In vivo glucose-6-phosphatase inhibitory,toxicity and antidiabetic potentials of 2-picolylamine thioureas in Swiss albino mice

The 2-picolylamine is a simplest analogue of the alkaloid that has secondary and tertiary nitrogen function in its cyclic structure like that of alkaloids that can be derivatized to a number of biologically active compounds. In connection to our previous work, in the present work, three thiourea derivatives (I = 1,3-bis(2-benzyl-3-phenyl-1-(pyridine-2-yl) propyl) thiourea, II = 1,3-bis (pyridin-2-ylmethyl) thiourea, and III = 1-(2-benzyl-3-phenyl-1-(pyridine-2-yl) propyl)-3-phenylthiourea) were synthesized using 2-picolylamine template which is a readily available synthetic analogue of naturally occurring alkaloid. The biological effect of the synthesized derivatives were monitored on the activity of glucose-6-phosphatase in Swiss albino mice (21-days). The derivatives were also tested for their potential toxicity in a 28-days sub-chronic toxicity studies by assessing their effects on different parameters like hematological, serum biochemistry and liver histology. The therapeutic effect of the safe derivative (I) was examined in streptozotocin-induced diabetic mice as well. The derivatives showed inhibition of the enzyme activity from good to an excellent degree. Compound I had the highest inhibition with 21.42 ± 5.113 mg of the released phosphate as compared to that of the positive control group (84.55 ± 3.213 mg). Only I turned out to be safe for use in animals without exerting any toxic or lethal effects on any of the assessed parameters in the used animal model. Compound I efficiently reversed the effects like hyperglycemia, hyperlipidemia and weight loss in the test animals. Out of these three-tested compounds, I was found safe to be use as therapeutic agent in diabetes complications. However, further toxicological studies in other animal models are needed as well.     

Salicylic Acid Induced Photosynthetic Adaptability of Raphanus sativus to Salt Stress is Associated with Antioxidant Capacity

Journal of Plant Growth Regulation - Despite the plethora of published reports on ameliorative effects of exogenously applied salicylic acid (SA) to plants under salt stress, a critical role of SA...     

LAP2 Proteins Chaperone GLI1 Movement between the Lamina and Chromatin to Regulate Transcription

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Systematic analysis of HD-ZIP transcription factors in sesame genome and gene expression profiling of SiHD-ZIP class I entailing drought stress responses at early seedling stage

Molecular Biology Reports - Sesame is an ancient oilseed crop, known for its high oil content and quality. Its sensitivity to drought at early seedling stage is one of the limiting factors...     

Assessment of Heavy Metals and Metalloids in Solanum tuberosum and Pisum sativum Irrigated with Urban Wastewater in the Suburbs of Sargodha City,Pakistan

Dietary exposure to heavy metals (viz., Ni, As, Fe, Cr, Mn, Co, Mo, Cu, Zn, Se, Cd, and Pb) has been recognized as a potential hazard to human health. This study investigates the level of contamination at two different sites in Pakistan, one irrigated with canal water (Site-I) and the other with urban wastewater (Site-II). At Site-II, irrigation with wastewater resulted in a significant increase in heavy metals and metalloids in soil and a subsequent build-up in two vegetables selected for study (Solanum tuberosum [potato] and Pisum sativum [pea]). Results showed that mean concentrations of heavy metals and metalloids in soil at Site-I were lower than those of Site-II. Mean concentrations of As and Cd in soil at both sites and for both vegetables were found above maximum permissible levels, while for both vegetables As at both sites and Cd, Mo, and Pb exceeded the suggested maximum levels for vegetables. High levels of some metals in the soils and vegetables could be due to unnecessary use of fertilizers and disposable water for irrigating the soils and the environmental cues prevalent in the areas, such as presence of ions that may bind the metals, often play an important role in uptake.     

Syntheses and biological activities of chalcone and 1,5-benzothiazepine derivatives: promising new free-radical scavengers, and esterase, urease, and alpha-glucosidase inhibitors

A series of 2,4-diaryl-2,3,4,5-tetrahydro- (36-40) and 2,4-diaryl-2,3-dihydro-1,5-benzothiazepines (25-35) have been synthesized from the corresponding chalcones 1-24. Both the benzothiazepines and chalcones were evaluated as DPPH free-radical scavengers and as inhibitors of cholinesterases, urease, and alpha-glucosidase. Compounds 2, 5, 6, 7, 10, 13, 18, 21, 36a, 37a, 37b, and 39a showed significant cholinesterase inhibiting activities. Among the 15 dihydro-1,5-benzothiazepines, 26, 32, and 35 exhibited significant radical-scavenging activities; and six tetrahydro-1,5-benzothiazepines (35, 36a, 36b, 37a, 37b, and 39a) were found to be inhibitors of AChE and BChE. Compounds 22, 25, 26, 33, 35, 36a, 37b, and 39a inhibited urease, and 25 and 27-31 were found to be potent inhibitors of alpha-glucosidase.     

A Drosophila Model of Intellectual Disability Caused by Mutations in the Histone Demethylase KDM5

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Health risk assessment of heavy metals and metalloids via dietary intake of a potential vegetable (Coriandrum sativum L.) grown in contaminated water irrigated agricultural sites of Sargodha,Pakistan

Levels of Mo, As, Se, Fe, Cu, Zn, Ni, and Pb were determined in a vegetable commonly consumed in Pakistan. Samples were collected from three different sites (Ratokala, Phularwan, and Mailowal) supplied with three different water sources. Mo and Pb in water and Mo and As in C. sativum were higher than the suggested standards at the international level. Lower bioconcentration factor and pollution load index were seen at Site-I than at other sites. A positive association was found between the rhizosphere metals and those of the vegetable at all three sites. Enrichment factor at three sites ranged from 0.28 to 10.39. The highest value of daily intake of metals was found for Fe (0.245 mg/kg/day) and of the health risk index for As (70.41) at the wastewater inundated site. It is inferred that uptake of Mo, As, Cu, Ni, and Pb through C. sativum represents a high health danger to the individuals using this vegetable.