CN102824341A - Application of gallocatechin in preparation of drugs for resisting benign prostatic hyperplasia - Google Patents
Application of gallocatechin in preparation of drugs for resisting benign prostatic hyperplasia Download PDFInfo
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- CN102824341A CN102824341A CN 201110161658 CN201110161658A CN102824341A CN 102824341 A CN102824341 A CN 102824341A CN 201110161658 CN201110161658 CN 201110161658 CN 201110161658 A CN201110161658 A CN 201110161658A CN 102824341 A CN102824341 A CN 102824341A
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- prostate
- prostatic hyperplasia
- gallocatechin
- benign prostatic
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Abstract
The invention discloses an application of gallocatechin in the preparation of drugs for resisting benign prostatic hyperplasia. According to the invention, through a prostatic hyperplasia model in ovariectomized rats induced by testosterone propionate, gallocatechin is selected as a therapeutic drug so as to observe the influence on rat prostate weight and index and pathological changes of prostate tissues. Research results show that gallocatechin can significantly reduce the prostate weight and prostate index of the animal model and improve pathological symptoms of prostate tissues.
Description
Technical field
The invention belongs to pharmaceutical field, relate to the new medical usage of nutgall catechin, be specifically related to the application of nutgall catechin in the anti-benign prostatic hyperplasia medicine of preparation.
Background technology
Benign prostatic hyperplasia
[1](benign prostatic hyperplasia is the common physiology pathological changes of elderly men BPH), and sickness rate is the trend of obvious rising in recent years.According to statistics, sickness rate that should disease among the male more than 60 years old reaches more than 70%, has a strong impact on gerontal patient's healthy and quality of life.The medicine that is used to treat BPH clinically mainly contains
[2]: α 1-adrenoreceptor antagonist, 5 inhibitor and natural product preparation etc.Because the untoward reaction of natural product preparation is few, be fit to life-time service, caused people's extensive concern in recent years.
((-)-Gallocatechin, GC) structural formula is as follows, molecular formula: C for nutgall catechin
15H
14O
7, the U.S. chemical abstract number of including (CASNo.): 3371-27-5; Be a kind of of green tea catechins, have the antioxidation isoreactivity
[3]But do not see that monomeric compound GC is used to prepare the report of anti-benign prostatic hyperplasia medicine.
Below be the molecular structural formula of GC:
List of references:
[1]Untergasser?G.，Madersbacher?S.，Berger?P..Benign?prostatic?hyperplasia：age-related tissue-remodeling[J].Experimental?Gerontology，2005，40(3)：121-128
[2] Weiqiang, Li Tao. the Drug therapy of benign prostatic hyperplasia. Chinese geriatrics magazine [J] .2006,25 (7): 557-559
[3]Plumb?G.W.，De?Pascual-Teresa?S.，Santos-Buelga?C.，et?al.Antioxidant?properties?of?gallocatechin?and?prodelphinidins?from?pomegranate?peel[J].Redox?Report，2002，7(1)：41-46.
[4] Wen Yaolin, Li Kun. a kind of preparation side of non-phenotype catechin monomers [P], and Chinese patent: 201010022636.8,2010-01-11
Summary of the invention
Technical problem to be solved by this invention is to seek a kind of safe, reliable, can effectively reduce BPH patient's weight of prostate and prostate index, improves the pathological change of prostata tissue.Thereby can effectively prevent and treat the product of benign prostatic hyperplasia.The present invention is directed to above-mentioned technical problem the application of a kind of nutgall catechin in the anti-benign prostatic hyperplasia medicine of preparation is provided.
The object of the invention can be realized through following technical scheme:
The application of nutgall catechin in the anti-benign prostatic hyperplasia medicine of preparation.
Above-mentioned application, nutgall catechin is used to prepare anti-benign prostatic hyperplasia drugs with function as active ingredient, can combine separately or with the pharmacy acceptable assistant, processes pharmaceutically acceptable any one dosage form according to conventional method.Described dosage form is preferably oral liquid, capsule, granule, injection, tablet or liposome.
