CN106729152A - The application of seed of Job's tears shell and seed of Job's tears kind bark extract and Chinese medicine composition and preparation method containing it - Google Patents
The application of seed of Job's tears shell and seed of Job's tears kind bark extract and Chinese medicine composition and preparation method containing it Download PDFInfo
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Abstract
The present invention proposes the application of seed of Job's tears shell and seed of Job's tears kind bark extract in acetylcholinesteraseinhibitors inhibitors, and a kind of Chinese medicine composition of acetylcholine esterase inhibition and preparation method thereof is proposed simultaneously, calculate by weight, the weight portion of each bulk drug is respectively in the Chinese medicine composition：1~10 part of 30~50 parts of seed of Job's tears shell, 30~50 parts of seed of Job's tears kind skin, 1~10 part of fructus alpiniae oxyphyllae, 1~10 part of ginkgo leaf, 1~10 part of pseudo-ginseng and the root of large-flowered skullcap.Mutual Synergistic between each component, with good inhibiting activity of acetylcholinesterase, can be applied to treat the newtype drug of Alzheimer's disease, and preparation method of the present invention can obtain the acetylcholinesterase inhibitor thing of high activity.
Description
Technical field
The present invention relates to technical field of traditional Chinese medicines, the more particularly to application of seed of Job's tears shell and seed of Job's tears kind bark extract and containing it
Chinese medicine composition and preparation method.
Background technology
Found through modern study, the active composition of coix seed is more and the two big outstanding features that are of high nutritive value, such as containing rich
Rich protein, carbohydrate, vitamin, Coixol, sitosterol, alkaloid, amino acid, adenosine and coix seed fat and coix seed are more
The nutritional ingredients such as sugar and active component, and rich in several amino acids and the various unrighted acids beneficial to human body.But, the heart of a lotus seed
Rice shell and seed of Job's tears kind skin are the byproducts of seed of Job's tears deep processing, but up to now, the resource is not efficiently utilized, if energy
Seed of Job's tears shell and seed of Job's tears kind skin are able to effectively utilize, the functional Chinese medicine composition of tool of high-quality is developed, and extend product
Product chain, will greatly improve its added value, there is great Social benefit and economic benefit.Present invention firstly provides seed of Job's tears shell and the heart of a lotus seed
Application of the rice kind bark extract in acetylcholine esterase inhibition preparation.
It is difficult that nerve degenerative diseases such as Alzheimer disease, Huntington's disease and Parkinson's disease etc. belong to clinical medicine
Topic and major disease category, Alzheimer disease are mainly shown as the extensive death of brain cell, and the brain of particularly basal ganglia region is thin
Born of the same parents.Under normal circumstances, to the brain cortex relevant with memory and cognition, it discharges acetyl courage to the Fiber Projections that basal ganglia region sends
Alkali.The formation of short-term memory must have the participation of acetylcholine, the content ratio of patient's acetylcholine transferase compared with normal person
Normal person reduces 90%.Acetylcholinesterase (AchE) is considered as the target spot of the screening anti-Alzheimer disease medicine of,
The nerve retrograde affections such as treatment Alzheimer disease are will be helpful to using the excessive AchE activity of Drug inhibition.Cholinergic drug
The levels of acetylcholine for being improved by suppressing cholinesterase (AchE) in patient body improves cognition and the behavior disorder of patient, subtracts
The progress of slow disease, to improving short-term memory effect substantially, such as huperzine, donepezil, Rivastigmine belong to cholinester
Enzyme inhibitor medicine, but curative effect is undesirable.Antioxidant vitamin E treatments have preferable security and tolerance, and stimulate
The neurotransmitter relevant with cognition improves brain environment.Also some other medicine such as selegiline, non-steroid
Anti-inflammatory agent etc., the medicine of all these treatment senile dementia is all to be improved.Existing clinical medicine can not meet treatment needs,
There are problems：As pharmaceutical activity is not strong, medicine time side effect long substantially, patient occur drug resistance, curative effect decline, import
Drug price costliness etc., is badly in need of research high-efficiency low-toxicity, the new drug of the anti-Alzheimer disease of few side effects.
