CN104523698B - Application of the hederagenin in preparation anti-endometrial cancer cell HEC-1 tumour medicine - Google Patents
Application of the hederagenin in preparation anti-endometrial cancer cell HEC-1 tumour medicine Download PDFInfo
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Abstract
The invention discloses hederagenin application in preparations of anti-tumor drugs.Hederagenin of the present invention is extracted from natural medicinal material teasel root, and teasel root is common Chinese medicine, there is long-term administration experience of traditional Chinese medicine, and the medicine is safe to use, is recorded without overt toxicity effect.Studies have shown that hederagenin has exact anti-tumor activity, significant effect is antitumor compared with Western medicine comparatively safe, Small side effects, has exploitation at the prospect of anti-tumor drug.
Description
The application be on 09 28th, 2013, application No. is 2013104529876, entitled ivy the applying date
The divisional application of sapogenin application in preparation of anti-tumor drugs.
Technical field:
The invention belongs to the field of Chinese medicines, and in particular to hederagenin application in preparation of anti-tumor drugs.
Technical background:
Tumour is one of the major factors of human death.Research anti-tumor drug has become a hot spot worldwidely.It closes
At drug while antitumor, huge injury is generated to human body.It studies and finds from natural drug and is effective and low toxicity
Compound is of great significance.
Hederagenin (Hederagenin), alias (3beta, 4alpha) -3,23-Dihydroxyolean-12-
en-28-oic acid；Hederagenin, molecular formula C30H48O4, structural formula are as follows:
Summary of the invention:
The purpose of the present invention is to provide hederagenin application in preparations of anti-tumor drugs.
The purpose of the present invention is achieved through the following technical solutions:
Hederagenin application in preparation of anti-tumor drugs.
Above-mentioned application is that the hederagenin has in body anti-tumor activity, described anti-swollen in body
Tumor activity are as follows: anti-breast cancer MCF-7 tumour, suppressing lung cancer A 549 tumour, anti-liver cancer and anti-Hep3B tumour, anti-gastric cancer MGC-803 tumour,
Inhibitor against colon carcinoma cells LoVo tumour, ovarian cancer resistance HO-8910PM tumour, anti-endometrial cancer cell HEC-1 tumour, resisting leukemia K 562
Tumour, anti-esophageal squamous carcinoma cell Eca-109 tumour.
Above-mentioned application is that the purity of the hederagenin is 50%~99%.
Above-mentioned application is that the anti-tumor drug includes hederagenin and pharmaceutically acceptable carrier
Or conventional edible adjuvant.
The dosage form of above-mentioned anti-tumor drug is any one pharmaceutically acceptable dosage form.
Hederagenin of the present invention is extracted from natural medicinal material teasel root, and teasel root is common Chinese medicine,
It is known to those skilled in the art as the method for raw material preparation different purity hederagenin using teasel root.
Known to those skilled in the art 25 ± 5 DEG C of room temperature of the present invention.
Beneficial effects of the present invention:
Hederagenin of the present invention is extracted from natural medicinal material teasel root, and teasel root is common Chinese medicine,
There is long-term administration experience of traditional Chinese medicine, the medicine is safe to use, record free of toxic effects.
Studies have shown that hederagenin has exact anti-tumor activity, significant effect, opposite peace antitumor compared with Western medicine
Entirely, Small side effects have exploitation at the prospect of anti-tumor drug.
Specific embodiment:
Embodiment 1: the preparation of trial drug hederagenin:
Hederagenin (self-control；Purity is 50%, 99%；Preparation method: taking teasel root medicinal material, appropriate to crush, with 90%
Ethyl alcohol extract 3 times, filtration merges 3 filtrates, ethyl alcohol is recovered under reduced pressure to no alcohol taste, with 50% ethyl alcohol be settled to 1g medicinal material/
The hydrochloric acid (commercially available, to analyze pure, mass fraction 37%) of liquor capacity score 7%~10% is added in 30mL, and water-bath reflux 3 is small
When, hydrolysis temperature (bath temperature) is 80 DEG C, and ethyl alcohol is recovered under reduced pressure to no alcohol taste in hydrolyzate, places 24~36 at room temperature
Hour, it precipitates, filtration, obtains sediment, it is 50% hederagenin sediment, warp that 65 DEG C or less, which are dried under reduced pressure to get purity,
A small amount of repeatedly washing, is washed through a small amount of 5% ethyl alcohol, and it is 99% hederagenin that 65 DEG C or less, which are dried under reduced pressure to get purity).
