The flower of Inula britannica contains various phenolic compounds with prophylactic properties. This study aimed to determine the anti-adipogenic effect of an I. britannica flower aqueous extract (IAE) and its underlying mechanisms in the 3T3-L1 preadipocytes and to identify the phenolic compounds in the extract. Treatment with IAE inhibited the adipogenesis of 3T3-L1 preadipocytes by showing a dose-dependently suppressed intracellular lipid accumulation and significantly mitigated expression levels of lipogenesis- and adipogenesis-associated biomarkers including transcription factors. IAE exerted an anti-adipogenic effect through the modulation of the early phases of adipogenesis including mitotic clonal expansion (MCE). Treatment with IAE inhibited MCE by arresting the cell cycle at the G0/G1 phase and suppressing the activation of MCE-related transcription factors. Furthermore, IAE inhibited adipogenesis by regulating the extracellular signal-regulated kinase 1/2 and Akt signaling pathways. Protocatechuic acid, chlorogenic acid, kaempferol-3-O-glucoside, and 6-methoxyluteolin, which are reported to exhibit anti-adipogenic properties, were detected in IAE. Therefore, modulation of early phases of adipogenesis, especially MCE, is a key mechanism underlying the anti-adipogenic activity of IAE. In summary, the anti-obesity effects of IAE can be attributed to its phenolic compounds, and hence, IAE can be used for the development of anti-obesity products.

Background General antiviral agents such as oseltamivir are associated with certain adverse effects and the emergence of resistance. This study investigated the phytochemical properties, antiviral activities, and safety of three herbs used in traditional Korean medicine. Methods Extracts of three medicinal herbs (Brassica juncea, Forsythia suspensa, and Inula britannica) were prepared using ethanol or water. The total phenolic, flavonoid, and saponin content, condensed tannin content, and reducing sugar content of the herb extracts were determined via phytochemical screening. Tandem mass analysis was performed using an ultra-performance liquid chromatography (UPLC)-electrospray ionization (ESI)-Q/Orbitrap instrument. Virus titrations were determined via tissue culture infective dose (TCID50) and cytotoxicity assays. Hemolysis and hepatotoxicity were measured to determine safety. Results Among the three medicinal herbs, F. suspensa showed the highest concentration of phenolic compounds, flavonoids, and saponins. The number of phytochemical compounds detected via tandem mass analysis of B. juncea, F. suspensa, and I. britannica was 5 (including sinigrin, m/z [M-H] = 358.02), 14 (including forsythoside A, m/z [M-H] = 623.19), and 18 (including chlorogenic acid, m/z [M-H] = 353.20), respectively. The antiviral effects of the B. juncea extracts (ethanol and water) and I. britannica extract (ethanol) were further investigated. The ethanol extract of B. juncea showed a 3 Log TCID50/25 μL virus titration reduction and the water extract showed a selectivity index of 13.668 against infected influenza H1N1 virus A/NWS/33. The B. juncea extracts did not show hemolysis activities and hepatotoxicity (< 20%). The ethanol extract of I. britannica showed the most effective virus titration decrease, whereas its hemolytic and hepatotoxicity values were the most significantly different compared to the control. Despite the high concentration of phytochemicals detected in F. suspensa, the extract showed approximately 1 Log TCID50/25 μL at the highest concentration. Conclusion B. juncea may show antiviral effects against H1N1 in a host. In addition, B. juncea may also show decreased disadvantages compared to other antiviral agents.

The aim of this study was to evaluate the antimicrobial efficacy of fermented Inula britannica extract (FIBE) against Staphylococcus aureus strains including methicillin‐resistant S. aureus (MRSA). I. britannica extract was fermented by Lactobacillus plantarum KCCM 11613P, and the pathogenicity of S. aureus strains was determined via assessment of coagulase, DNase, and hemolytic activities. Epicatechin concentration increased from 4.38 to 6.05 μg/mg during fermentation (p < 0.01). FIBE treatment inhibited coagulase release from S. aureus to levels below the inhibitory concentration. FIBE promoted the release of intracellular nucleic acids and N‐phenyl‐1‐naphthylamine absorption. In three S. aureus strains, damaged cells exhibited 21.58, 16.79, and 17.65% decreases in membrane potential induced by cell membrane depolarization, respectively (p < 0.05). Upon FIBE treatment in culture, the minimum inhibitory concentration of FIBE exerted a bacteriostatic effect. In conclusion, FIBE possesses antimicrobial properties, including inhibition of virulence factors, damage to cell membranes, and inhibition of bacterial growth. Practical applications Methicillin‐resistant Staphylococcus aureus (MRSA) is a serious concern in hospitals because of its known antibiotic resistance. Vancomycin and tigecycline are used for treating MRSA, but the appearance of vancomycin‐intermediate and multidrug‐resistant strains of these bacteria has created a demand for new antimicrobial agents. This study demonstrates the effective application of Inula britannica and fermentation technology for developing natural antimicrobial agents against methicillin‐resistant Staphylococcus aureus.