The content of the invention
Reflect with this, it is an object of the invention to propose seed of Job's tears shell and seed of Job's tears kind bark extract in acetylcholine esterase inhibition side
The application in face, while proposing a kind of Chinese medicine composition for being capable of acetylcholine esterase inhibition and preparation method thereof.
The technical proposal of the invention is realized in this way：
A kind of application of seed of Job's tears shell and seed of Job's tears kind bark extract in acetylcholinesteraseinhibitors inhibitors.
Further, it is applied to a kind of Chinese medicine composition of acetylcholine esterase inhibition activity.
A kind of Chinese medicine composition of acetylcholine esterase inhibition, calculates by weight, each raw material in the Chinese medicine composition
The weight portion of medicine is respectively：30~50 parts of seed of Job's tears shell, 30~50 parts of seed of Job's tears kind skin, 1~10 part of fructus alpiniae oxyphyllae, 1~10 part of ginkgo leaf,
1~10 part of 1~10 part of pseudo-ginseng and the root of large-flowered skullcap.
Further, calculate by weight, the weight portion of each bulk drug is respectively in the Chinese medicine composition：Seed of Job's tears shell 40
5 parts of part, 40 parts of seed of Job's tears kind skin, 5 parts of fructus alpiniae oxyphyllae, 5 parts of ginkgo leaf, 5 parts of pseudo-ginseng and the root of large-flowered skullcap.
Further, calculate by weight, seed of Job's tears shell：Seed of Job's tears kind skin：Fructus alpiniae oxyphyllae：Ginkgo leaf：Pseudo-ginseng：The mass ratio of the root of large-flowered skullcap
It is 8:8:1:1:1:1.
The preparation method of the Chinese medicine composition of the acetylcholine esterase inhibition, comprises the following steps：
(1) crush：Seed of Job's tears shell, seed of Job's tears kind skin, fructus alpiniae oxyphyllae, ginkgo leaf, pseudo-ginseng and root of large-flowered skullcap raw material were crushed to 100~
200 mesh sieves；
(2) soak：Add water and soaked；
(3) degreasing removes wax：Material is added in 2~10 times of sodium hydroxide solutions of 1~2% mass concentration of volume,
Stir and boil, carrying out degreasing to material removes 30~60min of Lasaxing Oilfield；
(4) clean：Centrifugation filtrate, by the precipitation washing obtained by centrifugation, water lotion merges that to obtain raw material thick with filtrate
Liquid；
(5) decoct：The thick liquid of raw material is heated into 10~20min at 120~140 DEG C；Then temperature is reduced to 60~70 DEG C,
Continue to heat 30~60min；High-temperature to 120~140 DEG C being risen again, continuing to heat 10~20min, centrifugation obtains material liquid；
(6) concentrate：Enrichment materials liquid is the thick paste of relative density 1.1~1.2 under room temperature environment.
Further, in the step (2), 2~10 times of water of volume are added to carry out 1~12h of immersion treatment.
Further, in the step (3), material is added to 5 times of sodium hydroxide solutions of 1% mass concentration of volume
In, stir and boil, carrying out degreasing to material removes Lasaxing Oilfield 30min.
Further, step (5) decoction process is：10min is heated at 130 DEG C；Then temperature is reduced to 65 DEG C,
Continue to heat 60min；High-temperature to 130 DEG C is risen again, continues to heat 10min.
