CN108785290A - The purposes of Resina Draconis chalcones active ingredient in medicine preparation - Google Patents
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Abstract
The present invention relates to field of medicaments, more particularly to the medical usage of a kind of Resina Draconis and its active ingredient.The present invention provides a kind of Resina Draconis and its chalcones active ingredient to prepare the purposes in inhibiting osteoclast formation or inhibiting the drug or health products of osteoclastic bone resorption.At least one purposes for being used to prepare the drug or health products that inhibit osteoclast formation or inhibition osteoclastic bone resorption of 3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one, lourerin B, dragon's blood element C, dragon's blood element D, sword-like leave 3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one or cochinchinenin C.The drug of preparation can be used for treating and preventing osteolytic disease.Resina Draconis Small side effects, it is non-toxic, it can take for a long time for preventing and treating administration.
Description
Technical field
The present invention relates to field of medicaments, more particularly to the medical usage of a kind of Resina Draconis and active ingredient.
Background technology
Normal bone tissues are tissues that is dynamic, persistently sexually revising in human body, rely primarily on the bone remoulding work(of osteoblast
Can, the bone information function of osteoclast carry out remolded configuration.It is this when the increase of internal amount of osteoclast or the enhancing of bone information function
Bone stable state will be broken, and to induce various osteolytic relevant diseases, such as osteoporosis, be mainly shown as that bone tissue is micro-
Structure is destroyed, and bone density reduction causes bone strength to reduce, brittleness increases etc..
Resina Draconis extracts from babassu Sanguis Draxonis or Liliaceae dracaena plant swordleaf dragon tree [national standard：
WS3-082 (Z-016) -99 (Z)], it is common drug in tcm clinical practice,《Sheng Nong's herbal classic》Reputation is " promoting blood circulation panacea ", existing
Think it with a variety of physiological activity such as anti-oxidant, antibacterial, anti-inflammatory, antithrombotic for pharmaceutical research.Research reports that it can be used for
The treatment of hypertrophic scar, diabetes or angiocardiopathy, or have the effect of analgesic.There are many chemical compositions of Resina Draconis,
Middle 3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one, lourerin B, dragon's blood element C, dragon's blood element D, sword-like leave 3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one and cochinchinenin C etc. belong to chalcones
Close object.
Invention content
Resina Draconis is provided it is an object of the invention to overcome in place of above-mentioned the deficiencies in the prior art and chalcones are effective
The medical usage of ingredient.
To achieve the above object, the technical solution that the present invention takes is：Inventor studies the chalcone found in Resina Draconis
Effective constituents can inhibit osteoclast formation or inhibit bone information function, therefore it provides chalcones in a kind of Resina Draconis
Active ingredient is preparing the purposes in inhibiting osteoclast formation or inhibiting the drug or health products of osteoclastic bone resorption.
In a preferred example, the active ingredient is 3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one, lourerin B, dragon's blood element C, dragon's blood element D, sword-like leave dragon's blood element
A, at least one of cochinchinenin C.
3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one, lourerin B, dragon's blood element C, dragon's blood element D, sword-like leave 3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one, the structural formula of cochinchinenin C are as follows：
3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one,Lourerin B,
Dragon's blood element C,Dragon's blood element D,Sword-like leave 3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one,Cochinchinenin C.
Inventor has carried out drug efficacy study to it, the results showed that 3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one, lourerin B, dragon's blood element C, dragon's blood element D, sword-like leave
3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one, cochinchinenin C can inhibit osteoclast formation or inhibit osteoclastic bone resorption.
In a preferred example, the 3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one, lourerin B, dragon's blood element C, dragon's blood element D, sword-like leave 3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one and sword-like leave dragon
Sanguinin C inhibits osteoclast formation by inhibiting or weakening the effect of RANKL or inhibits osteoclastic bone resorption.
