CN101889999B - Novel pharmaceutical use of kaempferol - Google Patents

Novel pharmaceutical use of kaempferol Download PDF

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Publication number
CN101889999B
CN101889999B CN2010102199740A CN201010219974A CN101889999B CN 101889999 B CN101889999 B CN 101889999B CN 2010102199740 A CN2010102199740 A CN 2010102199740A CN 201010219974 A CN201010219974 A CN 201010219974A CN 101889999 B CN101889999 B CN 101889999B
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China
Prior art keywords
kaempferol
tyrosinase
effect
arbutin
kaempferide
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Expired - Fee Related
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CN2010102199740A
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Chinese (zh)
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CN101889999A (en
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辛燕
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Individual
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Abstract

The invention relates to a kaempferide, which is characterized in that: a tyrosinase inhibitor for inhibiting melanogenesis of normal human melanocytes is a application. The tyrosinase inhibitor has the advantages that: the kaempferide has obvious effect of inhibiting the melanogenesis of the normal human melanocytes and the enzymatic activity of tyrosinase; and the inhibiting effect is better than that of the whitening preparation arbutin well-known in the world, but the influence on cell morphology and proliferation is relatively light, so the kaempferide is an inhibitor which has low cytotoxicity and application prospect and can inhibit the melanogenesis and the enzymatic activity of the tyrosinase.

