CN107260777A - A kind of fiveleaf akebia fruit with antitumor activity refines total saposins and its application - Google Patents
A kind of fiveleaf akebia fruit with antitumor activity refines total saposins and its application Download PDFInfo
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- CN107260777A CN107260777A CN201710507576.0A CN201710507576A CN107260777A CN 107260777 A CN107260777 A CN 107260777A CN 201710507576 A CN201710507576 A CN 201710507576A CN 107260777 A CN107260777 A CN 107260777A
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- akebia fruit
- fiveleaf akebia
- ethanol
- total saposins
- antitumor activity
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- 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)
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- 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
- A61K2236/331—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones using water, e.g. cold water, infusion, tea, steam distillation, decoction
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- 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
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- 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
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- 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
- A61K2236/51—Concentration or drying of the extract, e.g. Lyophilisation, freeze-drying or spray-drying
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- 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
- A61K2236/53—Liquid-solid separation, e.g. centrifugation, sedimentation or crystallization
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Abstract
Total saposins are refined the invention discloses a kind of fiveleaf akebia fruit with antitumor activity, it is prepared by following methods：Fiveleaf akebia fruit medicinal material is taken, crushes, takes medicinal powder, add ethanol, centrifugation is extracted in heating under slight boiling condition, takes ethanol extract, adjusts neutrality to obtain sample solution, upper macroporous absorbent resin, first it is washed with deionized water de-, then is eluted with 20~30% ethanol elution impurity eliminations, then with ethanol and n-butanol mixed solution, finally eluted with butanol solution, obtain fiveleaf akebia fruit and refine total saposins.The present invention carries out going deep into system research to fiveleaf akebia fruit chemical composition, filter out the optimal process that total saposins refine position for preparing, preparation method is workable, in particular by optimal macroreticular resin process for separation and purification, obtained total saposins refine position active constituent content and are up to more than 95%, with significant antitumor activity, and technique simple and stable, cost is low, is adapted to industrialized production.
Description
Technical field
The present invention relates to a kind of Chinese medicine, and in particular to a kind of fiveleaf akebia fruit with antitumor activity refines total saposins and its should
With.
Background technology
Tumour has turned into the number one killer for 21 century threatening human survival, and China is one of world's cancer country occurred frequently, and
And present a rapidly rising trend every year.Clinically the medicine for the treatment of tumour mainly has chemicals at present, but due to chemotherapeutics poison
Property big, also human autoimmune's cell such as kill leucocyte, lymphocyte of non-selectivity while tumour cell is killed, lead
Pathogenic people because of autoimmunity inferior capabilities accompanying infection, patient usually due to using erious adverse reaction, and survival rate is low, and expense
It is high.
Traditional Chinese medicine has unique advantage in terms of tumour is treated, and the natural class medicine by representative of Chinese medicine has poison is secondary to make
With small, action target spot is various, better tolerance the features such as, be more and more taken seriously in terms of tumour is treated.
Fiveleaf akebia fruit is Ben Tongke plants akebi, threeleaf akebia, Bai Bentong dry mature fruit.Property it is bitter, tremble with fear.Return liver, courage,
Stomach, bladder warp.With dispersing stagnated hepatoqi, promoting blood circulation and stopping pain, dissipating bind, diuresis.For treat gastral cavity the side of body distending pain, dysmenorrhoea Amenorrhea, subcutaneous nodule lump in the abdomen,
Difficult urination.
The content of the invention
Goal of the invention：Present invention aim to address the deficiencies in the prior art, fiveleaf akebia fruit chemical composition is deeply ground
Study carefully, filter out the optimal process that total saposins refine position for preparing, the fiveleaf akebia fruit total saposins active ingredient prepared contains
Amount is high, and antitumor activity is strong, and adverse reaction is low, and security is good, and has obvious activity to kinds of tumors, achieves extraordinary
Unexpected technique effect.
Technical scheme：In order to realize the above object the technical scheme that the present invention takes is：
A kind of fiveleaf akebia fruit with antitumor activity refines total saposins, and it is prepared by following methods：
Fiveleaf akebia fruit medicinal material is taken, is crushed, medicinal powder is taken, the ethanol of 6~12 times of volumes is added, then heats in micro-boiling shape
Extracted under state 1~3 time, 1~2h, centrifugation, take ethanol extract every time, adjust neutrality to obtain sample solution, upper macroporous absorbent resin is first
Be washed with deionized water and slough carbohydrate water-solubility impurity, then with the ethanol elution impurity elimination of volumetric concentration 20~30%, then with ethanol and
N-butanol mixed solution is eluted, and is finally eluted with butanol solution, merges ethanol and n-butanol mixed solution eluent and positive fourth
Alcoholic solution eluent, is concentrated to give fiveleaf akebia fruit and refines total saposins.
