CN110403951A - A kind of ophiopogonin D preparation and its blood lipid-lowering medicine new application - Google Patents
A kind of ophiopogonin D preparation and its blood lipid-lowering medicine new application Download PDFInfo
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- CN110403951A CN110403951A CN201910408678.6A CN201910408678A CN110403951A CN 110403951 A CN110403951 A CN 110403951A CN 201910408678 A CN201910408678 A CN 201910408678A CN 110403951 A CN110403951 A CN 110403951A
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- Prior art keywords
- ophiopogonin
- preparation
- opd
- dosage
- blood
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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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
Abstract
The present invention discloses a kind of ophiopogonin D preparation, and said preparation contains the 0.1-0.4mg/kg ophiopogonin D calculated with experimental rat dosage, and the content is the people's dosage obtained by weight of experimental rat dosage is to calculate basis.The present invention also provides a kind of application of ophiopogonin D preparation in the drug that preparation has effect for reducing blood fat.Ophiopogonin D preparation of the present invention has the function of reducing blood lipid, and having exploitation is new blood lipid-lowering medicine potentiality, and its validity, safety and controllability Study data are very friendly, and druggability is strong.
Description
Technical field
The present invention relates to chemical medicine field, in particular to a kind of ophiopogonin D preparation and its blood lipid-lowering medicine new application.
Background technique
Radix Ophiopogonis, sweet in flavor, slight bitter, cold nature return stomach, lung, the heart channel of Hang-Shaoyin.Have Yin nourishing and lung moistening, reinforcing stomach reg fluid, relieving restlessness and restlessness function
Effect, for diseases such as dryness of the lung dry cough, cough for deficiency of Yin consumptive disease, larynx numbness pharyngalgia, injury thirst, Heat Diabetes, vexed insomnia, dry constipation of intestines.It is existing
Nowadays clinic is usually used in treating the diseases such as arrhythmia cordis and myocardial ischemia, such as forms ginseng by Radix Ophiopogonis and 2 taste drug matching of red ginseng
Wheat injection is the fiest-tire medication of the heart diseases such as clinical treatment coronary heart disease.
Ophiopogonin D (OPD) and ophiopogonin D ' (OPD ') is that a kind of saponin component is extracted from Chinese medicine Radix Ophiopogonis, two
Person's isomer each other, structural formula is as shown in Figure 1:
In current research, the overwhelming majority is accounted for for the research of OPD, some researches show that OPD is living with very strong pharmacology
Property, it may be possible to the material base of Radix Ophiopogonis performance curative effect.As OPD structure can be realized with induced cytochrome P450 enzyme 2J to intracellular
Ca2+Stable state regulation reduces cardiac muscle cell apoptosis to inhibit oxidative stress.OPD can also be by influencing tumour cell division week
Phase, inducing apoptosis of tumour cell.
But the pharmacology of OPD ' and the correlative study in terms of toxicity are rarely reported, and some researches show that OPD ' has very strong
Cytotoxicity, in H9C2In cell, when OPD ' concentration is greater than 5 μm of ol/L, the obvious shrinkage of H9C2 cellular morphology, cell survival rate
It is remarkably decreased, apoptosis rate significantly rises, and has concentration dependent.
Summary of the invention
Present invention aims at disclosing a kind of ophiopogonin D preparation and its blood lipid-lowering medicine new application, object of the present invention is to
It is achieved through the following technical solutions.
A kind of ophiopogonin D preparation, said preparation contain the 0.1-0.4mg/kg Radix Ophiopogonis calculated with experimental rat dosage
Saponin D, and the content is the people's dosage obtained by weight of experimental rat dosage is to calculate basis.Preferably, the system
Agent contains 0.1mg/kg ophiopogonin D, the 0.25mg/kg ophiopogonin D, 0.3mg/kg wheat calculated with experimental rat dosage
Winter saponin D, 0.35mg/kg ophiopogonin D, 0.38mg/kg ophiopogonin D, and the content can be according to experimental rat to medicament
People's dosage that amount obtains for the conversion of calculating basis.
The object of the invention, which also resides in, provides a kind of ophiopogonin D preparation answering in the drug that preparation has effect for reducing blood fat
With.
