• Biomolecules & Therapeutics
• /
• 제28권4호
• /
• pp.361-369
• /
• 2020

Tofacitinib, a Janus kinase inhibitor, was developed for the treatment of rheumatoid arthritis. Recently, it has been associated with an increased change in arthritis development in patients with diabetes. Herein, we evaluated the pharmacokinetics of tofacitinib after intravenous (10 mg/kg) and oral (20 mg/kg) administration to rats with streptozotocin-induced diabetes mellitus and control rats. Following intravenous administration of tofacitinib to rats with streptozotocin-induced diabetes mellitus, area under the plasma concentration-time curve from time zero to infinity of tofacitinib was significantly smaller (33.6%) than that of control rats. This might be due to the faster hepatic intrinsic clearance (112%) caused by an increase in the hepatic cytochrome P450 (CYP) 3A1(23) and the faster hepatic blood flow rate in rats with streptozotocin-induced diabetes mellitus than in control rats. Following oral administration, area under the plasma concentration-time curve from time zero to infinity of tofacitinib was also significantly smaller (55.5%) in rats with streptozotocin-induced diabetes mellitus than that in control rats. This might be due to decreased absorption caused by the higher expression of P-glycoprotein and the faster intestinal metabolism caused by the higher expression of intestinal CYP3A1(23), which resulted in the decreased bioavailability of tofacitinib (33.0%) in rats with streptozotocin-induced diabetes mellitus. In summary, our findings indicate that diabetes mellitus affects the absorption and metabolism of tofacitinib, causing faster metabolism and decreased intestinal absorption in rats with streptozotocin-induced diabetes mellitus.

• 동의생리병리학회지
• /
• 제21권2호
• /
• pp.474-478
• /
• 2007

This study evaluated effects of Yanggyuksanhwa-tang(YST) on diabetic rats. Diabetic condition in rats was induced by streptozotocin injection. Then control effect of YST was observed with changes of serum glucose, insulin, and triglyceride levels and hepatic glucokinse activity. YST treatment was resulted significant decrease of high serum glucose level of diabetic rats induced by streptozotocin at 5th day of YST treatment. YST treatment was resulted increase of low serum insulin level of diabetic rats induced by streptozotocin, but it was not significant statistically. YST treatment was resulted significant decrease of high serum triglyceride level of diabetic rats induced by streptozotocin at 3rd and 5th of YST treatment. YST treatment was resulted significant increase of low hepatic glucokinase activity of diabetic rats induced by streptozotocin at 5th day of YST treatment. These results suggest that YST has effects on serum glucose control against cerebral inchemic damage under diabetic condition.

• 대한약침학회지
• /
• 제3권2호
• /
• pp.99-130
• /
• 2000

This study was carried out to investigate the effects of Liriopis Tuber Herbal-Acupuncture on Diabetes Mellitus induced by streptozotocin in rat. Body weight, serum insulin, glucose, triglyceride, HDL cholesterol, free cholesterol and total protein were measured in streptozotocin induced diabetic rat injected with Liriopis Tuber Herbal-Acupuncture solution at Pisu(BL20) respectively for 30 days. In order to study the effects of Liriopis Tuber Herbal-Acupuncture at Pisu(BL20) on Diabetes Mellitus induced by Streptozotocin in rat, The groups were divided into five groups; Normal group(non treated group), N.-Saline group(administration of injection with normal saline at BL20 in 30 days after streptozotocin injection), Control group(non treated group after streptozotocin injection), H. Acup. group (administration of Liriopis Tuber Herbal-Acupuncture at BL20 in 30 days after streptozotocin injection), and Acup. group (administration of acupuncture at BL20 in 30 days after streptozotocin injection). The results obtained were summarized as follows; 1. As compared with Control group, there wae no significant tendency to diminish the rate of weight loss in H. - Acup. group. 2. As compared with Control group, there wae signiticant increase of serum insulin level in H. -Acup. group. 3. As compared with Control group, there was decrease of glucose level in H.- Acup. group. 4. As compared with Control group, there was decrease of triglyceride level in H. - Acup. group. 5. As compared with Control group, trere wae increase of HDL cholesterol level in H. - Acup. group. 6. As compared with Control group, there was significant increase of free cholesterol level in H. - Acup. group. 7. As compared with Control group, there was Increase of total protein level in H. - Acup. group. According to above mentioned results, Liriopis Tuber Herbal-Acupuncture was expected to be effective in treatment of Diabetes Mellitus and its complications.

