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
Z-Ligustilide, a major phthalide isolated from a widely used traditional Chinese medicine Ligusticum chuanxiong, possesses various pharmacological activities including neuroprotective, anti-inflammatory, antiproliferative and vasorelaxing effects. However, it is unstable and inclined to degrade in natural conditions, which limits its study and application greatly. In this study, degradation behavior of Z-ligustilide and its degradation products stored at room temperature under direct sunlight were investigated and structure elucidated by HPLC-UV, UPLC-QTOF-MS and NMR. Z-ligustilide degradation and total five degradation products were generated and detected. Two degradation products were unequivocally identified as senkyunolide I and senkyunolide H by comparison with reference compounds. Another two degradation products were further isolated by semi-preparative HPLC and structure elucidated as (E)-6, 7-trans-dihydroxyligustilide and (Z)-6, 7-epoxyligustilide by 1H and 13C NMR, respectively. The degradation pathways of Z-ligustilide were finally proposed. Oxidation, hydrolysis and isomerization are the major degradation reactions.
Subject(s)
4-Butyrolactone , Metabolism , Benzofurans , Metabolism , Chromatography, High Pressure Liquid , Hydrolysis , Ligusticum , Chemistry , Magnetic Resonance Spectroscopy , Metabolic Networks and Pathways , Oxidation-Reduction , Plant Roots , Chemistry , Plants, Medicinal , Chemistry , Spectrometry, Mass, Matrix-Assisted Laser Desorption-IonizationABSTRACT
<p><b>OBJECTIVE</b>To analyze and identify the chemical constituents in rat brain tissues after oral administration of Chuanxiong Rhizoma extracts.</p><p><b>METHOD</b>The dosed and blank rat brain tissues were analyzed by UPLC-Q-TOF-MS. Different peaks were observed in total ion chromatograms and then identified according to their retention time, accurate mass weight, MS and MS/MS data.</p><p><b>RESULT</b>After oral administration of Chuanxiong Rhizoma extracts, 3 compounds were absorbed into rat brain tissues through BBB. They were identified as senkyunolide I, senkyunolide A and ligustilide.</p><p><b>CONCLUSION</b>The study is helpful for interpreting effective substance of Ligusticum chuanxiong.</p>