CN101816719B - Peach blossom or peach leaf general flavone and application thereof in preparing medicines or health care products for lowering blood sugar and fat and preventing and/or treating diabetes and complications - Google Patents
Peach blossom or peach leaf general flavone and application thereof in preparing medicines or health care products for lowering blood sugar and fat and preventing and/or treating diabetes and complications Download PDFInfo
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Abstract
The invention relates to peach blossom or peach leaf general flavone, a peach blossom or peach leaf original extract, a pharmaceutical composition containing a peach blossom or peach leaf original extract and/or peach blossom or peach leaf general flavone, and application thereof in preparing medicines or health care products for lowering blood sugar and fat and preventing and/or treating diabetes and complications thereof. In the invention, the peach blossom or peach leaf original extract is obtained by taking a rosaceous plant-peach blossom or peach leaves as raw materials and then extracting with water or alcohol with the carbon number of 1-6; and the peach blossom or peach leaf general flavone is obtained by utilizing macroporous resin to carrying out absorbing, separating and purifying on the original extract. The peach blossom or peach leaf original extract, the peach blossom or peach leaf general flavone and the pharmaceutical composition containing the peach blossom or peach leaf original extract and/or the peach blossom or peach leaf general flavone have good curative effect, few side effects and low cost in preventing and treating diabetes, especially Type II diabetes and complications thereof.
Description
Technical field
The present invention relates to Flos persicae or Folium Persicae total flavones, Flos persicae or Folium Persicae primary extract, and they are being prepared blood sugar lowering blood fat, are preventing and/or treating the purposes in diabetes and complication medicine or health product.
Background technology
Diabetes (diabetes) are to act on that body causes hypoinsulinism, insulin resistant etc. and a series of metabolism disorder syndromes such as the sugar that causes, protein, fat, power and water Xie Zhi by various virulence factors such as inherited genetic factors, immunologic function disorder, infected by microbes and toxin thereof, free radical toxin, Nervous and Mental Factors, take clinically hyperglycemia as main feature.
Diabetes are mainly divided type 1 diabetes and type 2 diabetes mellitus, and wherein, in diabetics, the shared ratio of type 2 diabetes mellitus is about 95%, and type 2 diabetes mellitus is along with the change of growth in the living standard and life style, more and more occurred frequently and rejuvenation.Because blood glucose continues to raise, cause that general metabolism is disorderly, can invisiblely cause the chronic complicating diseases of many tissues such as heart, blood vessel, kidney, nerve and organ, so that finally because of nonfunction threat to life.
In prior art, the medicine that is used for the treatment of diabetes is mainly Western medicine and some Chinese medicine and western medicine compound preparations.Although these medicines can effectively reduce blood glucose, because lasting use can cause the infringement of medicine to body, thereby its use is strictly limited.The Chinese medicine preparation that at present also occurs being used for the treatment of diabetes, they are proved to be has certain effect to the adjusting of diabetes, however Chinese medicine ingredients is complicated, and each component drug effect is indefinite, and quality is wayward, is unfavorable for being prepared into pharmaceutical preparation.In addition, the effect of existing diabetes medicament only limits to reduce blood glucose, cannot reduce and delay the development of diabetes chronic pathological changes.
Summary of the invention
Technical problem to be solved by this invention is to provide a kind of Flos persicae or Folium Persicae total flavones in order to overcome the deficiencies in the prior art, this total flavonoids substance and the pharmaceutical composition that comprises this total flavonoids substance not only can effectively reduce blood pressure and blood lipoid, and can reduce and delay the development of diabetes chronic pathological changes.
The present invention also will provide a kind of Flos persicae or Folium Persicae primary extract simultaneously, and it can be used in and prevents and/or treats diabetes, reaches the object of the development that reduces blood pressure and blood lipoid and delaying chronic pathological changes.
The present invention also will provide the pharmaceutical composition that has comprised above-mentioned Flos persicae or Folium Persicae total flavones or Flos persicae or Folium Persicae primary extract in addition, this pharmaceutical composition can be used as medicine and is used for the treatment of diabetes or blood sugar lowering blood fat, also can be used as health product for the generation of prevent diabetes.
For solving above technical problem, a kind of technical scheme that the present invention takes is:
Flos persicae or a Folium Persicae total flavones, it prepares by the following method:
(1), to take Flos persicae or Folium Persicae be raw material, take the alcohol of water or carbon number 1～6 as extracting solvent, at the temperature of 10 ℃～100 ℃, extracts, and obtains the extracting solution of Flos persicae/leaf;
(2), make the extracting solution of described Flos persicae/leaf carry out separation by macroporous adsorbent resin and obtain Flos persicae or Folium Persicae total flavones.
According to the present invention, the described Flos persicae as raw material or Folium Persicae can be Flos persicae or the Folium Persicae of the common Fructus Persicae of Rosaceae Prunus Fructus Persicae Subgenus, Xinjiang Fructus Persicae, Prunus davidiana or almond.The described alcohol as extracting solvent is preferably one or more the mixture being selected from methanol, ethanol, n-butyl alcohol, isobutanol, and the mass percent concentration of alcohol can be 5wt%～95wt%.Preferably, make to be extracted at 45 ℃～100 ℃ temperature extracting solvent and carry out.
