CN101152201A - Application of isoquercitrin in preparation of drugs for preventing and/or treating depression - Google Patents
Application of isoquercitrin in preparation of drugs for preventing and/or treating depression Download PDFInfo
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- CN101152201A CN101152201A CNA2006101527173A CN200610152717A CN101152201A CN 101152201 A CN101152201 A CN 101152201A CN A2006101527173 A CNA2006101527173 A CN A2006101527173A CN 200610152717 A CN200610152717 A CN 200610152717A CN 101152201 A CN101152201 A CN 101152201A
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- isoquercitrin
- antidepressant drug
- new purposes
- pharmaceutically acceptable
- drugs
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- OVSQVDMCBVZWGM-IDRAQACASA-N Hirsutrin Natural products O([C@H]1[C@H](O)[C@H](O)[C@H](O)[C@@H](CO)O1)C1=C(c2cc(O)c(O)cc2)Oc2c(c(O)cc(O)c2)C1=O OVSQVDMCBVZWGM-IDRAQACASA-N 0.000 title claims abstract description 29
- FVQOMEDMFUMIMO-UHFFFAOYSA-N Hyperosid Natural products OC1C(O)C(O)C(CO)OC1OC1C(=O)C2=C(O)C=C(O)C=C2OC1C1=CC=C(O)C(O)=C1 FVQOMEDMFUMIMO-UHFFFAOYSA-N 0.000 title claims abstract description 29
- GXMWXESSGGEWEM-UHFFFAOYSA-N isoquercitrin Natural products OCC(O)C1OC(OC2C(Oc3cc(O)cc(O)c3C2=O)c4ccc(O)c(O)c4)C(O)C1O GXMWXESSGGEWEM-UHFFFAOYSA-N 0.000 title claims abstract description 29
- OVSQVDMCBVZWGM-QSOFNFLRSA-N quercetin 3-O-beta-D-glucopyranoside Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1OC1=C(C=2C=C(O)C(O)=CC=2)OC2=CC(O)=CC(O)=C2C1=O OVSQVDMCBVZWGM-QSOFNFLRSA-N 0.000 title claims abstract description 29
- 239000003814 drug Substances 0.000 title claims abstract description 9
- 229940079593 drug Drugs 0.000 title abstract description 6
- 239000000725 suspension Substances 0.000 claims description 5
- 208000020401 Depressive disease Diseases 0.000 claims description 3
- 239000002552 dosage form Substances 0.000 claims description 3
- 230000002265 prevention Effects 0.000 claims description 3
- 239000002775 capsule Substances 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 238000002347 injection Methods 0.000 claims description 2
- 239000007924 injection Substances 0.000 claims description 2
- 239000007788 liquid Substances 0.000 claims description 2
- 239000003826 tablet Substances 0.000 claims description 2
- 239000000935 antidepressant agent Substances 0.000 claims 6
- 150000002148 esters Chemical class 0.000 claims 3
- 229930182470 glycoside Natural products 0.000 claims 3
- 150000002338 glycosides Chemical class 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 1
- 239000000243 solution Substances 0.000 claims 1
- 241000699670 Mus sp. Species 0.000 description 11
- 238000002474 experimental method Methods 0.000 description 6
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 5
- RTHCYVBBDHJXIQ-MRXNPFEDSA-N (R)-fluoxetine Chemical compound O([C@H](CCNC)C=1C=CC=CC=1)C1=CC=C(C(F)(F)F)C=C1 RTHCYVBBDHJXIQ-MRXNPFEDSA-N 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- 229960002464 fluoxetine Drugs 0.000 description 4
- 230000009182 swimming Effects 0.000 description 4
- 238000012360 testing method Methods 0.000 description 4
- 241000581650 Ivesia Species 0.000 description 3
- 241000699666 Mus <mouse, genus> Species 0.000 description 3
- 230000037396 body weight Effects 0.000 description 3
- 201000010099 disease Diseases 0.000 description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
- 241001465754 Metazoa Species 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 238000007796 conventional method Methods 0.000 description 2
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 description 1
- 206010010144 Completed suicide Diseases 0.000 description 1
- 239000004677 Nylon Substances 0.000 description 1
- 229940124532 absorption promoter Drugs 0.000 description 1
- -1 absorption promoters Substances 0.000 description 1
- 230000003078 antioxidant effect Effects 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- 239000006071 cream Substances 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 230000002526 effect on cardiovascular system Effects 0.000 description 1
- 239000000945 filler Substances 0.000 description 1
- 235000003599 food sweetener Nutrition 0.000 description 1
- 239000003205 fragrance Substances 0.000 description 1
- 230000009760 functional impairment Effects 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- VNWKTOKETHGBQD-UHFFFAOYSA-N methane Chemical compound C VNWKTOKETHGBQD-UHFFFAOYSA-N 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 239000000178 monomer Substances 0.000 description 1
- 208000031225 myocardial ischemia Diseases 0.000 description 1
- 229920001778 nylon Polymers 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 235000019353 potassium silicate Nutrition 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 230000005180 public health Effects 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- NTHWMYGWWRZVTN-UHFFFAOYSA-N sodium silicate Chemical compound [Na+].[Na+].[O-][Si]([O-])=O NTHWMYGWWRZVTN-UHFFFAOYSA-N 0.000 description 1
- 238000001179 sorption measurement Methods 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
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- Medicinal Preparation (AREA)
Abstract
本发明公开了异槲皮苷的一种新用途，即异槲皮苷在预防和/或治疗抑郁症药物中的应用。The invention discloses a new application of isoquercitrin, that is, the application of isoquercitrin in drugs for preventing and/or treating depression.
