CN1431221A - Total saponin of polygara aureocauda dunn and madication combination as well as its preparing method - Google Patents
Total saponin of polygara aureocauda dunn and madication combination as well as its preparing method Download PDFInfo
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Abstract
A common saponin of yellowstem milkwort with hypolipemic activity and its medicinal composition and preparing process are disclosed. The said common saponin is prepared from the yellowstem milkwort through extracting in water, chromatography by resin column, eluting with water or alcohol, and collecting the liquid.
Description
Technical field
The present invention relates to plant amedica Radix Polygalae fallacis efficient part and extraction and separation method thereof, and the pharmaceutical composition that contains the Radix Polygalae fallacis efficient part, be specially that extraction separation has the efficient part of lipopenicillinase and cardiac vascular activity from Radix Polygalae fallacis, and be prepared into pharmaceutical composition.
Background technology
Radix Polygalae fallacis is the dry root of Polygalaceae polygala Radix Polygalae fallacis (Polygala fallax Hemsl.[PaureocaudaDunn.]), is Guangxi medicine commonly used among the people.Main product Jiangxi, Hunan, Guangdong, Guangxi and Yunnan, the mountain valley sylvan life of being born in height above sea level 1150-1650m, the other dark and damp place of water (referring to: Chinese Academy of Sciences's Chinese Plants will, the 43 volume, the third volume of a work. Beijing: Science Press, 1997:151-152.).Sweet, the little hardship of this taste, flat.Have help, strong, clearing damp, the stasis of blood effect of loosing cures mainly weak puffiness, acute, chronic hepatitis, waist and leg ache, wound.Yellow win light etc. reported the clinical observation of Radix Polygalae fallacis treatment hyperlipidemia 30 examples (referring to the Hunan Journal of Traditional Chinese Medicine, 1999,15 (3): 6-7), but all do not relate to the basic substance of Radix Polygalae fallacis tool effect for reducing fat and curative effect.
Summary of the invention
The technical problem to be solved in the present invention is: for guiding, the lipopenicillinase activity of Radix Polygalae fallacis is carried out the screening of efficient part as biological activity how, and the chemical ingredients of research efficient part, and the pharmaceutical composition that contains this efficient part.
The technical problem that solves also comprises: but the extraction and separation method of the lipopenicillinase efficient part suitability for industrialized production of research Radix Polygalae fallacis, it not only requires technology simple relatively, and will reach the content standard of registration medicine regulation, and that will ensure the quality of products simultaneously is stable.Because have only the content conformance with standard just can reach clinical efficacy, steady quality could guarantee stable curative effect.
For solving the problems of the technologies described above, the invention provides following technical scheme.
A kind of Radix Polygalae fallacis total saponins with effect for reducing fat is characterized in that preparing as follows:
With the Radix Polygalae fallacis aqueous extract, the macroporous resin column of last D101, HP20 or AB8 model, water and aqueous ethanol gradient elution are collected the 60-70% ethanol eluate, get the Radix Polygalae fallacis total saponins.
A kind of preparation method with Radix Polygalae fallacis total saponins of effect for reducing fat, it is characterized in that: with the Radix Polygalae fallacis aqueous extract, the macroporous resin column of last D101, HP20 or AB8 model, water and aqueous ethanol gradient elution, collect the 60-70% ethanol eluate, get the Radix Polygalae fallacis total saponins.
The preparation method of described Radix Polygalae fallacis total saponins is: with the Radix Polygalae fallacis aqueous extract, the macroporous resin column of last D101 or AB8 model behind water and the 30-40% ethanol elution, is collected the 60-70% ethanol eluate respectively, gets the Radix Polygalae fallacis total saponins.And the present invention is with the Radix Polygalae fallacis aqueous extract, without concentrating, directly goes up resin column.
The preparation method of described Radix Polygalae fallacis total saponins, when separating with resin column, applied sample amount is about by medicinal material weight: macroporous resin volume ratio 2～1: 1.When separating with resin column, mode is that applied sample amount is about by medicinal material weight: macroporous resin volume ratio 1.5: 1 preferably; Collect 65% ethanol eluate.
