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Siegesbeckia glabrescens (Compositae), an annual herb indigenous to Korean mountainous regions and has been eaten as a food in Korea. This study investigated ABTS, DPPH and nitric oxide (NO) radical-scavenging activities, and melanin production and TYR inhibitory effects-guided fractionation to identify therapeutic phytochemicals from S. glabrescens that can attenuate oxidation and melanogenesis in murine melanoma B16F10 cells. Nine compounds with inhibitory effects on melanin production, and TYR activity, and ABTS, DPPH, and NO radical scavenging activity were isolated from the 100% ethanol fraction from S. glabrescens . Among the nine compounds, kirenol (K), methyl ent-16α, 17-dihydroxy-kauran-19-oate (MDK) had strong inhibitory effects on melanin production and TYR activity with antioxidant effects. Western blot analysis revealed that K and MDK suppressed tyrosinase-related protein (TYRP)-1, TYRP-2 and microphthalmia-associated transcription factor (MITF) expression. Moreover, these two compounds inhibited intracellular reactive oxygen species (ROS) level in tert-butyl hydroperoxide ( t -BHP)-treated B16F10 cells. Our results suggest that S. glabrescens containing active compounds such as K and MDK, which has antioxidant and antimelanogenesis effects, is the potent therapeutic and functional material for the prevention of oxidation-induced hyperpigmentation.

Siegesbeckia glabrescens is generally grown in fields or roadsides in Korea and used for the treatment of inflammatory diseases. The effects of S. glabrescens on periodontitis are unknown. In this study, we determined the effects of an S. glabrescens 30% EtOH extract (SGE) on periodontitis and analyzed the antioxidant activity (DPPH, ABTS, and SOD), antimicrobial (disc diffusion, MIC, and MBC), inhibition of GTFs, biofilm formation, and the anti-inflammation of lipopolysaccharide from P. gingivalis (LPS-PG)-induced primary equine periodontal ligament fibroblasts (PDLFs). We report that SGE increased DPPH, ABTS, and SOD antioxidant activities in a dose-dependent manner. SGE caused a clear zone with a diameter of 15 mm or more against periodontal pathogens. SGE (2.50 mg/mL) inhibited GTFs and biofilm by 89.07% and 85.40%, respectively. SGE treatment (100 µg/mL) also significantly decreased the secretion of inflammatory mediators in sensitized PDLF, including cytokines and matrix metalloproteinase (MMP)-3, -8, -9, and -13. Overall, we confirmed that SGE had excellent antioxidant, antimicrobial, and anti-inflammatory effects against periodontal pathogens. These results suggest that it has the potential to develop as a prophylactic agent for periodontitis. [ABSTRACT FROM AUTHOR]

Siegesbeckia glabrescens is generally grown in fields or roadsides in Korea and used for the treatment of inflammatory diseases. The effects of S. glabrescens on periodontitis are unknown. In this study, we determined the effects of an S. glabrescens 30% EtOH extract (SGE) on periodontitis and analyzed the antioxidant activity (DPPH, ABTS, and SOD), antimicrobial (disc diffusion, MIC, and MBC), inhibition of GTFs, biofilm formation, and the anti-inflammation of lipopolysaccharide from P. gingivalis (LPS-PG)-induced primary equine periodontal ligament fibroblasts (PDLFs). We report that SGE increased DPPH, ABTS, and SOD antioxidant activities in a dose-dependent manner. SGE caused a clear zone with a diameter of 15 mm or more against periodontal pathogens. SGE (2.50 mg/mL) inhibited GTFs and biofilm by 89.07% and 85.40%, respectively. SGE treatment (100 µg/mL) also significantly decreased the secretion of inflammatory mediators in sensitized PDLF, including cytokines and matrix metalloproteinase (MMP)-3, -8, -9, and -13. Overall, we confirmed that SGE had excellent antioxidant, antimicrobial, and anti-inflammatory effects against periodontal pathogens. These results suggest that it has the potential to develop as a prophylactic agent for periodontitis.

The aim of this study is to elucidate the anti-inflammatory effects of Siegesbeckia glabrescens extract in vitro. The n-butanol fraction (100 µg/ml) of S. glabrescens had an approximately 92% inhibitory effect on nitrite production from lipopolysaccharide (LPS)-induced macrophage cells, whereas other fractions showed relatively low nitric oxide (NO) inhibition. The n-butanol and ethyl acetate fractions of S. glabrescens showed significant chemical NO quenching to approximately 39-46% in the cell-free system, and showed the decreases of inducible nitric oxide synthase (iNOS) transcription potently. The hexane, n-butanol, and ethyl acetate fractions of S. glabrescens showed approximately 90-96% inhibition of prostaglandin E2 (PGE2) synthesis. The ethyl acetate, n-butanol, and aqueous fractions of S. glabrescens showed a potent inhibition of LPS-induced cyclooxygenase-2 (COX-2) mRNA transcription. All S. glabrescens extract-fractions showed significant decreases of IL-1β biosynthesis to 69.7-97.0%, as compared to LPS-induced IL-1β production in macrophage cells. [ABSTRACT FROM AUTHOR]