CN106491591A - Linderolide H are preparing the application reduced in hypoglycemic medicament - Google Patents
Linderolide H are preparing the application reduced in hypoglycemic medicament Download PDFInfo
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- CN106491591A CN106491591A CN201610822162.2A CN201610822162A CN106491591A CN 106491591 A CN106491591 A CN 106491591A CN 201610822162 A CN201610822162 A CN 201610822162A CN 106491591 A CN106491591 A CN 106491591A
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- linderolide
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- antidiabetic medicine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/365—Lactones
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Abstract
The invention discloses a kind of applications of Linderolide H in antidiabetic medicine is prepared.The present invention provides a kind of brand-new selection and thinking for current antidiabetic medicine, has widened the selection field of antidiabetic medicine, and the also development for the technical field contributes；The application of the Linderolide H of the present invention has been proved to significant anti-diabetic effect；What the present invention was selected is the compound with clear and definite chemical constitution.Purposes of the Linderolide H according to the present invention in treatment antidiabetic medicine is prepared belongs to first public, as framework types belong to brand-new framework types, and which is prevented and treated diabetic activity and is unexpectedly strong, there is no the possibility that any enlightenment is given by other compounds, possess prominent substantive distinguishing features, be simultaneously used for treating anti-diabetic obviously with significant progressive.
Description
Technical field
The present invention relates to the new application of compound L inderolide H, more particularly to Linderolide H are in preparation reduction
Application in hypoglycemic medicament.
Background technology
Diabetes (diabetes mellitus) are one of modal chronic disease, wherein diabetes B now
(II diabetes mellitus of Type, are called Non-Insulin Dependent Diabetes Mellitus, non-insulin-depentdiabetes
Mellitus, NIDDM) account for more than the 90% of diabetic.Diabetes are one in developed country and developing country
Increasingly serious problem, it cause serious and costly consequence, including blind, heart disease and ephrosis etc..According to estimates, from
2000 to the year two thousand fifty, the number of whole world diabetic will increase by 165%.According to the statistics of IDF, mesh
There is 4.3% population in front China with diabetes, and the number of patient will break through 50,000,000 in following 20 years.Diabetes are modern
The second killer in disease, its harm to human body are only second to cancer, seriously threaten the health of the mankind, and present glycosuria
Disease has the tendency of extension and rejuvenation, how to prevent diabetes from having become the big problem that current the world of medicine pays close attention to.
Compound L inderolide H according to the present invention be one deliver within 2013 (Qing Liu, et al.,
Sesquiterpene lactones from the roots of Lindera strychnifolia.Phytochemistry,
87 (2013) 112 118.) noval chemical compound, the compound have brand-new framework types, and current purposes merely relates to anticancer
Effect (Qing Liu, et al., Sesquiterpene lactones from the roots of Lindera
Strychnifolia.Phytochemistry, 87 (2013) 112 118.), for Linderolide H according to the present invention
Purposes in reduction hypoglycemic medicament is prepared belongs to first public, and due to belonging to brand-new structure type, and which is for reduction
Blood sugar activity is unexpectedly strong, and there is no the possibility for being provided any enlightenment by other compounds, possesses prominent substance special
Point, is simultaneously used for reducing blood sugar obviously with significant progressive.
Content of the invention
The present invention proposes Linderolide H and is preparing the application reduced in hypoglycemic medicament.Find out from pharmacological evaluation,
Linderolide H has preferably drop hypoglycemic effect.As first public Linderolide H of the invention are reducing blood sugar
The pharmacologic action of aspect.
Shown in the compound L inderolide H structures such as formula (I)：
The technical scheme is that：The application of Linderolide H, is specifically applied to prepare antidiabetic medicine.
The invention has the beneficial effects as follows：
1) present invention provides a kind of brand-new selection and thinking for current antidiabetic medicine, has widened antidiabetic
Selection field, the also development for the technical field contribute；2) application of Linderolide H of the invention has been proved to
Significant anti-diabetic effect.
Above all：The present invention carries out the hypoglycemic experiment of animal used as test to Linderolide H, in lasting gavage fat
On the basis of fat breast makes rat produce insulin resistance, the low dose of Streptozotocin impaired isle β cells of application cause rat serum
Sugar is raised, and made animal model is similar with diabetes B.Rat model of type 2 diabetes mellitus gives Linderolide H treatments
Afterwards, Linderolide H height, the blood glucose value of neutralization low dose group are compared with model group blood glucose value, it may have significant difference (P<
0.01) blood glucose value before and after, Linderolide H are high, neutralization low dose group is administered compares, it may have significant difference (P<
0.01), illustrate that Linderolide H have good hypoglycemic activity to experimental type 2 diabetes mellitus.
Purposes of the Linderolide H according to the present invention in treatment antidiabetic medicine is prepared belongs to first public,
As framework types belong to brand-new framework types, and which is prevented and treated diabetic activity and is unexpectedly strong, and does not exist by other
Compound provides the possibility of any enlightenment, possesses prominent substantive distinguishing features, is simultaneously used for treating anti-diabetic obviously with aobvious
The progress of work.
Specific embodiment
The preparation method of compound L inderolide H involved in the present invention referring to document (Qing Liu, et al.,
Sesquiterpene lactones from the roots of Lindera strychnifolia.Phytochemistry,
87(2013)112–118.)
