CN104147024A - Novel application of resveratrol derivatives - Google Patents
Novel application of resveratrol derivatives Download PDFInfo
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- CN104147024A CN104147024A CN201410412707.3A CN201410412707A CN104147024A CN 104147024 A CN104147024 A CN 104147024A CN 201410412707 A CN201410412707 A CN 201410412707A CN 104147024 A CN104147024 A CN 104147024A
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- verakanol derivative
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Abstract
The invention relates to a novel application of resveratrol derivatives. The novel application of resveratrol derivatives is blood fat reduction. The molecular structural formula of resveratrol derivatives is shown in the description. The molecular formula of the resveratrol derivatives is C20H22O9, the molecular weight is 406, the unsaturation degree n is equal to 10, and the resveratrol derivatives are named as 3'-hydroxylresveratrol and 4'-O-beta-D-pyranylglucoside. The high-purity compounds and alcohol extracts of the provided resveratrol derivatives have a prominent effect on reducing blood fat, have a very good curative effect, do not have any side or toxic effect, and is suitable for promotion and application.
Description
Technical field
The present invention relates to a kind of medical technical field, relate in particular to a kind of new purposes of Verakanol derivative.
Background technology
Hyperlipidemia often causes atherosclerosis, and hypertension causes the relevant diseases such as diabetes, and human health is formed greatly and threatened.But this brings side effect to patient in sick in treatment to take chemicals.Though common Chinese medicine side effect is little, effect is not obvious.
Summary of the invention
For above problem, the present invention proposes a kind of Verakanol derivative and has the new purposes of obvious blood fat reducing.
The present invention is achieved by the following technical solutions:
The new purposes of above-mentioned Verakanol derivative, has obvious effect for reducing blood fat, and the molecular structural formula of described Verakanol derivative is as follows:
The molecular formula of the Verakanol derivative of above-mentioned molecular structural formula is C20H22O9, and molecular weight is 406, degree of unsaturation n=10, and its name is called 3 '-hydroxyl resveratrol, 4 '-O-β-D-glucopyanoside.
The new purposes of described Verakanol derivative, wherein: the High Purity compound of the Verakanol derivative of described molecular structural formula and ethanol extract have the serum lipids in rats that treatment high fat diet methylate thiouracil brings out, serum triglycerides, T-CHOL and low-density lipoprotein cholesterol content be can obviously reduce, high density density lipoprotein cholesterol level and high/low density lipoprotein ratio increased.
The new purposes of described Verakanol derivative, wherein: High Purity compound and the ethanol extract of the Verakanol derivative of described molecular structural formula also have obvious regressive effect to intra-arterial atheromatous plaque.
The new purposes of described Verakanol derivative, wherein: the effective dose of described High Purity compound is that 35mg/kg～40mg/kg is oral; The minimum effective dose of described ethanol extract is 90mg/kg～100mg/kg.
The new purposes of described Verakanol derivative, wherein: the Verakanol derivative of described molecular structural formula can be from natural drug as extracted or synthetic Radix Rhei emodi, Rheum hotaoense C. Y. Cheng et C. T. Kao, Rheum officinale, Rheum tanguticum and Rhizoma Polygoni Cuspidati, Radix Polygoni Multiflori Chinese medicine.
Beneficial effect:
The new purposes of Verakanol derivative of the present invention is mainly reflected in, the Verakanol derivative of above-mentioned molecular structural formula has obvious effect for reducing blood fat, specifically the ethanol extract of the Verakanol derivative of above-mentioned molecular structural formula has the significantly therapeutical effect relevant to dosage with the oral hyperlipemia that rat high fat diet is caused of High Purity compound, intra-arterial atheromatous plaque is also had to obvious regressive effect, evident in efficacy and have no side effect, be suitable for propagation and employment.
Detailed description of the invention
The new purposes of Verakanol derivative of the present invention, its Verakanol derivative relating to can be from natural drug as extracted the Chinese medicines such as Radix Rhei emodi, Rheum hotaoense C. Y. Cheng et C. T. Kao, Rheum officinale, Rheum tanguticum and Rhizoma Polygoni Cuspidati, Radix Polygoni Multiflori, also can synthetic.
