CN110279738A - A kind of extracting method of antidepressant spermidine active component and the purposes of spermidine effective part extract - Google Patents
A kind of extracting method of antidepressant spermidine active component and the purposes of spermidine effective part extract Download PDFInfo
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- CN110279738A CN110279738A CN201910596030.6A CN201910596030A CN110279738A CN 110279738 A CN110279738 A CN 110279738A CN 201910596030 A CN201910596030 A CN 201910596030A CN 110279738 A CN110279738 A CN 110279738A
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- spermidine
- active component
- antidepressant
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- ATHGHQPFGPMSJY-UHFFFAOYSA-N spermidine Chemical compound NCCCCNCCCN ATHGHQPFGPMSJY-UHFFFAOYSA-N 0.000 title claims abstract description 154
- 229940063673 spermidine Drugs 0.000 title claims abstract description 76
- 239000000284 extract Substances 0.000 title claims abstract description 30
- 230000001430 anti-depressive effect Effects 0.000 title claims abstract description 25
- 239000000935 antidepressant agent Substances 0.000 title claims abstract description 15
- 238000000034 method Methods 0.000 title claims abstract description 14
- 229940005513 antidepressants Drugs 0.000 title claims abstract description 12
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims abstract description 28
- 235000003255 Carthamus tinctorius Nutrition 0.000 claims abstract description 16
- 244000020518 Carthamus tinctorius Species 0.000 claims abstract description 16
- 235000019441 ethanol Nutrition 0.000 claims abstract description 16
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 10
- 238000010992 reflux Methods 0.000 claims abstract description 8
- 239000012141 concentrate Substances 0.000 claims abstract description 7
- 238000010828 elution Methods 0.000 claims abstract description 7
- 235000013402 health food Nutrition 0.000 claims abstract description 6
- 239000002552 dosage form Substances 0.000 claims abstract description 5
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 4
- 239000002775 capsule Substances 0.000 claims abstract description 3
- 239000003349 gelling agent Substances 0.000 claims abstract description 3
- 239000008187 granular material Substances 0.000 claims abstract description 3
- 229940100688 oral solution Drugs 0.000 claims abstract description 3
- 239000006187 pill Substances 0.000 claims abstract description 3
- 238000013268 sustained release Methods 0.000 claims abstract description 3
- 239000012730 sustained-release form Substances 0.000 claims abstract description 3
- 239000003826 tablet Substances 0.000 claims abstract description 3
- 239000003814 drug Substances 0.000 claims description 16
- 239000000126 substance Substances 0.000 claims description 9
- 239000000463 material Substances 0.000 claims description 4
- PQMOXTJVIYEOQL-UHFFFAOYSA-N Cumarin Natural products CC(C)=CCC1=C(O)C(C(=O)C(C)CC)=C(O)C2=C1OC(=O)C=C2CCC PQMOXTJVIYEOQL-UHFFFAOYSA-N 0.000 claims description 2
- FSOGIJPGPZWNGO-UHFFFAOYSA-N Meomammein Natural products CCC(C)C(=O)C1=C(O)C(CC=C(C)C)=C(O)C2=C1OC(=O)C=C2CCC FSOGIJPGPZWNGO-UHFFFAOYSA-N 0.000 claims description 2
- 239000000843 powder Substances 0.000 claims description 2
- 238000000926 separation method Methods 0.000 claims description 2
- 238000002360 preparation method Methods 0.000 abstract description 14
- 238000012360 testing method Methods 0.000 abstract description 11
- 230000000694 effects Effects 0.000 abstract description 9
- 230000009182 swimming Effects 0.000 abstract description 7
- 238000001035 drying Methods 0.000 abstract description 6
- 238000012048 forced swim test Methods 0.000 abstract description 4