• Journal of Ginseng Research
• /
• 제16권3호
• /
• pp.190-197
• /
• 1992

The increased level of glucose, ketone bodies, non-esterified fatty acids and lactate in blood, decrease of glycogen content, phosphofructokinase activities and glucokinase activity and the increased level of glucose-6-phosphatase activity in the liver of streptozotocin injected rats were significantly moderated by ginseng saponin administration. It is not likely, however, that the hypoglycomic action of ginseng saponin might be due to their direct action on enzyme activities, since the saponin effect of servers enzymes in vitro was not enough to explain such an appreciable hypoglycemic activity of the saponin in streptozotocin induced diabetic rats, for which much work have to be done.

• International Journal of Industrial Entomology and Biomaterials
• /
• 제5권2호
• /
• pp.201-204
• /
• 2002

This study was undertaken to find effects of ethanol extracts from Bombyx mori on the hyperglycemia induced by streptozotocin in rats. Blood glucose level of rats increased depending on experimental days after streptozotocin treatment. But there was no difference in blood glucose level between the rats injected with ethanol extracts of B. mori and normal rats. There was no significant difference in the kidney fibrosis between the rats injected with ethanol extrscts of B. mori and normal rats at all ages examined. The transforming growth factor-$\beta$l ($TGF-{\beta}1$) protein was detected in the glomerulay endothelial cells and tubular epithelial cells of streptozotocin rats at 14 days of age. In the rats injected with ethanol extracts of B. mori to the kidneys, the $TGF-{\beta}1$ protein was detected very faintly. The $TGF-{\beta}1$ mRNA of streptozotocin rats increased at 14 days of age, and this was higher than the rats injected with ethanol extrscts of B. mori. Taken these together, the results suggest that the ethanol extracts of B. mori ameliorate hyperglycemia of the rats induced by streptozotocin.

• 한국식품위생안전성학회지
• /
• 제5권4호
• /
• pp.237-242
• /
• 1990

Streptozotocin에 의한 적혈구의 막 lipid peroxidation 측정시 TBA법의 적합성에 관하여 검토하기 위하여 Streptozotocin와 TBA의 직접반응 여부를 연구하였다. 여러 농도의 Streptozotocin 와 20% RBC suspension을 함께 배양한 후 lipid peroxidation을 TBA법으로 측정했을 때, Streptozotocin의 농도에 따라 흡광도가 증가하다가 100mM부터는 plateau를 이루었다. 그런데 적혈구를 제거한 대조실험에서도 발색단이 관찰되었다. 시험관에서 5mM의 Streptozotocin와 1% TBA를 산성조건에서 가열 직접 반응시킨 후 spectrum을 찍은 결과 TBA법 측정파장인 532nm에서 새로운 peak가 생겼다. 또 이 파장에서의 흡광도는 Streptozotocin 농도에 따라 증가하다가 25mM부터는 plateau가 되었다. 이러한 결과들은 적혈구와 Streptozotocin를 함께 배양하여 lipid peroxidation을 측정할 때, cell 내로 유입된 Streptozotocin 가 TBA와 직접반응을 할 수 있음을 제시한다. 그리고 다른 측정법인 lipid conjugation은 233nm에서의 흡수를 측정하는데. Streptozotocin 자체가 200-300nm에서 흡수를 나타내므로 이 방법으로도 lipid peroxidation 측정을 방해할 수 있다. 따라서 Streptozotocin에 의한 적혈구막의 lipid peroxidation은 TBA method 및 lipid conjugation 방법으로 측정하기는 부적합한 것으로 사료된다.

