Application of Aleppo pine extract for skin burn treatment.

OBJECTIVE: To investigate the Pinus halepensis extracts and determine its healing and antibacterial effects, and to evaluate the treatment of skin burns. METHODS: Aqueous and ethanolic extracts and topical based on Aleppo pine plant extracts were prepared. Thirty male and female Wistar rats were used to study the cutaneous toxicity of extracts from the bark of P. halepensis. The extracts' healing potential for burn wounds were also assessed by evaluating the clinical and macroscopic aspects of the wounds. The antibacterial activity of crude extracts of P. halepensis as well as its wound healing abilities was verified in this investigation. RESULTS: In animals with acute dermal toxicity, there were no signs of treatment-related toxicity or death. The extracts of these plants could be transformed into phytomedicines for the treatment of infected wounds. The results demonstrated that formulated ointments are successful in treating second-degree burns in rats and may be suitable for the short-term therapeutic treatment of second-degree burns. CONCLUSION: This study successfully answered our problem, regarding the efficacy of our extract for treating second-degree burns in rats. Further studies are needed to confirm these results by identifying the molecules responsible for these activities and examining their mechanism of action.

Design and prediction of novel pyrazole derivatives as potential anti-cancer compounds based on 2D-2D-QSAR study against PC-3, B16F10, K562, MDA-MB-231, A2780, ACHN and NUGC cancer cell lines.

Despite the decades of scientific studies for developing promising new therapies, cancer remains a major cause of illness and mortality, worldwide. Several cancer types are the major topic of research in drug discovery programs due to their global incidence cases and growing frequency. In the present study, using two different statistical approaches PCA (principal component analysis) and PLS (partial least squares), six 2D-QSAR (quantitative structure activity relationship) models have been developed for the set of compounds retrieved against seven cancer cell lines vizPC-3, B16F10, K562, MDA-MB-231, A2780, and ACHN. For the creation and validation of 2D-QSAR models, OECD (Organization for Economic Co-operation and Development) requirements have been strictly followed. All of the generated 2D-QSAR models produce a significant and high correlation coefficient value with several other statistical parameters. Moreover, developed 2D-QSAR models have been used for activity predictions of in-house synthesized 63 pyrazole derivatives compounds. Precisely, most statistically significant and accepted2D-QSAR model generated for each cancer cell line has been used to predict the pIC50 value (anti-cancer activity) of all 63 synthesized pyrazole derivatives. Furthermore, designing of novel pyrazole derivatives has been carried out by substituting the essential functional groups based on the best derived 2D-QSAR models for each cancer cell line, more precisely, based on the most significant molecular descriptors with enhanced anti-cancer activity. Finally, the prediction of the new designed molecules reveals higher pIC50 than the standard compounds.

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.

Novel Co(II) and Cu(II) coordination complexes constructed from pyrazole-acetamide: Effect of hydrogen bonding on the self assembly process and antioxidant activity.

In the present study, two pyrazole-acetamide derivatives namely N­(2­aminophenyl)­2­(5­methyl­1H­pyrazol­3­yl) acetamide (L1) and (E)­N­(2­(1­(2­hydroxy­6­methyl­4­oxo­4H­pyran­3­yl)ethylideneamino)phenyl)­2­(5­methyl­1H­pyrazol­3­yl) acetamide (L2) have been synthesized and characterized by infrared spectrophotometry (IR), nuclear magnetic resonance spectroscopy (NMR) and electrospray ionization-mass spectrometry (ESI-MS). Two coordination complexes of L1 and L2, namely [Co(L1)2(EtOH)2]·Cl2 (1) and [Cu(L2)]·H2O (2), respectively have been synthesized and characterized by elemental analysis and spectroscopic studies. The solid state structure of these two complexes was established by single crystal X-ray crystallography. In complex 1, the amide O and pyrazole N atoms of two molecules of L1 take part in coordination with octahedral Co(II) ions, the remaining two coordination sites being occupied by two EtOH molecules leading to a N2O4 coordination environment. On the other hand, the imine N atoms, pyrazole N and O atoms of the 2­hydroxy­6­methyl­4H­pyran­4­one function present in L2 are involved in coordination with Cu(II) ions, resulting in a distorted square planar geometry displaying a N2O4 chromophore, in complex 2. The crystal packing analysis of 1 and 2, revealed 1D and 2D supramolecular architectures respectively, via various hydrogen bonding interactions, which are discussed in the present account. Furthermore, the antioxidant activity of the ligands and their complexes were determined in vitro by 1,1­diphenyl­2­picrylhydrazyl (DPPH), 2,2'­azino­bis(3­ethylbenzothiazoline­6­sulphonic acid (ABTS) and ferric reducing antioxidant power(FRAP), showing that the ligands L1 and L2 and complexes 1 and 2 present significant antioxidant activity.

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.

Anabasis aretioides Coss. & Moq. phenolic compounds exhibit in vitro hypoglycemic, antioxidant and antipathogenic properties.

Background Based on our previous ethnobotanical survey, the non-investigated Saharan plant Anabasis aretioides Coss. & Moq., growing in the region of Errachidia, was selected for pharmacological investigation. In Moroccan traditional medicine, A. aretioides is being used for diabetes treatment. Thus, the current work aims at evaluating the antidiabetic, antioxidant, and antibacterial activities of the plant in relation to the digestive tract. Methods The different parts of the plant (aerial parts, roots, seeds) were extracted with methanol (MeOH) and screened in enzymatic assays for their inhibitory potential against α-amylase and α-glucosidase, as well as antioxidant and antibacterial activities. Furthermore, the phenolic compounds were analyzed using HPLC-DAD-QTOF-MS. Results The MeOH extracts of A. aretioides aerial parts, roots, and seeds, respectively, inhibited α-amylase (IC50 of 3148.07 µg/mL, 2440.20 µg/mL, 3395.71 µg/mL) and α-glucosidase (IC50 of 2940.59 µg/mL, 3521.81 µg/mL, 3393.83 µg/mL). Moreover, compared to aerial parts and seeds, the plant roots exhibited higher antioxidant capacity and a potent reducing power. In resazurin microplate assay, the plant parts displayed a minimal inhibitory concentration (MIC) ranging from 7.81 mg/mL to 31.25 mg/mL. Chemical analysis revealed 25 phenolic compounds, with chlorogenic acid as the main phenolic compound in the aerial parts, hesperidin in roots, and quercitrin in seeds. Conclusion Anabasis aretioides cited for treatment of diabetes shows promising antioxidant and antibacterial properties, as well as an ability to inhibit digestive enzyme, including α-amylase and α-glucosidase. Thus, our results explain in part the traditional use of this Saharan medicine and open doors for further in vivo mechanistic and functional studies.