CN103316012A - Application of Aspeverin in preparation of medicine for treating pancreas cancer - Google Patents
Application of Aspeverin in preparation of medicine for treating pancreas cancer Download PDFInfo
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- CN103316012A CN103316012A CN2013103045226A CN201310304522A CN103316012A CN 103316012 A CN103316012 A CN 103316012A CN 2013103045226 A CN2013103045226 A CN 2013103045226A CN 201310304522 A CN201310304522 A CN 201310304522A CN 103316012 A CN103316012 A CN 103316012A
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- aspeverin
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Abstract
The invention discloses an application of Aspeverin in the preparation of a medicine for treating pancreas cancer and belongs to the technical field of new application of medicines. It is found through in vitro MTT antineoplastic activity rating that Aspeverin also has a remarkable effect of inhibiting the growth of human pancreas cancer cell strains PANC-1 and BXPC-3. Thus, Aspeverin can be used in the preparation of medicines against pancreas cancer, and has a good development and application prospect. The application of Aspeverin in the preparation of a medicine for treating pancreas cancer is disclosed for the first time, and Aspeverin has unexpectedly strong inhibitory activity against pancreatic cancer cell.
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 cancer of pancreas medicine.
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., Aspeverin, a New Alkaloid from an Algicolous Strain of Aspergillus versicolor.Organic Letters, 2013,10 (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., Aspeverin, a New Alkaloid from an Algicolous Strain of Aspergillus versicolor.Organic Letters, 2013,10 (15), 2327 – 2329.), the purposes of the Aspeverin that the present invention relates in preparation treatment cancer of pancreas medicine belongs to open first.
Summary of the invention
The objective of the invention is to provides the application of Aspeverin in the anti-cancer of pancreas medicine of preparation according to not finding that it has the present situation of the report of anti-cancer of pancreas activity in the existing Aspeverin research.
Described compd A speverin, structure is shown in formula I:
The present invention finds by external MTT anti-tumor activity evaluation, the growth of the human pancreas cancer cell strain PANC-1 of Aspeverin and BXPC-3 also has significant inhibitory effect, and the IC50 value that suppresses this 2 strain cell growth is respectively 1.38 ± 0.39 μ M and 1.87 ± 0.26 μ M.Therefore, Aspeverin can have the excellent development application prospect for the preparation of anti-cancer of pancreas medicine.
Belong to open first for the purposes of the Aspeverin that the present invention relates in preparation treatment cancer of pancreas medicine, because framework types belongs to brand-new framework types, and its inhibition for pancreatic cancer 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 cancer of pancreas 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., Aspeverin, a New Alkaloid from an Algicolous Strain of Aspergillus versicolor.Organic Letters, 2013,10 (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 5 and digest compound Aspeverin, add dextrin 195 grams, mixing, conventional tabletting are made 1000.
Embodiment 2: the preparation of compd A speverin capsule involved in the present invention:
Get 5 and digest compound Aspeverin, add starch 195 grams, mixing is encapsulatedly made 1000.
Further specify its pharmaceutically active below by pharmacodynamic experiment.
Experimental example: adopt the growth inhibited effect of the human pancreas cancer cell strain of mtt assay assessing compound Aspeverin
1. method: the cell that is in the growth logarithmic (log) phase: human pancreas cancer cell strain PANC-1 and BXPC-3(buy 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, add the MTT of concentration 5mg/mL, continue to be put in CO
2Incubator is cultivated 4h, inhales along culture fluid top then and removes 100 μ L supernatants, adds 100 μ L DMSO, 10min is placed in the dark place, utilize microplate reader (Sunrise company product) to measure light absorption value (wavelength 570nm), and calculate the cell survival situation according to light absorption value, 6 repeating holes are established in each processing.Cell survival rate (%)=Δ OD drug treating/Δ OD blank * 100.
2. the growth of result: Aspeverin human pancreas cancer cell strain P PANC-1 and BXPC-3 has significant inhibitory effect.The IC50 value that this chemical compound suppresses human pancreas cancer cell strain PANC-1 and BXPC-3 growth is respectively 1.38 ± 0.39 μ M and 1.87 ± 0.26 μ M.
Shown that by above-described embodiment the growth of the human pancreas cancer cell strain PANC-1 of Aspeverin of the present invention and BXPC-3 has the good restraining effect.Prove that thus Aspeverin of the present invention has anti-cancer of pancreas activity, can be for the preparation of anti-cancer of pancreas medicine.
Claims (1)
1.Aspeverin the application in preparation treatment cancer of pancreas medicine, described compd A speverin structure is shown in formula I:
Formula I.
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| CN2013103045226A CN103316012A (en) | 2013-07-17 | 2013-07-17 | Application of Aspeverin in preparation of medicine for treating pancreas cancer |
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| CN103316012A true CN103316012A (en) | 2013-09-25 |
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| CN2013103045226A Pending CN103316012A (en) | 2013-07-17 | 2013-07-17 | Application of Aspeverin in preparation of medicine for treating pancreas cancer |
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN103285009A (en) * | 2013-06-03 | 2013-09-11 | 段仲达 | Application of Aspeverin in preparation of medicaments for treating pancreatic cancer |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN103285009A (en) * | 2013-06-03 | 2013-09-11 | 段仲达 | Application of Aspeverin in preparation of medicaments for treating pancreatic cancer |
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Application publication date: 20130925 |