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Six new dimeric lignans (1-6) and one new lignan glycoside (16) were isolated from Forsythia viridissima roots along with nine known lignans (7-15). Spectroscopic analyses and chemical methods were used to determine these new structures and their absolute configurations. Among these compounds, dimatairesinol (1) and viridissimaols A-E (2-6) were assigned as dimers of dibenzylbutyrolactone analogues. Furthermore, the isolated compounds were evaluated for their antiviral activities against coxsackievirus B3 (CVB3) and human rhinovirus 1B (HRV1B). In these tests, compounds 12 and 15 showed antiviral effects against CVB3 infection with IC50 values of 15.4 and 36.4 μM, respectively, while 2, 3, 8, and 9 showed activities against HRV1B with IC50 values of 45.7, 47.5, 13.0, and 43.2 μM, respectively.

The dried fruits of Forsythia viridissima have been prescribed to relive fever, pain, vomiting, and nausea in traditional medicine. Oxaliplatin (LOHP) is used to treat advanced colorectal cancer, however, it frequently induces peripheral neuropathies. This study was done to evaluate the neuroprotective effects of an aqueous extract of Forsythia viridissima fruits (EFVF) and its major constituents. Chemical constituents from EFVF were characterized and quantified with the UHPLC-diode array detector method, and three major constituents were identified as arctiin, matairesinol, and arctigenin. The in vitro cytotoxicity was measured by the Ez-cytox viability assay, and the in vivo neuroprotection activity was evaluated by a von Frey test in two rodent animal models that were administered LOHP. EFVF significantly alleviated the LOHP-induced mechanical hypersensitivity in the induction model. EFVF also prevented the induction of mechanical hyperalgesia by LOHP in the pre- and co-treatment of LOHP and EFVF. Consistently, EFVF exerted protective effects against LOHP-induced neurotoxicity as well as inhibited neurite outgrowths in PC12 and dorsal root ganglion cells. Among the major components of EFVF, arctigenin and matairesinol exerted protective effects against LOHP-induced neurotoxicity. Therefore, EFVF may be useful for relieving or preventing LOHP-induced peripheral neuropathy in cancer patients undergoing chemotherapy with LOHP.

Lignans are known to be an important class of phenylpropanoid secondary metabolites. In the course of our studies on the chemodiversity of lignans, the necessity arose to develop a method for the fast detection and identification of bioactive lignan subclasses. In this study, we detected 10 lignan derivatives of different extracts of F. viridissima by UHPLC-ESI-QTOF-MS. Lignan glycosides (1 and 2), lignans (3 and 4), and lignan dimers (5&ndash, 10) were identified by analysis of their exact masses and MSe spectra along with the characteristic mass fragmentation patterns and molecular formulas. We further investigated NO inhibitory effects of F. viridissima fractions and their major lignan derivatives to evaluate those anti-inflammatory effects. The methylene chloride fraction of F. viridissima as well as compounds 8 and 10 showed potent dose-dependent NO inhibitory effects on RAW 264.7 cells. Corresponding to the NO inhibition by compounds 8 and 10, lipopolysaccharide (LPS)-induced inducible nitric oxide synthase (iNOS) expression was notably reduced by both compounds. Our combined data with the bioactive results and the component analysis by UHPLC-ESI-QTOF-MS suggest that the methylene chloride fraction of F. viridissima roots could be potential anti-inflammatory agents and these are related to major lignans including dimeric dibenzylbutyrolactone lignans.

This study was conducted to investigate the antioxidative effects of Paeonia lactiflora Pall. (PL) seed extracts and Forsythia viridissima Lindl. (FVL) extracts on the antioxidative defense system and lipid peroxidation in the erythrocytes of rats fed a high-cholesterol diet. Sprague-Dawley male rats weighing 100±10 g were randomly assigned to nine experimental groups and fed 0.5% cholesterol. The HC group did not receive any supplement, while the MP1 group was supplemented with 0.1% methanol extract of PL seed, the MP2 group with 0.2% methanol extract of PL seed, the EP1 group with 0.05% ether-soluble fraction of PL seed, the EP2 group with 0.1% ether-soluble fraction of PL seed, the MS1 group with 0.05% methanol extract of FVL, the MS2 group with 0.1% methanol extract of FVL, the ES1 group with 0.025% ethyl acetate-soluble fraction of FVL, and the ES2 group with 0.05% ethyl acetate-soluble fraction of FVL. The experimental diets were fed ad libitum for 3 weeks. The erythrocyte SOD activity in the EP1 and EP2 groups increased 38% and 59%, respectively, when compared with the HC group, while the erythrocyte GSHpx activity in the EP1, EP2, and ES2 groups increased 30%, 31%, and 29%, respectively, when compared with the HC group. The level of erythrocyte TBARS was significantly lower in the MP2, EP1, and EP2 groups than in the HC group, yet the level of serum TBARS was significantly lower in the all supplemented groups than in the HC group. The level of serum HDL-TBARS was significantly lower in the EP1 and EP2 groups than in the HC group, while the level of serum LDL-TBARS was significantly lower in the all the supplemented groups than in the HC group. Accordingly, the results indicated that the PL seed extracts and FVL extracts reduced oxidative damage by activating the antioxidative defense system in the erythrocytes of rats fed a high-cholesterol diet.

Two new phenol glycosides forsythoside F and forsythoside G have been isolated from Forsythia viridissima stems and their structures were established based on the spectroscopic data and chemical transformations. D-2-O-methylapiose was for the first time characterized in the natural product