In a preferred example, the 3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one, lourerin B, dragon's blood element C, dragon's blood element D, sword-like leave 3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one and sword-like leave dragon
Sanguinin C is by inhibiting or weakening TRAcP genes, V-ATPase-d2 genes, CTSK genes, MMP9 genes, Calcitonin
Receptor genes, NFATc1 albumen, the expression of V-ATPase-d2 albumen or cathepsin K albumen or active oxygen generate into
And inhibits osteoclast formation or inhibit osteoclastic bone resorption.
The present invention also provides a kind of Resina Draconis to prepare the medicine for inhibiting osteoclast formation or inhibiting osteoclastic bone resorption
Purposes in object or health products.
In a preferred example, the drug for inhibiting osteoclast formation or inhibiting bone information function or health products are for molten
Bone disease.
In another preferred example, the osteolytic disease is osteoporosis, Paget osteopathy, osteomyelitis, bone cyst, bone
Myeloma, metastatic tumor of bone, osteoblastoma, nonossifying fibroma, giant cell tumor of bone.
3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one, lourerin B, dragon's blood element C, dragon's blood element D, sword-like leave 3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one, the cochinchinenin C of the present invention can pass through
The conventional method of this field is extracted from Resina Draconis and is obtained, and also can be bought or be utilized marketable material by commercial sources, pass through
Traditional compound synthesis method synthesis in the prior art obtains.Those skilled in the art can according to existing known technology
To synthesize the compound of the present invention.The compound of synthesis can further pass through column chromatography, high performance liquid chromatography or crystallization
Etc. modes be further purified.
Drug prepared by the purposes of the present invention can be by oral, intravenous, intramuscular, subcutaneous, nasal cavity, in rectum etc.
Approach is administered.Solid carrier is such as：Starch, lactose, phosphoric acid glycol, microcrystalline cellulose, brown sugar and white bole, pharmaceutical dosage form can be
Tablet, pulvis, and liquid carrier is such as：Sterile water, polyethylene glycol, nonionic surface active agent and edible oil (such as corn oil, flower
Oil generation and sesame oil), as long as being suitble to the characteristic of active constituent and required specific administration mode.In preparing pharmaceutical composition
Usually used adjuvant also can advantageously by including, e.g., flavoring agent, pigment, preservative and antioxidant such as vitamin E and Wei Sheng
Plain C.
The beneficial effects of the present invention are：Resina Draconis and 3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one, lourerin B, dragon's blood element C, dragon's blood element D, sword-like leave dragon's blood
Plain A or cochinchinenin C can inhibit osteoclast formation or inhibit osteoclastic bone resorption, can be used for preparing inhibition osteoclastic
Cell forms or inhibits the drug or health products of osteoclastic bone resorption.Resina Draconis Small side effects there is no the report of Resina Draconis toxicity
Road can be taken for a long time for preventing and treating administration.The details of various aspects of the present invention will be detailed in subsequent embodiment
Description will become apparent from by describing the features of the present invention and advantage.
Description of the drawings
Fig. 1 embodiments 1 inhibit osteoclast Analytical Chemical Experiment result figure.
The LrB of 1 various concentration gradient of Fig. 2 embodiments inhibits osteoclast to induce Analytical Chemical Experiment result figure.
Fig. 3 embodiments 2 inhibit bone information contractile studies figure.
3 inhibitory activity oxygen (ROS) of Fig. 4 embodiments generates experimental result picture.
4 gene expression detection experimental result picture of Fig. 5 embodiments.
5 protein expression assay result figure of Fig. 6 embodiments.
6 castration mouse osteoporosis model experimental result picture of Fig. 7 embodiments.
Specific implementation mode
The present inventor has found through laboratory research：3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one, lourerin B, dragon's blood element C, dragon's blood element D, sword-like leave 3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one
And cochinchinenin C can inhibit osteoclast formation and osteoclastic bone resorption, can inhibit bone loss, thus prove this
The Resina Draconis chalcones chemical composition of invention can be used for preparing the medicine for inhibiting osteoclast formation or inhibiting bone information function
Object or health products, for preventing or treating osteolytic disease.