High Purity compound and the ethanol extract of Verakanol derivative of the present invention have obvious effect for reducing blood fat, and its structural formula is as follows:
The molecular formula of the Verakanol derivative of above-mentioned molecular structural formula is C20H22O9, and molecular weight is 406, degree of unsaturation n=10, and its name is called 3 '-hydroxyl resveratrol, 4 '-O-β-D-glucopyanoside.
In order to prove whether the High Purity compound of Verakanol derivative of the above-mentioned molecular structural formula of the present invention and ethanol extract have the therapeutical effect of blood fat reducing to hyperlipidemia animal, the present invention specifically gets the high lipid food modeling of SD rat, after animal high blood lipid model causes, oral administration is done blood fat reducing therapeutic test again, after administration two weeks, survey lipids contents and aorta inwall Mottling formation.
Below in conjunction with specific experiment, the new purposes of Verakanol derivative of the present invention is done further to prove:
(1.1) preparation given the test agent
Be that ethanol extract is mixed with the suspension that concentration is 2.5mg/ml, 5.0mg/ml, 10.0mg/ml and 25.0mg/ml by 1% tragakanta solution by concentration;
It is 1.0,2.0 and 4.0mg/ml suspension that given the test agent (the High Purity compound of the Verakanol derivative of the above-mentioned molecular structural formula that concentration is 98%) is mixed with concentration by the tragakanta solution that is 1% by concentration;
(1.2) preparation control sample
After weighing by capsule (Chinese woods QINGZHI JIAONANG) content, the tragakanta solution preparation that is 1% by concentration becomes 28.8mg/ml suspension;
Pulverize by sample (Herb Gynostemmae Pentaphylli total glucosides tablet) last, the tragakanta solution preparation that is 1% by concentration becomes 4.32mg/ml suspension;
After weighing by capsule (Chinese woods QINGZHI JIAONANG) content, the tragakanta solution preparation that is 1% by concentration becomes 28.8mg/ml suspension;
Pulverize by tablet last, the tragakanta solution preparation that is 1% by concentration becomes 0.48mg/ml suspension;
(1.3) grouping
Get 130 of SD rats, be divided into 13 groups, 10 every group, establish 1 group of normal group (feeding common full nutrient fodder) and 12 groups of high lipid food groups;
(1.4) modeling
Adding Adeps Sus domestica 20%, cholesterol 4%, methylthiouracil 0.2% with normal diet feeds 4 weeks; Canthus blood sampling in the 3rd week, centrifugal 5 minutes separation of serum of 10000rpm, measure serum triglycerides (TG), serum total cholesterol (CHO), HDL-C (HDL-Ch) and low hdl cholesterol (LDL-Ch) with automatic biochemistry analyzer, and calculate the ratio (HDL/LDL) of HDL-Ch and LDL-Ch, confirm that hyperlipidemia model forms rear beginning administration;
(1.5) administration
Model group is to excipient; Ethanol extract is divided into 25,50,100 and 250mg/kg4 dosage group; High Purity compound is divided into 10,20 and 40mg/kg3 dosage group; Matched group is divided into Chinese woods QINGZHI JIAONANG 288mg/kg group, Herb Gynostemmae Pentaphylli total glucosides tablet 43.2mg/kg group, gemfibrozil capsule 288mg/kg group and 4 groups of simvastatin 4.8mg/kg group;
Oral administration, volume is 1ml/100g body weight, administration every day 1 time, successive administration 14 days, the 15th day animal chloral hydrate anesthesia, ventral aorta blood sampling, by above method separation of serum, measures TG, CHO, HDL-Ch and LDL-Ch; Calculate respectively meansigma methods and the standard deviation of the each lipid of the forward and backward serum of administration, and calculate the difference before and after each animals administer, compare with the change value after administration and the changing value of model control group, carry out the statistical test of the significance of difference with t test, P<0.05 represents significant difference, and P<0.01 represents difference highly significant; After dissection, get aorta 1.5～2cm from aortic root, along dorsal part longitudinal incision, 10% formalin is fixed, soudan III dyeing, after dyeing, lipid infiltration district and speckle present peony, dissect Microscopic observation Wall of Artery Mottling formation situation, and carrying out pathological changes classification according to following standard, and calculating the average of each group.
