Thymol derivative and its preparation method and application
A drug and compound technology, applied in the field of thymol derivatives and their preparation, can solve the problems of undiscovered pharmacologically active ingredients and in-depth research on chemical ingredients, and achieve the goal of simple and easy-to-operate preparation methods, low toxicity, and strong inhibitory effect Effect
- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
Method used
Image
Examples
preparation example Construction
[0038] Each step of the preparation method of the present invention can be further improved, for example:
[0039] In yet another specific embodiment of the present invention, in the step S1,
[0040] The solvent used in the extraction and the ratio of solid to liquid all have an impact on the impurity content of the crude extract and the extraction rate of active ingredients. The solvent is preferably 90-95% ethanol solution, more preferably 95% ethanol solution. The solid-liquid ratio of Perrin and ethanol is 1kg: 3-7L (preferably 1kg: 5L). The above extraction conditions can reduce the impurity content in the crude extract, thereby effectively improving the extraction rate of thymol derivatives.
[0041] It is further preferred to heat and reflux for extraction twice, each time for 2 hours.
[0042] In yet another specific embodiment of the present invention, in the step S2,
[0043] Use diatomite to adsorb the extract dissolved in methanol; use diatomite for better ads...
Embodiment 1
[0064] Embodiment 1: extraction and separation experiment
[0065] a. The Peilan sample was collected from Siyang County, Jiangsu Province in April 2017. After crushing 20 kg of dried stems and leaves of the whole peylan grass, add 100 L of 95% ethanol to soak for 2 hours, heat and reflux for extraction twice, each time for 2 hours, and concentrate the extract under reduced pressure to obtain 1.48 kg of extract;
[0066] b. Dissolve the extract in 2L of methanol, adsorb on 3.0kg of diatomaceous earth, dry, and successively elute with petroleum ether, dichloromethane, ethyl acetate, acetone, and methanol, each 10L, and concentrate the eluents respectively to obtain petroleum Ether fraction 407g, dichloromethane fraction 158g, ethyl acetate fraction 40g, acetone fraction 50g and methanol fraction 540g;
[0067] c. Separation of 400 g of petroleum ether by silica gel chromatography, followed by petroleum ether - ethyl acetate = 50:1; 25:1; 10:1; 5:1; 2:1; 1:1; 0:100 Gradient el...
Embodiment 2
[0074] Example 2: Research on the Antitumor Effect of Thymol Derivatives Compounds I and II
[0075] The clinically used antitumor drug 5-fluorouracil was used as the positive control drug, and the corresponding solvent was used as the negative control drug. Human lung cancer cell line (A549), human uterine cancer cell line (Hela), human liver cancer cell line (HepG2) and human breast Cancer cell line (MCF-7) is the tested cell line; the antitumor activity of the compound was tested in vitro by MTT method.
[0076] The test drug and the cells were co-cultured for 48 hours, and according to the results of the pre-experimental cell growth rate, 190 μL of cells at a certain density were inoculated in a 96-well culture plate (about 5×10 4 -1×10 5 pieces / hole).
[0077] After culturing for 24 hours and waiting for the cells to adhere to the wall, 10 μL of samples with serial concentrations were added respectively, and 5 replicate wells were set up for each sample, wherein the fin...
PUM
Login to View More Abstract
Description
Claims
Application Information
Login to View More