Embodiment 1 inhibits osteoclast Analytical Chemical Experiment
1.1 purpose：Study 3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one (LrA), lourerin B (LrB), dragon's blood element C (LrC), dragon's blood element D (LrD), sword-like leave
Effect in osteoclast atomization of 3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one (CcA) and cochinchinenin C (CcC) and to Bone Marrow Macrophage
Toxicity.
1.2 materials and reagent
3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one (LrA), lourerin B (LrB), dragon's blood element C (LrC), dragon's blood element D (LrD), sword-like leave 3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one (CcA)
And cochinchinenin C (CcC) is purchased from the Chengdu bio tech ltd Man Site (Sichuan Province Chengdu)；α-MEM culture mediums,
FBS (fetal calf serum) is purchased from gibco companies (Sydney, AUS city)；β-actin antibody, NFATc1 antibody, V-ATPase-d2
Antibody, CTSK antibody are purchased from Santa Cruz Biotechnology companies (California, USA)；MTS measure reagents
Box, ROS (active oxygen) reaction kit, PCR reaction kits are purchased from Promega companies (Sydney, AUS city)；M-CSF
(macrophage colony stimulating factor) reagent, RANKL (Nuclear factor kappa beta ligands) reagent are purchased from Australian University of West Australia School
Of Pathology and Laboratory Medicine (Perth, AUS city).
1.3 experimental method
Take healthy 12 week old C57BL/6J mouse (SPF grades, Australian University of West Australia School of
The laboratories Pathology and Laboratory Medicine provide), after ether inhalation anesthesia, using cervical dislocation
It puts to death.Mouse bilateral femur and shin bone are removed rapidly, in the culture dish for filling α-MEM culture mediums, rejects clean musculature,
Exposure ossis；Using 5ml syringes, marrow in pulp cavity is gone out into another clean culture dish, mixing is blown and beaten.Use strainer
The impurity in bone marrow suspension is filtered out, suspension is then centrifuged for, retains precipitation；(contain 10% tire ox blood using complete α-MEM culture mediums
Clearly, 1%P/S (penicillin/streptomycin) and 1:Precipitation 20M-CSF) is resuspended.By in the bone marrow neoplasms after resuspension to T75 culture bottles,
It is cultivated in cell incubator, replaces complete medium within the 2nd day, a subculture is then replaced every other day, until C57BL/6J mouse
Bone marrow macrophage (BMMs) is ripe (the about the 5th day long to 95% area of covering culture bottle).
Freshly extd C57BL/6J Bone Marrow Macrophages (BMMs) are being contained into complete medium (α-MEM cultures
Base+10%FBS+1%P/S+5%M-CSF) T75 culture bottles in cultivate, it is thin with every hole 6x103 after BMMs differentiation and maturations
The ratio kind of born of the same parents enters in 96 orifice plates.The RANKL for starting to be added 50ng/ul for second day per hole carries out osteoclast differentiation, experimental group
It is separately added into 3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one, lourerin B, dragon's blood element C, dragon's blood element D, sword-like leave 3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one and the cochinchinenin C of 10uM, control group
The PBS of same volume is added simultaneously.Primary differentiation liquid is replaced within every two days, until osteoclast differentiation and maturation.Wait for osteoclast point
Be melted into it is ripe after, fix 15 minutes using 2.5% glutaraldehyde, then carry out TRAcP (Tartrate resistant acid phosphatase) dye, mirror
Lower statistics each group osteoclast (nucleus amount >=3) quantity.