Compared with prior art, beneficial effects of the present invention are：
The present invention proposes the application of seed of Job's tears shell and seed of Job's tears kind bark extract in terms of acetylcholine esterase inhibition, and it has
Obvious acetylcholine ester enzyme inhibition rate.Based on seed of Job's tears shell and seed of Job's tears kind skin raw material, be equipped with fructus alpiniae oxyphyllae, ginkgo leaf, pseudo-ginseng with
And the Chinese medicine composition of a kind of acetylcholine esterase inhibition that the root of large-flowered skullcap is obtained, mutual Synergistic between each component, with good
Good inhibiting activity of acetylcholinesterase, can be applied to treat the newtype drug of Alzheimer's disease.Additionally, preparation side of the invention
Method can obtain the acetylcholinesterase inhibitor thing of high activity.
Specific embodiment
It is that the technical scheme in the present invention is clearly and completely described, it is clear that inventor is said in conjunction with the embodiments
It is bright, but the only a part of embodiment of the invention described by following examples, rather than whole embodiments.Based on the present invention
In embodiment, the every other implementation that those of ordinary skill in the art are obtained under the premise of creative work is not made
Example, belongs to the scope of protection of the invention.
The present invention proposes a kind of application of seed of Job's tears shell and seed of Job's tears kind bark extract in acetylcholine esterase inhibition activity, should
Used time, required various auxiliary materials or pharmaceutically acceptable when prepared by seed of Job's tears shell and seed of Job's tears kind bark extract addition into different dosage forms
After excipient or carrier, any suitable clinical preparation can be prepared into conventional drug formulation process, for example, can be
Injection (powder pin, freeze-dried powder, liquid drugs injection, transfusion etc.), tablet, oral liquid, granule, capsule, soft capsule, dripping pill etc..Its
In, described auxiliary material can be antioxygen complexing agent, filler, framework material etc.；Described pharmaceutically acceptable carrier is wood
Sugar alcohol, mannitol, lactose, fructose, glucan, glucose, polyvinylpyrrolidone, D-40, sodium chloride, grape
One or more in Calciofon or calcium phosphate, preferably mannitol or lactose.
Embodiment 1
A kind of seed of Job's tears shell and seed of Job's tears kind bark extract, have following preparation method to be obtained：
(1) crush：Seed of Job's tears shell, seed of Job's tears kind skin were crushed to 100~200 mesh sieves；
(2) soak：Add water and soaked；
(3) degreasing removes wax：Material is added in 5 times of sodium hydroxide solutions of 1% mass concentration of volume, is stirred
And boil, carrying out degreasing to material removes Lasaxing Oilfield 30min；
(4) clean：Centrifugation filtrate, by the precipitation washing obtained by centrifugation, water lotion merges that to obtain raw material thick with filtrate
Liquid；
(5) decoct：The thick liquid of raw material is heated into 10min at 130 DEG C；Then temperature is reduced to 65 DEG C, continues to heat
60min；High-temperature to 130 DEG C being risen again, continuing to heat 60min, centrifugation obtains material liquid；
(6) concentrate：Enrichment materials liquid is the thick paste of relative density 1.1~1.2 under room temperature environment, as product.
Acetylcholine esterase inhibition activity measurement result
1) experiment condition
A, material：DMSO (dimethyl sulfoxide (DMSO))；KH2PO4、K2HPO4·3 H2O；AchE enzymes；PNPG.
B, laboratory apparatus：The types of multi-function microplate reader Bio-Rad Model 680 (Bio-Rad Laboratories Inc.)
2) experimental technique and process
Sample treatment：The sample of 1mg embodiments 1 is dissolved in 20 μ L dimethyl sulfoxide (DMSO)s (DMSO) as mother liquor, 1 μ L mother liquors is taken and is added
Enter 249 μ L distilled water and be made into 200 μ gmL-1Solution.
The AchE inhibitory activity of determination sample in 96 hole elisa Plates.Concrete operations are as follows：In 96 hole elisa Plates successively
Add 20 μ L PB (100mM, pH 8.0), 25 μ L AChE (0.033U/mL, pH 8.0PB dissolved dilutions), 25 μ L sample solution
(40μg·mL- 1).After ice bath 5min, plus 15 μ L ATCI (0.6mM) and 15 μ L DTNB (1.5mM).After 37 DEG C are incubated 60min,
Its absorbance is determined under 412nm with ELIASA, experiment is averaged in triplicate, and inhibiting rate is calculated according to following formula：
Inhibition of enzyme activity rate %=[ABlank-(ASample-ABackground)]/ABlank×100
A in formulaBlank：It is not added with the absorption value after example reaction；
ASample：Add the absorption value after example reaction；
ABackground：Only it is loaded the absorption value of product.
