scholarly journals Acute toxicity and hypoglycemic activity of 7-chloro-4-thiosubstituted quinoline

Author(s):  
Ana Bogdan ◽  
◽  
Serhiy Brazhko ◽  
Iryna Labenskaya ◽  
Oleksandr Brazhko ◽  
...  
2016 ◽  
Vol 2016 ◽  
pp. 1-7 ◽  
Author(s):  
Marcela Soto-García ◽  
Martha Rosales-Castro ◽  
Gerardo N. Escalona-Cardoso ◽  
Norma Paniagua-Castro

Quercus sideroxyla is a wood species whose bark has phenolic compound and should be considered to be bioactive; the hypoglycemic and genotoxic properties of Q. sideroxyla bark were evaluated in this study. Total phenolic compound was determined in crude extract (CE) and organic extract (OE). The OE has the highest amount of phenols (724.1±12.0 GAE/g). Besides, both CE and OE demonstrated effect over the inhibition of α-amylase in vitro. Hypoglycemic activity was assessed by glucose tolerance curve and the area under curve (UAC); OE showed the highest hypoglycemic activity. In addition, diabetes was induced by streptozotocin (65 mg/kg) and the extracts (50 mg/kg) were administered for 10 days; OE showed hypoglycemic effect compared with diabetic control and decreased hepatic lipid peroxidation. Acute toxicity and genotoxicity were evaluated in CE; results of acute toxicity did not show any mortality. Besides, the comet assay showed that CE at a dose of 100 mg/kg did not show any genotoxic effect when evaluated at 24 h, whereas it induced slight damage at 200 mg/kg, with the formation of type 1 comets.


2018 ◽  
pp. 95-104
Author(s):  
M. I. Romanenko ◽  
D. G. Ivanchenko ◽  
T. A. Sharapova ◽  
I. M. Bilay ◽  
K. V. Aleksandrova

According to the International Diabetes Federation in 2015 were registered 59.8 million patients with diabetes in Europe. Synthetic drugs are widely applied in addition to a variety of insulins to normalize blood glucose level. It should be noted that the oral anti-diabetic drugs are the common therapeutic agents for the treatment of diabetes mellitus type II, and therefore the search for new non-toxic hypoglycemic agents is one of the most urgent problems of modern pharmaceutical science. It is known that 7,8-disubstituted xanthine derivatives exhibit hypoglycemic activity. The aim of this work lies in developing unique method to synthesize undocumented in other scientific papers 7-n-butyl-3-methyl-8-thioxanthine derivatives and also studying of their hypoglycemic activity. Acute toxicity of synthesized compounds has been studied with the application of Prozorovsky’s method. The glucose homeostasis characteristic has been performed on carbohydrate tolerance that has been determined by the glucose load test on the control group and on the intact rats. The reactions of 7-n-butyl-3-methyl-8-thioxanthine with benzylchlorides, bromoketones, esters and an amide of chloroacetic acid have been studied. Reactions of mentioned syntons proceed smoothly in aqueous propanol-2 environment and lead to the formation of the corresponding 8-benzyl-, benzoylmethylthioxanthines and xanthinyl-8-thioacetic acid derivatives. Accessible laboratory method has been elaborated to synthesize unspecified in scientific papers earlier 8-thiosubstituted 7-n-butyl-3-methylxanthine by reacting 7-n-butyl-3-methyl-8-thioxanthine with benzylchlorides, bromoketones, esters and an amide of chloroacetic acid, their structure having been proved by NMR-spectroscopy data. The acute toxicity of synthesized compounds has been studied. It has been established that LD50 is in the range 820–2477 mg/kg, i. e. obtained substances are low-toxic and practically non-toxic according to Sidorov’s classification. Also the study of hypoglycemic activity of synthesized compounds has been carried out. A significant perspective for further research to find the original antidiabetic agents has been shown by bioassay results. It has been found that 7-n-butyl-3-methylxanthinyl-8-thioacetamide is more active than reference substances.


2016 ◽  
Vol 14 (1(53)) ◽  
pp. 46-52
Author(s):  
V. O. Chornous ◽  
O. Ya. Melnyk ◽  
O. M. Hliebov ◽  
M. V. Tykhonenko ◽  
L. M. Sheremeta ◽  
...  

Planta Medica ◽  
2016 ◽  
Vol 81 (S 01) ◽  
pp. S1-S381
Author(s):  
GM Avila-Villarreal ◽  
DE Giles-Rivas ◽  
B Aguilar-Guadarrama ◽  
P Castillo-España ◽  
S Estrada-Soto

1968 ◽  
Vol 20 (03/04) ◽  
pp. 588-595 ◽  
Author(s):  
E. B Goodsell ◽  
R. A Krause ◽  
E. T Kimura

SummaryUbiquin (oligo-3-(N-methylmorpholinium)-l,2-propylene oxide chloride) is a stable, water soluble, active heparin antagonist producing prompt neutralization when administered in a 1:1 ratio to rats and dogs. Initial studies indicate that it is devoid of any effect on coagulation per se; nor are there any obvious side effects manifested during the process of neutralization. The acute toxicity is less than that of other compounds in use: toluidine blue, protamine and hexadimethrine.


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