CN103120665A - Application of Aphanamixoid A in medicine for treating prostatic cancer - Google Patents

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

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Publication number
CN103120665A
CN103120665A CN2012104128683A CN201210412868A CN103120665A CN 103120665 A CN103120665 A CN 103120665A CN 2012104128683 A CN2012104128683 A CN 2012104128683A CN 201210412868 A CN201210412868 A CN 201210412868A CN 103120665 A CN103120665 A CN 103120665A
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aphanamixoid
medicine
prostatic cancer
application
preparation
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李丽丽
龚霞
冯怡
吴俊华
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吴俊华
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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

The invention discloses an application of Aphanamixoid A in preparation of a medicine for treating prostatic cancer, and belongs to the technical field of new application of the medicine. The Aphanamixoid A has outstanding inhibiting effect on the growth of human prostatic cancer cell strains ALVA, gpc-1, 9L-B and Du145 through in-vitro MTT (Methyl Thiazolyl Tetrazolium) antineoplastic activity evaluation. Thus, the Aphanamixoid A can be used for preparing the medicine for resisting the prostatic cancer and has good development and application prospect; and the application of the Aphanamixoid A in preparation of the medicine for treating the prostatic cancer is firstly disclosed because a skeleton type belongs to a fire-new skeleton type and the inhibitory activity of the Aphanamixoid A on prostatic cancer cells is inconceivably high.

Description

The application of Aphanamixoid A in treatment carcinoma of prostate 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 the preparation antiprostate cancer.
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 carcinoma of prostate medicine, because framework types belongs to brand-new framework types, and its inhibition for prostate gland cancer cell 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 carcinoma of prostate 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 the preparation antiprostate cancer, and the structural formula of Aphanamixoid A is as shown in formula I:
Figure BDA0000230869671
Formula I
The present invention finds by external MTT anti-tumor activity evaluation, and Aphanamixoid A also has significant inhibitory action to the growth of human prostate cancer cell line ALVA, gpc-1,9L-B and Du145, suppresses the IC of this 4 strain Growth of Cells 50Value is respectively 0.39 ± 0.03 μ M, 0.15 ± 0.06 μ M, 0.13 ± 0.05 μ M and 0.14 ± 0.06 μ M.Therefore, Aphanamixoid A can for the preparation of antiprostate cancer, have good development prospect.
The purposes of the Aphanamixoid A that the present invention relates in preparation treatment carcinoma of prostate medicine belongs to open first, because framework types belongs to brand-new framework types, and its inhibition for prostate gland cancer cell 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 carcinoma of prostate 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 prostate cancer cell line
1. method: the cell that is in the growth logarithmic (log) phase: human prostate cancer cell line ALVA, gpc-1,9L-B and Du145(buy 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, the culture medium of the Aphanamixoid A of 0.01 μ M and 0.001 μ M.After cultivating 48 h, add the MTT of concentration 5 mg/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 570 nm), 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 prostate cancer cell line ALVA, gpc-1,9L-B and Du145.This compound suppresses the IC of human prostate cancer cell line ALVA, gpc-1,9L-B and Du145 growth 50Value is respectively: 0.39 ± 0.03 μ M, 0.15 ± 0.06 μ M, 0.13 ± 0.05 μ M and 0.14 ± 0.06 μ M.
Shown by above-described embodiment, Aphanamixoid A of the present invention has good inhibitory action to the growth of human prostate cancer cell line ALVA, gpc-1,9L-B and Du145.Prove thus, Aphanamixoid A of the present invention has the anti-prostate cancer activity, can be for the preparation of antiprostate cancer.

Claims (1)

1.Aphanamixoid the application of A in treatment carcinoma of prostate medicine, described compd A phanamixoid A structure is as shown in formula I:
Figure 523443DEST_PATH_IMAGE001
Formula I.
CN2012104128683A 2012-10-25 2012-10-25 Application of Aphanamixoid A in medicine for treating prostatic cancer Pending CN103120665A (en)

Priority Applications (1)

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Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102115483A (en) * 2009-12-30 2011-07-06 苏州天人合生物技术有限公司 Halogenated dideoxy sugar derivative, preparation method and application thereof

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102115483A (en) * 2009-12-30 2011-07-06 苏州天人合生物技术有限公司 Halogenated dideoxy sugar derivative, preparation method and application thereof

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