• The Journal of Korean Medicine
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• v.21 no.1
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• pp.77-83
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• 2000

This study investigated the effects of Siegesbeckia glabrescens, an antihypertensive remedy, on the contraction evoked by phenylephrine and KCl in isolated rat thoracic arata, and also analyzed antioxidative status in vitro. Siegesbeckia glabrescens revealed dose-dependent relaxation on phenylephrine(PE)/KCl-induced arterial contraction and more markedly on PE-induced contraction. Siegesbeckia glabrescens reduced malondialdehyde(MDA)levels, Phosphatidyl choline-liposome(PC-OOH) contents, linoleic acid-induced lipid peroxidation and exerted 1,1-diphenyl-2- picryl-hydrazyl(DPPH) radical scavenging effect, in vitro. These results indicated that Siegesbeckia glabrescens doesn't relaxe artery through a blocking α-adrenergic receptor and calcium channel mediated by voltage-operated calcium channel, and it s antioxidative effects may be involved in endothelium-dependent relaxation of arteries via vascular protective properites. (J Korean Oriental Med 2000;21(1):77-83)

• 대한동의생리학회:학술대회논문집
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• 2005.07a
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• pp.21-21
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• 2005

• Korean Journal of Pharmacognosy
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• v.43 no.4
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• pp.286-290
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• 2012

Many diterpenoids from Siegesbeckia species (Compositae) and their anti-inflammatory actions have been examined. In this research, high-performance liquid chromatography-ultraviolet spectrophotometer (HPLC-UV) method was used to compare the quantitative level of kirenol (ent-pimarane-type diterpenoid) in the aerial parts of Korean S. glabrescens and S. pubescens and the Chinese Siegesbeckiae Herba. Fingerprints of the two HPLC chromatograms of Korean S. glabrescens and S. pubescens were similar, but considerably different from Chinese Siegesbeckiae Herba. The content of kirenol in S. pubescens ($16.51{\pm}0.10$ mg/ml dry weight as mean${\pm}$RSD) was higher than S. glabrescens ($13.48{\pm}0.12$ mg/g dry weight). These values were considerably higher than the Chinese Siegesbeckiae Herba ($1.55{\pm}0.74$ mg/g dry weight). Thin layer chromatography (TLC) analysis demonstrated the containing of kirenol in the three plant materials, but the presence of siegeskaurolic acid (entkaurane-type diterpenoid) only in the Chinese Siegesbeckiae Herba.

• Biomolecules & Therapeutics
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• v.19 no.1
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• pp.27-32
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• 2011

The activation of microglia induces the overproduction of inflammatory mediators that are responsible for the neurodegenerative disorders including Alzheimer's disease and Parkinson's disease. The large amounts of prostaglandin $E_2$ ($PGE_2$) produced by inducible cyclooxygenase (COX-2) is one of the main inflammatory mediators that can contribute to neurodegeneration. The inhibition of COX-2 thus may provide therapeutic strategy for the treatment of neurodegenerative diseases. From the activity-guided purification of EtOAc soluble fraction of Siegesbeckia glabrescens, four compounds were isolated as inhibitors of $PGE_2$ production in LPS-activated microglia. Their structures were determined as 3, 4'-dimethylquercetin (1), 3, 7-dimethylquercetin (2), 3-methylquercetin (3) and 3, 7, 4'-trimethylquercetin (4) by the mass and NMR spectral data analysis. The compounds 1-4 showed dose-dependent inhibition of $PGE_2$ production in LPS-activated microglia with their $IC_{50}$ values of 7.1, 4.9, 4.4, $12.4\;{\mu}M$ respectively. They reduced the expression of protein and mRNA of COX-2 through the inhibition of I-${\kappa}B{\alpha}$ degradation and NF-$\kappa}B$ activity that were correlated with the inactivation of p38 and ERK. Therefore the active compounds from Siegesbeckia glabrescens may have therapeutic effects on neuro-inflammatory diseases through the inhibition of overproduction of $PGE_2$ and suppression of COX-2 overexpression.

• Journal of Microbiology and Biotechnology
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• v.27 no.2
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• pp.242-250
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• 2017

Anti-photoaging effects of standardized Siegesbeckia glabrescens extract (SGE) and its major active compound kirenol were investigated using Hs68 human dermal fibroblasts and hairless mice, respectively. UVB-irradiated hairless mice that received oral SGE (600 mg/kg/day) showed reduced wrinkle formation and skinfold thickness compared with the UVB-irradiated control. Furthermore, SGE treatment increased the mRNA levels of collagen synthesis genes (COL1A1, COL3A1, COL4A1, and COL7A1) and activated antioxidant enzyme (catalase), while suppressing matrix metalloproteinase (MMP-2, -3, -9, and -13) expression. In Hs68 fibroblasts, kirenol also significantly suppressed MMP expression while increasing the expression of COL1A1, COL3A1, and COL7A1. Collectively, our data demonstrate that both SGE and kirenol attenuated UVB-induced photoaging in hairless mice and fibroblasts through inhibition of the mitogen-activated protein kinases and nuclear factor kappa B pathways, suggesting that SGE has potential to serve as a natural anti-photoaging nutraceutical.

