CN110075104A - Kuwanon H is preparing the application in osteosporosis resistant medicament - Google Patents
Kuwanon H is preparing the application in osteosporosis resistant medicament Download PDFInfo
- Publication number
- CN110075104A CN110075104A CN201910513956.4A CN201910513956A CN110075104A CN 110075104 A CN110075104 A CN 110075104A CN 201910513956 A CN201910513956 A CN 201910513956A CN 110075104 A CN110075104 A CN 110075104A
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- China
- Prior art keywords
- kuwanon
- application
- follows
- zebra fish
- osteoporosis
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Classifications
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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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
Abstract
The invention discloses a kind of natural products to prepare the application in osteosporosis resistant medicament.The compound involved in the present invention arrived is Kuwanon H, Chinese are as follows: kuwanon H, molecular formula are as follows: C45H44O11, molecular weight are as follows: 760.82.Cell assay in vitro shows that the compound can promote the proliferation of 14 cell of MC3T3-E1Subclone, and internal animal experiment shows that it has significant therapeutic effect to the zebra fish osteoporosis of prednisone induction.
Description
Technical field
The present invention relates to a kind of natural products, are to be related to Kuwanon H to prepare osteosporosis resistant medicament more specifically
In application.
Background technique
Osteoporosis is one kind caused by many reasons with the reduction of bone tissue content, and the microstructure degeneration of bone is spy
Sign causes the brittleness of bone to increase, strength reduction and causing is prone to a kind of systemic skeletal disease fractured.With mankind society
Aging can be progressed into, the illness rate of osteoporosis increases year by year.Osteoporosis not only seriously threatens people's health,
Thus bring fracture has also brought heavy burden.
Bone remodeling is a complicated biological process, and in this course, osteoclast completes the absorption function of bone, at
Osteocyte dominates the formation function of bone, and the two generates and active coordination is that bone remodeling process maintains skeletal structure completely to close
Key.Healthy bone is in the state of bon e formation and bone resorption dynamic equilibrium, this balance once be broken can lead to osteoporosis,
A variety of bone metabolic diseases such as osteopetrosis.
More and more researches show that there are many active materials to have function of resisting osteoporosis, such as flavones in traditional Chinese medicine
Class, saponins, alkaloids, Coumarins, phenylpropionic acid compound etc., therefore finding in traditional Chinese medicine, there is anti-sclerotin to dredge
The active active principle of pine is the important channel for developing osteosporosis resistant medicament.Kuwanon H is moraceae plants contained in
A kind of flavone compound research shows that the compound has the effects that lowering blood pressure and blood fat, AntiHIV1 RT activity, but has no its anti-sclerotin
The research of loose aspect is reported.
Summary of the invention
The purpose of the present invention is: discovery Kuwanon H is preparing the application in osteosporosis resistant medicament.
The present invention is implemented as follows: Kuwanon H is preparing the application in osteosporosis resistant medicament, Chinese are as follows:
Kuwanon H, molecular formula are as follows: C45H44O11, molecular weight are as follows: and 760.82, the compound specific structure such as following formula.
For the anti-osteoporosis activity of clear Kuwanon H, inventor has carried out following experiment:
14 cell of MC3T3-E1Subclone is cultivated, which is studied to the shadow of osteoblastic proliferation using mtt assay
It rings, the results showed that, which can promote the proliferation of 14 cell of MC3T3-E1Subclone.
3dpf wild type AB strain zebra fish is randomly selected in 6 orifice plates, prednisone processing is given and establishes osteoporosis
Model.After 28 DEG C of incubators are handled 5 days, zebra fish is dyed with 0.2% calcein, takes pictures after dyeing and acquires number
According to zebra fish, first three fluorescence intensity for saving vertebrae evaluates therapeutic effect of the compound to zebra fish osteoporosis.Knot
Fruit shows that the compound can dramatically increase the bone density of zebra fish, has to the osteoporosis of prednisone induction and significantly controls
Treatment effect.
Present invention firstly discloses the compounds to the active function of osteoblast, and controls zebra fish osteoporosis
Treatment effect is studied, and illustrates that this compound can be used for preventing and treating the bone loss disease such as osteoporosis.The compound can promote
Bone precursor cells proliferation, has and reverses bone loss, improve the effect of bone density.It can be as preparing osteosporosis resistant medicament
Effective component.
Specific embodiment
The present invention is further described by the following examples, but embodiment is not delimit the scope of the invention.
The research that embodiment 1:Kuwanon H acts on osteoblast activity
MC3T3-E1Subclone l4 cell is inoculated into 96 orifice plates with the density in 5000/hole, changes drug containing afterwards for 24 hours
Culture medium, 10 μ L MTT (5mg/mL) are added in every hole after 48h, continue after being incubated for 4h, inhale and abandon each culture hole supernatant, be separately added into
150 μ L dimethyl sulfoxides vibrate 10min, measure OD value at 490nm wavelength with microplate reader, calculate proliferation rate, the results are shown in Table 1.
Influence of the 1 Kuwanon H of table to 14 cell Proliferation of MC3T3-E1Subclone
Compared with blank group, p < 0.01 * *
The result shows that each concentration group absorbance of Kuwanon H compared with blank control group, all have significant difference (p <
0.01), show that Kuwanon H has and facilitate bone cell proliferation effect.
Embodiment 2:Kuwanon H is to zebra fish osteoporosis therapy evaluation of effect
3dpf wild type AB strain zebra fish is randomly selected in 6 orifice plates, it is water-soluble to give prednisone processing to establish zebra
Fish Osteoporotic Model.Water-soluble respectively to osteoporosis model zebra fish to give 1 μM of Kuwanon H, positive control drug is according to replacing
300 μ g/mL concentration of phosphonic acids disodium, while Normal group (the normal zebra fish of fish culture water processing) and model control group are set.
