CN103030713A - Preparation method of low-molecular-weight glucan-niacin polymer with hypolipidemic activity - Google Patents
Preparation method of low-molecular-weight glucan-niacin polymer with hypolipidemic activity Download PDFInfo
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Abstract
The invention discloses a preparation method of a low-molecular-weight glucan-niacin polymer with a hypolipidemic activity and belongs to the field of biological chemistry. The preparation method comprises the following steps: activating beta-glucan 2,000 by an activating agent such as epoxy chloropropane, and coupling the activated beta-glucan 2,000 with niacin and niacin derivative methoxypyrazine. The mice test results show that the polymer has significant hypoglycemic capability. The preparation method is easy to operate, low in cost, low in environment pollution and suitable for large-scale application.
Description
Technical field
The present invention relates to the preparation method of a kind of LMD with hypolipidemic activity-nicotinic acid polymkeric substance, belong to biochemical field.
Background technology
Dextran claims again dextran, is a kind of polysaccharide.It is present in the mucus that certain micro-organisms secretes in process of growth.Dextran can replace a part of whole blood in the blood transfusion process, as the expansion agent (being called plasma substitute) of blood plasma volume.Its applied research at numerous areas such as medicine, food, chemical industry has obtained major progress.For the patient, the effect of dextran reducing blood-fat has research report.
Nicotinic acid is also referred to as vitamin B3, and it is one of 13 kinds of VITAMIN of needed by human, is a kind of water-soluble vitamins, belongs to vitamin B complex.Nicotinic acid is converted into niacinamide in human body, niacinamide is the integral part of cozymase and codehydrogenase Ⅱ, participates in HypercholesterolemicRats, the process that the oxidising process of tissue respiration and carbohydrate anaerobic are decomposed.When its consumption surpasses dosage as the VITAMIN effect, the effect of obvious adjusting blood fat can be arranged.Curative effect and the dosage of nicotinic acid adjusting blood fat are relevant with the front blood lipid level of taking medicine, and blood lipid level is unusually more obvious, and medication dose should be large, and curative effect is also more obvious.In addition, nicotinic acid derivates such as methoxy pyrazine and Vasonicit etc. also are used as blood lipid-lowering medicine widely.
Epoxy chloropropane is a kind of activating reagent commonly used, can act on hydroxyl, amino, carboxylic acid group, sulfydryl isoreactivity group.Use the hydroxyl of Epichlorohydrin activation dextran among the present invention, use epoxy group(ing) and niacin compound serving to carry out crosslinked.
Summary of the invention
The purpose of this invention is to provide the method for preparing small molecules dextran-nicotinic acid polymkeric substance, that the present invention designs is ingenious, mild condition, easy to operate, cost is low, environmental pollution is little, be suitable for large-scale application.
To achieve these goals, technical scheme of the present invention: the preparation method of a kind of LMD with hypolipidemic activity-nicotinic acid polymkeric substance may further comprise the steps:
(1) epoxy chloropropane method activation beta-glucan 2000;
(2) utilize niacin compound serving that the beta-glucan 2000 of activation is modified;
(3) modifying after product uses Sephadex G-50 to carry out sieve chromatography removal unreacting substance; Obtain LMD-nicotinic acid polymkeric substance, products therefrom has significant reducing blood-fat ability in mouse experiment, all has higher reducing blood-fat ability than original unmodified beta-glucan and nicotinic acid class material.
Preferably, in step (1), epoxy chloropropane and dextran hydroxyl molar ratio are 6 ︰ 1.
Preferably, the described reaction of step (1) is carried out in 0.8M NaOH solution, and temperature is 40 ℃.
Preferably, in step (2), niacin compound serving and beta-glucan 2000 epoxy group(ing) molar ratios are 2 ︰ 1.
Preferably, the described pH value in reaction of step (2) maintains 12, and temperature is 50 ℃.
The LMD of described preparation-nicotinic acid polymkeric substance has significant reducing blood-fat ability in mouse experiment, the reducing blood-fat ability all is better than beta-glucan and the niacin compound serving of unmodified.
Beneficial effect of the present invention:
1, the present invention activates its hydroxyl by epoxy chloropropane take natural dextran as matrix;
2, the present invention has optimized the ability of its reducing blood-fat by the modification to dextran.
