CN1799571A - Medicine for lowering blood sugar and treating women menopausal syndrome and preparation method thereof - Google Patents

Abstract

The invention provides a medicament for treating diabetes and women's climacteric metancholia, wherein the preparing process consists of extracting folium cajani with ethanol, depression concentrating the extract, dissolving into water and filtering, passing the filtrate through macroscopic adsorption resin, de-abstracting with ethanol, methanol or propanone, finally concentrating the obtained organic solution.

Description

Medicine of blood sugar lowering and climacteric syndrome and preparation method thereof

Technical field

The present invention relates to medicine of a kind of blood sugar lowering and treatment climacteric syndrome and preparation method thereof, belong to life science.

Background technology

In the prior art, cajanin, Longistylin A, Longistylin C, pinostrobin, vitexin, isovitexin, apigenin, luteolin etc. had once been reported from the Folium Cajani isolation identification.Former three belongs to the stilbene constituents, and all the other are flavonoid.Because structural difference, this two class (even similar and different structure) composition, their biological activity is different.Report more have antitumor, cardiac vascular activity, antioxidation and antibiotic etc.But do not see the content that the present invention relates to is arranged.

Summary of the invention

Technical problem to be solved by this invention provides a kind of new medicine that can effectively treat diabetes and climacteric syndrome.

Technical problem to be solved by this invention realizes by following technological approaches:

A kind of medicine for the treatment of diabetes and climacteric syndrome is prepared from by following method:

1), Folium Cajani pulverized after, use ethanol extraction, concentrating under reduced pressure gets steeping in wine cream behind the extracting liquid filtering.

2), above-mentioned steeping in wine cream is soluble in water, filter, filtrate is by macroporous adsorbent resin and with ethanol, methanol or acetone desorbing, the organic solution of gained is evaporated to dried, promptly.

In the drug prepared of the present invention, mainly contain Semen Cajani stilbene and Semen Cajani flavone component, can effectively treat diabetes and climacteric syndrome, also can be used for due to illness spay or chemicotherapy and cause artificial menopause women's treatment.

Further describe beneficial effect of the present invention by the following examples, it should be understood that these embodiment only are used for the purpose of illustration, never limit the scope of the invention.

The specific embodiment

The preparation of [embodiment] medicine of the present invention

The Folium Cajani 4kg that pulverizes adds 80% ethanol and crosses face, is heated to and boils, be incubated one hour, filter repetitive operation three times, the filtrate decompression that merges is concentrated into does not have the alcohol flavor, 1kg steeping in wine cream, the steeping in wine cream of gained is added 70 ℃ of hot water changes molten, filters (kieselguhr helps filter), the filtrate that obtains is passed through macroporous adsorptive resins, alcohol desorption, the alcoholic solution that obtains is evaporated to dried 164g Folium Cajani extract (I).

The hypoglycemic activity test of [test example 1] medicine of the present invention

One, test material and method

1, experimental animal: 60 of male mouse of kunming, body weight 20.56 ± 0.86g is available from animal institute of the Chinese Academy of Medical Sciences.

2, given the test agent: the Folium Cajani extract (I) that the embodiment of the invention 1 is prepared.

3, positive control drug: phenformin hydrochloride tablet (JIANGZHILING PIAN) (Shandong Boshan Pharmaceutical Co., Ltd., lot number 0206272).

4, laboratory animal grouping: being divided into is five groups, i.e. the high, medium and low dosage group of blank group, positive drug control group and given the test agent, every group of 12 animals.

5, modeling method: mice absolute fasting (changing bedding and padding) be can't help water after 18 hours, intraperitoneal administration chain urase element (Streptozotocin) 200mg/kg.(Sigma company product, lot number 971201)

6, testing index: body weight, fasting glucose and postprandial plasma glucose level (carbohydrate tolerance).

7, administration: gastric infusion, every day 1 time, a continuous week.The high, medium and low dosage group of given the test agent is given Folium Cajani extract 1200,600,300mg/kg respectively.The blank model group is given normal saline.

8, blood-sugar level measuring: water administration after 8 hours is can't help in mice absolute fasting (changing bedding and padding), and administration was got blood after 1 hour, measures the serum glucose value, sees Table 1.

9, carbohydrate tolerance test: administration is after 1 hour, and 2g/kg starch (10%) load is measured and given the sugar back 1,2 hour blood glucose value, sees Table 2.

Two, result of the test

The result: given the test agent high dose group and normal saline model control group compare, and the fasting blood sugar of administration group and postprandial plasma glucose level all have tangible reduction, have statistical significance, P＜0.05, and show dose-effect relationship.Given the test agent high dose group and positive control drug group (200mg/kg) compare, and not only hypoglycemic effect is better than insoral, and aspect increasing the weight of animals and reducing the animal dead rate, demonstrate its superiority (table 1 and table 2).

Table 1. Folium Cajani extract is to the influence of diabetic mice fasting glucose

	The blank group	Positive controls	Folium Cajani extract group (mg/kg)
						The dosage blood glucose value	Normal saline 14.62 ± 6.28	200mg/kg 12.07±3.17	1200 10.95±4.99*	600 14.78±7.86	300 14.01±7.21

*P＜0.05

Table 2. Folium Cajani extract is to the influence (carbohydrate tolerance) of diabetic mice post-prandial glycemia

	The blank group	Positive controls	Folium Cajani extract group (mg/kg)
						Dosage 1h 2h	Normal saline 16.06 ± 7.07 15.33 ± 8.32	200mg/kg 14.19±4.68 13.24±3.73	1200 12.44±2.23* 10.06±5.41	600 19.10±6.86 12.56±6.14	300 15.97±3.94 12.49±5.33

* P＜0.05 (with the comparison of blank group)

[test example 2] medicine of the present invention is tested HOS human osteoblast proliferation function.

