CN102885836B - Application of Gypensapogenin B in medicament for treating or preventing acute heart failure - Google Patents
Application of Gypensapogenin B in medicament for treating or preventing acute heart failure Download PDFInfo
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- CN102885836B CN102885836B CN201210417702.0A CN201210417702A CN102885836B CN 102885836 B CN102885836 B CN 102885836B CN 201210417702 A CN201210417702 A CN 201210417702A CN 102885836 B CN102885836 B CN 102885836B
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- heart failure
- gypensapogenin
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- NNUMQZNZQGQGCN-AGHUFMIKSA-N gypensapogenin b Chemical compound O=C1C(=C(C)C)CC([C@@H]2[C@@H]3[C@@]([C@@]4(CCC5=C([C@H]6CC[C@H](O6)C5(C)C)[C@H]4CC3)C)(C)CC2)=C1 NNUMQZNZQGQGCN-AGHUFMIKSA-N 0.000 title claims abstract description 50
- 206010007556 Cardiac failure acute Diseases 0.000 title claims abstract description 19
- 239000003814 drug Substances 0.000 title claims abstract description 12
- 238000002360 preparation method Methods 0.000 claims abstract description 11
- 238000011282 treatment Methods 0.000 claims description 11
- 238000011321 prophylaxis Methods 0.000 claims description 4
- 150000001875 compounds Chemical class 0.000 abstract description 11
- 230000000694 effects Effects 0.000 abstract description 3
- 206010019280 Heart failures Diseases 0.000 description 10
- 241000282472 Canis lupus familiaris Species 0.000 description 7
- 230000000747 cardiac effect Effects 0.000 description 6
- 241000282465 Canis Species 0.000 description 3
- 240000006509 Gynostemma pentaphyllum Species 0.000 description 3
- 235000002956 Gynostemma pentaphyllum Nutrition 0.000 description 3
- QGMRQYFBGABWDR-UHFFFAOYSA-M Pentobarbital sodium Chemical compound [Na+].CCCC(C)C1(CC)C(=O)NC(=O)[N-]C1=O QGMRQYFBGABWDR-UHFFFAOYSA-M 0.000 description 3
- 229960002275 pentobarbital sodium Drugs 0.000 description 3
- 229930182490 saponin Natural products 0.000 description 3
- 150000007949 saponins Chemical class 0.000 description 3
- 235000017709 saponins Nutrition 0.000 description 3
- 150000003648 triterpenes Chemical class 0.000 description 3
- 241001465754 Metazoa Species 0.000 description 2
- 230000004913 activation Effects 0.000 description 2
- 239000002671 adjuvant Substances 0.000 description 2
- 210000000709 aorta Anatomy 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 238000003304 gavage Methods 0.000 description 2
- 230000007246 mechanism Effects 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 230000002107 myocardial effect Effects 0.000 description 2
- INLFWQCRAJUDCR-IQVMEADQSA-N (1R,2S,4S,5'S,6R,7S,8R,9S,12S,13S)-5',7,9,13-tetramethylspiro[5-oxapentacyclo[10.8.0.02,9.04,8.013,18]icosane-6,2'-oxane] Chemical compound O([C@@H]1[C@@H]([C@]2(CC[C@@H]3[C@@]4(C)CCCCC4CC[C@H]3[C@@H]2C1)C)[C@@H]1C)[C@]11CC[C@H](C)CO1 INLFWQCRAJUDCR-IQVMEADQSA-N 0.000 description 1
- 206010002091 Anaesthesia Diseases 0.000 description 1
- 206010020850 Hyperthyroidism Diseases 0.000 description 1
- 235000003143 Panax notoginseng Nutrition 0.000 description 1
- 241000180649 Panax notoginseng Species 0.000 description 1
- 208000006193 Pulmonary infarction Diseases 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 230000002159 abnormal effect Effects 0.000 description 1
- 230000037005 anaesthesia Effects 0.000 description 1
- 208000007502 anemia Diseases 0.000 description 1
- 206010003119 arrhythmia Diseases 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 230000017531 blood circulation Effects 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 210000000481 breast Anatomy 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 230000035606 childbirth Effects 0.000 description 1
- 230000008602 contraction Effects 0.000 description 1
- 230000001472 cytotoxic effect Effects 0.000 description 1
- OORMXZNMRWBSTK-UHFFFAOYSA-N dammaran Natural products C1CCC(C)(C)C2CCC3(C)C4(C)CCC(C(C)CCCC(C)C)C4CCC3C21C OORMXZNMRWBSTK-UHFFFAOYSA-N 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 206010012601 diabetes mellitus Diseases 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 210000001198 duodenum Anatomy 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 210000003191 femoral vein Anatomy 0.000 description 1
- 230000006870 function Effects 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 230000036541 health Effects 0.000 description 1
- 230000004217 heart function Effects 0.000 description 1
- 230000000004 hemodynamic effect Effects 0.000 description 1
- 229940088597 hormone Drugs 0.000 description 1
- 239000005556 hormone Substances 0.000 description 1
- 230000008676 import Effects 0.000 description 1
- 238000001802 infusion Methods 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000010253 intravenous injection Methods 0.000 description 1
- 210000005240 left ventricle Anatomy 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
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- 230000004060 metabolic process Effects 0.000 description 1
