Chemical Composition of the Essential oil of The Leaves of Pimenta diocia (L.) Merr. & Pimenta racemosa (Mill.) cultivated in Egypt and Evaluation of Their in-vitro Antioxidant and Antidiabetic Activities

The aim of the study is to identify and characterize the chemical composition of the essential oil of both leaves of Pimenta diocia (L.) Merr. and Pimenta racemosa (Mill.)  as well as to evaluate their in-vitro antioxidant and anti-diabetic potency. Both leaves essential oil was analyzed by GC-MS analysis. Different in-vitro antioxidant tests were employed, namely, 1,1-diphenyl-2-picrylhydrazyl (DPPH), ferric thiocyanate (FTC), ferric reducing antioxidant power, thiobarbituric acid (TBA) and β-carotene-linoleate bleaching assay. Also, the present work aims to evaluate the α-amylase and α-glucosidase inhibition as well as glucose uptake by yeast cells of essential oils. Essential oil analysis of the leaves of Pimenta racemosa (Mill.) showed high amounts of eugenol (37.95%), β-Myrecene (21.01%), α-Pinene (17.82%), linalool (6.15%) and limonene (5.93%).  GC-MS data of leaves essential oil revealed the presence of  eugenol (30.17%), limonene (17.24),  α-Pinene (16.78%), linalool (9.71), 1,8 cineole (8.31%) and β-myrecene (5.21%) . Pimenta diocia (L.) Merr. and Pimenta racemosa (Mill.) leaves essential oil having antioxidant effect using various methods. In most of the oil samples and assays the antioxidant activity was higher than the one revealed by the positive control BHT. Both plants essential oil showed potent inhibition of α-Amylase at concentration 2.00 mg as it was inhibited by (75 and 63 %); with IC50 (0.95 and 1.13); respectively as well as inhibition of α-glucosidase enzyme by (61.42 and 53.00%) with IC50 (3.17 and 4.25); respectively. Also the percentage of glucose uptake by Pimenta diocia (L.) Merr. and Pimenta racemosa (Mill.) leaves essential oil at 2.00 mg/ml in the presence of 25 mM glucose is (63.49% and 49.61%); respectively. Conclusion: the present study clearly identified the Egyptian chemotype of Pimenta diocia (L.) Merr. and Pimenta racemosa (Mill.) leaves essential oil, it also displayed safe and promising antidiabetic and antioxidant properties. Therefore the essential oil of both species can be utilized as a natural antioxidant and antidiabetic as well as health benefits

Acridone-based acetylcholinesterase inhibitors: synthesis, antioxidant activity and molecular modeling

Acridone is a unique naturally occurring alkaloid known to associate with several biological activities. 2,3-dimethoxy-10-methyl-10,8a-dihydroacridin-9(8aH)-one (4) and its precursor 2-((3,4-dimethoxyphenyl)methylamino)benzoic acid (3) were synthesized and investigated for potential antioxidant and inhibitory activity against acetylcholinestrase. The synthetic pathway involves reaction of 2-(methylamino) benzoic acid (1) with 4-chloro-1,2-dimethoxybenzene (2) in presence of CuO and K2CO3 to give the precursor 3. Subsequent, cyclcondensation of 3 with Conc. H2SO4 afforded the anticipated acridone 4. Furthermore, the dimethoxyacridone derivative 4 showed potent antiacetylcholinesterase (ACHE) activity at (100 uM) with IC50 = 9.25 uM that is as potent as the reference drug rivastigmine. Assessment of total antioxidant activity of compounds 3 & 4 in comparison to known standard compounds revealed the following order: α-tocopherol > Acridone 4 > trolox > butylated hydroxyl anisole (BHA) > butylated hydroxyl toluene (BHT) > compound 3. Molecular docking characteristics of 3 & 4 within the active site of AChE (PDB: 1ACJ) co-crystallized with 9-amino-tetrahydroacridine (Tacrine) have been studied. Interestingly, the results revealed comparable binding poses to the co-crystallized ligand and demonstrates good correlation of the binding energy (DG) with the observed IC50-values. This finding suggests that compounds 3 & 4 exhibit good antioxidant effect and inhibition of acetylcholinesterase, which might provide profitable candidates in management of Alzheimer’s disease

Fatty acids Profile, Nutritional Values, Anti-diabetic and Antioxidant Activity of the Fixed Oil of Malva parviflora Growing in Egypt

In the current study, the fixed oil obtained from Malva parviflora seeds was tested for its physicochemical properties, fatty acids composition and nutritional value. The oil yield from the seed was 3.3%. The fatty acid composition was represented by 9 compounds, among which coriolic acid was the major fatty acid (31.60%), followed by pentadecanoic acid (30.05%). The antidiabetic and antioxidant activity of Malva parviflora seeds fixed oil (MPO) were also assessed. Diabetic rats were induced by injection of STZ (55mg/kg, i.p.) and diabetes was confirmed 48h after induction, and then allowed for 7 days to stabilize blood glucose level. MPO (1/100 LD50; 157mg/kg.b.w. and 1/50 LD50; 314mg/kg.b.w) was administered daily for 28 days. Treated diabetic rats significantly reduced elevated blood glucose, TC, TG, LDL-C, hepatic and renal TBARs and HP levels. The treatment also resulted in improved plasma insulin, HDL-C and GSH, SOD and CAT levels. These results clearly suggest that MPO may effectively normalize the impaired antioxidant status in streptozotocin induced diabetes as well as exert rapid protective effects against lipid peroxidation and ultimately reduce the risk of liver and renal complications