CN102872043B - Application of Gypensapogenin B in medicament of increasing level of leukocyte - Google Patents
Application of Gypensapogenin B in medicament of increasing level of leukocyte Download PDFInfo
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- CN102872043B CN102872043B CN201210417400.3A CN201210417400A CN102872043B CN 102872043 B CN102872043 B CN 102872043B CN 201210417400 A CN201210417400 A CN 201210417400A CN 102872043 B CN102872043 B CN 102872043B
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- 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 65
- 210000000265 leukocyte Anatomy 0.000 title claims abstract description 18
- 239000003814 drug Substances 0.000 title claims abstract description 9
- 238000002360 preparation method Methods 0.000 claims abstract description 11
- 150000001875 compounds Chemical class 0.000 abstract description 13
- 230000000694 effects Effects 0.000 abstract description 3
- 230000007812 deficiency Effects 0.000 abstract 3
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 241000699670 Mus sp. Species 0.000 description 11
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 description 9
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical group [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 9
- 210000004369 blood Anatomy 0.000 description 8
- 239000008280 blood Substances 0.000 description 8
- 230000001225 therapeutic effect Effects 0.000 description 7
- 241000699666 Mus <mouse, genus> Species 0.000 description 5
- 210000004279 orbit Anatomy 0.000 description 4
- 240000006509 Gynostemma pentaphyllum Species 0.000 description 3
- 235000002956 Gynostemma pentaphyllum Nutrition 0.000 description 3
- 229910019142 PO4 Inorganic materials 0.000 description 3
- 230000000610 leukopenic effect Effects 0.000 description 3
- 239000010452 phosphate Substances 0.000 description 3
- -1 phosphate amine Chemical class 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
- 208000032467 Aplastic anaemia Diseases 0.000 description 2
- CMSMOCZEIVJLDB-UHFFFAOYSA-N Cyclophosphamide Chemical compound ClCCN(CCCl)P1(=O)NCCCO1 CMSMOCZEIVJLDB-UHFFFAOYSA-N 0.000 description 2
- 239000002671 adjuvant Substances 0.000 description 2
- 210000001772 blood platelet Anatomy 0.000 description 2
- 210000001185 bone marrow Anatomy 0.000 description 2
- 210000002798 bone marrow cell Anatomy 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 210000004027 cell Anatomy 0.000 description 2
- 229960004397 cyclophosphamide Drugs 0.000 description 2
- 230000003203 everyday effect Effects 0.000 description 2
- 230000002607 hemopoietic effect Effects 0.000 description 2
- 210000005259 peripheral blood Anatomy 0.000 description 2
- 239000011886 peripheral blood Substances 0.000 description 2
- 210000000689 upper leg Anatomy 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
- 238000012449 Kunming mouse Methods 0.000 description 1
- 235000003143 Panax notoginseng Nutrition 0.000 description 1
- 241000180649 Panax notoginseng Species 0.000 description 1
- 206010033661 Pancytopenia Diseases 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 208000024389 cytopenia Diseases 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
- 230000007423 decrease Effects 0.000 description 1
- 238000003255 drug test Methods 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 238000001802 infusion Methods 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 201000002364 leukopenia Diseases 0.000 description 1
- 231100001022 leukopenia Toxicity 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 210000004976 peripheral blood cell Anatomy 0.000 description 1
- 230000003285 pharmacodynamic effect Effects 0.000 description 1
- 230000003449 preventive effect Effects 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 238000010254 subcutaneous injection Methods 0.000 description 1
- 239000007929 subcutaneous injection Substances 0.000 description 1
- 210000004881 tumor cell Anatomy 0.000 description 1
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- Medicinal Preparation (AREA)
- Steroid Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention relates to a new application of a compound Gypensapogenin B in the field of pharmacy. The invention relates to an application of the Gypensapogenin B in the preparation of a medicament for increasing the level of leukocyte. The application of the Gypensapogenin B provided by the invention in the preparation of the medicament for treating the deficiency of the leukocyte is disclosed for the first time; and a skeleton type belongs to a bran-new skeleton type, and the strong inhibition activity of the Gypensapogenin B on the deficiency of the leukocyte is unexpected, thus the possibility that other compounds give any implication does not exist, the application has outstanding substantive feature, and simultaneously, the application of the Gypensapogenin B in the prevention and treatment of the deficiency of the leukocyte is obviously improved.
