CN103356677B - Houttuynoid D treats in preparation or prevents the application in the medicine of acute heart failure - Google Patents
Houttuynoid D treats in preparation or prevents the application in the medicine of acute heart failure Download PDFInfo
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- CN103356677B CN103356677B CN201310256903.1A CN201310256903A CN103356677B CN 103356677 B CN103356677 B CN 103356677B CN 201310256903 A CN201310256903 A CN 201310256903A CN 103356677 B CN103356677 B CN 103356677B
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- 0 CCCCCCCCCC(Cc(c(O)c(cc1)O)c1C(Oc1cc(*)cc(O)c1C1=O)=C1OC(C(C1O)O)OC(C*)C1O)OC Chemical compound CCCCCCCCCC(Cc(c(O)c(cc1)O)c1C(Oc1cc(*)cc(O)c1C1=O)=C1OC(C(C1O)O)OC(C*)C1O)OC 0.000 description 1
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Abstract
Do you the invention provides Houttuynoid? D treats in preparation or prevents the application in the medicine of heart failure.The Houttuynoid that the present invention relates to? the purposes of D in preparation treatment acute heart failure medicine belongs to first public, because framework types belongs to brand-new framework types, and the activity of its treatment acute heart failure is unexpectedly strong, there is not the possibility being provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, be used for the treatment of acute heart failure simultaneously and obviously there is significant progress.
Description
Invention field
The present invention relates to HouttuynoidD treat in preparation or prevent the application in the medicine of acute heart failure.
Background technology
Heart failure (hearfailure, HF) refers to that cardiac function is abnormal and causes heart pump blood volume can not meet a kind of pathological and physiological condition of tissue metabolism's needs.Cause of disease inducement causes structure function low and Progressive symmetric erythrokeratodermia morbidity because cardiac overload, cardiac muscle itself, the limited any reason of diastole cause initial myocardial damage; And infect, anemia, gestation, childbirth, cardiac arrhythmia, pulmonary infarction, hyperthyroidism, diabetes, suppression heart medicine bring out and increase the weight of HF.Pathogeny thinks that the mechanism that HF occurs to develop is abnormal hemodynamics in the past; The later stage eighties 20th century recognizes that the activation of nerve-endocrine hormone plays an important role (sympathetic ↑ NE ↑ RAS ↑ wait activation); Specify that after the nineties that " Myocardial Remodeling " (remodelling) is the fundamental mechanism causing the generation of heart failure to develop gradually.
The compound H outtuynoidD that the present invention relates to is one and delivers (Chen in 2012, S.D.etal., 2012.HouttuynoidA-E, Anti-HerpesSimplexVirusActiveFlavonoidswithNovelSkeleton sfromHouttuyniacordata.OrganicLetters14 (7), 1772 – 1775.) New skeleton compound, this compound has brand-new framework types, current purposes only relates to anti-herpes simplex virus activity (Chen, S.D.etal., 2012.HouttuynoidA-E, Anti-HerpesSimplexVirusActiveFlavonoidswithNovelSkeleton sfromHouttuyniacordata.OrganicLetters14 (7), 1772 – 1775.), the purposes of the HouttuynoidD that the present invention relates in preparation treatment acute heart failure medicine is belonged to first public, because framework types belongs to brand-new framework types, and the activity of its treatment acute heart failure is unexpectedly strong, there is not the possibility being provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, be used for the treatment of acute heart failure simultaneously and obviously there is significant progress.
Summary of the invention
The invention provides HouttuynoidD treat in preparation or prevent the application in the medicine of acute heart failure.
Described compound H outtuynoidD structure is as shown in formula I:
The purposes of the HouttuynoidD that the present invention relates in preparation treatment acute heart failure medicine belongs to first public, because framework types belongs to brand-new framework types, and the activity of its treatment acute heart failure is unexpectedly strong, there is not the possibility being provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, be used for the treatment of acute heart failure simultaneously and obviously there is significant progress.
Detailed description of the invention
The preparation method of compound H outtuynoidD involved in the present invention is see document (Chen, S.D.etal., 2012.HouttuynoidA-E, Anti-HerpesSimplexVirusActiveFlavonoidswithNovelSkeleton sfromHouttuyniacordata.OrganicLetters14 (7), 1772 – 1775.).
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not by any restriction of specific embodiment, but be limited by claim.
Embodiment 1: the preparation of compound H outtuynoidD tablet involved in the present invention:
Get 20 g of compound HouttuynoidD, add the customary adjuvant 180 grams preparing tablet, mixing, conventional tablet presses makes 1000.
