CN105287487A - Applications of Solanoeclepin A in preparation of leukemia treatment drugs - Google Patents
Applications of Solanoeclepin A in preparation of leukemia treatment drugs Download PDFInfo
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- CN105287487A CN105287487A CN201510794819.4A CN201510794819A CN105287487A CN 105287487 A CN105287487 A CN 105287487A CN 201510794819 A CN201510794819 A CN 201510794819A CN 105287487 A CN105287487 A CN 105287487A
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- solanoeclepin
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Abstract
The present invention relates to applications of Solanoeclepin A in preparation of leukemia treatment drugs, and belongs to the field of medicine. The applications of Solanoeclepin A in preparation of leukemia treatment drugs comprise applications of Solanoeclepin A in preparation of leukemic cell proliferation inhibition drugs, and applications of Solanoeclepin A in preparation of leukemic cell apoptosis induction drugs. According to the present invention, Solanoeclepin A inhibits leukemic cell proliferation and induces leukemic cell apoptosis to treat leukemia; and the used of Houttuynoid B in preparation of leukemia treatment drugs are firstly disclosed, the skeleton type belongs to the completely-new skeleton type, and the leukemic cell inhibition activity of Solanoeclepin A is extremely strong.
Description
Technical field
The present invention relates to the novelty teabag of compound S olanoeclepinA, particularly relate to the application of SolanoeclepinA in preparation treatment leukemia medicament.
Background technology
Acute leukemia is the Clonal malignant disease of a class hematopoietic stem cell exception.Leukaemia in its clone loses the ability of further differentiation and maturation and is stuck in cytocerastic different phase.In bone marrow and other hemopoietic tissue, a large amount of hypertrophy of leukaemia is gathered and infiltrates other Organ and tissues, makes normal hematopoiesis suppressed simultaneously, clinical manifestation be anemia, hemorrhage, infect and each organ infiltration's symptom.According to statistics, leukemia accounts for about 3% of tumor total incidence, is modal a kind of malignant tumor in child and youth.Leukemic sickness rate in countries in the world, Europe and North America sickness rate the highest, its mortality rate is 3.2-7.4/10 ten thousand population.The medicine that searching can prevent and treat acute leukemia seems very urgent.
The compound S olanoeclepinA that the present invention relates to is one and delivers (Hsiang-Yu in 2014, etal., NovelSynthesisofRightSegmentofSolanoeclepinA.OrganicLett ers, 2014, 16, noval chemical compound 4166-4169.), this compound has brand-new framework types, current discovery its can cause food damage (Hsiang-Yu, etal., NovelSynthesisofRightSegmentofSolanoeclepinA.OrganicLett ers, 2014, 16, 4166-4169.), the purposes of the SolanoeclepinA that the present invention relates in preparation treatment leukemia medicament is belonged to first public, owing to belonging to brand-new structure type, and it is unexpectedly strong for treatment leukocythemia liveness, there is not the possibility being provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, for leukemic control, obviously there is significant progress simultaneously.
Summary of the invention
The object of the invention is to not find that it has the present situation of the report for the treatment of leukocythemia liveness according in existing SolanoeclepinA research, provide the application of SolanoeclepinA in preparation treatment leukemia medicament.
SolanoeclepinA, by suppressing leukaemia's (HL-60 cell) propagation and inducing leukemia cell (HL-60 cell) apoptosis, treats leukemia.
Described compound S olanoeclepinA, structure is as shown in formula I:
The purposes of the SolanoeclepinA that the present invention relates in preparation treatment leukemia medicament belongs to first public, and belong to brand-new framework types due to framework types, and its for the cytotoxicity of leukaemia and the biological activity of apoptosis induction strong unexpected, there is not the possibility being provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, for leukemic control, obviously there is significant progress simultaneously.
Detailed description of the invention
The preparation method of compound S olanoeclepinA involved in the present invention is see document (Hsiang-Yu, etal., NovelSynthesisofRightSegmentofSolanoeclepinA.OrganicLett ers, 2014,16,4166-4169.)
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 S olanoeclepinA tablet involved in the present invention:
Get 20 g of compound SolanoeclepinA, add the customary adjuvant 180 grams preparing tablet, mixing, conventional tablet presses makes 1000.
Embodiment 2: the preparation of compound S olanoeclepinA capsule involved in the present invention:
Get 20 g of compound SolanoeclepinA, 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: SolanoeclepinA suppresses HL-60 cell proliferation and HL-60 cells apoptosis
1 materials and methods
1.1 material RPMI1640 culture medium are purchased from Gibco company; Tetramethyl azo azoles salt (MTT), Rhodamine 123 are Sigma Products; Caspase-3,9 spectrophotometry test kits are purchased from the biological company limited of the triumphant base in Nanjing; Other chemical reagent are domestic analytical pure.
1.2 cell culture people promyelocytic leukemia cell line HL-60s are purchased from Chinese Academy of Sciences's Shanghai cell biological institute, be incubated in the RPMI1640 culture fluid containing 10% hyclone, penicillin 100kU/L, streptomycin 100mg/L, 37 DEG C, 5%CO2, cultivate in saturated humidity incubator, trophophase cell of taking the logarithm is tested.