According to the present invention, in step (2) before, the extracting solution that step (1) is obtained carries out remove impurity processing.A concrete aspect of processing according to remove impurity, its refer to by flocculating agent for example chitin join in extracting solution and carry out flocculation sediment, disgorging obtains the process of the solution of clarification afterwards.
According to further embodiment of the present invention: the detailed process of step (2) is: after described extracting solution is adsorbed by macroporous adsorbent resin, water, 5%～90% methanol or ethanol carry out eluting successively, Fractional Collections water and alcohol eluate, vacuum drying obtains Flos persicae or Folium Persicae total flavones.Wherein, described macroporous adsorbent resin can be 101 types, AB-8 type, D101 type, DM301 type, NKA-9 type, HPD100 type or HPD200 type macroporous adsorbent resin, preferably DM301 type macroporous adsorbent resin.In addition, one of ordinary skill in the art should be appreciated that for separation more easily carries out, and extracting solution can be carried out to concentration to a certain degree.
Another technical scheme that the present invention takes is: a kind of pharmaceutical composition for blood sugar lowering blood fat and/or prevention and treatment diabetes and complication thereof, at least comprises above-mentioned Flos persicae or Folium Persicae total flavones in its effective ingredient.Specifically, described compositions is various types of oral agents or injection or the compound preparation that Flos persicae or Folium Persicae total flavones and the acceptable pharmaceutical carrier of pharmacy are made.Wherein, described carrier refer to pharmaceutical field routine meet that preparation requires and any pharmaceutical carrier of selecting comprises that diluent is as starch, dextrin, microcrystalline Cellulose etc.; Wetting agent is as water, glycerol, polyvinylpyrrolidone etc.; Lubricant is as magnesium stearate, micropowder silica gel etc.; And other additive is as tetrafluoroethane, dimethyl ether etc.Described oral agents can be capsule, tablet, pill, granule, liquid preparation, slow releasing agent etc.
Pharmaceutical composition according to the present invention, its effective ingredient can also comprise that other is used for the treatment of the ingredient of diabetes and complication thereof, as sulfonylureas glimepiride or biguanides metformin or glitazone medicine pioglitazone or aldose reductase inhibitor epalrestat etc.; Described effective ingredient can also comprise Radix Puerariae and other Chinese crude drug primary extract.So, never same-action link, different mechanism of action come Synergistic treatment diabetes, diabetic complication and relevant metabolic disease.
The another technical scheme that the present invention takes is: a kind of Flos persicae or Folium Persicae primary extract, and it is that to take Flos persicae or Folium Persicae be raw material, and the alcohol of water or carbon number 1～6 of take is to extract solvent, and at the temperature of 10 ℃～100 ℃, preferably 45 ℃～100 ℃ are extracted acquisition.
Wherein, described extraction solvent is preferably one or more the mixture in methanol, ethanol, n-butyl alcohol, isobutanol, and the mass percent concentration of alcohol can be 5wt%～95wt%.Preferably, make to be extracted under the reflux temperature that extracts solvent and carry out.
One of ordinary skill in the art should be appreciated that when take water when extracting solvent, and primary extract both can liquid form, also can be used with solid form; When take alcohol when extracting solvent, need solvent to remove.
Above-mentioned Flos persicae or Folium Persicae primary extract are proved to be able to effectively reduce blood pressure and blood lipoid, thereby it can be used as the health product of prevent diabetes or is used as the effective ingredient for the treatment of diabetes medicament.For this reason, the pharmaceutical composition that the present invention also provides a kind of effective ingredient at least to comprise described Flos persicae or Folium Persicae primary extract, it is the acceptable various dosage forms of pharmacy that described primary extract and pharmaceutically acceptable carrier are made, such as tablet, capsule, injection etc.
As hereinbefore, also can by Flos persicae or Folium Persicae primary extract and other be to preventing and/or treating the composite use of ingredient of diabetes.
Experiment showed, Flos persicae of the present invention or Folium Persicae total flavones, Flos persicae or Folium Persicae primary extract, the pharmaceutical composition that comprises Flos persicae or Folium Persicae total flavones and/or Flos persicae or Folium Persicae primary extract is used for the treatment of diabetes and has particularly obtained good effect during type 2 diabetes mellitus.Dosage when one of ordinary skill in the art should be appreciated that treatment depends on character and the order of severity that comprises relevant disease, patient's age, body weight and individual reaction, and route of administration and administration number of times are at interior many factors.Dosed administration can be single dose form or multiple dose form.For concrete individuality, dosage and application method depend on symptom and patient's s own situation, and can according to concrete needs, be adjusted by doctor.
According to the present invention, adult's oral dose/day (in crude drug) of Flos persicae or Folium Persicae primary extract is about 30～500mg/kg, preferably 50～150mg/kg.When content is not less than 30%, dosing/day Coming-of-Age Day of Flos persicae or Folium Persicae total flavones is about 1mg～100mg/kg, and preferably 5mg～20mg/kg, divides 3～4 administrations.As when the intravenously administrable, Coming-of-Age Day consumption within one day, be about 0.2mg～30mg/kg, preferred 2mg～5mg/kg.