3) experimental result is as shown in table 1：
Table 1
| Blank | Background | The sample of embodiment 1 | |
| OD values | 0.014 | 0.208 | 0.221 |
| 0.013 | 0.222 | 0.243 | |
| 0.012 | 0.219 | 0.209 | |
| Average | 0.013 | 0.216 | 0.224 |
| Inhibiting rate (%) | 38.4 |
Cross above example and can be shown that seed of Job's tears shell proposed by the present invention and seed of Job's tears kind bark extract have preferably suppression to AchE
Activity, in can be applied to the medicine preparation of the nerve retrograde affections such as anti-Alzheimer disease, with important application prospect.
Embodiment 2
Based on the application, the present invention also proposes a kind of Chinese medicine composition of acetylcholine esterase inhibition, calculates by weight,
The weight portion of each bulk drug is respectively in the Chinese medicine composition：30 parts of seed of Job's tears shell, 30 parts of seed of Job's tears kind skin, 1 part of fructus alpiniae oxyphyllae, ginkgo
1 part of 1 part of leaf, 1 part of pseudo-ginseng and the root of large-flowered skullcap.
The preparation method of the Chinese medicine composition, comprises the following steps：
(1) crush：Seed of Job's tears shell, seed of Job's tears kind skin, fructus alpiniae oxyphyllae, ginkgo leaf, pseudo-ginseng and root of large-flowered skullcap raw material were crushed to 100~
200 mesh sieves；
(2) soak：Adding 10 times of water of volume carries out immersion treatment 6h；
(3) degreasing removes wax：Material is added in 5 times of sodium hydroxide solutions of 1% mass concentration of volume, is stirred
And boil, carrying out degreasing to material removes Lasaxing Oilfield 30min；
(4) clean：Centrifugation filtrate, by the precipitation washing obtained by centrifugation, water lotion merges that to obtain raw material thick with filtrate
Liquid；
(5) decoct：10min is heated at 130 DEG C；Then temperature is reduced to 65 DEG C, continues to heat 60min；High temperature is risen again
Degree continues to heat 10min to 130 DEG C, and centrifugation obtains material liquid；
(6) concentrate：Enrichment materials liquid is the thick paste of relative density 1.1~1.2 under room temperature environment.
Acetylcholine esterase inhibition activity measurement result
1) experiment condition
A, material：DMSO (dimethyl sulfoxide (DMSO)) (Ke Miou companies)；KH2PO4, K2HPO43 H2O (Shantou, Guangdong city west
Gansu Province chemical plant)；AchE enzymes (Sigma Co., USA)；PNPG (Sigma Co., USA)
B, laboratory apparatus：The types of multi-function microplate reader Bio-Rad Model 680 (Bio-Rad Laboratories Inc.)
2) experimental technique and process
Sample treatment：The sample of 1mg embodiments 2 is dissolved in 20 μ L dimethyl sulfoxide (DMSO)s (DMSO) as mother liquor, 1 μ L mother liquors is taken and is added
Enter 249 μ L distilled water and be made into 200 μ gmL-1Solution.
The AchE inhibitory activity of determination sample in 96 hole elisa Plates.Concrete operations are as follows：In 96 hole elisa Plates successively
Add 20 μ L PB (100mM, pH 8.0), 25 μ L AChE (0.033U/mL, pH 8.0PB dissolved dilutions), 25 μ L sample solution
(40μg·mL- 1).After ice bath 5min, plus 15 μ L ATCI (0.6mM) and 15 μ L DTNB (1.5mM).After 37 DEG C are incubated 60min,
Its absorbance is determined under 412nm with ELIASA, experiment is averaged in triplicate, and inhibiting rate is calculated according to following formula：
Inhibition of enzyme activity rate %=[ABlank-(ASample-ABackground)]/ABlank×100
A in formulaBlank：It is not added with the absorption value after example reaction；
ASample：Add the absorption value after example reaction；
ABackground：Only it is loaded the absorption value of product.
