Evaluation of antidiabetic effect of Cistus salviifolius L. (Cistaceae) in streptozotocin-nicotinamide induced diabetic mice.

OBJECTIVES: Cistus salviifoluis L. is a shrub from Cistaceae family used in many traditional medicines for the treatment of various diseases including diabetes mellitus. The aim of this study was to evaluate the in vivo antidiabetic potential of the aerial parts aqueous extract of Cistus salviifolius L. (CSA). METHODS: Experimental diabetes was induced in adult male mice by intra-peritoneal injection of Streptozotocin-nicotinamide (STZ-NC). CSA at a dose of 500 mg/kg was administered daily to the diabetic mice for four weeks. The effect of the extract on hyperglycemia, body weight, serum total cholesterol, triglycerides, hepatic and renal functional markers were determined. Histopathological examination of the mice pancreas was also performed. The diabetic animals treated with CSA were compared with animals treated by the standard drug metformin. RESULTS: Treatment with CSA showed a significant reduction in blood glucose, total triglycerides and creatinine levels and prevented the reduction of body weight caused by diabetes. Furthermore, histopathological analysis of the mice pancreas showed that the group treated with CSA reduced damage induced by STZ-NC on islets of Langerhans cells when compared to the diabetic control. CONCLUSIONS: The results suggest that the aqueous extract of Moroccan C. salviifolius L. possesses beneficial effect on treatment of diabetes.

Comparative Study of Leaf and Rootstock Aqueous Extracts of Foeniculum vulgare on Chemical Profile and In Vitro Antioxidant and Antihyperglycemic Activities.

Foeniculum vulgare is a medicinal plant used in Moroccan folk medicine to treat several diseases such as diabetes. The aim of this study was to determine the phenolic bioactive compounds and to evaluate the antioxidant and antihyperglycemic activities of Foeniculum vulgare leaf and rootstock extracts. Phenolic compounds of F. vulgare rootstock and leaf extracts were determined using HPLC-DAD-QTOFMS analysis. The antioxidant activity was evaluated using 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS•+) radicals. Moreover, the in vitro antihyperglycemic effects were tested by measuring the inhibition of α-amylase and α-glucosidase activities. HPLC-DAD-QTOFMS analysis identified thirty-two phenolic components in both leaf and rootstock extracts. Caffeic acid, quinic acid, and chlorogenic acid were the major compounds of F. vulgare leaf extract (FVLE), while the main compound of F. vulgare rootstock extracts (FVRE) was quinic acid. In the DPPH assay, F. vulgare leaf extract showed important antioxidant activity (IC50 = 12.16 ± 0.02 µg/mL) than F. vulgare rootstock extract (IC50 = 34.36 ± 0.09 µg/mL). Moreover, fennel leaf extracts revealed also the most powerful antioxidant activity (IC50 = 22.95 ± 0.4 µg/mL) in the ABTS assay. The in vitro antihyperglycemic activity showed that F. vulgare rootstock extract exhibited a remarkable inhibitory capacity (IC50 = 194.30 ± 4.8 µg/mL) of α-amylase compared with F. vulgare leaf extract (IC50 = 1026.50 ± 6.5 µg/mL). Furthermore, the inhibition of α-glucosidase was more importantly with F. vulgare rootstock (IC50 of 165.90 ± 1.2 µg/mL) than F. vulgare leaf extracts (203.80 ± 1.3 µg/mL). The funding of this study showed that F. vulgare rootstock and leaf extracts presented several phenolic compounds and showed important antioxidant and antidiabetic effects. We suggest that the identified molecules are responsible for the obtained activities. However, further studies focusing on the isolation and the determination of antioxidant and antidiabetic effects of F. vulgare rootstock and leaf main compounds are required.

Evaluation of In Vitro Antioxidant and Antidiabetic Activities of Aristolochia longa Extracts.