The even more ideal preparation method of described Radix Polygalae fallacis total saponins is: get the Radix Polygalae fallacis meal, soaked 3 hours, extract 3 times, three times amount of water is respectively 10,8,6 times of amounts, and three times extraction time is respectively 1.5,1.5,1 hour; With the Radix Polygalae fallacis aqueous extract, directly go up the D101 macroporous resin column, wash resin column earlier with water, wash with 40% ethanol again, continue and use 65% ethanol elution, collect 65% ethanol position, after the solvent recovered under vacuum, get the Radix Polygalae fallacis total saponins.
A kind of pharmaceutical composition that is used for lipopenicillinase wherein contains aforementioned each the Radix Polygalae fallacis total saponins and the pharmaceutically acceptable carrier of treatment significant quantity.
Aforementioned any one Radix Polygalae fallacis total saponins, the application in the preparation fat-reducing medicament.
Introduce the screening and the total saponins Study on extraction of Radix Polygalae fallacis efficient part below respectively in detail.
One, the screening of Radix Polygalae fallacis efficient part
The present invention is guiding with the biological activity, the lipopenicillinase activity of Radix Polygalae fallacis is carried out the screening of efficient part.From Radix Polygalae fallacis (PAD) aqueous extract, isolate 5 positions (Fr.1, Fr.2, Fr.3, Fr.4, Fr.5), select for use acute mouse hyperlipemia model normal and that abdominal injection 75% yolk solution forms to transfer the screening study of fat reactive site.
Fr.1 (12mg/kg) the TC content in the hyperlipidemia model mice serum that can significantly raise, and TC content in TC content in the normal mice serum and the hyperlipidemia model Mouse Liver is not had obvious effect.
Fr.2 (44mg/kg) can significantly reduce the content of TC in the normal mouse serum, and TC content in the rising hyperlipidemia model mice serum also has certain rising effect to TC content in the high fat Mouse Liver.
Fr.3 (50mg/kg) position can significantly reduce the content of TC in the normal mouse serum, also all can significantly reduce TC content P＜0.05 in the hyperlipidemia model Mouse Liver.TC content in the high fat mice serum there is not obvious influence.
Fr.4 (50mg/kg) position can extremely significantly reduce TC content in the hyperlipidemia model Mouse Liver, also TC content in TC content and the normal mouse serum in the hyperlipidemia model Mouse Liver serum is also had certain reduction effect simultaneously.It may mechanism be the synthetic of TC in the inhibition liver, or quickens liver to the TC metabolism, drains biological utilisation.
Fr.5 (4.8mg/kg) can significantly reduce TC content P＜0.05 in the hyperlipidemia model Mouse Liver, but can raise to TC content in the hyperlipidemia model mice serum.And TC content in the normal mouse blood is not had obvious effect.
PAD transfers fat mechanism of action more complicated, and each position may be to work and influence each other by different accent fat approach.Wherein the Fr.4 position is the main efficient part of PAD regulating blood fat.
Experiment purpose: utilize efficient part normal and the acute mouse hyperlipemia model screening PAD regulating blood fat that abdominal injection 75% yolk solution forms, study each position of examination PAD and transfer fat effect, provide experimental basis for developing two kind new medicines and further furtheing investigate.
Be subjected to the reagent thing:
Radix Polygalae fallacis aqueous extract (being called for short PAD) and extract part (Fr.1, Fr.2, Fr.3, Fr.4, Fr.5): China Medicine University of the unit of providing Chinese medicine compound prescription research department, lot number 20010805, compound method is in distilled water with each medicine dissolution, be mixed with required concentration, mouse ig 0.1ml/10g, rat ig1ml/100g.
Xuezhikang (being called for short XZK): Peking University of the unit of providing dimension letter bio tech ltd, lot number 20010203, specification is the 2g/ capsule.
Total cholesterol (TC) test kit: Shanghai Rong Sheng company of the unit of providing, lot number 20011103.
The Kunming mouse random packet.Total cholesterol (TC) test kit specification: 100ml/ box
Experimental animal: Kunming mouse, male, body weight 18-22g is provided by Green Dragon mountain feedlot.