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not by concrete real
Any restriction of example is applied, but is defined in the claims.
Embodiment 1：The preparation of compound L inderolide H tablets involved in the present invention：
20 g of compound Linderolide H are taken, addition prepares 180 grams of the customary adjuvant of tablet, mixed, conventional tablet presses
Make 1000.
Embodiment 2：The preparation of compound L inderolide H capsules involved in the present invention：
20 g of compound Linderolide H are taken, addition prepares customary adjuvant such as 180 grams of the starch of capsule, mixed, dress
Capsule makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Experimental example 1：Impacts of the Linderolide H to rat model of type 2 diabetes mellitus
1st, animal packet
Healthy Wistar rats (SPF levels), male, body weight 180-220g (are carried by Nanfang Medical Univ's Experimental Animal Center
For), free water is taken food, and is randomly divided into Normal group and modeling group, and modeling group sets up model, modeling success as follows
Model group animal is randomly divided into model control group, positive drug gliclazide group, high, normal, basic group of Linderolide H again afterwards,
According to the form below successive administration 1 week.
Administration time and dosage are shown in Table 1：
1 Linderolide H effect experiment animal packets of table
| Group | Number of animals (only) | Dosage (mg/kgBW) |
| Normal group | 12 | |
| Model control group | 12 | |
| Positive drug group | 12 | 35.5 |
| Low dose group | 12 | 0.2 |
| Middle dose group | 12 | 0.4 |
| High dose group | 12 | 0.8 |
2nd, prepared by rat model
The daily gavage distilled water of normal rats, the daily morning and evening gavage of high fat group rat make Fat Emulsion (1ml/ by oneself
100gBW).After continuous gavage Fat Emulsion 2 weeks, water 24h, 10 tail vein injection physiology salts of blank control group are can't help in animal fasting
Water, remaining rat equal tail vein injection 30mg/kgBW Streptozotocins (hereinafter abbreviated as STZ) solution (prepared before use).Give
After medicine 48h, water 12h is can't help in fasting, takes blood every 3 hours eyeball rear vein beards, empty according to the time-and-motion study of blood sugar detection kit
Abdomen blood glucose value, METHOD FOR CONTINUOUS DETERMINATION 3 times, fasting blood sugar >=16.7mmol/L for modeling success rat.
3rd, the measure of blood sugar
After last dose, water 12h is can't help in animal fasting, and eyeball rear vein beard takes blood, is surveyed according to the method for kit respectively
Determine blood glucose value.Using SPSS13.0 statistical softwares, the situation of change of each group blood glucose value is analyzed and compares.
4th, impacts of the Linderolide H to rat model of type 2 diabetes mellitus blood sugar
Experimental result is shown in Table 2, and as known from Table 2, after injection STZ, rat blood sugar rises, and fasting blood sugar after 72h >=
16.7mmol/L, illustrates diabetes model success.After administration, positive drug group, Linderolide H are high, neutralization low dose group
Blood glucose value compare with model group blood glucose value, have significant difference (P<0.01).
After the front blood sugar of each group administration and administration, the T inspections of blood sugar show, positive drug group, Linderolide H height, neutralization
Blood glucose value before and after low dose group administration compares, with significant difference (P<0.01).Result above shows, Linderolide
H can reduce the blood sugar of rat model of type 2 diabetes mellitus.
2 experimental result of table
| Group | Number of animals (only) | Blood glucose value before administration | Blood glucose value after administration |
| Normal group | 10 | 5.83±0.42 | 5.79±1.54 |
| Model control group | 9 | 13.38±2.46 | 35.18±2.31 |
| Positive drug group | 9 | 32.58±2.86 | 18.26±2.75**△△ |
| Low dose group | 8 | 31.39±2.21 | 23.64±2.52**△△ |
| Middle dose group | 10 | 35.89±1.74 | 18.12±2.42**△△ |
| High dose group | 9 | 36.48±2.97 | 17.72±3.56**△△ |
*p<0.05vs model group * * p<0.01vs model groups△p<Before 0.05vs is with group administration△△p<0.01vs is same to organize administration
Before
Conclusion：Linderolide H can significantly reduce the blood sugar of diabetes B animal model, can be used to preparation anti-
Diabetes medicament.
Claims (1)
- Applications of the 1.Linderolide H in hypoglycemic medicament is reduced, the compound L inderolide H structures such as formula (I) Shown：
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610822162.2A CN106491591A (en) | 2016-09-14 | 2016-09-14 | Linderolide H are preparing the application reduced in hypoglycemic medicament |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610822162.2A CN106491591A (en) | 2016-09-14 | 2016-09-14 | Linderolide H are preparing the application reduced in hypoglycemic medicament |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN106491591A true CN106491591A (en) | 2017-03-15 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610822162.2A Pending CN106491591A (en) | 2016-09-14 | 2016-09-14 | Linderolide H are preparing the application reduced in hypoglycemic medicament |
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| Country | Link |
|---|---|
| CN (1) | CN106491591A (en) |
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2016
- 2016-09-14 CN CN201610822162.2A patent/CN106491591A/en active Pending
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| C06 | Publication | ||
| PB01 | Publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20170315 |
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| WD01 | Invention patent application deemed withdrawn after publication |