CN106309453A - Application of Friedolanostanes in manufacture of medicaments for treating rectal cancer - Google Patents
Application of Friedolanostanes in manufacture of medicaments for treating rectal cancer Download PDFInfo
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- CN106309453A CN106309453A CN201610815270.7A CN201610815270A CN106309453A CN 106309453 A CN106309453 A CN 106309453A CN 201610815270 A CN201610815270 A CN 201610815270A CN 106309453 A CN106309453 A CN 106309453A
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- Prior art keywords
- friedolanostanes
- rectal cancer
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- medicaments
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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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention discloses application of Friedolanostanes in the manufacture of medicaments for treating rectal cancer and belongs to the technical field of new drug use. The invention has found that Friedolanostanes have a significant inhibitory effect on the growth of human rectal cancer cell strains LOVE1, LOVO, SW620 and SW480 by in vitro MTT antitumor activity evaluation. Therefore, Friedolanostanes can be used for the preparation of anti-rectal cancer drugs, and has a good development and application prospects. The application of Friedolanostanes according to the present invention in the manufacture of medicaments for treating rectal cancer is first disclosed and its inhibitory activity against rectal cancer cells is surprising.
Description
Technical field
The present invention relates to the new application of compound Friedolanostanes, particularly relate to Friedolanostanes in system
Application in standby treatment rectal cancer medicine.
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.Anticancer
The focus of the research and development of medicine always study of pharmacy.Having 74% in antitumor drug is natural product or derivatives thereof, such as Ramulus et folium taxi cuspidatae
Alcohol and derivant thereof are exactly the antitumor drug that application effectiveness comparison is good the most clinically.Therefore, from natural product, searching is anti-
Chemical compound for treating cancer or lead compound have great importance.
The compound Friedolanostanes that the present invention relates to be one within 2013, deliver (Saranyoo Klaiklay,
et al.,Friedolanostanes and xanthones from the twigs of Garcinia
Hombroniana.Phytochemistry, 85 (2013) 161 166.) noval chemical compound, this compound has brand-new skeleton
Type, current purposes merely relate to suppress hepatitis C virus (Saranyoo Klaiklay, et al.,
Friedolanostanes and xanthones from the twigs of Garcinia
Hombroniana.Phytochemistry, 85 (2013) 161 166.), for the Friedolanostanes that the present invention relates to
Purposes in preparation treatment rectal cancer medicine belongs to first public, and owing to belonging to brand-new structure type, and it is for directly
The inhibitory activity of colon-cancer cell is unexpectedly strong, and there is not the possibility being provided any enlightenment by other compounds, possesses prominent
Substantive distinguishing features, be simultaneously used for the preventing and treating of rectal cancer and obviously have the most progressive.
Summary of the invention
Do not find in it is an object of the invention to study according to existing Friedolanostanes that it has anti-rectal cancer and lives
Property the present situation of report, it is provided that Friedolanostanes application in preparation medicine for treating rectal cancer.
Described compound Friedolanostanes structure is as shown in formula I:
The present invention is found by external MTT antineoplastic activity evaluation, and Friedolanostanes is to people's rectum cancer cell strain
The growth of LOVE1, LOVO, SW620 and SW480 also has significant inhibitory action, suppresses the IC50 value point that this 4 strain cell grows
It is not 1.78 ± 0.45 μMs, 2.57 ± 0.74 μMs, 1.89 ± 0.43 μMs and 2.57 ± 0.38 μMs.Therefore,
Friedolanostanes can be used for preparing medicine for treating rectal cancer, has good development prospect.
The Friedolanostanes that the present invention relates to purposes in preparation treatment rectal cancer medicine is belonged to first
Open, owing to framework types belongs to brand-new framework types, and it must be expected not for the inhibitory activity of rectum cancer cell is strong
Arrive, there is not the possibility being provided any enlightenment by other compounds, possess prominent substantive distinguishing features, be simultaneously used for rectal cancer
Preventing and treating 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 concrete real
Execute any restriction of example, but be defined in the claims.
