CN117503779A - Preparation method and application of protopanoxadiol-based medicament - Google Patents
Preparation method and application of protopanoxadiol-based medicament Download PDFInfo
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- 239000003814 drug Substances 0.000 title claims abstract description 22
- 238000002360 preparation method Methods 0.000 title abstract description 13
- 208000018737 Parkinson disease Diseases 0.000 claims abstract description 18
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims abstract description 16
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims abstract description 12
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims abstract description 8
- 238000000034 method Methods 0.000 claims abstract description 7
- 208000008039 Secondary Parkinson Disease Diseases 0.000 claims abstract description 5
- 238000000605 extraction Methods 0.000 claims abstract description 5
- 229940089161 ginsenoside Drugs 0.000 claims abstract description 5
- 229930182494 ginsenoside Natural products 0.000 claims abstract description 5
- 238000004440 column chromatography Methods 0.000 claims abstract description 4
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- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 4
- 239000000825 pharmaceutical preparation Substances 0.000 claims description 5
- 239000004480 active ingredient Substances 0.000 claims description 4
- 239000000203 mixture Substances 0.000 claims description 4
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims description 3
- 102000003802 alpha-Synuclein Human genes 0.000 claims description 3
- 108090000185 alpha-Synuclein Proteins 0.000 claims description 3
- 239000011575 calcium Substances 0.000 claims description 3
- 229910052791 calcium Inorganic materials 0.000 claims description 3
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- 230000003412 degenerative effect Effects 0.000 claims description 2
- 238000009472 formulation Methods 0.000 claims 3
- 230000002708 enhancing effect Effects 0.000 claims 1
- 238000011321 prophylaxis Methods 0.000 claims 1
- 230000035899 viability Effects 0.000 claims 1
- 206010034010 Parkinsonism Diseases 0.000 abstract description 13
- 208000027089 Parkinsonian disease Diseases 0.000 abstract description 10
- 238000002474 experimental method Methods 0.000 abstract description 8
- PYXFVCFISTUSOO-HKUCOEKDSA-N (20S)-protopanaxadiol Chemical compound C1C[C@H](O)C(C)(C)[C@@H]2CC[C@@]3(C)[C@]4(C)CC[C@H]([C@@](C)(O)CCC=C(C)C)[C@H]4[C@H](O)C[C@@H]3[C@]21C PYXFVCFISTUSOO-HKUCOEKDSA-N 0.000 abstract description 5
- 230000000694 effects Effects 0.000 abstract description 5
- PYXFVCFISTUSOO-UHFFFAOYSA-N betulafolienetriol Natural products C1CC(O)C(C)(C)C2CCC3(C)C4(C)CCC(C(C)(O)CCC=C(C)C)C4C(O)CC3C21C PYXFVCFISTUSOO-UHFFFAOYSA-N 0.000 abstract description 4
- SWQINCWATANGKN-UHFFFAOYSA-N protopanaxadiol Natural products CC(CCC=C(C)C)C1CCC2(C)C1C(O)CC1C3(C)CCC(O)C(C)(C)C3CCC21C SWQINCWATANGKN-UHFFFAOYSA-N 0.000 abstract description 4
- 238000012795 verification Methods 0.000 abstract description 4
- 230000002265 prevention Effects 0.000 abstract description 2
- 241000699670 Mus sp. Species 0.000 description 13
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- 241001539473 Euphoria Species 0.000 description 6
- 206010015535 Euphoric mood Diseases 0.000 description 6
- 238000000465 moulding Methods 0.000 description 6
- PLRACCBDVIHHLZ-UHFFFAOYSA-N 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine Chemical compound C1N(C)CCC(C=2C=CC=CC=2)=C1 PLRACCBDVIHHLZ-UHFFFAOYSA-N 0.000 description 5
- WTDRDQBEARUVNC-LURJTMIESA-N L-DOPA Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-LURJTMIESA-N 0.000 description 5
- 241000699666 Mus <mouse, genus> Species 0.000 description 5
- 101001135571 Mus musculus Tyrosine-protein phosphatase non-receptor type 2 Proteins 0.000 description 5
- WTDRDQBEARUVNC-UHFFFAOYSA-N L-Dopa Natural products OC(=O)C(N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-UHFFFAOYSA-N 0.000 description 4
- 239000003795 chemical substances by application Substances 0.000 description 4
- 229960004502 levodopa Drugs 0.000 description 4
- 206010061296 Motor dysfunction Diseases 0.000 description 3
- 238000001514 detection method Methods 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- 238000012346 open field test Methods 0.000 description 3