Description
Technical field
The present invention relates to the new purposes of a kind of chemical compound Gypensapogenin B in pharmaceutical field.
Background technology
The chemical compound Gypensapogenin B that the present invention relates to is one and delivered (Li in 2012, 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 chemical compound has brand-new framework types, present 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.), belong to open first for the purposes of the Gypensapogenin B that the present invention relates in preparation treatment low leukocyte counts medicine, because framework types belongs to brand-new framework types, and it suppresses active unexpectedly strong for low leukocyte counts, there is not the possibility that is provided any enlightenment by other chemical compounds, possess outstanding substantive distinguishing features, the control that is used for simultaneously low leukocyte counts obviously has significant progress.
Summary of the invention
The object of the present invention is to provide the new application of Gypensapogenin B in pharmaceutical field.
The present invention relates to Gypensapogenin B as the application in the medicine of preparation leukocyte increasing.
Described chemical compound Gypensapogenin B structure is shown in formula I:
Formula I
The purposes of the Gypensapogenin B that the present invention relates in preparation treatment low leukocyte counts medicine belongs to open first, because framework types belongs to brand-new framework types, and it suppresses active unexpectedly strong for low leukocyte counts, there is not the possibility that is provided any enlightenment by other chemical compounds, possess outstanding substantive distinguishing features, the control that is used for simultaneously low leukocyte counts obviously has significant progress.
The specific embodiment
The preparation method of chemical 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 subjected to any restriction of specific embodiment, but limited by claim.
Embodiment 1: the preparation of chemical compound Gypensapogenin B tablet involved in the present invention:
Get 20 and digest compound Gypensapogenin B, add conventional adjuvant 180 grams of preparation tablet, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of chemical compound Gypensapogenin B capsule involved in the present invention:
Get 20 and digest compound Gypensapogenin B, add conventional adjuvant such as starch 180 grams of preparation capsule, mixing is encapsulatedly made 1000.
Further specify its pharmaceutically active below by pharmacodynamic experiment.
In order to understand better essence of the present invention, the below will illustrate its new purposes in pharmaceutical field with drug test and the result of Gypensapogenin B.
The hemoposieis of Gypensapogenin B:
One, the impact of mouse peripheral blood quantity of leucocyte
Method: 40 of Balb/c mices, 18-22g is female.Be divided into 3 groups by body weight, be respectively normal saline group, Gypensapogenin B 2.0mg/kg, Gypensapogenin B 4.0mg/kg, be divided into oral administration twice, totally 9 times four and half on 1st.Cut tail in 1 day, 3 days, 7 days, 14 days and get blood 20ul before administration, after the administration, F-820 platelet count instrument detects hemogram.
Table 1 Gypensapogenin B is on the impact (n=11) of mouse peripheral blood quantity of leucocyte
Natural law corresponding to the normal saline group compares: * p＜0.5
The result: with the normal saline group relatively, two dosage groups all manifest immediately after administration and rise white effect.
Two, Gypensapogenin B is to the therapeutical effect of the mice that loses blood
On the mice that loses blood affect 40 of ICR mices, ♀ ♂ half and half is divided into 4 groups (n=10).Except the normal saline group, every mice of other group is got the blood survey again and all respectively organizes index from eye socket venesection 0.5ml behind the 24h, then continuous 1 week of gastric infusion, behind the last administration 1h, gets blood from the eye socket venous plexus and surveys These parameters with F-800 whole blood platelet analyser.