The inventor adopts the inductive castrated rats prostatic hyperplasia model of Testosterone Propionate; Numerous candidate compounds are screened; Find that nutgall catechin (GC) can significantly reduce weight of prostate and the prostate index of animal pattern; Improve prostata tissue pathology symptom, demonstrate good prospects for application.
The nutgall catechin that the present invention relates to (GC) can be bought acquisition on market, as purity 98% nutgall catechin of U.S. sigma company ((-)-Gallocatechin, GC) etc.Also can prepare voluntarily, its preparation method is open in 201010022636.8 the Chinese patent at application number
[4]
The nutgall catechin that the present invention relates to (GC) is used for the medicine of preparation control benign prostatic hyperplasia (BPH), can be made into dosage forms such as oral liquid, capsule, granule, injection, tablet, liposome.
Description of drawings
Fig. 1 is each group rat prostate siphonal lobe tissue pathological slice result (HE, * 100).
A, normal wherein; B, model; C, GC low dose group; D, GC high dose group; E, finasteride.
The specific embodiment
Following embodiment can make those skilled in the art more fully understand the present invention, but does not limit the present invention in any way.
Embodiment 1 nutgall catechin is to the influence of rat prostate
1, laboratory animal
Male and healthy SD (Sprague-Dawley) rat, the cleaning level, body weight 250 ± 20g, available from west, Shanghai pul-Bi Kai laboratory animal company limited, quality certification numbering: 00800160568, production licence number: SCXK (Shanghai) 2008-0016.
2, modeling, grouping and administration
35 of above-mentioned rats, common one week of raising is to conform.After common observation is no abnormal, to get 7 at random and make the normal control group, all the other 28 are carried out modeling.With behind the etherization, under the aseptic condition, routine disinfection skin is extractd bilateral testes through scrotum earlier, the ligation of stump place, and to guarantee hemostasis, skin suture drips a certain amount of ofloxacin injection, to protect from infection.Intramuscular injection (im) penicillin 400,000 u/, for three days on end.
Perform the operation and castrated rats is divided into model group, nutgall catechin (GC) low dose group, nutgall catechin (GC) high dose group, positive drug finasteride group, 7 every group at random after 1 week.From castration the 8th day, every rat skin lower injection (sc) was dissolved in the Testosterone Propionate 4mg/kgd in the olive oil, normal group sc olive oil, continuous 30 days.The while gastric infusion.Each test sample and contrast medicine group add 5%CMC-Na as suspensoid with the distillation water as solvent, are configured to certain density suspension.From castration the 8th day, give certain density sample respectively by the 1mL/100g body weight, normal group and model group are given the distilled water of equal volume, every day 1 time, continuous 30 days.
3, draw materials and weigh
Administration 30 days, behind last administration 24h, after every group of rat weighed, anaesthetizes, disconnected neck was put to death rat, takes out each leaf texture of prostate (siphonal lobe and dorsal part leaf) rapidly, absorbs surface liquid with filter paper, peels off fatty tissue, and electronic balance is claimed its weight in wet base.Calculate rat prostate and each leaf index.
4, the prostata tissue pathology detect
The rat prostate pathological study adopts conventional haematoxylin-Yihong (HE) dyeing, and light microscopic is observed prostata tissue morphology and structural change down, comprises lumen of gland, epithelial cell and interstitial edema, hyperemia and cell infiltration situation.The concrete operations step is following:
(1) draws materials with fixing: after above-mentioned rat prostate tissue is weighed, get half fixation of tissue of siphonal lobe in 10% neutral formalin solution.
(2) dehydration, transparent, waxdip: adopt the automatic dehydration machine, program is set to: AF liquid 90min → 85% ethanol 90min → 95% ethanol I 90min → 95% ethanol II 90min → dehydrated alcohol I 90min → dehydrated alcohol II 90min → xylene I 30min → xylene II 30min → paraffin I 90min → paraffin II 90min → paraffin III 90min.
