CN101224246A - Preparing method of loquat leaf total triterpenic acid and antidiabetic use thereof - Google Patents
Preparing method of loquat leaf total triterpenic acid and antidiabetic use thereof Download PDFInfo
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- 241001092070 Eriobotrya Species 0.000 title abstract 5
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- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims abstract description 44
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Abstract
The invention relates to a preparation method for triterpene acid of loquat leaf and the function of lowering the blood glucose. The preparation method comprises that dry loquat leaves are firstly extracted by ethanol or methanol with certain concentration, reclaimed in ethanol with low condensation for sedimentation, and centrifuged, precipitated and refluxing-decolorized with diatomite or done with chromatography with siliceous earth column, and then eluted with ethanol and reclaimed in condition of decompression and dried to obtain the triterpene acid of loquat leaf. Total content of ursolic acid, oleanolic acid, maslinic acid, corosolic acid and tormentic acid in the triterpene acid reaches more than 50 percent (by weight), wherein, the content of the tormentic acid is to be 10-30 percent, the maslinic acid 4-20 percent, the corosolic acid 5-20 percent, the oleanolic acid 1-10 percent and the ursolic acid 5-20 percent. The triterpene acid of loquat leaf prepared by the invention can be used for curing diabetes mellitus or preparing pharmaceutic preparations used for treating diabetes mellitus and diabetic complication.
Description
Technical field:
The present invention relates to from the Chinese medicine Folium Eriobotryae, extract the method for preparing total triterpene acid, and the application of this extract aspect blood sugar lowering.
Background technology:
Diabetes are a kind of common endocrine metabolism diseases, belong to the diabetes category in Chinese medicine, are the third-largest illness of harm humans health after cardiovascular disease and cancer.Up to 1.25 hundred million, estimate that this numeral to 2025 year will be increased to 2.99 hundred million according to diabetics in the World Health Organization (WHO) report global range.Because large population base, the diabetics of China is about more than 3,000 ten thousand now, and absolute number of patients occupies first place in the world.Because diabetes have prevalence, disability rate and complication height, therefore become a kind of disease that medical circle is rather paid attention to.
In treatment of diabetes, mainly be to raise and prevent and treat complication by the medicine blood sugar control.In the medicine of treatment diabetes, two medicines are had outstanding performance aspect blood sugar lowering, and Chinese medicine is showing unique characteristics aspect the treatment complication, and the two has his own strong points.From present clinical used medicine, Western medicine all has certain limitation and untoward reaction, or even serious adverse effects very, as causes hypoglycemia, lactic acidosis etc.Therefore, take much count of both at home and abroad from natural product especially medicinal plants (Chinese herbal medicine) excavating always and the exploitation blood sugar decreasing effect is good, side effect is little, to the effective pharmaceutical preparation of complication.
Folium Eriobotryae is the dried leaves of Rosaceae Folium Eriobotryae platymiscium Folium Eriobotryae Eriobotrya japonica (Thunb.) Lindl., is conventional Chinese medicine simply, records in going through edition Chinese Pharmacopoeia and uses for tcm clinical practice.Folium Eriobotryae attaches to the lung and stomach meridians, and tool clearing away lung-heat to relieve cough, stopping nausea and vomiting by lowering the adverse flow of QI effect are used for the treatment of that cough due to lung-heat, QI rising in reverse order breathe, symptom such as gastric heat vomiting, dysphoria with smothery sensation are thirsty.Recently the triterpene acids chemical constituent that separation obtains from Folium Eriobotryae of discovering has significant hypoglycemic activity.
Summary of the invention:
The object of the present invention is to provide a kind of preparation method of Folium Eriobotryae total triterpenic acids, this preparation method not only technology is simple, the yield height, and the yield of each triterpenic acid component is improved.
Another object of the present invention is to provide a kind of medicinal plants preparation for the treatment of diabetes.
1. the preparation method of Folium Eriobotryae total triterpenic acids
(1) with the Folium Eriobotryae drying and crushing.
(2) extract with 30-95% ethanol or 30-95% methanol dipping, solid-liquid ratio 1: 3～10 extracts twice, each 15～30 days; Or heating and refluxing extraction, solid-liquid ratio 1: 3～10 extracts twice, each 1 to 5 hour.
