chamaejasmin and chamaechromone

A simple and efficient method based on ultrafiltration with liquid chromatography and mass spectrometry was used for the rapid screening and identification of ligands in the extracts of Stellera chamaejasme. The bound ligands, i.e. daphnoretin, isopimpinellin, chamaechromone, neochamaejasmin A, and chamaejasmine (purity of 96.8, 90.75, 91.41, 93.98, and 98.91%, respectively), were separated by semi-preparative high-performance liquid chromatography combined with high-speed counter-current chromatography. To the best of our knowledge, this is the first study to report the detection of potent lipoxidase and lactate dehydrogenase inhibitors in Stellera chamaejasme extracts. The results demonstrate that our method of ultrafiltration with liquid chromatography and mass spectrometry combined with mixed chromatography can be used to screen and confirm the bioactivity of all isolated compounds. This method also eliminates the need for separation of inactive compounds, thereby improving efficiency when studying bioactive substances. For some complex mixtures, neither semi-preparative high-performance liquid chromatography nor high-speed counter-current chromatography can purify all the target active compounds with high purity in a one-step separation. The combination of the two methods allow for efficient purification of target bioactive compounds with different polarities and physicochemical properties based on their complementary properties.

Topics: Biflavonoids; Chromatography, High Pressure Liquid; Coumarins; Countercurrent Distribution; Drug Evaluation, Preclinical; Flavones; Furocoumarins; Ligands; Molecular Structure; Thymelaeaceae; Ultrafiltration

Stellera chamaejasme L. is a traditional Chinese medicine with a long history to treat stubborn skin ulcer, and it also has antiviral and antitumor effects. Neochamaejasmine B (NCB), Neochamaejasmine A (NCA) and Chamaechromone (CMC) are the major components in dried roots of Stellera chamaejasme L.. Our studies suggested that NCB, NCA and CMC are inhibitors of Organic anion transporter 1 (OAT1). OAT1 is encoded by solute carrier family 22 member 6 gene (SLC22A6) in humans and plays a critical role in the organic anion drug uptake and excretion in the kidney. Lamivudine is the typical substrate of OAT1 and is frequently used in combination with other antiviral drugs in clinical antiviral treatments. The aim of this study is to investigate the interaction and its mechanism between these bi-flavone components in Stellera chamaejasme L. and lamivudine via OAT1 both in vitro and in vivo. In vitro, the uptake studies in Madin-Darby canine kidney (MDCK) cells overexpressing OAT1 suggested that NCB inhibited the uptake of 6-CFL and lamivudine.Similar results were obtained for NCA and CMC. NCB was a noncompetitive and competitive inhibitor interaction with OAT1. IC

Topics: Animals; Biflavonoids; Biological Availability; Biological Transport; Dogs; Dose-Response Relationship, Drug; Drugs, Chinese Herbal; Female; Flavones; Flavonoids; Humans; Inhibitory Concentration 50; Lamivudine; Madin Darby Canine Kidney Cells; Male; Organic Anion Transport Protein 1; Rats, Sprague-Dawley; Thymelaeaceae

Stellera chamaejasme L. (Thymelaeaceae) is a toxic perennial herb and widespread in Mongolia and the northern parts of China. Previous studies have revealed that Neochamaejasmin A (NCA), one of the main active ingredients in the plant roots, has many bioactivities such as inhibiting the P-gp-mediated efflux. But whether NCA affects ion channels is unknown. Here the whole cell patch clamp technique was used to investigate whether NCA affects ion channels, especially how it inhibits K

Topics: Animals; Biflavonoids; Biochemical Phenomena; Biophysical Phenomena; CHO Cells; Cricetulus; Flavones; Humans; Kv1.4 Potassium Channel; Molecular Structure; Thymelaeaceae

To establish a RP-HPLC fingerprint of milk Stellera chamaejasme.. The gradient elution mode was applied in chromatographic separation, and data were analysed by "Computer Aided Similarity Evaluation" software to compare the quality of milk Stellera chamaejasme samples from different habitats.. Samples from different habitats were of high similarity, and analysied milk Stellera chamaejasme chromone and E15 in the atlas.. The method is repeatable, and can be used in quality assessment of milk Stellera chamaejasme.

Topics: Animals; Biflavonoids; Chromatography, High Pressure Liquid; Drugs, Chinese Herbal; Flavones; Milk; Plant Roots; Quality Control; Reproducibility of Results; Technology, Pharmaceutical; Thymelaeaceae