Embodiment 2:
Hederagenin anti-human breast cancer in nude mice MCF-7 tumour, anti-lung cancer in nude mice A549 tumour, anti-hepatocellular carcinoma in nude mice Hep3B
Tumour, anti-nude mice colon cancer LoVo tumour, anti-ovarian Cancer of Nude Mice HO-8910PM tumour, resists anti-gastric cancer in nude mice MGC-803 tumour
Nude mice endometrial carcinoma cell HEC-1 tumour, anti-nude mice leukemia K562 tumour, anti-nude mice esophageal squamous cell carcinoma cell Eca-109 are swollen
Tumor experiment:
1. breast cancer MCF-7 nude mice is in body anti-tumor experiment
1.1 experimental methods:
The MCF-7 Human Breast Cancer Cells strain of logarithmic growth phase, is aseptically prepared into 1 × 10 afterwards8/ ml cell is outstanding
It is subcutaneous to be inoculated in armpit on the right side of BALB/c nude mouse with 0.1ml for liquid.Nude Mice is straight with vernier caliper measurement transplantable tumor
Diameter, to tumour growth to 100~300mm3Animal is grouped at random afterwards.Use the method for measurement knurl footpath, dynamic observation subject
Antitumor effect.The pendulous frequency of diameter of tumor is to survey 1 time for every 4 days.Administered volume is 0.4ml/20g.It is administered once a day,
It is administered 28 days altogether.Negative control group, which gavages, gives isometric physiological saline, and tamoxifen dosage is 4mg/kg, 99% ivy
The high dose of sapogenin is 405mg/kg, the middle dosage of 99% hederagenin is 135mg/kg, 99% hederagenin
Low dosage be 45mg/kg, 50% hederagenin is 270mg/kg.After 29 days, mouse is put to death, operation strips tumor mass and claims
Weight.
1.2 positive drugs:
Tamoxifen (producer: Yangzijiang Pharmaceutical Group Co., Ltd, lot number: 12070411, specification: piece × 60 10mg/
Piece).Preparation method: administration every time takes drug tamoxifen piece 10mg that CMC-Na 50ml is added, and being configured to concentration is 0.2mg/
The liquid of ml, administered volume 0.4ml/20g, i.e. dosage are 4mg/kg.
Tweight: administration group average knurl weight；Cweight: negative control group average knurl weight.
1.3 experimental result
Inhibiting effect that 1. hederagenin of table grows human breast carcinoma MCF-7 nude mouse xenograft tumor (n=10,)
| Group | Dosage (mg/kg) | Knurl weight (g) | Tumour inhibiting rate (%) |
| Negative control group | — | 0.60±0.14 | — |
| Tamoxifen | 4 | 0.16±0.11** | 73.33% |
| 99% hederagenin high dose group | 405 | 0.21±0.05** | 65.00% |
| 99% hederagenin low dose group | 135 | 0.22±0.06** | 63.33% |
| 99% hederagenin middle dose group | 45 | 0.23±0.05** | 61.67% |
| 50% Hederagenin tuples | 270 | 0.24±0.08** | 60.00% |
Note: compared with negative control group, P < 0.01 * P < 0.05, * *.
