• The Korea Journal of Herbology
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• v.38 no.6
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• pp.45-52
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• 2023

Objectives : Effects of baicalein (BA) on oxidative stress in RAW 264.7 mouse macrophages stimulated with peptidoglycan (PG) and lipopolysaccharide (LPS) were investigated. Methods : RAW 264.7 co-stimulated with LPS and PG were incubated with BA at concentrations of 25 and 50 µM. Incubation time was 18 h, 20 h, 22 h, 24 h, and 26 h. After incubation, the production of hydrogen peroxide in RAW 264.7 was measured with dihydrorhodamine 123 assay. Additionally, RAW 264.7 stimulated with PG were incubated with BA at concentrations of 25 and 50 µM for 24 h. After incubation, NO production was evaluated by griess reagent assay. Results : BA significantly inhibited hydrogen peroxide productions (p <0.05). In details, production of hydrogen peroxide in 'LPS and PG'-stimulated RAW 264.7 treated for 18 h with BA at concentrations of 25 and 50 µM was 91.27% and 89.22% of the control group treated with LPS and PG only, respectively; the production of hydrogen peroxide for 20 h was 92.19% and 90.58%, respectively; production of hydrogen peroxide for 22 h was 91.69% and 89.89%, respectively; production of hydrogen peroxide for 24 h was 92.4% and 90.19%, respectively; production of hydrogen peroxide for 26 h was 91.7% and 89.04%, respectively. Additionally, BA at the concentration of 50 and 100 µM significantly inhibited NO production in PG-induced RAW 264.7 (p <0.05). Conclusions : BA might have anti-oxidative activity related to its inhibition of hydrogen peroxide production in 'LPS and PG'-stimulated RAW 264.7 macrophages.

• Korean Journal of Food Science and Technology
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• v.34 no.3
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• pp.505-509
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• 2002

In the course of screening program for VHR DS-PTPase (dual-specificity protein tyrosine phosphatase) from natural sources, Gastrodia elata was selected. One compound showing potent inhibitory activity was isolated by the solvent extraction and column chromatography including silica gel, ODS RP-18, Sephades LH-20, and HPLC. This compound was identified as baicalein by several NMR techniques such as $^1H-NMR$, $^{13}C-NMR$, and DEPT. Baicalein showed selective inhibitory activity against VHR DS-PTPase with $IC_{50}=2.4\;{\mu}M$, and showed cytotoxicity against several human cancer cell lines with an $GI_{50}$ of $5.26{\sim}12.93\;{\mu}g/mL$ range, including, melanoma (LOX-IMVI), lung cancer (NCI H23 and A549), colon cancer (HCT 116 and SW 620), prostate cancer (PC-3), and leukemia (MOLT 4F).

• Natural Product Sciences
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• v.20 no.2
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• pp.102-106
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• 2014

Gumiganghwal-tang (GMT) is a traditional herbal prescription used for treatment of the common cold, pain, and inflammatory diseases. Variations in the amounts of bioactive components of GMT and GMT fermented with 10 Lactobacillus strains were investigated by high-performance liquid chromatography coupled with diode array detection (HPLC-DAD). Simultaneous qualitative and quantitative analyses of eleven bioactive compounds (prim-O-glucosylcimifugin, liquiritin, cimifugin, baicalin, liquiritigenin, wogonoside, baicalein, wogonin, butylphthalide, imperatorin, and isoimperatorin) were performed, with comparison of their retention times (tR) and UV spectra with those of standard compounds. The amounts of baicalin (8.71 mg/g), liquiritigenin (5.28 mg/g) and butylphthalide (5.10 mg/g) were the major compounds in GMT. We found that L. fermentum KFRI 145 fermented wogonoside and baicalin to their aglycones, wogonin and baicalein, respectively. These results indicated that L. fermentum KFRI 145 has potential as a functional starter culture for manufacturing fermented GMT.

• Natural Product Sciences
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• v.23 no.1
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• pp.46-52
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• 2017

The aim of this study was to evaluate the anti-Helicobacter pylori activity of fractions and major aglycon compounds (baicalein, chrysin, oroxylin A, wogonin) of Scutellariae Radix. Minimum inhibitory concentration (MIC) measurement, DPPH radical-scavenging assay, DNA protection assay, and urease inhibition analysis were performed. The ethyl acetate (EtOAc) fraction showed the potent anti-Helicobacter activity, and therefore, compounds in the EtOAc fraction were subjected to further assay. The MICs of chrysin, oroxylin A, and wogonin against Helicobacter pylori 26695 were 6.25, 12.5 and $25{\mu}g/mL$, respectively. Baicalein exhibited the most effective DPPH radical-scavenging activity. DNA protection using Fenton reaction, chrysin, oroxylin A, and wogonin showed effective DNA protective effect. This result was also confirmed by quantitative real-time polymerase chain reaction (qRT-PCR). Regarding Jack bean urease (0.5 mg/mL, 50 unit/mg) inhibition, 20 mM ofbaicalein and chrysin inhibited urease activity by 88.2% and 72.5%, respectively.