Preferably, the fiveleaf akebia fruit of the present invention with antitumor activity refines total saposins, and it is by with lower section
Method is prepared：
Fiveleaf akebia fruit medicinal material is taken, is crushed, medicinal powder is taken, 70% ethanol of 12 times of volumes is added, then heats in micro-boiling
Extracted 2 times under state, each 2h, centrifugation takes ethanol extract, adjust neutrality to obtain sample solution, upper D101 types macroporous absorbent resin,
First it is washed with deionized water and sloughs carbohydrate water-solubility impurity, then with the ethanol elution impurity elimination of volumetric concentration 30%, then with volume ratio 1：3
Ethanol and n-butanol mixed solution elution, finally eluted with butanol solution, merge ethanol and n-butanol mixed solution elution
Liquid and butanol solution eluent, are concentrated to give fiveleaf akebia fruit and refine total saposins.
Fiveleaf akebia fruit of the present invention with antitumor activity refines application of the total saposins in antineoplastic is prepared.
Preferably, the fiveleaf akebia fruit of the present invention with antitumor activity refines total saposins and is preparing anti-lung
Application in cancer, breast cancer, liver cancer, cervical carcinoma and gastric cancer medicament.
A kind of pharmaceutical preparation, the fiveleaf akebia fruit with antitumor activity that it includes described in claim 1 or 2 refines total soap
Glycosides；Preparation includes the formulations such as oral liquid, capsule, pill, tablet or granule.
Beneficial effect：Compared to the prior art the fiveleaf akebia fruit with antitumor activity that the present invention is provided refines total saposins has
Have the advantage that：
The present invention carries out going deep into system research to fiveleaf akebia fruit chemical composition, filters out the optimal total saposins that prepare and refines position
Process there is provided the fiveleaf akebia fruit with antitumor activity refine total saposins preparation method, it is workable, especially
Using optimal macroreticular resin process for separation and purification, obtained total saposins refine position active constituent content and are up to more than 95%,
And technique simple and stable, cost is low, is adapted to industrialized production.
Embodiment
With reference to specific embodiment, the present invention is furture elucidated, it should be understood that these embodiments be merely to illustrate the present invention and
Limitation the scope of the present invention is not used in, after the present invention has been read, various of equal value shapes of the those skilled in the art to the present invention
The modification of formula falls within the application appended claims limited range.
Embodiment 1
Fiveleaf akebia fruit with antitumor activity refines total saposins, and it is prepared by following methods：
Fiveleaf akebia fruit medicinal material is taken, is crushed, medicinal powder is taken, 70% ethanol of 12 times of volumes is added, then heats in micro-boiling
Extracted 2 times under state, each 2h, centrifugation takes ethanol extract, adjust neutrality to obtain sample solution, upper D101 types macroporous absorbent resin,
First it is washed with deionized water and sloughs carbohydrate water-solubility impurity, then with the ethanol elution impurity elimination of volumetric concentration 30%, then with volume ratio 1：3
Ethanol and n-butanol mixed solution elute 5 times of column volumes, finally with butanol solution elute 3 times of column volumes, merge ethanol and
N-butanol mixed solution eluent and butanol solution eluent, are concentrated to give fiveleaf akebia fruit and refine total saposins.HPLC detects total soap
Glycosides content 95%.
Take fiveleaf akebia fruit to refine total saposins and add lactose, cornstarch is well mixed, and adds magnesium stearate lubricant, and mixing is equal
Even, tablet is made in whole grain, then tabletting.
Embodiment 2
Fiveleaf akebia fruit with antitumor activity refines total saposins, and it is prepared by following methods：
Fiveleaf akebia fruit medicinal material is taken, is crushed, medicinal powder is taken, 70% ethanol of 6 times of volumes is added, then heats in micro-boiling shape
Extracted 3 times under state, each 2h, centrifugation takes ethanol extract, adjust neutrality to obtain sample solution, upper D101 types macroporous absorbent resin is first
It is washed with deionized water and sloughs carbohydrate water-solubility impurity, then with the ethanol elution impurity elimination of volumetric concentration 20%, then with volume ratio 1：3
Ethanol and n-butanol mixed solution elute 4 times of column volumes, finally elute 4 times of column volumes with butanol solution, merge ethanol and just
Butanol mixed solution eluent and butanol solution eluent, are concentrated to give fiveleaf akebia fruit and refine total saposins.HPLC detects total saposins
Content 94%.