(3) merge extractive liquid, is evaporated to the low alcoholic degree concentrated solution that contains alcohol amount≤50%.
(4) low alcoholic degree concentrated solution is under 1500-5000 rev/min speed centrifugal sedimentation 10-30 minute, must precipitate.
(5) add 2-10 to the precipitation part and doubly measure ethanol, after heating makes it dissolving, add 0.5-3 and doubly measure the decolouring of kieselguhr reflux, filtered while hot, filtrate decompression concentrate drying; Or add to precipitation part and to add 0.5-3 after 2-10 doubly measures the ethanol heating for dissolving and doubly measure kieselguhr and mix sample, cross siliceous earth column, mixing sample kieselguhr is 1: 1～5 with blank kieselguhr ratio, ethanol elution, ethanol elution concentrating under reduced pressure drying gets the Folium Eriobotryae total triterpenic acids extract.
2. the method for quality control of Folium Eriobotryae total triterpenic acids
Main effective ingredient with preparation method gained Folium Eriobotryae total triterpenic acids of the present invention is ursolic acid (ursolic acid), oleanolic acid (oleanolicacid), maslinic acid (maslinic acid), Corosolic acid (corosolic acid), termentic acid (tormentic acid).
Adopt efficient liquid-phase chromatography method (HPLC) to detect each content of effective, chromatographic condition is: chromatographic column immobile phase carbon 18 alkyl silica gel, and mobile phase methanol-0.04% phosphoric acid solution (88: 12), flow velocity 1ml/min detects wavelength 208nm.According to said method detect, the retention time of termentic acid, maslinic acid, Corosolic acid, oleanolic acid, ursolic acid is respectively 4.4min, 8.9min, 9.6min, 15.8min, 16.7min (seeing accompanying drawing), calculate by weight percentage, the total content of five index components is greater than 50% in the Folium Eriobotryae total triterpenic acids, wherein the content of termentic acid should reach 10-30%, the content of maslinic acid should reach 4-20%, the content of Corosolic acid should reach 5-20%, the content of oleanolic acid should reach 1-10%, and content of ursolic acid should reach 5-20%.
3. the hypoglycemic activity of Folium Eriobotryae total triterpenic acids
Drug efficacy study result to the diabetic mice due to normal mouse, alloxan and the streptozotocin shows, Folium Eriobotryae total triterpenic acids among the present invention can the utmost point reduces the blood sugar level of normal mouse, alloxan and streptozotocin diabetic mice significantly, improve serum insulin levels, point out it to can be used for treating diabetes.
Experiment one, Folium Eriobotryae total triterpenic acids are to the influence of normal mouse fasting glucose
Experimental technique: get (18～22g) 90 of normal male ICR mices, be divided into 9 groups at random, give Folium Eriobotryae total triterpenic acids 300mg/kg, gliclazide 50mg/kg, SHENQI JIANGTANG KELI 2000mg/kg and isopyknic 0.5% sodium carboxymethyl cellulose (CMC-Na) by 10ml/kg body weight per os respectively, administration every day 1 time, 7d continuously.During the last administration, each organizes administration behind the fasting 4h, continues fasting 2h again.The mouse orbit rear vein beard is got blood, and separation of serum is with determination of glucose oxidase blood glucose.
Result: as shown in table 1, compare with normal group, Folium Eriobotryae total triterpenic acids 300mg/kg and gliclazide the 50mg/kg all utmost point have reduced the fasting glucose (P＜0.01) of normal mouse significantly, and SHENQI JIANGTANG KELI 2000mg/kg does not have obvious influence to the fasting glucose of normal mouse.