- 239000004615 ingredient Substances 0.000 abstract description 2
- 238000004519 manufacturing process Methods 0.000 abstract description 2
- 239000011149 active material Substances 0.000 abstract 1
- 238000002474 experimental method Methods 0.000 description 15
- 229940079593 drug Drugs 0.000 description 12
- PNVNVHUZROJLTJ-UHFFFAOYSA-N venlafaxine Chemical compound C1=CC(OC)=CC=C1C(CN(C)C)C1(O)CCCCC1 PNVNVHUZROJLTJ-UHFFFAOYSA-N 0.000 description 11
- 241001465754 Metazoa Species 0.000 description 9
- 238000010171 animal model Methods 0.000 description 9
- 229960004688 venlafaxine Drugs 0.000 description 8
- 230000008859 change Effects 0.000 description 6
- 230000037396 body weight Effects 0.000 description 5
- 235000008504 concentrate Nutrition 0.000 description 5
- 230000002496 gastric effect Effects 0.000 description 5
- 239000006188 syrup Substances 0.000 description 5
- 235000020357 syrup Nutrition 0.000 description 5
- 239000003153 chemical reaction reagent Substances 0.000 description 4
- 206010067484 Adverse reaction Diseases 0.000 description 3
- 208000020401 Depressive disease Diseases 0.000 description 3
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 3
- 230000006838 adverse reaction Effects 0.000 description 3
- 238000004458 analytical method Methods 0.000 description 3
- 239000001768 carboxy methyl cellulose Substances 0.000 description 3
- 238000011161 development Methods 0.000 description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
- 239000012153 distilled water Substances 0.000 description 3
- 239000011521 glass Substances 0.000 description 3
- 230000010412 perfusion Effects 0.000 description 3
- 230000000144 pharmacologic effect Effects 0.000 description 3
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 3
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 3
- 230000000638 stimulation Effects 0.000 description 3
- 229930006000 Sucrose Natural products 0.000 description 2
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 2
- 230000009471 action Effects 0.000 description 2
- 125000002252 acyl group Chemical group 0.000 description 2
- 230000003542 behavioural effect Effects 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 244000144993 groups of animals Species 0.000 description 2
- 229960004801 imipramine Drugs 0.000 description 2
- BCGWQEUPMDMJNV-UHFFFAOYSA-N imipramine Chemical compound C1CC2=CC=CC=C2N(CCCN(C)C)C2=CC=CC=C21 BCGWQEUPMDMJNV-UHFFFAOYSA-N 0.000 description 2
- 238000001802 infusion Methods 0.000 description 2
- 230000002265 prevention Effects 0.000 description 2
- 238000001671 psychotherapy Methods 0.000 description 2
- 229960004793 sucrose Drugs 0.000 description 2
- 239000000725 suspension Substances 0.000 description 2
- AHOUBRCZNHFOSL-YOEHRIQHSA-N (+)-Casbol Chemical compound C1=CC(F)=CC=C1[C@H]1[C@H](COC=2C=C3OCOC3=CC=2)CNCC1 AHOUBRCZNHFOSL-YOEHRIQHSA-N 0.000 description 1
- XKFPYPQQHFEXRZ-UHFFFAOYSA-N 5-methyl-N'-(phenylmethyl)-3-isoxazolecarbohydrazide Chemical compound O1C(C)=CC(C(=O)NNCC=2C=CC=CC=2)=N1 XKFPYPQQHFEXRZ-UHFFFAOYSA-N 0.000 description 1
- 208000017194 Affective disease Diseases 0.000 description 1
- 208000007415 Anhedonia Diseases 0.000 description 1
- GDLIGKIOYRNHDA-UHFFFAOYSA-N Clomipramine Chemical compound C1CC2=CC=C(Cl)C=C2N(CCCN(C)C)C2=CC=CC=C21 GDLIGKIOYRNHDA-UHFFFAOYSA-N 0.000 description 1
- HTJDQJBWANPRPF-UHFFFAOYSA-N Cyclopropylamine Chemical compound NC1CC1 HTJDQJBWANPRPF-UHFFFAOYSA-N 0.000 description 1
- 206010013954 Dysphoria Diseases 0.000 description 1
- YCKRFDGAMUMZLT-UHFFFAOYSA-N Fluorine atom Chemical compound [F] YCKRFDGAMUMZLT-UHFFFAOYSA-N 0.000 description 1
- 241000713772 Human immunodeficiency virus 1 Species 0.000 description 1
- 229940123685 Monoamine oxidase inhibitor Drugs 0.000 description 1
