CN104510759A - Medicinal use of gilt-edged leech - Google Patents
Medicinal use of gilt-edged leech Download PDFInfo
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- CN104510759A CN104510759A CN201410109937.2A CN201410109937A CN104510759A CN 104510759 A CN104510759 A CN 104510759A CN 201410109937 A CN201410109937 A CN 201410109937A CN 104510759 A CN104510759 A CN 104510759A
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- hirudo
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Abstract
The invention relates to a new use of gilt-edged leech in gout prevention and treatment. Researches find that the gilt-edged leech has strong gout resistance, 1.50g medicine/kg can substantially reduce the level in uric acid in serum of a hyperuricemia mouse, 3.00g medicine/kg and 1.50 medicine/kg respectively substantially reduce the level of uric acid in the serum of a normal mouse, and the medicine can substantially inhibit toe swelling induced by sodium urate, has a pain easing effect and has small toxic side effects. The maximal tolerance dose of mice gavaged with gilt-edged leech powder is 23.09g medicine/kg body weight. The medicine can be used to prepare oral gout resistant medicines and health products.
Description
Technical field
The invention belongs to a kind of Chinese medicine powder---golden-rimmed Hirudo powder, proves to have new medical usage through pharmacological evaluation.Be the generation that golden-rimmed Hirudo powder significantly can suppress hyperuricemia mouse blood uric acid specifically, significantly reduce normal mouse blood uric acid levels; Significantly can suppress the toes swelling of being induced by Monosodium urate, have analgesic activity, toxic and side effects is little.The maximum tolerated dose of the golden-rimmed Hirudo powder of mouse gavaging is 23.09g medical material/kg body weight.Belong to the field of Chinese medicines.
Background technology
Gout (gout) is a kind of ancient disease, gout one word originates from Latin (gutta), at the synonym that the middle ancient times are foot pain (podagra) in medical science, its implication is that body fluid (juice) dirty one-tenth drips, and is the pernicious body fluid in infringement, weak joint.Modern medicine is thought, gout causes blood uric acid to raise with purine metabolism or abevacuation, and is the metabolic disease of feature with Monosodium urate crystallization calmness in connective tissue.In the past, gout is quite common in American-European countries, the rare Case report of China.And now, along with China's economic development, growth in the living standard, the change of people's dietary structure, the obvious increase of purine content in food, the sickness rate of gout sharply rises.According to estimates, the current patient with gout of China is about more than 1,200 ten thousand, and the too high person of Level of Serum Uric Acid about has 1.2 hundred million (accounting for 9% of population), and in 20-30 in the future, gout will become No. second metabolic disease being only second to diabetes in China.Gout not only can cause gouty arthritis, the decline of quality of life, even disabled, but also is the risk factor causing nephropathy, diabetes, cardiovascular disease, malignant tumor, parkinson etc.
The Western medicine mainly selected when gout acute attack has: colchicine, nonsteroidal anti-inflammatory agent (NSAIDs), adrenocortical hormone, analgesic etc.But although these medicine anti-inflammatory analgetic effects are fast, medical expense is high, does not have uric acid resisting effect while anti-inflammatory analgesic, and most drug toxic and side effects is quite obvious; Suppress uricopoiesis medicine allopurinol etc., be applicable to uricopoiesis too much, invalid or irritated by uricosuric, renal hypofunction or the person that has lithangiuria, have synergism with uricosuric, untoward reaction has heating, erythra, gastrointestinal reaction, liver function and bone marrow damage.Therefore, the anti-gout drugs developing high-efficiency low-toxicity is still the focus of study of pharmacy.
The drying of golden-rimmed Hirudo Xi Yi trematodiasis section animal Hirudinaria manillensis Poecilobdella manillensis Lesson is all, is conventional strong medicine, has removing blood stasis and stimulate the menstrual flow, and removing blood stasis disappears the merit of abdominal mass, is used for the treatment of blood stasis amenorrhea, lump in the abdomen mass in the abdomen, apoplectic hemiplegia, the diseases such as osteopatia sprain
[3].Modern pharmacology research shows, golden-rimmed Hirudo has the physiologically actives such as stronger anticoagulation, antithrombotic, antiplatelet aggregation, blood fat reducing
[4-6].But have no the report for the treatment of gout.