Due to the enforcement of above technical scheme, the present invention compared with prior art tool has the following advantages:
According to the test of pesticide effectiveness, Flos persicae/total flavones of the present invention and Flos persicae or Folium Persicae primary extract all can effectively reduce blood pressure and blood lipoid and delay the development of diabetes chronic pathological changes, and safety of the present invention is better.In addition, the present invention be take Flos persicae or Folium Persicae and is raw material, with low cost; And easily Flos persicae/total flavones and Flos persicae or Folium Persicae primary extract are mixed with to various pharmaceutical preparation.
Accompanying drawing explanation
Fig. 1 is the liquid chromatogram of reference substance mixed solution;
Fig. 2 is the liquid chromatogram of embodiment 10 samples;
Fig. 3 is the liquid chromatograms of embodiment 10 samples after further separated (eluting solvent the is 35% ethanol) purification of 100 order polyamides;
Fig. 4 is the liquid chromatograms of embodiment 10 samples after further separated (eluting solvent the is 50% ethanol) purification of 100 order polyamides.
The specific embodiment
Flos persicae (Prunus persica Batch) is the flower (peach blossom) of rosaceous plant Fructus Persicae Prunus persica (L.) Batsch or Prunus davidiana P.davidiana (Carr.) Franch..< < a thousand pieces of gold prescription > > carries: " eel-like figure body is drunk in Flos persicae three strains on an empty stomach ".Flos persicae nature and flavor are sweet, flat nontoxic, can help digestion pleasant, and phlegm retention, stagnant, the skin protection of our single reducing weight and beautifying features, is fabulous cosmetics.< < Prescriptions for Universal Relief > > says when introducing peach blossom wine function: adopt fresh Flos persicae March three, with first-class soaking in Chinese liquor, clothes, can remove sick beneficial face for a long time.Also once had peach tree, nature and flavor are bitter, flat, have and blood, QI invigorating, the function of quenching the thirst.Folium Persicae is the leaves (peach tree leaves) of rosaceous plant Fructus Persicae Prunus persica (L.) Batsch or Prunus davidiana P.davidiana (Carr.) Franch., bitter in the mouth, property is put down, return spleen kidney channel, [detailed outline] year Folium Persicae " is cured the wound cold; control wind syndrome of head, relieving bowels ", and [guiding principle grass converges and says] carried Folium Persicae and " broken married woman's blood and close abdominal mass due to blood stasis ".Core of the present invention is that to take Flos persicae or Folium Persicae be raw material, prepares its primary extract, and further by primary extract, obtains the total flavones composition with blood sugar lowering blood fat effect.
Below in conjunction with specific embodiment, the present invention is further detailed explanation, but the present invention is not limited to these embodiment.
Embodiment 1
Flos persicae primary extract according to the present embodiment, prepares as follows:
(1), get the birthday peaches dry Flos persicae of 1kg, by weight 1: 10 (flower: ratio water) is put into water and soaked half an hour, 75 ℃ of constant temperature water baths reflux 1 hour, filter, filtering residue refluxes for the second time, extracts so altogether merge extractive liquid, 3 times.
(2), in step (1) gained extracting solution, add chitin, flocculation sediment, disgorging obtains the extracting solution of clarification, 75 ℃ of concentrating under reduced pressure extracting solution, in 80 ℃ of vacuum dryings 24 hours, obtain 131.5 grams of left and right of dry primary extract, through qualitative test, show to contain in primary extract the chemical compositions such as flavonoid, organic acid, phenols, glycoside, polysaccharide, triterpene.
Embodiment 2
According to the Flos persicae primary extract of the present embodiment, take honey peach dry Flos persicae as raw material, according to the method identical with embodiment 1, extract, finally obtain primary extract 118.8g left and right, qualitative test result is with embodiment 1.
Embodiment 3
According to the Flos persicae primary extract of the present embodiment, take peento dry Flos persicae as raw material, according to the method identical with embodiment 1, extract, finally obtain primary extract 125.4g left and right, qualitative test result is with embodiment 1.
Embodiment 4
Folium Persicae primary extract according to the present embodiment, prepares as follows:
(1), get the dry Folium Persicae of birthday peaches of 1kg, by weight 1: 12 (leaf: ratio water) is put into water and soaked half an hour, 80 ℃ of constant temperature water baths reflux 1 hour, filter, filtering residue refluxes for the second time, extracts so altogether merge extractive liquid, 3 times;
(2), in step (1) gained extracting solution, add chitin, flocculation sediment, disgorging obtains the extracting solution of clarification, 75 ℃ of concentrating under reduced pressure, 80 ℃ of vacuum dryings 24 hours, obtain primary extract 173.4g left and right.
Embodiment 5
Folium Persicae primary extract according to the present embodiment, prepares as follows:
(1), get the dry Folium Persicae of honey peach of 1kg, by weight 1: 10 (flower: ratio water) is put into and extracted solvent water and soak half an hour, and 80 ℃ of constant temperature water baths reflux 1 hour, filter, and filtering residue refluxes for the second time, extracts so altogether merge extractive liquid, 3 times;
(2), in step (1) gained extracting solution, add chitin, flocculation sediment, disgorging obtains the extracting solution of clarification, 75 ℃ of concentrating under reduced pressure, 80 ℃ of vacuum dryings 24 hours, obtain primary extract 188.1g left and right.
