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CN1148198C - Non-toxic cotton seed extractions and their extraction process, medicinal composite and use as medicine for nervous system - Google Patents

Non-toxic cotton seed extractions and their extraction process, medicinal composite and use as medicine for nervous system Download PDF

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Publication number
CN1148198C
CN1148198C CNB98106650XA CN98106650A CN1148198C CN 1148198 C CN1148198 C CN 1148198C CN B98106650X A CNB98106650X A CN B98106650XA CN 98106650 A CN98106650 A CN 98106650A CN 1148198 C CN1148198 C CN 1148198C
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China
Prior art keywords
extract
nontoxic
water
cotton seed
semen gossypii
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Expired - Fee Related
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CNB98106650XA
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Chinese (zh)
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CN1232675A (en
Inventor
赵毅民
张汉庭
杨明
罗质璞
栾新慧
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Institute of Pharmacology and Toxicology of AMMS
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Institute of Pharmacology and Toxicology of AMMS
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Priority to CNB98106650XA priority Critical patent/CN1148198C/en
Publication of CN1232675A publication Critical patent/CN1232675A/en
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Publication of CN1148198C publication Critical patent/CN1148198C/en
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Abstract

The present invention relates to non-toxic cotton seed extract, a preparation thereof, a medicine composition containing the extract, and the medicament purpose thereof.