2. lung cancer A549 nude mice is in body anti-tumor experiment
2.1 experimental methods:
SPF grades BALB/c nude mice 60,6 week old, 16~18g of weight.Logarithmic growth phase A549 cell, use are sterile
It is 3 × 10 that PBS, which adjusts A549 cell concentration,7/ mL is inoculated with A549 cell 0.1mL in BALB/c nude mice dorsal sc, to subcutaneously move
It plants knurl product and reaches 75mm3When left and right (about 10d), it is grouped by knurl is long-pending with mice with tumor weight homeostatic principle.It is administered daily 1 time, gives
Medicine 28 days, during administration every 4 days with vernier caliper measurement transplantable tumor longest diameter (L) and shortest diameter (W).It is taken off after last dose 48h
Mortar puts to death mouse, cuts off transplantable tumor, weighs knurl weight.Isometric physiological saline, cis-platinum (DDP) dosage is injected intraperitoneally in negative control group
For 2mg/kg, the high dose of 99% hederagenin is 405mg/kg, and the middle dosage of 99% hederagenin is 135mg/
Kg, the low dosage of 99% hederagenin is 45mg/kg, 50% hederagenin is 270mg/kg.
2.2 positive drugs:
Cis-platinum (DDP) (Qilu Pharmaceutical Co., Ltd., batch number: 509017IDB, specification: every 10mg).Dosage is
2.0mg/kg, i.p.
Inhibiting effect that 2. hederagenin of table grows lung cancer A549 nude mouse xenograft tumor (n=10,)
| Group | Dosage (mg/kg) | Knurl weight (g) | Tumour inhibiting rate (%) |
| Negative control group | — | 0.69±0.10 | — |
| Cis-platinum | 2 | 0.13±0.09** | 81.16% |
| 99% hederagenin high dose group | 405 | 0.21±0.07** | 69.56% |
| 99% hederagenin low dose group | 135 | 0.22±0.04** | 68.12% |
| 99% hederagenin middle dose group | 45 | 0.23±0.06** | 66.67% |
| 50% Hederagenin tuples | 270 | 0.25±0.010** | 63.77% |
Note: compared with negative control group, P < 0.01 * P < 0.05, * *.
3. liver cancer Hep3B nude mice is in body anti-tumor experiment
3.1 experimental methods:
The Hep3B cell strain of logarithmic growth phase is mixed with physiological saline, single cell suspension is made, by every 1 × 107It is a
Cell injects on the outside of the right rear leg of nude mice back subcutaneously, and totally 60.After 4 days, there is tangibly hard mass.To growth of transplanted human
To about 0.3cm2, it is randomly divided into 6 groups, every group 10.It is administered daily 1 time, is administered 28 days altogether.Use vernier calliper within every 4 days during administration
Ruler measures transplantable tumor longest diameter (L) and shortest diameter (W).Mouse is put to death in dislocation after last dose 48h, is cut off transplantable tumor, is weighed tumor
Weight.Isometric physiological saline is injected intraperitoneally in negative control group, and Fluorouracil Injection (5-FU injection) dosage is 20mg/kg,
The high dose of 99% hederagenin is 405mg/kg, and the middle dosage of 99% hederagenin is 135mg/kg, and 99% often
The low dosage of spring rattan sapogenin is 45mg/kg, 50% hederagenin is 270mg/kg.
3.2 positive drugs:
Fluorouracil Injection (5-FU injection) (Tianjin Jin Yao Amino Acid Co., Ltd product, lot number 1311171).
5-FU control group dosage is 20mg/kg, i.p.
Inhibiting effect that 3. hederagenin of table grows liver cancer Hep3B nude mouse xenograft tumor (n=10,)
| Group | Dosage (mg/kg) | Knurl weight (g) | Tumour inhibiting rate (%) |
| Negative control group | — | 0.61±0.04 | — |
| Fluorouracil | 20 | 0.17±0.04** | 72.13% |
| 99% hederagenin high dose group | 405 | 0.21±0.05** | 65.57% |
| 99% hederagenin low dose group | 135 | 0.22±0.03** | 63.93% |
| 99% hederagenin middle dose group | 45 | 0.23±0.06** | 62.30% |
| 50% Hederagenin tuples | 270 | 0.24±0.07** | 60.66% |
Note: compared with negative control group, P < 0.01 * P < 0.05, * *.