Embodiment 6
According to the Folium Persicae primary extract of the present embodiment, the dry Folium Persicae of the peento of take is raw material, according to the method identical with embodiment 5, extracts, and finally obtains primary extract 174.8g left and right.
the effect research to type i diabetes mice due to alloxan of Flos persicae or Folium Persicae primary extract
1, test method: get clean level Male Kunming strain mice, 22-25g, fasting 12h, by 60mg/kg body weight tail vein injection alloxan solution.In the 4th day fasting 12h, survey fasting glucose >=11.0mmol/L person and be defined as diabetic mice, be divided at random model group and treatment group.Model group is pressed 20ml/kg body weight and is filled with distilled water, treatment group is divided into the Chinese birthday peaches flower water extract group (3g/kg of above-described embodiment, in raw medicinal herbs, as follows), China's birthday peaches leaf water extract groups (3.5g/kg), spend honey peach flower water extract group (3g/kg) in vain, spend honey peach leaf water extract group (3.5g/kg) in vain, Xinjiang peento flower water extract group (3g/kg), Xinjiang peento leaf water extract group (3.5g/kg) and acarbose matched group (0.1g/kg), gastric infusion every day 1 time, continuous 10 days, fasting 12h, surveys fasting blood sugar, relatively mice fasting glucose before and after administration.In administration 15 days, carry out glucosieloading test (oral glucose 2g/kg), the impact of comparative drug on diabetic mice carbohydrate tolerance due to alloxan.
2, result of the test
The results are shown in Table 1 and 2.Therefrom visible, the Flos persicae water extract of embodiment and Folium Persicae water extract all can reduce alloxan diabetes mice fasting glucose in various degree, and can obviously improve the glucose tolerance of mice.Although can effectively reduce blood glucose and perform the formal wedding ceremony to put down, it is not improved effect for glucose load.
Table 1 Flos persicae/leaf water extract is on the impact of alloxan diabetes mice fasting glucose (Mean ± SD, n=10)
Compare * P < 0.05, * * P < 0.01 with model after administration.
Table 2 Flos persicae or Folium Persicae primary extract are on the impact of alloxan diabetes glucose tolerance in mice (Mean ± SD, n=10)
Compare * P < 0.05, * * P < 0.01 with model after administration.
Embodiment 7
According to the Folium Persicae total flavones of the present embodiment, preparation by the following method:
(1), get the dry Folium Persicae of birthday peaches of 1kg, by weight 1: 12, (leaf: ratio water) is put into water and first soaked half an hour, refluxed 1 hour at 80 ℃ of constant temperature water baths, extracts altogether merge extractive liquid, 3 times;
(2) in step (1) gained extracting solution, add chitin, flocculation sediment, disgorging obtains the extracting solution of clarification, enter DM-301 macroporous resin column, carry out absorption and purification, 25%, 50%, 75%, 90% alcoholic solution of water, 2 times of post appearances carries out gradient elution successively, after eluent mixes, reclaims ethanol, through 80 ℃ of vacuum dryings, within 24 hours, obtains primary extract 48.85g left and right.Through identifying that wherein general flavone content can reach 45.32～51.64%.
Embodiment 8
According to the Folium Persicae total flavones of the present embodiment, its preparation method is substantially with embodiment 7, different, and in step (1), bath temperature is 45 ℃, finally obtains primary extract 41.32g left and right, and wherein general flavone content can reach 43.46～52.17%.
Embodiment 9
According to the Folium Persicae total flavones of the present embodiment, its preparation method is substantially with embodiment 7, and different is, in step (1), bath temperature is 75 ℃, the ethanol that extraction solvent is 45%, finally obtain primary extract 40.21g left and right, wherein general flavone content can reach 48.21～56.62%.
Embodiment 10
According to the Flos persicae total flavones of the present embodiment, preparation as follows:
(1), get the birthday peaches dry Flos persicae of 1kg, by weight the ratio of 1: 10, put into water and first soak half an hour, at 75 ℃ of constant temperature water baths, reflux 1 hour, extract altogether merge extractive liquid, 3 times;
(2), in step (1) gained extracting solution, add chitin, flocculation sediment, disgorging obtains the extracting solution of clarification, enter DM-301 macroporous resin column, carry out absorption and purification, 5%, 25%, 55%, 75%, 90% alcoholic solution of water, 2 times of post appearances carries out gradient elution successively, after eluent mixes, reclaims ethanol, through vacuum drying, within 24 hours, obtain primary extract 61.32g left and right, wherein general flavone content reaches 49.48～55.25%.
Embodiment 11
According to the Flos persicae total flavones of the present embodiment, preparation method is substantially with embodiment 10, different, extracts the ethanol that solvent is 45wt% in step (1), finally obtains primary extract 55.61g left and right, and wherein general flavone content can reach 51.29～54.32%.
Embodiment 12
According to the Flos persicae total flavones of the present embodiment, preparation method is substantially with embodiment 11, different, extracts the ethanol that solvent is 15wt% in step (1), finally obtains primary extract 49.25g left and right, and wherein general flavone content can reach 52.51～53.62%.
Embodiment 13
According to the Flos persicae total flavones of the present embodiment, preparation method is substantially with embodiment 10, different, and raw material is honey peach dry Flos persicae, and extraction solvent is water, finally obtains primary extract 60.06g left and right, and wherein general flavone content reaches 43.48～51.25%.
Embodiment 14
According to the Folium Persicae total flavones of the present embodiment, preparation method is substantially with embodiment 7, and different is that its raw material is the dry Folium Persicae of honey peach, finally obtains primary extract 38.53g left and right, and wherein general flavone content reaches 44.63～49.81%.