Below in conjunction with specific experiment result, the present invention is described further:
On the impact of serum lipids
(1) impact on serum triglycerides
After modeling, the each index of serum lipids all has significant change, model group TG compared with normal group raises approximately 2.2 times, CHO and LDL also obviously increase, it is obviously little compared with LDL value added that HDL increases degree, therefore HDL/LDL ratio obviously reduces, before the administration of each administration group, serum lipids index and normal group also have the significantly difference to highly significant.Each administration group and model group comparison, do not have notable difference.The modeling that shows this test is successful.
After administration 2 weeks, the oral rear rat blood serum triglyceride of High Purity compound 10～40mg/kg shows with dosage to be increased and reduces, but only there were significant differences with model group for 40mg/kg group, ethanol extract 25～250mg/kg also has similar impact, 100 with obviously reduce compared with model contrast when 250mg/kg dosage.Chinese woods QINGZHI JIAONANG and gemfibrozil 288mg/kg and simvastatin 4.8mg/kg also show the effect of obvious reduction TG.The results are shown in Table 1.
Table 1: the High Purity compound of the Verakanol derivative of the above-mentioned molecular structural formula of the present invention and the ethanol extract impact (± s, n=10) on rat blood serum triglyceride
*p<0.05,
*p<0.01 and model group comparison.
(2) impact on serum total cholesterol
After administration 2 weeks, the oral rear rat blood serum T-CHOL of High Purity compound 10～40mg/kg shows with dosage to be increased and reduces, but only there were significant differences with model group for 40mg/kg group, ethanol extract 25～250mg/kg also has similar impact, 100 with obviously reduce compared with model contrast when 250mg/kg dosage.Gemfibrozil 288mg/kg and simvastatin 4.8mg/kg also show the effect of obvious reduction CHO.The results are shown in Table 2.
Table 2: the High Purity compound of the Verakanol derivative of the above-mentioned molecular structural formula of the present invention and the ethanol extract impact (± s, n=10) on rat blood serum T-CHOL
*p<0.05,
*p<0.01 and model group comparison.
(3) impact on the high and low density lipoprotein-cholesterol of serum
After modeling, highdensity lipoprotein-cholesterol (HDL-Ch) and LDL-C (LDL-Ch) level all significantly raise, but it is more obvious that LDL-C level rising higher density lipoproteins-C raises, therefore HDL/LDL ratio significantly reduces.
After administration 2 weeks, the oral rear rat blood serum HDL-Ch of High Purity compound 10～40mg/kg shows to be increased with dosage, but only there were significant differences with model group for 40mg/kg group, and ethanol extract 25～250mg/kg also has similar impact, when 250mg/kg dosage, obviously increase compared with model contrast.Herb Gynostemmae Pentaphylli general glycoside 43.2mg/kg and gemfibrozil 288mg/kg highly significant rising HDL-Ch, simvastatin 4.8mg/kg also shows the effect of obvious increase HDL-Ch.The results are shown in Table 3.
The oral demonstration of High Purity compound reduces the trend of LDL-Ch.100 and the LDL-Ch of 250mg/kg ethanol extract significantly decline.Gemfibrozil and simvastatin also significantly reduce LDL-Ch.The results are shown in Table 4.
Table 3: the High Purity compound of the Verakanol derivative of the above-mentioned molecular structural formula of the present invention and the ethanol extract impact (± s, n=10) on rat blood serum highdensity lipoprotein-cholesterol
*p<0.05,
*p<0.01 and model group comparison.
Table 4: the High Purity compound of the Verakanol derivative of the above-mentioned molecular structural formula of the present invention and the ethanol extract impact (± s, n=10) on rat blood serum LDL-C
*p<0.05,
*p<0.01 and model group comparison.
High Purity compound 20 and 40mg/kg and ethanol extract 50～250mg/kg also significantly improve HDL/LDL ratio.The equal highly significant rising of Herb Gynostemmae Pentaphylli general glycoside, gemfibrozil and simvastatin HDL/LDL ratio.The results are shown in Table 5.
Table 5: the High Purity compound of the Verakanol derivative of the above-mentioned molecular structural formula of the present invention and the ethanol extract impact (± s, n=10) on the high/low density lipoprotein-cholesterol ratio of rat blood serum
*p<0.05,
*p<0.01 and model group comparison
Result of the test shows, the serum lipids in rats that the High Purity compound of the Verakanol derivative of the above-mentioned molecular structural formula of the present invention and ethanol extract have obvious treatment high fat diet methylate thiouracil to bring out.Serum triglycerides, T-CHOL and low-density lipoprotein cholesterol content be can obviously reduce, HDL-C content and high/low density lipoprotein ratio increased.The effective dose of High Purity compound is that 35mg/kg～40mg/kg is oral; The minimum effective dose of ethanol extract is 90mg/kg～100mg/kg.
