lignans and forsythiaside

Forsythiae Fructus, Lianqiao in Chinese, is one of the most fundamental herbs in Traditional Chinese Medicine. Both green Forsythia (GF) and ripe Forsythia (RF) are referred to Forsythiae Fructus in medicinal applications. In most cases, they are used without distinction. In this study, a metabolomics approach was performed to compare componential differences of two Forsythiae Fructus aqueous extracts subtypes. Principal component analysis (PCA) score plots from the UPLC-MS data showed clear separation between the two subtypes, indicating there are significant differences in the chemical components between GF and RF. Meanwhile, the anticancer activity of them was also compared. GF exhibited much stronger antitumor activity than RF against B16-F10 murine melanoma both in vitro and in vivo. 15 chemical compounds were identified as specific markers for distinguishing GF and RF. Among these marker compounds, forsythoside I, forsythoside A, forsythoside E and pinoresinol were demonstrated to be key important active compounds that account for the different anticancer efficacies of GF and RF. Our data suggest that GF and RF should be distinctively used in clinical applications, particularly in the anticancer formulas, in which GF should be preferentially prescribed.

Topics: Animals; Antineoplastic Agents, Phytogenic; Catechols; Cell Proliferation; Disaccharides; Female; Forsythia; Fruit; Furans; Glycosides; Lignans; Mass Spectrometry; Melanoma, Experimental; Metabolomics; Mice, Inbred C57BL; Phytotherapy; Plant Extracts; Skin Neoplasms; Tumor Cells, Cultured; Water

Forsythia suspensa extract has been proved as a potential antioxidant in the recent years. The present study was undertaken to obtain the optimal antioxidant fraction in vitro and examine its antioxidative potential against diquat-induced oxidative stress in male Sprague Dawley rats in vivo. In vitro, 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging experiment indicated that the CH2Cl2 fraction of F. suspensa (FSC) exerted the strongest scavenging activities; forsythoside A, forythialan A and phillygenin from it might be the major antioxidant constituents. In vivo, pretreatment of rats with different doses of FSC (25, 50 and 100 mg/kg bw) and vitamin C (100 mg/kg bw, positive control) for 15 days significantly lowered the tumor necrosis factor-alpha (TNF-alpha), interleukin-1beta (IL-1beta), and interleukin-6 (IL-6) in plasma compared to the negative control group. Also, FSC significantly increased the activities of superoxide dismutase (SOD), glutathione peroxidase (GSH-Px), and the levels of glutathione (GSH) in plasma, liver and kidney whereas it decreased the levels of malondialdehyde (MDA) in plasma and kidney. Moreover, the protective effect of FSC (100 mg/kg bw) was better than vitamin C. These results revealed that FSC exerted a protective effect against diquat-induced oxidative stress and is worthy of becoming a potential dietary antioxidant.

Topics: Animals; Antioxidants; Ascorbic Acid; Biphenyl Compounds; Cytokines; Diquat; Forsythia; Free Radicals; Fruit; Glycosides; Herbicides; Indicators and Reagents; Kidney; Lignans; Liver; Male; Oxidative Stress; Oxidoreductases; Picrates; Rats; Rats, Sprague-Dawley

To separate samples of complex natural products, highly efficient and selective separation methods should be developed. Herein, a selective enrichment method was developed to separate Forsythia suspensa components with "click oligo (ethylene glycol)" (OEG) column in reversed phase (RP) mode. In this method, F. suspensa aqueous extract was successfully separated. And three fractions with structure-related compounds were obtained. Fraction I mainly consisted of C(6)-C(2) natural alcohols and glycosides, fraction II mostly consisted of lignans, and fraction III mainly consisted of simple phenylpropanoids (SP). Then, the three fractions were separated with ultra-performance liquid chromatography (UPLC). Four more lignans were observed in fraction II, and eight more SP were observed in fraction III than that without OEG column. Fraction III was successively characterized by TOF-MS, 2 acids (caffeic acid and chlorogenetic acid), 26 SP with caffeoyl, and 2 SP with coumaroyl were characterized. The results prove that a valid method has been developed to selectively enrich SP and lignans. And the method combined with UPLC can efficiently separate SP and lignans. Furthermore, the TOF-MS method is effective to confirm the substituents of SP.

Topics: Chromatography, Liquid; Drugs, Chinese Herbal; Ethylene Glycol; Forsythia; Fruit; Glycosides; Lignans; Mass Spectrometry; Molecular Structure; Plant Extracts

A simple and reproducible HPLC-photodiode array detector method has been described for evaluating and controlling quality of Forsythia suspensa extract (FSE). First, by analysis of chromatographic fingerprints, the similarities of chromatograms of FSE samples from the same pharmaceutical company exceeded 0.999, 0.997 and 0.960, respectively, although they were much lower from different pharmaceutical companies. Second, by further comparing many batches of extract chromatograph charts with the corresponding reference herb materials, the "common peaks" 3, 5, 7 and 10 were defined as "marker peaks", which were identified as (+)-pinoresinol-beta-D-glucoside, forsythiaside, phillyrin and phillygenin, respectively. Third, four "marker peaks" were simultaneously determined based on fingerprint chromatogram for further controlling the quality of FSE quantitatively. Namely, the newly developed method was successfully applied to analyze 38 batches of FSE samples supplied by three pharmaceutical factories, which showed acceptable linearity, intra-day precision (RSD<2.76%), inter-day precision (RSD<3.43%) and the average recovery rates in the range of (95.38+/-2.96)% to (101.60+/-3.08)%. At last, hierarchical clustering analysis and Bayes discriminant analysis statistical methods were used to classify and differentiate the 38 FSE samples to provide the basis for guiding reasonable use of FSE and controlling its quality better.

Topics: Chromatography, High Pressure Liquid; Drugs, Chinese Herbal; Forsythia; Glucosides; Glycosides; Lignans; Magnetic Resonance Spectroscopy; Plant Extracts; Plants, Medicinal; Quality Control