents, antioxidant and antibacterial activities of acetone, ethanol, aqueous and blanched extracts. This study is therefore aimed to investigate and compare the phytochemical contents, antioxidant and antibacterial activities of acetone, ethanol, aqueous and blanched extracts of H. arborescens leaves. Methods: Phytochemical analysis for the total phenolic, flavonoid, proanthocyanidin, alkaloid and saponin contents of all the fractions were determined by spectroscopic methods, while the free radical scavenging potential of the extracts were evaluated using DPPH, ABTS radical scavenging and total antioxidant capacity assays. Micro dilution method was used to determine the Minimum Inhibitory Concentrations (MIC) of H. arborescens leaf extracts against Bacillus pumilus, Staphylococcus epidermidis, Staphylococcus aureus, Escherichia coli and Klebsiella pneumoniae. Results: Total phenol content of the extracts ranged between 15.10 mg GAE/g- 42.50 mg GAE/g, proanthocyanidin was 459-8402.1 mg QE/g, and flavonoid content of 109.24-235.79 mg QE/g. In addition, alkaloids (5.59%) and saponins (23.33%) were present in significant amounts. Based on the IC 50 values, the ethanol extract exhibited the highest total antioxidant activity (0.013 mg/mL) with highest inhibition against DPPH and ABTS radicals (0.06 and 0.049 mg/mL respectively). Considerable antibacterial activities were observed in the acetone, ethanol and blanched extracts with MIC values ranging from 1.563-12.5 mg/mL; however, the aqueous extract was inactive against all the bacteria strains. Conclusion: The study suggests that H. arborescens leaves could be a valuable source of bioactive compounds. Although the blanching process significantly decreased polyphenolic contents and antioxidant activities of the extracts, it increased the antibacterial compounds.

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Antiglycation Activity and HT-29 Cellular Uptake of Aloe-Emodin, Aloin, and Aloe arborescens Leaf Extracts.

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Antiglycation Activity and HT-29 Cellular Uptake of Aloe-Emodin, Aloin, and <i>Aloe arborescens</i> Leaf Extracts.

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