One, test material and method

Cell strain: HOS TE85 human osteoblast strain (from Institute of Basic Medical Sciences, Chinese Academy of Medical Sciences).

Drug treating time: 48 hours.

Observation index: 1. cell proliferation (MTT); 2. ³The H-proline participates in; 3. alkaline phosphatase activities

Given the test agent: embodiment of the invention drug prepared and cajanin monomer component.

Positive control medicine: estradiol (E ₂) (the sharp bioid in sky, Beijing factory product).

Result of the test: be respectively 10 at final concentration ^-7With 10 ^-8During g/ml, monomer cajanin and given the test agent can dose-dependent promotion osteoblastic proliferation, the collagen formation of energy irritation cell simultaneously.Show that they have the effect of stimulating osteoblast bone formation, but they are to not influence (seeing Table 3) of alkaline phosphatase activity.

Table 3. Folium Cajani extract is to the function of HOS TE85 cell bone formation

Group	Final concentration	The cell increment	3The H proline is mixed the people	Alkaline phosphatase activities
					The blank group	-	0.26±0.02	1399±77	1.91±0.28
Positive control E 2Group	10 -9M	0.26±0.01	2180±116**	2.34±0.28
					Monomer cajanin group	10 -8(g/ml)	0.30±0.01*	1664±253	2.15±0.28
10 -7(g/ml)	0.34±0.03*	2554±252**	2.28±0.28

Folium Cajani extract group	10 -8(g/ml)	0.30±0.02	1606±73*	2.15±0.28
					10 -7(g/ml)	0.33±0.03	2309±287**	2.03±0.18

* P＜0.05; * P＜0.01 (comparing) with the blank group

[test example 3] medicine of the present invention is to the influence of removal ovary rat model

One, test material and method:

1, laboratory animal: 60 female WISTAR rats that grow up, body weight 232.7g ± 11.0g is available from animal institute of the Chinese Academy of Medical Sciences.

2, animal model: adopting and removing bilateral ovaries (castration) rat is model.Concrete operations are as follows: cut rat abdomen, separate and the excision bilateral ovaries, sew up the abdominal cavity then.The Sham-operated control group rat, abdominal incision separates bilateral ovaries, is equivalent to the fat of ovary size near the spay, sews up then and closes the abdominal cavity.

3, given the test agent: embodiment of the invention drug prepared, to join and be high, medium and low dosage group, its concentration is respectively: 200mg/kg; 100mg/kg; 50mg/kg.

4, positive control drug: estradiol (E ₂) (the sharp bioid in sky, Beijing factory product), administration concentration is 0.5mg/kg.

5, experimental animal grouping (n=number of animals):

1. Sham-operated control group (n=8).

2. blank model group (n=11).

3. positive drug (E ₂) matched group (n=11): the positive drug group is given E ₂0.5mg/kg the rat castration is after two weeks, every day gastric infusion once, continuous eight weeks.

4. given the test agent administration group (n=10): the high, medium and low dosage group of given the test agent administration concentration respectively is: 200mg/kg, 100mg/kg, 50mg/kg.The rat castration is after two weeks, every day gastric infusion once, continuous eight weeks.

6, testing index: body weight, uterus weight and ovary weight, hormone serum level (putting the method for exempting from measures), the cut sections for microscopic examination of osteopathia reason.

Result of the test:

1. to the influence of castrated rats body weight and uterus weight: model group is compared with sham operated rats, and rat body weight obviously increases.After the administration, positive drug group and given the test agent height, middle dosage group rat body weight descend to some extent than model group; The model group uterus weight only is 20% of a sham operated rats; And the estradiol group is compared with model group, and rat uterus weight has increased by 108.3%, but still is lower than sham operated rats.Different with the estradiol group, the uterus weight of each dosage group of given the test agent does not obviously increase, and shows that it does not have stimulation to the uterus.

2. to the influence of castrated rats hormone serum level: after the excision of model group rat ovary, serum estradiol content obviously reduces, and FSH and LH obviously increase simultaneously; Give E ₂After positive controls, with model group relatively, serum E ₂Content increases by 57.7%, and FSH and LH reduce by 11.5% and 20.7% respectively.Given the test agent high dose group and model group compare, serum E ₂Content does not obviously increase, and FSH and LH then reduce by 11.5% and 15.2% respectively.Result of the test shows that medicine of the present invention can improve because the serum estrogen level reduces caused FSH and LH raises.

3. the influence that castrated rats osteopathia reason is changed: positive drug control group is being given E ₂After, the bone loss of 82% rat femur has obtained recovery.The high dose group rat of given the test agent treatment then has the bone loss of 60% femur to improve, and middle dosage is 30% to improve.Show that medicine of the present invention has the bone loss of inhibition, promotes the bone formation effect.

Claims (5)

1, the medicine of a kind of blood sugar lowering and treatment climacteric syndrome is prepared from by following step:

1), with the Folium Cajani ethanol extraction, concentrating under reduced pressure gets steeping in wine cream behind the extracting liquid filtering,

2), above-mentioned steeping in wine cream is soluble in water, filter, filtrate is by macroporous adsorbent resin and with ethanol, methanol or acetone desorbing, the organic solution of gained is evaporated to dried, promptly.

2, according to the described medicine of claim 1, it is characterized in that: be prepared into any suitable clinical preparation according to this area conventional formulation method.

3, the purposes of the described medicine of claim 1 in preparation treatment diabetes medicament.

4, the purposes of the described medicine of claim 1 in preparation treatment menopausal syndrome medicine.

5, the described medicine of claim 1 causes purposes in the artificial menopause medicine at preparation treatment oophorectomize or chemicotherapy.