Embodiment 15
According to the Flos persicae total flavones of the present embodiment, preparation as follows:
Get the Xinjiang peento dry Flos persicae of 1kg, by weight the ratio of 1: 10, putting into 45% ethanol first soaks half an hour, at 75 ℃ of constant temperature water baths, reflux 1 hour, extract altogether 3 times, each 1 hour, extract is after reclaiming ethanol, with chitin remove impurity, the absorption of use DM-301 macroporous resin column, separation and purification, 5%, 25%, 55%, 75%, 90% alcoholic solution of water, 2 times of post appearances carries out gradient elution successively, after mixing, eluent reclaims ethanol, through vacuum drying, within 24 hours, obtain primary extract 50.81g left and right altogether, wherein general flavone content reaches 47.52～51.33%.
Embodiment 16
According to the Folium Persicae total flavones of the present embodiment, preparation as follows:
Get the dry Folium Persicae of Xinjiang peento of 1kg, by weight the ratio of 1: 12, putting into extraction solvent water first soaks half an hour, at 80 ℃ of constant temperature water baths, reflux 1 hour, extract altogether 3 times, each 1 hour, extract is after reclaiming ethanol, with chitin remove impurity, the absorption of use DM-301 macroporous resin column, separation and purification, 5%, 25%, 55%, 75%, 90% alcoholic solution of water, 2 times of post appearances carries out gradient elution successively, after mixing, eluent reclaims ethanol, through vacuum drying, within 24 hours, obtain primary extract 41.01g left and right altogether, wherein general flavone content reaches 45.12～48.68%.
flos persicae or Folium Persicae total flavones qualitative test
1, conventional Flavonoid substances discrimination test: by the sample of embodiment 7 to 16 gained total flavones, apply conventional Flavonoid substances discrimination test method and detect, the results are shown in Table 3, all experiments are all positive, and 7 to 16 of embodiment obtain product all containing Flavonoid substances.
Table 3
Note: "+" represents positive findings; "-" represents negative findings.
2, liquid-phase chromatographic analysis: get embodiment 10 gained samples, analyze under following chromatographic condition: Shimadzu LC-10ADvp double pump, SPD-M10Avp DAD detector; Shimadzu Shim-Pack CLC-ODS (150mm * 4.6mm, 5 μ m) chromatographic column; Mobile phase: 0.1% acetic acid aqueous solution (A)-methanol (B), gradient elution; Ultraviolet detection wavelength: 289nm; Flow velocity: 1.0mL/min; Sample size: 20 μ L.Testing result is shown in Fig. 1 to 4.Fig. 1 is the liquid chromatogram of reference substance mixed solution, in figure: six chromatographic peaks are respectively coumarin (t=16.341), Quercitroside (t=22.914), Herba Astragali Melilotoidis (Herba Astragali Sinici) glycosides (t=23.507), naringenin (t=29.738), hesperetin (t=31.243), kaempferol (35.738).Contrast Fig. 1,2 to 4, visible coumarin, Herba Astragali Melilotoidis (Herba Astragali Sinici) glycosides, hesperetin, kaempferols etc. are the important composition composition of Flos persicae total flavones.
the effect research to type i diabetes mice due to alloxan of Flos persicae or Folium Persicae total flavones
1, test method: get clean level Male Kunming strain mice, 22-25g, fasting 12h, by 60mg/kg body weight tail vein injection alloxan solution.In the 4th day fasting 12h, survey fasting glucose >=11.0mmol/L person and be defined as diabetic mice, be divided at random model group and treatment group.Model group is pressed 20ml/kg body weight and is filled with distilled water, treatment group is divided into birthday peaches folic alcohol and carries total flavones group (150mg/kg, embodiment 9 samples), birthday peaches flower water extraction total flavones group (150mg/kg, embodiment 10 samples), birthday peaches flower alcohol extraction total flavones group (150mg/kg, embodiment 11 samples), honey peach Flos persicae water extraction total flavones group (150mg/kg, embodiment 13 samples), Xinjiang peento flower alcohol extraction total flavones group (150mg/kg, embodiment 15 samples), Xinjiang peento leaf water extraction total flavones group (150mg/kg, embodiment 16 samples) and acarbose matched group (100mg/kg), gastric infusion every day 1 time, continuous 10 days, fasting 12h, survey fasting blood sugar, compare administration front and back mice fasting glucose.In administration 15 days, carry out glucosieloading test (oral glucose 2g/kg), the impact of comparative drug on diabetic mice carbohydrate tolerance due to alloxan.
2, result of the test:
The results are shown in Table 4 and 5.Therefrom visible, the Flos persicae total flavones of embodiment and Folium Persicae total flavones all can effectively reduce alloxan diabetes mice fasting glucose, and can obviously improve the glucose tolerance of mice.Although can effectively reduce blood glucose and perform the formal wedding ceremony to put down, it is not improved effect for glucose load.
Table 4 Flos persicae or Folium Persicae total flavones are on the impact of alloxan diabetes mice fasting glucose (Mean ± SD, n=10)
Compare * P < 0.05, * * P < 0.01 with model after administration.
