• Journal of Microbiology and Biotechnology
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• 제26권11호
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• pp.1918-1923
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• 2016

Two baicalein derivatives, baicalin and oroxylin A, were synthesized in this study. These derivatives exhibit diverse biological activities, such as anxiolytic and anticancer activities as well as memory enhancement. In order to synthesize baicalin from aglycon baicalein using Escherichia coli, we utilized a glycosyltransferase that regioselectively transfers glucuronic acid from UDP-glucuronic acid to the 7-hydroxy group of baicalein. To increase baicalin productivity, an araA deletion E. coli mutant, which accumulates UDP-glucuronic acid, was used, and ugd, which converts UDP-glucose to UDP-glucuronic acid, was overexpressed. Using these strategies, approximately $720.3{\mu}M$ baicalin was synthesized from $1,000{\mu}M$ baicalein. Oroxylin A was then synthesized from baicalein. Two O-methyltransferases (OMTs), ROMT-15 and POMT-9, were tested to examine the production of oroxylin A from baicalein. E. coli harboring ROMT-15 and E. coli harboring POMT-9 produced reaction products that had different retention times, indicating that they are methylated at different positions; the structure of the reaction product from POMT-9 was consistent with oroxylin A, whereas that from ROMT-15 was 7-O-methyl baicalein. Using E. coli harboring POMT-9, approximately 50.3 mg/l of oroxylin A ($177{\mu}M$) was synthesized from 54 mg/l baicalein ($200{\mu}M$).

• Journal of Microbiology and Biotechnology
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• 제6권5호
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• pp.347-351
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• 1996

Flavonoid production by suspended cells of Scutellaria baicalensis Georgi was studied and the medium was optimized for cell growth and baicalin production. In SH medium the flavonoid production was not closely associated with the cell growth. A modified SH medium, FPM, was therefore designed for enhanced baicalin production. In FPM, both cell growth and baicalin production were increased by 1.5 times and 1.67 times than in the original SH medium, respectively. The increases could be attributed to the increased metabolic activities involved in the flavonoid biosynthesis as represented by enhanced activities of phenylalanine ammonia-lyase.

• Journal of Pharmaceutical Investigation
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• 제33권2호
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• pp.91-97
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• 2003

During the preparation of decoction from the mixture of Coptidis Rhizoma and Scutellariae Radix, insoluble copreciptate was formed. The coprecipitated product (COP) was composed of berberine and baicalin which was the active ingredient of Coptidis Rhizoma and Scutellariae Radix, respectively. COP was slightly soluble in water and could not be well absorbed after oral administration. This poor bioavailibility might be associated with its poor aqueous solubility. With the purpose of increasing the solubility and bioavailibility of COP, hydrolysis of COP by ${\beta}-glucuronidase$ was carried out. Hydrolyzed products (HOP) of COP were identified and assayed for active ingredients. The partition coefficient study, in situ absorption test, and pharmacokinetic study after oral administration were also performed. COP was found to be consisted of berberine and baicalin with molecular ratio of 1 to 1. This compound was hydrolyzed to berberine and baicalin by ${\beta}-glucuronidase$. The rate of hydrolysis was higher at higher temperature up to $50^{\circ}C$ and higher concentration of ${\beta}-glucuronidase$ up to 2500 unit under our experimental conditions. Baicalein, which is more liphophilic than baicalin, showed greater absorption in small intestine than baicalin did. The plasma concentrations of berberine and baicalein after oral administration of HOP were significantly higer than those of COP. The possible mechanism of increased bioavailibility of berberine and baicalein could be the hydrolysis of COP by ${\beta}-glucuronidase$. On the basis of the above results, it might be said that HOP should be a suitable preparation for increasing the bioavailibility of Coptidis Rhizoma and Scutellariae Radix.

• 동의생리병리학회지
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• 제19권4호
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• pp.922-927
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• 2005

In the present study, baicalin, baicalein, and wogonin, a major flavone isolated from Scutellaria Radix were examined for their effects on PMA-induced Interlukin-6 (IL-6), $interferon-\gamma(IFN-\gamma)$, tumor necrosis factor $(TNF)-\alpha$, IL-4, IL-10, and IL-13 productions in the PMA-stimulated $CD4^+$ Jurkat T cells. These three compounds inhibited PMA-induced Th1 cytokine $(IL-6,\;IFN-\gamma,\;TNF-\alpha)$ and Th2 cytokine (IL-4 and IL-13) productions in a concentration-dependent manner. But wogonin, but not baicalin baicalein, increased PMA-induced IL-10 production. These results suggest that baicalin, baicalein, and wogonin, a major flavone modulate Th1 and Th2 cytokine productions in $CD4^+$ Jurkat T cells and these properties may contribute to the anti-atopic dermatitis activity of Scutellaria Radix.

