ABSTRACT
Tumor is a disease with high mortality rate,which seriously threatens the human life and health.To study the antitumor effect,sensitization and anti-drug-resistant action of effective ingredients extracted from traditional Chinese medicine or natural medicine is a hotspot.Polymethoxyflavone is a class of flavonoids with strong anti-tumor activity found in recent years.In this paper,the research progress on anti-tumor action and its mechanisms of polymethoxyflavonoids is reviewed.
ABSTRACT
Sinensetin, a pentamethoxyflavone, is known to exert various pharmacological activities including anti-angiogenesis, anti-diabetic and anti-inflammatory activities. However, its effects on the human mast cell - 1 (HMC-1) mediated inflammatory mechanism remain unknown. To explore the mediator and cellular inflammatory response of sinensetin, we examined its influence on phorbol 12-myristate 13-acetate (PMA) plus A23187 induced inflammatory mediator production in a human mast cell line. In this study, interleukin (IL)-6 production was measured using the enzyme-linked immunosorbent assay and reverse transcription polymerase chain reaction. Sinensetin inhibited PMA plus A23187 induced IL-6 production in a dose-dependent manner as well as IL-4, IL-5 and IL-8 mRNA expression. Furthermore, sinensetin inhibited signal transducer and activator of transcription 3 (STAT3) phosphorylation, suggesting that sinensetin inhibits the production of inflammatory mediators by blocking STAT3 phosphorylation. Moreover, sinensetin was found to inhibit nuclear factor kappa B activation. These findings suggest that sinensetin may be involved in the regulation of mast cell-mediated inflammatory responses.
Subject(s)
Humans , Calcimycin , Enzyme-Linked Immunosorbent Assay , Interleukin-4 , Interleukin-5 , Interleukin-6 , Interleukin-8 , Interleukins , Mast Cells , NF-kappa B , Phosphorylation , Polymerase Chain Reaction , Reverse Transcription , RNA, Messenger , STAT3 Transcription Factor , TransducersABSTRACT
Objective To develop a method for content determination of sinensetin,eupatorin,and 3′-hydroxy-5,6,7, 4′-tetramethoxyflavone in Orthosiphon stamineus. Methods The determination was carried out on a Symmetry C18 column (4.6 mm×250 mm,5 μm) by HPLC.The mobile consisted of acetonitrile and water containing 0.05% H3 PO4 in gradient elution. The flow rate was 1 mL?min-1 ,the column temperature was 30 ℃ ,the detected wavelength was set at 365 nm, and the injection volume was 10 μL. Results The peak areas and the sample quantity of the three components presented good linear relationship in the range of 0. 50 - 5. 00 μg for sinensetin,0. 50 - 5. 00 μg for eupatorin, and 0. 05 - 0. 50 μg for 3′-hydroxy-5,6,7,4′-tetramethoxyflavone.The average recoveries were 101.26%,100.28% and 99.66%,respectively. RSD were 1.73%, 0.82% and 1.67%, respectively. Conclusion The method is proved to be simple,accurate and can be used for the quality evaluation of Orthosiphon stamineus.
ABSTRACT
Objective: The aim of the present study is to develop liquid chromatography (LC)/Time-of-flight mass spectrometry (TOF/MS) profile for methanol and water extracts of Orthosiphon stamineus leaf using SEN and RA as flavonoid and non-flavonoid polyphenolic markers in the extracts. The study also evaluates in vitro nitric oxide radical scavenging effect of the extracts. Method:Orthogonal Time of Flight Mass Spectrometer equipped with HPLC separation module was used in the analyses of the extract. The in vitro nitric oxide scavenging activity of the extracts was measured according to the method described by Rao. Results: The qualitative analysis of the extracts performed with HPLC-TOF/MS confirmed the presence sinensitin (SEN) and rosmarinic acid (RA) in the extracts. The extracts showed in vitro nitric oxide scavenging activities. Conclusions: The HPLC-TOF/MS method could be employed for quality determination of herbal medicinal products and formulations containing O. stamineus. The extracts may play a significant role in prevention of degenerate disease due to its ability to scavenge nitric oxide radical.
ABSTRACT
AIM: To develop a rapid HPLC method for quality control of traditional Chinese medicinal ingredients consisted of citrus flavonoids, naringin, hesperidin, neohesperidin, sinensetin and nobiletin. METHODS:Gradient elution with non-salt mobile phase ( methanol and water only) HPLC method on a Kromasil column ( 100-5C18-250A, 4.6 mm ×250 mm, 5 μm, C18 reverse phase) with peaks identification through DAD full UV wavelength scan. UV 284 nm and 332 nm profiles were observed. RESULTS: Satisfactory resolution, linearity, 95%～ 102% of recovery and 1.88 ～ 2.93% of repeatability were obtained for those five citrus flavonoids. Content of 6 Citrus aurantium L. based TCM ingredients were analyzed and identified. CONCLUSION: Rapid HPLC test method on citrus flavonoids was developed and can be in LC-MS identification.