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.In antitumor drug, have 74% to be the natural product or derivatives thereof, as paclitaxel and derivant thereof are exactly the reasonable antitumor drug of effect clinically at present.Therefore, from natural product, searching anticancer compound or lead compound have great importance.
The compound L ycojaponicumin B the present invention relates to is one and within 2012, delivers (Wang, X.J.et al., 2012.Lycojaponicumins A-C, Three Alkaloids with an Unprecedented Skeleton fromLycopodium japonicum.Organic Letters14 (10), 2614-2617.) New skeleton compound, this compound has brand-new framework types, belong to open first for the purposes in preparation treatment laryngeal carcinoma medicine the present invention relates to, and because framework types belongs to brand-new framework types, there do not is the possibility that is provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, control for laryngeal carcinoma simultaneously obviously has significant progress.
Summary of the invention
The invention provides the application of compound L ycojaponicumin B in preparing antitumor drug.
The present invention adopts following technical scheme: the application of Lycojaponicumin B in the anti-laryngeal carcinoma medicine of preparation, and the structural formula of LycojaponicuminB is as shown in formula I:
The present invention finds by external MTT anti-tumor activity evaluation, and Lycojaponicumin B also has significant inhibitory action to the growth of people's laryngeal cancer cell strain HEP-2, TU686, M2e and M4e, suppresses the IC of this 4 strain Growth of Cells
50value is respectively 1.52 ± 0.17 μ M, 1.25 ± 0.29 μ M, 2.38 ± 0.22 μ M and 3.19 ± 0.36 μ M.Therefore, Lycojaponicumin B can, for the preparation of anti-laryngeal carcinoma medicine, have good development prospect.
The purposes of the Lycojaponicumin B the present invention relates in preparation treatment carcinoma of tongue medicine belongs to open first, because framework types belongs to brand-new framework types, and its inhibition for Human Tongue Carcinoma Lines is active unexpectedly strong, there do not is the possibility that is provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, the control for carcinoma of tongue 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 compound L ycojaponicumin B involved in the present invention is referring to document (Wang, X.J.et al., 2012.Lycojaponicumins A-C, Three Alkaloids with an Unprecedented Skeleton from Lycopodium japonicum.Organic Letters14 (10), 2614-2617.).
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 compound L ycojaponicumin B tablet involved in the present invention:
Get 20 and digest compound Lycojaponicumin B, add conventional adjuvant 180 grams that prepare tablet, mix, conventional tablet machine is made 1000.
Embodiment 2: the preparation of compound L ycojaponicumin B capsule involved in the present invention:
Get 20 and digest compound Lycojaponicumin B, add the conventional adjuvant for preparing capsule as starch 180 grams, mix, encapsulatedly make 1000.
Further illustrate its pharmaceutically active below by pharmacodynamic experiment.
Experimental example: adopt the growth inhibited effect of mtt assay assessing compound Lycojaponicumin B to the strain of people's laryngeal cancer cell
1. method: in the cell of growth logarithmic (log) phase: people's laryngeal cancer cell strain HEP-2, TU686, M2e and M4e(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 24h is adherent.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 the 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 Lycojaponicumin B of 0.01 μ M and 0.001 μ M.After cultivating 48h, add the MTT of concentration 5mg/mL, continue to be put in CO
2incubator is cultivated 4h, then suck 100 μ L supernatants along culture fluid top, add 100 μ L DMSO, 10min is placed in 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: Lycojaponicumin B has significant inhibitory action to the growth of people's laryngeal cancer cell strain HEP-2, TU686, M2e and M4e.This compound suppresses the IC of people's laryngeal cancer cell strain HEP-2, TU686, M2e and M4e growth
50value is respectively: 1.52 ± 0.17 μ M, 1.25 ± 0.29 μ M, 2.38 ± 0.22 μ M and 3.19 ± 0.36 μ M.
By above-described embodiment, shown, Lycojaponicumin B of the present invention has good inhibitory action to the growth of people's laryngeal cancer cell strain HEP-2, TU686, M2e and M4e.Prove thus, Lycojaponicumin B of the present invention has anti-laryngeal carcinoma activity, can be for the preparation of anti-laryngeal carcinoma medicine.