4. -803 nude mice of Gastric Cancer MGC is in body anti-tumor experiment
4.1 experimental methods:
Prepare cell suspension, under mirror the low differentiation Patients with Mucinous Gastric Carcinoma MGC-803 cell strain cell concentration of adjustment people to 3,000,000,
Cell suspension 0.3mL (about 1,000,000 cells) injection nude mice nape is subcutaneous, sterile nursing 4 weeks, it is prepared into knurl source nude mice execution
Knurl source nude mice takes out transplantable tumor and shreds into 2mm3The tumor mass of size is seeded to each experimental mouse sterile nursing 1week and is prepared into lotus knurl
Nude mice.Isometric physiological saline is injected intraperitoneally in negative control group, and Fluorouracil Injection (5-FU injection) dosage is 20mg/
Kg, the high dose of 99% hederagenin are 405mg/kg, and the middle dosage of 99% hederagenin is 135mg/kg, 50%
The low dosage of hederagenin is 45mg/kg, and 50% hederagenin is 270mg/kg.It is administered daily 1 time, 28 is administered altogether
It.
4.2 positive drugs:
Fluorouracil Injection (5-FU injection) (Tianjin Jin Yao Amino Acid Co., Ltd product, lot number 1311171).
Inhibiting effect that 4. hederagenin of table grows -803 nude mouse xenograft tumor of Gastric Cancer MGC (n=10,)
| Group | Dosage (mg/kg) | Knurl weight (g) | Tumour inhibiting rate (%) |
| Negative control group | — | 0.58±0.08 | — |
| Fluorouracil | 50 | 0.15±0.06** | 74.14% |
| 99% hederagenin high dose group | 405 | 0.17±0.04** | 70.69% |
| 99% hederagenin low dose group | 135 | 0.18±0.05** | 68.97% |
| 99% hederagenin middle dose group | 45 | 0.20±0.03** | 65.52% |
| 50% Hederagenin tuples | 270 | 0.22±0.10** | 62.07% |
Note: compared with negative control group, P < 0.01 * P < 0.05, * *.
5. colon cancer LoVo nude mice is in body anti-tumor experiment
5.1 test method
BALB/C nude mice 60, be purchased from Chinese Academy of Medical Sciences's Shanghai Experimental Animal Center, age of mouse 4~6 weeks, weight 20~
25g is raised in nude mice room under the conditions of SPF.Aseptically, nude mouse right fore dorsal sc injection LoVo cell, note
Penetrate part and obvious skin mound occur, all after 7d to be vaccinated nude mouse and tubercle occur, Nude Mouse Model is established, then by with
Machine is divided into 6 groups, every group 10.Isometric physiological saline, Fluorouracil Injection (5-FU injection is injected intraperitoneally in negative control group
Liquid) intraperitoneal injection dosage is 20mg/kg, the high dose of 99% hederagenin is 405mg/kg, 99% hederagenin
Middle dosage be 135mg/kg, the low dosage of 99% hederagenin is 45mg/kg, 50% hederagenin is 270mg/
kg.It is administered daily 1 time, continuous 28d.
5.2 positive drug
5%5-FU injection (Tianjin Jin Yao Amino Acid Co., Ltd product, lot number 1311171).
Inhibiting effect that 5. hederagenin of table grows colon cancer LoVo nude mouse xenograft tumor (n=10,)
| Group | Dosage (mg/kg) | Knurl weight (g) | Tumour inhibiting rate (%) |
| Negative control group | — | 0.59±0.07 | — |
| Fluorouracil | 20 | 0.16±0.09** | 72.88% |
| 99% hederagenin high dose group | 405 | 0.18±0.03** | 69.49% |
| 99% hederagenin low dose group | 135 | 0.20±0.06** | 66.10% |
| 99% hederagenin middle dose group | 45 | 0.22±0.05** | 62.71% |
| 50% Hederagenin tuples | 270 | 0.21±0.09** | 64.41% |
Note: compared with negative control group, P < 0.01 * P < 0.05, * *.