The influence of table 1 EJ-1 normal mouse fasting glucose (X ± SD)
| Group | Dosage (mg/kg) | Route of administration | Number of animals (only) | Fasting glucose (m mol/L) |
| Normal group Folium Eriobotryae total triterpenic acids SHENQI JIANGTANG |
300 2000 50 | p.o p.o p.o p.o | 10 10 10 10 | 6.36±1.12 3.60±0.74 ** 5.79±1.47 3.81±0.86 ** |
*P＜0.01vs normal group
Experiment two, Folium Eriobotryae total triterpenic acids are to the influence of alloxan diabetes mouse blood sugar and serum insulin
Experimental technique: (18～22g) 10 as normal group to get normal male ICR mice at random, behind all the other mice fasting 16-17h, tail vein injection alloxan 65mg/kg, inject back 72 hours eye socket rear vein beards and get blood, separation of serum, prediction blood glucose, select 90 of the mices of fasting glucose＞12m mol/L, be divided into 9 groups at random, give Folium Eriobotryae total triterpenic acids 300mg/kg, gliclazide 50mg/kg, SHENQI JIANGTANG KELI 2000mg/kg and isopyknic 0.5%CMC-Na by 10ml/kg body weight per os respectively, every day 1 time, successive administration 14 days.Wherein, respectively organize fasting 4h before the 7th administration, continue fasting 2h after the administration, the mouse orbit rear vein beard is got blood then, and separation of serum is measured blood glucose.Fasting 4h before the last administration, 2h after the administration, mice is plucked eyeball and gets blood, and separation of serum is measured blood glucose and serum insulin with kit method.
The result: as shown in table 2, to compare with normal group, the fasting blood glucose level of alloxan diabetes mice extremely significantly raises, and serum insulin levels extremely significantly reduces (P＜0.01).Compare with model group, Folium Eriobotryae total triterpenic acids 300mg/kg is the 7th day and the 14th day respectively remarkable (P＜0.05) and the extremely remarkable fasting glucose that has reduced diabetic mice after administration (P＜0.01), the serum insulin levels of the diabetic mice that extremely significantly raise (P＜0.01).
Table 2 Folium Eriobotryae total triterpenic acids is to the influence of blood glucose and the serum insulin of alloxan diabetes mice (X ± SD)
| Group | Dosage (mg/kg) | Route of administration | Number of animals (only) | Fasting glucose (m mol/L) | Insulin (u IU/mL) | |
| The 7th day | The 14th day | |||||
| Normal group model group Folium Eriobotryae total triterpenic acids SHENQI JIANGTANG KELI |
300 20000 50 | p.o p.o p.o p.o p.o | 10 9 9 9 10 | 6.36±0.74 24.49±5.67 ## 17.18±5.51 * 20.43±6.54 19.44±4.21 * | 5.77±0.71 23.43±4.01 ## 11.08±6.23 ** 19.02±4.19 * 1 8.25±4.88 * | 10.53±3.80 5.96±1.82 ## 11.53±2.51 ** 14.63±4.61 ** 11.43±3.76 ** |
##P＜0.01 vs normal group;
*P＜0.05,
*P＜0.01 vs model group
Experiment three, Folium Eriobotryae total triterpenic acids are to the influence of streptozotocin blood glucose in diabetic mice and serum insulin
Experimental technique: (18～22g) 10 as normal group to take out normal male ICR mice at random, behind all the other mice fasting 16-17 h, tail vein injection streptozotocin 160mg/kg, inject back 72 hours eye socket rear vein beards and get blood, separation of serum, the prediction fasting glucose, select 90 of the mices of fasting glucose＞12m mol/L, be divided into 9 groups at random, give Folium Eriobotryae total triterpenic acids 300mg/kg, gliclazide 50mg/kg, SHENQI JIANGTANG KELI 2000mg/kg and isopyknic 0.5%CMC-Na by 10ml/kg body weight per os respectively, every day 1 time, successive administration 14 days.Wherein, respectively organize fasting 4h before the 7th administration, continue fasting 2h after the administration, the mouse orbit rear vein beard is got blood then, and separation of serum is measured blood glucose.Fasting 4h before the last administration, 2h after the administration, mice is plucked eyeball and gets blood, and separation of serum is measured blood glucose, serum insulin with kit method.
The result: as shown in table 3, to compare with normal group, the fasting blood glucose level of streptozotocin diabetic mice extremely significantly raises, and serum insulin levels extremely significantly reduces (P＜0.01).Compare with model group, Folium Eriobotryae total triterpenic acids 300mg/kg after administration the 7th and 14 day all the utmost point reduced the fasting glucose (P＜0.01) of diabetic mice significantly, the serum insulin levels of the diabetic mice that extremely significantly raise (P＜0.01).
