CN102872010B - Application of Aphanamixoid A in drugs for treating ovarian cancer - Google Patents

Application of Aphanamixoid A in drugs for treating ovarian cancer Download PDF

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CN102872010B
CN102872010B CN201210414051.XA CN201210414051A CN102872010B CN 102872010 B CN102872010 B CN 102872010B CN 201210414051 A CN201210414051 A CN 201210414051A CN 102872010 B CN102872010 B CN 102872010B
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aphanamixoid
ovarian cancer
drugs
application
preparing
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CN102872010A (en
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冯怡
龚霞
吴俊华
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Rudong Wenyuan Investment And Development Co Ltd
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Nanjing University
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Abstract

The invention discloses an application of Aphanamixoid A in preparing drugs for treating ovarian cancer and belongs to the technical field of new uses of the drugs. Discovered by extracorporeal methyl thiazolyl tetrazolium (MTT) antineoplastic activity evaluation, the Aphanamixoid A disclosed by the invention is also remarkable in action of inhibiting the growth of human ovarian cancer cell strains HO-8910, HOC1 and OVAC. Therefore, the Aphanamixoid A can be used for preparing the drugs for resisting the ovarian cancer, and is good in development and application prospect. The application of the Aphanamixoid A in preparing the drugs for treating the ovarian cancer is disclosed for the first time. The skeleton type of the Aphanamixoid A is fire-new, and moreover, how high the activity of inhibiting human ovarian cancer cells is unexpected.

Description

The application of Aphanamixoid A in treatment ovarian 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 preparing ovarian cancer resistance medicament.
Technical background
Cancer is to one of disease of human life's health hazard maximum, has a large amount of people to die from cancer every year.The research and development of cancer therapy drug are the focuses of study of pharmacy always.In antitumor drug, have 74% to be natural product or derivatives thereof, if paclitaxel and derivant thereof are exactly the reasonable antitumor drug of effect clinically at present.Therefore, from natural product, find anticancer compound or lead compound has great importance.
The compd A phanamixoid A the present invention relates to is one and within 2012, delivers (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.) New skeleton compound, this compound has brand-new framework types, current 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.), purposes for the Aphanamixoid A the present invention relates in preparation treatment ovarian cancer medicine belongs to open first, because framework types belongs to brand-new framework types, and its inhibition for ovarian cancer cell is active unexpectedly strong, there is not the possibility that is provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, control for ovarian cancer simultaneously obviously has significant progress.
Summary of the invention
The invention provides the application of compd A phanamixoid A in preparing antitumor drug.
The present invention adopts following technical scheme: the application of Aphanamixoid A in preparing ovarian cancer resistance medicament, and the structural formula of Aphanamixoid A is as shown in formula I:
Figure BDA0000230750971
The present invention finds by the evaluation of external MTT anti-tumor activity, and Aphanamixoid A also has significant inhibitory action to the growth of human oophoroma cell line HO-8910, HOC1 and OVAC, suppresses the IC of this 3 strain Growth of Cells 50value is respectively 0.25 ± 0.07 μ M, 0.33 ± 0.07 μ M and 0.11 ± 0.06 μ M.Therefore, Aphanamixoid A can, for the preparation of ovarian cancer resistance medicament, have good development prospect.
The purposes of the Aphanamixoid A the present invention relates in preparation treatment ovarian cancer medicine belongs to open first, because framework types belongs to brand-new framework types, and its inhibition for ovarian 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 for ovarian cancer simultaneously obviously has significant progress.
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subject to any restriction of specific embodiment, but be 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 subject to any restriction of specific embodiment, but be 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 180 grams of conventional adjuvants preparing tablet, mix, conventional tablet machine is 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 of preparing capsule as 180 grams of starch, mix, encapsulatedly make 1000.
Below by pharmacodynamic experiment, further illustrate its pharmaceutically active.
Experimental example: adopt the growth inhibited effect of mtt assay assessing compound Aphanamixoid A to human oophoroma cell line
1. method: the cell in growth logarithmic (log) phase: human oophoroma cell line HO-8910, HOC1 and OVAC(buy from Chinese Academy of Sciences's cell bank) with 1.5 * 10 4concentration kind is in 96 orifice plates.After cell culture 24 h are adherent, suck original culture medium.Test is divided into blank group, drug treating group.Blank group is changed 1640 culture medium containing 10% hyclone; It is 100 μ M that drug treating group is changed containing 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.Cultivate after 48 h, add the MTT of concentration 5mg/mL, continue to be put in CO 2incubator is cultivated 4 h, then along culture fluid top, suck 100 μ L supernatants, add 100 μ L DMSO, 10 min are placed in dark place, utilize microplate reader (Sunrise company product) to measure light absorption value (wavelength 570nm), and calculating 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 oophoroma cell line HO-8910, HOC1 and OVAC.This compound suppresses the IC of human oophoroma cell line HO-8910, HOC1 and OVAC growth 50value is respectively: 0.25 ± 0.07 μ M, 0.33 ± 0.07 μ M and 0.11 ± 0.06 μ M.
By above-described embodiment, shown, Aphanamixoid A of the present invention has good inhibitory action to the growth of human oophoroma cell line HO-8910, HOC1 and OVAC.Prove thus, Aphanamixoid A of the present invention has ovarian cancer resistance activity, can be for the preparation of ovarian cancer resistance medicament.

Claims (1)

  1. The application of 1.Aphanamixoid A in preparation treatment ovarian cancer medicine, described compd A phanamixoid A structure is as shown in formula I:
    Figure 787727DEST_PATH_IMAGE001
    Formula I.
CN201210414051.XA 2012-10-25 2012-10-25 Application of Aphanamixoid A in drugs for treating ovarian cancer Active CN102872010B (en)

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Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1580043A (en) * 2003-08-04 2005-02-16 财团法人佛教慈济综合医院 Anti malignant tumour southern radix bupleuri extract preparing method
CN101978959A (en) * 2010-10-18 2011-02-23 天津尚德药缘科技有限公司 Application of sphaelactone and derivative thereof to treatment of cancers

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1580043A (en) * 2003-08-04 2005-02-16 财团法人佛教慈济综合医院 Anti malignant tumour southern radix bupleuri extract preparing method
CN101978959A (en) * 2010-10-18 2011-02-23 天津尚德药缘科技有限公司 Application of sphaelactone and derivative thereof to treatment of cancers

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Aphanamixoid A, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya;Jie-Yun Cai, et al.;《ORGANIC LETTERS》;20120427;第14卷(第10期);2524–2527 *
Jie-YunCai et al..Aphanamixoid A

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