Embodiment
In order more clearly to understand technology contents of the present invention, describe in detail especially exemplified by following examples.
Embodiment 1 epoxy chloropropane and dextran hydroxyl ratio are on modifying the impact of rear epoxy group(ing) density
:
Beta-glucan 2000 is dissolved in 0.8M NaOH solution, reach 20g/L, add epoxy chloropropane according to dextran and epoxy chloropropane hydroxyl mol ratio (1:1,1:2,1:4,1:6,1:8,1:10), 40 ℃, 50 r/min vibration fixedly 1-4 hour.Mixture adds the ethanol of precooling, centrifugal 5 min of 12000 rpm behind static 10 min, and after the taking-up precipitation, with 3 final vacuum dryings of ethanol cleaning of precooling, the dextran of activation is dissolved with tri-distilled water, measures epoxy group(ing) density, the results are shown in Table 1
Table 1 epoxy chloropropane and dextran hydroxyl molar ratio are on modifying the impact of rear epoxy group(ing) density
| Beta-glucan 2000 and epoxy chloropropane hydroxyl mol ratio | Epoxy group(ing) density (μ mol/g) |
| 1:1 | 0.3 |
| 1:2 | 0.7 |
| 1:4 | 1.1 |
| 1:6 | 1.5 |
| 1:8 | 1.4 |
| 1:10 | 1.3 |
The dextran that embodiment 2 prepares-nicotinic acid polymkeric substance is on the impact of lipid of mice:
Set up the hyperlipidemia mouse model, get 10 of male mice in kunming, high lipid food (the every kg prescription of high lipid food: formed by 840 g basal feeds, the commercially available lard of 100 g, 10 g cholesterol, 50 g egg yolks of feeding and preparing voluntarily, other adds the abundant stirring and evenly mixing of an amount of tap water, granulation shape).Detect respectively on morphology and in the serum after 6 weeks, the result compares with the normal group mouse, and total cholesterol level all obviously raises in model group with hyperlipemia mouse quality and the serum.
Male mice in kunming is divided into 4 groups at random, is respectively normal group: mouse feeds with basal feed, and gavage 9 g/L NaCl solution; Model group with hyperlipemia: mouse feeds the high lipid food of preparing with voluntarily, and gavage 9 g/ L NaCl solution; The nicotinic acid control group: mouse feeds with high lipid food, and gavage 15 g/ L nicotinic acid aquas; Methoxy pyrazine control group: mouse feeds with high lipid food, and gavage 15 g/ L methoxy pyrazine aquas; The dextran control group: mouse feeds with high lipid food, and gavage 20 g/ L dextran aquas; Dextran-nicotinic acid group: mouse feeds with high lipid food, and gavage 15 g/ L dextran-nicotinic acid aquas; Dextran-methoxy pyrazine group: mouse feeds with high lipid food, and gavage 15 g/ L dextran-methoxy pyrazine aqua; Every group of 10 mouse, each organizes the equal ad lib of mouse, and aqua and NaCl solution gavage amount are 0.4 mL/ (d is only), continue to raise for 6 weeks.After each was organized mouse and raises 6 fasting at weekend, 12 h, eyeball was got blood, isolates serum, measured and respectively organized total cholesterol in the mice serum (T C), high density lipoprotein cholesterol fat (HDL-C) the results are shown in Table 2.
Table 2 dextran-nicotinic acid polymkeric substance is on the impact of lipid of mice
| Group | TC/（mmol/L） | HDL-C/（mmol/L） |
| Normal group | 3.25±0.19 | 2.09±0.14 |
| Model group with hyperlipemia | 6.32±0.22 | 2.67±0.17 |
| The nicotinic acid control group | 5.74±0.25 | 2.51±0.15 |
| The dextran control group | 5.87±0.16 | 2.59±0.13 |
| Dextran-nicotinic acid group | 4.43±0.21 | 2.32±0.24 |
| Dextran-methoxy pyrazine group | 4.51±0.18 | 2.39±0.19 |
As can be seen from the above embodiments, adopt dextran and the nicotinic acid class material of the reducing blood-fat ability contrast unmodified of method dextran of the present invention-nicotinic acid polymkeric substance in mouse model, be significantly improved.TC(mmol/L) be down to about 4.5 from 6.32.Therefore, employing the present invention can significantly put forward the reducing blood-fat ability of dextran, and further using for this its provides solid basis.