- 239000011734 sodium Substances 0.000 description 3
- 208000024891 symptom Diseases 0.000 description 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- 102000010909 Monoamine Oxidase Human genes 0.000 description 2
- 108010062431 Monoamine oxidase Proteins 0.000 description 2
- PVLHOJXLNBFHDX-XHJPDDKBSA-N Panaxadiol Chemical compound C[C@]1([C@H]2CC[C@@]3([C@@H]2[C@H](O)C[C@H]2[C@]3(CC[C@H]3C(C)(C)[C@@H](O)CC[C@@]32C)C)C)CCCC(C)(C)O1 PVLHOJXLNBFHDX-XHJPDDKBSA-N 0.000 description 2
- SYFJYASKXNAXKC-UHFFFAOYSA-N Panaxadiol Natural products CC1(C)CCCC(O1)C2CCC3(C)C2C(O)CC4C5(C)CCC(O)C(C)(C)C5CCC34C SYFJYASKXNAXKC-UHFFFAOYSA-N 0.000 description 2
- 241001529742 Rosmarinus Species 0.000 description 2
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- 238000004458 analytical method Methods 0.000 description 2
- 230000009194 climbing Effects 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- VYFYYTLLBUKUHU-UHFFFAOYSA-N dopamine Chemical compound NCCC1=CC=C(O)C(O)=C1 VYFYYTLLBUKUHU-UHFFFAOYSA-N 0.000 description 2
- 239000003112 inhibitor Substances 0.000 description 2
- 239000007928 intraperitoneal injection Substances 0.000 description 2
- -1 iron ions Chemical class 0.000 description 2
- 239000000463 material Substances 0.000 description 2
- 239000008354 sodium chloride injection Substances 0.000 description 2
- 238000002560 therapeutic procedure Methods 0.000 description 2
- 230000000007 visual effect Effects 0.000 description 2
- 206010006100 Bradykinesia Diseases 0.000 description 1
- 238000011740 C57BL/6 mouse Methods 0.000 description 1
- 206010010774 Constipation Diseases 0.000 description 1
- 229940098778 Dopamine receptor agonist Drugs 0.000 description 1
- 208000012661 Dyskinesia Diseases 0.000 description 1
- 208000006083 Hypokinesia Diseases 0.000 description 1
- 229920000426 Microplastic Polymers 0.000 description 1
- 206010061533 Myotonia Diseases 0.000 description 1
- 206010071390 Resting tremor Diseases 0.000 description 1
- 102000004357 Transferases Human genes 0.000 description 1
- 108090000992 Transferases Proteins 0.000 description 1
- 206010044565 Tremor Diseases 0.000 description 1
- 230000004075 alteration Effects 0.000 description 1
- DKNWSYNQZKUICI-UHFFFAOYSA-N amantadine Chemical compound C1C(C2)CC3CC2CC1(N)C3 DKNWSYNQZKUICI-UHFFFAOYSA-N 0.000 description 1
- 229960003805 amantadine Drugs 0.000 description 1
- 238000010171 animal model Methods 0.000 description 1
- 230000001078 anti-cholinergic effect Effects 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- 210000000467 autonomic pathway Anatomy 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- 208000010877 cognitive disease Diseases 0.000 description 1
- 230000001149 cognitive effect Effects 0.000 description 1
- 230000006378 damage Effects 0.000 description 1
- OORMXZNMRWBSTK-LGFJJATJSA-N dammarane Chemical compound C1CCC(C)(C)[C@@H]2CC[C@@]3(C)[C@]4(C)CC[C@H]([C@H](C)CCCC(C)C)[C@H]4CC[C@@H]3[C@]21C OORMXZNMRWBSTK-LGFJJATJSA-N 0.000 description 1
- 230000007850 degeneration Effects 0.000 description 1
- 238000010586 diagram Methods 0.000 description 1
- 238000007598 dipping method Methods 0.000 description 1
- 229960003638 dopamine Drugs 0.000 description 1
- 239000003136 dopamine receptor stimulating agent Substances 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 238000002651 drug therapy Methods 0.000 description 1
- 230000004064 dysfunction Effects 0.000 description 1
- 239000006260 foam Substances 0.000 description 1
- 238000005286 illumination Methods 0.000 description 1
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- 230000003340 mental effect Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
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- 208000020016 psychiatric disease Diseases 0.000 description 1
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- 239000000243 solution Substances 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
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Classifications
-
- 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Neurosurgery (AREA)
