CN105878237A - Drug composition for treating tongue cancer and preparation method and application thereof - Google Patents
Drug composition for treating tongue cancer and preparation method and application thereof Download PDFInfo
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- CN105878237A CN105878237A CN201610248852.1A CN201610248852A CN105878237A CN 105878237 A CN105878237 A CN 105878237A CN 201610248852 A CN201610248852 A CN 201610248852A CN 105878237 A CN105878237 A CN 105878237A
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
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- Pharmacology & Pharmacy (AREA)
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- Life Sciences & Earth Sciences (AREA)
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- General Health & Medical Sciences (AREA)
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Abstract
The invention discloses a drug composition for treating tongue cancer and belongs to the technical field of new application of drug. An active ingredient of the drug composition is composed of, by mass, 70% of a compound I and 30% of a compound II, the compound I is Clathridine A, and the compound II is Naamidine H. in-vitro MTT anti-tumor activity evaluation finds that the drug composition can be used for preparing anti-tongue-cancer drug and has good development and application prospect. It is the first time to disclose application of the drug composition in preparing drug for treating tongue cancer, and activity of the drug composition in inhibiting tongue cancer cells is unexpectedly high.
Description
Technical field
The present invention relates to the new application of compound composition, particularly relate to one treat tongue cancer drug compositions and preparation method thereof and
Application.
Background technology
Cancer is one of disease maximum to human life's health hazard, has substantial amounts of people to die from cancer every year.Cancer therapy drug
The focus of research and development always study of pharmacy.Having 74% in antitumor drug is natural product or derivatives thereof, such as paclitaxel and spread out
Biology is exactly the antitumor drug that application effectiveness comparison is good the most clinically.Therefore, from natural product find anticancer compound or
Lead compound has great importance.
The compound Clathridine A that the present invention relates to and Naamidine H be within 2012, deliver (Jayanta Das, et al.,
Total Syntheses of Kealiinines A-C.Org Lett., 14 (24) 6,210 6213.) noval chemical compound,
Both compounds have brand-new framework types, combine for the Clathridine A that the present invention relates to and Naamidine H
Thing purposes in preparation treatment tongue cancer drug belongs to first public, and owing to belonging to brand-new structure type, and it is for carcinoma of tongue
The inhibitory activity of cell is unexpectedly strong, and there is not the possibility being provided any enlightenment by other compounds, possesses prominent essence
Property feature, be simultaneously used for the preventing and treating of carcinoma of tongue and obviously have the most progressive.
Summary of the invention
Do not find that it has anti-tongue cancer in it is an object of the invention to study according to existing Clathridine A and Naamidine H
The present situation of the report of activity, it is provided that the compositions of Clathridine A and Naamidine H is in preparation anti-tongue cancer medicine
Application.
One treats tongue cancer drug compositions, and the active component of said composition is made up of compound I and compound II, this combination
In thing, the mass percent of compound I and compound II is respectively 70% and 30%, and described compound I is Clathridine A,
Structure is as shown in formula I, and described compound II is Naamidine H, shown in structure such as formula (II):
Described treatment tongue cancer drug compositions, preparation method is according to quality by the powder of compound I and the powder of compound II
Percent respectively 70% and 30% is sufficiently mixed, and adds adjuvant.Make preparation.
Described treatment tongue cancer drug compositions, carcinoma of tongue behaviour longue carcinoma PTca8113 and T6.
The application in preparation treatment tongue cancer drug of the described treatment tongue cancer drug compositions.
The present invention is found by external MTT antineoplastic activity evaluation, Clathridine A and the compositions pair of Naamidine H
The growth of people longue carcinoma PTca8113 and T6 also has significant inhibitory action, suppresses the IC50 that this 2 strain cell grows
Value is respectively 1.56 ± 0.23 μMs and 1.79 ± 0.32 μMs.Therefore, the present composition can be used for preparing anti-tongue cancer medicine,
There is good development prospect.
Present composition purposes in preparation treatment tongue cancer drug is belonged to first public, owing to framework types belongs to brand-new
Framework types, and it is unexpectedly strong for the inhibitory activity of Human Tongue Carcinoma Lines, do not exist be given by other compounds any
The possibility of enlightenment, possesses prominent substantive distinguishing features, and the preventing and treating being simultaneously used for carcinoma of tongue obviously has the most progressive.
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not by specific embodiment
Any restriction, but be defined in the claims.
Detailed description of the invention
The preparation method of compound Clathridine A and Naamidine H involved in the present invention sees document (Jayanta
Das, et al., Total Syntheses of Kealiinines A-C.Org Lett.2012,14 (24) 6,210 6213.).
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not by specific embodiment
Any restriction, but be defined in the claims.
Embodiment 1: the preparation of compound composition tablet involved in the present invention:
Taking 7 grams of Clathridine A and 3 grams of Naamidine H, add 190 grams of dextrin, mixing, Conventional compression is made
1000.