Description

The non-toxic cotton seed extract, its extracting method contains their pharmaceutical composition and as the purposes of anxiety and/or depressed medicine
The present invention relates to the non-toxic cotton seed extract, its extracting method contains their pharmaceutical composition and as the purposes of nervous system medicine.
Non-toxic cotton is by no gossypol that Cotton Gossypii is carried out obtain after selection-breeding or the breeding or the very low Cotton Gossypii of gossypol content.Non-toxic cotton seed is the seed of the mature fruit of non-toxic cotton, and it can be used as the feedstuff of domestic animal.But up to the present, the active ingredient and the biological activity of relevant non-toxic cotton seed do not see that utmost point road is arranged.
The objective of the invention is to seek and develop the new purposes of non-toxic cotton seed.
The inventor has now found that after deliberation the non-toxic cotton seed extract that obtains by following method demonstrates good nervous system biological activity, especially anxiety, antidepressant effect, the present invention is based on above discovery and is accomplished.
According to the present invention, extract of the present invention is following obtaining: with the non-toxic cotton seed organic solvent, and water-containing organic solvent or water extraction.Used organic solvent is selected from alcohols such as methanol, ethanol, propanol or butanols etc.; Halo alkanes such as dichloromethane, chlorine side etc.; Ethers such as petroleum ether or ether etc., esters such as methyl acetate, ethyl acetate or propyl acetate etc.
According to the present invention, non-toxic cotton seed extract of the present invention has following qualitative reaction:
A) 1% istain acetone soln and 10ml acetic acid are made into developer.Cotton seed is extracted object point on filter paper, spray above-mentioned developer on this filter paper, dry up, when treating that tart flavour is not too dense, filter paper is put into 100 ℃ of baking ovens bakings 5-10 minute, then show colors such as red, Huang on the filter paper with hair-dryer.
B) preparation of developer: A liquid is dissolved in 0.5 gram ferric chloride in the 50ml water and obtains; B liquid is dissolved in the 0.5 gram potassium ferricyanide in the 50ml water and obtains, and faces the time spent, and A, B two liquid equal-volumes are mixed.Cotton seed extract sample spot on paper, is sprayed above-mentioned solution, be the obvious blue speckle immediately.
C) with exsiccant cotton seed extract sample dissolution or be suspended in the 0.5ml acetic anhydride, drip 1 concentrated sulphuric acid, solution is aubergine, and the upper strata of solution gradually becomes green.
D) with the extraction object point of cotton seed on filter paper, spray 0.05% fluorescein aqueous solution, the scraps of paper are exposed to (or in iodine vapor) speckle displaing yellow, background become pale red soon in the bromine vapor.
E) with the dissolving of cotton seed extract, be placed into 10ml in vitro, add 10% alpha-Naphthol ethanol liquid.Shake up, drip a small amount of concentrated sulphuric acid along test tube again, the purpuric garland in the interface that liquid contacts with concentrated sulphuric acid in the test tube produces.
According to the present invention, first aspect present invention relates to the non-toxic cotton seed extract, and this extract demonstrates good biological activity to the human nervous system, especially anxiety and antidepressant activity.
According to the present invention, the invention still further relates to the method for preparing the non-toxic cotton seed extract, it comprises the non-toxic cotton seed organic solvent, water-containing organic solvent or water extraction.
According to the present invention, the invention still further relates to pharmaceutical composition, it comprises non-toxic cotton seed extract of the present invention and one or more pharmaceutical carriers or excipient as active ingredient.
According to the present invention, the invention still further relates to the purposes that the non-toxic cotton seed extract is used to prepare treatment nervous system disease such as anxiety, depressed medicine.
According to the present invention, non-toxic cotton seed extract of the present invention can use separately or with pharmaceutical compositions, and its administering mode can be decided as the case may be, but preferred oral.The dosage that gives non-toxic cotton seed of the present invention is generally the 1-300mg/kg body weight/day, preferred 5-150mg/kg body weight/day.
Further specify the present invention below by embodiment and biotic experiment, but this does not mean that any limitation of the invention.
Embodiment 1
The preparation of non-toxic cotton seed ligroin extraction
Non-toxic cotton seed 5kg was pulverized 100 mesh sieves, used Petroleum ether extraction then, used 10 liters at every turn, extracted three times, merge extractive liquid,, reduction vaporization gets the 320g ligroin extraction to doing, and it has aforesaid qualitative reaction feature.
Embodiment 2
The alcoholic acid preparation of getting thing of non-toxic cotton seed
With embodiment 1 Chinese medicine slag ethanol extraction, use 15 liters at every turn, extract three times, merge extractive liquid,, be evaporated to dried, the 510g ethanol extraction, it also has aforesaid qualitative reaction feature.
Embodiment 3
The preparation of non-toxic cotton seed n-butyl alcohol and water extract
Ethanol extraction among the embodiment 2 is water-soluble, to filter, filtrate is distributed extraction between n-butyl alcohol and water, get 20g n-butanol extract and 490g water extract, and they all have aforesaid qualitative reaction feature.
The biological activity of extract of the present invention
The angst resistance effect experiment:
1. the rat safety signal is removed (safety signal withdrawol) experiment
(1) method (referring to people such as document Thiebot MH., spiritual pharmacology (Psychopharmacology), 1991,103:415-24): the experiment carry out with MED rat control box system (U.S. Med company).
Male Wistar rat, initial body weight 100-130g, body weight 170~220g when experiment finishes.The animal random packet.Branch is trained and is tested two stages.Allow rat association by fixed ratio (FR) during training 1Strengthen (FR 1, promptly every depression bar once obtains a food ball), then excessively to FR 2, FR 4And FR 8, 18 minutes every days, be divided into 5 successive time periods: 1,4 minute; 2,4 minutes; 3,3 minutes; 4,4 minutes; 5,3 minutes.Wherein, 1,3,5 is the non-punishment phase, and right lamp bright (safety signal) is pressed FR 8Strengthen, 2,4 are the punishment phase, and left lamp bright (punishment signal) is pressed FR 1When strengthening, give the foot electric shock of ratio 50% at random.Train to stablize and experimentized in 10 days.Experimental arrangement keep above-mentioned preceding 3 time periods (totally 11 minutes but close at 2 phases (promptly punishing the phase) right lamps (safety signal), still presses FR for electric shock 1Strengthen record security phase (FR 8, 7 minutes) and safety signal remove the phase (FR 1, 4 minutes) and rat obtains the number of times that the food ball is strengthened.Result's ANOVA statistical analysis, relatively Dunett ' st check between group.Antianxiety drugs is not influencing FR 8The dosage of strengthening increases FR 1Strengthen.The results are shown in Table 1.
Table 1. is removed the angst resistance effect of the Semen Gossypii water extract of embodiment 3 in the experiment at the rat safety signal
Medicine (mg/kg) n strengthens number
Safe period, safety signal was removed the phase
(FR 8) (FR 1)
Normal saline (contrast) n 47 ± 12 20 ± 10
Diazepam 1.0 38 46 ± 8 33 ± 9 *
Buspirone 1.0 16 47 ± 14 45 ± 8 *
The water extract 100.0 7 52 ± 10 24 ± 13 of embodiment 3
200.0 14 45±13 31±10 *
400.0 17 46±12 29±12 *
X ± SD, with the matched group ratio, *P<0.05, *P<0.01.
(2) discuss:
As can be seen from Table 1, antianxiety drugs diazepam and buspirone all can significantly increase the reinforcement number that safety signal is removed the phase at 1mg/kg, and to there not being influence Safe period.Embodiment 3 Semen Gossypii water extract 100~400mg/kg also has similar effect, and is certain dose relationship, shows angst resistance effect.
2. rat Vogel (conflict experiment)
(1) method: experiment is considered instrument, list of references: Zhang Hanting etc., Chinese J Pharmacol Toxicol, 1995 with the Model-102 formed coke that U.S. Lafayette company produces; 9 (4): 254-7.Male Wistar rat, initial weight 180~220g, prohibit water after 48 hours body weight be 155~200g.The rat random packet is prohibited water and train it to lick water after 24 hours, does not add electric shock, licks water in 3 minutes and is no less than 300 times continuation and prohibits water and experimentize after 48 hours, and the vola gives the electric shock (whenever lick water give for 20 times 1 time shock by electricity) of 0.3mA simultaneously.Instrument record was automatically licked the waterside number in 3 minutes.Anti-burnt brave medicine increases this index.Statistical analysis is the same.The results are shown in Table 2.
The angst resistance effect of table 2. embodiment 3 water extracts on rat Vogel conflict model
Medicine (mg/kg) n licks the waterside number
Normal saline (contrast) 9 216 ± 151
Diazepam 3.0 8 467 ± 142 *
Embodiment 3 water extracts 100.0 7 356 ± 120
200.0 9 379±116
400.0 8 431±140 *
X ± SD. and matched group ratio, *P<0.05.
(2) discuss
As seen from Table 2, diazepam 3mg/kg can obviously increase the rat conflict phase and lick the waterside number, but embodiment 3 water extracts 100~400mg/kg also increase the conflict phase and lick the waterside number in dose dependent ground, be angst resistance effect.

