CN106389433A - Application of hetrazan in preparing drug for treating psoriasis - Google Patents
Application of hetrazan in preparing drug for treating psoriasis Download PDFInfo
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- CN106389433A CN106389433A CN201611116017.9A CN201611116017A CN106389433A CN 106389433 A CN106389433 A CN 106389433A CN 201611116017 A CN201611116017 A CN 201611116017A CN 106389433 A CN106389433 A CN 106389433A
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- Prior art keywords
- hetrazan
- cell
- day
- human
- treating psoriasis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
Abstract
The invention discloses application of hetrazan in preparing a drug for treating psoriasis. The adult administration dosage of hetrazan is 60-70 mg/kg/day, preferably 63-66 mg/kg/day, and the optimal dosage is 64 mg/kg/day. Through human promyelocytic leukemia cell (HL-60 cell) differentiation promoting experiments, human immortal keratinized cell and Michigan cancer fund-7 breast cancer cell proliferation inhibiting experiments and in-vivo blood calcium activity improving experiments, it can be concluded that hetrazan has high affinity to VDR acceptors, has a high inhibiting effect on proliferation of human keratinized cells and human breast cancer cells, has weak capacity of increasing blood calcium and can be used for treating psoriasis at different degrees.
Description
Technical field
The present invention relates to technical field of western medicines, specifically a kind of hetrazan is in preparation treatment psoriasis
Application.
Background technology
Psoriasis is commonly called as " psoriasis ", is a kind of common chronic inflammatory skin being easy to recur, characteristic lesions
For the multilayer silvery white scales of skin that peel off is covered with red papules or patch.At most, male sex's morbidity is more than women, and the north is more than between twenty and fifty morbidity
South, winter in spring is easily sent out or increases, and alleviates summer and autumn more.Etiology and pathogenesis are completely clear and definite, and research finds, the sending out of this disease
Disease and inherent cause, infection streptococcus, immunologic dysfunction, dysbolism and hormonal change etc. are relevant.Clinically there are four kinds
Type：Homeliness type, pustular type, erythrodermic and arthropathica.
Psoriasis is not a kind of infectious disease, and the communicable tinea disease of it and tinea of feet and hands etc is different, is a kind of inflammation
Rather than by fungus-caused disease.Why patients congregate in some places, are because everybody similar living environment, family
Race's genetic predisposition, identical predisposition thereto etc. leads to, and is not to infect to cause.The psoriatic cause of disease：1. environment：For a long time
Live in the relatively dry or cold place of weather.2. heredity：The patient that there are about 15-30% has family's morbidity history.3. disease：
Permanent immunity function or cryptorrhea.Have been reported that the psoriatic of 10-20% is often accompanied by acute upper respiratory infection medical history.
4. damage：The various damage of skin, infection can induce.
Hetrazan, to filaria adult（In addition to filaria volvulus）And microfilaria all has killing action.Specifically, citron
Acid diethylamide piperazine is used for bancroft's filaria, Wuchereria malayi and infection by Loa loa, is also used for onchocercosis.Once or many to former three
Can effect a radical cure after secondary treatment, but to onchocercosis, because this product can not kill adult, therefore can not effect a radical cure, also can be used for tropical acidophilus
Polycythemia patient, additionally, hetrazan is also effective to roundworm infection.At present, hetrazan is used only for
Expelling parasite, its effect in addition to expelling parasite need to study further.
Content of the invention
It is an object of the invention to provide a kind of new opplication of hetrazan, specifically it is in preparation treatment psoriasis
Application in medicine.
For achieving the above object, the present invention provides following technical scheme：
Application in preparation treatment psoriasis for the hetrazan.
As the further scheme of the present invention：Adult's dosage of described hetrazan is 60-70mg/kg/
Day.
As the further scheme of the present invention：Adult's dosage of described hetrazan is 63-66mg/kg/
Day.
As the further scheme of the present invention：Adult's dosage of described hetrazan is 64mg/kg/ day.
Compared with prior art, the invention has the beneficial effects as follows：
In the present invention, through promoting people in loop（HL-60 cell）Analytical Chemical Experiment, suppression people's immortality keratinocyte
Test with the experiment of Michigan cancer foundation -7 Cells Proliferation of Human Breast Cancer, the internal calcemic activities that rise, draw to draw a conclusion：Citric acid
Diethylcarbamazine has stronger affinity to VDR acceptor, has stronger suppression to make people's keratinocyte and human breast cancer cell propagation
With, and the ability of its liter of hypercalcemia is very weak, can be used for treating different degrees of psoriasis.