The preparation technology of Radix Polygalae fallacis aqueous extract (being called for short PAD) and extract part (Fr.1, Fr.2, Fr.3, Fr.4, Fr.5)
Modeling method and TC measure: successive administration 5d, normal group and model group are given equivalent distilled water respectively, fasting 20hr after the 5d administration, get blood with kapillary through eye socket, place 1hr down at 4 ℃, the centrifugal 15min of 3000rpm measures TC content with the serum sucking-off more then, and the examination medicine is to the effect of normal mouse.7d continues administration or water, and 9d plays administration or water behind the continuous fasting 16hr, and behind the 2hr, the freshly prepared 75% yolk solution 0.5ml/ of abdominal injection only causes the mouse hyperlipemia model, gets blood with kapillary through eye socket in the 20hr after the modeling, survey TC content.Then mouse is taken off cervical vertebra execution and get liver,, add extract (ethanol: 2ml acetone=1: 1), homogenate in homogenizer with left lobe of liver part (200mg).Homogenate is put centrifugal (3000rpm) 15min behind 4 ℃ of following 12hr of refrigerator, gets supernatant liquor, to be measured (translating H.G: Wo Geer referring to: Du Guanhua (Du GH) compiles pharmacological experiment guide-new drug and find and the scientific and technological 2001.785-787. of press of pharmacological evaluation [M]).
Grouping and dosage: get 90 male mice in kunming, standard body weight is divided into 10 groups at random.Normal group, model group, positive controls (XZK 180mg/kg), aqueous extract group (733.5mg/kg), Fr.1 position group (12mg/kg), Fr.2 position group (44mg/kg), Fr.3 position group (50mg/kg), Fr.4 position group (50mg/kg), Fr.5 position group (4.8mg/kg).Experimentize by 1..
Influence to TC content in the normal mice serum: all can reduce TC content in the normal mouse serum by table 1. visible Fr.2, Fr.3, Fr.4 position.
Table 1. medicine is to the influence (X ± SD n=10) of TC content in the normal mice serum
Group dosage Content of TC in serum velocity of variation %
(mg/kg) (mg/ml)
Normal group 0.9193 ± 0.1404
XZK organizes 180.0 0.8813 ± 0.0580-4.13
Aqueous extract group 733.5 0.9295 ± 0.1356 1.11
Fr.1 position group 12.0 0.8980 ± 0.9012-2.32
Fr.2 position group 44.0 0.7708 ± 0.1239
The Δ Δ-16.15
Fr.3 position group 50.0 0.7949 ± 0.05880
The Δ Δ-13.53
Fr.4 position group 50.0 0.7935 ± 0.1792
The Δ Δ-13.68
Fr.5 position group 4.8 0.9140 ± 0.2632-0.58
ΔP＜0.05,
The Δ ΔP＜0.01VS normal group
Influence to TC content in the high fat mice serum: the visible mouse hyperlipidemia model modeling success of table 2. (p＜0.01).XZK, Fr.4 position can reduce TC content, and the Fr.3 part also has the trend of certain reduction TC content.Table 2. medicine is to influence (X ± SD n=10) the group dosage Content of TC in serum velocity of variation % of TC content in the hyperlipidemia model mice serum
(mg/kg) (mg/ml) normal group 1.2762 ± 0.02508 138.46 model group 3.0432 ± 0.01284
The Δ ΔXZK organizes 180 2.4092 ± 0.8468
*-20.83 aqueous extract groups 733.5 1.7801 ± 0.1883
*Group 50 2.4454 ± 0.9406-19.64Fr.4 position ,-41.51Fr.1 position group 12 3.1239 ± 0.8337 2.65Fr.2 position group, 44 3.1161 ± 0.5802 2.40Fr.3 position group 50 2.1039 ± 0.6332
*-30.86Fr.5 position group 4.8 3.1143 ± 0.8352 2.34
ΔP＜0.05,
The Δ ΔP＜0.01 VS normal group,
*P＜0.05,
*P＜0.01 VS model group table 3. medicine is to influence (X ± SD n=10) the group dosage Content of TC in serum velocity of variation % of TC content in the hyperlipidemia model Mouse Liver
(mg/kg) (mg/mg) normal group 0.005156 ± 0.000706 model group 0.006052 ± 0.000582
The Δ Δ17.38XZK organize 180 0.005354 ± 0.000511
*Group 12 0.005910 ± 0.000476-2.35Fr.2 position ,-11.53 aqueous extract groups 733.5 0.005794 ± 0.000552-4.26Fr.1 position group 44 0.006488 ± 0.000506 7.20Fr.3 position group 50 0.005368 ± 0.000709
*-11.30Fr.4 position group 50 0.005309 ± 0.000624
*-12.28Fr.5 position group 4.8 0.005117 ± 0.000568
*-15.45
ΔP＜0.05,
The Δ ΔP＜0.01 VS normal group,
*P＜0.05,
*P＜0.01 VS model group
Influence to TC content in the hyperlipidemia model Mouse Liver: by TC in the visible chmice acute hyperlipidemia model liver of table 3. significantly raise (P＜0.05).XZK can significantly reduce content in the liver (P＜0.05); Fr.3, Fr.4, Fr.5 also all can significantly reduce TC content (P＜0.05).Decocting liquid has certain reduction effect (P＜0.05).
