CN110183462A - Application of the sesquiterpene small molecule compound in preparation treatment colon cancer drug, food or health care product - Google Patents
Application of the sesquiterpene small molecule compound in preparation treatment colon cancer drug, food or health care product Download PDFInfo
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- CN110183462A CN110183462A CN201910594347.6A CN201910594347A CN110183462A CN 110183462 A CN110183462 A CN 110183462A CN 201910594347 A CN201910594347 A CN 201910594347A CN 110183462 A CN110183462 A CN 110183462A
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- colon cancer
- sesquiterpene
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- molecule compound
- food
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- JYTUSYBCFIZPBE-AMTLMPIISA-N lactobionic acid Chemical compound OC(=O)[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@@H]1O[C@H](CO)[C@H](O)[C@H](O)[C@H]1O JYTUSYBCFIZPBE-AMTLMPIISA-N 0.000 description 1
- 210000002429 large intestine Anatomy 0.000 description 1
- 150000002632 lipids Chemical class 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 208000019423 liver disease Diseases 0.000 description 1
- 208000020816 lung neoplasm Diseases 0.000 description 1
- 210000001165 lymph node Anatomy 0.000 description 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
- 108020004999 messenger RNA Proteins 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- 230000009401 metastasis Effects 0.000 description 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 1
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- 229940016286 microcrystalline cellulose Drugs 0.000 description 1
- 229960004857 mitomycin Drugs 0.000 description 1
- 210000004400 mucous membrane Anatomy 0.000 description 1
- WQEPLUUGTLDZJY-UHFFFAOYSA-N n-Pentadecanoic acid Natural products CCCCCCCCCCCCCCC(O)=O WQEPLUUGTLDZJY-UHFFFAOYSA-N 0.000 description 1
- KVBGVZZKJNLNJU-UHFFFAOYSA-M naphthalene-2-sulfonate Chemical compound C1=CC=CC2=CC(S(=O)(=O)[O-])=CC=C21 KVBGVZZKJNLNJU-UHFFFAOYSA-M 0.000 description 1
- 235000001968 nicotinic acid Nutrition 0.000 description 1
- 239000011664 nicotinic acid Substances 0.000 description 1
- 235000020824 obesity Nutrition 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical class CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- 229940049964 oleate Drugs 0.000 description 1
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 description 1
- 230000008520 organization Effects 0.000 description 1
- 150000003891 oxalate salts Chemical class 0.000 description 1
- 235000019629 palatability Nutrition 0.000 description 1
- 239000012188 paraffin wax Substances 0.000 description 1
- MLVSYGCURCOSKP-FXCPCPCLSA-N parkeol Chemical group CC1(C)[C@@H](O)CC[C@]2(C)C3=CC[C@]4(C)[C@@H]([C@@H](CCC=C(C)C)C)CC[C@@]4(C)[C@@H]3CC[C@H]21 MLVSYGCURCOSKP-FXCPCPCLSA-N 0.000 description 1
- VLTRZXGMWDSKGL-UHFFFAOYSA-M perchlorate Inorganic materials [O-]Cl(=O)(=O)=O VLTRZXGMWDSKGL-UHFFFAOYSA-M 0.000 description 1
- VLTRZXGMWDSKGL-UHFFFAOYSA-N perchloric acid Chemical compound OCl(=O)(=O)=O VLTRZXGMWDSKGL-UHFFFAOYSA-N 0.000 description 1
- JRKICGRDRMAZLK-UHFFFAOYSA-L peroxydisulfate Chemical compound [O-]S(=O)(=O)OOS([O-])(=O)=O JRKICGRDRMAZLK-UHFFFAOYSA-L 0.000 description 1
- 150000003016 phosphoric acids Chemical class 0.000 description 1
- 229940075930 picrate Drugs 0.000 description 1
- OXNIZHLAWKMVMX-UHFFFAOYSA-M picrate anion Chemical compound [O-]C1=C([N+]([O-])=O)C=C([N+]([O-])=O)C=C1[N+]([O-])=O OXNIZHLAWKMVMX-UHFFFAOYSA-M 0.000 description 1
- 229950010765 pivalate Drugs 0.000 description 1
- IUGYQRQAERSCNH-UHFFFAOYSA-N pivalic acid Chemical compound CC(C)(C)C(O)=O IUGYQRQAERSCNH-UHFFFAOYSA-N 0.000 description 1
- 238000004321 preservation Methods 0.000 description 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 238000004393 prognosis Methods 0.000 description 1
- 238000001959 radiotherapy Methods 0.000 description 1
- 238000003753 real-time PCR Methods 0.000 description 1
- 201000001275 rectum cancer Diseases 0.000 description 1
