CN103463006A - Application of racemosins A in preparation of medicine treating or preventing chronic heart failure - Google Patents
Application of racemosins A in preparation of medicine treating or preventing chronic heart failure Download PDFInfo
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- CN103463006A CN103463006A CN2013104712049A CN201310471204A CN103463006A CN 103463006 A CN103463006 A CN 103463006A CN 2013104712049 A CN2013104712049 A CN 2013104712049A CN 201310471204 A CN201310471204 A CN 201310471204A CN 103463006 A CN103463006 A CN 103463006A
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- racemosins
- heart failure
- chronic heart
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Abstract
The invention provides the application of the racemosins A in preparation of the medicine treating or preventing the chronic heart failure, and particularly provides the therapeutic effect of the racemosins A on the acute heart failure or the chronic heart failure. The application of the racemosins A in preparation of the medicine treating the chronic heart failure is disclosed for the first time. The matrix type of the racemosins A belongs to a brand new matrix type. The racemosins A has the advantages of being high in activity for treating the chronic heart failure and prominent in substantive features, and makes remarkable progress in treating the chronic heart failure.
Description
Technical field
The present invention relates to the new purposes of compound R acemosins A, relate in particular to the application of Racemosins A in preparation treatment or preventing chronic heart failure medicine.
Background technology
Heart failure (hear failure, HF) refers to that cardiac function causes the heart pump blood volume can not meet a kind of pathological and physiological condition of tissue metabolism's needs extremely.Cause of disease inducement causes initial myocardial damage because of cardiac overload, cardiac muscle itself, the limited any reason of diastole and causes structure function lowly and the morbidity of carrying out property; And infect, anemia, gestation, childbirth, cardiac arrhythmia, pulmonary infarction, hyperthyroidism, diabetes, inhibition heart medicine bring out and increase the weight of HF.Pathogeny thinks that the mechanism of HF genesis is abnormal hemodynamics in the past; The later stage eighties 20th century is recognized the activation of nerve-endocrine hormone play an important role (sympathetic ↑ NE ↑ RAS ↑ wait activation); After the nineties, clear and definite gradually " Myocardial Remodeling " is (remodelling) fundamental mechanism that causes the genesis of heart failure.
The compound R acemosins A the present invention relates to is one and within 2013, delivers (Ding-Quan Liu, et al., Racemosins A and B, two novel bisindole alkaloids from the green alga Caulerpa racemosa.Fitoterapia, 91 (2013): 15 – 20.) noval chemical compound, this compound has brand-new framework types, and current purposes finds that it can weaken beta-amyloyd peptide
25-35(A β
25 – 35) human neuroblastoma cell SH-SY5Y cell injury (the Ding-Quan Liu that causes, et al., Racemosins A and B, two novel bisindole alkaloids from the green alga Caulerpa racemosa.Fitoterapia, 91 (2013): 15 – 20.), the purposes of the Racemosins A the present invention relates in preparation treatment or preventing chronic heart failure medicine belongs to open first.
Summary of the invention
The object of the invention is to, according in existing Racemosins A research, not finding that it has the present situation of the report for the treatment of or preventing chronic heart failure activity, provides the application of Racemosins A in preparation treatment or preventing chronic heart failure medicine.
Described compound R acemosins A structure is as shown in formula I:
Formula I
The purposes of the Racemosins A the present invention relates in preparation treatment chronic heart failure belongs to open first, because framework types belongs to brand-new framework types, and the activity of its treatment chronic heart failure is strong, possess outstanding substantive distinguishing features, be used for the treatment of chronic heart failure simultaneously and obviously there is significant progress.
The specific embodiment
The preparation method of compound R acemosins A involved in the present invention is referring to document (Ding-Quan Liu, et al., Racemosins A and B, two novel bisindole alkaloids from the green alga Caulerpa racemosa.Fitoterapia, 91 (2013): 15 – 20.)
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subject to any restriction of specific embodiment, but be limited by claim.