- Psychology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention provides a preparation method and application of a protopanoxadiol-based medicament, comprising the following steps of: taking 1100mg of ginsenoside Rb, adding 1M hydrochloric acid, and hydrolyzing in water bath at 70deg.C for 6 hr to obtain mixed liquid; adjusting the pH value of the mixed solution to 7 by using 1M sodium hydroxide, and adding three times of volume of ethyl acetate for extraction for three times; concentrating the combined ethyl acetate part under reduced pressure, performing gel column chromatography, detecting by TLC, and collecting target component to obtain protopanoxadiol; the invention is based on unexpected findings and combined with experimental verification, and further provides a method for preventing and treating primary parkinsonism, secondary parkinsonism and denatured parkinsonism by using protopanaxadiol, which provides a verification experiment to prove that the preparation has remarkable treatment effect and further provides a new idea for clinical prevention and treatment of parkinsonism.
Description
Technical Field
The invention relates to the technical field of medicine preparation, in particular to a preparation method and application of a protopanoxadiol-based medicament.
Background
Parkinson's disease, also known as "paralysis agitans", is a common senile nervous system degenerative disease, and the pathogenic cause is degeneration and lesions of dopamine neurons; has characteristic movement symptoms including resting tremor, bradykinesia, myotonia, and disturbance of posture balance, and also has non-movement symptoms including constipation, dysolfaction, sleep disorder, autonomic nerve dysfunction, and mental and cognitive disorders;
methods for clinically treating parkinson's disease include drug therapy, surgical therapy, and traditional Chinese medicine therapy; although the methods have all made remarkable progress in the treatment of parkinsonism, the treatment of parkinsonism at home and abroad is still mainly carried out by medicaments at present; the clinic medicines for treating Parkinson's disease include dopamine receptor agonist, monoamine oxidase B (MAO-B) inhibitor, anticholinergic medicine, compound levodopa preparation, catechol-oxygen-methyl transferase (COMT) inhibitor, amantadine and neuroprotectant;
although surgical treatment has proven effective in treating motor symptoms of parkinson's disease, it can cause varying degrees of injury to the cognitive areas, brain language, mood, etc. of the patient.
The invention is based in part on the surprising discovery that the extraction of active ingredients of protopanoxadiol in combination with a pharmaceutical carrier is effective in treating parkinson's disease, and the protopanoxadiol structurally belongs to dammarane type tetracyclic tri-post ginsenoside compounds, and no related research report has been made on the use of 20-s protopanoxadiol in preventing parkinson's disease.
Disclosure of Invention
The invention aims to provide a preparation method and application thereof based on protopanoxadiol, and a preparation method and application thereof, so as to solve the problems in the prior art.
In order to achieve the above purpose, the present invention provides the following technical solutions:
a method for preparing a protopanoxadiol-based medicament, comprising the steps of:
s1, taking 1100mg of ginsenoside Rb, adding 1M hydrochloric acid, and hydrolyzing in a water bath at 70 ℃ for 6 hours to obtain a mixed liquid;
s2, adjusting the pH value of the mixed solution to 7 by using 1M sodium hydroxide, and adding three times of volume of ethyl acetate for extraction for three times;
s3, concentrating the ethyl acetate part under reduced pressure, then performing gel column chromatography, detecting by TLC, and collecting target components to obtain protopanoxadiol;
s4, mixing the carrier medicine with protopanoxadiol as an active ingredient to prepare a pharmaceutical preparation.
The application of the protopanoxadiol-based medicament is characterized in that the pharmaceutical preparation is one of oral preparation, injection, sustained release agent, controlled release agent, granule and syrup.
Preferably, the pharmaceutical formulation of protopanoxadiol can prevent parkinson's disease including one or more of primary parkinson's disease, secondary parkinson's disease, and degenerative parkinson's disease.