- RXHIKAIVEMAPRU-JRIGQVHBSA-N sequiterpene Natural products C1=C(C)[C@@H](OC(C)=O)[C@H](O)[C@@]2(O)[C@H](C)CC[C@@H](C(C)=C)[C@H]21 RXHIKAIVEMAPRU-JRIGQVHBSA-N 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 150000004354 sesquiterpene derivatives Chemical class 0.000 description 1
- 150000003384 small molecules Chemical class 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- 210000004876 tela submucosa Anatomy 0.000 description 1
- 229950004288 tosilate Drugs 0.000 description 1
- 238000013518 transcription Methods 0.000 description 1
- 230000035897 transcription Effects 0.000 description 1
- 150000003648 triterpenes Chemical class 0.000 description 1
- 230000005740 tumor formation Effects 0.000 description 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 description 1
- ZDPHROOEEOARMN-UHFFFAOYSA-M undecanoate Chemical compound CCCCCCCCCCC([O-])=O ZDPHROOEEOARMN-UHFFFAOYSA-M 0.000 description 1
- 229940070710 valerate Drugs 0.000 description 1
- NQPDZGIKBAWPEJ-UHFFFAOYSA-N valeric acid Chemical compound CCCCC(O)=O NQPDZGIKBAWPEJ-UHFFFAOYSA-N 0.000 description 1
- 239000003981 vehicle Substances 0.000 description 1
- 210000003462 vein Anatomy 0.000 description 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
- 229920002554 vinyl polymer Polymers 0.000 description 1
- 230000009385 viral infection Effects 0.000 description 1
- 230000004580 weight loss Effects 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/10—Spiro-condensed systems
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
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- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
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- Engineering & Computer Science (AREA)
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- Polymers & Plastics (AREA)
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- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Coloring Foods And Improving Nutritive Qualities (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The present invention provides a kind of application of sesquiterpene small molecule compound in preparation treatment colon cancer drug, food or health care product, the invasion of colon cancer cell and transfer ability can be inhibited to have carried out experimental verification compound TCN, the expression of SCD1 can be lowered by being experimentally confirmed TCN, and then influence the invasion transfer of colon cancer cell.TCN can not only effectively inhibit the transfer ability of colon cancer cell, and without obvious toxic-side effects, provide new direction for the research of successive treatment colon cancer disease.
Description
Technical field
The present invention relates to medicinal usage technical fields, and in particular to a kind of sesquiterpene small molecule compound is controlled in preparation
Treat the application in colon cancer drug, food or health care product.
Background technique
Colorectal cancer (carcinoma oflarge intestine) is one of the kinds of tumor in China, including the carcinoma of the rectum and
Disease incidence rises most fast one of tumour over colon cancer, and nearly twenty or thirty year, and colorectal cancer has occupied the malignant tumour cause of the death at present
The the 4th, 5 or 6, the disease incidence 24/about 100000ths in China, male is slightly higher.And with the development of economy, life
Horizontal raising and living-pattern preservation, disease incidence will also be in the trend constantly risen.
Many large intestine epidemiologies studies have shown that causing many because being known as of colorectal cancer, such as dietary factor, occupation
Factor, physical exertion, inherent cause, disease factor and other carcinogenic factors etc..Colon cancer occurrence and development process can divide five ranks
Section), 0: cancer cell appears in mucous membrane of colon or colon inner wall；I: cancer cell reaches submucosa；II: colon cancer penetrates colon
Wall；III: cancer cell begins to diffuse into lymph node；IV: tumor nodule is formed in the tissue of pericolonic, and cancer is begun to transfer to
Liver, Fei Deng remote organization.
