CN103120680A - Application of Aphanamixoid A in medicine for treating nasopharyngeal carcinoma - Google Patents

Abstract

The invention discloses an application of Aphanamixoid A in preparing a medicine for treating nasopharyngeal carcinoma, and belongs to the technical field of new application of the medicine. The Aphanamixoid A has outstanding inhibiting effect on the growth of human nasopharyngeal carcinoma cell strains HNE1, HNE2, HONE1 and CNE1 through in-vitro MTT (Methyl Thiazolyl Tetrazolium) antineoplastic activity evaluation. Thus, the Aphanamixoid A can be used for preparing the medicine for resisting the nasopharyngeal carcinoma and has good development and application prospect; and the application of the Aphanamixoid A in preparation of the medicine for treating the nasopharyngeal carcinoma is firstly disclosed because a skeleton type belongs to a fire-new skeleton type and the inhibitory activity of the Aphanamixoid A on nasopharyngeal carcinoma cells is inconceivably high.

Description

The application of Aphanamixoid A in the treatment medicine for nasopharyngeal

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-medicine for nasopharyngeal 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 medicine for nasopharyngeal, because framework types belongs to brand-new framework types, and its inhibition for nasopharyngeal carcinoma 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 nasopharyngeal carcinoma 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-medicine for nasopharyngeal of preparation, and the structural formula of Aphanamixoid A is as shown in 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 nasopharyngeal carcinoma cell line HNE1, HNE2, HONE1 and CNE1, suppresses the IC of this 4 strain Growth of Cells ₅₀Value is respectively 0.11 ± 0.02 μ M, 0.49 ± 0.05 μ M, 0.23 ± 0.02 μ M and 0.41 ± 0.04 μ M.Therefore, Aphanamixoid A can for the preparation of anti-medicine for nasopharyngeal, have good development prospect.

Belong to open first for the purposes of the Aphanamixoid A that the present invention relates in preparation treatment medicine for nasopharyngeal, because framework types belongs to brand-new framework types, and its inhibition for nasopharyngeal carcinoma 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 nasopharyngeal carcinoma 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 nasopharyngeal carcinoma cell line

1. method: the cell that is in the growth logarithmic (log) phase: human nasopharyngeal carcinoma cell line HNE1, HNE2, HONE1 and CNE1(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 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 nasopharyngeal carcinoma cell line HNE1, HNE2, HONE1 and CNE1.This compound suppresses the IC of human nasopharyngeal carcinoma cell line HNE1, HNE2, HONE1 and CNE1 growth ₅₀Value is respectively: 0.11 ± 0.02 μ M, 0.49 ± 0.05 μ M, 0.23 ± 0.02 μ M and 0.41 ± 0.04 μ M.

Shown by above-described embodiment, Aphanamixoid A of the present invention has good inhibitory action to the growth of human nasopharyngeal carcinoma cell line HNE1, HNE2, HONE1 and CNE1.Prove thus, it is active that Aphanamixoid A of the present invention has anti-nasopharyngeal carcinoma, can be for the preparation of anti-medicine for nasopharyngeal.

Claims (1)

1.Aphanamixoid the application of A in the treatment medicine for nasopharyngeal, described compd A phanamixoid A structure is as shown in formula I:

Formula I.