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Antihyperglycaemic activity of 2,4:3,5-dibenzylidene-D-xylose-diethyl dithioacetal in diabetic mice.

Gruzman A, Elgart A, Viskind O, Billauer H, Dotan S, Cohen G, Mishani E, Hoffman A, Cerasi E, Sasson S - J. Cell. Mol. Med. (2012)

Bottom Line: The effective blood EH-36 concentration in treated animals was 2 μM.This stimulatory effect was mediated by Thr(172) -phosphorylation in AMPK.These findings indicate that EH-36 is a promising prototype molecule for the development of novel antidiabetic drugs.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmacology, Institute for Drug Research, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel.

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Related in: MedlinePlus

Antihyperglycaemic effects of EH-36 in STZ-C57BL/6 and KKAy diabetic mice. (A) STZ-C57BL/6 mice were injected s.c. twice daily for 4 days 10 mg EH-36/kg body weight (black circles) or 150 μl sesame oil (open circles). Blood glucose levels were determined at the indicated times. (B) KKAy mice were similarly treated with EH-36 (black squares) or the vehicle (open squares). (C) Plasma insulin levels were determined in samples taken from the EH-36- and oil-treated KKAy mice described in (B). (D) Normal (non-diabetic) C57BL/6 mice were treated with EH-36 or oil as described above. The blood glucose levels at day zero were 7.8 ± 0.6 and 7.6 ± 0.9 mM for the control and EH-36 treated group, respectively. Mean ± S.E.M., n = 5–10, *P < 0.05 in comparison with the oil-treated groups.
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fig02: Antihyperglycaemic effects of EH-36 in STZ-C57BL/6 and KKAy diabetic mice. (A) STZ-C57BL/6 mice were injected s.c. twice daily for 4 days 10 mg EH-36/kg body weight (black circles) or 150 μl sesame oil (open circles). Blood glucose levels were determined at the indicated times. (B) KKAy mice were similarly treated with EH-36 (black squares) or the vehicle (open squares). (C) Plasma insulin levels were determined in samples taken from the EH-36- and oil-treated KKAy mice described in (B). (D) Normal (non-diabetic) C57BL/6 mice were treated with EH-36 or oil as described above. The blood glucose levels at day zero were 7.8 ± 0.6 and 7.6 ± 0.9 mM for the control and EH-36 treated group, respectively. Mean ± S.E.M., n = 5–10, *P < 0.05 in comparison with the oil-treated groups.

Mentions: The effect of EH-36 on blood glucose levels was evaluated following its s.c. injection (10 mg/kg of EH-36, twice a day) to STZ-treated C57BL/6 mice and KKAy diabetic mice. EH-36 demonstrated marked antihyperglycaemic activity: it significantly reduced blood glucose in STZ-treated C57BL/6 mice by 33% and 54% on days 3 and 4 of treatment, respectively, whereas oil treatment (vehicle) had no effect (Fig. 2A). EH-36 was even more effective in KKAy diabetic mice: blood glucose was reduced by 39%, 55% and 60% on days 2, 3 and 4 of treatment, respectively (Fig. 2B). Similar results were observed in these animals when the treatment was extended to 7 days. Yet, normoglycaemia was not attained in the diabetic mice following these 4- and 7 day treatments. In the rest of the experiment the mice were treated with EH-36 for 4 days to minimize the accumulation of oil at the sites of injection and to lower the risk of developing inflammatory reactions. In parallel with the reduction of blood glucose concentration, the KKAy mice, which are usually hyperinsulinaemic, became normoinsulinaemic during this treatment (Fig. 2C). The glucose-lowering effect of EH-36 was not restricted to diabetic animals: Figure 2D shows that it reduced blood glucose also by 20–25% in normoglycaemic control C57BL/6 mice.


Antihyperglycaemic activity of 2,4:3,5-dibenzylidene-D-xylose-diethyl dithioacetal in diabetic mice.

Gruzman A, Elgart A, Viskind O, Billauer H, Dotan S, Cohen G, Mishani E, Hoffman A, Cerasi E, Sasson S - J. Cell. Mol. Med. (2012)

Antihyperglycaemic effects of EH-36 in STZ-C57BL/6 and KKAy diabetic mice. (A) STZ-C57BL/6 mice were injected s.c. twice daily for 4 days 10 mg EH-36/kg body weight (black circles) or 150 μl sesame oil (open circles). Blood glucose levels were determined at the indicated times. (B) KKAy mice were similarly treated with EH-36 (black squares) or the vehicle (open squares). (C) Plasma insulin levels were determined in samples taken from the EH-36- and oil-treated KKAy mice described in (B). (D) Normal (non-diabetic) C57BL/6 mice were treated with EH-36 or oil as described above. The blood glucose levels at day zero were 7.8 ± 0.6 and 7.6 ± 0.9 mM for the control and EH-36 treated group, respectively. Mean ± S.E.M., n = 5–10, *P < 0.05 in comparison with the oil-treated groups.
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Related In: Results  -  Collection

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fig02: Antihyperglycaemic effects of EH-36 in STZ-C57BL/6 and KKAy diabetic mice. (A) STZ-C57BL/6 mice were injected s.c. twice daily for 4 days 10 mg EH-36/kg body weight (black circles) or 150 μl sesame oil (open circles). Blood glucose levels were determined at the indicated times. (B) KKAy mice were similarly treated with EH-36 (black squares) or the vehicle (open squares). (C) Plasma insulin levels were determined in samples taken from the EH-36- and oil-treated KKAy mice described in (B). (D) Normal (non-diabetic) C57BL/6 mice were treated with EH-36 or oil as described above. The blood glucose levels at day zero were 7.8 ± 0.6 and 7.6 ± 0.9 mM for the control and EH-36 treated group, respectively. Mean ± S.E.M., n = 5–10, *P < 0.05 in comparison with the oil-treated groups.
Mentions: The effect of EH-36 on blood glucose levels was evaluated following its s.c. injection (10 mg/kg of EH-36, twice a day) to STZ-treated C57BL/6 mice and KKAy diabetic mice. EH-36 demonstrated marked antihyperglycaemic activity: it significantly reduced blood glucose in STZ-treated C57BL/6 mice by 33% and 54% on days 3 and 4 of treatment, respectively, whereas oil treatment (vehicle) had no effect (Fig. 2A). EH-36 was even more effective in KKAy diabetic mice: blood glucose was reduced by 39%, 55% and 60% on days 2, 3 and 4 of treatment, respectively (Fig. 2B). Similar results were observed in these animals when the treatment was extended to 7 days. Yet, normoglycaemia was not attained in the diabetic mice following these 4- and 7 day treatments. In the rest of the experiment the mice were treated with EH-36 for 4 days to minimize the accumulation of oil at the sites of injection and to lower the risk of developing inflammatory reactions. In parallel with the reduction of blood glucose concentration, the KKAy mice, which are usually hyperinsulinaemic, became normoinsulinaemic during this treatment (Fig. 2C). The glucose-lowering effect of EH-36 was not restricted to diabetic animals: Figure 2D shows that it reduced blood glucose also by 20–25% in normoglycaemic control C57BL/6 mice.

Bottom Line: The effective blood EH-36 concentration in treated animals was 2 μM.This stimulatory effect was mediated by Thr(172) -phosphorylation in AMPK.These findings indicate that EH-36 is a promising prototype molecule for the development of novel antidiabetic drugs.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmacology, Institute for Drug Research, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel.

Show MeSH
Related in: MedlinePlus