Keybrown9964

Objectives The aim was the synthesis of novel substituted 5-[morpholino(phenyl)methyl]-thiazolidine-2,4-diones and screening for their in vivo hypoglycemic activity and in vitro anti-inflammatory activity, as well as molecular docking studies to find out active potential lead molecules. Materials and methods Substituted aromatic aldehydes, thiazolidine-2,4-dione, and morpholine on Mannich reaction gave the title compounds. They were characterized by physical and spectral methods. In vivo hypoglycemic activity was examined in alloxan induced Wistar albino rats by tail tipping method. In vitro anti-inflammatory activity was tested by human red blood cell (HRBC) membrane stabilization and protein denaturation. Using AutoDock, molecular docking studies were carried out to find out the best fit ligands. Results Series of substituted 5-[morpholino(phenyl)methyl]-thiazolidine-2,4-diones were synthesized and chemically they were confirmed by spectral techniques. Acute toxic studies of in vivo hypoglycemic activity rehypoglycemic and anti-inflammatory activities. Compounds 4h and 4n exhibited higher binding affinity at PPARγ receptor protein and compound 4k exhibited higher binding affinity at COX isoenzymes' active sites in molecular docking studies.Objectives Cnidoscolus aconitifolius Mill. I.M.Johnst. Selleck MV1035 is a medicinal plant widely used in ethnomedicine for the treatment of cancer and other diseases. Materials and methods The effects of methanol extracts of the leaf, stem, and root barks were evaluated on breast (MCF-7) and lung (NCI-H460) cancer cells at 1-250 μg/mL using the SRB assay and the extracts were screened for phytochemicals using the standard method. Results The stem and root extracts showed no activity at the maximum concentration, while the leaf extract at 100 μg/mL showed remarkable cell growth inhibition against breast (-14.50±0.58) and lung cancer (+53.29±4.57) in vitro. The extracts showed the presence of saponins, terpenes, cardiac glycosides, and phenolic compounds. Partitioning of the active leaf extract further enhanced its activity as the chloroform fraction exhibited GI50, LC50, and total growth inhibition (TGI) of 22.5, 68.75, and 43.75 μg/mL against breast cancer, respectively, and GI50 and TGI of 35.4 and 55.8 μg/ mL against lung cancer cells, respectively. However, the aqueous fraction showed no cytotoxicity against either cell line. Conclusion These results justified the ethnomedicinal uses of the plant against tumor-related ailments. Isolation of the constituents responsible for the observed activity needs to be carried out to further support this claim.Tobacco smoke from regular cigarettes contains a number of harmful chemicals such as nicotine, arsenic, benzene, carbon monoxide, heavy metals, and tobacco-derived nitrosamines. About 1% of over 7000 chemical substances formed by burning tobacco are identified as the leading causes or possible risk factors of smoking-related diseases such as lung cancer, cardiovascular diseases, and emphysema. The concept of heating tobacco without combustion and smoke has been designed for more than two decades. The products developed with this idea, known as "Heat-Not-Burn" tobacco cigarettes, were first introduced in the late 1980s but did not achieve commercial success. However, the tobacco giants have been trying to remarket tobacco heating systems with new technological and modified features for over 10 years. I-Quit-Ordinary-Smoking (iQOS®) is one of the latest heat-not-burn tobacco products, first launched in Japan and Italy. The company then made a submission to the Food and Drug Administration as a modified-risk tobacco product application to sell its own tobacco-heating device iQOS® under its Marlboro® brand in the USA with reduced-risk claims in 2016, but it was rejected. This device is, however, now sold in more than four dozen countries. There are some striking claims that iQOS®, which is described as a novel hybrid product between traditional cigarettes and electronic cigarettes, offers an alternative way to substantially reduce the amount of harmful components compared with traditional cigarettes by its new technology in which tobacco is heated up to 350°C instead of being burnt. It is claimed to produce vapour containing nearly 90% less toxic substances than cigarette smoke and not be a source of second-hand smoking negatively affecting indoor air quality. The purpose of this article is to objectively review the potential effects of iQOS® on human health and the environment by searching and integrating the published research findings.Objectives Ionizing radiation (IR) induces DNA damage in normal cells, leading to genotoxicity. The radioprotective effects of co-treatment with curcumin and piperine were investigated against genotoxicity induced by IR in human normal lymphocytes. Materials and methods Human blood samples were pretreated with curcumin at different concentrations (5, 10, and 25 μg/mL) and/or piperine (2.5 μg/mL) and then were exposed to IR at a dose 1.5 Gy. The radioprotective effects of curcumin and piperine were assessed by micronucleus (MN) assay. Results Curcumin and piperine reduced the percentage of MN induced by IR in lymphocytes. Piperine alone significantly reduced genotoxicity induced by IR as compared to curcumin alone at all concentrations. An additive radioprotective effect was observed with combination of piperine and curcumin at the low concentration of 5 μg/mL, while this synergistic effect was not observed with curcumin at the higher concentrations of 10 and 25 μg/mL. Conclusion Piperine has a potent radioprotective effect at low concentration as compare to curcumin. However, an additive radioprotective effect was observed with co-treatment with piperine and curcumin at low concentration, while piperine increased the percentage of MN in normal lymphocytes when co-treated with curcumin at higher concentration.Objectives Moringa peregrina has long been used in folk medicine to treat diseases including fever, headache, burns, constipation, gut pains, and inflammation. Nitric oxide (NO) and interleukin-1β (IL-1β) play an important role in the pathophysiology of inflammation. The objectives of this study were to determine the effect of M. peregrina seed ethanolic extract (MPSE) on the viability of and NO and IL-1β production by lipopolysaccharide (LPS)-activated macrophage (J774A.1) cell line. Materials and methods The 3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyltetrazolium bromide assay was used to determine the cytotoxic effect of MPSE treatment at concentrations ranging from 31.15 to 1000 μg/mL. The NO concentration was determined by Griess assay and IL-1β proinflammatory cytokine concentration by enzyme-linked immunosorbent assay in the supernatant of MPSE-treated LPS-activated J774A.1 cell culture. Results The results show that the MPSE was not cytotoxic at 1000 μg/mL but significantly (p less then 0.001) inhibited NO and IL-1β production by the LPS-activated macrophage J774A.