4) experimental result is as shown in table 2：
Table 2
Embodiment 3
A kind of Chinese medicine composition of acetylcholine esterase inhibition, calculates by weight, each raw material in the Chinese medicine composition
The weight portion of medicine is respectively：40 parts of seed of Job's tears shell, 40 parts of seed of Job's tears kind skin, 5 parts of fructus alpiniae oxyphyllae, 5 parts of ginkgo leaf, 5 parts of pseudo-ginseng and the root of large-flowered skullcap 5
Part.
The preparation method of the Chinese medicine composition of the acetylcholine esterase inhibition, comprises the following steps：
(1) crush：Seed of Job's tears shell, seed of Job's tears kind skin, fructus alpiniae oxyphyllae, ginkgo leaf, pseudo-ginseng and root of large-flowered skullcap raw material were crushed to 100~
200 mesh sieves；
(2) soak：Adding 10 times of water of volume carries out immersion treatment 6h；
(3) degreasing removes wax：Material is added in 5 times of sodium hydroxide solutions of 1% mass concentration of volume, is stirred
And boil, carrying out degreasing to material removes Lasaxing Oilfield 30min；
(4) clean：Centrifugation filtrate, by the precipitation washing obtained by centrifugation, water lotion merges that to obtain raw material thick with filtrate
Liquid；
(5) decoct：10min is heated at 130 DEG C；Then temperature is reduced to 65 DEG C, continues to heat 60min；High temperature is risen again
Degree continues to heat 10min to 130 DEG C, and centrifugation obtains material liquid；
(6) concentrate：Enrichment materials liquid is the thick paste of relative density 1.1~1.2 under room temperature environment.
Acetylcholine esterase inhibition activity measurement result
1) experiment condition
A, material：DMSO (dimethyl sulfoxide (DMSO)) (Ke Miou companies)；KH2PO4, K2HPO43 H2O (Shantou, Guangdong city west
Gansu Province chemical plant)；AchE enzymes (Sigma Co., USA)；PNPG (Sigma Co., USA)
B, laboratory apparatus：The types of multi-function microplate reader Bio-Rad Model 680 (Bio-Rad Laboratories Inc.)
2) experimental technique and process
Sample treatment：The sample of 1mg embodiments 3 is dissolved in 20 μ L dimethyl sulfoxide (DMSO)s (DMSO) as mother liquor, 1 μ L mother liquors is taken and is added
Enter 249 μ L distilled water and be made into 200 μ gmL-1Solution.
The AchE inhibitory activity of determination sample in 96 hole elisa Plates.Concrete operations are as follows：In 96 hole elisa Plates successively
Add 20 μ L PB (100mM, pH 8.0), 25 μ L AChE (0.033U/mL, pH 8.0PB dissolved dilutions), 25 μ L sample solution
(40μg·mL- 1).After ice bath 5min, plus 15 μ L ATCI (0.6mM) and 15 μ L DTNB (1.5mM).After 37 DEG C are incubated 60min,
Its absorbance is determined under 412nm with ELIASA, experiment is averaged in triplicate, and inhibiting rate is calculated according to following formula：
Inhibition of enzyme activity rate %=[ABlank-(ASample-ABackground)]/ABlank×100
A in formulaBlank：It is not added with the absorption value after example reaction；
ASample：Add the absorption value after example reaction；
ABackground：Only it is loaded the absorption value of product.