6. oophoroma HO-8910PM nude mice is in body anti-tumor experiment
6.1 experimental methods:
4~6 week old female BAl BIcs/c nude mice is selected, by 2 × 107A HO-8910PM cell is suspended in 0.2mL serum-free
In RPMI-1640 culture medium, nude mice back is injected into close to right hindlimb and subcutaneously establishes ovarian Cancer of nude mice subcutaneous transplantation knurl model,
Postoperative nude mice continues raising in the laboratory SPF.After being inoculated with 2 weeks, to transplantable tumor, the bulk grows to 100~150mm3, by tumor bearing nude mice
6 groups are randomly divided into, every group 10, negative control group stomach-filling gives distilled water 0.2mL/ only, and Docetaxel dosage is 0.5mg/
Kg, the high dose of 99% hederagenin are 405mg/kg, and the middle dosage of 99% hederagenin is 135mg/kg, 99%
The low dosage of hederagenin is 45mg/kg, 50% hederagenin is 270mg/kg.
It is administered daily 1 time, is administered 28 days altogether.8th week execution nude mice takes subcutaneous transplantation tumor tissue, measures tumor quality；Suppression
Ratio of outflow=(1- administration group average knurl weight/negative control group average knurl weight) × 100%.
6.2 positive drugs:
Docetaxel group (0.5mg/kg) (Hengrui Medicine).
Inhibiting effect (the n=that 6. hederagenin of table grows oophoroma HO-8910PM nude mouse xenograft tumor
10,)
Note: compared with negative control group, P < 0.01 * P < 0.05, * *.
7. endometrial carcinoma cell HEC-1 nude mice is in body anti-tumor experiment
7.1 experimental methods:
With 75% ethanol disinfection nude mice bilateral back part skin on superclean bench, adjusted with the extraction of 1ml empty needle
Concentration (1 × 108ml-1) endometrial carcinoma cell suspension, every side inoculates 0.2ml and (contains cell number 2 × 107It is a).Modeling
Whether the modeling of evaluation in the 10th day succeeds.60 nude mices are randomly divided into 6 groups, every group 10 after model foundation.Respectively at modeling the
It is administered within 11 days, stomach-filling gives distilled water 0.2mL/ only to negative control group respectively, cisplatin dose 3mg/kg, 99% Hederagenin
Member high dose be 405mg/kg, the middle dosage of 99% hederagenin is 135mg/kg, 99% hederagenin it is low
Dosage is 45mg/kg, 50% hederagenin is 270mg/kg.It is administered daily 1 time, successive administration 4 weeks.
7.2 positive drugs and carcinoma of endometrium HEC-I cell:
Carcinoma of endometrium HEC-I cell is purchased from Cell Bank of Chinese Academy of Sciences, and cis-platinum is purchased from Sigma.
Inhibiting effect (the n that 7. hederagenin of table grows endometrial carcinoma cell HEC-1 nude mouse xenograft tumor
=10,)
| Group | Dosage (mg/kg) | Knurl weight (g) | Tumour inhibiting rate (%) |
| Negative control group | — | 0.62±0.07 | — |
| Cis-platinum | 3 | 0.15±0.06** | 75.81% |
| 99% hederagenin high dose group | 405 | 0.18±0.07** | 70.97% |
| 99% hederagenin low dose group | 135 | 0.22±0.03** | 64.52% |
| 99% hederagenin middle dose group | 45 | 0.25±0.05** | 59.68% |
| 50% Hederagenin tuples | 270 | 0.24±0.11** | 61.29% |
Note: compared with negative control group, P < 0.01 * P < 0.05, * *.