Summary of the invention
The object of this invention is to provide and a kind of there is active high, golden-rimmed Hirudo powder that toxic and side effects is little.For the preparation of anti-antipodagric medicine and health product.
Through a large amount of experiments, we find, golden-rimmed Hirudo powder not only has the pharmacological action of above report, the gout effect that also tool is very strong, 1.50g medical material/kg significantly can reduce hyperuricemia mice serum uric acid level, 3.00g medical material/kg, 1.50g medical material/kg all can significantly reduce Normal Mouse Serum uric acid level, significantly can suppress the toes swelling of being induced by Monosodium urate, have analgesic activity, toxic and side effects is little.The maximum tolerated dose of the golden-rimmed Hirudo powder of mouse gavaging is 23.09g medical material/kg body weight.Demonstrate feature that is efficient, low toxicity, demonstrate great development prospect.
Concrete facts mode
The golden-rimmed Hirudo of the extraction of the golden-rimmed Hirudo powder of embodiment 1: 1000g, lyophilizing processing and fabricating forms.
The studies on acute toxicity of the golden-rimmed Hirudo powder of embodiment 2
Choose healthy adult mice 40, observe 3d, be then divided into 2 groups at random, i.e. Normal group (giving isopyknic distilled water), golden-rimmed Hirudo group, often organize 20, male and female half and half.Gavage gives Cmax, the golden-rimmed Hirudo of maximum volume, then observes 14d.Observe the diet situation of mice, body weight, signs of toxicity (comprising outward appearance behavior, secretions, excretion thing etc.) and death condition, after 14d, put to death mice, dissect the state that mice observes major organs.
10min after gavage, all there is exception in contrast and golden-rimmed Hirudo group mice.In 14d, all mices occur without death, diet, outward appearance, behavior, secretions, excretion thing are all without exception, the normal growth of Mouse Weight is not made significant difference, after golden-rimmed Hirudo powder 14d, put to death mice, the situation of anatomic observation main organs, all without exception with main organs volume, color, the quality such as Normal group golden-rimmed Hirudo group mouse core, liver, lung, the mice maximum tolerated dose of golden-rimmed Hirudo is 23.09g medical material/kg body weight.Be equivalent to 138.54 times of quantity, it is safe that golden-rimmed Hirudo is applied in range of doses.
The golden-rimmed Hirudo of embodiment 3 is on the impact of uric acid level
Golden-rimmed Hirudo is on the impact of hyperuricemia mice uric acid
Choose body weight 18 ~ 22g Kunming mouse 60, male and female half and half, be divided into 6 groups at random, often organize 10, i.e. Normal group, model group, positive drug allopurinol tablet (50mg/kg) group, high, medium and low (the 3.00g medical material .kg of golden-rimmed Hirudo
-1, 1.50g medical material .kg
-1, 0.75g medical material .kg
-1) dosage group.Gastric infusion, 1 time/d, Normal group and model group gavage such as to give at the capacity distilled water, continuous 12d.Last administration 1h pneumoretroperitoneum injection hypoxanthine 10mg/kg, after 1h, eyeball gets blood, the centrifugal 10min of 3000r/min, gets supernatant and surveys serum uric acid.
Experimental result shows, compares with Normal group, and model group mice serum uric acid content obviously raises, and has significant difference (P<0.05), prompting modeling success.After giving golden-rimmed Hirudo, compare with model group, golden-rimmed Hirudo 1.50g medical material .kg
-1dosage group can significantly reduce mice serum uric acid content, and difference has significance (P<0.01).In table 1.
The golden-rimmed Hirudo of table 1 is on the impact of the hyperuricemia mice uric acid that hypoxanthine is induced
Note: compare with model group, * * P<0.01, * P<0.05
Golden-rimmed Hirudo is on the impact of normal mouse retention acid
Choose body weight 18 ~ 22g Kunming mouse 40, male and female half and half, be divided into 4 groups at random, often organize 10, i.e. Normal group, high, medium and low (the 3.00g medical material .kg of golden-rimmed Hirudo
-1, 1.50g medical material .kg
-1, 0.75g medical material .kg
-1) dosage group.Gastric infusion, 1 time/d, Normal group and model group gavage such as to give at the capacity distilled water, continuous 12d.Last administration 1h eyeball gets blood, the centrifugal 10min of 3000r/min, gets supernatant and surveys serum uric acid.
