CN106265650A - Ternatusine A application in preparation reduces hypoglycemic medicament - Google Patents
Ternatusine A application in preparation reduces hypoglycemic medicament Download PDFInfo
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- CN106265650A CN106265650A CN201610805119.5A CN201610805119A CN106265650A CN 106265650 A CN106265650 A CN 106265650A CN 201610805119 A CN201610805119 A CN 201610805119A CN 106265650 A CN106265650 A CN 106265650A
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- ternatusine
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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
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
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- Life Sciences & Earth Sciences (AREA)
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- General Health & Medical Sciences (AREA)
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Abstract
The invention discloses a kind of Ternatusine A application in preparing antidiabetic medicine, the application of the Ternatusine A of the present invention has been proved to significant anti-diabetic effect；There is the compound of clear and definite chemical constitution, belong to brand-new framework types, and its preventing and treating diabetic activity is strong, possesses prominent substantive distinguishing features, be simultaneously used for treating anti-diabetic and obviously have the most progressive.
Description
Technical field
The present invention relates to the new application of compound Ternatusine A, particularly relate to Ternatusine A and reduce in preparation
Application in hypoglycemic medicament.
Background technology
Diabetes (diabetes mellitus) are all ask the most serious in developed country and developing country
Topic, it causes serious and costly consequence, including blind, heart disease and nephropathy etc..According to estimates, from 2000 to 2050
Year, the number of whole world diabetics will increase by 165%.According to the statistics of IDF, at present in state-owned 4.3%
Population suffer from diabetes, in following 20 years, the number of patient will break through 50,000,000.Diabetes are second in modern diseases
Killer, it is only second to cancer to the harm of human body, and the health of the mankind in serious threat.
The compound Ternatusine A that the present invention relates to be one within 2013, deliver (Zhi lai Zhan, et al.,
Ternatusine A,a New Pyrrole Derivative with an Epoxyoxepino Ring from
Ranunculus ternatus.ORGANIC LETTERS, 2013,15 (8): 1,970 1973.) noval chemical compound, this compound
Having brand-new framework types, current purposes merely relates to antibacterial (Zhi lai Zhan, et al., Ternatusine A, a
New Pyrrole Derivative with an Epoxyoxepino Ring from Ranunculus
Ternatus.ORGANIC LETTERS, 2013,15 (8): 1,970 1973.), the Ternatusine A that the present invention relates to is in system
The purposes in hypoglycemic medicament of making preparation for dropping belongs to first public.
Summary of the invention
The present invention proposes Ternatusine A application in preparation reduces hypoglycemic medicament.Find out from pharmacological evaluation,
Ternatusine A has hypoglycemic effect of preferably dropping.Owing to the present invention first public Ternatusine A is reducing blood glucose
The pharmacologic action of aspect.
Described compound Ternatusine A structure is as shown in formula I:
The technical scheme is that the application of Ternatusine A, be specifically applied to prepare antidiabetic medicine.
The invention has the beneficial effects as follows:
The present invention carries out the blood sugar lowering experiment of laboratory animal to Ternatusine A, illustrates that Ternatusine A is to experiment
Property type 2 diabetes mellitus has good hypoglycemic activity.The Ternatusine A that the present invention relates to is at preparation treatment antidiabetic medicine
In purposes belong to first public, owing to framework types belongs to brand-new framework types, and its preventing and treating diabetic activity is strong
Unexpected, there is not the possibility being provided any enlightenment by other compounds, possess prominent substantive distinguishing features, be simultaneously used for controlling
Treat anti-diabetic and obviously have the most progressive.
Detailed description of the invention
The preparation method of compound Ternatusine A involved in the present invention see document (Zhilai Zhan, et al.,
Ternatusine A,a New Pyrrole Derivative with an Epoxyoxepino Ring from
Ranunculus ternatus.ORGANIC LETTERS,2013,15(8):1970–1973.)
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not by concrete real
Execute any restriction of example, but be defined in the claims.