Table 3 Gypensapogenin B is to because of leukopenic therapeutical effect due to losing blood
Compare with model group: * p＜0.05 * * p＜0.01 * * * p＜0.001
The result shows, the blood-letting mice is through taking Gypensapogenin B treatment after 7 days, 2 administration groups respectively at model group relatively, leukocyte is significantly higher than model group, near the normal saline group.
Three, Gypensapogenin B is to the hypocellular therapeutical effect of cyclophosphamide hyperamization
To 40 of the preventive and therapeutic effect ICR mices of mouse bone marrow cells hemopoietic function damage, ♀ ♂ dual-purpose is divided into 4 groups (n=10), i.e. normal saline group, modeling group, 1.2mg/kg group and 0.6mg/kg group, oral administration, every day 1 time.0th, other respectively organized respectively lumbar injection cycli phosphate amine 80mg/kg of mice, then continued administration 3 days except the normal saline group on 5th, 10.1h after the last administration gets blood from the eye socket venous plexus, surveys leukocyte, gets femur bone marrow counting number of nucleated cells.
Table 4 Gypensapogenin B is to the leukopenic therapeutical effect of caused by cyclophosphamide
Compare with model group: * p＜0.05 * * p＜0.01 * * * p＜0.001
The result shows, compares with the normal saline group, and cycli phosphate amine can make the mouse bone marrow cells damage, cause peripheral blood cells to descend, Gypensapogenin B group compares with model group, all can obviously resist cycli phosphate amine induced mice leukopenia, and prompting this product has the effect that improves hemopoietic function.
Four, Gypensapogenin B is to leukopenic therapeutical effect due to stupid
Impact on Induced Aplastic Anemia Mice: 48 of Kunming mouses, ♀ ♂ dual-purpose is divided into 4 groups (n=12), except the normal saline group, other group mouse subcutaneous injection benzene 0.5ml/kg, continuous 12 days, the same day of modeling, the while oral administration, every day 1 time, totally 18 days, 1h after the last administration, the eye socket venous plexus is got blood, surveys leukocyte, gets femur bone marrow counting number of nucleated cells.
Table 5 Gypensapogenin B is to the therapeutical effect of cytopenia due to the benzene
Compare with model group: * p＜0.05 * * p＜0.01
The result shows, 2 administration groups respectively at model group relatively all can obviously be resisted the leukocytic decline of Induced Aplastic Anemia Mice due to the benzene.
Conclusion: Gypensapogenin B is leukocyte increasing significantly, can be used for preparing the Antileukopemia medicine.
Claims (1)
1.Gypensapogenin B the preparation leukocyte increasing medicine in application, described chemical compound Gypensapogenin B structure as
Formula IShown in:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210417400.3A CN102872043B (en) | 2012-10-26 | 2012-10-26 | Application of Gypensapogenin B in medicament of increasing level of leukocyte |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210417400.3A CN102872043B (en) | 2012-10-26 | 2012-10-26 | Application of Gypensapogenin B in medicament of increasing level of leukocyte |
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| Publication Number | Publication Date |
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| CN102872043A CN102872043A (en) | 2013-01-16 |
| CN102872043B true CN102872043B (en) | 2013-10-23 |
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Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104784175A (en) * | 2015-05-12 | 2015-07-22 | 南京大学 | Application of derivative of Daphmalenine A in preparation of drugs for increasing white blood cells |
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2012
- 2012-10-26 CN CN201210417400.3A patent/CN102872043B/en active Active
Non-Patent Citations (2)
| Title |
|---|
| Ning Li等.Triterpenes possessing an unprecedented skeleton isolated from hydrolyzateof total saponins from Gynostemma pentaphyllum.《European Journal of Medicinal Chemistry》.2012,第50卷173-178. |
| Triterpenes possessing an unprecedented skeleton isolated from hydrolyzateof total saponins from Gynostemma pentaphyllum;Ning Li等;《European Journal of Medicinal Chemistry》;20120203;第50卷;173-178 * |
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| CN102872043A (en) | 2013-01-16 |
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