Specific embodiment
Below in conjunction with the embodiment of the present invention, the technical scheme in the embodiment of the present invention is clearly and completely described,
Obviously, described embodiment is only a part of embodiment of the present invention, rather than whole embodiments.Based in the present invention
Embodiment, the every other embodiment that those of ordinary skill in the art are obtained under the premise of not making creative work, all
Belong to the scope of protection of the invention.
Embodiment 1
In the embodiment of the present invention, application in preparation treatment psoriasis for the hetrazan, this hetrazan
Adult's dosage is 60-70mg/kg/ day, and preferably adult's dosage is 63-66mg/kg/ day, dosage of being most preferably grown up
For 64mg/kg/ day.Specifically, using auxiliary material acceptable in pharmacy and technique, hetrazan is made treatment silver bits
Medicine, you can for psoriatic treatment.
To illustrate hetrazan to psoriatic therapeutic action below by animal experiment.
Test example 1
Promote people in loop（HL-60 cell）Analytical Chemical Experiment（Vitamin D receptor agonist activity is tested）
Experimental technique：Take the logarithm the HL-60 cell in growth period, adjustment cell density is 1 × 104The cell suspension of individual living cells,
Arrange tested group according to requirement of experiment（Hetrazan）, positive controls（Tacalcitol）, negative control group（Non- open loop steroid
Body biostearin D acceptor (VDR) activator LG190155）, every group sets 3 parallel holes, is placed in 37 DEG C, 5%CO2And saturated humidity
Incubator in culture 96h.200 μ L are added to contain phorbol exters（TPA, final concentration of 200ng ml-1）1%NBT solution mixing, put into
37 DEG C of incubation 30min, then supernatant will be removed after cell centrifugation, every part of sample adds the dimethyl sulfoxide (DMSO) of 150 μ L, shakes under room temperature
Swing 20min, survey the absorbance under 570nm wavelength, after be converted into medium effective concentration.
Experimental result is as follows：The medium effective concentration of hetrazan is 0.032 μM, and the half of Tacalcitol is effectively dense
Spend for 0.007 μM, the medium effective concentration of LG190155 is 9.700 μM, illustrates that hetrazan has and Tacalcitol phase
Similar good vitamin D receptor agonist activity.
Test example 2
Suppression people's immortality keratinocyte（HaCaT cell）With Michigan cancer foundation -7 breast cancer cell（MCF-7 cell）
Proliferation experiment
Experimental technique：Take the logarithm the HaCaT cell in growth period and MCF-7 cell, adjustment cell density is 2 × 104Individual/ml, connects
Plant every hole inoculating cell suspension 200 μ L in 3 piece of 96 well culture plate；Tested group, positive controls, negative control group；Cell connects
Plant dosing after 24h, every group sets 3 parallel holes, is placed in 37 DEG C, 5%CO2And culture in the incubator of saturated humidity, cultivate 48h respectively
After abandon supernatant, every hole adds the DMEM nutrient solution of the MTT and 200 μ L that 20 μ L concentration are 5mg/ml to continue culture 4h, and every hole adds 150
μ L dimethyl sulfoxide (DMSO) vibrates 10min on shaking table, measures the OD value of wavelength 570nm with ELIASA（D570）Experiment repetition 3
Secondary, after be converted into medium effective concentration.
Experimental result is as follows：Hetrazan suppresses the medium effective concentration of keratinocyte propagation to be 2.24 μM, suppression
The medium effective concentration of Cells Proliferation of Human Breast Cancer processed is 0.45 μM, and Tacalcitol suppresses the half of keratinocyte propagation effectively dense
Spend for 2.07 μM, the medium effective concentration of suppression Cells Proliferation of Human Breast Cancer is 0.06 μM, LG190155 suppression keratinocyte increases
The medium effective concentration grown is 16.62 μM, and the medium effective concentration of suppression Cells Proliferation of Human Breast Cancer is 1.05 μM, and citric acid is described
Diethylcarbamazine has the activity of the good suppression keratinocyte similar with Tacalcitol and breast cancer tumor cells propagation.
