CN109846876A - Application and its medicine preparation of the Lignanoids compounds in antitumor - Google Patents
Application and its medicine preparation of the Lignanoids compounds in antitumor Download PDFInfo
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- CN109846876A CN109846876A CN201910313578.5A CN201910313578A CN109846876A CN 109846876 A CN109846876 A CN 109846876A CN 201910313578 A CN201910313578 A CN 201910313578A CN 109846876 A CN109846876 A CN 109846876A
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- neolignan
- hemlock spruce
- chinese hemlock
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Abstract
The application and its medicine preparation that the present invention relates to Lignanoids compounds in antitumor specifically provide a kind of by new pharmaceutical use associated with Dihydrosinapyl alcohol and two neolignan A of Chinese hemlock spruce.On the one hand Dihydrosinapyl alcohol promotes the dissolution of two neolignan A of Chinese hemlock spruce in water, on the other hand the nausea and vomiting toxic side effect of two neolignan A of Chinese hemlock spruce is inhibited, the two combination has the synergy of Synergy and attenuation, lays a good foundation for two neolignan A of Chinese hemlock spruce applied to clinic.
Description
Technical field
The present invention relates to a kind of anti-tumor drugs, exist in particular to two neolignan A of Chinese hemlock spruce combination Dihydrosinapyl alcohol
Application and its medicine preparation in antitumor.
Background technique
After 20 middle of century, developed country, developing country's lung cancer morbidity and mortality rise rapidly.According to 1973
~1975 Nian Sannian All death retrospective surveys and Chinese mortality of malignant tumors sample investigation in 1990~1992 years show: lung in China
Mortality of carcinoma is increased to the 17.54/10 ten thousand of the nineties by the 7.09/10 ten thousand of the 1970s, rises 147.39% (wherein
Male rises 158.94%, 122.55%) women rises.
Currently, still can not contain its ascendant trend although existing treatment means have significant progress.With
The transformation of medical model, tumor efficiency evaluation emphasis be also converted to by pursuing local remission rate merely in higher life matter
On the basis of amount and longer life span, highest Tumor response rate is obtained.In recent years, Treatment of Lung Cancer with Chinese Medicine is stablizing disease
Stove extends life span, improves life quality etc. and played significant curative effect, is not only applied alone effectively, and can with operation,
Radiotherapy, chemotherapy combined are with improving clinical efficacy and reducing toxicity, using cheap Chinese medicine treating cancer in clinical practice
In increasingly show advantage.By the research of the mechanism of action to Chinese medicine, help to find the useful effect position of medicinal material, effectively
Ingredient also provides thinking so that the standardization application for Chinese medicine provides reference for clinical development new drug.
Chinese patent CN109053641A discloses two Ne olignans of one kind and method for separating and preparing and application,
Wherein two neolignan A of Chinese hemlock spruce in vitro anti-tumor activity experiment in display have good antitumor activity, can be used for preparing anti-
Tumour medicine.However, rat shows apparent different thermophilic behavior, further experimental study when the compound is used for experiment in vitro
It was found that two neolignan A of Chinese hemlock spruce has the toxic side effect of nausea and vomiting.
Summary of the invention
In order to reduce by the toxic side effect of two neolignan A of Chinese hemlock spruce, the purpose of the present invention is to provide a kind of two new woods of Chinese hemlock spruce
Rouge element A is combined application and its pharmaceutical composition of the Dihydrosinapyl alcohol in antitumor.
In order to achieve the object of the present invention, the Dihydrosinapyl alcohol with solubilization that inventor will have found in early-stage study
It is combined with two neolignan A of Chinese hemlock spruce, on the one hand promotes the dissolution of two neolignan A of Chinese hemlock spruce, on the other hand inhibit Chinese hemlock spruce two
The nausea and vomiting toxic side effect of neolignan A, to reach the antitumor purpose of Synergy and attenuation.Specifics, skill of the invention
Art scheme overview is as follows: two neolignan A of Chinese hemlock spruce is combined Dihydrosinapyl alcohol application in preparation of anti-tumor drugs.
It should be noted that tumour of the present invention includes breast cancer, cancer of the esophagus, gastric cancer, lung cancer, intestinal cancer, liver cancer, palace
Neck cancer etc., two neolignan A (TNA) of Chinese hemlock spruce of the present invention, shown in chemical structural formula such as formula (I), Dihydrosinapyl alcohol
Shown in the chemical structural formula such as formula (II) of (Dihydrosinapyl alcohol, DSA).
It is further preferred that anti-tumor drug of the present invention is injection.Two new wood of Chinese hemlock spruce in the injection
The mass ratio of rouge element A and Dihydrosinapyl alcohol is 5-60:1.Still further preferably, two neolignan of Chinese hemlock spruce in the injection
The mass ratio of A and Dihydrosinapyl alcohol is 20-40:1.In an embodiment most preferably of the invention, the injection
The mass ratio of middle two neolignan A of Chinese hemlock spruce and Dihydrosinapyl alcohol is 30:1.