Detailed description of the invention
The preparation method of compound Friedolanostanes involved in the present invention sees document (Saranyoo
Klaiklay, et al., Friedolanostanes and xanthones from the twigs of Garcinia
hombroniana.Phytochemistry,85(2013)161–166.)
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not by concrete real
Execute any restriction of example, but be defined in the claims.
Embodiment 1: the preparation of compound Friedolanostanes tablet involved in the present invention:
Take 20 g of compound Friedolanostanes additions and prepare the customary adjuvant 180 grams of tablet, mixing, Conventional compression
Machine makes 1000.
Embodiment 2: the preparation of compound Friedolanostanes capsule involved in the present invention:
Take 20 g of compound Friedolanostanes additions and prepare the customary adjuvant such as starch 180 grams of capsule, mixing,
Encapsulated make 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Experimental example: use mtt assay to evaluate the compound Friedolanostanes growth inhibited to people's rectum cancer cell strain
Effect
1. method: be in the cell of growth logarithmic (log) phase: people rectum cancer cell strain LOVE1, LOVO, SW620 and SW480 (purchase
Buy from Chinese Academy of Sciences's cell bank) with 1.5 × 104Concentration kind is in 96 orifice plates.Original training is sucked after cell cultivation 24h is adherent
Support base.Test is divided into blank group, drug treating group.Blank group changes 1640 culture medium containing 10% hyclone；Medicine
It is 100 μMs that process group is changed containing concentration, 50 μMs, 10 μMs, 1 μM, 0.1 μM, 0.01 μM and the Friedolanostanes of 0.001 μM
Culture medium.After cultivating 48h, add the MTT of concentration 5mg/mL, continue to be put in CO2Incubator cultivates 4h, then along culture fluid
Top sucks 100 μ L of supernatant, adds 100 μ L DMSO, and 10min is placed in dark place, utilizes microplate reader (Sunrise Products) to survey
Determining light absorption value (wavelength 570nm), and calculate cell survival according to light absorption value, each process sets 6 repeating holes.Cell survival
Rate (%)=Δ OD drug treating/Δ OD blank × 100.
2. result: the Friedolanostanes life to people rectum cancer cell strain P LOVE1, LOVO, SW620 and SW480
Long have significant inhibitory action.Suppression people rectum cancer cell strain LOVE1, LOVO, SW620 and SW480 growth of this compound
IC50 value is respectively 1.78 ± 0.45 μMs, 2.57 ± 0.74 μMs, 1.89 ± 0.43 μMs and 2.57 ± 0.38 μMs.
Shown by above-described embodiment, the Friedolanostanes of the present invention to people rectum cancer cell strain LOVE1, LOVO,
The growth of SW620 and SW480 has good inhibiting effect.Thus proving, the Friedolanostanes of the present invention has anti-
Rectal cancer activity, can be used for preparing medicine for treating rectal cancer.
Claims (1)
1.Friedolanostanes application in treatment rectal cancer medicine, described compound Friedolanostanes structure
As shown in formula I:
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610815270.7A CN106309453A (en) | 2016-09-11 | 2016-09-11 | Application of Friedolanostanes in manufacture of medicaments for treating rectal cancer |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610815270.7A CN106309453A (en) | 2016-09-11 | 2016-09-11 | Application of Friedolanostanes in manufacture of medicaments for treating rectal cancer |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN106309453A true CN106309453A (en) | 2017-01-11 |
Family
ID=57786590
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610815270.7A Pending CN106309453A (en) | 2016-09-11 | 2016-09-11 | Application of Friedolanostanes in manufacture of medicaments for treating rectal cancer |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN106309453A (en) |
-
2016
- 2016-09-11 CN CN201610815270.7A patent/CN106309453A/en active Pending
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| WD01 | Invention patent application deemed withdrawn after publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20170111 |