- 241000233855 Orchidaceae Species 0.000 description 1
- RMUCZJUITONUFY-UHFFFAOYSA-N Phenelzine Chemical compound NNCCC1=CC=CC=C1 RMUCZJUITONUFY-UHFFFAOYSA-N 0.000 description 1
- 208000028017 Psychotic disease Diseases 0.000 description 1
- 240000000111 Saccharum officinarum Species 0.000 description 1
- 235000007201 Saccharum officinarum Nutrition 0.000 description 1
- 208000010340 Sleep Deprivation Diseases 0.000 description 1
- 230000001133 acceleration Effects 0.000 description 1
- 239000002390 adhesive tape Substances 0.000 description 1
- 150000001335 aliphatic alkanes Chemical class 0.000 description 1
- 229930013930 alkaloid Natural products 0.000 description 1
- 229960000836 amitriptyline Drugs 0.000 description 1
- KRMDCWKBEZIMAB-UHFFFAOYSA-N amitriptyline Chemical compound C1CC2=CC=CC=C2C(=CCCN(C)C)C2=CC=CC=C21 KRMDCWKBEZIMAB-UHFFFAOYSA-N 0.000 description 1
- 230000000259 anti-tumor effect Effects 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
- 230000003078 antioxidant effect Effects 0.000 description 1
- 235000006708 antioxidants Nutrition 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 229960004606 clomipramine Drugs 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 230000002920 convulsive effect Effects 0.000 description 1
- 230000000994 depressogenic effect Effects 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 231100000673 dose–response relationship Toxicity 0.000 description 1
- 229960005426 doxepin Drugs 0.000 description 1
- ODQWQRRAPPTVAG-GZTJUZNOSA-N doxepin Chemical compound C1OC2=CC=CC=C2C(=C/CCN(C)C)/C2=CC=CC=C21 ODQWQRRAPPTVAG-GZTJUZNOSA-N 0.000 description 1
- 238000002651 drug therapy Methods 0.000 description 1
- 230000008451 emotion Effects 0.000 description 1
- 229930003935 flavonoid Natural products 0.000 description 1
- 150000002215 flavonoids Chemical class 0.000 description 1
- 235000017173 flavonoids Nutrition 0.000 description 1
- 229910052731 fluorine Inorganic materials 0.000 description 1
- 239000011737 fluorine Substances 0.000 description 1
- 150000002334 glycols Chemical class 0.000 description 1
- 230000036541 health Effects 0.000 description 1
- 238000004128 high performance liquid chromatography Methods 0.000 description 1
- 239000005457 ice water Substances 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- HZVOZRGWRWCICA-UHFFFAOYSA-N methanediyl Chemical class [CH2] HZVOZRGWRWCICA-UHFFFAOYSA-N 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- YHXISWVBGDMDLQ-UHFFFAOYSA-N moclobemide Chemical compound C1=CC(Cl)=CC=C1C(=O)NCCN1CCOCC1 YHXISWVBGDMDLQ-UHFFFAOYSA-N 0.000 description 1
- 229960004644 moclobemide Drugs 0.000 description 1
- 239000002899 monoamine oxidase inhibitor Substances 0.000 description 1
- 229940087524 nardil Drugs 0.000 description 1
- 229930014626 natural product Natural products 0.000 description 1
- 210000005036 nerve Anatomy 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 229960002296 paroxetine Drugs 0.000 description 1
- 230000002085 persistent effect Effects 0.000 description 1
- 238000001126 phototherapy Methods 0.000 description 1
- 229920000768 polyamine Polymers 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 108090000765 processed proteins & peptides Proteins 0.000 description 1
- 238000004064 recycling Methods 0.000 description 1
- 230000033764 rhythmic process Effects 0.000 description 1
- 229960002073 sertraline Drugs 0.000 description 1
- VGKDLMBJGBXTGI-SJCJKPOMSA-N sertraline Chemical compound C1([C@@H]2CC[C@@H](C3=CC=CC=C32)NC)=CC=C(Cl)C(Cl)=C1 VGKDLMBJGBXTGI-SJCJKPOMSA-N 0.000 description 1
- 230000035939 shock Effects 0.000 description 1
- 239000002893 slag Substances 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- -1 spermidine class compound Chemical class 0.000 description 1