How unobvious the early symptom of colon cancer is, and middle and advanced stage has been arrived in most of patients diagnosis discovery, and colon cancer can drench
Bar transfer, hematogenous metastasis shift in enteric cavity and abdominal metastas etc., so that treatment is difficult.The concealment of colon cancer onset, China's intestinal cancer are early
The ratio that phase makes a definite diagnosis only has 5%-10%.Early stage colon cancer can be cured by operation, and for Advanced Colon Cancer patient, usually
The methods of chemotherapy, radiotherapy need to be taken to control tumour, extend the life cycle of patient.Chemotherapy is main
Using general chemotherapeutics such as fluorouracil (5 FU 5 fluorouracil and capecitabine), mitomycin and adriamycins, lack for knot
The efficiently special clinical treatment drug of intestinal cancer.
Stearyl-coenzyme A desaturase 1 (stearoyl-Coenzyme A desaturase1, SCD1) is also known as fatty acid
Δ 9- desaturase is to be catalyzed saturated fatty acid (SFA) rate-limiting enzyme for change to monounsaturated fatty acids (MUFA), with obesity,
Generation, the development of a series of metabolic syndrome such as fatty hepatic disease, insulin resistance and tumour are closely related；In recent years
Research finds that SCD1 plays a significant role in tumor invasion and metabasis progress.Hui Ran etc. [1] is sent out in colorectal cancer cell
Existing SCD1 high expression in Colorectal Carcinoma, negatively correlated with colorectal cancer prognosis, experiment in vitro is shown, SCD1 can lead to
It crosses promotion epithelial-mesenchymal conversion (EMT) and then promotes the progress of colorectal cancer.In addition, SCD1 can increase single unsaturated lipid
The amount of fat acid (MUFA), SCD1-MUFA is by inhibiting PTEN/Akt access to promote the invasion of colorectal cancer cell and move later
It moves.Wang H etc. [2] has found that SCD1 stablizes interference cell strain cell invasion ability and is decreased obviously in clear cell carcinoma of kidney.
Daniel Mauvoisin etc. [3] is targeted in breast cancer cell strike drop SCD1 after, the invasive ability of cell weakens.
CN02803679.4 discloses one kind and contains triterpene dihydro butyrospermol, dihydro lupeol and/or dihydro
The composition of parkeol, the composition are suitable as a kind of drug, a kind of food supplement or as a kind of cosmetics；Institute
It states composition and is preparing a kind of drug, a kind of food supplement or a kind of purposes of cosmetics, the immune tune for mammal
Section is as inhibited virus infection, cardiovascular disease, cancer, hypersensitivity and/or inflammatory response.CN201810288278.1 is provided
A kind of pharmaceutical composition and its application for treating colon cancer, the pharmaceutical composition of the treatment colon cancer is by 2- { 3- [(7- { 3-
[ethyl (2- hydroxyethyl) amino] propoxyl group } quinazoline -4- base) amino] -1H- pyrazoles -5- base }-N- (3- fluorophenyl) acetyl
Amine and 1,8- dihydroxy -3- carboxyl anthraquinone form；There is inhibiting effect to colon cancer cell line SW1116 in vivo.
Trichothecin (TCN) is a kind of sesquiterpene small molecule compound of originated from fungus, does not temporarily have it to be used to prepare treatment
The relevant report of colon cancer drug.
[1]Ran,H.,Y.Zhu,R.Deng,et al.Stearoyl-CoA desaturase-1promotes
colorectal cancer metastasis in response to glucose by suppressing PTEN[J].J
Exp Clin Cancer Res,2018.37(1):p.54.
[2]Wang,H.,Y.Zhang,Y.Lu,et al.The role of stearoyl-coenzyme A
desaturase 1in clear cell renal cell carcinoma[J].Tumour Biol,2016.37(1):
p.479-89.
[3]Mauvoisin,D.,C.Charfi,A.M.Lounis,et al.Decreasing stearoyl-CoA
desaturase-1expression inhibits beta-catenin signaling in breast cancer cells
[J].Cancer Sci,2013.104(1):p.36-42.