8. leukemia K 562 nude mice is in body anti-tumor experiment
8.1 experimental methods:
The K562 cell strain of logarithmic growth phase in biological clean bench, with the RPMI1640 culture medium for being free of serum
It is configured to 1 × 1012A/L single cell suspension.It is thin with sterile 1ml syringe subcutaneous vaccination 0.1ml at 60 nude mices right side armpits
Born of the same parents' suspension, and it is denoted as inoculation the 1st day.In inoculation the 12nd day, most of nude mice is tangible to arrive subcutaneous tumor.Filter out gross tumor volume
About 100mm360 tumor bearing nude mices, be divided into negative control group (water, 10ml/kg are steamed in sterilizing two), positive right by randomization
According to group, the high, medium and low dosage group of 99% hederagenin and 50% Hederagenin tuples, totally 6 groups, every group 10.In grouping
Start to be administered within the 2nd day afterwards.CTX group, which is injected intraperitoneally, gives the sterile CTX normal saline solution that concentration is 2.5mg/ml, and every 2 days 1
It is secondary；Negative control group, each dosage group of 99% hederagenin, the equal gastric infusion of 50% Hederagenin tuples, 1 time a day,
Total 28d.Each group presses every nude mice 10ml/kg administration.Cyclophosphamide (CTX) dosage is 25mg/kg, 99% hederagenin
High dose be 405mg/kg, the middle dosage of 99% hederagenin is 135mg/kg, low dose of 99% hederagenin
Amount is 45mg/kg, 50% hederagenin is 270mg/kg.
8.2 positive drugs:
Syklofosfamid ampoule (CTX, lot number 10052341, Hengrui Medicine Co., Ltd., Jiangsu Prov.).
Inhibiting effect that 8. hederagenin of table grows leukemia K 562 nude mouse xenograft tumor (n=10,)
| Group | Dosage (mg/kg) | Knurl weight (g) | Tumour inhibiting rate (%) |
| Negative control group | — | 0.64±0.10 | — |
| Cyclophosphamide | 25 | 0.15±0.08** | 76.56% |
| 99% hederagenin high dose group | 405 | 0.18±0.09** | 71.88% |
| 99% hederagenin low dose group | 135 | 0.20±0.07** | 68.75% |
| 99% hederagenin middle dose group | 45 | 0.24±0.08** | 62.50% |
| 50% Hederagenin tuples | 270 | 0.23±0.11** | 64.06% |
Note: compared with negative control group, P < 0.01 * P < 0.05, * *.
9. esophageal squamous cell Eca-109 nude mice is in body anti-tumor experiment
9.1 experimental methods:
Every mouse dorsal sc injection about 0.2mL sterile esophageal squamous carcinoma cell Eca-109 cell suspension (contains 6.0 × 106~
8.0×106Cell), after inoculation every two days with vernier caliper measurement knurl longest diameter a and shortest diameter b, calculate gross tumor volume V=
1/2ab2, long to about 0.2cm to gross tumor volume after 1 week3Random grouping afterwards, every group 10.Negative control group intraperitoneal injection is isometric
Physiological saline, Fluorouracil Injection (5-FU injection) intraperitoneal injection dosage are 10mg/kg, the height of 99% hederagenin
Dosage is 405mg/kg, and the middle dosage of 99% hederagenin is 135mg/kg, and the low dosage of 99% hederagenin is
45mg/kg, 50% hederagenin are 270mg/kg.It is to be administered daily 1 time, continuous 28d.
9.2 positive drugs:
5-Fu (10mL/0.25g) (Tianjin Jin Yao Amino Acid Co., Ltd product, lot number 1311171), 5-Fu is pressed
10mg/kg intraperitoneal injection.
Inhibiting effect (the n that 9. hederagenin of table grows esophageal squamous cell Eca-109 nude mouse xenograft tumor
=10,)
| Group | Dosage (mg/kg) | Knurl weight (g) | Tumour inhibiting rate (%) |
| Negative control group | — | 0.63±0.12 | — |
| Fluorouracil | 10 | 0.17±0.07** | 73.02% |
| 99% hederagenin high dose group | 405 | 0.19±0.05** | 69.84% |
| 99% hederagenin low dose group | 135 | 0.21±0.06** | 66.67% |
| 99% hederagenin middle dose group | 45 | 0.24±0.04** | 61.90% |
| 50% Hederagenin tuples | 270 | 0.23±0.09** | 63.49% |
Note: compared with negative control group, P < 0.01 * P < 0.05, * *.