Experimental result shows, compares with Normal group, after giving golden-rimmed Hirudo, and golden-rimmed Hirudo 3.00g medical material .kg
-1, 1.50g medical material .kg
-1dosage group all can significantly reduce mice serum uric acid content, and difference has significance (P<0.01).In table 2.
The golden-rimmed Hirudo of table 2 is on the impact of normal mouse retention acid
Note: compare with matched group, * * P<0.01, * P<0.05
The golden-rimmed Hirudo of embodiment 4 causes the impact of rat paw edema to micro-crystal type Monosodium urate crystallization (MSU)
[9]
The preparation of MSU: put by 5g uric acid in 1000mL boiling water, adjusts pH to 7.4 with NaOH, is heated to 95 DEG C.Put room temperature condition cooling and stir gently, filter and obtain MSU, MSU being placed in 200 DEG C of high temperature sterilizes, facing the suspension that the used time is made into 100mg/mL with physiological saline solution for subsequent use.
Choose body weight 180 ~ 220g Wistar male rat 50, be divided into 5 groups at random, often organize 10, i.e. Normal group, model group, positive drug allopurinol tablet group (20mg/kg), high and low (the 1.50g medical material .kg of golden-rimmed Hirudo
-1, 0.38g medical material .kg
-1) dosage group.Gastric infusion, 1 time/d, Normal group and model group gavage such as to give at the capacity distilled water, continuous 15d.After last administration 1h, causing inflammation in Rat Right metapedes plantar subcutaneous injection 0.15mL MSU (100mg/mL), measuring right back sufficient sole of the foot Zhou Jing respectively at causing scorching front and back.To observe and measure after injection 1h, 2h, 3h, 4h, 5h, 6h, 7h not pedal swelling situation and Zhou Jing thereof after Rat Right in the same time, calculate its swelling.Swelling degree of the paw=(t time Zhou Jing-t
0time Zhou Jing)/t
0time Zhou Jing × 100%.
Result shows, compares with Normal group, and model group rats swelling degree of the paw obviously raises, and has significant difference (P<0.01), prompting modeling success.Compare with model group, golden-rimmed Hirudo 0.75g medical material .kg
-1dosage group significantly can suppress rat paw edema, and difference has significance (P<0.05, P<0.01).The results are shown in Table 3.
The golden-rimmed Hirudo of table 3 causes the impact of rat paw edema on MSU
Note: compare with model group, * * P<0.01, * P<0.05
The analgesic activity of the golden-rimmed Hirudo of embodiment 5
On the impact of the mouse hot-plate threshold of pain by 50 in advance through the female mice (mice of removing irritation <5s and blunt >30s) of screening, be divided into 5 groups at random, i.e. Normal group, positive controls (rotundine, 0.06g.kg
-1), high, medium and low (the 3.00g medical material .kg of golden-rimmed Hirudo
-1, 1.50g medical material .kg
-1, 0.75g medical material .kg
-1) dosage group.Ig administration, gives to wait capacity normal saline according to group to normal.After administration, 60min surveys pain threshold.
Kunming mouse 50 is got in the impact that Dichlorodiphenyl Acetate causes mouse writhing to react, and male and female half and half are divided into 5 groups at random, often organizes 10.Grouping, administration is the same.1h after administration, each Mus lumbar injection 0.6% acetum 0.2ml/ only, count the writhing response number of times that in 10min, each mice occurs after 5min.
Compare with Normal group, each dosage group of golden-rimmed Hirudo does not all significantly improve the mouse hot-plate threshold of pain (P<0.05, P<0.01).
Compare with Normal group, golden-rimmed Hirudo 3.00g medical material .kg
-1, 0.75g medical material .kg
-1dosage group all significantly can reduce acetic acid and cause mouse writhing number of times (P<0.05).The results are shown in Table 4.
The analgesic activity of the golden-rimmed Hirudo of table 4
Note: compare with matched group, * * P<0.01, * P<0.05
Claims (9)
1. a golden-rimmed Hirudo powder for prevention and therapy gout, is characterized in that golden-rimmed Hirudo powder obtains from golden-rimmed Hirudo lyophilizing processing.
