CN108888621A - L-spd inhibits application and its application method on near-sighted drug in preparation - Google Patents
L-spd inhibits application and its application method on near-sighted drug in preparation Download PDFInfo
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- CN108888621A CN108888621A CN201810518730.9A CN201810518730A CN108888621A CN 108888621 A CN108888621 A CN 108888621A CN 201810518730 A CN201810518730 A CN 201810518730A CN 108888621 A CN108888621 A CN 108888621A
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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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/10—Ophthalmic agents for accommodation disorders, e.g. myopia
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Abstract
A kind of l-spd inhibits application and its application method on near-sighted drug in preparation, passes through the l-spd in Chinese herbal medicine Japanese Stephania Root（L-SPD）Come while excitement D1 receptor and antagonism D2 receptor, it is suppressed that the extension of vitreous chamber and axis oculi during ultrastructure in form deprivation myopia, to inhibit the formation of zoopery myopia.
Description
Technical field
The present invention relates to myopia fields, and in particular to a kind of l-spd inhibits on near-sighted drug in preparation
Application and its application method.
Background technique
Dopamine is a kind of important monoamine neurotransmitter for adjusting organism many vital movements and physiological function.View
Dopamine on film plays an important role during adjusting eyeball development and axis oculi is grown.Early animal studies table
Bright, DOPAMINE CONTENT IN RABBIT reduces in retina in ultrastructure in form deprivation myopia forming process, is restored to normal level again in convalescence,
Its changing rule lapses to that degree height is consistent with ultrastructure in form deprivation myopia, and dopamine is prompted to take part in the formation of myopia.Separately grind
Study carefully the progress for showing that dopamine receptor non-selective agonist apomorphine can inhibit the animal myopias such as chicken, monkey, further
Illustrate that dopamine plays important protective effect during the occurrence and development of myopia.
Dopamine is played a role and acting on dopamine receptor.Early period drug research the results show that dopamine D 1 by
The regulating and controlling effect of body and D2 receptor in myopia is complicated and not yet clear.D1 receptor stimulating agent SKF38393 can inhibit cavy,
The mypia progression of mouse, but do not influence the ultrastructure in form deprivation myopia of chicken, and D1 receptor antagonist SCH23390 can promote it is small
The myopia progression of chicken.On the other hand, D2 receptor stimulating agent Quinpirole is more intricate to the myopia progression effect of animal：
It promotes the mypia progression of cavy, but inhibits the myopia progression of chicken, and to the myopia of mouse with dependence in different agent
Measure and play the effect of double regulation control.
L-spd（L-SPD）, it is a kind of active constituent extracted from Chinese herbal medicine Stephania, has
The dual pharmacological of excitement D1 receptor and antagonism D2 receptor effect simultaneously.
Discovery there is no to have L-SPD to the report of myopia effect so far.We guess, can use it to dopamine D 1
Double action with D2 receptor can achieve the purpose that intervention development of myopia to large extent, provide theory for its clinical application
Foundation.
Summary of the invention
In order to solve the deficiencies in the prior art, the present invention provides l-spds to inhibit on near-sighted drug in preparation
Application and its application method.
The technical solution that the present invention uses is：A kind of l-spd answering on the near-sighted drug of preparation inhibition
With.
The l-spd（L-SPD）It is obtained by being extracted in Chinese herbal medicine Japanese Stephania Root.
The l-spd（L-SPD）The dosage in myopia is being inhibited to be 4-40 mg/kg/day.
A kind of application method of l-spd, includes the following steps：Under dark condition, by left-handed Japanese Stephania Root pyridine
Alkali（L-SPD）It is dissolved in 10% dimethyl formamide solution（DMF）In, PH to 5 ~ 6 is adjusted with acetic acid, and make it completely dissolved, black
It is injected intraperitoneally under dark condition.
The beneficial effects of the invention are as follows：The present invention provides a kind of l-spds to inhibit on near-sighted drug in preparation
Application and its application method, pass through the l-spd in Chinese herbal medicine Japanese Stephania Root（L-SPD）Come while excitement D1 receptor
With antagonism D2 receptor, it is suppressed that the extension of vitreous chamber and axis oculi during ultrastructure in form deprivation myopia, to inhibit animal
The formation of experimental myopia.
Detailed description of the invention
The influence that Fig. 1 .L-SPD develops mouse emmetropia.
Influence of Fig. 2 L-SPD to mouse ultrastructure in form deprivation myopia.
Specific embodiment
Experimental animal is three week old C57BL/6 mouse.The qualified mouse of screening is randomly divided into two big groups, is normal respectively
Dioptric development group and ultrastructure in form deprivation myopia group.The former raises in normal illumination environment, and the latter carries out continuing the simple eye of surrounding
Form deprivation, Second eye are own control eye.Each big group is randomly divided into four groups again：Respectively blank control group, solvent group
（10% dimethylformamide）, low-dose drugs group（4mg/kg）With high dose medicament group（40mg/kg）.Continuous surrounding is daily
Intraperitoneal injection.Before experiment and after experiment, the diopter and axiallength of measurement record mouse, anterior chamber depth are brilliant respectively
The eyeballs biological parameter such as body thickness and vitreous cavity depth, and compare diopter and each biology before and after each group mouse experiment
The variation of parameter.