Experimental result (seeing Table 4.) shows: PAD transfers fat mechanism of action more complicated, may work and influence each other by different accent fat approach in each position.Wherein the Fr.4 position may be the main efficient part of PAD regulating blood fat.
Fr.4 (50mg/kg) position can extremely significantly reduce TC content in the hyperlipidemia model Mouse Liver, also TC content in TC content and the normal mouse serum in the hyperlipidemia model Mouse Liver serum is also had certain reduction effect simultaneously.It may mechanism be the synthetic of TC in the inhibition liver, or quickens liver to the TC metabolism, drains biological utilisation.
Each position of table 4.PAD is to the high fat mouse of interpretation of result group normal mouse of the influence of TC content
In the serum in the content serum of TC in the TC content liver TC content XZK without obvious effect significantly reduce significantly reduce decocting liquid without obvious effect extremely significantly reduces the Fr1 position without obvious effect necessarily the rising effect without obvious effect Fr.2 position significantly reduce the certain rising effect of certain rising effect Fr.3 position extremely significantly reduce without obvious effect significantly reduce the Fr.4 position reduce extremely significantly reduce remarkable reduction Fr.5 position without obvious effect necessarily the rising effect significantly reduce
Two, total saponins Study on extraction
1, behind the water extraction, merge three times aqueous extract, filter or the centrifugal impurity of removing, cross D101 (HP20, AB8) macroporous resin, applied sample amount is medicinal material (weight): macroporous resin (volume) is 1.5: 1, treat that resin fully adsorbs saponin(e after, wash with aquae destillata, remove water-soluble impurity, wash with 35-40% ethanol again, further remove impurity, continue and take off with the 60-70% washing with alcohol, collect 60-70% ethanol position, with Tenuifolin in the Radix Polygalae fallacis is reference substance, measures total saponin content, and the Radix Polygalae fallacis total saponin content reaches more than 50%.
2, once extracted with the alcoholic solution of different concns, alcohol extract and water extract carry out the pharmacodynamic observation and the comparison of effect for reducing fat with the hyperlipemia model mouse, and the result shows both pharmacodynamics no significant differences.
3, alcohol extract is crossed macroporous resin,, superfine settling is arranged on macroporous resin, cause extracting solution not passed through smoothly and absorption, so adopted extraction process by water to extract the Radix Polygalae fallacis total saponins afterwards because the fat-soluble component that alcohol extract proposes is more.
4, in extraction process by water, also carried out the concentrating of extracting solution after, the test of crossing macroporous resin, the result shows that the water extract is gone up macroporous resin after concentrating again, the yield of total saponins and content is obviously decline all:
1) 150kg that feeds intake extracts by best extraction process by water, and the water extract is concentrated into medicinal material (weight): extracting solution (volume) 1: 2, and concentrated solution is crossed macroporous resin, and through above-mentioned separation purifying technique, the total saponins yield is 0.46%;
2) 150kg that feeds intake, best extraction process by water extracts, and the water extract is concentrated into medicinal material (weight): extracting solution (volume) 1: 2, concentrated solution is spray dried to medicinal powder, and the water-soluble back of medicinal powder is after macroporous resin, and through above-mentioned separation purifying technique, total total saponins yield is 0.5%
3) same medicinal material, by (being preparation method of the present invention) described extraction under aforementioned 1, separate, the total saponins yield is 2-2.3%, may be because due to the Radix Polygalae fallacis saponin(e acidity after deliberation, saponin component be constantly destroyed and caused the decline of saponin(e yield and content in the heating concentration process.
