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Abstract Repeated column separation yielded four enterolactone type lignans from Forsythia koreana flowers (FKF), whose chemical structures were identified using several spectral technics. FKF MeOH extract (FKFM) and four lignans significantly recovered aloxan induced pancreatic islet in zebrafish. Especially, aglycones, 1 and 3, exhibited relatively higher activity than the lignan glycosides, 2 and 4. Therefore, FKFM was fermented using a Microbacterium esteraromaticum, BGP1, to yield the fermented FKFM (FKFM-BGP1). FKFM and FKFM-BGP1 were extracted using n-butanol to give n-BuOH fraction of each, FKFM-nB and FKFM-BGP1-nB, respectively. FKFM-BGP1-nB showed higher activity than FKFM-nB, as well the content of the aglycones, 1 and 3, in FKFM-BGP1-nB, 2.42 ± 0.01% and 1.15 ± 0.01%, was revealed to be much higher than that in FKFM-nB, 0.01 ± 0.01% and 0.01 ± 0.01%, respectively. In conclusion, the lignan aglycones 1 and 3 as well FKFM-BGP1-nB from F. koreana flowers were proved to be potential anti-diabetic agents. Furthermore, we suggest that antidiabetic efficacy of FKFM-BGP1-nB might be related to lignan aglycones 1 and 3.

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A simple method to prepare a high-content rutin fraction from Forsythia koreana flowers (HRFK) is described. Rutin, isolated for the first time from the flowers, was identified from spectroscopic data including nuclear magnetic resonance, mass spectrometry, and infrared. As a result of HPLC quantitative analysis, the content of rutin was found to be 80.0±0.02% in HRFK. Our previous study reported that F koreana MeOH extract (FK) significantly recovered alloxan-induced pancreatic islets in zebrafish. However, HRFK as well as rutin exhibited an enhanced anti-diabetic effect compared to FK in our latest experiments. In conclusion, HRFK, as well as rutin and FK, have potential as anti-diabetic agents. [ABSTRACT FROM AUTHOR]

The antioxidant activities of the water and ethanol extracts of F. koreana flowers were evaluated using DPPH, superoxide anion (• ), and nitric oxide (•NO) radical scavenging activity assays. The SC50 values of the water extract of F. koreana on DPPH, • and •NO were 48.39, 24.36 and 100.21 µg mL−1, respectively. The SC50 values of the ethanol extract of F. koreana on the aforesaid free radicals were 57.50, 49.00 and 146.08 µg mL−1, respectively. Further, the total phenolic contents of both extracts were determined and expressed as milligram gallic acid equivalent (GAE) per gram of extract. The water extract exhibited a higher phenolic content (113.78 mg GAE g−1), while the ethanol extract showed 94.53 mg GAE g−1. Our findings demonstrate that the water and ethanol extracts of F. koreana flowers might be potential natural sources of antioxidative additives for use in the food and other allied industries. [ABSTRACT FROM PUBLISHER]

Abstract: The activation of microglia plays an important role in a variety of brain disorders by the excessive production of inflammatory mediators such as nitric oxide (NO), prostaglandin E2 (PGE2) and proinflammatory cytokines. We investigated here whether pinoresinol isolated from the fruits of Forsythia koreana Nakai inhibits the inflammatory responses in LPS-activated microglia. Pinoresinol inhibited the production of NO, PGE2, TNF-α, IL-1β and IL-6 in LPS-activated primary microglia. Also, pinoresinol attenuated mRNA and protein levels of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2) and proinflammatory cytokines in LPS-activation. However, most of these inhibitory effects of pinoresinol have been mediated by extracellular-signal-regulated kinase (ERK) 1/2 mitogen-activated protein kinase (MAPK) phosphorylation and the NF-κB dependent. The results suggest that pinoresinol attenuates inflammatory responses of microglia and could be potentially useful in modulation of inflammatory status in brain disorders. [Copyright &y& Elsevier]

