CN103120682A - Application of Aphanamixoid A in medicine for treating bladder cancer - Google Patents

Application of Aphanamixoid A in medicine for treating bladder cancer Download PDF

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Publication number
CN103120682A
CN103120682A CN2012104137729A CN201210413772A CN103120682A CN 103120682 A CN103120682 A CN 103120682A CN 2012104137729 A CN2012104137729 A CN 2012104137729A CN 201210413772 A CN201210413772 A CN 201210413772A CN 103120682 A CN103120682 A CN 103120682A
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aphanamixoid
bladder cancer
medicine
application
preparing
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黄蓉
冯怡
龚霞
吴俊华
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吴俊华
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Abstract

The invention discloses an application of Aphanamixoid A in preparing a medicine for treating bladder cancer, and belongs to the technical field of new application of the medicine. The Aphanamixoid A has outstanding inhibiting effect on the growth of a human bladder cancer cell strain T-24 through in-vitro MTT (Methyl Thiazolyl Tetrazolium) antineoplastic activity evaluation. Thus, the Aphanamixoid A can be used for preparing the medicine for resisting the bladder cancer and has good development and application prospect; and the application of the Aphanamixoid A in preparing the medicine for treating the bladder cancer is firstly disclosed because a skeleton type belongs to a fire-new skeleton type and the inhibitory activity of the Aphanamixoid A on bladder cancer cells is inconceivably high.

Description

The application of Aphanamixoid A in treatment bladder cancer medicine
Technical field
The present invention relates to the new purposes of compd A phanamixoid A, relate in particular to the application of Aphanamixoid A in preparation anti-bladder cancer medicine.
Technical background
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 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 phanamixoid A that the present invention relates to is one and delivered (Cai in 2012, J. Y. et al., 2012. Aphanamixoid A, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 2524 – 2527.) New skeleton compound, this compound has brand-new framework types, present purposes only relates to insect antifeedant activity (Cai, J. Y. et al., 2012. Aphanamixoid A, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 2524 – 2527.), belong to open first for the purposes of the Aphanamixoid A that the present invention relates in preparation treatment bladder cancer medicine, because framework types belongs to brand-new framework types, and its inhibition for transitional cell bladder carcinoma cell line is active unexpectedly strong, there is not the possibility that is provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, the control that is used for simultaneously bladder cancer obviously has significant progress.
Summary of the invention
The invention provides the application of compd A phanamixoid A in the preparation antitumor drug.
The present invention adopts following technical scheme: the application of Aphanamixoid A in preparation anti-bladder cancer medicine, and the structural formula of Aphanamixoid A is as shown in formula I:
Figure BDA0000230859641
The present invention finds by external MTT anti-tumor activity evaluation, and Aphanamixoid A also has significant inhibitory action to the growth of human bladder cancer cell's strain T-24, suppresses the IC of this 1 strain Growth of Cells 50Value is respectively 0.11 ± 0.02 μ M.Therefore, Aphanamixoid A can for the preparation of the anti-bladder cancer medicine, have good development prospect.
The purposes of the Aphanamixoid A that the present invention relates in preparation treatment bladder cancer medicine belongs to open first, because framework types belongs to brand-new framework types, and its inhibition for transitional cell bladder carcinoma cell line is active unexpectedly strong, there is not the possibility that is provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, the control that is used for simultaneously bladder cancer obviously has significant progress.
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 phanamixoid A involved in the present invention is referring to document (Cai, J. Y. et al., 2012. Aphanamixoid A, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 2524 – 2527.).
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 phanamixoid A tablet involved in the present invention:
Get 20 and digest compound Aphanamixoid A, add conventional adjuvant 180 grams that prepare tablet, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of compd A phanamixoid A capsule involved in the present invention:
Get 20 and digest compound Aphanamixoid A, add the conventional adjuvant such as starch 180 grams that prepare capsule, mixing is encapsulatedly made 1000.
Further illustrate its pharmaceutically active below by pharmacodynamic experiment.
Experimental example: adopt mtt assay assessing compound Aphanamixoid A to the growth inhibited effect of human bladder cancer cell's strain
1. method: the cell that is in the growth logarithmic (log) phase: human bladder cancer cell's strain T-24(buys from Chinese Academy of Sciences's cell bank) with 1.5 * 10 4The concentration kind is in 96 orifice plates.Suck original culture medium after cell culture 24 h are adherent.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, 0.01 μ M, 0.001 μ M, the culture medium of the Aphanamixoid A of 0.0001 μ M and 0.00001 μ M.After cultivating 48 h, add the MTT of concentration 5mg/mL, continue to be put in CO 2Incubator is cultivated 4 h, then suck 100 μ L supernatants along culture fluid top, add 100 μ L DMSO, 10 min are placed in the dark place, utilize microplate reader (Sunrise company product) to measure light absorption value (wavelength 570nm), and calculating 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. result: Aphanamixoid A has significant inhibitory action to the growth of human bladder cancer cell's strain T-24.This compound suppresses the IC of human bladder cancer cell's strain T-24 growth 50Value is: 0.11 ± 0.02 μ M.
Shown by above-described embodiment, Aphanamixoid A of the present invention has good inhibitory action to the growth of human bladder cancer cell's strain T-24.Prove thus, Aphanamixoid A of the present invention has the anti-bladder cancer activity, can be for the preparation of the anti-bladder cancer medicine.

Claims (1)

1.Aphanamixoid the application of A in treatment bladder cancer medicine, described compd A phanamixoid A structure is as shown in formula I:
Figure 2012104137729100001DEST_PATH_IMAGE001
Formula I.
CN2012104137729A 2012-10-25 2012-10-25 Application of Aphanamixoid A in medicine for treating bladder cancer Pending CN103120682A (en)

Priority Applications (1)

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Application Number Priority Date Filing Date Title
CN2012104137729A CN103120682A (en) 2012-10-25 2012-10-25 Application of Aphanamixoid A in medicine for treating bladder cancer

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CN103120682A true CN103120682A (en) 2013-05-29

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CN (1) CN103120682A (en)

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
CAI, J. Y. ET AL: "Aphanamixoid A, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya", 《ORGANIC LETTERS》 *
夏菠等: "类柠檬苦素的生物活性研究进展", 《农业品加工 学刊》 *

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Application publication date: 20130529