Embodiment
Example 1: the preparation of Radix Polygalae fallacis total saponins
Get Radix Polygalae fallacis 150kg, be ground into meal, soaked 3 hours, adopt the deionized water of 10 times of medicinal material weight to decoct three times, extraction time was respectively 1.5 hours.Merge three times aqueous extract, filter or the centrifugal impurity of removing, cross the HP20 macroporous resin, applied sample amount is medicinal material (weight): macroporous resin (volume) is 2: 1, after treating that resin fully adsorbs saponin(e, wash with the 500L aquae destillata, remove water-soluble impurity, wash with 400L 40% ethanol again, further remove impurity, continue and take off with 500L 65% washing with alcohol, collect 65% ethanol position, vacuum reclaims ethanol, the vacuum-drying extract, getting Radix Polygalae fallacis total saponins 3.6kg (yield 2.3%) is reference substance with Tenuifolin in the Radix Polygalae fallacis, the colorimetric method for determining total saponin content, and the Radix Polygalae fallacis total saponin content reaches 50%.(the total saponin content measuring method is referring to Liu Youping, Wan Deguang, Liu Tao etc.; The content " Chengdu University of Traditional Chinese Medicine's journal " 2000,23 (1) of the different places of production of spectrophotometry Radix Polygalae total saponins: 26-28, down together).
Example 2: the preparation of Radix Polygalae fallacis total saponins
Get Radix Polygalae fallacis 150kg, be ground into meal, soaked 3 hours, extract 3 times, three times amount of water is respectively 10,8,6 times of amounts, and three times extraction time is respectively 1.5,1.5,1 hour.
Merge three times aqueous extract, filter or the centrifugal impurity of removing, cross the D101 macroporous resin, applied sample amount is medicinal material (weight): macroporous resin (volume) is 1.5: 1, treat that resin fully adsorbs saponin(e after, wash with the 400L aquae destillata, removing water-soluble impurity (measures with fehling reagent, to the sugar-free reaction), wash with 300L 40% ethanol again, further remove impurity, continue and take off with 400 65% washing with alcohol, collect 65% ethanol position, vacuum reclaims ethanol, vacuum-drying extract, get Radix Polygalae fallacis total saponins 3kg (yield 2%), with Tenuifolin in the Radix Polygalae fallacis is reference substance, the colorimetric method for determining total saponin content, and the Radix Polygalae fallacis total saponin content reaches 60%.
Example 2: the accent fat effect at total saponins position
Instrument and reagent: Beckman DU640 nucleic acid protein analyser, Zocor (SJZ) is provided by Hangzhou Mo Shadong; TC, TG, LDL-C and HDL-C test kit are to give birth to company's product in Beijing.MDA and SOD test kit are that company's product is built up in Nanjing.Implement the Radix Polygalae fallacis total saponins (Total Saponins of PAD is called for short PTS) of preparation in 1, face and use preceding dilute with water.
The SD male rat, 180g-220g is provided by Green Dragon mountain feedlot, animal conformity certification number: SCXK (Soviet Union) 2001-0010.
Experimental technique (referring to: Tong Jiming (Tong XM) Liu Yuling (Liu YL) Fu Jingchun (Fu JC). the Caulis et Folium Scutellariae total flavones is transferred blood fat research [J]. herbal medicine (Chin Trad and Herb Drugs), 2000.31 (3): 196-199; Cai Xiucheng (CaiXC) Guo Ying (Guo Y) Yan Yan (Yan Y). borage oil is to the influence [J] of lipid metabolism and lipid peroxidation. Chinese Pharmacological circular (Chin Pharm Bull) 1996,12 (6): 551-553; Du Guanhua (Du GH) translates H.G: Wo Geer and compiles pharmacological experiment guide-new drug discovery and scientific and technological 2001.785-787 of press of pharmacological evaluation [M]; . the clinical blood fat of Zhao Shuiping (Zhao SP) is learned [M] Hunan science tech publishing house 1997,357)
High lipid food prescription: 1.5% cholesterol, 0.5% bovine bile, 0.2% Thyreostat I, 10% lard, 87.8% basal feed.
Modeling method: normal one week of forage feed of male SD rat, measure serum TC content, divide into groups according to TC content and body weight: normal control group, model control group, positive controls (Zocor 10mg/kg SJZ), PTS low dose group (25mg/kg), middle dosage group (50mg/kg), high dose group (100mg/kg).All the other are respectively organized rat and give high lipid food modeling each administration group successive administration simultaneously continuously except that the normal control group during preventive administration, use normal feed behind the 21d instead, and continue administration 14d, and normal control group, model control group are given equivalent distilled water respectively.All the other are respectively organized rat and give the high lipid food modeling continuously except that the normal control group during therapeutic administration, and stop modeling behind the 21d and use normal feed instead, each administration group successive administration 14d of while, normal control group and model control group are given equivalent distilled water respectively.