• Archives of Pharmacal Research
• /
• 제23권5호
• /
• pp.461-466
• /
• 2000

Tectorigenin and kaikasaponin III from the flowers of Pueraria thunbergiana showed potent hypoglycemic and hypolipidemic effects in the streptozotocin-induced diabetic rats. Intraperitoneal administration of these two compounds with 5 and 10 mg/kg, respectively, for seven days to streptozotocin-induced rats significantly reduced the blood glucose, total cholesterol, LDL- and VLDI-cholesterol and triglyceride levels when compared with those of control group. Glycitein in which 5-OH is unlinked and tectoridin (7-O-glycoside of tectorigenin) isolated from the flowers of P. thunbergiana did not improve hyperglycemia and hyperlipidemia. In addition, tectorigenin showed in vitro antioxidant effects on 1,1-diphenyl-B-pirylhydrazyl (DPPH) radical, xanthine-xanthine oxidase superoxide anion radical, and lipid peroxidation in rat microsomes induced by enzymatic and non-enzymatic methods. We further found that tectorigenin and kaikasaponin III protected the Vero cell line(normal monkey kidney) from injury by hydrogen peroxide. From these findings, it seems likely that the antioxidant action of tectorigenin and kaikasaponin III may alleviate the streptozotocin-induced toxicity and contribute to hypoglycemic and hypolipidemic effects.

• 대한예방한의학회지
• /
• 제3권1호
• /
• pp.83-100
• /
• 1999

This present study was carried out to investigate the effect of Saengjingamrotang and Saengjingamrotang plus Radix Trichosanthis in streptozotocin induced hyperglycemic rats. Body weight, serum levels of glucose insulin total cholesterol triglyceride and urine levels of volume glucose protein were measured in streptozotocin induced hyperglycemic rats orally receiving extracts of Saengjingamrotang and Saengjingamrotang plus Radix Trichosanthis for 4 days. According to above mentioned results, Saengjingamrotang and Saengjingamrotang plus Radix Trichosanthis have the effect of decreased blood sugar, serum lipid levels and urine volume, protein, glucose in streptozotocin induced hyperglycemic rats, and so they were expected to be appled to the treatment of diabetes mellitus.

• 한국식품영양과학회지
• /
• 제20권3호
• /
• pp.203-208
• /
• 1991

The present study was undertaken in order to elucidate the effects of pretreatment with nicotinamide on changes in the hepatic metabolizing enzyme system inducted by streptozotocin (STZ). In rats, STZ(50mg/kg) administered by tail vein caused a significant rise in hepatic aniline hydroxylase and a decrease in aminopyrine N-demethylase when compared to control (p<0.05). Pretreatment with nicotinamice inhibited these effects (p<0.05). Similarly, STZ induced changes in hepatic microsomal cytochrome P-450 activity were inhibited by pretreatment with nicotinamide (p<0.05). However, changes in UDP-glucuronyl transferase and sulfortransferase activity were not significantly different(p>0.05). Pretreatment with nicotinamide also prevented STZ induced increases in glutathion S-tranferase activity when compared to the control(p<0.05). There results suggest that nicotinamide pretreatment suppresses STZ-induced changes in the hepatic metabolizing enzyme system.

• 생약학회지
• /
• 제40권3호
• /
• pp.213-217
• /
• 2009

This study was done to investigate the antioxidative effect of polygoni radix in Streptozotocin (STZ)-induced diabetic rats. Diabetes was induced by intravenous injection of STZ at a dose of 45 mg/kg dissolved in citrate buffer. The ethanol extract of Polygoni radix was orally administrated once a day for 7 days. The contents of Total cholesterol, triglyceride (TG) were significantly decreased in Polygoni radix treated STZ-sample group compared with to the those of STZ-control group. The hepatic cytosolic activities of glutathione-s-transferase (GST), superoxide dismutase (SOD) were significantly increased, Also the content of glutathione (GSH) was incresaed in Polygoni radix treated STZ-sample group compared with to the those of STZ-control group. but the content of malondialdehyde (MDA) and the hepatic cytosolic activity of Catalase (CAT) were decreaed but not statistical significant. These results indicated that ethanol extract of polygoni radix was effective for the antidxidative in the STZ-induced diabetic rats.