Rasheda Akter

Antidiabetic and antidiarrhoeal effects on ethanolic extract of Psidium guajava (L.) Bat. leaves in Wister rats

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Comparative Studies on Antidiabetic effect with phytochemical screening of Azadirachta indicia and Andrographis paniculata

The present study was undertaken to evaluate the antidiabetic properties with phytochemical screening of the ethanol leaves extracts of two common indigenous medicinal plants of Bangladesh -Azadirachta indica (Neem) and Andrographis peniculata (Kalomegh) on experimental animal model. Hypoglycemic activity of the concentrated ethanolic (90%) extract of Azadirachta indica and Andrographis peniculata were studied compared with that of a reference antidiabetic drug glimeperide in both glucose loaded and alloxan induced diabetic rats. The acute toxicity of these two plants extract was also studied. Experimental results showed that ethanol leaves extract (1 gm/kg) of Azadirachta indica and Andrographis peniculata significantly (P<0.01) reduced the elevated blood glucose level by 36.91 % and 40.65 % respectively in glucose loaded rats and 30.20 % and 32.18 % respectively in alloxan induced diabetic rats compared to the respective diabetic control group. This study strongly suggested that ethanol leaves extracts of Azadirachta indica and Andrographis peniculata possess significant antidiabetic activity and could be a potential source for treatment of diabetes mellitus.

Antioxidative Potential of the Polyphenolics of Stephania japonica var. Discolor (Blume) Forman: A Chromatographic (High-Performance Liquid Chromatography) and Spectrophotometric Measure

This study investigated the quantitative phytochemical contents, total phenolics, total flavonoids, total carotenoids, antioxidative capacity, tannin, proanthocyanidins, lycopene, chlorophyll a, and chlorophyll b of the Stephania japonica extract. Comprehensive antioxidative effects of the extract were also investigated. Quantitative assays were conducted through both spectrophotometric and high-performance liquid chromatographic methods. Antioxidative effects were measured through FeCl3 reducing power, metal chelating power, reducing power, 2,2’-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid (ABTS) scavenging activity, N, N-dimethyl-1,4-diaminobenzene free radical scavenging activity, superoxide radical scavenging activity, and nitric oxide scavenging effect. The contents of total phenolics, total flavonoids, total carotenoids, total antioxidative capacity, tannin, proanthocyanidins, lycopene, chlorophyll a, and chlorophyll b were found to be 47.32 ± 0.75 mg tannic acid equivalent, 61.41 ± 1.58 mg catechin equivalent, 63.29 ± 2.21 mg, 22.85 ± 0.70 mg ascorbic acid equivalent, 76.17 ± 0.97 mg tannic acid equivalent, 94.96 ± 4.49 mg catechin equivalent, 22.19 ± 0.79 µg, 22.19 ± 0.79 µg, 7.52 ± 1.24 mg, and 10.43 ± 2.11 mg, respectively, in 1 g of ethanol extract. A high concentration of epicatechin, p-coumaric acid, and rutin hydrate and moderate concentration of caffeic acid and quercetin was detected in the extract. The IC50 value for ferric reducing power assay, metal chelating assay, reducing power assay, ABTS scavenging assay, N, N-dimethyl-1,4-diaminobenzene scavenging assay, superoxide scavenging assay and nitric oxide (NO) assay were 465.06 ± 7.32 µmol ascorbic acid/g, 1656.52, 270.55, 457.27, 632.74, 217.5, and 464.00 µg/mL, respectively. No beta carotene was detected in the extract. The extract was demonstrated to be a very potential source of antioxidative metabolites.

In silico ADME/T and 3D QSAR analysis of KDR inhibitors -

Tyrosine kinases (KDR) have been considered as a potential targets for the design of new anticancer agents. Recently, a series of N-4-chlorophenylnaphthamides has been reported with KDR inhibitory activity. In order to demonstrate the pharmacokinetics and the relationship between the structures and their inhibition of KDR, 3D-QSAR and in silico ADME/T analysis were performed on a dataset of 13 compounds. Quantum chemical parameters such as LUMO energy, HOMO energy, ionization energy (I), electron affinity (A), chemical potential (μ), hardness (η) and electrophilicity (χ) of the compounds are calculated by using semi-empirical SCF-MO method at PM3 level of theory and various SlogP descriptors from MOE software. In silico ADME/T analysis was performed by using different software’s Discovery Studio 2.5, TOPKAT and QikProp 4.3. From in silico ADME and Toxicity studies, it was revealed that selected derivatives have good oral absorptions and metabolisms with no BBB penetration. QSTR (Quantitative Structure Toxicity Relationship) studies by using TOPAK in various computational animal models, showed high LD50 values and the compounds are found to be noncarcenogenic. Moreover, three different QSAR models were generated by Partial Least Squares (PLS) Regression method having correlation coefficient (Q2) of 0.86382, 0.84372, and 0.82629, respectively. These models conclude a significant relationship of KDR inhibition with dipole moment (D), LUMO energy (ELUMO), hardness (η) and electrophilicity (χ), and hydrophobicity of compounds, regarding N-4-chlorophenylnaphthamides.