Preventive administration: 60 rats are divided into 6 groups every group 10 at random.Press modeling and administration under the 2.2. item.Respectively at 21d, 35d, continuous fasting 12hr, ether is slightly anaesthetized after eye socket is got blood, places 1hr down at 4 ℃, and the centrifugal 15min of 3500rpm gets determination of serum TC, TG and MDA content then.The therapeutic administration: 48 rats are divided into 6 groups every group 8 at random.Press modeling and administration under the 2.2. item.In the continuous fasting 12h of 35d rat, ether is slightly anaesthetized after eye socket is got blood, places 1h down at 4 ℃, and the centrifugal 15min of 3500rpm gets determination of serum TC, TG, LDL-C, HDL-C and MDA content and SOD activity then.Then rat is taken off cervical vertebra execution and get liver, get left lobe of liver leading edge portion (about 200mg) and add extract (ethanol: 2ml homogenate acetone=1: 1).The centrifugal 15min of 3500rpm behind 4 ℃ of following placement 12h of homogenate, get supernatant liquor, mensuration TC and TG content (referring to: 12. Cai Xiu become (Cai XC) Guo Ying (Guo Y) Yan Yan (Yan Y). and borage oil is to the influence [J] of lipid metabolism and lipid peroxidation. Chinese Pharmacological circular (Chin Pharm Bull) 1996,12 (6): 551-553).
Statistical procedures: all data are all represented with X ± S form, adopt t check carrying out statistical analysis.
Preventative to the influence of PTS to TC, TG, MDA in the serum: by table 5, table 6 as seen, TC, TG and all significantly risings of MDA content in the model group rat blood serum behind high lipid food hello the 21d.PTS has certain reduction trend to TC, TG and MDA content, and especially high dosage has significant difference.Stop modeling continuing administration after 14 days model group TC, TG and MDA content all descend to some extent, have significant difference but compare with normal group.Compare PAD total saponins high dosage with model group and still can reduce TC in the serum, TG and MDA content significantly.Above result shows that PTS has certain prophylactic effect.
The administration of table 5 total saponins after 21 days to effect (X ± S, n=10) group dosage (mg/kg) TC (mmol/l) TG (mmol/l) MDA (mmol/l) normal group-2.11 ± 0.70 0.26 ± 0.064 4.78 ± 0.68 control group-12.42 ± 3.30 of TC in the serum and TG
The Δ Δ0.53 ± 0.22
The Δ Δ6.53 ± 1.52
The Δ ΔSJZ 10 11.36 ± 2.80 0.36 ± 0.15 5.51 ± 1.30PTS 25 11.51 ± 3.07 0.36 ± 0.11 5.88 ± 1.13
50 10.87±3.54 0.34±0.087
* 5.68±1.05
100 9.45±3.01
* 0.32±0.071
** 5.40±0.56
*
ΔP＜0.01VS normal group;
*P＜0.05,
*P＜0.01VS control group
The administration of table 6 total saponins after 35 days to the effect of TC in the serum and TG (X ± S, n=10)
Dosage group TC (mmol/l) TG (mmol/l) MDA (mmol/l)
(mg/kg) normal group-1.85 ± 0.25 0.22 ± 0.054 4.55 ± 0.44 control group-2.61 ± 0.48
The Δ Δ0.33 ± 0.065
Δ5.33 ± 0.86
ΔSJZ 10 2.21 ± 0.35
*0.25 ± 0.038
*4.45 ± 0.33
*PTS 25 2.43 ± 0.31 0.31 ± 0.062
*4.74 ± 0.48
50 2.24±0.30 0.31±0.11 4.68±0.40
*
100 2.21 ± 0.28
*0.25 ± 0.049
*4.53 ± 0.42
* ΔP＜0.05,
The Δ ΔP＜0.01 VS normal group;
*P＜0.05,
*P＜0.01VS control group
Therapeutic is to the influence of PTS to lipid and MDA, SOD: by table 7 as seen: high lipid food feed change behind the rat 21d feed behind the normal feed 14d TC, TG in the model group serum, LDL-C content significantly raises and HDL-C significantly reduces.But TC, TG are starkly lower than model group mutually with LDL-C content in the PTS group rat blood serum, and HDL-C significantly raises and certain dosage correlation is arranged.The result shows that PTS has regulating effect to the blood fat of hyperlipidemia rats.