5) experimental result is as shown in table 3：
Table 3
Embodiment 4
A kind of Chinese medicine composition of acetylcholine esterase inhibition, calculates by weight, each raw material in the Chinese medicine composition
The weight portion of medicine is respectively：50 parts of seed of Job's tears shell, 50 parts of seed of Job's tears kind skin, 10 parts of fructus alpiniae oxyphyllae, 10 parts of ginkgo leaf, 10 parts of pseudo-ginseng and Huang
10 parts of a kind of reed mentioned in ancient books.
The preparation method of the Chinese medicine composition of the acetylcholine esterase inhibition, comprises the following steps：
(1) crush：Seed of Job's tears shell, seed of Job's tears kind skin, fructus alpiniae oxyphyllae, ginkgo leaf, pseudo-ginseng and root of large-flowered skullcap raw material were crushed to 100~
200 mesh sieves；
(2) soak：Adding 10 times of water of volume carries out immersion treatment 6h；
(3) degreasing removes wax：Material is added in 5 times of sodium hydroxide solutions of 1% mass concentration of volume, is stirred
And boil, carrying out degreasing to material removes Lasaxing Oilfield 30min；
(4) clean：Centrifugation filtrate, by the precipitation washing obtained by centrifugation, water lotion merges that to obtain raw material thick with filtrate
Liquid；
(5) decoct：10min is heated at 130 DEG C；Then temperature is reduced to 65 DEG C, continues to heat 60min；High temperature is risen again
Degree continues to heat 10min to 130 DEG C, and centrifugation obtains material liquid；
(6) concentrate：Enrichment materials liquid is the thick paste of relative density 1.1~1.2 under room temperature environment.
Acetylcholine esterase inhibition activity measurement result
1) experiment condition
A, material：DMSO (dimethyl sulfoxide (DMSO)) (Ke Miou companies)；KH2PO4, K2HPO43 H2O (Shantou, Guangdong city west
Gansu Province chemical plant)；AchE enzymes (Sigma Co., USA)；PNPG (Sigma Co., USA)
B, laboratory apparatus：The types of multi-function microplate reader Bio-Rad Model 680 (Bio-Rad Laboratories Inc.)
2) experimental technique and process
Sample treatment：The sample of 1mg embodiments 4 is dissolved in 20 μ L dimethyl sulfoxide (DMSO)s (DMSO) as mother liquor, 1 μ L mother liquors is taken and is added
Enter 249 μ L distilled water and be made into 200 μ gmL-1Solution.
The AchE inhibitory activity of determination sample in 96 hole elisa Plates.Concrete operations are as follows：In 96 hole elisa Plates successively
Add 20 μ L PB (100mM, pH 8.0), 25 μ L AChE (0.033U/mL, pH 8.0PB dissolved dilutions), 25 μ L sample solution
(40μg·mL- 1).After ice bath 5min, plus 15 μ L ATCI (0.6mM) and 15 μ L DTNB (1.5mM).After 37 DEG C are incubated 60min,
Its absorbance is determined under 412nm with ELIASA, experiment is averaged in triplicate, and inhibiting rate is calculated according to following formula：
Inhibition of enzyme activity rate %=[ABlank-(ASample-ABackground)]/ABlank×100
A in formulaBlank：It is not added with the absorption value after example reaction；
ASample：Add the absorption value after example reaction；
ABackground：Only it is loaded the absorption value of product.
6) experimental result is as shown in table 4：
Table 4
Embodiment 2 to embodiment 4 experimental result understand, a kind of Chinese medicine composition of acetylcholine esterase inhibition, by weight
Amount part calculates, and optimum formula is the formula of embodiment 3, as：40 parts of seed of Job's tears shell, 40 parts of seed of Job's tears kind skin, 5 parts of fructus alpiniae oxyphyllae, ginkgo
5 parts of 5 parts of leaf, 5 parts of pseudo-ginseng and the root of large-flowered skullcap, i.e., when seed of Job's tears shell：Seed of Job's tears kind skin：Fructus alpiniae oxyphyllae：Ginkgo leaf：Pseudo-ginseng：The mass ratio of the root of large-flowered skullcap
It is 8:8:1:1:1:When 1, its acetylcholine esterase active inhibiting rate is best.
