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Preparation and diabetic use of Gibberellins

a technology of gibberellin and gibberellin a3 is applied in the field of preparation and diabetic use of gibberellin, which can solve the problems of ineffective gibberellin and no room or very little room at the receptor site, and achieve the effect of extremely low gibberellin a3 toxicity to mammals

Inactive Publication Date: 2005-09-29
JENKINS PETER JAMES +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

"The patent text describes the discovery of a group of compounds called Gibberellins that can mimic the actions of growth factors like insulin and have potential to treat diabetes and its complications. These compounds are smaller than traditional growth factors and can bind to a range of receptors, making them effective in stimulating cell growth and function. The text also discusses the low toxicity and non-carcinogenicity of Gibberellins. The patent provides a pharmaceutical formulation containing Gibberellins for the treatment of diabetes and related conditions."

Problems solved by technology

The physical bulkiness of these growth factors leaves no room or very little room at the receptor sites for which Gibberellins can bind.
This results in Gibberellins being ineffective when growth factors with sufficient binding affinity are present in sufficient quantities.

Method used

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  • Preparation and diabetic use of Gibberellins
  • Preparation and diabetic use of Gibberellins

Examples

Experimental program
Comparison scheme
Effect test

example 2

Preparation of Gibberellin A2 Salts and Esters

[0148] (a) Preparation of Gibberellin A3 sodium salt: A solution of 346 mg (1 mmole) of Gibberellin A3 was dissolved in 1.5 ml of methanol, was added to a solution of NaHCO3 (84 mg, 1 mmole) in 2 ml H2O. The whole mixture was evaporated under reduced pressure to dryness. The residue was then dissolved in water (2 ml) and freeze dried to afford Gibberellin A3 sodium salt was a white solid at quantitative yield.

[0149] (b) Preparation of Gibberellin A3 zinc salt: 100 mg of Gibberellin A3 sodium salt was dissolved in 10 ml water, then passed through a column (20 ml) Dowex 50 Zinc ion form resin. The column was then washed with 30 ml H2O. The effluent and washings were combined and vacuum evaporated to small volume, then freeze dried to afford Gibberellin A3 zinc salt as a white solid at quantitative yield.

[0150] (c) Preparation of Gibberellin A3 ethyl ester: 346 mg (1 mmole) of Gibberellin A3 was dissolved in a mixture of acetone (10 ml) ...

example 3

[0151] (a) Effect of Gibberellin A3 on cell growth compared to EGF in vitro. Human skin cell culture experiments were conducted by using keratinocytes media. Each well was seeded with 1,500 cells. Incubation was carried out at 37° C. for a period of five days. The experiments are shown as follows:

ExperimentMediaResults3.1Perfect keratinocyte mediumVery good growth (cell(containing EGF)division rate = 100)3.2Perfect keratinocyte mediumVery good growth (cell(containing EGF) plusdivision rate = 100)Gibberellin A3 (5□g / ml)3.3Keratinocyte mediumPoor growthcontaining no EGF3.4Keratinocyte mediumVery good growth (cellcontaining no EGF, butdivision rate ≈ 100)containing Gibberellin A3(5□g / ml)

Experiments 3.1 and 3.3 indicated that EGF (Epidermal Growth Factor) is essential for cell growth. Experiment 2 indicated that the presence of both EGF and Gibberellin A3 had no additive effect on the rate of cell growth. Experiment 4 gave an indication that Gibberellin A3 alone can stimulate cell gr...

example 4

[0153] The effect of a mixture of Gibberellin A3 with Gibberellins A4 and / or A7 was compared to that of IGF-1 on the cell growth in vitro. The results were similar to those in example 3(b).

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Abstract

The present invention relates to application of compounds of formula (1) (Gibberellins) and their derivatives for the preparation of a pharmaceutical composition or medicaments for the treatment of diabetes, its complications and associated conditions, including obesity, micro and macro vascular diseases, nephropathy, neuropathy, eye diseases, diabetic ulcerations and the like. The method results the normalization of serum glucose level and other physiological conditions.

Description

[0001] The present invention relates to the use of compounds of formula (1) (Gibberellins) and their derivatives for the treatment of diabetes, its complications and associated conditions, including obesity, micro and macro vascular diseases, nephropathy, neuropathy, eye diseases, diabetic ulcerations and the like, and their use for the preparation of pharmaceutical compositions or medicaments for treatment of these conditions. The invention results the normalization of serum glucose level and other physiological conditions. FIELD OF THE INVENTION [0002] The present invention relates to the application of a group of compounds known as Gibberellins and their derivatives for the preparation of a pharmaceutical composition for the treatment of diabetes and related conditions, as well as a method for treating these and other conditions by administering Gibberellins and / or their pharmaceutically acceptable salts or esters including glycoside esters, active esters or lactones. Moreover, t...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/19A61K31/343A61K35/74C07D307/00A61K45/00A61P1/04A61P3/04A61P3/10A61P9/00A61P27/02
CPCA61K31/19A61K31/704A61K31/22A61P1/04A61P13/12A61P25/00A61P27/02A61P3/10A61P3/04A61P43/00A61P9/00
Inventor JENKINS, PETER JAMESWU, MINNIEWU, DAVID SHINE
Owner JENKINS PETER JAMES