The separation of 1.3 human peripheral blood single nucleus cells (PBMC)
Aseptic collection health donors venous blood, anticoagulant heparin (every milliliter of whole blood adds the 200U/ml heparin sodium aqua of 0.1ml), PBS equimultiple dilute blood, 1:4 adds human lymphocyte separating medium, the centrifugal 20min of 2000rpm, uses serum-free RPMI-1640 culture medium 1500rpm10min centrifuge washing 2 times after collecting milky white layer, obtain mononuclearcell, trypan blue exclusion rate is greater than 95%, is resuspended in the RPMI-1640 culture medium of 10%FCS for subsequent use.
The impact that 1.4SolanoeclepinA grows HL-60 cell and human PBMC
Inoculation HL-60 cell and human PBMC and 96 orifice plates, 2 × 104, every hole cell (100ul).37 DEG C, 5%CO
2after cultivating 24h under condition, experimental group once adds 0.625,1.25,2.5,5.0, the SolanoeclepinA of 10.0ug/mL, continue to cultivate respectively 24,48, after 72h, stop cultivating, if only add the matched group of culture fluid, each dosage group establishes 4 multiple holes.Experiment terminates front 4h, every hole adds 20ulMTT solution (5g/L), continue to hatch 4h, stop cultivating, careful suction abandons supernatant, every hole adds 150uLDMSO, concussion 10min, selects 570nm wavelength, and automatic enzyme connection detector measures each hole absorbance (A) value, repeat experiment 3 times, and calculate its growth inhibition ratio (CI).CI=(negative control group A value-experimental group A value)/negative control group A value × 100%.
1.5 Flow Cytometry Assay apoptosis rates
Collect 0,2.5,5.0, each group of cell of 10.0ug/mLSolanoeclepinA process 48h, PBS washs 2 times, adds 70% ethanol of pre-cooling in-20 DEG C of fixing 24h, 200uLPI dye liquor is added after centrifuge washing, 50ulRNA enzyme, 4 DEG C of lucifuges place the centrifugal 5min of 20min, 1500rpm.Adjustment cell concentration is 1 × 105/ml ~ 1 × 106/ml, and flow cytometer analysis, excitation source is argon laser, and excitation wavelength is 488nm.
1.6 this experimental result of statistical analysis applied statistics are analyzed
Software SPSS13.0 process, all experimental results adopt x ± s to represent, compare employing one factor analysis of variance between group.
2 results
The affect matched group HL-60 Growth of Cells of 2.1SolanoeclepinA on HL-60 cell and PBMC growth enlivens, through 0.625,1.25,2.5,5.0, the HouttuynoidB process of 10.0ug/mL 24,48, after 72h, HL-60 Growth of Cells slowing down all in various degree, and in the time, concentration dependent.Under same concentrations, cultivate 72hSolanoeclepinA to human PBMC's almost unrestraint effect, compare with HL-60 cell and have significant difference (P<0.05) (see table 1).
Table 1SolanoeclepinA is on the impact (x ± s, n=4) of HL-60 cell proliferation
* p<0.05**p<0.01 is compared with 24h; Compare with 48h
△p<0.05
△ △p<0.01; Compare with 72h
▲p<0.05
▲ ▲p<0.01
2.2 Flow cytometry HL-60 apoptosis
After the SolanoeclepinA effect 48h of HL-60 cell and variable concentrations, through flow cytometry analysis, result display has all occurred representing apoptotic hypodiploid peak before G1 phase peak, along with SolanoeclepinA concentration lift-rising is high within the scope of finite concentration, HL-60 apoptosis rate raises, and wherein 10.0ug/mLSolanoeclepinA effect 48h apoptosis rate reaches (22.16 ± 4.87) % (table 2).
Impact (x ± s, n=3) on HL-60 apoptosis rate after table 2SolanoeclepinA effect 48h
* p<0.05 is compared, * * p<0.01 with negative control group
Conclusion: SolanoeclepinA can suppress leukaemia's (HL-60 cell) to breed and inducing leukemia cell (HL-60 cell) apoptosis, therefore, can be used for treating leukemia.
Claims (1)
- The application of 1.SolanoeclepinA in treatment leukemia medicament, described compound S olanoeclepinA structure is as shown in formula I:
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| Application Number | Priority Date | Filing Date | Title |
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| CN201510794819.4A CN105287487A (en) | 2015-11-18 | 2015-11-18 | Applications of Solanoeclepin A in preparation of leukemia treatment drugs |
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| CN201510794819.4A CN105287487A (en) | 2015-11-18 | 2015-11-18 | Applications of Solanoeclepin A in preparation of leukemia treatment drugs |
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| CN105287487A true CN105287487A (en) | 2016-02-03 |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113234087A (en) * | 2021-05-12 | 2021-08-10 | 安顺市人民医院 | Solanoeclepin A structural analogue SMS-01 of tetranortriterpenes natural product |
-
2015
- 2015-11-18 CN CN201510794819.4A patent/CN105287487A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113234087A (en) * | 2021-05-12 | 2021-08-10 | 安顺市人民医院 | Solanoeclepin A structural analogue SMS-01 of tetranortriterpenes natural product |
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Application publication date: 20160203 |
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| WD01 | Invention patent application deemed withdrawn after publication |