- 150000003431 steroids Chemical class 0.000 description 1
- 230000004936 stimulating effect Effects 0.000 description 1
- RWRDLPDLKQPQOW-UHFFFAOYSA-N tetrahydropyrrole Substances C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 238000002604 ultrasonography Methods 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
- A23L33/105—Plant extracts, their artificial duplicates or their derivatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/28—Asteraceae or Compositae (Aster or Sunflower family), e.g. chamomile, feverfew, yarrow or echinacea
- A61K36/286—Carthamus (distaff thistle)
-
- 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
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2236/00—Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
- A61K2236/30—Extraction of the material
- A61K2236/33—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones
- A61K2236/333—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones using mixed solvents, e.g. 70% EtOH
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2236/00—Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
- A61K2236/30—Extraction of the material
- A61K2236/39—Complex extraction schemes, e.g. fractionation or repeated extraction steps
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2236/00—Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
- A61K2236/50—Methods involving additional extraction steps
- A61K2236/55—Liquid-liquid separation; Phase separation
Abstract
The invention belongs to effective ingredient in Chinese extractive technique field, a kind of extracting method of antidepressant spermidine active component and the purposes of spermidine effective part extract are provided.Drying safflower or the safflower dregs of a decoction, 60-90% alcohol reflux extract, and are concentrated under reduced pressure, and concentrate is suppressed to press in standby column progress in C18 and be rapidly purified, and 10-100% ethyl alcohol or water elution are concentrated and dried up to spermidine effective part extract.Spermidine active component can significantly reduce the dead time in Mouse Forced Swim Test and rat force swimming test, and spermidine active component has apparent antidepressant effect.Spermidine active component provided by the invention is a kind of preparation process simplicity, significant effect, natural antidepression active materials safe and reliable, easy to industrialized production, can be prepared into the dosage forms such as capsule, tablet, granule, gelling agent, sustained release agent, oral solution or pill for antidepressant or health food.
Description
Technical field
The invention belongs to effective ingredient in Chinese extractive technique fields, and in particular to a kind of antidepressant spermidine active component
Extracting method and spermidine effective part extract purposes.
Background technique
Depression is a kind of common affective disease, be mainly shown as it is significant and enduringly depressed, slightly
Patients with depression shows as dysphoria, anhedonia, and serious person shows as pessimistic despair, and all day anxiously, one day seems like a year,
It is overwhelmed with sorrow, often there is introgression.Depression has the characteristics that high disease incidence, high recurrence rate and disability rate are high.World health group
It knits and has been classified as one of ten big heavy diseases, with the development of the social economy, the accelerating rhythm of life, the pressure of people increases
Add, various emotion impacts increase, and incidence of depression is caused to increase year by year.The serious harmfulness an urgent demand researcher of depression
Study on Acceleration and the higher antidepressant of the better safety of development efficacy.