Summary of the invention
For the above-mentioned technical problems in the prior art, the present invention provides a kind of sesquiterpene micromolecular chemical combination
Application of the object in preparation treatment colon cancer drug, food or health care product, can inhibit invasion and the migration energy of colon cancer cell
Power.
On the one hand, the present invention provides a kind of sesquiterpene small molecule compounds in preparation treatment colon cancer drug, food
Application in product or health care product, the sesquiterpene small molecule compound is structural formula shown in formula (I) or it can pharmaceutically connect
The salt received:
Wherein R is R1- C (=O)-；The R1For alkyl, alkenyl, alkynyl or aromatic radical；
The alkyl, alkenyl, alkynyl and aromatic radical optionally further by hydrogen, halogen, hydroxyl, nitro, cyano, amino,
Amino C1-6Alkyl, C1-6Alkyl amino or monosubstituted or identical or different polysubstituted of aminoacyl.
Further, the R1For C1-6Alkyl, C2-6Alkenyl, C2-6Alkynyl or C6-12Aromatic radical.
Further, the R1For methyl, ethyl, normal-butyl, n-pentyl, isopropyl, 1- acrylic, vinyl, 2- third
Alkenyl, 1- cyclobutenyl, acetenyl, 1- propinyl, 2-propynyl or phenyl.
Further, the sesquiterpene small molecule compound is structural formula (that is: Trichothecin shown in formula (II)
Or its pharmaceutically acceptable salt (TCN)):
Further, the pharmaceutically acceptable salt refers to that those salt forms are aobvious and easy for pharmaceutical chemistry man
See, i.e., they are substantially nontoxic and can provide required pharmacokinetic property, palatability, absorption, distribution, metabolism or row
It lets out." pharmaceutically acceptable salt " refers to the organic salt and inorganic salts of the compound of the present invention.It is pharmaceutically acceptable nontoxic
The salt that acid is formed includes, but is not limited to, and inorganic acid salt formed by reacting with amino groups to form has hydrochloride, hydrobromate, phosphoric acid
Salt, sulfate, perchlorate and acylate such as acetate, oxalates, maleate, tartrate, citrate, amber
Hydrochlorate, malonate, or these salt are obtained by other methods described in the books or literature such as ion-exchange.Its other medicine
Acceptable salt includes adipate, malate, 2 hydroxy propanoic acid salt, alginates, ascorbate, aspartic acid on
Salt, benzene sulfonate, benzoate, bisulphate, borate, butyrate, camphor hydrochlorate, camsilate, cyclopentyl propionate,
Digluconate, lauryl sulfate, esilate, formates, fumarate, gluceptate, phosphoglycerol
Salt, gluconate, Hemisulphate, enanthate, caproate, hydriodate, 2- hydroxy-ethanesulfonate salt, lactobionate, lactic acid
Salt, laruate, lauryl sulfate, malate, mesylate, 2- naphthalene sulfonate, nicotinate, nitrate, oleate, palm fibre
Palmitic acid hydrochlorate, pamoate, pectate, persulfate, 3- phenylpropionic acid salt, picrate, pivalate, propionate, stearic acid
Salt, rhodanate, tosilate, undecylate, valerate, etc..Salt obtained by an appropriate base includes alkali metal,
Alkaline-earth metal, the salt of ammonium.
Further, the sesquiterpene small molecule compound lowers the expression of SCD1.
Further, the sesquiterpene small molecule compound inhibits invasion and the transfer ability of colon cancer cell.
On the other hand, the present invention provides a kind of pharmaceutical composition, which is characterized in that described pharmaceutical composition includes sequiterpene
Alkenes small molecule compound and pharmaceutically acceptable carrier；Described pharmaceutical composition be used to prepare treatment colon cancer drug,
Food or health care product.
Further, the pharmaceutically acceptable carrier be selected from microcrystalline cellulose, starch, starch slurry, amylum pregelatinisatum,
In magnesium stearate, lactose, superfine silica gel powder, polyvinylpyrrolidone, ethyl alcohol, dextrin, cane sugar powder or croscarmellose sodium
It is one or more.