Embodiment 2: the preparation of compound composition capsule involved in the present invention:
Take 7 grams of Clathridine A and 3 grams of Naamidine H, add starch 190 grams, mixing, encapsulated make 1000
Grain.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Experimental example: the growth of people's longue carcinoma is pressed down by the present composition using mtt assay to evaluate COMPOUNDS EXAMPLE 1 preparation
Make and use
1. method: be in the cell of growth logarithmic (log) phase: people longue carcinoma PTca8113 and T6 (buys from the Chinese Academy of Sciences
Cell bank) with 1.5 × 104Concentration kind is in 96 orifice plates.Original culture medium is sucked after cell cultivation 24h is adherent.Test
It is divided into blank group, drug treating group.Blank group changes 1640 culture medium containing 10% hyclone；Drug treating group is more
Changing containing concentration is 100 μMs, 50 μMs, 10 μMs, 1 μM, 0.1 μM, 0.01 μM and the enforcement of 0.001 μM
The culture medium of the present composition of example 1 preparation, it is 100 μMs that matched group is changed containing concentration, 50 μMs, 10 μMs, 1 μM,
0.1 μM, the culture medium of reference substance prepared by the individually oriented compound I of 0.01 μM and 0.001 μM and compound II.Training
After supporting 48h, add the MTT of concentration 5mg/mL, continue to be put in CO2Incubator cultivates 4h, then along on culture fluid
Portion sucks 100 μ L of supernatant, adds 100 μ L DMSO, and 10min is placed in dark place, utilizes microplate reader (Sunrise company
Product) measure light absorption value (wavelength 570nm), and calculate cell survival according to light absorption value, each process sets 6 repetitions
Hole.Cell survival rate (%)=Δ OD drug treating/Δ OD blank × 100.
2. result: the growth of people longue carcinoma P PTca8113 and T6 is had by the present composition of embodiment 1 preparation
Significantly inhibitory action.The IC50 value of this compound composition suppression people longue carcinoma PTca8113 and T6 growth is respectively
1.56 ± 0.23 μMs and 1.79 ± 0.32 μMs, and matched group suppression people's carcinoma of tongue prepared by individually oriented compound I and compound II is thin
The IC50 value of born of the same parents strain PTca8113 and T6 growth is respectively 0.13 ± 0.09 μM and 0.22 ± 0.12 μM.
Being shown by above-described embodiment, the present composition of embodiments of the invention 1 preparation is to people longue carcinoma PTca8113
Growth with T6 has good inhibiting effect.Thus proving, the present composition of embodiments of the invention 1 preparation has
Anti-tongue cancer activity, can be used for preparing anti-tongue cancer medicine.
Claims (4)
1. a treatment tongue cancer drug compositions, it is characterised in that the active component of said composition is by compound I and chemical combination
Thing II forms, and in said composition, the mass percent of compound I and compound II is respectively 70% and 30%, described
Shown in the structure of compound I such as formula (I), shown in the structure such as formula (II) of described compound II:
2. treat tongue cancer drug compositions as claimed in claim 1, it is characterised in that: preparation method is by compound I
Powder and the powder of compound II be sufficiently mixed according to mass percent respectively 70% and 30%, add adjuvant, system
Become preparation.
3. treat tongue cancer drug compositions as claimed in claim 1, it is characterised in that: carcinoma of tongue behaviour longue carcinoma
PTca8113 and T6.
4. treatment tongue cancer drug compositions application in treatment tongue cancer drug as claimed in claim 1.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610248852.1A CN105878237A (en) | 2016-04-19 | 2016-04-19 | Drug composition for treating tongue cancer and preparation method and application thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610248852.1A CN105878237A (en) | 2016-04-19 | 2016-04-19 | Drug composition for treating tongue cancer and preparation method and application thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105878237A true CN105878237A (en) | 2016-08-24 |
Family
ID=56705181
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610248852.1A Pending CN105878237A (en) | 2016-04-19 | 2016-04-19 | Drug composition for treating tongue cancer and preparation method and application thereof |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103251609A (en) * | 2013-06-03 | 2013-08-21 | 南京正亮医药科技有限公司 | Application of Aspeverin in preparation of medicines for treating tongue cancer |
| CN103263431A (en) * | 2013-06-03 | 2013-08-28 | 南京正亮医药科技有限公司 | Application of polyflavanostilbene A in preparation of medicaments for treating tongue carcinoma |
-
2016
- 2016-04-19 CN CN201610248852.1A patent/CN105878237A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103251609A (en) * | 2013-06-03 | 2013-08-21 | 南京正亮医药科技有限公司 | Application of Aspeverin in preparation of medicines for treating tongue cancer |
| CN103263431A (en) * | 2013-06-03 | 2013-08-28 | 南京正亮医药科技有限公司 | Application of polyflavanostilbene A in preparation of medicaments for treating tongue carcinoma |
Non-Patent Citations (2)
| Title |
|---|
| JAYANTA DAS等: "Total Syntheses of Kealiinines A-C", 《ORGANIC LETTERS》 * |
| 潘剑剑: "《海洋生物知多少（一）》", 31 January 2011, 中国时代经济出版社 * |
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| PB01 | Publication | ||
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Application publication date: 20160824 |