Chnoospora minima: a Robust Candidate for Hyperglycemia Management, Unveiling Potent Inhibitory Compounds and Their Therapeutic Potential.
The present study aimed to isolate a bioactive compound from Sri Lankan edible marine brown algae, Chnoospora minima, to manage diabetes. The de-polysaccharide crude methanolic extract was partitioned using hexane, chloroform, and ethyl acetate with increased polarity. The samples were subjected to determine the quantitative phytochemical analysis, antioxidants, and antidiabetic potentials. Further, the potent antidiabetic fraction was selected to isolate an active compound using bioactivity-guided fractionation. From the selected extract, the chloroform fraction exhibited comparatively high TPC (59.01 ± 1.86 mg GAE/g), TFC (5.14 ± 0.43 mg QE/g) and alkaloid content (2.79 ± 0.31 PE/g of extract). Crude methanol extract exhibited a potent DPPH activity (IC50: 0.48 ± 0.01 mg/mL) whereas the ethyl acetate fraction elicited a maximum ABTS activity (IC50: 0.064 ± 0.001 mg/mL) and a ferrous iron-chelating capacity (IC50: 0.019 mg/mL). Similarly, the chloroform fraction exhibited the highest FRAP (20.34 ± 1.72 mg TE/g) and ORAC (19.72 ± 2.92 mg TE/g) capacities. The potent inhibitory activity of α-amylase (IC50:3.17 ± 0.02 µg/mL) and α-glucosidase (IC50: 1.99 ± 0.01 µg/mL) enzymes and glucose diffusion was observed in the chloroform fraction. Similarly, the chloroform extract exhibited a potent BSA-glucose (IC50: 202.43 ± 5.71 µg/mL), BSA-MGO (IC50: 124.30 ± 2.85 µg/mL) antiglycation model and reversing activities (EC50BSAglucose: 98.99 ± 0.35 µg/mL; EC50BSA-MGO: 118.89 ± 1.58 µg/mL). Depending on the hypoglycemic activity, fucoxanthin was isolated as the active compound which showed a notable change in the functional group. Molecular docking studies were conducted on the compound, and binding energy was observed to be - 6.56 kcal/mol and - 4.83 kcal/mol for α-amylase and α-glucosidase enzymes, respectively, which confirmed the hypoglycemic effect of the isolated compounds. However, more studies are required to understand the mechanistic insights of these observations.
Gunathilaka TL
,Bandaranayake U
,Boudjelal M
,Ali R
,Silva RM
,Samarakoon KW
,Ranasinghe P
,Peiris LDC
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Anacardium humile St. Hil as a novel source of antioxidant, antiglycation and α-amylase inhibitors molecules with potential for management of oxidative stress and diabetes.
The substantial increase in diabetes cases worldwide has been a major public health problem, and the use of medicinal plants can be considered an interesting alternative to control the disease and its complications. Anacardium humile St. Hill. (Anacardiaceae) is a typical plant from the Brazilian savanna, popularly known for its antidiarrheal, expectorant, antidiabetic and anti-inflammatory properties, however, few studies have fully described its biological properties. This study aimed to investigate in vitro and ex vivo the antioxidant and antiglycation potential of A. humile ethanolic extract, its organic fractions and three isolated molecules (quercetin, catechin and gallic acid), their capacity to inhibit the glycolytic enzyme α-amylase, as well as their cytotoxic effects against RAW264.7 macrophages.
The ethanolic extract of A. humile, its organic fractions and three isolated molecules (catechin, quercetin and gallic acid) were tested for their antioxidant (ORAC, FRAP and DPPH) and antiglycation (BSA/Fructose, BSA/Methylglyoxal, Arginine/Methylglyoxal and Lysine/Methylglyoxal) capacities, and also for its potential to inhibit the enzyme α-amylase. Additionally, bioactive compounds present in the A. humile leaves fractions were elucidated by an HPLC-ESIMS/MS analysis.
The analysis showed relevant antioxidant activity of DCM (1264.85 ± 76.90 μM Trolox eq/g ORAC; 216.71 ± 1.04 μM Trolox eq/g FRAP and 3.03 ± 0.08 IC50 μg/mL IC50 DPPH) and EtOAc (1300.11 ± 33.04 ORAC, 236.21 ± 23.86 FRAP and 3.03 ± 0.14 μg/mL IC50 DPPH) fractions and also of the isolated molecules, mainly gallic acid (1291.19 ± 8.41 μM Trolox eq/g ORAC, 1103.52 ± 31.48 μM Trolox eq/g FRAP and 0.78 ± 0.11 μg/mL IC50 DPPH). Concerning the antiglycation activity, all samples inhibited over 88% in the BSA-FRU method. In the BSA-MGO and ARG-MGO methods, the Hex, DCM, EtOAc fractions and the isolated molecule catechin stood out. However, in the LYS-MGO model, only the isolated molecules showed significant results. In α-amylase assay, all fractions, for exception Hex, presented notable inhibition capacity with low IC50 values, especially DCM, EtOAc, ButOH and H2O (IC50 0.56 ± 0.10, 0.84 ± 0.01, 0.74 ± 0.03 and 0.79 ± 0.06 μg/mL, respectively). Tests using hepatic tissue showed a notorious capacity of the DCM, AcOEt and ButOH fractions, as well as of the isolated molecules to inhibit lipid peroxidation and ROS production, and also to preserve thiol groups. Molecules of great antioxidant potential were found in our samples, such as kaempferol, quercetin, catechin, gallic acid and luteolin.
A. humile extract and its organic fractions showed promising antioxidant and antiglycation potential and a prominent capacity to inhibit the α-amylase enzyme. Hence, this study presents new results and stimulates further research to elucidate the biological properties of A. humile and its capacity to manage DM and its complications.
Lima Júnior JP
,Franco RR
,Saraiva AL
,Moraes IB
,Espindola FS
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