Freshly extd C57BL/6J Bone Marrow Macrophages (BMMs) are being contained into complete medium (α-MEM cultures
Base+10%FBS+1%P/S+5%M-CSF) T75 culture bottles in cultivate, it is thin with every hole 6x103 after BMMs differentiation and maturations
The ratio kind of born of the same parents enters in 96 orifice plates.The RANKL for starting to be added 50ng/ul for second day per hole carries out osteoclast differentiation, experimental group
It is separately added into the dragon's blood lourerin B of 1,2.5,5,10uM, the PBS of same volume is added in control group simultaneously.It replaces within every two days primary
Break up liquid, until osteoclast differentiation and maturation.After osteoclast differentiation and maturation, 15 minutes are fixed using 2.5% glutaraldehyde,
It then carries out TRAcP (Tartrate resistant acid phosphatase) to dye, statistics each group osteoclast (nucleus amount >=3) number under mirror
Amount.
By the BMMs of differentiation and maturation with every hole 6x103The ratio kind of a cell enters in 96 orifice plates, proceeds by within second day dry
In advance：Experimental group is separately added into 3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one, lourerin B, dragon's blood element C, dragon's blood element D, sword-like leave 3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one and the sword-like leave of 10uM per hole
The PBS of same volume is added in dragon's blood element C, control group, and it is small that 48 are cultivated in the α-MEM culture mediums containing 10%FBS and 1%P/S
When, 20ul MTS reagents are then added per hole, use ELISA reading machines (German BMG) to detect 490nm after being protected from light culture 2 hours
Luminosity number is to determine MTS absorbances.
1.4 experimental result
As a result show that the amount of osteoclast of experimental group is considerably less than control group, 3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one, lourerin B, dragon's blood element C, dragon
Sanguinin D, sword-like leave 3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one and cochinchinenin C have a degree of inhibiting effect, wherein LrB to the formation of osteoclast
Inhibiting effect it is most apparent (Fig. 1 c, d).Toxicity test for each ingredient is the results show that each ingredient (schemes BMMs nontoxicitys
1b).Meanwhile this research intervenes the induction atomization of osteoclast using the LrB of various concentration gradient, as a result shows
Show, LrB starts to inhibit the formation of osteoclast, the inhibiting effect of 10uM concentration more apparent in low concentration (2.5uM).(figure
2)
Embodiment 2 inhibits bone information functional experiment
2.1 purpose：Study 3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one (LrA), lourerin B (LrB), dragon's blood element C (LrC), dragon's blood element D (LrD), sword-like leave
The effect of 3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one (CcA) and cochinchinenin C (CcC) to bone information function.
2.2 experiment materials are the same as embodiment 1
2.3 experimental method
By the BMMs of differentiation and maturation with every hole 1x105Osteoclast differentiation is carried out in a cell kind to collagen plate, until broken
Osteocyte initially forms, and then cell is transferred in hydroxy-apatite slabstone, continues osteoclast induction, experimental group difference
3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one, lourerin B, dragon's blood element C, dragon's blood element D, sword-like leave 3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one and the cochinchinenin C of 10uM is added, control group is simultaneously
The PBS of same volume is added.After osteoclast differentiation and maturation, the half bore in same group of cell is subjected to TRAcP dyeing, it is another
Partly rinsed, dried, observe amount of osteoclast and hydroxyapatite absorbing state respectively, and using Image J softwares into
Row quantitative analysis.
2.4 experimental result
As a result show that the bone information area of experimental group bone plate is significantly less than control group, 3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one, lourerin B, dragon's blood element C,
Dragon's blood element D, sword-like leave 3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one and cochinchinenin C have a degree of inhibiting effect to the bone information function of osteoclast,
The wherein inhibiting effect of LrB is most apparent.(Fig. 3)
3 inhibitory activity oxygen (ROS) of embodiment generates experiment
3.1 purpose：Lourerin B (LrB) is studied in RANKL induces osteoclast atomization, active oxygen (ROS) is produced
Raw effect.
