CN102885809B - Application of Aphanamixoid A in preparing medicament for treating pancreatic cancer - Google Patents

Abstract

The invention discloses application of Aphanamixoid A in preparation of a medicament for treating pancreatic cancer and belongs to the technical field of new application of medicaments. In-vitro methyl thiazolyl tetrazolium (MTT) anti-tumor activity evaluation shows that the Aphanamixoid A has a remarkable inhibiting effect on growth of human pancreatic cancer cell lines PANC-1 and BXPC-3. Therefore, the Aphanamixoid A can be used for preparing the pancreatic cancer resistant medicament, and has a good development and application prospect. The Aphanamixoid A in preparation of the medicament for treating the pancreatic cancer is disclosed for the first time, the skeleton type is a brand-new skeleton type, and the Aphanamixoid A has unexpected strong inhibiting activity on pancreatic cancer cells.

Description

Application of Aphanamixoid A in the preparation of drugs for treating pancreatic cancer

technical field

The present invention relates to a new application of compound Aphanamixoid A, in particular to the application of Aphanamixoid A in the preparation of anti-pancreatic cancer drugs. the

technical background

Cancer is one of the most harmful diseases to human life and health, and a large number of people die of cancer every year. The research and development of anticancer drugs has always been a hot spot in pharmaceutical research. 74% of anti-tumor drugs are natural products or their derivatives, such as paclitaxel and its derivatives are anti-tumor drugs with better clinical application effect at present. Therefore, it is of great significance to search for anticancer compounds or lead compounds from natural products. the

The compound Aphanamixoid A involved in the present invention is a published in 2012 (Cai, J. Y. et al., 2012. Aphanamixoid A, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 252 –2527.), a new skeleton compound, which has a new skeleton type, and its current use only involves 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.), the use of Aphanamixoid A involved in the present invention in the preparation of drugs for the treatment of pancreatic cancer is the first disclosure, because the skeleton type belongs to a new skeleton type, and it is for The inhibitory activity of pancreatic cancer cells is unexpectedly strong, there is no possibility of giving any inspiration from other compounds, it has outstanding substantive features, and it is obviously a significant progress in the prevention and treatment of pancreatic cancer. the

Contents of the invention

The invention provides the application of compound Aphanamixoid A in the preparation of antitumor drugs. the

The present invention adopts the following technical scheme: the application of Aphanamixoid A in the preparation of anti-pancreatic cancer drugs, the structural formula of Aphanamixoid A is shown in formula (I):

In the present invention, through MTT anti-tumor activity evaluation in vitro, it is found that Aphanamixoid A also has a significant inhibitory effect on the growth of human pancreatic cancer cell lines PANC-1 and BXPC-3, and the IC ₅₀ values for inhibiting the growth of these two cell lines are 0.24±0.03 respectively μM and 0.22±0.04 μM. Therefore, Aphanamixoid A can be used to prepare anti-pancreatic cancer drugs, and has good development and application prospects.

The use of Aphanamixoid A involved in the present invention in the preparation of drugs for the treatment of pancreatic cancer is disclosed for the first time. Since the skeleton type belongs to a new skeleton type, and its inhibitory activity against pancreatic cancer cells is unexpectedly strong, there is no evidence given by other compounds. The possibility of enlightenment has outstanding substantive features, and at the same time, it is obviously a significant progress in the prevention and treatment of pancreatic cancer. the

The present invention will be described in further detail below through examples, but the protection scope of the present invention is not limited by any specific examples, but is defined by the claims. the

Detailed ways

The preparation method of the compound Aphanamixoid A involved in the present invention can be found in literature (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

Below by embodiment the present invention is described in further detail, but protection scope of the present invention is not subject to any restriction of specific embodiment, but is defined by claims. the

Embodiment 1: the preparation of compound Aphanamixoid A tablet involved in the present invention:

Get 20 grams of compound Aphanamixoid A, add 180 grams of conventional excipients for tablet preparation, mix well, and make 1000 tablets with a conventional tabletting machine. the

Embodiment 2: the preparation of compound Aphanamixoid A capsule involved in the present invention:

Get 20 grams of compound Aphanamixoid A, add conventional adjuvants such as starch 180 grams for the preparation of capsules, mix well, and pack into capsules to make 1000 tablets. the

The following pharmacodynamic experiments will further illustrate its drug activity. the

Experimental example: MTT method was used to evaluate the growth inhibitory effect of compound Aphanamixoid A on human pancreatic cancer cell lines

1. Methods: Cells in the logarithmic phase of growth: human pancreatic cancer cell lines PANC-1 and BXPC-3 (purchased from the Cell Bank of the Chinese Academy of Sciences) were seeded in 96-well plates at a concentration of 1.5×10 ⁴ . After 24 h of cell culture, the original medium was aspirated. The experiment was divided into blank control group and drug treatment group. The blank group was replaced with 1640 medium containing 10% fetal bovine serum; the drug-treated group was replaced with the medium containing Aphanamixoid A at concentrations of 100 μM, 50 μM, 10 μM, 1 μM, 0.1 μM, 0.01 μM and 0.001 μM. After culturing for 48 h, add MTT at a concentration of 5 mg/mL, continue to culture in a CO ₂ incubator for 4 h, then suck 100 μL of supernatant along the upper part of the culture solution, add 100 μL of DMSO, place in the dark for 10 min, use A microplate reader (product of Sunrise Company) was used to measure the absorbance (wavelength 570nm), and the cell survival was calculated according to the absorbance, and 6 replicate wells were set for each treatment. Cell survival rate (%)=ΔOD _{drug treatment} /ΔOD _{blank control} ×100.

2. Results: Aphanamixoid A significantly inhibited the growth of human pancreatic cancer cell lines PANC-1 and BXPC-3. The compound inhibits the growth of human pancreatic cancer cell lines PANC-1 and BXPC-3 with IC ₅₀ values of 0.24±0.03μM and 0.22±0.04μM, respectively.

The above examples show that Aphanamixoid A of the present invention has a good inhibitory effect on the growth of human pancreatic cancer cell lines PANC-1 and BXPC-3. This proves that the Aphanamixoid A of the present invention has anti-pancreatic cancer activity and can be used to prepare anti-pancreatic cancer drugs. the

Claims (1)

1. The application of 1.Aphanamixoid A in preparation treatment cancer of pancreas medicine, described compd A phanamixoid A structure is as shown in formula I:

   

   Formula I.