Preferably, the protopanaxadiol can enhance the activity of dopaminergic neurons by stabilizing the concentration of calcium and iron ions, and reduce the secretion of alpha-synuclein so as to play a role in preventing and treating parkinsonism.
Compared with the prior art, the invention has the following beneficial effects:
despite the wide variety of drugs clinically used to treat parkinson's disease, there is still no drug that can radically treat parkinson's disease and the condition gradually aggravates as the patient's time of onset increases; based on unexpected discovery and combined with experimental verification, the invention further provides a method for preventing and treating primary parkinsonism, secondary parkinsonism and denatured parkinsonism by using protopanoxadiol, and provides a verification experiment to prove that the composition has remarkable treatment effect; and further provides a new idea for clinical prevention and treatment of the parkinsonism.
Drawings
FIG. 1 is a graph showing the analysis of motor dysfunction in a model mouse with improved parkinsonism by using panaxadiol in an open field experiment;
FIG. 2 is a graph showing the analysis of motor dysfunction of a model mouse in which the model mouse is modified by the panaxadiol in a pole climbing experiment;
FIG. 3 is a structural diagram of protopanoxadiol.
Detailed Description
The following description of the embodiments of the present invention will be made clearly and completely with reference to the accompanying drawings, in which it is apparent that the embodiments described are only some embodiments of the present invention, but not all embodiments. All other embodiments, which can be made by those skilled in the art based on the embodiments of the invention without making any inventive effort, are intended to be within the scope of the invention.
Embodiment one:
the embodiment provides a preparation method of a protopanoxadiol-based medicament, which comprises the following steps of:
s1, taking 1100mg of ginsenoside Rb, adding 1M hydrochloric acid, and hydrolyzing in a water bath at 70 ℃ for 6 hours to obtain a mixed liquid;
s2, adjusting the pH value of the mixed solution to 7 by using 1M sodium hydroxide, and adding three times of volume of ethyl acetate for extraction for three times;
s3, concentrating the ethyl acetate part under reduced pressure, then performing gel column chromatography, detecting by TLC, and collecting target components to obtain protopanoxadiol;
s4, mixing the carrier medicine with protopanoxadiol as an active ingredient to prepare a pharmaceutical preparation.
According to the preparation method, based on the application of the protopanoxadiol medicament, the pharmaceutical preparation is one of oral preparation, injection, sustained release agent, controlled release agent, granule and syrup, and can prevent one or more of primary parkinsonism, secondary parkinsonism and denatured parkinsonism, and the protopanoxadiol can strengthen the activity of dopaminergic neurons by stabilizing the concentration of calcium and iron ions and reduce the secretion of alpha-synuclein so as to play a role in preventing and treating parkinsonism.
The molecular formula of the protopanoxadiol is as follows: c (C) 30 H 52 O 3 The structural formula is shown in figure 1.
Experimental reference: protection of MPTP-induced motor dysfunction in mice by 20-s protopanoxadiol;
1. instrument and materials
The instrument is selected from:
animal behavioural mine (euphoria, shanghai), animal mine behavioural image acquisition card (euphoria, shanghai), visual track animal mine behavioural analysis software (euphoria, shanghai), animal behavioural pole-climbing experimental device (euphoria, shanghai), animal pole-climbing behavioural image acquisition card (euphoria, shanghai), visual track animal pole-climbing behavioural analysis software (euphoria, shanghai).
Materials:
protopanaxadiol (purity 95%, homemade), levodopa (Changxing pharmaceutical Co., ltd., CAS: 59-92-7), C57 mice (purchased from Kunming medical university, pass number: SCXK (Yunnan) -2011004).
2. Method of
2.1 molding: c57BL/6 male mice MPTP (30 mg/kg) was given intraperitoneally 1 time/day for 5 days; the control group was given the same dose of 0.9% sodium chloride injection.