Embodiment 1: the preparation of compound R acemosins A tablet involved in the present invention:
Get 5 and digest compound Racemosins A and add dextrin 195 grams, mix, conventional tabletting is made 1000.
Embodiment 2: the preparation of compound R acemosins A capsule involved in the present invention:
Get 5 and digest compound Racemosins A and add starch 195 grams, mix, encapsulatedly make 1000.
Further illustrate its pharmaceutically active below by pharmacodynamic experiment.
The impact of experimental example 1:Racemosins A on the chronic heart failure rat
Test method and result: 100 of rats, male and female half and half, get 100 lumbar injection doxorubicin hydrochloride 2mg/kg, and 1 time weekly, totally 6 weeks.Be divided at random 10 groups, i.e. NS group, Captopril tablets 12.5mg/kg group, gastric infusion Racemosins A0.2mg/kg group, gastric infusion Racemosins A2.5mg/kg group, gastric infusion Racemosins A5.0mg/kg group.Within the 5th week, rise and give Racemosins A gavage each group every day, administration 21 days.20% urethane 1.1g/kg intraperitoneal injection of anesthesia, peeling operation trachea intubate, the total tremulous pulse in right side that simultaneously dissociates, insert homemade ventricle intubate (diameter 1mm is full of 1% heparin) through it, traces blood pressure curve; Continue again to insert, make it by the left side arterial valve, enter left ventricle, trace the intraventricular pressure curve, Automatic analysis left ventricular systolic pressure (LVSP), the maximum climbing speed (+dp/dtmax) of intraventricular pressure, the data such as intraventricular pressure maximum falling speed (dp/dtmax) and the myocardium maximal velocity of contraction of actual measurement (Vpm).Separately get 10 rats as Normal group, do not give doxorubicin hydrochloride, all the other operate with above-mentioned, and between group, the T check, carry out statistical procedures.
The impact (n=10) of table 1Racemosins A on the chronic heart failure Cardiac Function in Rat
Compare △: p<0.05, △ △: p<0.01 with the NS group
Table 1 result of the test shows can the raise LVSP of the Heart Failure Wistar Rats that caused by doxorubicin hydrochloride of Racemosins A gastric infusion 0.2mg/kg group ,+dp/dtmax, the reduction of-dp/dtmax and Vpm (with NS, organizing comparison, P<0.05); Can significantly the raise LVSP of the Heart Failure Wistar Rats that caused by doxorubicin hydrochloride of Racemosins A gastric infusion 2.5mg/kg, 5.0mg/kg ,+dp/dtmax, the reduction of-dp/dtmax and Vpm (with the NS group relatively, P<0.01).
Conclusion: Racemosins A has the effect of significant treatment or preventing chronic heart failure, can be used for preparing the medicine for the treatment of or preventing chronic heart failure.
Claims (1)
1.Racemosins the application of A in preparation treatment or preventing chronic heart failure medicine, described compound R acemosinsA structure is as shown in formula I:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2013104712049A CN103463006A (en) | 2013-10-11 | 2013-10-11 | Application of racemosins A in preparation of medicine treating or preventing chronic heart failure |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2013104712049A CN103463006A (en) | 2013-10-11 | 2013-10-11 | Application of racemosins A in preparation of medicine treating or preventing chronic heart failure |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN103463006A true CN103463006A (en) | 2013-12-25 |
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ID=49788204
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2013104712049A Pending CN103463006A (en) | 2013-10-11 | 2013-10-11 | Application of racemosins A in preparation of medicine treating or preventing chronic heart failure |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN103463006A (en) |
-
2013
- 2013-10-11 CN CN2013104712049A patent/CN103463006A/en active Pending
Non-Patent Citations (2)
| Title |
|---|
| DING-QUAN LIU: "Racemosins A and B, two novel bisindole alkaloids from the green alga caulerpa racemosa", 《FITOTERAPIA》 * |
| 谷晓辉: "新型海洋双吲哚类生物碱的研究进展", 《有机化学》 * |
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Application publication date: 20131225 |