• Korean Journal of Plant Resources
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• v.27 no.6
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• pp.635-641
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• 2014

Scutellaria baicalensis $G_{EORGI}$ (Scutellariae Radix) has been used to clear heat and to dry dampness in the stomach or intestines, which manifests as diarrhea or dysenteric disorder. In this study, we investigated the effective preparation of active components in Scutellariae Radix using the methods of solvent extraction and absorption fractionation for the development of new functional food or pharmaceuticals. The marker substances, baicalin, baicalein, wogonoside, and wogonin were directly isolated from the Scutellariae Radix. There chemical structures were elucidated by spectroscopic analysis. The Scutellariae Radix was extracted with hot water. To enhance yield of flavonoids in Scutellariae Radix, the hot water extract was dissolved in ethanol with concentration dependent manner. The precipitates were separated using centrifugal techniques at 10,000 rpm. Supernatant liquid was applied to the HPLC for quantification of major compounds. Separately, the hot water extract was absorbed on Diaion HP-20 resin. And then, the absorbed fraction was eluted with methanol for HPLC. The contents of baicalin, baicalein, wogonoside and wogonin in different treatment methods were analyzed by HPLC. Total amount of four major components were 16.9% in 50% ethanol extract, 21.7% in 70% ethanol extract, 20.5% in 90% ethanol extract, and 39.3% in absorbed fraction of Diaion HP-20 resin. In these results, we found that resin absorption method is suitable for the extraction of enriched flavonoids from Scutellariae Radix.

• Journal of Practical Agriculture & Fisheries Research
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• v.25 no.1
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• pp.20-35
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• 2023

Chemical preservatives have a good effect on antibacterial activity, but many side effects on the human body have been reported. Recently, the development of natural preservatives that are harmless to the human body and have preservative functions and self-efficacy is active. In addition, in order to increase the absorption rate of natural products by the human body, the method of fermentation using strains is also increasing. Therefore, this study selected varieties that are harmless to the human body and have good antibacterial activity. 1. The yield of origin, thickness and solvent was investigated. Scutellaria baicalensis Georgi was made in China and received a yield of 21.88% from 50% ethyl alcohol extract. Salvia miltiorrhiza Bunge was made in Korea and received a yield of 25.62% from 50% ethyl alcohol extract. Dryopteris crassirhizoma Nakai was made in China and received a yield of 6.50% from 70% ethyl alcohol extract. 2. The solid fermentation with the S. baicalensis and S. miltiorrhiza with B. Subtilis yield gained 24.40%, 39.30%, and D. crassirhizoma obtained 11.10% yield when fermented with L. casei. 3. After the liquid fermentation, a clear zone of 9mm was identified for the S. aureus strain in the S. baicalensis, and the antibacterial activity was not confirmed in S. miltiorrhiza and D. crassirhizoma. 4. When the S. baicalensis was fermented with L. Casei, it showed high antibacterial activity in C. albicans and S. aureus. S. miltiorrhiza showed antibacterial activity in S. aureus when it was solid with S. cerevisiae. When the spectators were solid with L. casei and S. cerevisiae, antibacterial activity was high in E. coli and S. aureus. Overall, the antibacterial activity after fermentation was much higher than when fermented. 5. The change in active ingredients was baicalin 101.57, baicalein 28.26, and wogonin 5.33mg/g in the S. baicalensis that did not ferment solid. When solid fermentation with S. cerevisiae, the content of baicalinin with baicalin 94.31, baicalein 30.41, and wogonin 3.57mg/g was found to have increased. S. miltiorrhiza that was not fermented, salvianolic acid A was 1.82mg/g, and when fermented with S. cerevisiae, it increased to 5.70mg/g. The active ingredients of the spectators were flavaspidic acid AP, flavaspidic acid PB, flavaspidic acid AB, and flavaspidic acid BB.

• The Korean Journal of Physiology and Pharmacology
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• v.17 no.5
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• pp.393-403
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• 2013

Baicalein (BA), a plant-derived active flavonoid present in the root of Scutellaria baicalensis, has been widely used for the treatment of stress-related neuropsychiatric disorders including depression. Previous studies have demonstrated that repeated restraint stress disrupts the activity of the hypothalamic-pituitary-adrenal (HPA) axis, resulting in depression. The behavioral and neurochemical basis of the BA effect on depression remain unclear. The present study used the forced swimming test (FST) and changes in brain neurotransmitter levels to confirm the impact of BA on repeated restraint stress-induced behavioral and neurochemical changes in rats. Male rats received 10, 20, or 40 mg/kg BA (i.p.) 30 min prior to daily exposure to repeated restraint stress (2 h/day) for 14 days. Activation of the HPA axis in response to repeated restraint stress was confirmed by measuring serum corticosterone levels and the expression of corticotrophin-releasing factor in the hypothalamus. Daily BA administration significantly decreased the duration of immobility in the FST, increased sucrose consumption, and restored the stress-related decreases in dopamine concentrations in the hippocampus to near normal levels. BA significantly inhibited the stress-induced decrease in neuronal tyrosine hydroxylase immunoreactivity in the ventral tegmental area and the expression of brain-derived neurotrophic factor (BDNF) mRNA in the hippocampus. Taken together, these findings indicate that administration of BA prior to the repeated restraint stress significantly improves helpless behaviors and depressive symptoms, possibly by preventing the decrease in dopamine and BDNF expression. Thus, BA may be a useful agent for the treatment or alleviation of the complex symptoms associated with depression.