To sum up, ingenious, the mild condition of dextran of the present invention-nicotinic acid polymkeric substance method design, easy to operate, cost is low, environmental pollution is little, be suitable for large-scale application.
In this specification sheets, the present invention is described with reference to its specific embodiment.But, still can make various modifications and conversion obviously and not deviate from the spirit and scope of the present invention.Therefore, specification sheets is regarded in an illustrative, rather than a restrictive.
Claims (1)
1. the preparation method of the LMD with hypolipidemic activity-nicotinic acid polymkeric substance is characterized in that step is:
(1) epoxy chloropropane method activation beta-glucan 2000: use the epoxy chloropropane of 6 times of beta-glucan 2000 hydroxyls, activate in the solution of 0.8M NaOH, temperature is 40 ℃;
(2) utilize niacin compound serving that the beta-glucan 2000 of activation is modified: with Dextran 200 0 activation products of step (1) gained and nicotinic acid or the coupling of nicotinic acid derivates methoxy pyrazine of twice epoxide equivalent, modifier and beta-glucan 2000 epoxy group(ing) molar ratios are 2 ︰ 1, the modification reaction condition is pH12, and temperature is 50 ℃;
(3) modifying after product uses Sephadex G-50 to carry out sieve chromatography removal unreacting substance; Obtain LMD-nicotinic acid polymkeric substance, products therefrom has significant reducing blood-fat ability in mouse experiment, all has higher reducing blood-fat ability than original unmodified beta-glucan and nicotinic acid class material.
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106084083A (en) * | 2016-07-05 | 2016-11-09 | 潍坊医学院 | A kind of marine algae polysaccharide derivant and preparation method thereof |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1998008603A1 (en) * | 1996-08-30 | 1998-03-05 | Upfront Chromatography A/S | Isolation of immunoglobulins |
| CN1342170A (en) * | 1999-02-05 | 2002-03-27 | 维特罗莱夫英国有限公司 | Process for cross-linking hyaluronic acid to polymers |
| US6365186B1 (en) * | 1997-11-05 | 2002-04-02 | Geltex Pharmaceuticals, Inc. | Combination therapy for treating hypercholesterolemia |
| CN101095964A (en) * | 2006-06-26 | 2008-01-02 | 房新雨 | Method for preparing glucosan gel rubber embolism microsphere suspending liquid |
-
2012
- 2012-12-21 CN CN2012105609017A patent/CN103030713A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1998008603A1 (en) * | 1996-08-30 | 1998-03-05 | Upfront Chromatography A/S | Isolation of immunoglobulins |
| US6365186B1 (en) * | 1997-11-05 | 2002-04-02 | Geltex Pharmaceuticals, Inc. | Combination therapy for treating hypercholesterolemia |
| CN1342170A (en) * | 1999-02-05 | 2002-03-27 | 维特罗莱夫英国有限公司 | Process for cross-linking hyaluronic acid to polymers |
| CN101095964A (en) * | 2006-06-26 | 2008-01-02 | 房新雨 | Method for preparing glucosan gel rubber embolism microsphere suspending liquid |
Non-Patent Citations (2)
| Title |
|---|
| CHUAN-XIN ZHANG, ZE-MEI GE, TIE-MING CHENG AND RUN-TAO LI: "Synthesis and analgesic activity of secondary amine analogues of pyridylmethylamine and positional isomeric analogues of ABT-594", 《BIOORGANIC & MEDICINAL CHEMISTRY LETTERS》, no. 16, 31 December 2006 (2006-12-31), pages 2013 - 2015 * |
| MANUEL SBNCHEZ-CHAVES: "Preparation of dextran-bioactive compound adducts by the direct esterification of dextran with bioactive carboxylic acids", 《POLYMER》, vol. 10, no. 38, 31 December 1997 (1997-12-31), pages 2501 - 2502 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106084083A (en) * | 2016-07-05 | 2016-11-09 | 潍坊医学院 | A kind of marine algae polysaccharide derivant and preparation method thereof |
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