CN103127074A - Application of Aphanamixoid A to ileocecum cancer treatment medicine - Google Patents

Application of Aphanamixoid A to ileocecum cancer treatment medicine Download PDF

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Publication number
CN103127074A
CN103127074A CN 201210412952 CN201210412952A CN103127074A CN 103127074 A CN103127074 A CN 103127074A CN 201210412952 CN201210412952 CN 201210412952 CN 201210412952 A CN201210412952 A CN 201210412952A CN 103127074 A CN103127074 A CN 103127074A
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aphanamixoid
application
ileocecum cancer
ileocecum
human
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周未末
冯怡
龚霞
吴俊华
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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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Abstract

The invention discloses application of Aphanamixoid A to preparation of human ileocecum cancer treatment medicine and belongs to the technical field of novel application of medicine. In-vitro MTT antineoplastic activity evaluation shows that the Aphanamixoid A has the significant effect of inhibiting human ileocecum cancer cell lines HCT-8 from growing. Therefore, the Aphanamixoid A can be used for preparing the ileocecum cancer resistance medicine and has good development and application prospects. The application of the Aphanamixoid A to preparation of the human ileocecum cancer treatment medicine is made public for the first time, the skeleton type is fully novel, and inhibitory activity on the human ileocecum cancer cells is surprisingly strong.

Description

The application of Aphanamixoid A in treatment ileocecum cancer drug
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 anti-ileocecum cancer drug of preparation.
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 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 compounds, possesses outstanding substantive distinguishing features, the control that is used for simultaneously the ileocecum 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 the anti-ileocecum cancer drug of preparation, and the structural formula of Aphanamixoid A is as shown in formula I:
Figure BDA0000230862621
The present invention finds by external MTT anti-tumor activity evaluation, and Aphanamixoid A also has significant inhibitory action to the growth of human ileocecal carcinoma cell strain HCT-8, suppresses the IC of this 1 strain Growth of Cells 50Value is respectively 0.83 ± 0.10 μ M.Therefore, Aphanamixoid A can for the preparation of anti-ileocecum cancer drug, have good development prospect.
The purposes of the Aphanamixoid A that the present invention relates in preparation treatment ileocecum cancer drug belongs to open first, 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 compounds, possess outstanding substantive distinguishing features, the control that is used for simultaneously the ileocecum 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 ileocecal carcinoma cell strain
1. method: the cell that is in the growth logarithmic (log) phase: human ileocecal carcinoma cell strain HCT-8(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 ileocecal carcinoma cell strain HCT-8.This compound suppresses the IC of human ileocecal carcinoma cell strain HCT-8 growth 50Value is respectively: 0.83 ± 0.10 μ M.
Shown by above-described embodiment, Aphanamixoid A of the present invention has good inhibitory action to the growth of human ileocecal carcinoma cell strain HCT-8.Prove thus, it is active that Aphanamixoid A of the present invention has anti-ileocecum cancer, can be for the preparation of anti-ileocecum cancer drug.

Claims (1)

1.Aphanamixoid the application of A in treatment ileocecum cancer drug, described compd A phanamixoid A structure is as shown in formula I:
Figure DEST_PATH_IMAGE001
Formula I.
CN 201210412952 2012-10-25 2012-10-25 Application of Aphanamixoid A to ileocecum cancer treatment medicine Withdrawn CN103127074A (en)

Priority Applications (1)

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CN 201210412952 CN103127074A (en) 2012-10-25 2012-10-25 Application of Aphanamixoid A to ileocecum cancer treatment medicine

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Application Number Priority Date Filing Date Title
CN 201210412952 CN103127074A (en) 2012-10-25 2012-10-25 Application of Aphanamixoid A to ileocecum cancer treatment medicine

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CN103127074A true CN103127074A (en) 2013-06-05

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CN 201210412952 Withdrawn CN103127074A (en) 2012-10-25 2012-10-25 Application of Aphanamixoid A to ileocecum cancer treatment medicine

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CN (1) CN103127074A (en)

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Application publication date: 20130605