L-SPD is dissolved in 10% dimethyl formamide solution（DMF）In, PH to 5 ~ 6 is adjusted with acetic acid, and make it completely dissolved.
Consulting lot of documents, comprehensively consider drug effective dose 50 and its in conjunction with receptor after specific biological effect after select
Dosage is respectively the L-SPD solution of 4mg/kg and 40mg/kg, and solvent group gives isometric DMF solution.Daily morning bright light
Isometric drug or solvent is injected intraperitoneally in 1 hour afterwards.To avoid drug from decomposing in light, all drugs and solvent injection process are equal
It is unified in darkroom and carries out.
Biological parameter difference before testing in each group and between group it is not significant (P > 0.05).After experiment, emmetropia
Biological parameter in development group each group between mouse eyes is not statistically significant（P >0.05, paired t-test）.It is small between each group
Biological parameter is also without significant statistical difference between mouse images of left and right eyes（P >0.05, one-way analysis of variance）.Illustrate 4 weeks
L-SPD drug-treated does not influence the emmetropia development of mouse.
After experiment, simple form deprivation group and form deprivation solvent group have all induced apparent myopia amount（FD：8.07
± 1.40 D；FD+Vehicle：9.32 ± 0.90 D), the L-SPD of low dosage 4mg/kg/day inhibits about 90% shape to feel
The property deprived myopia (FD+L-SPD-4 vs FD+Vehicle：0.79 ± 1.83 D vs, 9.32 ± 0.90 D,P <
0.01, one-way analysis of variance), and the L-SPD of high dose 40mg/kg/day inhibits about 70% ultrastructure in form deprivation myopia（FD
+L-SPD-40 vs FD-Vehicle：2.76 ± 1.30 D vs, 9.32 ± 0.90 D,P < 0.01）.Meanwhile it is more molten
Agent group is compared, and the L-SPD of low dosage 4mg/kg/day also inhibits vitreous cavity depth (FD+L-SPD-4 vs FD+
Vehicle：0.029 ± 0.010 mm vs, 0.008 ± 0.006 mm,P <0.05, one-way analysis of variance) and axis oculi
Extension (FD+L-SPD-4 vs FD+Vehicle：0.031 ± 0.011 mm vs, 0.003 ± 0.007 mm,P <
0.05, one-way analysis of variance).Therefore, intraperitoneal injection L-SPD can inhibit the formation of mouse ultrastructure in form deprivation myopia.
Experimental result is as shown in Figure 1 and Figure 2：
Fig. 1 is the influence that L-SPD develops mouse emmetropia.As a result illustrate, the L-SPD processing of various dose does not influence just
Diopter, vitreous cavity depth and the axiallength of normal dioptric development mouse.
Fig. 2 is influence of the L-SPD to mouse ultrastructure in form deprivation myopia.As a result illustrate, the L-SPD of 4mg/kg and 40mg/kg
Processing group is formed by myopia amount and is obviously less than solvent group, while the L-SPD processing of 4mg/kg also inhibits vitreous chamber depth
The extension of degree and axiallength, illustrates that L-SPD inhibits the development of ultrastructure in form deprivation myopia.*P<0.05, * *P<0.01,
One-way analysis of variance.
The above is only a preferred embodiment of the present invention, protection scope of the present invention is not limited merely to above-mentioned implementation
Example, all technical solutions belonged under thinking of the present invention all belong to the scope of protection of the present invention.It should be pointed out that for the art
Those of ordinary skill for, several improvements and modifications without departing from the principles of the present invention, these improvements and modifications
It should be regarded as protection scope of the present invention.
Claims (4)
1. a kind of l-spd inhibits the application on near-sighted drug in preparation.
2. l-spd according to claim 1 inhibits the application on near-sighted drug in preparation, which is characterized in that
The l-spd（L-SPD）It is obtained by being extracted in Chinese herbal medicine Japanese Stephania Root.
3. l-spd according to claim 1 inhibits the application on near-sighted drug in preparation, which is characterized in that
The l-spd（L-SPD）The dosage in myopia is being inhibited to be 4-40 mg/kg/day.
4. a kind of application method of l-spd described in claim 1, which is characterized in that include the following steps：?
Under dark condition, by l-spd（L-SPD）It is dissolved in 10% dimethyl formamide solution（DMF）In, PH is adjusted with acetic acid
It to 5 ~ 6, and makes it completely dissolved, is injected intraperitoneally under dark condition.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201810518730.9A CN108888621B (en) | 2018-05-25 | 2018-05-25 | Application of levo-stepholidine in preparing medicine for inhibiting myopia and use method thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201810518730.9A CN108888621B (en) | 2018-05-25 | 2018-05-25 | Application of levo-stepholidine in preparing medicine for inhibiting myopia and use method thereof |
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| Publication Number | Publication Date |
|---|---|
| CN108888621A true CN108888621A (en) | 2018-11-27 |
| CN108888621B CN108888621B (en) | 2021-02-26 |
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| CN201810518730.9A Active CN108888621B (en) | 2018-05-25 | 2018-05-25 | Application of levo-stepholidine in preparing medicine for inhibiting myopia and use method thereof |
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