After 28 DEG C of incubators are handled 5 days, zebra fish is dyed with 0.2% calcein, is taken pictures after dyeing and analyzes statistics
First three section vertebrae of zebra fish accumulates optical density, and statistical procedures result is indicated with mean ± SE.
The result shows that the zebra fish vertebrae of model control group accumulates optical density p < 0.01 compared with Normal group, mention
Representation model constructs successfully；Positive control drug disodium etidronate group zebra fish vertebrae accumulation optical density (43625 pixel) with
Model control group (14294 pixel) compares p < 0.01, and the effect of zebra fish osteoporosis therapy is 113%, prompts positive drug pair
The zebra fish osteoporosis of prednisone induction has significant therapeutic effect.The zebra fish vertebrae of Kuwanon H group is accumulated
Optical density has significant difference (p < 0.01) compared with model control group, illustrates the zebra fish that Kuwanon H induces prednisone
Osteoporosis has significant therapeutic effect.See Table 2 for details.
Therapeutic effect (n=10) of the 2 Kuwanon H of table to zebra fish osteoporosis
Compared with model control group, p < 0.01 * *
The results show that the compound can dramatically increase the bone density of zebra fish, have to the osteoporosis of prednisone induction
Have significant therapeutic effect.
In addition, inventor explain, the research of the compound of the application be inventor in the true of experimentation the study found that
The application is with another patent application submitted on the same day " Kuwanon G is preparing the application in osteosporosis resistant medicament " although seeing
Get up similar, and in experimental method use identical experimental method, but to the research of both compounds all, experiment
And the data that experiment generates all are true, rather than the false application that data are made up is carried out for patent numbers.It is all
The progress of experiment has the formalities such as contract, the documentary evidence of commission experimental unit, needs, can be provided at any time if examined.
Claims (1)
1. a kind of natural products is preparing the application in osteosporosis resistant medicament, it is characterised in that: the compound is Kuwanon
H, Chinese are as follows: kuwanon H, molecular formula are as follows: C45H44O11, molecular weight are as follows: and 760.82, specific structure such as following formula:
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201910513956.4A CN110075104A (en) | 2019-06-14 | 2019-06-14 | Kuwanon H is preparing the application in osteosporosis resistant medicament |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201910513956.4A CN110075104A (en) | 2019-06-14 | 2019-06-14 | Kuwanon H is preparing the application in osteosporosis resistant medicament |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN110075104A true CN110075104A (en) | 2019-08-02 |
Family
ID=67424269
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201910513956.4A Pending CN110075104A (en) | 2019-06-14 | 2019-06-14 | Kuwanon H is preparing the application in osteosporosis resistant medicament |
Country Status (1)
| Country | Link |
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| CN (1) | CN110075104A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113181168A (en) * | 2021-05-31 | 2021-07-30 | 西南大学 | Application of sanggenon H in preparing medicine for resisting Alzheimer's disease |
| CN114539282A (en) * | 2022-02-25 | 2022-05-27 | 南京中医药大学 | Compound with anti-osteoporosis effect and preparation method and application thereof |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105452269A (en) * | 2013-06-17 | 2016-03-30 | 尤妮金公司 | Compositions and methods for joint health |
| CN106588947A (en) * | 2016-12-07 | 2017-04-26 | 江西中医药大学 | Prenylflavonoids from jackfruit and their new use in anti-osteoporosis |
| CN107206040A (en) * | 2014-06-16 | 2017-09-26 | 尤尼根公司 | For managing or improving bone disorders, cartilage disorder or combination thing and method |
| US20180064779A1 (en) * | 2014-06-16 | 2018-03-08 | Unigen, Inc. | Compositions and Methods for Managing or Improving Bone Disorders, Joint Disorders, Cartilage Disorders, or a Combination Thereof |
-
2019
- 2019-06-14 CN CN201910513956.4A patent/CN110075104A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105452269A (en) * | 2013-06-17 | 2016-03-30 | 尤妮金公司 | Compositions and methods for joint health |
| CN107206040A (en) * | 2014-06-16 | 2017-09-26 | 尤尼根公司 | For managing or improving bone disorders, cartilage disorder or combination thing and method |
| US20180064779A1 (en) * | 2014-06-16 | 2018-03-08 | Unigen, Inc. | Compositions and Methods for Managing or Improving Bone Disorders, Joint Disorders, Cartilage Disorders, or a Combination Thereof |
| CN106588947A (en) * | 2016-12-07 | 2017-04-26 | 江西中医药大学 | Prenylflavonoids from jackfruit and their new use in anti-osteoporosis |
Non-Patent Citations (3)
| Title |
|---|
| HUIJUAN WANG等: "Sanggenon C Stimulates Osteoblastic Proliferation and Differentiation, Inhibits Osteoclastic Resorption,and Ameliorates Prednisone-Induced Osteoporosis in Zebrafish Model", 《MOLECULES》 * |
| 张静等: "桑白皮不同部位对实验性高脂糖尿病小鼠的影响", 《中药新药与临床药理》 * |
| 肖川云等: "波罗蜜根中的异戊烯基黄酮类成分", 《药学学报》 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113181168A (en) * | 2021-05-31 | 2021-07-30 | 西南大学 | Application of sanggenon H in preparing medicine for resisting Alzheimer's disease |
| CN114539282A (en) * | 2022-02-25 | 2022-05-27 | 南京中医药大学 | Compound with anti-osteoporosis effect and preparation method and application thereof |
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| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| RJ01 | Rejection of invention patent application after publication | ||
| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20190802 |