The treatment method of depression is more, such as psychotherapy, sleep deprivation treatment, phototherapy and electric convulsive treatment, but still
Based on drug therapy, while treated by psychotherapy.The drug for the treatment of depression is mainly based on chemicals at present, such as tricyclic
Class (clinic common imipramine, amitriptyline, doxepin, trimethyl imipramine, chlorimipramine etc.), monoamine oxidase inhibitors
(clinic common nardil, isocarbossazide, cyclopropylamine, Moclobemide etc.), selectivity 5-HT reuptake inhibitor (the common fluorine west of clinic
Spit of fland, Paxil, Sertraline, western general peptide orchid etc.) etc., but there is treatment and compose narrow, poor resistance, toxic side effect in these chemicals
Greatly, the problems such as expensive.Therefore, discovery and initiative have from persistent, adverse reaction rate low natural products
The drug of good antidepression effect, it has also become the hot spot currently studied both at home and abroad.
Currently, separated from safflower obtain a chemical component more than 250, including flavonoids, alkaloids, carbene class, alkane
Base glycols, organic acid, steroid, spermidine class etc..Wherein, spermidine derivatives have (H2N(CH2)3NH(CH2)4NH2) structural unit polyamine compounds, be a kind of special composition in safflower, that show extensive raw for document report
Object activity, such as it is anti HIV-1 virus, antitumor, anti-oxidant, but the spermidine in safflower is special in nerve and psychosis
It is that effect in terms of depression has no document report, and the preparation of a kind of spermidine also has not been reported in safflower.
Summary of the invention
The purpose of the present invention is to provide a kind of extracting method of antidepressant spermidine active component and spermidine are effective
The purposes of extractive part.
To achieve the above object, the invention provides the following technical scheme: a kind of antidepressant spermidine active component mentions
Take method, the specific steps are as follows: take dry safflower or the safflower dregs of a decoction, 60-90% alcohol reflux extracts 1-2 times, is concentrated under reduced pressure, dense
Contracting liquid is suppressed to press in standby column progress in C18 and be rapidly purified, and W1/W2 1-10, the W1 are sample quality to be separated in terms of mg,
W2 is the quality of C18 post separation material in terms of g;10-100% ethyl alcohol or water elution are concentrated and dried and mention up to spermidine active component
Take object.
The spermidine that the three cumarin acyl groups that spermidine effective part extract obtained contains 4 various configurations replace
Substance, total content are 50% or more.
The application of spermidine effective part extract, the spermidine effective part extract are preparing antidepressant drug
Or the application in health food.
The antidepressant drug is that pharmacy is made in the pharmaceutically acceptable auxiliary material of spermidine effective part extract addition
Acceptable regular dosage form.
The dosage form is capsule, tablet, powder, granule, gelling agent, sustained release agent, oral solution or pill.
The spermidine effective part extract is containing there are four the spermidine classes that three coumaric acyls of various configuration replace
Substance (structure is shown in Fig. 1), total content are detailed in attached drawing 2 up to 50% or more.
The present invention has the advantages that as is evident below:
The present invention has advanced optimized the process as spermidine active component preparation process, simultaneously for further recycling
Chinese medicine slag also has great importance.
Present invention finds the medicinal functions of spermidine active component, are used for antidepressant effect, and can be prepared into pre-
Anti- and/or treatment depression drug, thus for spermidine active component is medicinal or the clinical application developing of healthcare function is new
Field.
Classical antidepression animal model experiment is the result shows that spermidine active component has apparent antidepressant effect.
Spermidine active component pharmacological action of the invention is stronger, function the effect of for preventing, improving and treat depression
Effect is obvious, action is very fast, adverse reaction is smaller, cheap, has a good application prospect.
The present invention can be used alone spermidine active component preparation prevent and treat depression drug or health food.
Detailed description of the invention
Fig. 1 is the chemical structural formula of 4 spermidines;
Fig. 2 is spermidine class compound HPLC map (nm of λ=300) in the safflower dregs of a decoction.
Specific embodiment
In conjunction with specific embodiments, the present invention is further explained.But these embodiments be only limitted to illustrate the present invention rather than
It limits the scope of the invention.
The experimental method of specific experiment condition is not specified in embodiment, operates usually according to normal condition, or according to production
The conditional operation of manufacturer's recommended.