Table 3 Folium Eriobotryae total triterpenic acids is to the influence of streptozotocin blood glucose in diabetic mice and serum insulin (X ± SD)
| Group | Dosage (mg/kg) | Route of administration | Number of animals (only) | Fasting glucose (m mol/L) | Insulin (μ IU/mL) | |
| The 7th day | The 14th day | |||||
| Normal group model group Folium Eriobotryae total triterpenic acids SHENQI JIANGTANG KELI |
300 20000 50 | p.o p.o p.o p.o p.o | 10 10 10 10 9 | 6.75±0.86 22.76±4.21 ## 13.44±3.39 ** 18.16±5.81 16.72±5.88 * | 6.60±0.79 21.96±4.82 ## 11.47±3.65 ** 16.29±5.32 * 15.90±4.46 * | 29.68±9.47 10.05±23 ## 18.51±2.35 ** 16.54±6.75 * 15.11±3.56 * |
##P＜0.01 vs normal group;
*P＜0.05,
*P＜0.01 vs model group
Description of drawings:
Accompanying drawing is the HPLC figure of the Folium Eriobotryae total triterpenic acids sample of the inventive method preparation, and wherein retention time is that the component of 4.4min, 8.9min, 9.6min, 15.8min, 16.7min correspondence is respectively termentic acid, maslinic acid, Corosolic acid, oleanolic acid, ursolic acid.
The specific embodiment:
Embodiment 1: dry Folium Eriobotryae 1.0kg is ground into coarse powder, use 80% ethanol 8L successively, 6L merceration twice, each 15 days, merging impregnation liquid merges, be evaporated to the concentrated solution of alcoholic degree about 30%, centrifuge sedimentation and centrifugation (4000 rev/mins of rotating speeds are put in cooling, 15 minutes), must precipitate 46g, add 95% ethanol 230ml heating for dissolving, add 92g kieselguhr again and mix sample, get 92g kieselguhr dress post, behind the last sample, with 95% ethanol 2000ml eluting, eluent merges, decompression recycling ethanol, evaporate to dryness gets pale yellow powder 35g, is the Folium Eriobotryae total triterpenic acids extract.The Folium Eriobotryae total triterpenic acids extract is analyzed through HPLC, termentic acid 21.7%, maslinic acid 10.5%, Corosolic acid 13.6%, oleanolic acid 3.1%, ursolic acid 10.6%.
Embodiment 2: dry Folium Eriobotryae 1.0kg is ground into coarse powder, use 80% ethanol 6L successively, 4L heating and refluxing extraction 2 times, merge extractive liquid, is evaporated to the concentrated solution of alcoholic degree about 20%, cooling, put centrifuge sedimentation and centrifugation (2000 rev/mins of rotating speeds, 15 minutes), must precipitate 41g, add 95% ethanol 205ml heating for dissolving, add 41g kieselguhr again and mix sample, get 82g kieselguhr dress post, behind the last sample, with 95% ethanol 2000ml eluting, eluent merges, decompression recycling ethanol, evaporate to dryness, get pale yellow powder 32g, be the Folium Eriobotryae total triterpenic acids extract.The Folium Eriobotryae total triterpenic acids extract is analyzed through HPLC, termentic acid 20.9%, maslinic acid 10.1%, Corosolic acid 14.2%, oleanolic acid 3.0%, ursolic acid 8.9%.
Embodiment 3: dry Folium Eriobotryae 1.0kg is ground into coarse powder, uses 80% ethanol 6L successively, 4L heating and refluxing extraction 2 times, merge extractive liquid, is evaporated to the concentrated solution of alcoholic degree about 20%, cooling, put centrifuge sedimentation and centrifugation (2000 rev/mins of rotating speeds, 15 minutes), must precipitate 43g, add 95% ethanol 215ml heating for dissolving, add 43g kieselguhr again and mix sample, the reflux decolouring, filtered while hot, decompression recycling ethanol, evaporate to dryness, get pale yellow powder 34g, be the Folium Eriobotryae total triterpenic acids extract.The Folium Eriobotryae total triterpenic acids extract is analyzed through HPLC, termentic acid 18.3%, maslinic acid 10.4%, Corosolic acid 14.7%, oleanolic acid 2.6%, ursolic acid 8.9%.