Claims (5)

1. be used for the treatment of anxiety and/or depressed nontoxic Semen Gossypii extract, wherein nontoxic Semen Gossypii is from the seed of non-toxic cotton mature fruit, non-toxic cotton is that described extract is following to be obtained by no gossypol that Cotton Gossypii is carried out obtain after selection-breeding or the breeding or the very low Cotton Gossypii of gossypol content:
A) nontoxic Semen Gossypii Petroleum ether extraction, or
B) with remaining medicinal residues ethanol extraction after a) PetroChina Company Limited.'s ether extracts, or
C) with b) in ethanol extraction in water and n-butyl alcohol, distribute, obtain the extract of water and n-butyl alcohol respectively.
2. prepare the method for nontoxic Semen Gossypii extract, it comprises:
A) nontoxic Semen Gossypii Petroleum ether extraction, or
B) with remaining medicinal residues ethanol extraction after a) PetroChina Company Limited.'s ether extracts, or
C) with b) in ethanol extraction in water and n-butyl alcohol, distribute, obtain the extract of water and n-butyl alcohol respectively.
3. be used for the treatment of anxiety and/or depressed pharmaceutical composition, it comprises nontoxic Semen Gossypii extract and one or more pharmaceutical carriers or excipient as claim 1 requirement of active ingredient.
4. nontoxic Semen Gossypii extract is used for preparing treatment anxiety and/or depressed medicine purposes.
5. the purposes of claim 4, wherein said nontoxic Semen Gossypii extract is the nontoxic Semen Gossypii extract in the claim 1.
CNB98106650XA 1998-04-17 1998-04-17 Non-toxic cotton seed extractions and their extraction process, medicinal composite and use as medicine for nervous system Expired - Fee Related CN1148198C (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CNB98106650XA CN1148198C (en) 1998-04-17 1998-04-17 Non-toxic cotton seed extractions and their extraction process, medicinal composite and use as medicine for nervous system

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Application Number Priority Date Filing Date Title
CNB98106650XA CN1148198C (en) 1998-04-17 1998-04-17 Non-toxic cotton seed extractions and their extraction process, medicinal composite and use as medicine for nervous system

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CN1148198C true CN1148198C (en) 2004-05-05

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WO2002076473A1 (en) * 2001-03-26 2002-10-03 Academy Of Military Medical Sciences Institute Of Pharmacology And Toxicology Quercetin derivative and its medicinal use

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