Additionally, by taking the optimum formula of embodiment 3 as an example, studying the technological parameter of preparation method, embodiment 5 and embodiment are carried out
6：
Embodiment 5
A kind of preparation method of the Chinese medicine composition of acetylcholine esterase inhibition, comprises the following steps：
(1) crush：Seed of Job's tears shell, seed of Job's tears kind skin, fructus alpiniae oxyphyllae, ginkgo leaf, pseudo-ginseng and root of large-flowered skullcap raw material were crushed to 100~
200 mesh sieves；
(2) soak：Adding 2 times of water of volume carries out immersion treatment 1h；
(3) degreasing removes wax：Material is added in 2 times of sodium hydroxide solutions of 1% mass concentration of volume, is stirred
And boil, carrying out degreasing to material removes Lasaxing Oilfield 30min；
(4) clean：Centrifugation filtrate, by the precipitation washing obtained by centrifugation, water lotion merges that to obtain raw material thick with filtrate
Liquid；
(5) decoct：The thick liquid of raw material is heated into 10min at 120 DEG C；Then temperature is reduced to 60 DEG C, continues to heat
30min；High-temperature to 120 DEG C being risen again, continuing to heat 10min, centrifugation obtains material liquid；
(6) concentrate：Enrichment materials liquid is the thick paste of relative density 1.1~1.2 under room temperature environment.
Acetylcholine esterase inhibition activity measurement result：Acetylcholine esterase active inhibiting rate is 60.5%.
Embodiment 6
A kind of preparation method of the Chinese medicine composition of acetylcholine esterase inhibition, comprises the following steps：
(1) crush：Seed of Job's tears shell, seed of Job's tears kind skin, fructus alpiniae oxyphyllae, ginkgo leaf, pseudo-ginseng and root of large-flowered skullcap raw material were crushed to 100~
200 mesh sieves；
(2) soak：Adding 5 times of water of volume carries out immersion treatment 12h；
(3) degreasing removes wax：Material is added in 10 times of sodium hydroxide solutions of 2% mass concentration of volume, stirring is equal
Even and boil, carrying out degreasing to material removes Lasaxing Oilfield 60min；
(4) clean：Centrifugation filtrate, by the precipitation washing obtained by centrifugation, water lotion merges that to obtain raw material thick with filtrate
Liquid；
(5) decoct：The thick liquid of raw material is heated into 20min at 140 DEG C；Then temperature is reduced to 70 DEG C, continues to heat
60min；High-temperature to 140 DEG C being risen again, continuing to heat 20min, centrifugation obtains material liquid；
(6) concentrate：Enrichment materials liquid is the thick paste of relative density 1.1~1.2 under room temperature environment.
Acetylcholine esterase inhibition activity measurement result：Acetylcholine esterase active inhibiting rate is 62.3%.
In sum, the present invention proposes seed of Job's tears shell and seed of Job's tears kind bark extract answering in terms of acetylcholine esterase inhibition
With, and it has obvious acetylcholine ester enzyme inhibition rate.Based on seed of Job's tears shell and seed of Job's tears kind skin raw material, fructus alpiniae oxyphyllae, silver are equipped with
A kind of Chinese medicine composition of acetylcholine esterase inhibition that apricot leaf, pseudo-ginseng and the root of large-flowered skullcap are obtained, mutually cooperates between each component
Synergy, with good inhibiting activity of acetylcholinesterase, can be applied to treat the newtype drug of Alzheimer's disease.Additionally,
Preparation method of the present invention can obtain the acetylcholinesterase inhibitor thing of high activity.
Presently preferred embodiments of the present invention is the foregoing is only, is not intended to limit the invention, it is all in essence of the invention
Within god and principle, any modification, equivalent substitution and improvements made etc. should be included within the scope of the present invention.