Table 7 total saponins is to influence (X ± S, n=8) group dosage (mg/kg) TC (mmol/l) TG (mmol/l) LDL-C (mmol/l) HDL-C (mmol/l) normal group-1.74 ± 0.23 0.46 ± 0.13 0.63 ± 0.26 0.70 ± 0.089 control group-3.50 ± 0.62 of blood fat
The Δ Δ0.58 ± 0.084
Δ1.85 ± 0.57
The Δ Δ0.57 ± 0.063
The Δ ΔSJZ 10 2.85 ± 0.48
*0.48 ± 0.085
*1.28 ± 0.32
*0.66 ± 0.12
*PTS 25 3.07 ± 0.67 0.52 ± 0.084 1.41 ± 0.41 0.61 ± 0.12
50 2.94±0.33
* 0.50±0.13 1.30±0.24
* 0.67±0.13
*
100 2.75±0.42
** 0.47±0.099
* 1.14±0.37
** 0.69±0.098
**
ΔP＜0.05,
The Δ ΔP＜0.01 VS normal group;
*P＜0.05,
*P＜0.01 VS control group
Influence to lipid content in the liver: by table 8 as seen, TC and TG content are all apparently higher than normal group in the model control group liver, and PTS group TC content is starkly lower than model group, especially PTS high dose group (P＜0.05).And PTS does not have obvious influence to liver TG content.The result shows that PTS is similar to SJZ to the effect of liver lipid, can reduce TC content and TG is not had obvious effect.
Table 8 total saponins is to influence (X ± S, n=8) group dosage (mg/kg) TC (μ mol/mg) TG (μ mol/mg) normal group-2.22 ± 0.12 3.92 ± 1.43 control group-3.74 ± 0.54 of lipid in the liver
The Δ Δ7.11 ± 0.84
The Δ ΔSJZ 10 3.04 ± 0.39
*6.93 ± 0.60PTS 25 3.58 ± 0.13 6.80 ± 0.89
50 3.23±0.53 7.08±0.62
100 3.14±0.55
* 7.15±0.72
ΔP＜0.01 VS normal group;
*P＜0.05,
*P＜0.01 VS control group
PTS is to the influence of MDA in the serum and SOD: by table 9 as seen: compare in the model group rat blood serum MDA content P＜0.01 that significantly raises with normal group, SOD is active significantly to be reduced.Each administration group and model group relatively, SJZ and PTS can significantly reduce serum MDA, and the PTS activity of SOD in serum that can significantly raise, and certain dosage correlation is arranged.The result shows that PTS has certain resistance of oxidation, may be to work by lipid content in SOD activity improving and the reduction serum.
Table 9 total saponins to MDA in the serum and SOD influence m (X ± S, n=8)
Dosage MDA SOD group
(mg/kg) (mmol/l) (NU/ml) normal group-9.65 ± 0.58 300.77 ± 26.95 control group-12.79 ± 0.89
The Δ Δ266.97 ± 19.70
The Δ ΔSJZ 10 10.66 ± 0.89
*283.35 ± 24.61PTS 25 11.33 ± 1.37
*296.06 ± 23.31
*
50 10.66±1.26
** 297.24±26.99
*
100 10.51 ± 1.20
*300.67 ± 20.54
* The Δ ΔP＜0.01 VS normal group,
*P＜0.05
*P＜0.01 VS control group
Claims (10)
1, a kind of Radix Polygalae fallacis total saponins with effect for reducing fat is characterized in that: preparation as follows,
With the Radix Polygalae fallacis aqueous extract, the macroporous resin column of last D101, HP20 or AB8 model, water and aqueous ethanol gradient elution are collected the 60-70% ethanol eluate, get the Radix Polygalae fallacis total saponins.
2, a kind of preparation method with Radix Polygalae fallacis total saponins of effect for reducing fat, it is characterized in that: with the Radix Polygalae fallacis aqueous extract, the macroporous resin column of last D101, HP20 or AB8 model, water and aqueous ethanol gradient elution, collect the 60-70% ethanol eluate, get the Radix Polygalae fallacis total saponins.