Table 5 Flos persicae or Folium Persicae total flavones are on the impact of alloxan diabetes glucose tolerance in mice (Mean ± SD, n=10)
Note: compare * P < 0.05, * * P < 0.01 with model after administration.
the effect research of the type ii diabetes rat that Flos persicae or Folium Persicae total flavones cause STZ
1, test method: get clean level SD male rat, 150～180g, feeds 60 days fasting 12h with high lipid food, with 40mg/kg dosage, lumbar injection STZ solution, after 4d, after fasting 12h, look into fasting glucose >=11.0mmol/L person and be defined as diabetes rat, be divided at random model group and treatment group.Model group gavages distilled water by 5ml/kg body weight, treatment group is divided into birthday peaches folic alcohol and carries total flavones group (100mg/kg, embodiment 9 samples, ), birthday peaches flower water extraction total flavones group (100mg/kg, embodiment 10 samples), birthday peaches flower alcohol extraction total flavones group (100mg/kg, embodiment 11 samples), honey peach Flos persicae water extraction total flavones group (100mg/kg, embodiment 13 samples), Xinjiang peento flower alcohol extraction total flavones group (100mg/kg, embodiment 15 samples), Xinjiang peento leaf water extraction total flavones group (100mg/kg, embodiment 16 samples) and acarbose matched group (60mg/kg), , gastric infusion every day 1 time, continuous 10 days, fasting 12h, survey fasting blood sugar, compare administration front and back rat fasting blood-glucose.In 20 days fasting 12h of administration, survey serum triglycerides (TG), cholesterol (TC), free fatty (FFA) concentration.
2, result of the test:
The results are shown in Table 6 and table 7.As seen from the table, the Folium Persicae total flavones of embodiment, Flos persicae total flavones and acarbose all can effectively reduce blood glucose.And Folium Persicae total flavones, Flos persicae total flavones have inhibitory action in various degree to abnormal rising of rat fat, relatively there were significant differences with model group.
Table 6 Flos persicae or Folium Persicae total flavones are on the impact of STZ diabetes rat fasting glucose (mmol/L, Mean ± SD)
Note: compare with model,
*p < 0.05,
*p < 0.01.
Table 7 Flos persicae or Folium Persicae total flavones are on the impact of STZ diabetes rat blood lipid level (mmol/L, Mean ± SD)
Note: compare with model after administration,
*p < 0.05,
*p < 0.01.
the effect research to rat whole blood platelet aggregation of Flos persicae or Folium Persicae total flavones
1, test method: get clean level male rat, 200 ± 20g, be divided at random 6 groups: Normal group (0.5%CMC), aspirin group (30mg/kg), birthday peaches leaf flavonoids group (100mg/kg, embodiment 9 samples), birthday peaches flower water extraction total flavones group (100mg/kg, embodiment 10 samples), honey peach flower water extraction total flavones group (100mg/kg, embodiment 13 samples) and peento flower alcohol extraction total flavones group (100mg/kg, embodiment 15 samples), the continuous gastric infusion of animal 2 weeks, after last administration 1 hour, eye socket venous plexus is got blood, each 0.5ml is to special glass silication test tube anticoagulant heparin (final concentration 30Uml-1), use respectively ADP (final concentration is 5 μ molL-1) induction to assemble, measure the maximum cluster set of whole blood platelet (unit: Ω) in 5min.Accurate for guaranteeing result, in 2h, surveyed at ambient temperature.
2, result of the test:
The results are shown in Table 8.Folium Persicae total flavones, each Flos persicae total flavones and aspirin all can effectively reduce the maximum gathering of platelet, and relatively there were significant differences with model group.
Table 8 Flos persicae or Folium Persicae total flavones are to the effect of normal rat whole blood platelet aggregation (n=10, Mean ± SD)
Note: with normal control comparison after administration,
*p < 0.05,
*p < 0.01.
flos persicae or the effect of Folium Persicae total flavones to rat experiment thrombosis
1, test method: get clean level male rat, 200 ± 50g, be divided at random 5 groups: Normal group (0.5%CMC), aspirin group (30mg/kg), birthday peaches leaf flavonoids group (100mg/kg, embodiment 9 samples), birthday peaches flower water extraction total flavones group (100mg/kg, embodiment 10 samples), honey peach flower water extraction total flavones group (100mg/kg, embodiment 13 samples) and peento flower alcohol extraction total flavones group (100mg/kg, embodiment 15 samples), the continuous gastric infusion of animal 2 weeks, 1h lumbar injection after last administration (20% urethane 5mlkg-1) anesthesia, make common carotid artery vessel endothelium and induced endothelial thrombus model, separated bilateral carotid, the standby blood sampling of left common carotid is used, its underlying small pieces plastic sheeting (4cm * 1.8cm) after right carotid separation, for the protection of blood vessel surrounding tissue, suction is had to 20%FeCl
3the small pieces filter paper (0.5cm * 0.5cm) of solution spreads in right carotid.After applying the scraps of paper, within 7 minutes, remove the scraps of paper, after the removal scraps of paper, after 25 minutes, cut right carotid thrombosis position blood vessel, be put on filter paper and blot remaining blood, with analytical balance, measure thrombus weight.
2, result of the test:
The results are shown in Table 9.Therefrom visible, Folium Persicae total flavones, each Flos persicae total flavones have obvious reducing effect to rat suppository weight in wet base, and relatively there were significant differences with Normal group.