Abstract:Antioxidative and cytotoxic effects of chamomile (Matricaria chamomilla) fermented by Lactobacillus plantarum were investigated to improve their biofunctional activities. Total polyphenol (TP) content was measured by the Folin-Denis method, and the antioxidant activities were assessed by the 1,1-diphenyl-2-picrylhydrazyl (DPPH) method and β-carotene bleaching method. AGS, HeLa, LoVo, MCF-7, and MRC-5 (normal) cells were used to examine the cytotoxic effects by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium (MTT) assay. The TP content of fermented chamomile reduced from 21.75 to 18.76 mg gallic acid equivalent (mg GAE)/g, but the DPPH radical capturing activity of fermented chamomile was found to be 11.1% higher than that of nonfermented chamomile after 72 h of fermentation. Following the β-carotene bleaching, the antioxidative effect decreased because of a reduction in pH during fermentation. Additionally, chamomile fermented for 72 h showed a cytotoxic effect of about 95% against cancer cells at 12.7 mg solid/ml of broth, but MRC-5 cells were significantly less sensitive against fermented chamomile samples. These results suggest that the fermentation of chamomile could be applied to develop natural antioxidative and anticancer products.

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Abstract:The inhibitory effects of Lactobacillus plantarum-fermented and non-fermented Inula britannica extracts on the tyrosinase activity were comparatively investigated to examine whether and how they improve the whitening activity, and the contents of total flavonoids and polyphenolics as bioactive compounds were determined. The skin whitening activity using in vitro or ex vivo tyrosinase and L-3,4-dihydroxyphenylalanine (L-DOPA) staining was examined. The total flavonoid content (TFC) was increased by 13.4% after 72 h-fermentation. The viabilities of the B16F10 cells treated with the fermented and non-fermented control extracts were 100.26% and 92.15% at 500 µg/ml, respectively. In addition, the inhibition of tyrosinase activity was increased by the fermented samples from 29.33% to 41.74% following fermentation for up to 72 h. The tyrosinase activity of the untreated control group was increased to 145.69% in B16F10 cells. The results showed that I. britannica fermented by L. plantarum dose-dependently inhibited tyrosinase activity, which was stimulated by α-melanocyte stimulating hormone. These results suggest that lactic fermented I. britannica extracts can be used as effective skin-whitening materials.

Aims This study aimed synergistic effects of three herbs in Salmonella via increased membrane permeability and apoptosis. Methods and Results Using high‐performance liquid chromatography, four types of phenylethyl glycosides and a lignan were detected in the herb mixture (Brassica juncea, Forsythia suspensa, and Inula britannica). During treatment with the herb mixture (1×, 2×, or 4× the MIC), viable cells decreased to 1·87 log CFU per ml (Salmonella Gallinarum) and 2·33 log CFU per ml (Salmonella Enteritidis) after 12 h of incubation according to inhibition of tricarboxylic acid cycle (P < 0·01). In addition, N‐phenyl‐1‐naphthylamine uptake increased from 229·00 to 249·67 AU in S. Gallinarum and from 232·00 to 250·67 AU in S. Enteritidis (P < 0·05), whereas membrane potential decreased from 8855·00 to 3763·25 AU and from 8703·67 to 4300·38 AU, respectively. Apoptotic Salmonella cells were observed by confocal laser scanning microscopy and flow cytometry. Transmission electron microscopy observations with negative staining showed protein leakage from damaged Salmonella. Conclusions These results showed the synergistic effect of the three herbs against avian pathogenic Salmonella induced by membrane damage and apoptosis. Significance and Impact of the Study Salmonella causes enormous economic losses in the poultry industry. These results indicated that potency of natural antimicrobial agents due to apoptosis in Salmonella.

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