CN102861024B - Application of Gypensapogenin A in medicine for increasing white blood cell - Google Patents
Application of Gypensapogenin A in medicine for increasing white blood cell Download PDFInfo
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- CN102861024B CN102861024B CN201210415362.8A CN201210415362A CN102861024B CN 102861024 B CN102861024 B CN 102861024B CN 201210415362 A CN201210415362 A CN 201210415362A CN 102861024 B CN102861024 B CN 102861024B
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- gypensapogenin
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- blood cell
- white blood
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- PYGRZYXAMLFMOS-IBMFSSKUSA-N gypensapogenin a Chemical compound O=C1C(=C(C)C)CC=C1[C@@H]1[C@@H](CC[C@H]2[C@]3(CCC4=C2[C@H]2CC[C@H](O2)C4(C)C)C)[C@@]3(C)CC1 PYGRZYXAMLFMOS-IBMFSSKUSA-N 0.000 title claims abstract description 67
- 210000000265 leukocyte Anatomy 0.000 title claims abstract description 15
- 239000003814 drug Substances 0.000 title claims abstract description 9
- 150000001875 compounds Chemical class 0.000 abstract description 13
- 230000003405 preventing effect Effects 0.000 abstract 2
- 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
- 238000002360 preparation method Methods 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
- 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
- 230000007423 decrease Effects 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 230000003203 everyday effect Effects 0.000 description 2
- 230000002607 hemopoietic effect Effects 0.000 description 2
- 239000000203 mixture Substances 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
- 238000013459 approach Methods 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
- 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
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 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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Abstract
The invention relates to novel application of a compound Gypensapogenin A in the pharmaceutical field. The invention relates to application of Gypensapogenin A in preparing a medicine for increasing white blood cell. The application of Gypensapogenin A in preparing the medicine for treating aleucemia, which is provided by the invention, is disclosed for the first time. The skeleton type belongs to brand-new skeleton type, and the aleucemia preventing activity of Gypensapogenin A is extremely strong, so that no possibility for providing any prompt by other compounds exists. Gypensapogenin A has outstanding actual characteristics. Meanwhile, Gypensapogenin A has outstanding progress when being used for preventing aleucemia.
Description
Technical field
The present invention relates to the new purposes of a kind of compound Gypensapogenin A in pharmaceutical field.
Background technology
The compound Gypensapogenin A 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 A 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 compounds, possesses outstanding substantive distinguishing features, for the control of low leukocyte counts, obviously there is significant progress simultaneously.
Summary of the invention
The object of the present invention is to provide the new application of Gypensapogenin A in pharmaceutical field.
The present invention relates to Gypensapogenin A as the application of preparing in the medicine of leukocyte increasing.
Described compound Gypensapogenin A structure is as shown in formula I:
Formula I
The purposes of the Gypensapogenin A 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 compounds, possess outstanding substantive distinguishing features, for the control of low leukocyte counts, obviously there is significant progress simultaneously.
The specific embodiment
The preparation method of compound Gypensapogenin A 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 A tablet involved in the present invention:
Get 20 and digest compound Gypensapogenin A, add 180 grams of conventional adjuvants preparing tablet, mix, conventional tablet machine is made 1000.
Embodiment 2: the preparation of compound Gypensapogenin A capsule involved in the present invention:
Get 20 and digest compound Gypensapogenin A, 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.
In order to understand better essence of the present invention, the drug test with Gypensapogenin A and result are illustrated to its new purposes in pharmaceutical field below.
The hemoposieis of Gypensapogenin A:
One, the impact of mouse peripheral blood quantity of leucocyte
Method: 40 of Balb/c mices, 18-22g is female.By body weight, be divided into 3 groups, be respectively normal saline group, Gypensapogenin A 2.0mg/kg, Gypensapogenin A 4.0mg/kg, within 1st, be divided into twice oral administration, totally 9 times four and half.Before administration, after administration, within 1 day, 3 days, 7 days, 14 days, cut tail and get blood 20ul, F-820 platelet count instrument detects hemogram.
The impact (n=11) of table 1 Gypensapogenin A on mouse peripheral blood quantity of leucocyte
Natural law comparison corresponding to normal saline group: * p<0.5
Result: with the comparison of normal saline group, two dosage groups all manifest immediately and rise white effect after administration.