2.2 grouping: c57BL/6 male mice are randomly divided into a control group, a model group, a protopanaxadiol group and a positive group, and 10 mice are selected from each group. The administration dose of the protopanoxadiol group is 10mg/kg, and rosemary is administrated by intragastric administration (the first 5 days) while MPTP is administrated during molding, and only rosemary is administrated by intragastric administration for 14 days after molding is finished; the dosage of the positive group is 10mg/kg, levodopa is given by intraperitoneal injection (the first 7 days) simultaneously with MPTP during molding, and only levodopa is given for 14 days after molding is finished; the model group was given 1% cmc-Na by intragastric administration while MPTP was administered, and only 1% cmc-Na was administered for 14 days at the end of molding; the control group was given 1% CMC-Na by intraperitoneal injection with 0.9% sodium chloride injection and fed normally.
2.3 behavioural detection
2.3.1 open field test (open-field test)
The open field experimental box is 50cm x 40cm long x wide x high, and is provided with a video detection system directly above and connected with a computer analysis software system. The interior of the entire field case was white, in contrast to black C57BL/6 mice. The mine field test box is placed in a place with dark animal illumination and quiet environment, so that the influence of the environment on mice is reduced. The experimental animals are transported to a behavioural laboratory in advance, and are adapted to the environment for about 3 hours, so that the tension of mice is reduced. When the experiment starts, the mice are gently placed at the center of the square box, so that the mice can freely move in the open field test box, and the independent movement of the mice is observed through the video detection system and the computer. The system synchronously and automatically records the activity condition of the mice within 5 minutes. At the end of each mouse experiment, the bottom of the box is wiped by dipping low-concentration alcohol with a towel, and the volatilization of the low-concentration alcohol is dissipated, so that the experiment results of other mice are not affected by smell.
2.3.2 rod climbing experiments (pole-clampingtest)
A foam plastic pellet with the diameter of 2.5cm is fixed on the top end of a wooden rod with the length of 60cm and the diameter of 1cm, and 2 layers of gauze are wound on the wooden rod to prevent slipping. The mouse head was placed up on top of the ball and the following 3 times were recorded: the time required for the mice to climb the full length of the pole.
3. Results and assays of the improvement of model mice dyskinesia by protopanaxadiol are shown in figures 1 and 2.
Although embodiments of the present invention have been shown and described, it will be understood by those skilled in the art that various changes, modifications, substitutions and alterations can be made therein without departing from the principles and spirit of the invention, the scope of which is defined in the appended claims and their equivalents.
Claims (4)
1. A method for preparing a protopanoxadiol-based medicament, comprising the steps of:
s1, taking 1100mg of ginsenoside Rb, adding 1M hydrochloric acid, and hydrolyzing in a water bath at 70 ℃ for 6 hours to obtain a mixed liquid;
s2, adjusting the pH value of the mixed solution to 7 by using 1M sodium hydroxide, and adding three times of volume of ethyl acetate for extraction for three times;
s3, concentrating the ethyl acetate part under reduced pressure, then performing gel column chromatography, detecting by TLC, and collecting target components to obtain protopanoxadiol;
s4, mixing the carrier medicine with protopanoxadiol as an active ingredient to prepare a pharmaceutical preparation.
2. The use of a protopanoxadiol-based medicament according to claim 1, wherein the pharmaceutical formulation is one of an oral formulation, an injection, a sustained release formulation, a controlled release formulation, a granule, a syrup.
3. The use of a protopanoxadiol-based medicament according to claim 2, wherein the protopanoxadiol-based pharmaceutical formulation is capable of preventing parkinson's disease comprising one or more of primary parkinson's disease, secondary parkinson's disease, degenerative parkinson's disease.
4. The use of a protopanoxadiol-based medicament according to claim 2, wherein said protopanoxadiol is capable of acting as a prophylactic treatment for parkinson by stabilizing the calcium and iron ion concentrations, enhancing the viability of dopaminergic neurons, and reducing α -synuclein secretion.
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| Application Number | Priority Date | Filing Date | Title |
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| CN202311480193.0A CN117503779A (en) | 2023-11-08 | 2023-11-08 | Preparation method and application of protopanoxadiol-based medicament |
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| Application Number | Priority Date | Filing Date | Title |
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| CN202311480193.0A CN117503779A (en) | 2023-11-08 | 2023-11-08 | Preparation method and application of protopanoxadiol-based medicament |
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| CN202311480193.0A Pending CN117503779A (en) | 2023-11-08 | 2023-11-08 | Preparation method and application of protopanoxadiol-based medicament |
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