Table 9 Flos persicae or Folium Persicae total flavones are to the effect of normal rat whole blood platelet aggregation (n=10, Mean ± SD)
| Group | Dosage (mg/kg) | Thrombosis length | Wet weight of thrombus |
| Normal control | -- | 1.04±0.05 | 7.82±1.88 |
| Aspirin | 30 | 1.1±0.14 | 4.90±2.72 ＊＊ |
| Birthday peaches leaf flavonoids | 100 | 1.11±0.11 | 4.94±2.79 ＊＊ |
| Birthday peaches flower total flavones | 100 | 1.06±0.43 | 4.69±2.08 ＊＊ |
| Honey peach flower total flavones | 100 | 1.13±0.22 | 5.11±2.36 ＊ |
| Peento flower total flavones | 100 | 1.09±0.18 | 4.78±2.31 ＊＊ |
Note: with normal control comparison,
*p < 0.05,
*p < 0.01.
Embodiment 17
Containing a pharmaceutical composition for Flos persicae primary extract, be tablet, it can be prepared by the following method: the Flos persicae primary extract 10g that gets embodiment 1 gained, add amylum pregelatinisatum 5g, dextrin 5g, mixes, and adopts 50% ethanol wet method to granulate, being cooled to 60 ℃ is dried below, granulate, adds Pulvis Talci 0.5g, mixes, be pressed into 100, Flos persicae primary extract content is 0.1g/ sheet.
The pharmaceutical tablet composition of the present embodiment can be used for blood sugar lowering blood fat, preventing/treating diabetes and complication thereof.
Embodiment 18
Containing a pharmaceutical composition for Flos persicae total flavones, be injection, it can be prepared by the following method: the Flos persicae total flavones 50g that gets embodiment 10 gained, being dissolved in 425ml 25% ethanol dissolves, prepare solution, with activated carbon decolorizing, filter, inject water and make 5% aqueous solution 1000ml, with microporous filter membrane (Φ 0.20 μ m), filter to clear and bright, sterilizing, aseptic subpackaged, every bottle of 2ml, sealing.
Embodiment 19
A compound preparation for Flos persicae total flavones and pioglitazone, it can be prepared by the following method: get the Flos persicae total flavones 5g of embodiment 10 gained, pioglitazone 1.5g, dextrin 25g, microcrystalline Cellulose 10g, mixes, adopt 50% ethanol wet method to granulate, be cooled to 60 ℃ and be dried below, granulate, adds magnesium stearate 0.2g, mix, record 100 of capsules, average every contains total flavones 0.05g, pioglitazone 0.015g.
Embodiment 20
Containing a pharmaceutical composition for Folium Persicae primary extract, be tablet, its preparation process is: the Folium Persicae primary extract 10g that gets embodiment 4 gained, add amylum pregelatinisatum 5g, dextrin 5g, mixes, and adopts 50% ethanol wet method to granulate, being cooled to 60 ℃ is dried below, granulate, adds Pulvis Talci 0.5g, mixes, be pressed into 100, Folium Persicae primary extract content is 0.1g/ sheet.
Embodiment 21
A pharmaceutical composition for Folium Persicae total flavones and pioglitazone, is capsule, and its preparation process is: the Folium Persicae total flavones 5g that gets embodiment 9 gained, pioglitazone 1.5g, dextrin 25g, microcrystalline Cellulose 10g, mix, adopt 50% ethanol wet method to granulate, be cooled to 60 ℃ and be dried below, granulate, add magnesium stearate 0.2g, mix, record 100 of capsules, average every contains total flavones 0.05g, pioglitazone 0.015g.
Above the present invention is described in detail; its object is to allow the personage who is familiar with this art can understand content of the present invention and be implemented; can not limit the scope of the invention with this; the equivalence that all spirit according to the present invention are done changes or modifies, and all should be encompassed in protection scope of the present invention.
Claims (22)
1. for blood sugar lowering blood fat and/or prevent and/or treat diabetes and a Flos persicae total flavones for complication, it is characterized in that: described Flos persicae total flavones prepares by the following method:
(1), take Flos persicae as raw material, take the alcohol of water or carbon number 1～6 as extracting solvent, at the temperature of 10 ℃～100 ℃, extract, obtain the extracting solution of Flos persicae;
(2), make the extracting solution of described Flos persicae carry out the separated described Flos persicae total flavones that obtains by macroporous adsorbent resin.
2. Flos persicae total flavones according to claim 1, is characterized in that: the described Flos persicae as raw material is the Flos persicae of the common Fructus Persicae of Rosaceae Prunus Fructus Persicae Subgenus, Xinjiang Fructus Persicae, Prunus davidiana or almond.
3. Flos persicae total flavones according to claim 1, it is characterized in that: the described alcohol as extracting solvent is one or more the mixture being selected from methanol, ethanol, n-butyl alcohol, isobutanol, and the mass percent concentration scope of described alcohol is 5wt%～95wt%.
4. Flos persicae total flavones according to claim 1, is characterized in that: in step (1), described in be extracted at temperature 45 C～100 ℃ and carry out.
5. Flos persicae total flavones according to claim 1, is characterized in that: the described method of preparing Flos persicae total flavones is also included in step (2) before, and the extracting solution that step (1) is obtained carries out remove impurity processing.