Two, the therapeutical effect of Gypensapogenin A to 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 normal saline group, other organizes every mice from eye socket venesection 0.5ml, gets blood again and survey all each group indexs after 24h, and then continuous gastric infusion 1 week, after last administration 1h, gets the full whole bliid platelet analyzer of blood F-800 from eye socket venous plexus and survey These parameters.
Table 3 Gypensapogenin A is to because of leukopenic therapeutical effect due to losing blood
With model group comparison: * p<0.05 * * p<0.01 * * * p<0.001
Result shows, blood-letting mice is through taking Gypensapogenin A treatment after 7 days, and 2 administration groups are respectively at model group comparison, and leukocyte is significantly higher than model group, approaches normal saline group.
Three, Gypensapogenin A is to the hypocellular therapeutical effect of cyclophosphamide hyperamization
40 of the preventive and therapeutic effect ICR mices that mouse bone marrow cells hemopoietic function is damaged, ♀ ♂ 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, except normal saline group, other respectively organized mice lumbar injection cycli phosphate amine 80mg/kg respectively, then continued administration 3 days on 5th, 10.1h after last administration, gets blood from eye socket venous plexus, surveys leukocyte, gets femur bone marrow counting number of nucleated cells.
Table 4 Gypensapogenin A is to the leukopenic therapeutical effect of caused by cyclophosphamide
With model group comparison: * p<0.05 * * p<0.01 * * * p<0.001
Result shows, with the comparison of normal saline group, cycli phosphate amine can make mouse bone marrow cells damage, cause peripheral blood cells to decline, Gypensapogenin A group and model group comparison, all can obviously resist cycli phosphate amine induced mice leukopenia, and prompting this product has the effect that improves hemopoietic function.
Four, Gypensapogenin A is to leukopenic therapeutical effect due to stupid
On the impact of Induced Aplastic Anemia Mice: 48 of Kunming mouses, ♀ ♂ dual-purpose, is divided into 4 groups (n=12), except normal saline group, other group mouse subcutaneous injection benzene 0.5ml/kg, continuous 12 days, the same day of modeling, oral administration simultaneously, every day 1 time, totally 18 days, 1h after last administration, eye socket venous plexus is got blood, surveys leukocyte, gets femur bone marrow counting number of nucleated cells.
The therapeutical effect of table 5 Gypensapogenin A to cytopenia due to benzene
With model group comparison: * p<0.05 * * p<0.01
Result shows, 2 administration groups are respectively at model group comparison, all can obviously resist the leukocytic decline of Induced Aplastic Anemia Mice due to benzene.
Conclusion: Gypensapogenin A is leukocyte increasing significantly, can be used for preparing Antileukopemia medicine.
Claims (1)
- The application of 1.Gypensapogenin A in the medicine of preparing leukocyte increasing, described compound Gypensapogenin A structure as formula Ishown in:
formula I.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210415362.8A CN102861024B (en) | 2012-10-26 | 2012-10-26 | Application of Gypensapogenin A in medicine for increasing white blood cell |
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| CN201210415362.8A CN102861024B (en) | 2012-10-26 | 2012-10-26 | Application of Gypensapogenin A in medicine for increasing white blood cell |
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| CN102861024A CN102861024A (en) | 2013-01-09 |
| CN102861024B true CN102861024B (en) | 2014-04-16 |
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Families Citing this family (2)
| 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 |
| CN105232538A (en) * | 2015-07-16 | 2016-01-13 | 南京海澳斯生物医药科技有限公司 | Composition and application thereof in preparing medicines for raising leukocytes |
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- 2012-10-26 CN CN201210415362.8A patent/CN102861024B/en active Active
Non-Patent Citations (4)
| Title |
|---|
| Li, N. et al..Triterpenes possessing an unprecedented skeleton isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum.《European Journal of Medicinal Chemistry》.2012,第50卷第173–178页. |
| Triterpenes possessing an unprecedented skeleton isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum;Li, N. et al.;《European Journal of Medicinal Chemistry》;20120203;第50卷;第173-178页 * |
| Two new dammaran sapogenins from leaves of Panax notoginseng. Planta Medica;Wei, J.X. et al.;《Planta Medica》;19821231;第45卷(第3期);第167-171页 * |
| Wei, J.X. et al..Two new dammaran sapogenins from leaves of Panax notoginseng. Planta Medica.《Planta Medica》.1982,第45卷(第3期),第167-171页. |
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