Technical background
Cancer is to one of maximum disease of human life's health hazard, 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.74% is had to be natural product or derivatives thereof in antitumor drug, if paclitaxel and derivant thereof are exactly the current reasonable antitumor drug of effect clinically.Therefore, from natural product, anticancer compound is found or lead compound has great importance.
The compound L ycojaponicumin B that the present invention relates to is one and delivers (Wang in 2012, X.J.et al., 2012.Lycojaponicumins A-C, Three Alkaloids with an UnprecedentedSkeleton from Lycopodium japonicum.Organic Letters 14 (10), New skeleton compound 2614-2617.), this compound has brand-new framework types, the purposes in preparation treatment laryngeal carcinoma medicine that the present invention relates to is belonged to first public, and belong to brand-new framework types due to framework types, there is not the possibility being provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, control simultaneously for laryngeal carcinoma obviously has significant progress.
Summary of the invention
The invention provides compound L ycojaponicumin B and prepare the application in 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 Lycojaponicumin B is as shown in formula I:
Formula I
The present invention is found by external MTT antineoplastic activity evaluation, and the growth of Lycojaponicumin B to the strain of people's laryngeal cancer cell HEP-2, TU 686, M2e and M4e also has significant inhibitory action, suppresses the IC of this 4 strain Growth of Cells
50value is respectively 1.52 ± 0.17 μMs, 1.25 ± 0.29 μMs, 2.38 ± 0.22 μMs and 3.19 ± 0.36 μMs.Therefore, Lycojaponicumin B for the preparation of anti-laryngeal carcinoma medicine, can have good development prospect.
The purposes of the Lycojaponicumin B that the present invention relates in preparation treatment tongue cancer drug belongs to first public, because framework types belongs to brand-new framework types, and its inhibit activities for Human Tongue Carcinoma Lines is unexpectedly strong, there is not the possibility being provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, the control simultaneously for carcinoma of tongue obviously has significant progress.
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not by any restriction of specific embodiment, but be limited by claim.
Detailed description of the invention
The preparation method of compound L ycojaponicumin B involved in the present invention is see document (Wang, X.J.et al., 2012.Lycojaponicumins A-C, Three Alkaloids with an Unprecedented Skeleton from Lycopodiumjaponicum.Organic Letters 14 (10), 2614-2617.).
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not by 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 g of compound Lycojaponicumin B, add the customary adjuvant 180 grams preparing tablet, mixing, conventional tablet presses makes 1000.
Embodiment 2: the preparation of compound L ycojaponicumin B capsule involved in the present invention:
Get 20 g of compound Lycojaponicumin B, add prepare capsule customary adjuvant as starch 180 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Experimental example: adopt mtt assay assessing compound Lycojaponicumin B to the growth inhibited effect of people's laryngeal cancer cell strain
1. method: the cell being in growth logarithmic (log) phase: the strain of people's laryngeal cancer cell HEP-2, TU 686, M2e and M4e (buying from Chinese Academy of Sciences's cell bank) are with 1.5 × 10
4concentration kind is in 96 orifice plates.Original culture medium is sucked after cell culture 24h is adherent.Test is divided into blank group, drug treating group.Blank group changes 1640 culture medium containing 10% hyclone; It is 100 μMs that drug treating group is changed containing concentration, 50 μMs, 10 μMs, 1 μM, 0.1 μM, the culture medium of the Lycojaponicumin B of 0.01 μM and 0.001 μM.After cultivating 48h, add the MTT of concentration 5mg/mL, continue to be put in CO
2incubator cultivates 4h, then 100 μ L supernatants are sucked along culture fluid top, add 100 μ L DMSO, 10min is placed in dark place, microplate reader (Sunrise Products) is utilized to measure light absorption value (wavelength 570nm), and calculating cell survival according to light absorption value, 6 repeating holes are established in each process.Cell survival rate (%)=Δ OD
drug treating/ Δ OD
blank× 100.
2. result: the growth of Lycojaponicumin B to the strain of people's laryngeal cancer cell HEP-2, TU 686, M2e and M4e has significant inhibitory action.This compound suppresses the IC of the strain of people's laryngeal cancer cell HEP-2, TU 686, M2e and M4e growth
50value is respectively: 1.52 ± 0.17 μMs, 1.25 ± 0.29 μMs, 2.38 ± 0.22 μMs and 3.19 ± 0.36 μMs.
Shown by above-described embodiment, the growth of Lycojaponicumin B of the present invention to the strain of people's laryngeal cancer cell HEP-2, TU 686, M2e and M4e has good inhibitory action.Prove thus, it is active that Lycojaponicumin B of the present invention has anti-laryngeal carcinoma, can for the preparation of anti-laryngeal carcinoma medicine.