• 한국자원식물학회지
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• 제28권4호
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• pp.526-532
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• 2015

Scutellaria baicalensis Georgi (SJ) is a perennial plant and its root has been used in oriental traditional medicine for treatment of fever, inflammation, diarrhea and anticancer effect, etc. In this study, plant tissue culture system for SJ was developed. Stem piece of younger plant was optimum explant for callus induction and growth on MS medium supplemented with NAA 1.0 ㎎/L plus BA 0.5 ㎎/L. Plantlet regeneration through callus culture was well on MS medium containing NAA 1.0 mg/L. SJ has been known biologically active substances such as baicalin, baiclein, and wogonin. This study was carried out to examine the effect of plant growth regulators for production of baicalin, baicalein, and wogonin through callus culture. The HPLC pattern of callus extract was identical to that of standard solution, it shows that the callus produced by tissue culture has the same flavonoids composition of SJ. Baicalin, baicalein, and wogonin production was 471.5~52.8 ㎍/g, 137.6~4.0 ㎍/g, and 16.6~1.3 ㎍/g, respectively, on MS media with nine different plant growth regulator combinations. This may indicate that plant tissue culture of SJ possible to produce the biologically active substances effectively

• 한국자원식물학회지
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• 제31권6호
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• pp.652-659
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• 2018

In this study, baicalin, as a marker substance of Scutellariae Radix, was quantitatively analyzed by a high performance liquid chromatography-photodiode array detector (HPLC-DAD). We identified wogonoside, baicalein, and wogonin in the Scutellariae Radix by a high performance liquid chromatography-electrospray ionization-mass spectrometer (HPLC-ESI-MS). The baicalin was separated on a Xterra C18 column ($5{\mu}m$, $4.6{\times}250mm$) using mobile phase consisting of 38% acetonitrile in 0.68% phosphoric acid. The baicalin spectrum in the Scutellariae Radix extracts was coincided by comparing with UV-visible spectrum (200-550 nm) of baicalin standard in the library. The amount of baicalin in Scutellariae Radix was 10.46%, which is higher than KFDA's guideline. The marker substances of Scutellariae Radix showed a strong base peak $[M]^+$ in the positive detection mode following as; baicalin (m/z; $271[MH^+-sugar]^+$, $447[M+H]^+$), wogonoside (m/z; $285[MH^+-sugar]^+$, $461[M+H]^+$), baicalein (m/z; $271\;[M+H]^+$), wogonin (m/z; $285[M+H]^+$). These results are consistent with the fragment pattern and molecular weight of standard components from literature.

• 한국토양비료학회지
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• 제22권3호
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• pp.234-238
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• 1989

황금근(黃芩根)의 품질(品質)을 향상(向上)시키기 위만 합리적(合理的)인 재배법정립(栽培法定立)에 필요한 기초자료를 얻기 위하여 재배지토양이화학성(栽培地土壤理化學性) 및 황금근(黃芩根)에 함유(含有)된 무기성분함량(無機性分含量)이 baicalin함량(含量)에 미치는 영향(影響)을 조사(調査)하였다. 황금근(黃芩根) 중(中) 규소함량(奎素含量)은 0.28~1.26 %, 인함양(燐含量)은 0.17~0.46%, 가리함량(加里含量)은 1.00~1.49의 범위에 속(屬)하였다. 황금근(黃芩根) 중(中) baicalin함량(含量)은 안동산(安東産)이 11.41~14.76%, 의성산(義城産)이 13.67~16.31 %이었다. 토양(土壤) 중(中) 점토(粘土), 유기물(有機物) 및 치환성(置換性) K, Ca, Mg의 함량(含量)은 황금근(黃芩根)의 질소(窒素) 및 인(燐)의 함량(含量)과 부(負)의 상관(相關)이 인정(認定)되었다. 토양(土壤) 중(中) 치환성(置換性) 가리함량(加里含量)은 baicalin함량(含量)과 정(正)의 상관(相關)이 인정(認定)되었다. 황금근(黃芩根) 중(中) 질소(窒素) 및 인(燐)의 함량(含量)은 baicalin함량(含量)과 부(負)의 상관(相關)이 인정(認定)되었으나, 가리함량(加里含量)은 유의성(有意性)이 없었다.