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- 230000003680 myocardial damage Effects 0.000 description 1
- 210000004165 myocardium Anatomy 0.000 description 1
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- 230000003285 pharmacodynamic effect Effects 0.000 description 1
- 230000005622 photoelectricity Effects 0.000 description 1
- 230000004962 physiological condition Effects 0.000 description 1
- 230000002980 postoperative effect Effects 0.000 description 1
- 230000035935 pregnancy Effects 0.000 description 1
- 230000007575 pulmonary infarction Effects 0.000 description 1
- 238000007634 remodeling Methods 0.000 description 1
- 230000029058 respiratory gaseous exchange Effects 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 238000012109 statistical procedure Methods 0.000 description 1
- 230000002889 sympathetic effect Effects 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
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- 238000002627 tracheal intubation Methods 0.000 description 1
- 210000004881 tumor cell Anatomy 0.000 description 1
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention provides an application of Gypensapogenin B in the preparation of a medicament for treating or preventing acute heart failure. The application of Gypensapogenin B in the preparation of the medicament for treating or preventing acute heart failure is firstly disclosed; since the skeleton type belongs to an entirely new skeleton type and the activity for treating acute heart failure is previously unimagined high without any possibility of giving out revelation by other compounds, the application has outstanding substantial characteristics; and simultaneously, the application for treating acute heart failure is obviously advanced.
Description
Invention field
The present invention relates to the application of Gypensapogenin B in the medicine of preparation treatment or prophylaxis of acute heart failure.
Background technology
Heart failure (hear failure, HF) refers to that cardiac function causes 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 that HF occurs to develop 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 generation development of heart failure.
The compound Gypensapogenin B the present invention relates to is one and within 2012, delivers (Li, N. et al., 2012. Triterpenes possessing an unprecedented skeleton isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum. European Journal of Medicinal Chemistry 50, 173 – 178.) New skeleton compound, this compound has brand-new framework types, current purposes only relates to the cytotoxic activity (Li of human tumor cell line, N. et al., 2012. Triterpenes possessing an unprecedented skeleton isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum. European Journal of Medicinal Chemistry 50, 173 – 178.), purposes for the Gypensapogenin B the present invention relates in preparation treatment acute heart failure medicine belongs to open first, 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 that is 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 the application of Gypensapogenin B in the medicine of preparation treatment or prophylaxis of acute heart failure.
Described compound Gypensapogenin B structure is as shown in formula I:
The purposes of the Gypensapogenin B the present invention relates in preparation treatment acute heart failure medicine belongs to open first, 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 that is 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.
The specific embodiment
The preparation method of compound Gypensapogenin B involved in the present invention is referring to document (Li, N. et al., 2012. Triterpenes possessing an unprecedented skeleton isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum. European Journal of Medicinal Chemistry 50, 173 – 178. and Wei, J.X. et al., 1982. Two new dammaran sapogenins from leaves of Panax notoginseng. Planta Medica, 45 (3): 167-171.).
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 Gypensapogenin B tablet involved in the present invention:
Get 20 and digest compound Gypensapogenin B, add 180 grams of conventional adjuvants preparing tablet, mix, conventional tablet machine is made 1000.
Embodiment 2: the preparation of compound Gypensapogenin B capsule involved in the present invention:
Get 20 and digest compound Gypensapogenin B, add the conventional adjuvant of preparing capsule as 180 grams of starch, mix, encapsulatedly make 1000.
Below by pharmacodynamic experiment, further illustrate its pharmaceutically active.
Test example: the therapeutical effect of Gypensapogenin B to dog acute heart failure
1 material animal health adult dogs body weight 12.5 ~ 13.5 kg.Pentobarbital sodium (Sigma, import subpackage, specification: 25g); Instrument U.S. BIC16 leads physiograph (production of U.S. BIC Corp.); Electromagnetic flowmeter (MFV-3200 type): Japanese photoelectricity company produces.