Conclusion:
Hederagenin has in body anti-tumor activity.Specifically in body anti-tumor activity are as follows: anti-human breast cancer in nude mice MCF-7
Tumour, anti-lung cancer in nude mice A549 tumour, anti-hepatocellular carcinoma in nude mice Hep3B tumour, anti-gastric cancer in nude mice MGC-803 tumour, anti-nude mice colon
Cancer LoVo tumour, anti-ovarian Cancer of Nude Mice HO-8910PM tumour, anti-nude mice endometrial carcinoma cell HEC-1 tumour, the white blood of anti-nude mice
Sick K562 tumour, anti-nude mice esophageal squamous cell carcinoma cell Eca-109 tumour.
Embodiment 3: purity is 99% hederagenin, purity is 50% hederagenin sample formulation
The preparation method of 98% hederagenin capsule: 99% hederagenin powder in Example 1 is added
1%~15% starch or other pharmaceutically acceptable carriers or conventional edible adjuvant (or other pharmaceutically acceptable loads
Body or conventional edible adjuvant: pharmaceutically acceptable carrier includes the auxiliary material of oral formulations auxiliary material or Parenteral.
Administration route can be oral, injection, local administration etc..According to the technique and scheme of the present invention, the composition can be oral system
Agent or injection preparation, wherein oral preparation includes capsule, soft capsule, granule, oral solution, tablet, dripping pill etc..It is used
Auxiliary material includes: starch, sucrose, lactose, Icing Sugar, glucose, mannitol, xylitol, polyethylene glycol, isopropanol, Tween-80, sweet
Oil, propylene glycol, microcrystalline cellulose sodium, dextrin, cyclodextrin, sodium chloride, vitamin C, cysteine, citric acid, sodium thiosulfate,
The customary adjuvants such as sodium sulfite, stearate and gelatin, the later period preparation process and equipment of preparation belong to the routine of pharmaceutical field
Technology, this is not limited by the present invention, and therefore it will not be described in detail herein), it is wetting with 90% ethyl alcohol (or ethyl alcohol, water of other concentration)
Agent prepares softwood, crosses the granulation of 20 meshes, drying at 60 DEG C, and 20 meshes arrange to get conforming particle, fill No. 0 capsule, be
0.315g/ again, wherein 0.015g/ auxiliary material grain, 99% hederagenin grain of 0.300g.It takes daily 3 times, it is 1-3 each.
The preparation method of 50% hederagenin capsule: 50% hederagenin powder in Example 1 is added
1%~15% starch or other pharmaceutically acceptable carriers or conventional edible adjuvant, with 90% ethyl alcohol (or other concentration
Ethyl alcohol, water) it is wetting agent, softwood is prepared, the granulation of 20 meshes, drying at 60 DEG C are crossed, 20 meshes arrange to get conforming particle, fill 0
Number capsule is 0.315g/ and weighs, wherein 0.015g/ auxiliary material grain, 50% hederagenin grain of 0.300g.Take daily 3 times, often
It is 2-4 secondary.
Claims (3)
1. application of the hederagenin in preparation anti-endometrial cancer cell HEC-1 tumour medicine.
2. application according to claim 1, it is characterised in that the purity of the hederagenin is 50%~99%.
3. application according to claim 1, it is characterised in that the anti-tumor drug includes hederagenin and medicine
Acceptable carrier or conventional edible adjuvant on.
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| CN201310452987.6A CN103463098B (en) | 2013-09-28 | 2013-09-28 | Application of hederagenin for preparing antineoplastic drugs |
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| CN101125880A (en) * | 2007-08-13 | 2008-02-20 | 中国科学院新疆理化技术研究所 | Bindwood sapogenin and its preparation method and use |
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| CN101125880A (en) * | 2007-08-13 | 2008-02-20 | 中国科学院新疆理化技术研究所 | Bindwood sapogenin and its preparation method and use |
| CN102443619A (en) * | 2010-10-09 | 2012-05-09 | 苏州宝泽堂医药科技有限公司 | Method for extracting chlorogenic acid and hederagenin from honeysuckle flower |
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