Compared with prior art, the present invention have it is following the utility model has the advantages that
The present invention provides a kind of sesquiterpene small molecule compounds in preparation treatment colon cancer drug, food or health care
Application in product can inhibit the invasion of colon cancer cell and transfer ability to carry out experimental verification compound TCN, pass through reality
The expression of SCD1 can be lowered by verifying bright TCN, and then influence the invasion transfer of colon cancer cell.TCN can not only be effective
Inhibit the transfer ability of colon cancer cell, and without obvious toxic-side effects, the research for successive treatment colon cancer disease is provided newly
Direction.
Detailed description of the invention
Fig. 1 Westernblot detects the protein expression level of SCD1 in HCT-116 and LoVo cell；
Fig. 2 Transwell detects TCN processing to the invasion of colon cancer cell and the influence of transfer ability；
Fig. 3 TCN inhibits transfer ability in colon cancer cell body.(A) the fixed nude mice lung tissue of Bouin ' s fixer is black
Color arrows Lung metastases tubercle；(B) quantity statistics of every group of Lung neoplasm, * P < 0.05；(C) nude mice lung tissue section H&E contaminates
Color；(D) nude mice weight time graph.
Specific embodiment
The technical scheme in the embodiments of the invention will be clearly and completely described below, it is clear that described implementation
Example is only a part of the embodiment of the present invention, instead of all the embodiments.Based on the embodiments of the present invention, this field is common
Technical staff's every other embodiment obtained, shall fall within the protection scope of the present invention.Unless otherwise defined, hereinafter made
All technical terms are identical as the normally understood meaning of those skilled in the art.Technical term used herein is
In order to describe the purpose of specific embodiment, it is not intended to and limits the scope of the invention.
Embodiment 1
In complete medium [1640 (gibco company, article No. C11875500BT)+10% fetal calf serums of cell
(BiologicalIndustries company, article No. 04-001-1ACS)] in add TCN, make final concentration be respectively 0.25 μM and
It 0.5 μM, after cultivating colon cancer cell HCT116, LOVO for 24 hours, is detected respectively using real-time PCR and western blot
The mRNA (Figure 1A) of SCD1 molecule and protein expression situation (Figure 1B) in HCT116 and LOVO cell, it can be found that TCN from Fig. 1
Transcription and the expression of SCD1 are lowered with dosage-dependent manner.
Embodiment 2
HCT116 cell is inoculated in respectively to be covered with matrigel glue (lower layer's figure, Invasion) and not to spread matrigel glue
The cell Transwell of (upper layer figure, Migration), after detecting (0 μM, 0.25 μM, 0.5 μM) processing 48h of various concentration TCN,
The invasion of HCT116 and LOVO cell and transfer ability, statistics traverse to the cell number at the cell the Transwell back side.As a result as schemed
Shown in 2.
It is found from Fig. 2, TCN processing group (0.25,0.5 μM of group) is relative to untreated fish group (0 μM of group), the cell number passed through
It significantly reduces, it is confirmed that TCN can inhibit invasion and the transfer ability of colon cancer cell.
Embodiment 3
By 1 × 106A colon cancer HCT116 cell is by establishing transplanted tumor in nude mice mould in tail vein injection to nude mouse
Type.
Tumor formation nude mice is divided into three groups, every group 4, is respectively as follows: control group (Vehicle), low dosage TCN group
(0.5mg/kg) and high dose TCN group (1mg/kg).
Respectively by intraperitoneal injection various concentration TCN drug therapy, once every other day, and nude mice weight is recorded.
After treatment end, after lung tissue being fixed with Bouin ' s fixer, count Lung metastases tubercle number.
Further lung tissue is dehydrated, is sliced after paraffin embedding, H&E dyeing is carried out.
Relative to control group, the Lung metastases tubercle quantity of low dosage TCN group and high dose TCN group is substantially reduced (Fig. 3 B).
Meanwhile the nude mice weight of low dosage and high dose TCN group and control group do not have difference, i.e., the performance (figure such as no weight loss
3D).It can show that TCN has the transfer ability for inhibiting colon cancer cell in vivo from Fig. 3, and without obvious toxic-side effects.
To sum up, small molecule compound TCN is shifted by the invasion for inhibiting the expression of SCD1 to influence colon cancer cell.