In addition, injection refers to the general designation of the dosage form for injection in the present invention.Further preferred note of the present invention
Penetrating agent is injection or freeze-dried powder injection.
Second object of the present invention is to provide a kind of antitumor medicine composition, which contains Chinese hemlock spruce
Two neolignan A and Dihydrosinapyl alcohol can be injection, or oral preparation, the oral preparation include tablet,
Capsule, granule, dripping pill etc..These oral preparations can be on the basis of above-mentioned active constituent, and being added can in pharmacy
Auxiliary material, such as filler, disintegrating agent, lubricant, adhesive, solubilizer, sustained-release matrix material, pass through the routine of this field
Preparation process is prepared.
It is further preferred that active constituent is only by two neolignan A of Chinese hemlock spruce and Dihydrosinapyl alcohol group in the pharmaceutical composition
At.Still further preferably, in the pharmaceutical composition active constituent by two neolignan A of Chinese hemlock spruce and Dihydrosinapyl alcohol according to
Mass ratio is 5-60:1 composition.Still further preferably, in the pharmaceutical composition active constituent by two neolignan A of Chinese hemlock spruce
With Dihydrosinapyl alcohol according to mass ratio be 20-40:1 form.In an embodiment most preferably of the invention, the medicine
Active constituent is made of two neolignan A of Chinese hemlock spruce and Dihydrosinapyl alcohol according to mass ratio for 30:1 in compositions.
Compared with prior art, the invention has the following beneficial effects: Dihydrosinapyl alcohols and two neolignan A of Chinese hemlock spruce to join
With on the one hand promoting the dissolution of two neolignan A of Chinese hemlock spruce in water, on the other hand inhibit the evil of two neolignan A of Chinese hemlock spruce
The heart vomits toxic side effect, and the two combination has the synergy of Synergy and attenuation, establishes for two neolignan A of Chinese hemlock spruce applied to clinic
Basis.
Specific embodiment
The invention will now be further described with reference to specific embodiments, the advantages and features of the present invention will be with description and
It is apparent.It should be understood that described, examples are merely exemplary, does not constitute any restrictions to protection scope of the present invention.This
Field technical staff should be understood that without departing from the spirit of the invention can details to technical solution and form carry out
Modifications or substitutions, but these modifications or substitutions each fall within protection scope of the present invention.In addition, particular technique is not specified in embodiment
Operating procedure or condition person, described ordinary skill or condition or according to product description according to the literature in the art
It carries out.Reagents or instruments used without specified manufacturer, being can be by the conventional reagent or instrument product of commercially available acquisition.
Test example 1
Wistar rat 24, male, natural lighting in 12 hours, free water, adaptive feeding, i.e., by chow diet with
Give rat simultaneously after kaolin quota of feed, and two kinds of feeds are taken out and claimed by timing daily, observation feed surface whether there is or not bite mark,
Until rat no longer gnaws kaolin, it is then randomly divided into following three groups: NS group, TNA group, TNA-DSA group, every group 8
Rat.Fasted for one day prior is tested, starts to test morning next day, on the basis of rat weight, physiological saline is given in the injection of NS group
10ml/kg, physiological saline 10ml/kg is given in injection respectively again after 1 hour at interval；The injection of TNA group gives Chinese hemlock spruce two neolignan A
300mg/kg, interval inject again after 1 hour and give physiological saline 10ml/kg；The injection of TNA-DSA group gives Chinese hemlock spruce two neolignans
A300mg/kg, interval inject again after 1 hour and give Dihydrosinapyl alcohol 10mg/kg.Injection system is intraperitoneal injection.Observation is each
Organize the different thermophilic kaolin behavior of rat in 24 hours upon administration, the chow diet of every rat of calculating and kaolinic consumption
Amount, referring to table 1.
For test statistics the results show that comparing blank control, injection gives the TNA group rat of two neolignan A of Chinese hemlock spruce to height
The intake of ridge soil increases considerably (P < 0.01), illustrates that two neolignan A of Chinese hemlock spruce can cause rat different thermophilic kaolin behavior occur.
Compared to TNA group, injection gives the TNA-DSA group rat of two neolignan A of Chinese hemlock spruce and Dihydrosinapyl alcohol to kaolinic intake
It significantly reduces (P < 0.01), illustrates that Dihydrosinapyl alcohol can reduce cause the spitting property side effect of two neolignan A of Chinese hemlock spruce.