Embodiment 1: the preparation of compound Ternatusine A tablet involved in the present invention:
Taking 5 g of compound Ternatusine A, add 195 grams of dextrin, mixing, Conventional compression makes 1000.
Embodiment 2: the preparation of compound Ternatusine A capsule involved in the present invention:
Take 5 g of compound Ternatusine A, add starch 195 grams, mixing, encapsulated make 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
The experimental example 1:Ternatusine A impact on rat model of type 2 diabetes mellitus
1, animal packet
Healthy Wistar rat (SPF level), male, body weight 180-220g (is carried by Nanjing Medical University's Experimental Animal Center
For), feed of freely drinking water, it is randomly divided into Normal group and modeling group, modeling group sets up model, modeling success as follows
After model group animal is randomly divided into model control group, positive drug gliclazide group, high, normal, basic group of Ternatusine A again,
According to the form below successive administration 1 week.
Administration time and dosage are shown in Table 1:
Table 1 Ternatusine A effect experiment animal is grouped
2, prepared by rat model
Normal rats gavage every day distilled water, the high fat group rat every day of gavage self-control sooner or later fat milk (1ml/
100gBW).Gavage fat milk is after 2 weeks continuously, and water 24h, 10 tail vein injection physiology salt of blank group are can't help in animal fasting
Water, remaining rat equal tail vein injection 30mg/kgBW streptozotocin (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 blood sugar detection test kit time-and-motion study
Abdomen blood glucose value, METHOD FOR CONTINUOUS DETERMINATION 3 times, fasting blood sugar >=16.7mmol/L for modeling success rat.
3, the mensuration of blood glucose
After last is administered, water 12h is can't help in animal fasting, and eyeball rear vein beard takes blood, surveys respectively according to the method for test kit
Determine blood glucose value.Use SPSS13.0 statistical software, analyze and respectively organize the situation of change of blood glucose value.
4, the Ternatusine A impact on rat model of type 2 diabetes mellitus blood glucose
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, Ternatusine A is high, neutralize low dose group
Blood glucose value compare with model group blood glucose value, all have significant difference (P < 0.01).
Each group be administered before blood glucose and the T inspection display of blood glucose, positive drug group after being administered, Ternatusine A is high, neutralize
Blood glucose value before and after low dose group is administered compares, and has significant difference (P < 0.01).Result above shows, Ternatusine
A can reduce the blood glucose of rat model of type 2 diabetes mellitus.
Table 2 experimental result
| Group | Number of animals (only) | Blood glucose value before being administered | Blood glucose value after administration |
| Normal group | 10 | 6.98±0.42 | 6.87±1.52 |
| Model control group | 9 | 14.12±3.67 | 35.97±2.53 |
| Positive drug group | 9 | 32.47±2.58 | 17.26±3.57**△△ |
| Low dose group | 8 | 32.87±2.48 | 22.687±4.26**△△ |
| Middle dosage group | 10 | 33.75±2.89 | 16.65±2.38**△△ |
| High dose group | 9 | 37.49±2.52 | 18.10±3.23**△△ |
* p < 0.05vs model group * * p < 0.01vs model group△Before p < 0.05vs is administered with group△△P < 0.01vs is with organizing administration
Before
Conclusion: Ternatusine A can significantly reduce the blood glucose of type 2 diabetes mellitus animal model, can be used to preparation anti-
Diabetes medicament.
Claims (1)
1.Ternatusine A application in reducing hypoglycemic medicament, described compound Ternatusine A structure such as formula I
Shown in:
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107814823A (en) * | 2017-11-15 | 2018-03-20 | 南京正亮医药科技有限公司 | A kind of compound for treating diabetes and its application |
-
2016
- 2016-09-06 CN CN201610805119.5A patent/CN106265650A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107814823A (en) * | 2017-11-15 | 2018-03-20 | 南京正亮医药科技有限公司 | A kind of compound for treating diabetes and its application |
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Application publication date: 20170104 |