Claims (4)
1. the preparation method of a Folium Eriobotryae total triterpenic acids and function of blood sugar reduction thereof
1. a method of extracting and prepare total triterpene acid from Folium Eriobotryae has significant function of blood sugar reduction according to the prepared total triterpene acid of this method.
2. the preparation method of Folium Eriobotryae total triterpenic acids according to claim 1, it is characterized in that may further comprise the steps: Folium Eriobotryae extracts or heating and refluxing extraction through 30-95% ethanol or 30-95% methanol dipping, obtain low alcoholic degree concentrated solution after removing alcohol, concentrated solution is through high speed centrifugation, separate, must precipitate, precipitation is the column chromatography decolouring after dissolve with ethanol, kieselguhr reflux or mixes sample, gets the Folium Eriobotryae total triterpenic acids extract.
3. Folium Eriobotryae total triterpenic acids according to claim 1, it is characterized in that counting by weight percentage, five index components ursolic acids (ursolicacid), oleanolic acid (oleanolic acid), maslinic acid (maslinic acid), Corosolic acid (corosolic acid), the total content of termentic acid (tormenticacid) is greater than 50%, wherein the content of termentic acid should reach 10-30%, the content of maslinic acid should reach 4-20%, the content of Corosolic acid should reach 5-20%, the content of oleanolic acid should reach 1-10%, and content of ursolic acid should reach 5-20%.
4. Folium Eriobotryae total triterpenic acids according to claim 1 has significant function of blood sugar reduction, can directly apply to the raw material of treatment diabetes or conduct treatment preparations for diabetes.
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102078400A (en) * | 2010-12-28 | 2011-06-01 | 江苏省中国科学院植物研究所 | Preparation method of extract of total triterpene acid of loquat leaf |
| CN102048851B (en) * | 2009-11-09 | 2013-03-13 | 臻里生物科技股份有限公司 | Loquat leaf cell extract for protecting liver and/or reducing fat and preparation method and application thereof |
| CN104147171A (en) * | 2014-08-28 | 2014-11-19 | 蒋君军 | Extraction method for triterpene acid component from herb residue of loquat leaf |
| CN111067932A (en) * | 2019-11-25 | 2020-04-28 | 中国药科大学 | A Prunellae Spica and/or herba Spinaciae effective component and its application in medicine for treating diabetes and diabetic nephropathy |
| US20210290714A1 (en) * | 2018-09-14 | 2021-09-23 | National Guard Health Affairs | Composition and method for treating skin disorders |
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- 2008-01-25 CN CN 200810018820 patent/CN101224246B/en not_active Expired - Fee Related
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102048851B (en) * | 2009-11-09 | 2013-03-13 | 臻里生物科技股份有限公司 | Loquat leaf cell extract for protecting liver and/or reducing fat and preparation method and application thereof |
| CN102078400A (en) * | 2010-12-28 | 2011-06-01 | 江苏省中国科学院植物研究所 | Preparation method of extract of total triterpene acid of loquat leaf |
| CN102078400B (en) * | 2010-12-28 | 2012-01-04 | 江苏省中国科学院植物研究所 | Preparation method of extract of total triterpene acid of loquat leaf |
| CN104147171A (en) * | 2014-08-28 | 2014-11-19 | 蒋君军 | Extraction method for triterpene acid component from herb residue of loquat leaf |
| US20210290714A1 (en) * | 2018-09-14 | 2021-09-23 | National Guard Health Affairs | Composition and method for treating skin disorders |
| US11903987B2 (en) * | 2018-09-14 | 2024-02-20 | National Guard Health Affairs | Artificial compositions comprising corosolic acid, oleanolic acid; and ursolic acid in a form of an emulsion, salve, ointment, suspension, or gel |
| CN111067932A (en) * | 2019-11-25 | 2020-04-28 | 中国药科大学 | A Prunellae Spica and/or herba Spinaciae effective component and its application in medicine for treating diabetes and diabetic nephropathy |
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