CN110368379A - Kuwanon G is preparing the application in osteosporosis resistant medicament - Google Patents

Kuwanon G is preparing the application in osteosporosis resistant medicament Download PDF

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Publication number
CN110368379A
CN110368379A CN201910513945.6A CN201910513945A CN110368379A CN 110368379 A CN110368379 A CN 110368379A CN 201910513945 A CN201910513945 A CN 201910513945A CN 110368379 A CN110368379 A CN 110368379A
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CN
China
Prior art keywords
kuwanon
follows
zebra fish
osteoporosis
application
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Pending
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CN201910513945.6A
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Chinese (zh)
Inventor
王慧娟
彭礼军
陈琳
田民义
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Guizhou University
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Guizhou University
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Priority to CN201910513945.6A priority Critical patent/CN110368379A/en
Publication of CN110368379A publication Critical patent/CN110368379A/en
Pending legal-status Critical Current

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35Heterocyclic 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
    • A61K31/352Heterocyclic 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 
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs 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 G, Chinese are as follows: phellinus ketone G, molecular formula are as follows: C40H36O11, molecular weight are as follows: 692.71.Cell assay in vitro shows that the compound can promote the proliferation of 14 cell of MC3T3-E1 Subclone, and internal animal experiment shows that it has significant therapeutic effect to the zebra fish osteoporosis of prednisone induction.

Description

Kuwanon G is preparing the application in osteosporosis resistant medicament
Technical field
The present invention relates to a kind of pharmaceutical technology, especially Kuwanon G to prepare answering in osteosporosis resistant medicament With.
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 G is moraceae plants contained in A kind of flavone compound, research shows that the compound have the effects that slow down atherosclerosis, it is anti-inflammatory, relieving asthma, antibacterial, but Have no the research report in terms of its anti-osteoporosis.
Summary of the invention
The purpose of the present invention is: discovery Kuwanon G is preparing the application in osteosporosis resistant medicament.
The present invention is implemented as follows: Kuwanon G is preparing the application in osteosporosis resistant medicament, Chinese are as follows: Phellinus ketone G, molecular formula are as follows: C40H36O11, molecular weight are as follows: and 692.71, the compound specific structure such as following formula.
For the anti-osteoporosis activity of clear Kuwanon G, 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 G 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 table 1Kuwanon G to 14 cell Proliferation of MC3T3-E1Subclone
Compared with blank group, p < 0.01 * *
The result shows that 0.1,1 and 10 μm of ol/L Kuwanon G group absorbance compared with blank control group, all has significantly Sex differernce (p < 0.01) shows that Kuwanon G can promote the proliferation of osteoblast.
Embodiment 2:Kuwanon G 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 G, 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 G group is accumulated Optical density has significant difference (p < 0.01) compared with model control group, illustrates the zebra fish that Kuwanon G induces prednisone Osteoporosis has significant therapeutic effect.See Table 2 for details.
Therapeutic effect (n=10) of the table 2Kuwanon G to zebra fish osteoporosis
Compared with model control group, p < 0.01 * *
Cell assay in vitro shows that the compound can promote the proliferation of 14 cell of MC3T3-E1Subclone, internal animal Experiments have shown that it has significant therapeutic effect to the zebra fish osteoporosis of prednisone induction.

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 G, Chinese are as follows: phellinus ketone G, molecular formula are as follows: C40H36O11, molecular weight are as follows: and 692.71, specific structure such as following formula:
CN201910513945.6A 2019-06-14 2019-06-14 Kuwanon G is preparing the application in osteosporosis resistant medicament Pending CN110368379A (en)

Priority Applications (1)

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CN201910513945.6A CN110368379A (en) 2019-06-14 2019-06-14 Kuwanon G is preparing the application in osteosporosis resistant medicament

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Application Number Priority Date Filing Date Title
CN201910513945.6A CN110368379A (en) 2019-06-14 2019-06-14 Kuwanon G is preparing the application in osteosporosis resistant medicament

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CN110368379A true CN110368379A (en) 2019-10-25

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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112602711A (en) * 2020-12-15 2021-04-06 吉林大学 Application of natural compound mulberry flavone in inhibiting fruit and vegetable fungi
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
CN117016449A (en) * 2023-09-26 2023-11-10 南京中医药大学 Construction method of zebra fish bone mass loosening model

Citations (3)

* Cited by examiner, † Cited by third party
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

Patent Citations (3)

* Cited by examiner, † Cited by third party
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
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 (4)

* Cited by examiner, † Cited by third party
Title
BING LIN等: "Rapid, microwave-accelerated synthesis and anti-osteoporosis activities evaluation of Morusin scaffolds and Morusignin L scaffolds", 《BIOORGANIC & MEDICINAL CHEMISTRY LETTERS》 *
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 (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112602711A (en) * 2020-12-15 2021-04-06 吉林大学 Application of natural compound mulberry flavone in inhibiting fruit and vegetable fungi
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
CN117016449A (en) * 2023-09-26 2023-11-10 南京中医药大学 Construction method of zebra fish bone mass loosening model

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