Detailed description of the invention:
The structural formula of Fig. 1 OPD
Fig. 2 weight and organ coefficient
Index relevant to haemolysis in Fig. 3 blood routine (red blood cell, net are knitted red)
Experimental example 1: the effect for reducing blood fat of ophiopogonin D
Experimental design:
Dosage: ophiopogonin D dosage is 0.25mg/kg；
Administration mode: tail vein injection；
Administration time: 28 days；
Index collection: serum, automatic clinical chemistry analyzer measure the concentration of Triglycerides in Serum.
Data are as follows:
Influence of 1 ophiopogonin D of table to Triglycerides in Serum
Note: " * " indicates p < 0.05
4. conclusion: OPD plays the role of reducing blood lipid
The internal hemolytic experiment of experimental example 2:OPD
5 experimental groups are set, are that blank control group, OPD are applied alone group, OPD ' to be applied alone group, OPD+OPD ' combination group (mixed respectively
Given simultaneously after conjunction), OPD → OPD ' group (first to OPD, interval half an hour gives OPD ' again).
In order to comprehensively collect index, blood (blood routine and the blood biochemical of animal are acquired respectively after the administration is complete
Analysis), the urine (urine analysis of blood) of animal, conventional experimental data (weight, organ coefficient), some ginsengs relevant to haemolysis
Number (organs and tissues inspection, blood shadow analysis, blood film etc.).Surprisingly, blood lipid is had found inside blood biochemistry data
With the beneficial effect data of blood glucose.
One, test procedure:
Sample configuration method: OPD and OPD ' is configured to the mother liquor of high concentration with pure methanol respectively, then by the mother of high concentration
Liquid is diluted to required concentration.Because of OPD and OPD ' physiological saline solubility it is poor, therefore prepare when, by test tube one
Disposed upright dropwise instills mother liquor in normal saline dilution liquid in being vortexed on turbula shaker.Until OPD and OPD ' dissolution it is close
Saturation.General final injection give experimental animal by test solution, the content general control of methanol is 5% or so.
Administration mode: tail vein injection
Dosage period: 28 days
Dosage setting: OPD (0.25mg/kg), OPD ' (0.25mg/kg)
Experiment group: blank control group, OPD be applied alone group, OPD ' be applied alone group, OPD+OPD ' combination group (after mixing at the same to
Give), OPD → OPD ' group (first to OPD, interval half an hour gives OPD ' again).Every group 10.
Two, experimental data:
1 weight of table and organ coefficient
Blood routine data:
2 blood routine data of table
Blood biochemistry data:
Blood biochemistry data of the table 3 in addition to blood glucose and blood lipid
Routine urinalysis data:
The control of dosage of the present invention: being no more than 5 μ g/ml with the concentration of OPD ' in blood, (hemolysis in vitro tests haemolysis
The concentration of rate corresponding OPD ' when being 5%, clinic think that hemolysis rate is an acceptable limit value less than 5%) it is criterion, it is long
When phase medication, this dosage should also be further decreased, thus the blood concentration of OPD ' be no more than 5 μ g/ml may be considered one to
The limit value of medicine.But the blood concentration of OPD can not have upper limit value.
With the dosage of blood concentration conversion drug, ignore the distribution time that drug administration by injection enters blood.Such as when experiment is dynamic
When object (rat) weight is 200g, internal blood volume is about 10ml, then dosage is 10mlx5 μ g/ml=50 μ g, 50 μ
G/200g=0.25 μ g/g=0.25mg/kg.
The research of the invention finds that ophiopogonin D has the function of reducing blood lipid, having exploitation is new blood lipid-lowering medicine potentiality, and
Its validity, safety and controllability Study data are very friendly, and druggability is strong.
Embodiment 1
A kind of ophiopogonin D preparation, containing the 0.1mg/kg ophiopogonin D calculated with experimental rat dosage, and should
Content is the people's dosage obtained by weight of experimental rat dosage is to calculate basis；Ophiopogonin D preparation has in preparation
There is the application in the drug of effect for reducing blood fat.