• 한국식품저장유통학회지
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• 제12권4호
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• pp.350-354
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• 2005

황금의 천연항균제 개발을 위하여 황금의 일반성분 및 미량물질들을 분석하였으며 항균활성물질의 검색을 위하여 LC-MS를 이용하였고 검색되어진 성분들에 대해서는 항균력 비교시험을 하였으며 항균활성물질들에 대해서는 HPLC를 이용하여 그 양을 정량하였다. 황금의 일반성분으로는 수분 $8.93\%$, 탄수화물 $67.93\%$, 조회분 $4.13\%$, 조단백질 $15.30\%$ 및 조지방 $3.71\%$ 이었고 미량성분에 있어서는 칼륨 12,050mg/kg과 마그네슘4,296 mg/kg의 함량이 현저하게 높았다. LC-MS 분석결과 황금추출물에 있어서 분자량 445의 peak는 baicalin, 분자량 283의 peak는 wogonin, 분자량 269의 peak는 baicalein으로 확인되었다. disk method를 이용하여 항균력을 시험한 결과 baicalin이 주된 항균물질임을 추정할 수 있었으며, 메탄올 및 물추출물의 baicalin 함량을 분석한 결과 물추출물은 $0.75\%$이었고 메탄올추출물은 $0.82\%$로서 메탄올추출물에 있어서 baicalin 함량이 약간 높은 결과를 얻었다.

• 분석과학
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• 제10권2호
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• pp.91-104
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• 1997

황금은 예로부터 한방의학에서 해독작용에 사용되어 왔다. 이제까지 황금의 분석적인 관점은 황금의 주성분에 대한 분리와 감도를 증대시키는 데 있었다. 황금에 존재하는 세 가지 다른 flavonoid인 baicalin, baicalein, wogonin을 분석하기 위하여 diode array 검출기(280nm)와 ODS 역상 컬럼을 사용하여 HPLC로 측정하였다. 이 때 이동상은 아세토니트릴과 0.1M 인산을 사용하고, flow rate는 1mL/min로 하였다. 이 조건에서의 검출시간은 baicalin이 7.65분, baicalein이 11.65분, wogonin이 14.12분이었다. 이 분석방법으로서 산지에 따른 황금성분의 양을 비교한 결과 baicalin은 전북 순창산에서, baicalein과 wogonin은 전남 벌교산에서 많이 검출되었다. 추출효율 실험결과 상온용출도 우수하였다. 산의 종류 중 특히 0.2M 초산을 사용했을 때 추출효율이 가장 좋았으며, 추출의 효율성이나 안정성을 고려할 때 혼합 용매의 비율은 아세토니트릴/0.2M 인산(75:25)의 조건에서 추출하는 것이 우수하였다.

• 한국식품위생안전성학회지
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• 제32권3호
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• pp.193-198
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• 2017

본 연구는 건강기능식품 중 baicalin, eleutheroside E, ligustilide를 효과적으로 분석할 수 있는 방법을 확립하기 위하여 수행되었다. 이에 LC-MS/MS를 이용하여 신속하고 효율적으로 동시분석할 수 있는 시험법을 확립하였으며, 확립된 시험법에 대해 특이성, 검출한계, 정량한계, 정확도, 정밀도에 대한 검증을 통하여 유효성을 확인하고자 하였다. 표준용액을 이용하여 검량선을 작성한 결과 $r^2$ > 0.99 이상의 직선성을 확인하였고, baicalin, eleutheroside E, ligustilide에 대한 정량한계는 각각 $39.3{\mu}g/L$, $106.7{\mu}g/L$, $76.1{\mu}g/L$이었으며, 검출한계는 각각 $13.0{\mu}g/L$, $35.2{\mu}g/L$, $25.1{\mu}g/L$이었다. 또한 평균 회수율은 각 성분에 대해 108.0~109.9%, 99.8~101.3%, 91.4~97.2%로 나타났으며, 반복정밀도는 상대표준편차 5%이하, 실험실간 재현성은 9%이하로 나타나 정확성, 재현성이 우수하였으며 이는 AOAC 가이드라인에서 제시한 기준에 모두 적합한 수준이었다. 따라서 개발된 분석법은 향후 건강기능식품 중 baicalin, eleutheroside E, ligustilide를 동시분석하는데 효과적으로 활용할 수 있을 것으로 판단된다.