2. application according to claim 1, is characterized in that: golden-rimmed Hirudo powder is used for prevention and therapy gout.
3. a golden-rimmed Hirudo powder for prevention and therapy gout, is characterized in that golden-rimmed Hirudo powder obtains from golden-rimmed Hirudo lyophilizing processing.
4. application according to claim 3, is characterized in that: golden-rimmed Hirudo powder is used for prevention and therapy gout.
5. the application according to claim 1,2,3,4, is characterized in that: the golden-rimmed Hirudo powder containing therapeutic dose and one or more pharmaceutically acceptable drug excipients, or the preparation can made with the other medicines of golden-rimmed Hirudo powder prescription.
6. pharmaceutical preparation according to claim 5, is characterized in that preferably containing the golden-rimmed Hirudo powder of 1%-99% and 99%-1% pharmaceutical excipient, or other can the medicine of prescription.Preferably containing the golden-rimmed Hirudo powder of 20%-60% and 80%-40% pharmaceutical excipient, or other can the medicine of prescription.Preferably select the golden-rimmed Hirudo powder containing 30%-70% and 70%-30% pharmaceutical excipient, or other can the medicine of prescription.
7. pharmaceutical preparation according to claim 5, is characterized in that said medicine is the dosage form of oral formulations.
8. require described pharmaceutical preparation according to right 7, it is characterized in that said oral formulations is selected from tablet, pill, capsule, soft capsule, granule, suspensoid, drop, any one in the middle of oral liquid.
9. the pharmaceutical excipient according to claim 1,2,3,4 comprises filler, disintegrating agent etc., and filler is selected from starch, lactose, microcrystalline Cellulose, dextrin, calcium phosphate etc.; Disintegrating agent is selected from sodium carboxymethyl cellulose, hyprolose, polyvinylpolypyrrolidone; Also can select and add adhesive, wetting agent and lubricant.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410109937.2A CN104510759A (en) | 2014-03-24 | 2014-03-24 | Medicinal use of gilt-edged leech |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410109937.2A CN104510759A (en) | 2014-03-24 | 2014-03-24 | Medicinal use of gilt-edged leech |
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| CN104510759A true CN104510759A (en) | 2015-04-15 |
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|---|---|---|---|
| CN201410109937.2A Pending CN104510759A (en) | 2014-03-24 | 2014-03-24 | Medicinal use of gilt-edged leech |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107998385A (en) * | 2017-12-08 | 2018-05-08 | 广西卫生职业技术学院 | Purposes of the hirudin as prevention antihyperuricemic disease drug |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1557446A (en) * | 2004-01-15 | 2004-12-29 | 广州敬修堂（药业）股份有限公司 | Compound medicine for treating gout |
| CN101406584A (en) * | 2008-11-27 | 2009-04-15 | 蒋月芝 | Agent for treating gout |
| CN102362995A (en) * | 2011-11-28 | 2012-02-29 | 山东中医药大学附属医院 | Chinese medicinal preparation for treating acute gouty arthritis, and preparation method thereof |
-
2014
- 2014-03-24 CN CN201410109937.2A patent/CN104510759A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1557446A (en) * | 2004-01-15 | 2004-12-29 | 广州敬修堂（药业）股份有限公司 | Compound medicine for treating gout |
| CN101406584A (en) * | 2008-11-27 | 2009-04-15 | 蒋月芝 | Agent for treating gout |
| CN102362995A (en) * | 2011-11-28 | 2012-02-29 | 山东中医药大学附属医院 | Chinese medicinal preparation for treating acute gouty arthritis, and preparation method thereof |
Non-Patent Citations (2)
| Title |
|---|
| 修霞等: "水蛭化学成分及其药理作用探讨综述", 《中国热带医学》 * |
| 苏承武等: "天然水蛭素冻干粉实验结果的分析", 《蛇志》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107998385A (en) * | 2017-12-08 | 2018-05-08 | 广西卫生职业技术学院 | Purposes of the hirudin as prevention antihyperuricemic disease drug |
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Application publication date: 20150415 |