A kind of embodiment 1: preparation method of the spermidine active component with antidepressant effect, comprising the following steps: take
The drying safflower dregs of a decoction, 60% alcohol reflux extract 1 time, are concentrated under reduced pressure, and concentrate is suppressed pressure in standby column progress in C18 quickly pure
Change preparation, W1/W2 1(mg/g), 60% ethanol elution is concentrated and dried up to spermidine active component, and yield is reachable
95.79%。
By analysis: spermidine effective part extract is containing there are four the spermidines that three coumaric acyls of various configuration replace
Substance, specific structure are shown in that Fig. 1, total content are detailed in attached drawing 2 up to 50% or more.
A kind of embodiment 2: preparation method of the spermidine active component with antidepressant effect, comprising the following steps: take
The drying safflower dregs of a decoction, 75% alcohol reflux extract 1 time, are concentrated under reduced pressure, and concentrate is suppressed pressure in standby column progress in C18 quickly pure
Change preparation, W1/W2 5(mg/g), 50% ethanol elution is concentrated and dried up to spermidine active component, and yield is reachable
97.22%。
A kind of embodiment 3: preparation method of the spermidine active component with antidepressant effect, comprising the following steps: take
The drying safflower dregs of a decoction, 90% alcohol reflux extract 1 time, are concentrated under reduced pressure, and concentrate is suppressed pressure in standby column progress in C18 quickly pure
Change preparation, W1/W2 10(mg/g), 40% ethanol elution is concentrated and dried up to spermidine active component, and yield is reachable
92.79%。
A kind of embodiment 4: preparation method of the spermidine active component with antidepressant effect, comprising the following steps: take
The drying safflower dregs of a decoction, 75% alcohol reflux extract 2 times, are concentrated under reduced pressure, and concentrate is suppressed pressure in standby column progress in C18 quickly pure
Change preparation, W1/W2 5(mg/g), make eluting solvent with 50% ethyl alcohol, be concentrated and dried up to spermidine active component, yield can
Up to 93.52%.
A kind of embodiment 5: preparation method of the spermidine active component with antidepressant effect, comprising the following steps: take
Drying safflower, 75% alcohol reflux extract 1 time, are concentrated under reduced pressure, and concentrate is suppressed pressure in standby column progress and rapidly purifies system in C18
It is standby, W1/W2 5(mg/g), 50% ethanol elution is concentrated and dried up to spermidine active component, and yield is up to 90.32%.
Embodiment 6: Mouse Forced Swim Test
Laboratory apparatus and reagent: animal behavior video analytic system (Chengdu TME Technology Co., Ltd.), thermometer, timer,
Organic glass cylinder, animal gastric perfusion needle.Total spermidine effective part extract, (CMC-Na, Tianjin are triumphant logical for sodium carboxymethylcellulose
Chemical reagent Co., Ltd), VENLAFAXINE HCL (Chengdu Kanghong Medicine Group Co.ltd).
Experimental animal and administration: male ICR mouse (Beijing Vital River Experimental Animals Technology Co., Ltd., credit number:
The capital SCXK() 2016-0006), 18-22g after adaptable fed 1 week, is randomly divided into 5 groups, every group 12.Venlafaxine administration
Dosage is 0.05g/kg, and total spermidine effective part extract dosage is 0.1g/kg, 0.05g/kg, 0.025g/kg, blank pair
Isometric distilled water is given according to group.Groups of animals is according to weight daily stomach-filling 1 time, each 1ml/20g, continuous 14 days.
Experimental method: after last dose 1h, mouse is placed in high 25cm, the organic glass cylinder of diameter 10cm, depth of water 15cm
In, water temperature is 23 ± 2 DEG C.The swimming behavior situation that mouse in 6min is recorded with animal behavior video analytic system, after analysis
The dead time of mouse forced swimming test (refers to that mouse stops struggle or show floating state, only small limb in water in 4min
Body is moved to keep head to keep afloat).
