CN102058613A - New application of antineoplastic constituent compound in solanum nigrum - Google Patents

New application of antineoplastic constituent compound in solanum nigrum Download PDF

Info

Publication number
CN102058613A
CN102058613A CN2011100053503A CN201110005350A CN102058613A CN 102058613 A CN102058613 A CN 102058613A CN 2011100053503 A CN2011100053503 A CN 2011100053503A CN 201110005350 A CN201110005350 A CN 201110005350A CN 102058613 A CN102058613 A CN 102058613A
Authority
CN
China
Prior art keywords
solamargine
solasonine
group
weight ratio
injection
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
CN2011100053503A
Other languages
Chinese (zh)
Other versions
CN102058613B (en
Inventor
陈荣
冯林
李海岛
周娟
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Hainan Simcere Pharmaceutical Co ltd
Original Assignee
Jiangsu Simcere Pharmaceutical R&D Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Jiangsu Simcere Pharmaceutical R&D Co Ltd filed Critical Jiangsu Simcere Pharmaceutical R&D Co Ltd
Priority to CN201110005350.3A priority Critical patent/CN102058613B/en
Publication of CN102058613A publication Critical patent/CN102058613A/en
Application granted granted Critical
Publication of CN102058613B publication Critical patent/CN102058613B/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Landscapes

  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The invention relates to the application of ratio compounds of two simplex components in plant solanum nigrum extracts to preparing medicaments for treating liver cancer.

