CN103251613A - Application of Aspeverin in preparation of medicines for treating ileocecum cancer - Google Patents
Application of Aspeverin in preparation of medicines for treating ileocecum cancer Download PDFInfo
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- CN103251613A CN103251613A CN2013102173922A CN201310217392A CN103251613A CN 103251613 A CN103251613 A CN 103251613A CN 2013102173922 A CN2013102173922 A CN 2013102173922A CN 201310217392 A CN201310217392 A CN 201310217392A CN 103251613 A CN103251613 A CN 103251613A
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- aspeverin
- ileocecum
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Abstract
The invention discloses an application of Aspeverin in preparation of medicines for treating ileocecum cancer, and belongs to the technical field of new medicinal applications. In vitro MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) antitumor activity evaluation discovers that the Aspeverin also has an obvious inhibition function on the growth of a human ileocecum cancer cell strain HCT-8. Consequently, the Aspeverin can be used for preparing anti-ileocecum cancer medicines and has good development and application prospects. The application of Aspeverin in preparation of medicines for treating ileocecum cancer is disclosed for the first time, and the Aspeverin has an unexpected strong effect of inhibiting the ileocecum cancer cell activity.
Description
Technical field
The present invention relates to the new purposes of compd A speverin, relate in particular to the application of Aspeverin in preparation treatment ileocecum cancer drug.
Background technology
Cancer is to one of disease of human life's health hazard maximum, and annual have a large amount of people to die from cancer.The research and development of cancer therapy drug are the focuses of study of pharmacy always.Having 74% to be the natural product or derivatives thereof in the antitumor drug, is exactly the reasonable antitumor drug of effect clinically at present as paclitaxel and derivant thereof.Therefore, searching anticancer compound or lead compound have great importance from natural product.
The compd A speverin that the present invention relates to is one and delivered (Nai-Yun Ji in 2013, et al., 2013.Aspeverin, a New Alkaloid from an Algicolous Strain of Aspergillus versicolor.Organic Letters10 (15), 2327 – 2329.) noval chemical compound, this chemical compound has brand-new framework types, present purposes only relates to and suppresses to swim vegeto-animal growth (Nai-Yun Ji, et al., 2013.Aspeverin, a New Alkaloid from an Algicolous Strain of Aspergillus versicolor.Organic Letters10 (15), 2327 – 2329.), belong to open first for the purposes of the Aspeverin that the present invention relates in preparation treatment ileocecum cancer drug, owing to belong to brand-new structure type, and its inhibition for the ileocecum cancerous cell is active unexpectedly strong, there is not the possibility that is provided any enlightenment by other chemical compounds, possess outstanding substantive distinguishing features, the control that is used for the ileocecum cancer simultaneously obviously has obvious improvement.
Summary of the invention
The objective of the invention is to provides the application of Aspeverin in the anti-ileocecum cancer drug of preparation according to not finding that it has the present situation of the report of anti-ileocecum cancer activity in the existing Aspeverin research.
Described compd A speverin structure is shown in formula I:
Formula I
The present invention finds that by external MTT anti-tumor activity evaluation the growth of the people's ileocecum of Aspeverin JEG-3 HCT-8 also has significant inhibitory effect, and the IC50 value that suppresses this 1 strain cell growth is respectively 0.97 ± 0.23 μ M.Therefore, Aspeverin can have the excellent development application prospect for the preparation of anti-ileocecum cancer drug.
Belong to open first for the purposes of the Aspeverin that the present invention relates in preparation treatment ileocecum cancer drug, because framework types belongs to brand-new framework types, and its inhibition for the ileocecum cancerous cell is active unexpectedly strong, there is not the possibility that is provided any enlightenment by other chemical compounds, possess outstanding substantive distinguishing features, the control that is used for the ileocecum cancer simultaneously obviously has obvious improvement.
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subjected to any restriction of specific embodiment, but limited by claim.
The specific embodiment
The preparation method of compd A speverin involved in the present invention is referring to document (Nai-Yun Ji, et al., 2013.Aspeverin, a New Alkaloid from an Algicolous Strain of Aspergillus versicolor.Organic Letters10 (15), 2327 – 2329.)
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subjected to any restriction of specific embodiment, but limited by claim.
Embodiment 1: the preparation of compd A speverin tablet involved in the present invention:
Get 20 and digest compound Aspeverin, add conventional adjuvant 180 grams of preparation tablet, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of compd A speverin capsule involved in the present invention:
Get 20 and digest compound Aspeverin, add conventional adjuvant such as starch 180 grams of preparation capsule, mixing is encapsulatedly made 1000.
Further specify its pharmaceutically active below by pharmacodynamic experiment.
Experimental example: adopt the growth inhibited effect of the people's ileocecum of mtt assay assessing compound Aspeverin JEG-3
1. method: the cell that is in the growth logarithmic (log) phase: people's ileocecum JEG-3 HCT-8(buys from Chinese Academy of Sciences's cell bank) with 1.5 * 10
4The concentration kind is in 96 orifice plates.Cell culture 24h inhales adherent back and goes original culture medium.Test is divided into blank group, drug treating group.Blank group is changed 1640 culture medium that contain 10% hyclone; It is 100 μ M that the replacing of drug treating group contains concentration, 50 μ M, 10 μ M, 1 μ M, 0.1 μ M, the culture medium of the Aspeverin of 0.01 μ M and 0.001 μ M.After cultivating 48h, the MTT that adds concentration 5mg/mL, continue to be put in the CO2 incubator and cultivate 4h, inhale along culture fluid top then and remove 100 μ L supernatants, add 100 μ L DMSO, 10min is placed in the dark place, utilizes microplate reader (Sunrise company product) to measure light absorption value (wavelength 570nm), and according to light absorption value calculating cell survival situation, 6 repeating holes are established in each processing.Cell survival rate (%)=Δ OD drug treating/Δ OD blank * 100.
2. the growth of the people's ileocecum of result: Aspeverin JEG-3 HCT-8 has significant inhibitory effect.The IC50 value that this chemical compound suppresses people's ileocecum JEG-3 HCT-8 growth is respectively 0.97 ± 0.23 μ M.
Shown that by above-described embodiment the growth of the people's ileocecum of Aspeverin of the present invention JEG-3 HCT-8 has the good restraining effect.Prove that thus Aspeverin of the present invention has anti-ileocecum cancer activity, can be for the preparation of anti-ileocecum cancer drug.
Claims (1)
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CN2013102173922A CN103251613A (en) | 2013-06-03 | 2013-06-03 | Application of Aspeverin in preparation of medicines for treating ileocecum cancer |
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CN2013102173922A CN103251613A (en) | 2013-06-03 | 2013-06-03 | Application of Aspeverin in preparation of medicines for treating ileocecum cancer |
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CN103251613A true CN103251613A (en) | 2013-08-21 |
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CN2013102173922A Pending CN103251613A (en) | 2013-06-03 | 2013-06-03 | Application of Aspeverin in preparation of medicines for treating ileocecum cancer |
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Application publication date: 20130821 |