Experimental result: distinguishing weighed each group mouse weight before experiment and after experiment, observes spermidine to mouse weight
Influence, as a result between table 1, experimental data by Mean ± SD indicate.As shown in Table 1, each group mouse weight before experiment and after experiment
Change no significant difference, illustrates that drug itself has no effect on the weight of animals, without obvious adverse reaction.
Influence (g) of 1 spermidine of table to experiment front and back mouse weight
Influence of the spermidine to the dead time in Mouse Forced Swim Test is shown in Table 2, and data are indicated by Mean ± SD.By table 2
It is found that each administration group dead time is reduced, and compared with blank control group after gastric infusion 14 days, except spermidine is high
All have outside dosage group significant difference (P < 0.05OrP < 0.01).
Influence (n=12) of 2 spermidine of table to the dead time in mouse forced swimming test
Compared with blank control group: *P < 0.05There are significant difference, * *P < 0.01There is extremely significant sex differernce.7 mouse of embodiment
Qutstanding tail test
Laboratory apparatus and reagent: animal behavior video analytic system (Chengdu TME Technology Co., Ltd.), thermometer, timer,
Organic glass cylinder, animal gastric perfusion needle.Total spermidine effective part extract, (CMC-Na, Tianjin are triumphant logical for sodium carboxymethylcellulose
Chemical reagent Co., Ltd), VENLAFAXINE HCL (Chengdu Kanghong Medicine Group Co.ltd).
Experimental animal and administration: experimental animal and administration are the same as embodiment 6.
Experimental method: after last dose 1h, will stick on hanged hook at Mouse Tail-tip 1cm, and hand rest mouse by its
It is linked into animal behavior video analytic system observation case, records the desperate behavior of mouse in 6min, mouse in 4min after analysis
Dead time.
Experimental result: influence of the spermidine to the dead time in rat force swimming test is as shown in table 3, and experimental data is by Mean
± SD is indicated.As shown in Table 3, consistent with Mouse Forced Swim Test result, spermidine active component middle dose group (0.05g/
Kg) spermidine active component low dose group (0.025g/kg) can be reduced the dead time in Tail suspension test, with blank pair
According to group more all have significant difference (P < 0.05OrP < 0.01), and certain dose dependent is presented.Mouse forces trip
Swimming test and rat force swimming test result all show that spermidine active component has apparent antidepressant effect, effect and classics
Antidepression chemicals Venlafaxine is suitable.
Influence (n=12) of 3 spermidine of table to the dead time in Tail suspension test
Compared with blank control group: *P < 0.05There are significant difference, * *P < 0.01There is extremely significant sex differernce
In conclusion this experimental results showed that spermidine active component can to significantly reduce behavioral despair animal models of depression small
Dead time in mouse.Hence, it can be determined that spermidine active component has significant antidepressant effect, it can be used for preparing prevention
And/or the drug or health food for the treatment of depression.
Embodiment 8: chronic unpredictable Stress model (CUMS)
Laboratory apparatus and reagent: animal behavior video analytic system (Chengdu TME Technology Co., Ltd.), prologue chamber (from
System), thermometer, timer, animal gastric perfusion needle, 1000 ml graduated cylinders, stopwatch, clip, medical adhesive tape.Spermidine active component, sugarcane
Sugar (development in science and technology Co., Ltd is recovered in Tianjin), sodium carboxymethylcellulose (CMC-Na, the triumphant logical limited public affairs of chemical reagent in Tianjin
Department), VENLAFAXINE HCL (Chengdu Kanghong Medicine Group Co.ltd).
Experimental animal and administration: male SD rat (Beijing Vital River Experimental Animals Technology Co., Ltd., credit number:
The capital SCXK() 2016-0006), 180-220g after adaptable fed 1 week, is randomly divided into 6 groups, every group 10.Venlafaxine is given
Pharmaceutical quantities are 0.05g/kg, total high, medium and low dosage of spermidine effective part extract be 34.6mg/kg, 17.3mg/kg,
8.65mg/kg, blank control and model control group give isometric distilled water.Groups of animals is according to weight daily stomach-filling 1 time, often
Secondary 10ml/200g, continuous 28 days.