Description

The new purposes of anti-tumor active ingredient compositions in the Herba Solani Nigri
Technical field
The present invention relates to the application of ratio compositions in preparation treatment liver-cancer medicine of two monomer components in the plant black nightshade extract, described monomer component is respectively solamargine and solasonine.
Background technology
Herba Solani Nigri Solalum Nigrum L. is annual Solanum herbaceous plant, and all there is growth most of at home provinces and regions.The herb hyoscine, cold in nature, bitter in the mouth is hot little sweet, slightly poisonous, returns lung, urinary bladder channel.Can dissipating blood stasis for subsidence of swelling, heat-clearing and toxic substances removing has the effect of anticancer, and treatment pain commonly used is swollen, tumor etc.Herba Solani Nigri also has certain dietary function in addition, therefore has good medical value.Be rich in steroid alkaloid in the plant, these steroid alkaloids all are present in Solanum nigrum stem, leaf, root, really with the form of glycosides, and aglycon is solasodine (solasodine).
Solasonine (solasonine, CAS 19121-58-5) and solamargine (solamargine, CAS 20311-51-7) is two main in Herba Solani Nigri alkaloid components, in in vitro tests, two chemical compounds all show the destructiveness of cell membrane fat, both show cooperative effect, the destructiveness of solamargine is stronger, rhamnose wherein may play important function in the combining of guiding glycoalkaloid and cell, some studies show that solamargine, thereby solamargine can be regulated the expression of Tumor Necrosis Factor Receptors and cause cancer cell-apoptosis, and 2 rhamnose may play a decisive role in triggering natural death of cerebral cells.
Figure BDA0000043537980000011
Solasonine (solasonine)
Figure BDA0000043537980000021
Solamargine (solamargine)
WO2004002497 discloses solasonine (solasonine) and the experiment in vitro result of solamargine (solamargine) compositions in A2058 (human melanoma cell), NO36, LS174T (human colon cancer cell), LNCaP (Human Prostate Cancer Cells), 786-O tumor cell lines such as (people's kidney clear cell adenocarcinoma cells) and NHDF-Ad (normal adult skin flbroblast), NHRE.The application in the treatment liver-cancer medicine of unexposed solasonine of this application (solasonine) and solamargine (solamargine) compositions, the prompting of also not being correlated with.
Summary of the invention
The present invention relates to the application of ratio compositions in preparation treatment liver-cancer medicine of two monomer components in the plant black nightshade extract, described monomer component is respectively solamargine and solasonine.
The weight ratio of solamargine and solasonine is 1: 1-10: 1, and preferred weight ratio is 2: 1~10: 1, preferred weight ratio is 4: 1~10: 1.The weight ratio of further preferred solamargine and solasonine is 6.5: 1~7.5: 1, and weight ratio is further more preferably from 6.5: 1 or 7: 1 or 7.5: 1.
Can also contain solvent in the above-mentioned pharmaceutical composition, can be so that solasonine and solamargine mix better.Described solvent can be selected the mixture of water, water-miscible organic solvent or water-miscible organic solvent and water for use.Water-miscible organic solvent commonly used mainly contains alcohols solvent, ether solvent, ketones solvent etc.The mixture of solvent preferred water, water-miscible organic solvent and water among the present invention.Be more preferably the glacial acetic acid aqueous solution of low concentration.
Beneficial effect of the present invention has been to provide a kind of solamargine and the application of solasonine compositions in preparation treatment liver-cancer medicine.The solamargine of preferred proportion and solasonine compositions table reveal lower toxicity among the present invention, and can effectively reduce relative tumor proliferation rate with respect to blank group, single medicine group.
The specific embodiment
The invention will be further described in the mode of embodiment below, provides implementation detail of the present invention, but be not to be intended to limit protection scope of the present invention.
The preparation of embodiment 1 injection
Solasonine injection: get solasonine 140mg, add slowly that 1.5% glacial acetic acid solution makes it dissolving and to 100mL, promptly.
Solamargine injection: get solamargine 140mg, add slowly that 1.5% glacial acetic acid solution makes it dissolving and to 100mL, promptly.
Composite injection A (weight ratio 4: 1): get solamargine 112mg and solasonine 28mg, add slowly that 1.5% glacial acetic acid solution makes it dissolving and to 100mL, promptly.
Composite injection B (weight ratio 7: 1): get solamargine 122.5mg and solasonine 17.5mg, add slowly that 1.5% glacial acetic acid solution makes it dissolving and to 100mL, promptly.
Composite injection C (weight ratio 4: 1): get solamargine 56mg and solasonine 14mg, add slowly that 1.5% glacial acetic acid solution makes it dissolving and to 100mL, promptly.
Composite injection D (weight ratio 7: 1): get solamargine 60.9mg and solasonine 8.7mg, add slowly that 1.5% glacial acetic acid solution makes it dissolving and to 100mL, promptly.
Composite injection E (weight ratio 4: 1): get solamargine 168mg and solasonine 42mg, add slowly that 1.5% glacial acetic acid solution makes it dissolving and to 100mL, promptly.
Composite injection F (weight ratio 7: 1): get solamargine 184.1mg and solasonine 26.3mg, add slowly that 1.5% glacial acetic acid solution makes it dissolving and to 100mL, promptly.
Embodiment 2 sets up HepG2 transplanted tumor in nude mice model
Recovery and amplification HepG2 cell; To be amplified to enough cells, collecting cell, to be made into concentration be 2 * 10 with not containing 1640 of serum 7The cell suspension of cell/ml.
Select 60 of BALB/c-nude nude mouses (SPF level, 5-6 age in week, male); The right side subcutaneous vaccination of nude mice back, 0.1ml/, promptly every nude inoculation cell number is 2 * 10 6Observe out tumor situation and tumor size after the inoculation.
The contrast of embodiment 3 effects
3.1 grouping: treat that tumor grows to volume 150mm 3During the left and right sides, select from 60 nude mices that 36 gross tumor volumes are close, shape nude mice preferably, be divided into 6 groups, 6 every group.
Group 1: matched group, give 1.5% glacial acetic acid solution, per 10 gram body weight lumbar injection 0.1ml, every administration then stops administration four days, totally 3 weeks after three days.
Group 2: give positive drug--cisplatin injection (concentration 0.6mg/ml), per 10 gram body weight lumbar injection 0.1ml, 1 time weekly, totally 3 weeks.
Group 3~group 6 gives the part injection of configuration among the embodiment 1, per 10 gram body weight lumbar injection 0.1ml, and every administration then stops administration four days, totally 3 weeks after three days.Wherein organize 3 and give the solasonine injection; Group 4 gives the solamargine injection; Group 5 gives composite injection A, and group 6 gives composite injection B.
3.2 administration: grouping back administration on the same day, be made as Day1, administering mode is the same.
3.3 measure: measure gross tumor volume weekly 3 times, Day21 puts to death nude mice, calculates relative tumor proliferation rate.
3.4 detect index and computational methods
(tumor volume, TV), computing formula is gross tumor volume
Figure BDA0000043537980000041
L wherein 1, l 2Represent length and width respectively.
(relative tumor volume, RTV), computing formula is relative tumour volume TV wherein 1(Day1) gross tumor volume during for minute cage administration, TV tGross tumor volume when measuring each time.
Relative tumor proliferation rate T/C (%), computing formula is Wherein RTC (T) is treatment group RTV; RTC (C) is blank group RTV.
Drug effect result to people's hepatocarcinoma HepG2 Nude Mice
Figure BDA0000043537980000044
*: P<0.05 * *: P<0.01, compare with the blank group
Experimental result shows composite injection A group dead 2 nude mices altogether, animal dead does not appear in composite injection B group, but weight loss 16.9%, from mortality rate and weight loss rate, in this experiment under this dosage composite injection A group toxicity stronger, composite injection B group toxicity relatively a little less than.
From relative tumor proliferation rate drug effect, composite injection A group all shows certain tumor killing effect with composite injection B group, but both drug effect no difference of science of statistics.
In this experiment, consider from relative tumor proliferation rate, mortality rate, weight loss percentage ratio three aspects that each group of monomer and mixture compares, composite injection B group shows preferably tumor proliferation rate and more weak toxicity relatively.According to drug research technological guidance principle, antitumor drug therapeutic evaluation standard T/C%≤60%, and process statistical procedures p<0.05 is effective.Under 14mg/kg dosage, monomer and mixture drug effect toxicity compare, and composite injection B group has certain tumor killing effect to HepG2 people's cancer bare mouse different species transplanted tumor, also shows more weak toxicity.