3.2 experiment materials are the same as embodiment 1
3.3 experimental method
By the BMMs of differentiation and maturation with every hole 6x103The ratio kind of a cell enters in 96 orifice plates.Start within second day to add per hole
The RANKL for entering 50ng/ul carries out osteoclast differentiation, while experimental group is separately added into the LrB of 10uM, and same volume is added in control group
Long-pending PBS replaces primary differentiation liquid for every two days.Use within 4th day 2', 7'- dichlorofluorescins diacetate esters (H2DCF) examination
Agent carries out fluorescent staining, horizontal using Nikon confocal microscopy each groups ROS, and uses NIS-Elements Viewer
Software analysis of fluorescence intensity.
3.4 experimental result
The results show that early stage osteoclast formation (third day), the LrB of 10uM can apparent inhibitory activity oxygen production
It is raw.(Fig. 4)
4 gene expression detection of embodiment is tested
4.1 purpose：LrB is studied to the RANKL osteoclast formations induced and the relevant gene expression of bone information function
It influences.
4.2 experiment materials are the same as embodiment 1
4.3 experimental method
By the BMMs of differentiation and maturation with every hole 8x104The ratio kind of a cell enters in 6 orifice plates.Start within second day to be added per hole
The RANKL of 50ng/ul carries out osteoclast differentiation, while experimental group is separately added into the LrB of 5uM, 10uM, and control group is added identical
The PBS of volume replaces a subculture in every two days.After the 6th day (osteoclast differentiation and maturation), Trizol lysates are used
Lytic cell, and extract RNA；Reverse transcription is carried out using Oligo-dT, then using SYBR Green methods, use
ViiATM7Real-time PCR instruments are detected, and target gene primer sequence is respectively：
TRAcP(5'-T GTGGCCATCTTTATGCT-3'；5'-GTCATTTCTTTGGGGCTT-3'), V-ATPase-d2
(5'-GTGAGACCTTGGAAGACCTGAA-3'；
5'-GAGAAATGTGCTCAGGGGCT-3'), CTSK (5'-GGGAGAAAAACCTGAAGC-3'；5'-
ATTCTGGGGACTCAGAGC-3'), MMP9 (5'-CGTGTCTGGAGATTCGACTTGA-3'；
5'-TTGGAAACTCACACGCCAGA-3'), Calcitonin receptor (5'-
TGGTTGAGGTTGTGCCCA-3'；5'-CTCGTGGGTTTGCCTCATC-3').
Each target gene expression quantity is analyzed using △ △ Ct methods.
4.4 experimental result
Research selects the LrB of various concentration gradient to intervene the osteoclast formation that RANKL is induced, the results show that LrB is to broken
Osteocyte forms relevant TRAcP, bone information function relevant V-ATPase-d2, CTSK and MMP9, Calcitonin
The gene expressions such as Receptor have inhibiting effect, and are in dose dependent.(Fig. 5)
5 protein expression assay of embodiment
5.1 purpose：LrB is studied to the RANKL osteoclast formations induced and the relevant protein expression of bone information function
Effect.
5.2 experiment materials are the same as embodiment 1.
5.3 experimental method
By the BMMs of differentiation and maturation with every hole 8x104The ratio kind of a cell enters in 6 orifice plates.Start within second day to be added per hole
The RANKL of 50ng/ul carries out induction osteoclast differentiation, while the LrB of 10uM is added in experimental group, and same volume is added in control group
PBS, every two days replace a subculture.After the 6th day (osteoclast differentiation and maturation), cracked using RIPA lysates thin
Born of the same parents, and extract albumen.Using SDS-PAGE electrophoresis liquid protein isolates, transferring film is carried out using nitrocellulose membrane, then in 4 DEG C of environment
NFATc1, V-ATPase-d2, CTSK and β-actin protein antibodies are incubated overnight, are incubated corresponding secondary antibody 2 hours, are then used
ECL developer solutions, 4000 visualizers of LAS develop.Image is analyzed using Gel-pro softwares.