• 대한동의생리학회:학술대회논문집
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• 2005.02a
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• pp.25-25
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• 2005

• Journal of Physiology & Pathology in Korean Medicine
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• v.19 no.3
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• pp.640-646
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• 2005

This study was performed for the investigation of anticancer effects of Siegesbeckia glabrescens(SG) on HepG2 cells, a human hepatoma cell line. In the previous study, we examined the involvement of nitric oxide (NO) on anti-proliferative and apoptotic efficacy of SG in vascular smooth muscle cells. The possible mechanism of the apoptotic effects of SG was investigated in HepG2 cells. SG showed potent cytotoxic activity in HepG2 but not chang cells, liver normal cells. SG treatment caused morphological change such as cell shrinkage, nuclei condensation and cell blebbing in HepG2 cells. SG also increased the nitrite production of HepG2 cells in a dose-dependent manner. Furthermore, L-NNA treatment inhibited the anti-proliferative effect of SG. From RT-PCR, SG decreased Bcl-2 but no affected on Bax. Western blot for procaspase-3 and COX-2 showed that degradation of procaspase-3 protein level or inhibition of COX-2 protein expression by SG treatment. In addition, the apoptotic effect of SG was also demonstrated by DNA laddering. In conclusion, SG-induced HepG2 cells death can occur via apoptosis which was dose-dependent, and associated with apoptosis-related Bcl-2/Bax gene expressions, COX-2 inhibition, caspase-3 activation and NO pathway. These results suggest that SG is potentially useful as a chemotherapeutic/chemopreventive agent in hepatocellular carcinoma.

• Journal of Physiology & Pathology in Korean Medicine
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• v.20 no.5
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• pp.1233-1240
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• 2006

We have recently demonstrated that Siegesbeckia glabrescens(SG), a herbal medicine, induces apoptosis via nitric oxide(NO) production in human aortic smooth muscle cells(HASMCS). However, the molecular pathways involved in SG-mediated apoptosis are not fully understand. In the present study, we investigated the cellular mechanisms of SG-induced apoptosis in HASMCS. SG induced NO production through inducible nitric oxide synthase(iNOS) induction. The apoptotic effect of SG was attenuated by L-NNA, a NOS inhibitor. In the presence of L-NNA, the degradation of procaspase-3 by SG was inhibited. SG treatment induced a decrease in Bcl-2 expression but did not affect the expression of Bax. In addition, SG treatment evoked both down-regulation of PKC ${\alpha}$ and inhibition of PKC ${\alpha}$ phosphorylation. These downregulations were reversed by addition of L-NNA. It seems likely to De a downregulation of PKC${\alpha}$ due to long term treatment with PMA. Taken together, these results suggest that apoptotic effects of SG may be due to NO production via iNOS mRNA expression. Furthermore, Bcl-2 and PKC${\alpha}$ downregulation, and caspase-3 activation may be involved in the mechanisms for apoptotic effects by SG.

• Journal of Convergence for Information Technology
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• v.9 no.9
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• pp.245-251
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• 2019

This study was conducted to investigate the anti-oxidative, anti-oxidative and tyrosinase inhibitory effects of MeOH 80% extract and hexane, chloroform, ethyl acetate, butanol and aqueous fraction on three kinds of compositae plants in Korea. In the antimicrobial effect, the extract and chloroform fraction of Eclipta prostrata and hexane fraction of Carpesium abrotanoides L. and chloroform fraction of Siegesbeckia glabrescens exhibited significant inhibition. The antioxidant activity of ethyl acetate and butanol fractions was more than 90% in all three plants. In case of tyrosinase activity, showed a potent inhibition ethlyacetate fraction of Siegesbeckia glabrescens and Carpesium abrotanoides L, which were higher than control group. In MeOH 80% extracts, there was not found to have antimicrobial, anti-oxidant and tyrosinase inhibitory activity, however there was ethylacetate fraction of Siegesbeckia glabrescens to show effectss commonly in the three assay system.

• 대한동의생리학회:학술대회논문집
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• 2004.07a
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• pp.13-13
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• 2004