Lignans are a large class of secondary metabolites in plants, with numerous biological effects in mammals, including antitumor and antioxidant activities. Sesamin, the most abundant furofuran-class lignan in sesame seeds (Sesamum plants), is produced by the cytochrome P450 enzyme CYP81Q1 from the precursor lignan, pinoresinol. In contrast, Forsythia plants produce dibenzylbutyrolactone-class lignans, such as matairesinol, from pinoresinol via the catalysis of pinoresinol/lariciresinol reductase (PLR) and secoisolariciresinol dehydrogenase. Here we present the engineering of lignan biosynthesis in Forsythia cell suspension cultures for the development of an efficient production method of beneficial lignans. A suspension cell culture prepared from leaves of Forsythia koreana produced lignans, mainly pinoresinol and matairesinol glucosides, at levels comparable with that obtained from the leaves. In an attempt to increase the pinoresinol content in Forsythia, we generated a transgenic cell line overexpressing an RNA interference (RNAi) construct of PLR (PLR-RNAi). Down-regulation of PLR expression led to a complete loss of matairesinol and an accumulation of approximately 20-fold pinoresinol in its glucoside form in comparison with the non-transformant. Moreover, the Forsythia transgenic cells co-expressing CYP81Q1 and PLR-RNAi exhibited production of sesamin as well as accumulation of pinoresinol glucoside. These data suggest Forsythia cell suspension to be a promising tool for the engineering of lignan production. To the best of our knowledge, this is the first report on transgenic production of an exogenous lignan in a plant species. [ABSTRACT FROM PUBLISHER]

Abstract: Aim of the study: The fruits of Forsythia koreana have long been used in Chinese medicine to treat inflammatory disorders. However, the pharmacological data is not sufficient to clearly establish a scientific rationale for the anti-inflammatory medicinal use of this plant material, and the search for its active principles has been limited so far. Materials and methods: Phylligenin (lignan) was isolated from the fruits of Forsythia koreana and its anti-inflammatory activity was examined. Results and conclusion: Phylligenin (1–100μM) and the methanol extract of Forsythia koreana fruits inhibited cyclooxygenase-2 (COX-2)-mediated prostaglandin E2 and inducible nitric oxide synthase (iNOS)-mediated nitric oxide (NO) synthesis from lipopolysaccharide-treated RAW 264.7 cells. In the mechanism study, phylligenin inhibited iNOS expression and nuclear factor-κB (NF-κB) activation but had no effect on COX-2 expression. Moreover, phylligenin significantly inhibited mouse carrageenan-induced paw edema by intraperitoneal administration (22.1–34.7% inhibition at 12.5–100mg/kg). These pharmacological properties indicate that phylligenin possesses significant anti-inflammatory activity in vitro and in vivo, and may provide the scientific rationale for anti-inflammatory use of the fruits of Forsythia koreana. [Copyright &y& Elsevier]

Abstract: Nitric oxide (NO) is recognized as a mediator and regulator of inflammatory responses. Rengyolone, a cyclohexylethanoid isolated from the fruits of Forsythia koreana, exhibits anti-inflammatory activity with unknown mechanism. In this study, we found that rengyolone has a strong inhibitory effect on the production of nitric oxide (NO) and tumor necrosis factor-α (TNF-α). Rengyolone also inhibited inducible nitric oxide synthase (iNOS) gene expression and cyclooxygenase 2 (COX-2) by lipopolysaccharide (LPS). In order to explore the mechanism responsible for the inhibition of iNOS gene expression by rengyolone, we investigated its effect on LPS-induced nuclear factor-κB (NF-κB) activation. The LPS-induced DNA binding activity of NF-κB was significantly inhibited by rengyolone, and this effect was mediated through inhibition of the degradation of inhibitory factor-κBα and phosphorylation of p38 MAP kinase. Furthermore, rengyolone suppressed the expression of ICE protein in IL-1β-treated D10S cells. Taken together, these results suggest that rengyolone attenuates the inflammation through inhibition of NO production and iNOS expression by blockade of NF-κB and p38 MAPK activation in LPS-stimulated RAW 264.7 cells. [Copyright &y& Elsevier]