Test example 3
Internal liter calcemic activities
Experimental technique：10 weeks cleaning grade mouse, average weight is 22 ± 2g；This mouse is randomly divided into 5 groups, every group 10 little
Mouse, respectively blank group（Physiological saline）, control group Tacalcitol（5μg/kg）, hetrazan low dosage（32mg/kg）、
Hetrazan middle dosage（64mg/kg）, and hetrazan high dose（128mg/kg）.Before administration, experiment mice is daily
Give 40mg calcium, the forage feed of 200mg phosphorus and 40 unit vitamin D, weigh once within every 3 days.After raising 7 days, each component
Other subcutaneous administrations, are administered 7 days, blank group gives equal volume physiological saline, freely takes the photograph under relative humidity 65% environment altogether
Water, ingest, weigh 1 time within every 3 days.
Experimental result is as follows：The blood calcium concentration of blank group is 8.7mg/dl, and the blood calcium concentration of control group is 10.3mg/dl,
The blood calcium concentration of hetrazan low dosage is 8.3mg/dl, and the blood calcium concentration of hetrazan middle dosage is 8.6mg/
Dl, the blood calcium concentration of hetrazan low dosage is 8.5mg/dl, illustrates that hetrazan no affects on calcium level.
In sum：Hetrazan have excellent vitamin D receptor agonist activity, suppression people's keratinocyte and
The activity of human breast cancer cells propagation, and it is very weak to rise blood calcium ability.Therefore, hetrazan can be used for treat by
The psoriasis of vitamin D receptor mediation.
It is obvious to a person skilled in the art that the invention is not restricted to the details of above-mentioned one exemplary embodiment, Er Qie
In the case of the spirit or essential attributes of the present invention, the present invention can be realized in other specific forms.Therefore, no matter
From the point of view of which point, embodiment all should be regarded as exemplary, and be nonrestrictive, the scope of the present invention is by appended power
Profit requires rather than described above limits, it is intended that all in the implication and scope of the equivalency of claim by falling
Change is included in the present invention.
Moreover, it will be appreciated that although this specification is been described by according to embodiment, not each embodiment only wraps
Containing an independent technical scheme, only for clarity, those skilled in the art should for this narrating mode of specification
Using specification as an entirety, the technical scheme in each embodiment can also form those skilled in the art through appropriately combined
Understandable other embodiment.
Claims (4)
1. application in preparation treatment psoriasis for the hetrazan.
2. hetrazan according to claim 1 preparation treatment psoriasis in application it is characterised in that
Adult's dosage of described hetrazan is 60-70mg/kg/ day.
3. hetrazan according to claim 2 preparation treatment psoriasis in application it is characterised in that
Adult's dosage of described hetrazan is 63-66mg/kg/ day.
4. hetrazan according to claim 3 preparation treatment psoriasis in application it is characterised in that
Adult's dosage of described hetrazan is 64mg/kg/ day.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201611116017.9A CN106389433A (en) | 2016-12-07 | 2016-12-07 | Application of hetrazan in preparing drug for treating psoriasis |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201611116017.9A CN106389433A (en) | 2016-12-07 | 2016-12-07 | Application of hetrazan in preparing drug for treating psoriasis |
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| Publication Number | Publication Date |
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| CN106389433A true CN106389433A (en) | 2017-02-15 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN201611116017.9A Pending CN106389433A (en) | 2016-12-07 | 2016-12-07 | Application of hetrazan in preparing drug for treating psoriasis |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102740888A (en) * | 2009-11-24 | 2012-10-17 | 奥尔德生物制药公司 | Antibodies to IL-6 and use there |
| CN103193695A (en) * | 2013-04-22 | 2013-07-10 | 中国药科大学 | 3-phenyl-3-pyrrolyl pentane derivative and medical application thereof |
-
2016
- 2016-12-07 CN CN201611116017.9A patent/CN106389433A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102740888A (en) * | 2009-11-24 | 2012-10-17 | 奥尔德生物制药公司 | Antibodies to IL-6 and use there |
| CN103193695A (en) * | 2013-04-22 | 2013-07-10 | 中国药科大学 | 3-phenyl-3-pyrrolyl pentane derivative and medical application thereof |
Non-Patent Citations (1)
| Title |
|---|
| "《中国医师药师临床用药指南》" * |
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Application publication date: 20170215 |
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