Claims (9)
1. the application of seed of Job's tears shell and seed of Job's tears kind bark extract, it is characterised in that the application in acetylcholinesteraseinhibitors inhibitors.
2. the application of seed of Job's tears shell according to claim 1 and seed of Job's tears kind bark extract, it is characterised in that be applied to a kind of suppression
The Chinese medicine composition of acetylcholine esterase active processed.
3. a kind of Chinese medicine composition of acetylcholine esterase inhibition, it is characterised in that calculate by weight, the Chinese medicine composition
In the weight portion of each bulk drug be respectively：30~50 parts of seed of Job's tears shell, 30~50 parts of seed of Job's tears kind skin, 1~10 part of fructus alpiniae oxyphyllae, ginkgo leaf
1~10 part of 1~10 part, 1~10 part of pseudo-ginseng and the root of large-flowered skullcap.
4. the Chinese medicine composition of acetylcholine esterase inhibition according to claim 3, it is characterised in that by weight
Calculate, the weight portion of each bulk drug is respectively in the Chinese medicine composition：40 parts of seed of Job's tears shell, 40 parts of seed of Job's tears kind skin, 5 parts of fructus alpiniae oxyphyllae,
5 parts of 5 parts of ginkgo leaf, 5 parts of pseudo-ginseng and the root of large-flowered skullcap.
5. the Chinese medicine composition of acetylcholine esterase inhibition according to claim 3, it is characterised in that by weight
Calculate, seed of Job's tears shell：Seed of Job's tears kind skin：Fructus alpiniae oxyphyllae：Ginkgo leaf：Pseudo-ginseng：The mass ratio of the root of large-flowered skullcap is 8:8:1:1:1:1.
6. the preparation method of the Chinese medicine composition of acetylcholine esterase inhibition according to claim 3, it is characterised in that bag
Include following steps：
(1) crush：Seed of Job's tears shell, seed of Job's tears kind skin, fructus alpiniae oxyphyllae, ginkgo leaf, pseudo-ginseng and root of large-flowered skullcap raw material were crushed to 100~200
Mesh sieve；
(2) soak：Add water and soaked；
(3) degreasing removes wax：Material is added in 2~10 times of sodium hydroxide solutions of 1~2% mass concentration of volume, is stirred
Uniform and boil, carrying out degreasing to material removes 30~60min of Lasaxing Oilfield；
(4) clean：Centrifugation filtrate, by the precipitation washing obtained by centrifugation, water lotion merges with filtrate and obtains the thick liquid of raw material；
(5) decoct：The thick liquid of raw material is heated into 10~20min at 120~140 DEG C；Then temperature is reduced to 60~70 DEG C, is continued
30~60min of heating；High-temperature to 120~140 DEG C being risen again, continuing to heat 10~20min, centrifugation obtains material liquid；
(6) concentrate：Enrichment materials liquid is the thick paste of relative density 1.1~1.2 under room temperature environment.
7. the preparation method of the Chinese medicine composition of acetylcholine esterase inhibition according to claim 6, it is characterised in that institute
State in step (2), add 2~10 times of water of volume to carry out 1~12h of immersion treatment.
8. the preparation method of the Chinese medicine composition of acetylcholine esterase inhibition according to claim 6, it is characterised in that institute
State in step (3), material be added in 5 times of sodium hydroxide solutions of 1% mass concentration of volume, stir and boil,
Degreasing is carried out to material and removes Lasaxing Oilfield 30min.
9. the preparation method of the Chinese medicine composition of acetylcholine esterase inhibition according to claim 6, it is characterised in that institute
Stating step (5) decoction process is：10min is heated at 130 DEG C；Then temperature is reduced to 65 DEG C, continues to heat 60min；Rise again
High-temperature continues to heat 10min to 130 DEG C.
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| WO2024033946A1 (en) * | 2022-08-10 | 2024-02-15 | Dr Dozo Laboratories | Compositions and use in methods for treating a cognitive deficit |
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