5.4 experimental result
The results show that LrB obviously inhibits NFATc1 protein expressions relevant to osteoclast formation in third day；In third
It start to inhibit with relevant V-ATPase-d2, CTSK protein expression of bone information function, wherein be inhibiting effect at the 5th day compared with
It is apparent.(Fig. 6)
6 castration mouse osteoporosis model of embodiment
6.1 purpose：Study effects of the LrB to osteoporosis caused by estrogen deficiency mouse
6.2 experiment material
10 week old C57BL/6J female mices are bought from Traditional Chinese Medicine University Of Guangzhou's animal experimental center, other are the same as embodiment 1.
6.3 experimental method
Zoopery carries out in animal experimental center SPF grades of animal house of Traditional Chinese Medicine University Of Guangzhou, animal protocols and
Ethic review has submitted a report asking for the approval of Animal Experimental Ethical examination board of Traditional Chinese Medicine University Of Guangzhou.24 10 week old C57BL/6J are female
Property mouse adaptability raise 1 week after, be randomly divided into two groups：Model group (OVX) 16, sham-operation group (Sham) 8, OVX groups row
Back bilateral notch gives and extracts bilateral ovaries and ligature bilateral salpingo, and Sham groups give the bilateral notch of same OVX groups, but do not pluck
Except ovary or tubal ligation.After adaptability is raised 3-5 days, OVX groups are divided into two groups at random：Control group (OVX+PBS) group 8
Only, experimental group (OVX+LrB) 8；The same period intervenes mouse with LrB solution or PBS：(OVX+LrB) group gives intraperitoneal injection
LrB solution (4mg/kg), (OVX+PBS) and Sham groups give intraperitoneal injection same volume PBS, inject 1 time within every 2 days, co-injection 20
It is secondary.After (about 6 weeks) are completed in injection, same period row cervical dislocation puts to death three groups of mouse, carries out bilateral femur bone tissue materials.With stock
Bone lower end is region of interest, carries out micro-CT scannings to each group femur respectively, to observe the variation of bone tissue micro-structure, and makes
It is rebuild with NRecon softwares, region of interest (the 1mm ranges of 0.5mm under epiphysis) is quantitatively divided using CTAn softwares
Analysis carries out three-dimensional reconstruction using CTvox softwares to region of interest.
6.4 experimental result
Micro-CT scannings, analysis are carried out by region of interest of distal femur, the results show that with sham-operation group (Sham) phase
Than trabecular volume (BV/TV), bone trabecula quantity (Tb.N) and the bone trabecula thickness (Tb.Th) of model group are substantially reduced, and bone is small
Beam dispersion (Tb.Sp) obviously increases.This shows that this experimental animal models successfully.Compared with model group, the bone trabecula of LrB groups
Volume and bone trabecula quantity obviously increase, and bone trabecula dispersion is substantially reduced.(Fig. 7 b) distal femur region of interest cancellous bone three
It is consistent with above-mentioned quantitative analysis results to tie up reconstruction model.(Fig. 7 a) the above result shows that, LrB can inhibit female to a certain extent
Anhormonia causes osteoporosis.
Finally, it should be noted that the above embodiments are merely illustrative of the technical solutions of the present invention rather than is protected to the present invention
The limitation of range is protected, although being explained in detail to the present invention with reference to preferred embodiment, those skilled in the art should
Understand, technical scheme of the present invention can be modified or replaced equivalently, without departing from the essence of technical solution of the present invention
And range.
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<213>Artificial sequence
<400> 4
cgtgtctgga gattcgactt gattggaaac tcacacgcca ga 42
<210> 5
<211> 37
<212> DNA
<213>Artificial sequence
<400> 5
tggttgaggt tgtgcccact cgtgggtttg cctcatc 37
Claims (8)
1. chalcones active ingredient is preparing the medicine for inhibiting osteoclast formation or inhibiting osteoclastic bone resorption in Resina Draconis
Purposes in object or health products.