Obviously, the above embodiments are merely examples for clarifying the description, and does not limit the embodiments.It is right
For those of ordinary skill in the art, can also make on the basis of the above description it is other it is various forms of variation or
It changes.There is no necessity and possibility to exhaust all the enbodiments.And it is extended from this it is obvious variation or
It changes still within the protection scope of the invention.
Claims (9)
1. a kind of application of sesquiterpene small molecule compound in preparation treatment colon cancer drug, food or health care product,
It is characterized in that, the sesquiterpene small molecule compound is structural formula or its pharmaceutically acceptable salt shown in formula (I):
Wherein R is R1- C (=O)-；The R1For alkyl, alkenyl, alkynyl or aromatic radical；
The alkyl, alkenyl, alkynyl and aromatic radical are optionally further by hydrogen, halogen, hydroxyl, nitro, cyano, amino, amino
C1-6Alkyl, C1-6Alkyl amino or monosubstituted or identical or different polysubstituted of aminoacyl.
2. sesquiterpene small molecule compound according to claim 1 is in preparation treatment colon cancer drug, food or guarantor
Application in strong product, which is characterized in that the R1For C1-6Alkyl, C2-6Alkenyl, C2-6Alkynyl or C6-12Aromatic radical.
3. sesquiterpene small molecule compound according to claim 1 is in preparation treatment colon cancer drug, food or guarantor
Application in strong product, which is characterized in that the R1For methyl, ethyl, normal-butyl, n-pentyl, isopropyl, 1- acrylic, ethylene
Base, 2- acrylic, 1- cyclobutenyl, acetenyl, 1- propinyl, 2-propynyl or phenyl.
4. sesquiterpene small molecule compound according to claim 1 is in preparation treatment colon cancer drug, food or guarantor
Application in strong product, which is characterized in that the sesquiterpene small molecule compound is structural formula or its pharmacy shown in formula (II)
Upper acceptable salt:
5. sesquiterpene small molecule compound according to claim 1 is in preparation treatment colon cancer drug, food or guarantor
Application in strong product, which is characterized in that the pharmaceutically acceptable salt refers to the organic salt or inorganic of structural formula shown in formula (I)
Salt.
6. sesquiterpene small molecule compound according to claim 1 is in preparation treatment colon cancer drug, food or guarantor
Application in strong product, which is characterized in that the sesquiterpene small molecule compound lowers the expression of SCD1.
7. sesquiterpene small molecule compound according to claim 1 is in preparation treatment colon cancer drug, food or guarantor
Application in strong product, which is characterized in that the sesquiterpene small molecule compound inhibits the invasion and migration of colon cancer cell
Ability.
8. a kind of pharmaceutical composition, which is characterized in that described pharmaceutical composition includes sesquiterpene small molecule compound and medicine
Acceptable carrier on；The sesquiterpene small molecule compound is structural formula shown in formula (I) or its is pharmaceutically acceptable
Salt；Described pharmaceutical composition is used to prepare drug, food or the health care product for the treatment of colon cancer.
9. pharmaceutical composition according to claim 8, which is characterized in that the pharmaceutically acceptable carrier is selected from crystallite
Cellulose, starch, starch slurry, amylum pregelatinisatum, magnesium stearate, lactose, superfine silica gel powder, polyvinylpyrrolidone, ethyl alcohol, paste
One of essence, cane sugar powder or croscarmellose sodium are a variety of.
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN87104045A (en) * | 1985-10-17 | 1988-11-09 | 尼奥尔克斯公司 | Trichothecent conjugates |
| US7015244B1 (en) * | 1998-08-11 | 2006-03-21 | Mark Zamoyski | Inhalable chemical debridement for COPD |
-
2019
- 2019-07-03 CN CN201910594347.6A patent/CN110183462A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN87104045A (en) * | 1985-10-17 | 1988-11-09 | 尼奥尔克斯公司 | Trichothecent conjugates |
| US7015244B1 (en) * | 1998-08-11 | 2006-03-21 | Mark Zamoyski | Inhalable chemical debridement for COPD |
Non-Patent Citations (2)
| Title |
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