Claims (7)

1. solamargine and the solasonine compositions application in preparation treatment liver-cancer medicine.
2. according to the application described in the claim 1, the weight ratio that it is characterized in that solamargine and solasonine is 1:1~10:1.
3. according to the application described in the claim 1, the weight ratio that it is characterized in that solamargine and solasonine is 2:1~10:1.
4. according to the application described in the claim 1, the weight ratio that it is characterized in that solamargine and solasonine is 4:1~10:1.
5. according to the application described in the claim 1, the weight ratio that it is characterized in that solamargine and solasonine is 6.5:1~7.5:1.
6. according to the application described in the claim 1, the weight ratio that it is characterized in that solamargine and solasonine is 6.5:1 or 7:1 or 7.5:1.
7. according to each described application among the claim 1-6, it is characterized in that described compositions can also comprise other pharmaceutically acceptable inactive ingredients.
CN201110005350.3A 2011-01-12 2011-01-12 The purposes of anti-tumor active ingredient compositions in Herba Solani Nigri Active CN102058613B (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201110005350.3A CN102058613B (en) 2011-01-12 2011-01-12 The purposes of anti-tumor active ingredient compositions in Herba Solani Nigri

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN201110005350.3A CN102058613B (en) 2011-01-12 2011-01-12 The purposes of anti-tumor active ingredient compositions in Herba Solani Nigri

Publications (2)

Publication Number Publication Date
CN102058613A true CN102058613A (en) 2011-05-18
CN102058613B CN102058613B (en) 2015-12-16

Family

ID=43994239

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201110005350.3A Active CN102058613B (en) 2011-01-12 2011-01-12 The purposes of anti-tumor active ingredient compositions in Herba Solani Nigri

Country Status (1)

Country Link
CN (1) CN102058613B (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112957364A (en) * 2021-03-29 2021-06-15 杭州立效生物医药科技有限公司 Medicine for treating renal tubular injury and application thereof

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040247715A1 (en) * 2003-06-05 2004-12-09 G & E Herbal Biotechnology Co., Ltd. Water soluble extract from plant of solanum genus and the preparation process thereof, and pharmaceutical composition containing the water soluble extract

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040247715A1 (en) * 2003-06-05 2004-12-09 G & E Herbal Biotechnology Co., Ltd. Water soluble extract from plant of solanum genus and the preparation process thereof, and pharmaceutical composition containing the water soluble extract

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
KAP-RANG LEE, ET AL.: "Glycoalkaloids and Metabolites Inhibit the Growth of Human Colon (HT29) and Liver (HepG2) Cancer Cells", 《J. AGRIC. FOOD CHEM.》 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112957364A (en) * 2021-03-29 2021-06-15 杭州立效生物医药科技有限公司 Medicine for treating renal tubular injury and application thereof