CUMS depression model establish: stimulating factor include: fasting, prohibit water, constraint, folder tail, ultrasound stimulation, 4 DEG C of ice-water baths,
Foot shock, thermostimulation, round the clock disorder.Give a kind of stimulation at random daily, every kind of stimulation is no more than 4 times.Except blank control group
Outside, modeling program is raised and implemented to the equal single cage of remaining each group, and the modeling time is 28d.Modeling starts rear gastric infusion simultaneously, drug
Group gives respective concentration drug, and model group and blank control group give isometric distilled water.
Testing index:
Weight: in experiment the 0th, 7,14,21,28d weighing rat body weight.
Syrup preference rate: modeling starts and terminates to measure 1% syrup consumption of rat, calculates syrup preference rate.
Spacious field experiment: rat is put into spacious field case 5min, and rat passes through lattice number and upright number in 4min after record.
Experimental result: influence of the spermidine active component to indexs such as CUMS rat body weight, syrup preference rate, spacious field experiments
From table 4,5,6: spermidine active component can improve by CUMS modeling stress caused by rat body weight increases slowly, spacious
Energy reduces and declines to the preference of sweetness of cane sugar in the experiment of field, shows that spermidine active component has well to a certain extent
Antidepressant effect, pharmacological activity meets or exceeds antidepression Western medicine Venlafaxine.
Influence (x ± s, n=10, the unit: g) that 4 modeling of table and administration change rat body weight
Compared with model control group: * *p<0.01, *p<0.05Compared with blank control group:## p<0.01, # p<0.05
The influence (x ± s, n=10) of 5 modeling of table and administration to CUMS rat syrup preference rate
Compared with model control group: * *p<0.01, *p<0.05Compared with blank control group:## p<0.01, # p<0.05
The influence that 6 spermidine active component of table tests CUMS rat spacious field
Compared with model control group: * *p<0.01, *p<0.05Compared with blank control group:## p<0.01, # p<0.05
In conclusion this experimental results showed that spermidine active component can to significantly reduce behavioral despair animal models of depression small
Dead time in mouse improves by CUMS modeling stress caused rat body weight increasess slowly, energy drops in spacious field experiment
It is low and the preference of sweetness of cane sugar is declined, show it to a certain extent with good antidepressant effect, pharmacological activity reaches
It or is more than antidepression Western medicine Venlafaxine.Hence, it can be determined that spermidine active component has significant antidepressant effect, can use
In preparation prevention and/or the drug or health food for the treatment of depression.
Claims (5)
1. a kind of extracting method of antidepressant spermidine active component, it is characterised in that: specific step is as follows: taking dry safflower
Or the safflower dregs of a decoction, 60-90% alcohol reflux extract 1-2 times, are concentrated under reduced pressure, concentrate is suppressed pressure in standby column progress in C18 quick
Purifying, W1/W2 1-10, the W1 are sample quality to be separated in terms of mg, and W2 is the quality of C18 post separation material in terms of g;
10-100% ethyl alcohol or water elution are concentrated and dried up to spermidine effective part extract.
2. a kind of extracting method of antidepressant spermidine active component according to claim 1, it is characterised in that: obtained
The spermidine substance that the three cumarin acyl groups that the spermidine effective part extract obtained contains 4 configurations replace, total content are
50% or more.
3. the spermidine active component that the extracting method of antidepressant spermidine active component according to claim 1 obtains
The application of extract, it is characterised in that: the spermidine effective part extract is preparing antidepressant drug or health food
In application.
4. the application of spermidine effective part extract according to claim 3, it is characterised in that: the antidepressant medicine
Object is that pharmaceutically acceptable regular dosage form is made in the pharmaceutically acceptable auxiliary material of spermidine effective part extract addition.
5. the application of spermidine effective part extract according to claim 4, it is characterised in that: the dosage form is capsule
Agent, tablet, powder, granule, gelling agent, sustained release agent, oral solution or pill.
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