(3) FFPE.
(4) section and paster: the wax stone that embedding is good is fixed on the microtome, serial section, and thick 4 μ m plate in 50 ℃ of water, are attached on the microscope slide again.
(5) roasting sheet: 60 ℃ of roasting sheet 30min.
(6) HE dyeing: process is following, and xylene I 5min → xylene II 5min → dehydrated alcohol 2min → 95% ethanol 2min → 80% ethanol 2min → flowing water flushing 2min → distilled water 1min → haematoxylin dyeing 6min → flowing water is towards the 3min → hydrochloride alcohol differentiation 2s → anti-blue 5s of flowing water flushing 2min → ammonia → washing 1min → Yihong 10s → distilled water 1s → 80% ethanol 2s → 95% ethanol 2s → dehydrated alcohol 2s (2 times) → xylene 2s
(7) neutral gum mounting
Prostata tissue is learned and is changed sick judgment criteria: normally be "-" that extent of disease accounts for the full visual field and is "+" below 1/4; Pathological changes changes obviously, and scope accounts for about 1/3 and is " ++ "; Pathological changes is serious, and scope accounts for the full visual field about 1/2 and is " +++".
5, statistical procedures
All results all adopt the SPSS11.5 statistical software to handle; Weight of prostate and index measurement data are all represented with MEAN ± S.E.M; Group difference adopts one factor analysis of variance (F check), and variance has homogeneous, more then adopts the LSD check in twos; With P＜0.05 is the significant difference standard, and P＜0.01 is the significant differences standard.Histo pathological change is ranked data; Therefore statistical analysis adopts rank test; All groups relatively adopt Kruskal-Wallis H check, and other groups adopt Mann-Whitney U check with the model group multiple comparisons, with the Bonferroni method inspection level are proofreaied and correct; Inspection level after the correction is 0.004, and promptly P＜0.004 has been regarded as statistical significance.
6, result of the test
6.1 influence to each leaf weight of rat prostate
Each processed group of table 1 is to the influence of each leaf weight of castrated rats prostate (MEAN ± S.E.M)
Annotate: compare with model group:
*P＜0.05,
*P＜0.01
6.2 to the exponential influence of each leaf of rat prostate
Each processed group of table 2 is to the exponential influence of each leaf of castrated rats prostate (MEAN ± S.E.M)
Annotate: compare with model group:
*P＜0.05,
*P＜0.01
6.3, to the histopathologic influence of rat prostate
Each processed group of table 3 causes the influence of BPH rat prostate siphonal lobe pathological change to Testosterone Propionate
Annotate: compare with model group, P＜0.004 has been regarded as statistical significance
Be each group rat prostate siphonal lobe tissue pathological slice result (HE, * 100) like Fig. 1.Wherein, A is normal; B is a model; C is the GC low dose group; D is the GC high dose group; E is a finasteride.
6.4 the result sums up
Result of the test shows that nutgall catechin (GC) has the inductive castrated rats human prostate prostate of remarkable reduction Testosterone Propionate weight, prostate index, improves rat model prostate pathology and changes, compare with model group, difference have significance (
*P＜0.05) and highly significant property (
*P＜0.01); Approaching with the positive drug finasteride, have a good application prospect.