Embodiment 2: the preparation of compound H outtuynoidD capsule involved in the present invention:
Get 20 g of compound HouttuynoidD, add prepare capsule customary adjuvant as starch 180 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Test example: HouttuynoidD is to the therapeutical effect of dog acute heart failure
1 material animal health adult dogs body weight 12.5 ~ 13.5kg.Pentobarbital sodium (Sigma, import subpackage, specification: 25g); Instrument U.S. BIC16 leads physiograph (production of BIC Corp. of the U.S.); Electromagnetic flowmeter (MFV-3200 type): Japanese photoelectricity company produces.
2 test methods and result
Dog is divided at random NS group (waiting capacity solvent), gastric infusion HouttuynoidD2.0mg/kg group, 1.0mg/kg group, 0.2mg/kg group, often organizes 6.Fasting is after 12 hours, and intravenous injection pentobarbital sodium 40mg/kg anaesthetizes, tracheal intubation, artificial respiration, monitoring aortic pressure (AP) and electrocardiogram.Breast is opened in left side, plugs in conduit to left room pressure and rate of pressure change (± dp/dt thereof from the apex of the heart
max).Waltan-Brodie strain bow is implanted left ventricle antetheca, measures myocardial contraction.With electromagnetic flowmeter determination ascending aorta blood flow.Using ascending aorta flow as cardiac output (CO), calculate cardiac index (CI), index (SI) of often fighting, work done (SW) of often fighting, left heart work done (LVW).Parameters record and BIC physiograph.Postoperative half an hour, parameters reaches stable.From femoral vein constant speed gasing injection pentobarbital sodium (0.5mL/kgmin), with ± dp/dt
maxdropping to about 1000mHg/s is that leading indicator forms acute heart failure.After acute heart failure model stability, each treated animal duodenum gives relative medicine.Between group, T inspection, carries out statistical procedures.
Table 1HouttuynoidD is on the impact (n=6, X ± s) of heart failure canine dp/dt
Compare with NS group,
p<0.05,
p<0.01
Table 2HouttuynoidD is on the impact (n=6, X ± s) of heart failure canine cardiac work
Compare with before administration
*p<0.05,
*p<0.01; Compare with NS group
p<0.05,
p<0.01
Result is as shown in table 1,2, and instillation various dose HouttuynoidD can increase SW, the LVW ,+dp/dt (comparing with model group matched group, p<0.05orp<0.01) of Heart Failure Dogs.Gavage various dose HouttuynoidD can increase SW, the LVW ,+dp/dt (comparing with model group matched group, p<0.01orp<0.05) of Heart Failure Dogs.
Table 3HouttuynoidD is on the kinemic impact of heart failure canine (n=6, X ± s)
Compare with before administration
*p<0.05,
*p<0.01; Compare with NS group
p<0.05,
p<0.01
Result is as shown in table 3, and instillation various dose HouttuynoidD can increase the cardiac output (comparing with model control group, p<0.01orp<0.05) of Heart Failure Dogs.Gavage various dose HouttuynoidD can increase the cardiac output (comparing with model control group, p<0.01orp<0.05) of Heart Failure Dogs.
Conclusion: HouttuynoidD significantly can improve acute heart failure, can be used for preparing the medicine for the treatment of or preventing heart failure.
Claims (1)
1.HouttuynoidD preparation treatment or prevention acute heart failure medicine in application, described compound H outtuynoidD structure as
formula Ishown in:
formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310256903.1A CN103356677B (en) | 2013-06-24 | 2013-06-24 | Houttuynoid D treats in preparation or prevents the application in the medicine of acute heart failure |
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| CN201310256903.1A CN103356677B (en) | 2013-06-24 | 2013-06-24 | Houttuynoid D treats in preparation or prevents the application in the medicine of acute heart failure |
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| CN103356677A CN103356677A (en) | 2013-10-23 |
| CN103356677B true CN103356677B (en) | 2016-02-24 |
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2013
- 2013-06-24 CN CN201310256903.1A patent/CN103356677B/en active Active
Non-Patent Citations (1)
| Title |
|---|
| Houttuynoid A-E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata;CHEN,S.D. et al.,;《ORGANIC LETTERS》;20121231;第14卷(第7期);1772-1775 * |
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Inventor after: Zhu Ping Inventor after: Ding Hao Inventor after: Shu Gang Inventor after: Zhuang Jian Inventor after: Chen Jimei Inventor after: Zhao Mingyi Inventor after: Li Jiaxin Inventor after: Zhu Shuoji Inventor after: Tian Weimao Inventor after: Zhu Xiaolan Inventor after: Li Jiani Inventor before: Ding Shengyu |
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