ABSTRACT
This is to report the screening, extracting and validating antitumor components and compounds from Stellera chamaejasme L. under the case of discrete distribution of active data. In this work, different components from Stellera chamaejasme L. were collected by HPD macroporous resin and polyamide resin column, and their antitumor activity on A549 were tested by MTT assay. Activity results indicate that activity of components at 30-39 min is more potent than that of Stellera chamaejasme L. extract, and the activity of components at 33.97 min is equivalent to positive drug, cis-platinum at 100 microg x mL(-1), but with totally different mode of action. Under the case of discrete activity, the weight analysis is capable of screening active components and compounds from natural products.
Subject(s)
Humans , Antineoplastic Agents, Phytogenic , Pharmacology , Cell Line, Tumor , Drug Screening Assays, Antitumor , Thymelaeaceae , ChemistryABSTRACT
<p><b>OBJECTIVE</b>To screen the best antitumor components of Stellera chamaejasme and their sensitive cell lines.</p><p><b>METHOD</b>Sixteen different components of alcohol extracts from S. chamaejasme, including HH, H1-H8, JH and J1-J8, were got by gradient column chromatography eluted with alcohol in different concentrations. In the first screening, the solvent control group, the drug group, the positive group and the blank group were set up. Then the human cancer cell lines such as hepatocarcinoma BEL-7402, SK-HEP-1, and lung cancer A549, NCI-H157 were processed with the components, and the concentration for each drug group was 100 mg x L(-1). Thus, the 48 hour suppression ratio to the four kinds of cancer cells for each component were compared by the SRB method, to select the most inhibitive components and the most sensitive cell lines, which were used as the subjects of the second screening. In the second screening, each component including the concentration of 6.25, 12.5, 25, 50, 100 mg x L(-1) was used to treat the sensitive cell lines and the inhibition rates to each cell line of 24, 48, 72 h by the SRB assay were detected. Also, the IC50 of each component was calculated and their main chemical composition was analyzed by UPLC-MS.</p><p><b>RESULT</b>The inhibition effect to the proliferation of the different cancer cells has great difference among 16 components, and the lung cancer cells are more sensitive to them than the hepatocarcinoma cells. Besides, the inhibition rates of JS, J6 and H8 are higher than the other components and their effect has a certain time and concentration dependence. At 72 h, the inhibition rate of each component ranges from (60.57 +/- 3.83)% to (96.66 +/- 0.51)% for lung cancer cells, and IC50 from (9.61 +/- 0.79) mg x L(-1) to (55.76 +/- 2.31) mg x L(-1). J5, J6 and H8 are the biflavonoids.</p><p><b>CONCLUSION</b>The biflavonoids in alcohol extracts from S. chamaejasme have exerted a satisfactory inhibitory effect on the lung cancer cell proliferation.</p>
Subject(s)
Humans , Antineoplastic Agents, Phytogenic , Chemistry , Pharmacology , Cell Line, Tumor , Cell Proliferation , Inhibitory Concentration 50 , Liver Neoplasms , Lung Neoplasms , Plant Extracts , Chemistry , Pharmacology , Thymelaeaceae , Chemistry , Tumor Cells, CulturedABSTRACT
Epimedium was obtained from different habitats, and their bioactive components for inhibiting RAW264.7 were screened by MTT assay. Results indicate that epimedium from different habitats displayed significant different activities. By means of model population analysis (MPA), a latent bioactive component, baohuoside-I was got. Activity of baohuoside-I wasvalidated and prior to icariin. MPA can be used for bioactive components screening.