(4) impact on Wall of Artery Mottling formation
Rat feeding high lipid food 1 month, intra-arterial has obvious atherosclerosis plaque forming, and given the test agent High Purity compound and ethanol extract are after oral 2 weeks, and intra-arterial speckle has minimizing trend, and high dose and model group relatively have notable difference.Gemfibrozil and simvastatin also obviously reduce the formation of intra-arterial atheromatous plaque.Result of the test is in table 6.
Table 6: the High Purity compound of the Verakanol derivative of the above-mentioned molecular structural formula of the present invention and the ethanol extract impact (± s, n=10) on rat aorta inwall Mottling formation
*p<0.05,
*p<0.01 and model group comparison.
In summary, the High Purity compound of the Verakanol derivative of the above-mentioned molecular structural formula of the present invention has the significantly therapeutical effect relevant to dosage with the oral hyperlipemia that rat high fat diet is caused of ethanol extract, intra-arterial atheromatous plaque is also had to obvious regressive effect, and the Verakanol derivative of the above-mentioned molecular structural formula of the present invention has obvious effect for reducing blood fat.
Claims (5)
1. a new purposes for Verakanol derivative, has obvious effect for reducing blood fat, and the molecular structural formula of described Verakanol derivative is as follows:
The molecular formula of the Verakanol derivative of above-mentioned molecular structural formula is C20H22O9, and molecular weight is 406, degree of unsaturation n=10, and its name is called 3 '-hydroxyl resveratrol, 4 '-O-β-D-glucopyanoside.
2. the new purposes of Verakanol derivative as claimed in claim 1, it is characterized in that: the High Purity compound of the Verakanol derivative of described molecular structural formula and ethanol extract have the serum lipids in rats that treatment high fat diet methylate thiouracil brings out, serum triglycerides, T-CHOL and low-density lipoprotein cholesterol content be can obviously reduce, high density density lipoprotein cholesterol level and high/low density lipoprotein ratio increased.
3. the new purposes of Verakanol derivative as claimed in claim 1, is characterized in that: High Purity compound and the ethanol extract of the Verakanol derivative of described molecular structural formula also have obvious regressive effect to intra-arterial atheromatous plaque.
4. the new purposes of Verakanol derivative as claimed in claim 1, is characterized in that: the effective dose of described High Purity compound is that 35mg/kg～40mg/kg is oral; The minimum effective dose of described ethanol extract is 90mg/kg～100mg/kg.
5. the new purposes of Verakanol derivative as claimed in claim 1, is characterized in that: the Verakanol derivative of described molecular structural formula can from natural drug as Radix Rhei emodi, Rheum hotaoense C. Y. Cheng et C. T. Kao, Rheum officinale, Rheum tanguticum and Rhizoma Polygoni Cuspidati, Radix Polygoni Multiflori Chinese medicine extract or synthetic.
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| CN201410412707.3A CN104147024A (en) | 2014-08-20 | 2014-08-20 | Novel application of resveratrol derivatives |
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| CN201410412707.3A CN104147024A (en) | 2014-08-20 | 2014-08-20 | Novel application of resveratrol derivatives |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1294912A (en) * | 1999-11-05 | 2001-05-16 | 中国人民解放军军事医学科学院放射医学研究所 | Blood sugar reducing compound |
| CN102058678A (en) * | 2010-12-10 | 2011-05-18 | 成都华西天然药物有限公司 | Medicine or health-care food composition for treating fatty liver |
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2014
- 2014-08-20 CN CN201410412707.3A patent/CN104147024A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1294912A (en) * | 1999-11-05 | 2001-05-16 | 中国人民解放军军事医学科学院放射医学研究所 | Blood sugar reducing compound |
| CN102058678A (en) * | 2010-12-10 | 2011-05-18 | 成都华西天然药物有限公司 | Medicine or health-care food composition for treating fatty liver |
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Application publication date: 20141119 |