Take fiveleaf akebia fruit to refine total saposins and add lactose, cornstarch is well mixed, and after granulation, filling capsule obtains capsule
Agent.Comparative example 1
Fiveleaf akebia fruit with antitumor activity refines total saposins, and it is prepared by following methods：
Fiveleaf akebia fruit medicinal material is taken, is crushed, medicinal powder is taken, 70% ethanol of 6 times of volumes is added, then heats in micro-boiling shape
Extracted 3 times under state, each 2h, centrifugation takes ethanol extract, adjust neutrality to obtain sample solution, upper D101 types macroporous absorbent resin is first
It is washed with deionized water and sloughs carbohydrate water-solubility impurity, then with the ethanol elution impurity elimination of volumetric concentration 20%, then with body ethanol elution 8
Times column volume, merges ethanol eluate, is concentrated to give fiveleaf akebia fruit and refines total saposins.HPLC detects total saponin content 72%.Implement
The anticancer experiment in vitro of example 3
With human lung cancer (MCF-7), breast cancer (A-5408), human liver cancer (SMMC-7451), human cervical carcinoma (Hela) and people's stomach
5 kinds of knurl strains of cancer (SGC-7901), carry out anticancer experiment in vitro, with embodiment 1, embodiment 2 using tetrazolium bromide reducing process (MTT)
It is test medicine to refine total saposins with the fiveleaf akebia fruit that comparative example 1 is prepared, using endoxan as positive controls, with sample
Solvent is that physiological saline is negative control group.Specific experiment result is as shown in table 1：
The fiveleaf akebia fruit of table 1 refines inhibitory action (IC of the total saposins to 5 plants of tumour cells50For half inhibiting rate)
The present invention filters out the preparation method that optimal fiveleaf akebia fruit refines total saposins by many experiments, using preferred second
Alcohol and n-butanol mixed solvent are as optimal elution solution, and the fiveleaf akebia fruit prepared refines the high purity of total saposins
95%.Whole stabilization of industry, easily real industrialized production, cost is low, achieves extraordinary technique effect.
And more than test result indicates that：The fiveleaf akebia fruit with antitumor activity that the present invention is provided refines total saposins pair
Lung cancer, breast cancer, human liver cancer, human cervical carcinoma and human gastric cancer are respectively provided with obvious inhibitory action, show the present invention provide have
The fiveleaf akebia fruit of antitumor activity, which refines total saposins, has the effect of very strong anti-human malignant tumour, can be used for malignancy disease
Treatment.
Described above is only the preferred embodiment of the present invention, it is noted that for the ordinary skill people of the art
For member, under the premise without departing from the principles of the invention, some improvements and modifications can also be made, these improvements and modifications also should
It is considered as protection scope of the present invention.
Claims (5)
1. a kind of fiveleaf akebia fruit with antitumor activity refines total saposins, it is characterised in that it is prepared by following methods：
Fiveleaf akebia fruit medicinal material is taken, is crushed, medicinal powder is taken, the ethanol of 6~12 times of volumes is added, then heats under slight boiling condition
Extract 1~3 time, 1~2h, centrifugation, take ethanol extract every time, adjust neutrality to obtain sample solution, upper macroporous absorbent resin is first spent
Ion water elution removes carbohydrate water-solubility impurity, then with the ethanol elution impurity elimination of volumetric concentration 20~30%, then with ethanol and positive fourth
Mixed alkoxide solution is eluted, and is finally eluted with butanol solution, merges ethanol and n-butanol mixed solution eluent and n-butanol is molten
Liquid eluent, is concentrated to give fiveleaf akebia fruit and refines total saposins.
2. the fiveleaf akebia fruit according to claim 1 with antitumor activity refines total saposins, it is characterised in that it is by following
Method is prepared：
Fiveleaf akebia fruit medicinal material is taken, is crushed, medicinal powder is taken, 70% ethanol of 12 times of volumes is added, then heats in slight boiling condition
Lower to extract 2 times, each 2h, centrifugation takes ethanol extract, adjusts neutrality to obtain sample solution, upper D101 types macroporous absorbent resin is first used
Carbohydrate water-solubility impurity is removed in deionized water elution, then with the ethanol elution impurity elimination of volumetric concentration 30%, then with volume ratio 1：3 second
Alcohol and the elution of n-butanol mixed solution, are finally eluted with butanol solution, merge ethanol and n-butanol mixed solution eluent and
Butanol solution eluent, is concentrated to give fiveleaf akebia fruit and refines total saposins.
3. the fiveleaf akebia fruit with antitumor activity described in claim 1 or 2 refines total saposins in antineoplastic is prepared
Using.
4. the fiveleaf akebia fruit with antitumor activity described in claim 1 or 2 refines total saposins and is preparing anti-lung cancer, breast cancer,
Application in liver cancer, cervical carcinoma and gastric cancer medicament.
5. a kind of pharmaceutical preparation, it is characterised in that it includes the fiveleaf akebia fruit with antitumor activity described in claim 1 or 2
Refined total saposins；Preparation includes oral liquid, capsule, pill, tablet or granule.
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110464686A (en) * | 2019-09-18 | 2019-11-19 | 深圳波顿香料有限公司 | The preparation method and application of Akebia Fruit natural surfactant |
| CN111494442A (en) * | 2020-06-02 | 2020-08-07 | 陕西科技大学 | Method for improving extraction yield of total saponins in akebia trifoliata peels |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110464686A (en) * | 2019-09-18 | 2019-11-19 | 深圳波顿香料有限公司 | The preparation method and application of Akebia Fruit natural surfactant |
| CN111494442A (en) * | 2020-06-02 | 2020-08-07 | 陕西科技大学 | Method for improving extraction yield of total saponins in akebia trifoliata peels |
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