CN101138567A - Natural glycosides component having good effect of reducing blood sugar - Google Patents

Abstract

The invention discloses a natural small-molecule glycoside compound of better hypoglycemic activity, which is selected from the natural similar compounds through screening test. The invention provides a better choice for the development of the compound and the new drug in clinically treating diabetes.

Description

The natural nucleoside composition that a kind of effect of reducing blood sugar is good

The invention belongs to the preferred of curative effect in the class novel blood sugar lowing plant compound, the curative effect of natural stilbene glycosides compound that promptly has hypoglycemic activity is preferred, therefrom obtained the good natural component of a kind of effect of reducing blood sugar, and served as the hypoglycemic clinically purposes of complex of basis composition with this composition.

Data shows, the onset diabetes rate of China 0.3% rose to present more than 4% (part big city nearly 6%) before 1980.The diabetics number has reached about 4,000 ten thousand at present, and prevalence occupies the second place of the world, and the medical expense that is used for diabetics every year is up to 83,300,000,000 yuan.World Health Organization's prediction will reach 5,000 ten thousand to China diabetes patient in 2025.

According to World Health Organization's recent statistics, there is diabetics 1.25 hundred million in the whole world, and average per minute is dead because of diabetic complication with regard to 6 people are arranged, and the death that diabetes cause occupies the 5th of the present world cause of death.World Health Organization (WHO) has classified diabetes as one of three big difficult disease.

At present the hypoglycemic drug of using clinically is except that insulin, and majority is a chemical synthetic drug, is apparent in view and take the toxic and side effects that chemical synthetic drug brings to the patient for a long time.Chinese medicine compound determined curative effect, no obvious toxic and side effects, but curative effect comes Chinese patent medicine kind slow and that process few.Still Given this hypoglycemic drug that is prepared from of monomer-free native compound on the pharmaceutical market, on the basis of patent ZL 99122378.0, has therefrom obtained the good monomeric compound of a kind of effect of reducing blood sugar through further investigation so far.

Following biological assessment embodiment will the present invention is described in detail.

Following chemical compound is carried out the biological assessment test

A R1＝OH；R2＝glucosyl；R3＝H

B R1＝OH；R2＝CH3；R3＝glucosyl

C R1＝H；R2＝CH3；R3＝glucosyl

The evaluation of embodiment 1 hyperglycemia mouse model

Mainly observed the treatment influence of compd A～C,, estimated with the clinical treatment diabetics positive contrast medicine of metformin commonly used to the hyperglycemia mice of alloxan modeling.

Select the KM mice, fasting is after 6～8 hours, and tail vein injection alloxan 80mg/kg was qualified more than the selection blood glucose value 11mmol/L after 72 hours, grouping.Every day gastric infusion, continuous use 12 days is measured blood glucose.The result is as follows:

Group	Number of animals (only)	Dosage (mg/kg)	Blood glucose (mmol/L) before the administration	Blood glucose after the administration (mmol/L)
					Blank group model group metformin group A group B group C group	10 10 10 10 10 10	500 500 500 500	7.72±2.48 21.12±7.72 19.80±7.00 20.22±8.08 20.26±7.68 20.01±7.79	8.01±1.16 42.34±4.12 37.13±5.20 33.60±7.78 36.42±6.39 37.08±8.63

The influence of 2 pairs of normal mouse carbohydrate tolerance of embodiment

Mainly observed the influence of compd A～C,, estimated with the positive contrast medicine of clinical diabetes curative glyburide to the normal mouse carbohydrate tolerance.

Select 10 every group of KM mices, every day gastric infusion, continuous use 12 days gavages high liquid glucose again, measures the blood sugar concentration gavage different time after the high liquid glucose.The result is as follows:

Group	Dosage (mg/kg)	Blood glucose (mmol/L) before the administration	Blood glucose after the administration (mmol/L)
							0’	30’	60’	120’
			Normal group metformin group A group B group C group	50 500 500 500	2.31±1.02 0.95±0.73 2.07±1.82 2.53±1.86 2.23±0.45	1.76±3.57 19.59±7.90 7.93±2.42 7.95±1.36 7.72±2.38					30.54±7.72 25.51±9.43 18.53±9.14 21.83±12.01 25.30±7.02	2336±4.61 2083±9.85 1232±6.02 19.54±11.51 1725±6.66	8.75±3.38 11.22±8.66 6.27±2.56 8.94±7.26 6.69±2.29

No matter to the blood sugar decreasing effect of hyperglycemia mouse model group, still to the raising of normal mouse carbohydrate tolerance, the A chemical compound all shows best effect.

Claims (3)

1. from following natural nucleoside compound, screen the chemical compound of hypoglycemic activity the best.

Result: have the natural nucleoside compound of following array structure, be the preferable monomer component of curative effect in such big right blood-sugar decreasing active.

2. a compositions that is used for hypoglycemic drug is characterized in that with the chemical compound in the claim 1 and pharmaceutical excipient and/or carrier composition.

3. pharmaceutical composition according to claim 2 can be any peroral dosage forms such as tablet, granule, capsule.