2. purposes according to claim 1, which is characterized in that the active ingredient is 3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one, lourerin B, dragon's blood element
C, at least one of dragon's blood element D, sword-like leave 3-(2,4-Dimethoxy-phenyl)-1-(4-hydroxy-phenyl)-propan-1-one, cochinchinenin C.
3. purposes according to claim 2, which is characterized in that the active ingredient is by inhibiting or weakening the work of RANKL
With inhibition osteoclast formation in turn or inhibit osteoclastic bone resorption.
4. purposes according to claim 3, which is characterized in that the active ingredient by inhibit or weaken TRAcP genes,
V-ATPase-d2 genes, CTSK genes, MMP9 genes, Calcitonin Receptor genes, NFATc1 albumen, V-
The expression of ATPase-d2 albumen or cathepsin K albumen or active oxygen generate and then inhibit osteoclast formation or inhibit broken
Osteoclastic bone resorption.
5. Resina Draconis is preparing the purposes in inhibiting osteoclast formation or inhibiting the drug or health products of osteoclastic bone resorption.
6. according to the purposes described in claim 1-5 any one, which is characterized in that the drug or health products are used for osteolytic
Disease.
7. purposes according to claim 6, which is characterized in that the osteolytic disease is osteoporosis, Paget bones
Disease, osteomyelitis, bone cyst, myeloma, metastatic tumor of bone, osteoblastoma, nonossifying fibroma, giant cell tumor of bone.
8. purposes according to claim 6, which is characterized in that the dosage form of the drug is solid-state tablet, pulvis.
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109771544A (en) * | 2019-02-28 | 2019-05-21 | 武汉互联益嘉实科技有限公司 | A kind of preparation method and application of Sanguis Draxonis flavoniod |
| CN110538174A (en) * | 2019-09-26 | 2019-12-06 | 刘予豪 | Application of dracorhodin in preparing medicine |
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| CN102406787A (en) * | 2011-05-12 | 2012-04-11 | 中南民族大学 | Application of dragon's blood and flavonoid chemical component thereof in serving as antagonist of capsaicin receptor TRPV1 (transient receptor potential vanilloid 1) |
| CN105153100A (en) * | 2015-09-14 | 2015-12-16 | 丽水市农业科学研究院 | Preparation method and application of flavonoid compounds in dragon's blood |
| CN107625759A (en) * | 2017-09-11 | 2018-01-26 | 广州中医药大学第附属医院 | Application of the cajanin in suppressing osteoclast formation and preventing osteoporosis agents |
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2018
- 2018-04-18 CN CN201810358407.XA patent/CN108785290B/en active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102406787A (en) * | 2011-05-12 | 2012-04-11 | 中南民族大学 | Application of dragon's blood and flavonoid chemical component thereof in serving as antagonist of capsaicin receptor TRPV1 (transient receptor potential vanilloid 1) |
| CN105153100A (en) * | 2015-09-14 | 2015-12-16 | 丽水市农业科学研究院 | Preparation method and application of flavonoid compounds in dragon's blood |
| CN107625759A (en) * | 2017-09-11 | 2018-01-26 | 广州中医药大学第附属医院 | Application of the cajanin in suppressing osteoclast formation and preventing osteoporosis agents |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109771544A (en) * | 2019-02-28 | 2019-05-21 | 武汉互联益嘉实科技有限公司 | A kind of preparation method and application of Sanguis Draxonis flavoniod |
| CN109771544B (en) * | 2019-02-28 | 2021-11-30 | 中南民族大学 | Preparation method and application of dragon's blood total flavone |
| CN110538174A (en) * | 2019-09-26 | 2019-12-06 | 刘予豪 | Application of dracorhodin in preparing medicine |
| CN110538174B (en) * | 2019-09-26 | 2023-03-07 | 刘予豪 | Application of dracorhodin in preparing medicine |
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| Publication number | Publication date |
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| CN108785290B (en) | 2021-03-16 |
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