3, the preparation method of Radix Polygalae fallacis total saponins according to claim 2, it is characterized in that: with the Radix Polygalae fallacis aqueous extract, the macroporous resin column of last D101 or AB8 model, respectively behind water and the 30-40% ethanol elution, collect the 60-70% ethanol eluate, get the Radix Polygalae fallacis total saponins.
4, the preparation method of Radix Polygalae fallacis total saponins according to claim 2 is characterized in that: with the Radix Polygalae fallacis aqueous extract, without concentrating, directly go up resin column.
5, the preparation method of Radix Polygalae fallacis total saponins according to claim 2 is characterized in that: when separating with resin column, applied sample amount is about by medicinal material weight: macroporous resin volume ratio 2～1: 1.
6, the preparation method of Radix Polygalae fallacis total saponins according to claim 5 is characterized in that: when separating with resin column, applied sample amount is about by medicinal material weight: macroporous resin volume ratio 1.5: 1.
7, the preparation method of Radix Polygalae fallacis total saponins according to claim 2 is characterized in that: collect 65% ethanol eluate.
8, the preparation method of Radix Polygalae fallacis total saponins according to claim 6 is characterized in that: get the Radix Polygalae fallacis meal, soaked 3 hours, extract 3 times, three times amount of water is respectively 10,8,6 times of amounts, three times extraction time is respectively 1.5,1.5,1 hour; With the Radix Polygalae fallacis aqueous extract, directly go up the D101 macroporous resin column, wash resin column earlier with water, wash with 40% ethanol again, continue and use 65% ethanol elution, collect 65% ethanol position, after the solvent recovered under vacuum, get the Radix Polygalae fallacis total saponins.
9, the pharmaceutical composition that is used for lipopenicillinase wherein contains each the Radix Polygalae fallacis total saponins and the pharmaceutically acceptable carrier of claim 1-8 for the treatment of significant quantity.
10, any one Radix Polygalae fallacis total saponins among the claim 1-8, the application in the preparation fat-reducing medicament.
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102911243A (en) * | 2011-08-02 | 2013-02-06 | 苏州宝泽堂医药科技有限公司 | Preparation method of high-purity reinioside C |
| CN102908404A (en) * | 2011-08-02 | 2013-02-06 | 苏州宝泽堂医药科技有限公司 | Method for extracting total saponin from polygala aureocauda Dunn |
| CN112043749A (en) * | 2020-08-17 | 2020-12-08 | 武汉自在生物科技有限公司 | Application of radix Polygalae Fallacis extract in preparing medicine for treating ulcerative colitis |
| CN112168878A (en) * | 2020-10-20 | 2021-01-05 | 广西壮族自治区中国科学院广西植物研究所 | Radix polygalae fallax hemsl-water lotus lipid-lowering composition and preparation method thereof |
| CN114209736A (en) * | 2022-01-19 | 2022-03-22 | 广西壮族自治区中国科学院广西植物研究所 | Application of total saponins of Polygala fallax Hemsl |
-
2003
- 2003-01-29 CN CNB03112786XA patent/CN1186351C/en not_active Expired - Fee Related
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102911243A (en) * | 2011-08-02 | 2013-02-06 | 苏州宝泽堂医药科技有限公司 | Preparation method of high-purity reinioside C |
| CN102908404A (en) * | 2011-08-02 | 2013-02-06 | 苏州宝泽堂医药科技有限公司 | Method for extracting total saponin from polygala aureocauda Dunn |
| CN112043749A (en) * | 2020-08-17 | 2020-12-08 | 武汉自在生物科技有限公司 | Application of radix Polygalae Fallacis extract in preparing medicine for treating ulcerative colitis |
| CN112168878A (en) * | 2020-10-20 | 2021-01-05 | 广西壮族自治区中国科学院广西植物研究所 | Radix polygalae fallax hemsl-water lotus lipid-lowering composition and preparation method thereof |
| CN112168878B (en) * | 2020-10-20 | 2022-04-01 | 广西壮族自治区中国科学院广西植物研究所 | Radix polygalae fallax hemsl-water lotus lipid-lowering composition and preparation method thereof |
| CN114209736A (en) * | 2022-01-19 | 2022-03-22 | 广西壮族自治区中国科学院广西植物研究所 | Application of total saponins of Polygala fallax Hemsl |
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|---|---|
| CN1186351C (en) | 2005-01-26 |
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