Table 1: each group rat kaolin intake and food ration compare
Compared with TNA group,*P<0.01
Test example 2
Human liver cancer cell HepG-2, human breast cancer cell line Bcap-37, the human lung carcinoma cell line LTEP of logarithmic growth phase will be in
96 orifice plates are inoculated in 100 holes μ L/, adherent growth sucks supernatant, the medical fluid 100 of various concentration is added in every hole after 24 hours
μL.Each concentration sets 5 multiple holes, and sets the fetal calf serum culture medium control for not adding medical fluid.Cancer cell continues in 37 DEG C, 5%CO2
It is cultivated in incubator 24 hours, then 10 μ L MTT are added in every hole, continue culture 4 hours in carbon dioxide incubator, it takes out,
Supernatant is sucked, 150 hole μ L/ DMSO is added, light absorption value is surveyed under 490nm wavelength using microplate reader, calculates IC50, referring to table 2.
Table 2: half effective inhibition concentration (μM) of the different tested materials to tumour cell
Test statistics the results show that two neolignan A of Chinese hemlock spruce to human liver cancer cell HepG-2, human breast cancer cell line Bcap-37,
Human lung carcinoma cell line LTEP is significantly inhibited, and Dihydrosinapyl alcohol acts on the equal unrestraint of three kinds of cancer cells.
Claims (10)
1. two neolignan A of Chinese hemlock spruce is combined Dihydrosinapyl alcohol application in preparation of anti-tumor drugs.
2. application according to claim 1, which is characterized in that the anti-tumor drug is injection.
3. application according to claim 2, which is characterized in that two neolignan A of Chinese hemlock spruce and dihydro in the injection
The mass ratio of sinapinic alcohol is 5-60:1.
4. application according to claim 2, which is characterized in that two neolignan A of Chinese hemlock spruce and dihydro in the injection
The mass ratio of sinapinic alcohol is 20-40:1.
5. application according to claim 2, which is characterized in that two neolignan A of Chinese hemlock spruce and dihydro in the injection
The mass ratio of sinapinic alcohol is 30:1.
6. application according to claim 2, which is characterized in that the injection is injection or injection freeze-dried powder
Agent.
7. a kind of antitumor medicine composition, which is characterized in that the pharmaceutical composition contains two neolignan A of Chinese hemlock spruce and dihydro
Sinapinic alcohol.
8. antitumor medicine composition according to claim 7, which is characterized in that in the pharmaceutical composition active constituent by
Two neolignan A of Chinese hemlock spruce and Dihydrosinapyl alcohol composition.
9. antitumor medicine composition according to claim 8, which is characterized in that in the pharmaceutical composition active constituent by
Two neolignan A of Chinese hemlock spruce and Dihydrosinapyl alcohol are that 5-60:1 is formed according to mass ratio.
10. antitumor medicine composition according to claim 9, which is characterized in that active constituent in the pharmaceutical composition
It is made of two neolignan A of Chinese hemlock spruce and Dihydrosinapyl alcohol according to mass ratio for 20-40:1.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201910313578.5A CN109846876B (en) | 2019-04-18 | 2019-04-18 | Application of lignan compound in resisting tumor and preparation of medicine thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201910313578.5A CN109846876B (en) | 2019-04-18 | 2019-04-18 | Application of lignan compound in resisting tumor and preparation of medicine thereof |
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| Publication Number | Publication Date |
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| CN109846876A true CN109846876A (en) | 2019-06-07 |
| CN109846876B CN109846876B (en) | 2021-05-25 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN201910313578.5A Active CN109846876B (en) | 2019-04-18 | 2019-04-18 | Application of lignan compound in resisting tumor and preparation of medicine thereof |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010044685A1 (en) * | 2008-10-17 | 2010-04-22 | Auckland Uniservices Limited | Nitrophenyl mustard alcohols, their corresponding phosphates and their use as targeted cytotoxic agents |
| CN109053641A (en) * | 2018-08-22 | 2018-12-21 | 遵义医学院 | Two Ne olignans of one kind and method for separating and preparing and application |
-
2019
- 2019-04-18 CN CN201910313578.5A patent/CN109846876B/en active Active
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010044685A1 (en) * | 2008-10-17 | 2010-04-22 | Auckland Uniservices Limited | Nitrophenyl mustard alcohols, their corresponding phosphates and their use as targeted cytotoxic agents |
| CN109053641A (en) * | 2018-08-22 | 2018-12-21 | 遵义医学院 | Two Ne olignans of one kind and method for separating and preparing and application |
Non-Patent Citations (2)
| Title |
|---|
| 杨志宏 等: "辣椒提取物对3 种异嗜高岭土模型大鼠的止呕作用", 《中国新药杂志》 * |
| 赵友兴 等: "云南铁杉中一个新的倍半木脂素(英文)", 《云南植物研究》 * |
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| Publication number | Publication date |
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| CN109846876B (en) | 2021-05-25 |
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