Embodiment 2
A kind of ophiopogonin D preparation, containing the 0.25mg/kg ophiopogonin D calculated with experimental rat dosage, and should
Content is the people's dosage obtained by weight of experimental rat dosage is to calculate basis；Ophiopogonin D preparation has in preparation
There is the application in the drug of effect for reducing blood fat.
Embodiment 3
A kind of ophiopogonin D preparation, containing the 0.3mg/kg ophiopogonin D calculated with experimental rat dosage, and should
Content is the people's dosage obtained by weight of experimental rat dosage is to calculate basis；Ophiopogonin D preparation has in preparation
There is the application in the drug of effect for reducing blood fat.
Embodiment 4
A kind of ophiopogonin D preparation, containing the 0.35mg/kg ophiopogonin D calculated with experimental rat dosage, and should
Content is the people's dosage obtained by weight of experimental rat dosage is to calculate basis；Ophiopogonin D preparation has in preparation
There is the application in the drug of effect for reducing blood fat.
Embodiment 5
A kind of ophiopogonin D preparation, containing the 0.38mg/kg ophiopogonin D calculated with experimental rat dosage, and should
Content is the people's dosage obtained by weight of experimental rat dosage is to calculate basis；Ophiopogonin D preparation has in preparation
There is the application in the drug of effect for reducing blood fat.
Claims (7)
1. a kind of ophiopogonin D preparation with effect for reducing blood fat, it is characterised in that said preparation contains with experimental rat to medicament
The 0.1-0.4mg/kg ophiopogonin D calculated is measured, and the content can be and change according to experimental rat dosage to calculate basis
Obtained people's dosage.
2. ophiopogonin D preparation as described in claim 1, it is characterised in that said preparation contains 0.1mg/kg ophiopogonin D.
3. ophiopogonin D preparation as described in claim 1, it is characterised in that said preparation contains 0.25mg/kg ophiopogonin D.
4. ophiopogonin D preparation as described in claim 1, it is characterised in that said preparation contains 0.3mg/kg ophiopogonin D.
5. ophiopogonin D preparation as described in claim 1, it is characterised in that said preparation contains 0.35mg/kg ophiopogonin D.
6. ophiopogonin D preparation as described in claim 1, it is characterised in that said preparation contains 0.38mg/kg ophiopogonin D.
7. application of the ophiopogonin D preparation in the drug that preparation has effect for reducing blood fat as described in claim 1-6 is any.
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| CN201910408678.6A CN110403951A (en) | 2019-05-16 | 2019-05-16 | A kind of ophiopogonin D preparation and its blood lipid-lowering medicine new application |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN115089600A (en) * | 2022-06-28 | 2022-09-23 | 广东医科大学 | Application of ophiopogonin D in preparing anti-rotavirus drugs |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101327221A (en) * | 2008-07-18 | 2008-12-24 | 中国药科大学 | Medical use of Ophiopogon root saponin D as tissue factor pathway inhibitor |
| CN108042554A (en) * | 2017-10-27 | 2018-05-18 | 陈思禹 | Application of the ophiopogonin D on treatment metabolic syndrome drug is prepared |
-
2019
- 2019-05-16 CN CN201910408678.6A patent/CN110403951A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101327221A (en) * | 2008-07-18 | 2008-12-24 | 中国药科大学 | Medical use of Ophiopogon root saponin D as tissue factor pathway inhibitor |
| CN108042554A (en) * | 2017-10-27 | 2018-05-18 | 陈思禹 | Application of the ophiopogonin D on treatment metabolic syndrome drug is prepared |
Non-Patent Citations (1)
| Title |
|---|
| SIYU CHEN等: "Ophiopogonin D alleviates high-fat diet–induced metabolic syndrome and changes the structure of gut microbiota in mice", 《THE FASEB JOURNAL》 * |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN115089600A (en) * | 2022-06-28 | 2022-09-23 | 广东医科大学 | Application of ophiopogonin D in preparing anti-rotavirus drugs |
| CN115089600B (en) * | 2022-06-28 | 2023-08-04 | 广东医科大学 | Application of ophiopogonin D in preparation of rotavirus resistant medicines |
| WO2024001265A1 (en) * | 2022-06-28 | 2024-01-04 | 广东医科大学 | Use of ophiopogonin d in preparing anti-rotavirus medicament |
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Application publication date: 20191105 |
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