6. Flos persicae total flavones according to claim 1, it is characterized in that: the detailed process of step (2) is: after described extracting solution is adsorbed by macroporous adsorbent resin, the methanol of water, 5wt%～90wt% or ethanol carry out eluting successively, Fractional Collections water and alcohol eluate, vacuum drying obtains described Flos persicae total flavones.
7. according to the Flos persicae total flavones described in claim 1 or 6, it is characterized in that: described macroporous adsorbent resin is 101 types AB-8 type, D101 type, DM301 type, NKA-9 type, HPD100 type or HPD200 type macroporous adsorbent resin.
8. Flos persicae total flavones according to claim 6, is characterized in that: in step (2), the linear gradient elution method that adopts eluting solvent concentration to increase is gradually carried out described eluting.
A Flos persicae total flavones as described in any one claim in claim 1 to 8 and/or contain as described in the pharmaceutical composition of Flos persicae total flavones preparing blood sugar lowering blood fat, preventing and/or treating the purposes in diabetes and complication medicine or health product.
10. for blood sugar lowering blood fat and/or prevent and/or treat diabetes and a pharmaceutical composition for complication, it is characterized in that: in the effective ingredient of described pharmaceutical composition, at least comprise the Flos persicae total flavones described in any one in claim 1 to 8.
11. pharmaceutical compositions according to claim 10, is characterized in that: described pharmaceutical composition is oral agents or the injection that described Flos persicae total flavones and the acceptable pharmaceutical carrier of pharmacy are made.
12. pharmaceutical compositions according to claim 10, is characterized in that: described pharmaceutical composition is the compound preparation that contains described Flos persicae total flavones and the acceptable pharmaceutical carrier of pharmacy.
13. 1 kinds of Flos persicae primary extracts are being prepared blood sugar lowering blood fat, are being prevented and/or treated the purposes in diabetes medicament or health product, described Flos persicae primary extract is to take Flos persicae as raw material, take the alcohol of water or carbon number 1～6 as extracting solvent, at the temperature of 10 ℃～100 ℃, extract acquisition.
14. purposes according to claim 13, is characterized in that: described in be extracted at temperature 45 C～100 ℃ and carry out.
15. 1 kinds of pharmaceutical compositions that contain Flos persicae primary extract are being prepared blood sugar lowering blood fat, are being prevented and/or treated the purposes in diabetes medicament or health product, described Flos persicae primary extract is to take Flos persicae as raw material, take the alcohol of water or carbon number 1～6 as extracting solvent, at the temperature of 10 ℃～100 ℃, extract acquisition.
16. purposes according to claim 15, is characterized in that: described in be extracted at temperature 45 C～100 ℃ and carry out.
17. 1 kinds of Folium Persicae total flavones are being prepared blood sugar lowering blood fat, are being prevented and/or treated the purposes in diabetes and complication medicine or health product, and described Folium Persicae total flavones prepares by the following method:
(1), take Folium Persicae as raw material, take the alcohol of water or carbon number 1～6 as extracting solvent, at the temperature of 10 ℃～100 ℃, extract, obtain the extracting solution of Folium Persicae;
(2), make the extracting solution of described Folium Persicae carry out the separated described Folium Persicae total flavones that obtains by macroporous adsorbent resin.
18. 1 kinds of pharmaceutical compositions that contain Folium Persicae total flavones are being prepared blood sugar lowering blood fat, are being prevented and/or treated the purposes in diabetes and complication medicine or health product, and described Folium Persicae total flavones prepares by the following method:
(1), take Folium Persicae as raw material, take the alcohol of water or carbon number 1～6 as extracting solvent, at the temperature of 10 ℃～100 ℃, extract, obtain the extracting solution of Folium Persicae;
(2), make the extracting solution of described Folium Persicae carry out the separated described Folium Persicae total flavones that obtains by macroporous adsorbent resin.
19. 1 kinds of Folium Persicae primary extracts are being prepared blood sugar lowering blood fat, are being prevented and/or treated the purposes in diabetes and complication medicine or health product, described Folium Persicae primary extract is to take Folium Persicae as raw material, take the alcohol of water or carbon number 1～6 as extracting solvent, at the temperature of 10 ℃～100 ℃, extract acquisition.
20. purposes according to claim 19, is characterized in that: described in be extracted at temperature 45 C～100 ℃ and carry out.
21. 1 kinds of pharmaceutical compositions that contain Folium Persicae primary extract are being prepared blood sugar lowering blood fat, are being prevented and/or treated the purposes in diabetes and complication medicine or health product, described Folium Persicae primary extract is to take Folium Persicae as raw material, take the alcohol of water or carbon number 1～6 as extracting solvent, at the temperature of 10 ℃～100 ℃, extract acquisition.
22. purposes according to claim 21, is characterized in that: described in be extracted at temperature 45 C～100 ℃ and carry out.
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| CN200910186884.3A CN101816719B (en) | 2009-12-31 | 2009-12-31 | Peach blossom or peach leaf general flavone and application thereof in preparing medicines or health care products for lowering blood sugar and fat and preventing and/or treating diabetes and complications |
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| CN108279278B (en) * | 2017-12-29 | 2020-09-04 | 广州白云山和记黄埔中药有限公司 | Method for separating flavonoid components and application thereof |
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| 王磊.天津地区14种果树叶提取物的研究.< * |
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