Description

A kind of pharmaceutic usage of kaempferol
Technical field
The present invention relates to a kind of purposes of kaempferol, belong to field of traditional Chinese.
Background technology
Most of pigment obstacle dermatoses such as pathogeny such as chloasma, freckle and melanism still imperfectly understand; Wherein the chloasma treatment is the most difficult; And buccal, forehead, upper lip, nose and following chin etc. with face are sent out the zone for good, are mainly caused by inherited genetic factors, ultraviolet radiation, gestation, oral contraceptive or antiepileptic.Be more common in the east young and middle-aged women, its number of the infected accounts for the 0.25-4% of department of dermatologry prescription on individual diagnosis patient number in Southeast Asia, and sickness rate is 50-70% among the anemia of pregnant woman, and oral contraceptive person sickness rate is 8-29%, and the also sustainable existence of mottle after part patient childbirth or the drug withdrawal.Chromatopathys such as chloasma bring very big psychological burden because influence patient's beauty treatment to the patient, and existing medicine for removing speckle has that life cycle is grown, uncertain therapeutic efficacy is cut and defective such as zest is strong.But because its pathogenic factor is unclear fully as yet up to now, also do not have highly effective Therapeutic Method, well-known, owing to the demand of medical cosmetology, Solu-Eze more and more receives people's attention in recent years.Many depigmenting agents have been found at present; But several kinds of depigmenting agents seldom such as Arbutin, methylgenistein and Aloe resin B are only arranged to pigment cell's no cytotoxicity; Other all show cytotoxicity in various degree; And the Solu-Eze of existing no cytotoxicity exists life cycle long; Defectives such as uncertain therapeutic efficacy is cut, zest is strong are not especially received good effect when treatment chloasma etc., therefore seek the striving direction that little, the eutherapeutic depigmenting agent of toxic and side effects becomes researcher.
Method and the medicine of the treatment of most of so far pigment obstacle dermatoses are unsatisfactory, and it is long that ubiquity treatment cycle, and patient dependence is relatively poor, effect instability, curative effect defective such as often vary with each individual.And Chinese medicine accumulated rich experience, and it is low to have toxicity at aspects such as chromatopathy such as treatment chloasma, and characteristics such as determined curative effect receive people's attention just day by day.Research in China Chinese herbal medicine effect historical of long standing and well established, Chinese herbal medicine resource is extremely abundant, and kind surplus medicinal plants has 15,000 approximately, the overwhelming majority are demanded research and development urgently, wherein much are Chinese distinctive medicinal plants.In recent years; China has obtained remarkable progress at the aspects such as development and use of natural resources, and the chemical constitution study of conventional Chinese medicine has been carried out a large amount of work, has obtained important achievement; Therefrom be divided into from identifying thousands of kinds of chemical compounds; Wherein much demonstrate certain biological activity, this has important function to illustrating Effective Components of Chinese Herb and quality control thereof etc., still; The effective substance of most conventional Chinese medicines and mechanism of action thereof cause most of conventional Chinese medicine drug effects not clear as yet not by deep research.And herbal medicine efficacy shortage modern science representation language, thereby be difficult for being understood.Therefore utilize modern science and technology to set up biological activity model or target spot, the mechanism of action of utilization modern science language performance Chinese medicine, thus let the world understand Chinese medicine better.The medicine of in recent years, from plant amedica, seek low toxicity, treating pigmented dermatosis has efficiently become the focus of people's research.
Summary of the invention
The purpose of this invention is to provide that a kind of toxicity is low, synthetic to the normal human melanocytes melanocyte, tyrosinase activity has the obvious suppression effect, and effect is superior to the purposes of the melanogenic kaempferol of inhibition normal human melanocytes of arbutin.
The purposes of kaempferol of the present invention is to suppress the application of the melanogenic tyrosinase inhibitor of normal human melanocytes as preparation.
Kaempferol is called kaempferol, campherol, Rhizoma Kaempferiae flavonol and kaempferol, maoyancaosu, thesine etc. again.Kaempferol is one of active component of many plants such as Rhizoma Kaempferiae rhizome, Sophora japonica L. fruit, Herba Hyperici, Stigma Croci; Have antibiotic; Antiinflammatory and press down enzyme effect (suppressing an eye aldose reductase activity), and can improve the anti-tumor property (anti-skin carcinoma) of mice, but antiulcer and suppress the activity of hiv protease also; Kaempferol can extract at laboratory, also can directly buy from market, as: the green clear biological engineering company limited in Shaanxi (address: one tunnel No. 177 A5404 in Fengcheng City, Xi'an) just have kaempferol to sell.
Advantage of the present invention is: kaempferol is synthetic to the normal human melanocytes melanocyte, tyrosinase activity has the obvious suppression effect; And being eager to excel of the preparation arbutin of whitening that inhibitory action is generally acknowledged now in the world; But the form of pair cell and the influence of propagation are lighter; Therefore explain that kaempferol is that a kind of cytotoxicity is less, the synthetic inhibitor with tyrosinase activity of application prospect melanocyte is arranged.
The specific embodiment
We find that the mode that kaempferol relies on concentration suppresses the activity of Mushroom Tyrosinase when utilizing Mushroom Tyrosinase DOPA speed oxidizing process to measure the variable concentrations kaempferol to the activity influence of Mushroom Tyrosinase, and inhibitory action reaches the highest during with 500 μ M.Then the normal human melanocytes during we cultivate with the kaempferol intervention, observe it to the melanocyte tyrosinase activity, melanocyte is synthetic and the influence of cell proliferation, the result shows the rising along with kaempferol concentration, and the maximum inhibition of TYR is strengthened gradually; Along with the prolongation of action time, the kaempferol of same concentrations is also strengthened the active inhibitory action of TYR.Inhibition to melanin content also is to strengthen gradually, and along with the prolongation of action time, the kaempferol of same concentrations is also strengthened the inhibitory action of melanin content.Compare with another kind of skin-whitening agents arbutin, the kaempferol group effect 48 of 10,25,50,75,100 μ moL, 72h obviously strengthen than arbutin the inhibitory action of TYR, and be the most obvious with 72h.Kaempferol has inhibitory action to melanin content; Compare with arbutin; Though the arbutin group also has inhibitory action and presents dose-effect and time-effect relationship melanin content; But the arbutin group is starkly lower than the kaempferol experimental group to the inhibition strength of melanin content, and is the most obvious to the inhibitory action of melanin content at the kaempferol group effect 48h of 10,25,50,75,100 μ moL.Kaempferol has short proliferation function to MC.Effect strengthens during 1 μ moL, when 5 μ moL, the MC proliferation function is obviously suppressed, but the kaempferol of 5,10,50,100 μ moL is to increase with concentration, and is in rising trend to the rate of increase of MC, the strongest in the 48h effect.Compare with arbutin, arbutin is along with concentration increases obvious more for the rate of increase inhibitory action of MC.But along with its concentration increases and the prolongation of action time, melanocytic dendron is obvious by the multipole trend that transforms to the two poles of the earth, and cell grows fine.Cell proliferation not necessarily is directly proportional with the amount of melanocyte, and more close with the variation relation of melanocyte dendron, and the melanocytic melanocyte synthetic quantity in the two poles of the earth is than low many of multipole melanocyte; The synthetic activity with tryrosinase of melanocyte is proportionate.We think short proliferation function and the active result of its restraint of tyrosinase contradiction not of kaempferol performance, and kaempferol is in higher concentration during like 500 μ moL, and the cell growing way is still good.And arbutin cell growing way when 50 μ moL is poorer than 500 μ moL kaempferols.

Claims (1)

1. the purposes of a kaempferol is characterized in that: suppress the application of the melanogenic tyrosinase inhibitor of normal human melanocytes as preparation.
CN2010102199740A 2010-06-25 2010-06-25 Novel pharmaceutical use of kaempferol Expired - Fee Related CN101889999B (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN2010102199740A CN101889999B (en) 2010-06-25 2010-06-25 Novel pharmaceutical use of kaempferol

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Application Number Priority Date Filing Date Title
CN2010102199740A CN101889999B (en) 2010-06-25 2010-06-25 Novel pharmaceutical use of kaempferol

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CN101889999A CN101889999A (en) 2010-11-24
CN101889999B true CN101889999B (en) 2012-07-18

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CN2010102199740A Expired - Fee Related CN101889999B (en) 2010-06-25 2010-06-25 Novel pharmaceutical use of kaempferol

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Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1443056A (en) * 2000-07-19 2003-09-17 株式会社资生堂 External preparations for beautifying skin

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1443056A (en) * 2000-07-19 2003-09-17 株式会社资生堂 External preparations for beautifying skin

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
王芳.桑叶中酪氨酸酶抑制成分的研究.《浙江工商大学博士学位论文》.2009,参见第95页第2段,图4-1、4-2. *

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