The preparation of embodiment 2 nutgall catechin gallic acid ester liposomees
Is that the ratio of 3g: 1g: 0.1g is dissolved in dehydrated alcohol and chloroform (volume ratio of dehydrated alcohol and chloroform is 1: 1 with lecithin and cholesterol and nutgall catechin in quality; Cumulative volume is 15ml) mixed solution in and add vitamin E 2mg and obtain solution A; With an amount of folic acid 33mg be dissolved in the 330 μ l dimethyl sulfoxines solution B; Solution A, B are mixed and add the 9g lactose get mixture C, this solution C is obtained immobilized artificial membrane except that desolvating; The gained immobilized artificial membrane is water-soluble, after aquation, obtain liposome, with this liposome through 0.2 μ m membrane filtration, with liposome solutions in high pressure homogenizer under pressure 200-400Mpa supercharging homogenizing 2h step by step, the liposome that obtains is the solution of clear and bright homogeneous.The liposome solutions lyophilization that obtains except that desolvating, is obtained freeze dried nutgall catechin liposome.Freeze dried nutgall catechin liposome powder is added distilled water jolting dissolving, and measure particle diameter with Ls-230 type laser light scattering particle size analyzer (U.S. Beckman Coulter company).The particle diameter of liposome is respectively 92.4nm ± 4.8nm (n=3).With sem observation gained liposome.Under ultramicroscope, observing liposome is ball, and result big or small and with particle size analyzer determination matches.Using ultrafiltration to measure liposome encapsulation is 92.8%, and the 48h percolation ratio is 0.8%.
The preparation of embodiment 3 nutgall catechin capsules
Prescription: nutgall catechin 500g, starch 15g, magnesium stearate 5g (about 0.5%) processes 1000.
Prepare: after nutgall catechin gallic acid ester, starch, magnesium stearate were crossed 80 mesh sieves, mix homogeneously in the capsulae vacuus of packing into, promptly got.
The preparation of embodiment 4 nutgall catechin tablets
Prescription: nutgall catechin 500g, starch 40g, 10% starch slurry 24g, dried starch 23g (about 4%), magnesium stearate 3g (about 0.5%) processes 1000.
Preparation: nutgall catechin gallic acid ester is crossed 80 mesh sieves, with the starch mixing, add starch slurry and process soft material, after granulating with 14 mesh sieves, put 70～80 ℃ of dry backs in 12 mesh sieve granulate, behind adding dried starch and the magnesium stearate mixing, tabletting promptly gets.
Claims (4)
1. the application of nutgall catechin in preparation control benign prostatic hyperplasia medicine.
2. application according to claim 1; It is characterized in that: nutgall catechin is used to prepare the medicine of anti-benign prostatic hyperplasia as active ingredient; Can combine separately or with the pharmacy acceptable assistant, process pharmaceutically acceptable any one dosage form according to conventional method.
3. application according to claim 2 is characterized in that described pharmaceutical dosage form is: oral liquid, capsule, granule, injection, tablet or liposome.
4. application according to claim 3 is characterized in that described pharmaceutical dosage form is: capsule, tablet or liposome.
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| CN 201110161658 CN102824341A (en) | 2011-06-16 | 2011-06-16 | Application of gallocatechin in preparation of drugs for resisting benign prostatic hyperplasia |
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| CN 201110161658 CN102824341A (en) | 2011-06-16 | 2011-06-16 | Application of gallocatechin in preparation of drugs for resisting benign prostatic hyperplasia |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112425568A (en) * | 2020-12-11 | 2021-03-02 | 上海市计划生育科学研究所 | Method for establishing benign prostatic hyperplasia BPH dog model with EMT characteristics |
| CN112891350A (en) * | 2021-04-02 | 2021-06-04 | 宁夏医科大学 | Application of trigonelline in preparing medicine for preventing or treating prostatic hyperplasia |
-
2011
- 2011-06-16 CN CN 201110161658 patent/CN102824341A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112425568A (en) * | 2020-12-11 | 2021-03-02 | 上海市计划生育科学研究所 | Method for establishing benign prostatic hyperplasia BPH dog model with EMT characteristics |
| CN112891350A (en) * | 2021-04-02 | 2021-06-04 | 宁夏医科大学 | Application of trigonelline in preparing medicine for preventing or treating prostatic hyperplasia |
| CN112891350B (en) * | 2021-04-02 | 2022-09-27 | 宁夏医科大学 | Application of trigonelline in preparing medicine for preventing or treating prostatic hyperplasia |
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Application publication date: 20121219 |