Description
技术领域technical field
本发明涉及异槲皮苷的一种新用途，特别是涉及异槲皮苷在制备预防和/或治疗抑郁症药物中的应用。The present invention relates to a new application of isoquercitrin, in particular to the application of isoquercitrin in the preparation of drugs for preventing and/or treating depression.
背景技术Background technique
由于现代社会经济的高速发展与精神需求的显著增强，抑郁症发生率逐年提高。在过去10年中，抑郁症已成为世界上最普遍的公共卫生疾病之一。人在一生中患抑郁症可能性是10％-25％，其最严重后果是自杀，每年超过100万人。根据世界精神病协会年会上发表的数字，目前全球抑郁症患者每年以113％的增长率逐渐增加，抑郁症已成为“21世纪的流行病”。WHO公布的关于“疾病负担”的调查表明，以因病造成的伤残(功能缺损)统计，抑郁症目前占第二位，仅次于慢性阻塞性肺部疾病(到2020年将仅次于缺血性心脏病)。Due to the rapid development of modern social economy and the significant enhancement of spiritual needs, the incidence of depression has increased year by year. Over the past 10 years, depression has become one of the most prevalent public health diseases in the world. The possibility of people suffering from depression in their lifetime is 10%-25%, and its most serious consequence is suicide, which exceeds 1 million people every year. According to the figures published at the annual meeting of the World Psychiatric Association, the number of patients with depression worldwide is gradually increasing at a rate of 113% every year, and depression has become "the epidemic of the 21st century". According to the survey on "burden of disease" released by WHO, depression currently ranks second in terms of disability (functional impairment) caused by disease, second only to chronic obstructive pulmonary disease (by 2020 it will be second only to ischemic heart disease).
目前，已报道的异槲皮苷主要作用是对肝和抗氧化作用及对心血管的作用。At present, the main effects of isoquercitrin have been reported on the liver and antioxidant effects and the cardiovascular effects.
发明内容Contents of the invention
本发明的目的是提供异槲皮苷的一种新用途。The purpose of the present invention is to provide a new application of isoquercitrin.
本发明发明人的研究表明，异槲皮苷具有预防和/或治疗抑郁症的作用。The research of the inventors of the present invention shows that isoquercitrin has the effect of preventing and/or treating depression.
上述异槲皮苷可为市售异槲皮苷也可按常规方法进行制备。The above-mentioned isoquercitrin can be commercially available isoquercitrin or can be prepared according to conventional methods.
需要的时候，在上述药物中还可以加入一种或多种药学上可接受的载体。所述载体包括药学领域常规的稀释剂、赋形剂、填充剂、粘合剂、湿润剂、崩解剂、吸收促进剂、表面活性剂、吸附载体、润滑剂等，必要时还可以加入香味剂、甜味剂等。When necessary, one or more pharmaceutically acceptable carriers can also be added to the above drugs. The carrier includes conventional diluents, excipients, fillers, binders, wetting agents, disintegrating agents, absorption promoters, surfactants, adsorption carriers, lubricants, etc. in the pharmaceutical field, and fragrances can also be added if necessary agents, sweeteners, etc.
本发明的药物可以制成注射剂、片剂、粉剂、粒剂、胶囊、口服液、膏剂、霜剂等多种形式。上述各种剂型的药物均可以按照药学领域的常规方法制备。The medicine of the present invention can be made into multiple forms such as injections, tablets, powders, granules, capsules, oral liquids, ointments, and creams. The above-mentioned medicines in various dosage forms can be prepared according to conventional methods in the field of pharmacy.
上述药物的用量一般为0.1-0.6mg异槲皮苷/kg体重/天。The dosage of the above-mentioned drugs is generally 0.1-0.6 mg isoquercitrin/kg body weight/day.
