Objective: To evaluate the in vitro anti-diabetic effects of Bryonia dioica roots extracts, including water-acetone extracts and their ethyl acetate and butanol fractions, and chloroform-methanol extracts. Methods: The total phenolic, flavonoid, flavonol, and saponin contents in the Bryonia dioica root extracts (chloroform-methanol extracts, water-acetone extracts and their ethyl acetate and butanol fractions) were determined using colorimetric methods with Folin-Ciocalteu, aluminum trichloride, and vanillin reagents, respectively. The in vitro anti-diabetic activity was evaluated by measuring the half-maximal inhibitory concentration (IC50) values of these root extracts against α-amylase and α-glucosidase activities, evaluating their effects on α-amylase kinetics, quantifying the inhibition of bovine serum albumin (BSA) glycation using fluorometry to assess advanced glycation end products (AGE) production, and determining glucose uptake by isolated rat hemidiaphragm. Additionally, molecular docking analysis was conducted to investigate the binding affinity and interaction types between Bryonia dioica ligands (cucurbitacin B, bryogénin, vitexin, and isovitexin) and target enzymes, and a phytochemical-targets interaction network was constructed. Results: For α-amylase inhibition, ethyl acetate fraction demonstrated the most potent activity (IC50 = 145.95 µg/mL), followed by chloroform-methanol extract (IC50 = 300.86 µg/mL). Water-acetone root extracts and their ethyl acetate and butanol fractions inhibited the α-glucosidase activity with IC50 values ranging from 562.88 to 583.90 µg/mL. Both ethyl acetate and butanol fractions strongly inhibited non-enzymatic BSA glycation (IC50 = 318.26 and 323.12 µg/mL, respectively). The incubation of isolated rat hemidiaphragms with the ethyl acetate fraction (5 mg/mL) significantly increased glucose uptake (35.16%; P < 0.0001), exceeding the effects of insulin (29.27%), chloroform-methanol extract (24.07%), and catechin (15.27%). Molecular docking revealed that cucurbitacin B exhibited the strongest docking scores against α-amylase (– 16.4 kcal/mol), and α-glucosidase (– 14.2 kcal/mol). Compared with other ligands, isovitexin formed the maximum number of hydrogen bonds with the α-amylase active site residues (Asp300, Asp197, and Glu233), α-glucosidase residues (Ser13, Arg44, Met86, Gly10, Asp39, and Tyr131) and other residues (Arg195, Trp59, His299, and Tyr62). Network analysis identified 36 overlapping targets between Bryonia dioica phytochemicals and type 2 diabetes mellitus-associated genes, with cucurbitacins and polyphenols interacting with α-amylase, α-glucosidase, and Glut4 translocation pathway targets. Conclusion Bryonia dioica root extracts demonstrated promising in vitro anti-diabetic activity through multiple mechanisms, including the inhibitory effect on digestive enzymes, protein antiglycation potential, and enhancement of glucose uptake, suggesting their potential as a source for anti-diabetic drugs development.

AIM: The aqueous methanolic extracts of two plants from Algeria, Helichrysum stoechas subsp. rupestre and Phagnalon saxatile subsp. saxatile, were investigated for their antioxidant activity. METHOD: Total phenolics, flavonoids, and tannins were determined by spectrophotometric techniques. In vitro antioxidant and radical scavenging profiling was determined by spectrophotometric methods, through: Total antioxidant capacity, and radical scavenging effects by the DPPH and ABTS methods, reducing and chelating power, and blanching inhibition of the β-carotene. RESULTS: All of the extracts showed interesting antioxidant and radical scavenging activity. The highest contents in phenolics, tannins, and the highest total antioxidant capacity as gallic acid equivalents of 97.5 ± 0.33 mg GAE/g DW was obtained for the flowers of H. stoechas subsp. rupestre extract in the phosphomolybdenum assay. An extract of the leafy stems of P. saxatile subsp. saxatile revealed the highest content of flavonoids, and the highest antioxidant activity by the radical scavenging and β-carotene assays when compared with standards. The best activity was by the scavenging radical DPPH with an IC50 value of 5.65 ± 0.10 μg·mL(-1). CONCLUSION The studied medicinal plants could provide scientific evidence for some traditional uses in the treatment of diseases related to the production of reactive oxygen species (ROS) and oxidative stress.
Algeria ; Antioxidants ; analysis ; pharmacology ; Asteraceae ; chemistry ; Benzothiazoles ; metabolism ; Biphenyl Compounds ; metabolism ; Flavonoids ; analysis ; pharmacology ; Helichrysum ; chemistry ; Oxidative Stress ; drug effects ; Phenols ; analysis ; pharmacology ; Picrates ; metabolism ; Plant Extracts ; chemistry ; pharmacology ; Plant Structures ; chemistry ; Spectrophotometry ; methods ; Sulfonic Acids ; metabolism ; Tannins ; analysis ; pharmacology