2 test methods and result
Dog is divided into NS group (waiting capacity solvent) at random, gastric infusion Gypensapogenin B 2.0 mg/kg groups, 1.0 mg/kg groups, 0.2 mg/kg group, 6 every group.After fasting 12 hours, the 40 mg/kg anesthesia of intravenous injection pentobarbital sodium, tracheal intubation, artificial respiration, monitoring aortic pressure (AP) and electrocardiogram.Left side opening breast, plugs in conduit to left constant pressure and rate of pressure change (± dp/dt thereof from the apex of the heart
max).Waltan-Brodie strain bow is implanted to left ventricle antetheca, measure myocardial contraction.With electromagnetic flowmeter determination ascending aorta blood flow.Using ascending aorta flow as cardiac output (CO), calculate cardiac index (CI), the index (SI) of often fighting, the work done (SW) of often fighting, left heart work done (LVW).Parameters record and BIC physiograph.Postoperative half an hour, it is stable that parameters reaches.From femoral vein constant speed gasing injection pentobarbital sodium (0.5 mL/kgmin), with ± dp/dt
maxdropping to approximately 1000 mHg/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 check, carries out statistical procedures.
Table 1 Gypensapogenin B is on the impact of heart failure canine dp/dt (n=6, X ± s)
Compare with NS group,
@p<0.05,
@@p<0.01
Table 2 Gypensapogenin B is on the impact of heart failure canine cardiac work (n=6, X ± s)
With comparison * p<0.05 before administration, * * 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 Gypensapogenin B can increase SW, LVW ,+dp/dt(and the comparison of model group matched group of Heart Failure Dogs, p<0.05or p<0.01).Gavage various dose Gypensapogenin B can increase SW, LVW ,+dp/dt(and the comparison of model group matched group of Heart Failure Dogs, p<0.01or p<0.05).
Table 3 Gypensapogenin B is on the kinemic impact of heart failure canine (n=6, X ± s)
With comparison * p<0.05 before administration, * * p<0.01; Compare with NS group
@p<0.05,
@@p<0.01
Result is as shown in table 3, and instillation various dose Gypensapogenin B can increase the cardiac output (with model control group comparison, p<0.01or p<0.05) of Heart Failure Dogs.Gavage various dose Gypensapogenin B can increase the cardiac output (with model control group comparison, p<0.01or p<0.05) of Heart Failure Dogs.
Conclusion: Gypensapogenin B can significantly improve acute heart failure, can be used for preparing the medicine for the treatment of or preventing heart failure.
Claims (1)
- The application of 1.Gypensapogenin B in the medicine of preparation treatment or prophylaxis of acute heart failure, described compound Gypensapogenin B structure as formula Ishown in:
formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210417702.0A CN102885836B (en) | 2012-10-26 | 2012-10-26 | Application of Gypensapogenin B in medicament for treating or preventing acute heart failure |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210417702.0A CN102885836B (en) | 2012-10-26 | 2012-10-26 | Application of Gypensapogenin B in medicament for treating or preventing acute heart failure |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102885836A CN102885836A (en) | 2013-01-23 |
| CN102885836B true CN102885836B (en) | 2014-04-16 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201210417702.0A Active CN102885836B (en) | 2012-10-26 | 2012-10-26 | Application of Gypensapogenin B in medicament for treating or preventing acute heart failure |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN102885836B (en) |
-
2012
- 2012-10-26 CN CN201210417702.0A patent/CN102885836B/en active Active
Non-Patent Citations (2)
| Title |
|---|
| Ning Li, et al.Triterpenes possessing an unprecedented skeleton isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum.《European Journal of Medicinal Chemistry》.2012,第50卷173-178. |
| Triterpenes possessing an unprecedented skeleton isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum;Ning Li, et al;《European Journal of Medicinal Chemistry》;20120203;第50卷;173-178 * |
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| Publication number | Publication date |
|---|---|
| CN102885836A (en) | 2013-01-23 |
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Owner name: QIDONG TIANFEN ELECTRIC TOOL TECHNOLOGY INNOVATION Free format text: FORMER OWNER: WU JUNHUA Effective date: 20141126 |
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Effective date of registration: 20141126 Address after: Qidong City, Jiangsu province 226241 Nantong lvsigang Tianfen electric tools trade city comprehensive building Patentee after: Qidong Tianfen Electric Tool Technology Innovation Center Address before: 210009 No. 22, Hankou Road, Gulou District, Jiangsu, Nanjing Patentee before: Wu Junhua |