A method involving high-performance liquid chromatography coupled with electrospray MS-MS has been developed for the analysis of the constituents of the fruits, leaves, and stems of Forsythia koreana. Ten compounds including caffeoyl glycosides and lignans could be separated and detected with good sensitivity. The MS-MS spectra obtained provided information about their structures, for example the sugar and aglycone moieties present. Supercritical-fluid extraction was also used to improve the efficiency of extraction of arctigenin, which has the highest anti-inflammatory activity of the compounds produced by this plant. Although carbon dioxide without any modifier extracted only 66% of that obtained by extraction with methanol, an 80:20 ( v/v) carbon dioxide-methanol mixture greatly enhanced the extraction yield-to 110%. [ABSTRACT FROM AUTHOR]

Six lignans including two new lignans were obtained as the principal components of the Forsythia koreana flowers via silica gel (SiO 2 ), octadecyl SiO 2 (ODS) as well as Sephadex LH-20 column chromatography. In addition to two new lignans, named koreanaside A ((7R,8S,7'R,8'S)-7,7'-diepoxy-5'-hydroxy-3,3'-dimethoxylignan 4-O-β-d-glucopyranoside) and koreanaside B ((7R,8S,7'S,8'R)-7,9'-epoxy-9,5',7'-trihydroxy-3,3'-dimethoxylignan 4-O-β-d-glucopyranoside), four known lignans were identified to be (+)-phylligenin, (-)-epipinoresinol, pinoresinol, and tinosposide A. The structures and absolute configurations of koreanasides A and B were established by means of analysis of spectroscopic data (NMR, IR, FAB-MS, and CD), whereas the structures of known lignans were identified by comparison their NMR and MS values with those in the reported literature. Their chemical structures including configuration were established by means of analysis of spectroscopic data (NMR, IR, FAB-MS, and CD) but also comparison of their NMR and MS values with those in the reported literature. This is the first article for isolation of six lignans of F. koreana flowers. Koreanasides A and B showed high radical scavenging activity with oxygen radical absorbance capacity (ORAC) values of 0.97 ± 0.01 and 1.02 ± 0.01, respectively. Koreanaside A also prohibited expressing VCAM-1 in MOVAS cells with 80.5% at 25 mg/mL., (© 2018 Wiley-VHCA AG, Zurich, Switzerland.)

Background: Breast cancer is the most common malignant disease in women. The patients with advanced breast cancer develop metastasis to bone. Bone metastasis and skeletal-related events by breast cancer are frequently associated with the invasiveness of breast cancer cells and osteoclasts-mediated bone resorption. Forsythia koreana is used in oriental traditional medicine to treat asthma, atopy, and allergic diseases. The aim of this study was to evaluate the inhibitory effects of F. koreana extracts on the invasion of breast cancer cells and bone resorption by osteoclasts., Methods: Cell viability was measured by an MTT assay and the migration and invasion of MDA-MB-231 cells were detected by a Boyden chamber assay. The formation of osteoclasts and pit was detected using tartrate-resistant acid phosphatase staining and calcium phosphate-coated plates, respectively. The activities of matrix metalloproteinases (MMPs) and cathepsin K were evaluated by gelatin zymography and a cathepsin K detection kit., Results: The fruit and leaf extracts of F. koreana significantly inhibited the invasion of MDA-MB-231 cells at noncytotoxic concentrations. The fruit extract of F. koreana reduced the transforming growth factor β1-induced migration, invasion and MMPs activities of MDA-MB-231 cells. In addition, the fruit, branch, and leaf extracts of F. koreana also inhibited the receptor activator of nuclear factor kappa-B ligand-induced osteoclast formation and osteoclast-mediated bone-resorbing activity by reducing the activities of MMPs and cathepsin K., Conclusions: The extracts of F. koreana may possess the potential to inhibit the breast cancer-induced bone destruction through blocking invasion of breast cancer cells, osteoclastogenesis, and the activity of mature osteoclasts.