Oxidative stress plays a major role in diabetic physiopathology; hence, the interest of using natural antioxidants as therapeutic tools exists. The aim of this study was the evaluation of in vitro antioxidant activity and inhibitory potential of organic extracts from Aristolochia longa roots against key enzymes linked to hyperglycemia. Antioxidant activity was performed using 2,2'-diphenyl-1-picrylhydrazyl (DPPH) and 2,2-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS) radicals and ferric reducing/antioxidant power (FRAP) methods. The α-Glucosidase and ß-Galactosidase inhibitory activities were investigated using an in vitro model. Moreover, phytochemical analysis of tested extracts was carried out. The aqueous fraction of this herb exhibited the highest antioxidant activity for both DPPH and ABTS methods, IC50=125.40±2.40 µg/mL and IC50=65.23±2.49 µg/mL, respectively. However, the ethyl acetate fraction possessed the strongest inhibitory effect towards α-Glucosidase (IC50=1.112±0.026 mg/mL). Furthermore, the result showed high levels of phenolic content. The results showed that this plant could be a significant source of medically important natural compounds.

Potential antidiabetic activity and molecular docking studies of novel synthesized 3.6-dimethyl-5-oxo-pyrido[3,4-f][1,2,4]triazepino[2,3-a]benzimidazole and 10-amino-2-methyl-4-oxo pyrimido[1,2-a]benzimidazole derivatives.

Diabetes affects a large population of the globe and is considered as a leading cause of death. Many synthetic and natural inhibitors have been developed for diabetes treatment. Herein, we report the potential antidiabetic activity of two new heterocyclic systems, namely 3.6-dimethyl-5-oxo-pyrido[3,4f][1,2,4]triazepino[2,3-a]benzimidazole (I) and 10-amino-2-methyl-4-oxo pyrimido[1,2-a]benzimidazole (II) against three related enzymes: α-amylase, α-glucosidase and ß-galactosidase. Compounds I and II were synthesized by the action of DMF-DMA and dimethyl sulfate in the presence of water on 2-methyl-3H-benzimidazolo[1,2b][1,2,4]triazepin-4(5H)-one, and are characterized by single X-ray diffraction. The binding interaction modes in the active sites of I and II and targeted enzymes (stable complexes ligand-receptor) are emphasized using the molecular docking approach by applying the Lamarckian genetic algorithm method. Furthermore, plausible mechanisms have been proposed explaining their synthesis. Hirshfeld surface analysis reveals the nature of molecular interactions and fingerprint plots provide information about the percentage contribution from each individual molecular contact to the structure surface. Graphical abstract Left Molecular packing of 1,4-dimethyl-2-oxo-pyrimido[1,2-a]benzimidazole hydrate. Right Docking active site of α-glucosidase.

Antioxidant Activity and Inhibitory Potential of Cistus salviifolius (L.) and Cistus monspeliensis (L.) Aerial Parts Extracts against Key Enzymes Linked to Hyperglycemia.

Cistus genus (Cistaceae) comprises several medicinal plants used in traditional medicines to treat several pathological conditions including hyperglycemia. These include Cistus salviifolius L. (CS) and Cistus monspeliensis L. (CM), still not fully explored as a source of metabolites with therapeutic potential for human diseases. In this study, the antioxidant α-amylase and α-glucosidase enzyme inhibitory effects of aqueous and hydromethanolic extracts from the aerial parts of Moroccan CS and CM were investigated. Antioxidant activity has been assessed using 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS) radicals and ferric reducing/antioxidant power (FRAP) methods. The α-amylase and α-glucosidase inhibitory activity has been assessed using an in vitro model. Moreover, mineral and phenolic contents of CS and CM were analyzed. The extracts of both species exhibited potent antioxidant activity in all used systems and possess strong inhibitory effect towards α-glucosidase (IC50: 0.95 ± 0.14 to 14.58 ± 1.26 µg/mL) and significant inhibitory potential against α-amylase (IC50: 217.10 ± 0.15 to 886.10 ± 0.10 µg/mL). Furthermore, the result showed high levels of phenolic content and unexpectedly some higher levels of mineral content in CS. The results suggest that the phenolic rich extracts of CS and CM may have a therapeutic potential against diseases associated with oxidative stress and may be useful in the management of hyperglycemia in diabetic patients.