• Asian Pacific Journal of Cancer Prevention
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• v.14 no.12
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• pp.7179-7186
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• 2013

Background and Aims: Scutellaria is one of the most popular traditional Chinese herbal remedies against various human diseases, including cancer. In this study, we examined the active effects of Scutellaria extract and its main flavonoid constituents on the proportion of side population cells within human multiple myeloma cell line RPMI8226 in vitro and explored the potential molecular mechanisms involved. Materials and Methods: The contents of flavonoids in ethanolic extract of Scutellaria baicalensis Georgi were determined using high performance liquid chromatography. The antiproliferative effect of the ethanolic extract on RPMI-8226 was determined by CCK assay. Apoptosis was measured by annexin combining with propidium iodide in a flow cytometer. Cell cycle analysis was performed by propidium iodide staining in combination with flow cytometry analysis. Hoechst 33342 exclusion assay was used for the identification of side population within RPMI8226 cells. The expression of ABCG2 protein was assessed by Western blotting assay. Results: The content of major flavonoids constitutents of Scutellaria extract was baicalin (10.2%), wogonoside (2.50%), baicalein (2.29%), and wogonin (0.99%), respectively. The crude Scutellaria extract did not show significant anti-proliferative effect, apoptosis induction and cell cycle arrest in RPMI-8226 within the concentrations of $1-75{\mu}g/mL$. However, the ethanolic extract, baicalein, wogonin and baicalin reduced the side population cells in RPMI-8226, and data showed that baicalein and wogonin had stronger inhibitory effects. Correspondingly, they also exhibited significant effects on decreasing the expression level of ABCG2 protein in RPMI-8226 in vitro. Conclusions: Our results for the first time demonstrated a novel mechanism of action for Scutellaria extract and its main active flavonoids, namely targeting SP cells by modulating the expression of ABCG2 protein. This study provides an insight for new therapeutic strategies targeting cancer stem cells of multiple myeloma.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.43 no.3
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• pp.201-210
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• 2017

Scutellariae baicalensis (S. baicalensis) has been traditionally used for anti-inflammatory effect. This study was designed to compare the antioxidant and whitening effects of S. baicalensis extract and its fermented extract by Leuconostoc mesenteroides (L. mesenteroides). Fermented extract of S. baicalenins was prepared by inoculation of L. mesenteroides after the extraction procedure with 70% ethanol. S. baicalensis extract and its fermented extract was investigated via high-performance liquid chromatography (HPLC). Simultaneous qualitative analysis of two bioactive components; baicalin and baicalein was achieved by comparing their retention times ($t_R$) and UV spectra with those of the standard components. Cell viability test results indicated that both S. baicalensis extract and its fermented extract were non-toxicity. In DPPH radical scavenging ability, $SC_{50}$ values of the fermented extract was $34.43{\mu}g/mL$ as a result of more effective than S. baicalensis extract. In nontoxic concentration rage, fermented extract of S. baicalensis showed strong melanin production inhibitory effect in ${\alpha}$-melanocyte stimulating hormone (MSH)-stimulated B16F10 cell ($IC_{50}=68.17{\mu}g/mL$). These results suggested that fermented extracts of S. baicalensis has considerable potential as a cosmetics ingredient with an antioxidant and anti-wrinkle and whitening effects.

• Food Science and Preservation
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• v.12 no.4
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• pp.350-354
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• 2005

It was carried out for development of natural antimicrobial on Scutellariae Radix by measuring the general nutritional composition and mineral contents. This study analyzed it with LC-MS to identify antimicrobial activity substance in the Scutellariae Radix extract, its content was analyzed using HPLC. The searching substance was examined antimicrobial activity by disk method. The approximate composition of Scutellariae Radix was $8.93\%$ of moisture, $4.13\%$ of crude ash, $15.30\%$ of crude protein, $3.71\%$ of crude fat, $67.93\%$ of carbohydrate, respectively. Scutellariae Radix was contained high contents of minerals such as K(12,050 mg/kg),. Mg(4,295 mg/kg), remarkably. It was identified that molecular weight 445' peak was baicalin, molecular weight 283' peak was wogonin and molecular weight 269' peak was baicalein on Scutellariae Radix extract Baicalin showed remarkable antimicrobial activity against V. parahaemolyticus and L monocytogenes when examined by disk method, which was estimated antimicrobial activity substance in the Scutellariae Radix extract. The content of baicalin was $0.75\%$(with D.W.) and $0.82\%$(with methanol) in the Scutellariae Radix extract using HPLC.