在对比实验中，发现给小白鼠口服三七总皂苷及其单体，可以显著改善小鼠强制游泳试验和悬尾试验中的不动时间，将在抑郁症的预防和/或治疗中发挥重要的作用。In a comparative experiment, it was found that oral administration of Panax notoginseng saponins and its monomers to mice can significantly improve the immobility time in the forced swimming test and tail suspension test of mice, which will play an important role in the prevention and/or treatment of depression. role.
具体实施方式Detailed ways
实施例1、小鼠强迫游泳实验Embodiment 1, mouse forced swimming experiment
采用小鼠抑郁模型-强迫游泳实验(FST)，具体：Using the mouse depression model-forced swimming test (FST), specifically:
ICR雄性小鼠，体重18-20g，饲养稳定三天，自由进食，50只小鼠，随机均分为5组：空白(水10ml/kg)阳性(氟西汀)和五个不同剂量异槲皮苷，各组均灌胃给药。实验开始前30分钟给药，然后将小鼠放入直径10cm，内有25℃，10cm高的水玻璃缸中游泳6min，记录后4min的不动时间。比较给药组的不动时间与空白组是否有显著性差异。结果如表1所示，表明各组与空白组相比有显著性差异，可以显著改善小鼠强制游泳实验的不动时间。ICR male mice, body weight 18-20g, fed for three days, free to eat, 50 mice were randomly divided into 5 groups: blank (water 10ml/kg) positive (fluoxetine) and five different doses of isoquer Dermatosin, each group were administered intragastrically. Administration was administered 30 minutes before the start of the experiment, and then the mice were put into a 10cm-diameter, 25°C, 10cm-high water glass tank to swim for 6 minutes, and the immobility time of the last 4 minutes was recorded. Compare whether there is a significant difference between the immobility time of the administration group and the blank group. The results are shown in Table 1, indicating that each group has a significant difference compared with the blank group, and can significantly improve the immobility time of the mouse forced swimming test.
表1.异槲皮苷对强制小鼠游泳不动时间影响的比较Table 1. Comparison of the effect of isoquercitrin on the immobility time of forced mice to swim
实施例2、小鼠悬尾实验Embodiment 2, mouse tail suspension experiment
采用小鼠悬尾实验对实施例1的结果进行验证，实验方法如下：The results of Example 1 were verified by mouse tail suspension experiment, and the experimental method was as follows:
ICR雄性小鼠，ICR雄性小鼠，体重18-20g，饲养稳定三天，自由进食，50只小鼠，随机均分为5组：空白(水10ml/kg)阳性(氟西汀)和五个不同剂量异槲皮苷。各组均灌胃给药。给药30min后，用尼龙绳系住小鼠尾端1cm处，将其倒挂在距底面15cm处，观察小鼠6min内的绝对不动时间，比较给药组与空白组(10ml水/kg)不动时间是否存在显著性差异。结果如表2示，ICR male mice, ICR male mice, body weight 18-20g, feeding stable for three days, free to eat, 50 mice were randomly divided into 5 groups: blank (water 10ml/kg) positive (fluoxetine) and five different doses of isoquercitrin. All groups were intragastrically administered. After 30 minutes of administration, tie the mouse tail 1cm with a nylon rope, hang it upside down at 15cm from the bottom, observe the absolute immobility time of the mice within 6 minutes, and compare the administration group with the blank group (10ml water/kg) Is there any significant difference in immobility time. The results are shown in Table 2,
表2.异槲皮苷对小鼠悬尾不动时间影响的比较Table 2. Comparison of the effects of isoquercitrin on tail suspension time in mice
Claims (5)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2006101527173A CN101152201A (en) | 2006-09-25 | 2006-09-25 | Application of isoquercitrin in preparation of drugs for preventing and/or treating depression |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2006101527173A CN101152201A (en) | 2006-09-25 | 2006-09-25 | Application of isoquercitrin in preparation of drugs for preventing and/or treating depression |
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| Publication Number | Publication Date |
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| CN101152201A true CN101152201A (en) | 2008-04-02 |
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| CNA2006101527173A Pending CN101152201A (en) | 2006-09-25 | 2006-09-25 | Application of isoquercitrin in preparation of drugs for preventing and/or treating depression |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111821312A (en) * | 2020-09-08 | 2020-10-27 | 广州中医药大学第一附属医院 | Use of isoquercitrin in the preparation of medicines and/or health care products against myelosuppressive cells |
-
2006
- 2006-09-25 CN CNA2006101527173A patent/CN101152201A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111821312A (en) * | 2020-09-08 | 2020-10-27 | 广州中医药大学第一附属医院 | Use of isoquercitrin in the preparation of medicines and/or health care products against myelosuppressive cells |
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| PB01 | Publication | ||
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| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
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Open date: 20080402 |