Also Published As

Publication number Publication date
CN102058613B (en) 2015-12-16

Similar Documents

Publication Publication Date Title
JP6375037B2 (en) Pharmaceutical composition containing crude drugs (組成)
CN105078956A (en) Application of forsythin aglycone in preparing medicine for preventing or treating liver injury or liver failure
CN103989695B (en) A kind of pharmaceutical composition and application thereof treating bronchial asthma
CN108815218A (en) Medical composition and its use
CN110585233B (en) Antitumor composition and pharmaceutical application thereof
CN103908611A (en) Traditional Chinese medicine preparation for treating colon cancer and preparation method of traditional Chinese medicine preparation
CN110368445A (en) A kind of Chinese medicine composition and its preparation method and application for treating psoriasis
CN110025705A (en) A kind of Chinese medicine composition and its preparation method and application for treating atopic dermatitis
CN103816448B (en) A kind of Chinese medicine composition treating pulmonary tuberculosis
CN102058613B (en) The purposes of anti-tumor active ingredient compositions in Herba Solani Nigri
CN105168500A (en) Pharmaceutical composition used for curing infantile dental ulcer and preparation method for pharmaceutical composition
CN107496525A (en) A kind of Chinese medicine composition for treating cancer pain disease and its application
CN104095904B (en) A kind of pharmaceutical composition for treating courage relevant disease, preparation method and its usage
CN102526387B (en) Medicinal composition for treating early-stage diabetic foot and preparation method thereof
CN108721442B (en) Traditional Chinese medicine composition and preparation for treating burns, scalds and diaper dermatitis and preparation method thereof
CN106138697B (en) Chinese medicinal composition for preventing complications and relieving side effects of radiotherapy and chemotherapy of tumor patients
CN103251869B (en) Traditional Chinese medicinal psoralen-containing composition for treating stomach cancer and preparation method and application thereof
CN104666927A (en) Traditional Chinese medicine composition and application thereof in regulating human immune functions and/or resisting tumors
CN109663012A (en) Dispelling wind and heat, removing toxic substances relieving sore-throat Chinese medicine composition and the preparation method and application thereof
CN103263475A (en) Traditional chinese medicine composition
CN103341109A (en) Natural drug extract and preparation method thereof
CN103566058B (en) A kind of double blue or green composition of medicine, preparation method and applications
CN103356769A (en) Natural drug extract, preparation method and application thereof
CN102552440A (en) Anti-asthmatic and anti-inflammatory medicament and preparation method and application thereof
CN105963423A (en) Pharynx-heat-clearing and larynx-moistening soft capsule preparation and method for preparing pharynx-heat-clearing and larynx-moistening soft capsule preparation

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C53 Correction of patent of invention or patent application
CB02 Change of applicant information

Address after: 210042 Xuanwu District, Xuanwu District, Jiangsu, Nanjing No. 699 -18

Applicant after: Jiangsu Simcere Pharmaceutical Research Company Limited

Address before: 210042 -18, Xuanwu Avenue, Xuanwu District, Jiangsu, Nanjing, 669

Applicant before: Jiangsu Simcere Pharmaceutical Research Company Limited

C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
ASS Succession or assignment of patent right

Owner name: JIANGSU SIMCERE PHARMACEUTICAL CO., LTD.

Effective date: 20150625

C41 Transfer of patent application or patent right or utility model
TA01 Transfer of patent application right

Effective date of registration: 20150625

Address after: 210042 Xuanwu District, Xuanwu District, Jiangsu, Nanjing No. 699 -18

Applicant after: Jiangsu Simcere Pharmaceutical Research Company Limited

Applicant after: Jiangsu Simcere Pharmaceutical Co., Ltd.

Address before: 210042 Xuanwu District, Xuanwu District, Jiangsu, Nanjing No. 699 -18

Applicant before: Jiangsu Simcere Pharmaceutical Research Company Limited

C14 Grant of patent or utility model
GR01 Patent grant
C41 Transfer of patent application or patent right or utility model
TR01 Transfer of patent right

Effective date of registration: 20160711

Address after: 210042 Xuanwu District, Xuanwu District, Jiangsu, Nanjing No. 699 -18

Patentee after: Jiangsu Simcere Pharmaceutical Co., Ltd.

Address before: 210042 Xuanwu District, Xuanwu District, Jiangsu, Nanjing No. 699 -18

Patentee before: Jiangsu Simcere Pharmaceutical Research Company Limited

Patentee before: Jiangsu Simcere Pharmaceutical Co., Ltd.

TR01 Transfer of patent right
TR01 Transfer of patent right

Effective date of registration: 20201229

Address after: 570311 No. 2 Yaogu No. 3 Road, Xiuying District, Haikou City, Hainan Province

Patentee after: Hainan Simcere Pharmaceutical Co.,Ltd.

Address before: 210042 699 Xuanwu Road, Xuanwu District, Nanjing, Jiangsu -18

Patentee before: JIANGSU SIMCERE PHARMACEUTICAL Co.,Ltd.