• 생명과학회지
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• 제32권2호
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• pp.86-93
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• 2022

Lupeol은 pentacyclic triterpene의 일종으로 다양한 질병에 약리 효과가 있는 것으로 보고되어 있으나, lupeol이 포도당 흡수에 미치는 영향은 아직 보고된 바 없다. 본 연구에서 3T3-L1 지방세포에서 포도당 흡수에 대한 lupeol의 효과를 조사하였다. 그 결과, Lupeol은 3T3-L1 지방세포에서 GLUT4를 원형질막으로 이동시켜 포도당 흡수를 촉진하였으며, 이는 PI3K/AKT 및 AMPK 경로의 활성화와 관련되어 있었다. PI3K/AKT 경로에서 lupeol은 PI3K를 활성화시키는 insulin receptor substrate 1의 인산화와 AKT의 인산화를 촉진하지만 비정형 단백질 키나아제 C isoforms ζ 및 λ의 인산화는 촉진하지 않았다. 반면, lupeol은 5 'AMP-activated protein kinase의 인산화를 촉진하였고, Lupeol의 의한 AMPK의 활성화는 원형질막-GLUT4의 발현과 세포내 포도당 흡수를 증가시키는 것으로 확인되었다. 3T3-L1 지방세포에서 lupeol에 의한 포도당 흡수 효과는 PI3K 억제제인 wortmannin 및 AMPK 억제제인 Compound C에 의해 억제됨을 통해 확인하였다. 본 연구 결과는 lupeol이 3T3-L1 지방세포에서 PI3K/AKT 및 AMPK 경로를 통해 원형질막 GLUT4의 발현을 자극함으로써 인슐린 감수성을 증가시켜 포도당 흡수를 촉진할 수 있음을 제시하고 있다.

• 분석과학
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• 제12권2호
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• pp.136-140
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• 1999

Sorbus Cortex를 실리카겔 칼럼크로마토그래피하여 lupane계 triterpenoids인 lupenone과 lupeol을 분리, 분광학적 방법으로 화학적 구조를 확인한 후 그 화합물들을 3종의 Sorbus Cortex에 대한 정량분석 표준품으로 이용하였다. Lupenone과 lupeol은 VA-5MS[(5%-phenyl)methylpolysiloxane, $30m{\times}0.25mm$, $0.25{\mu}m$] 칼럼으로 기체크로마토그래피법으로 분석하였으며 lupenone과 lupeol의 함량은 시료의 종류에 관계없이 각각 0.050~0.056%와 0.772~0.834%로 나타났다.

• Natural Product Sciences
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• 제7권3호
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• pp.76-82
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• 2001

The pharmacological activities of the acetonitrile (MeCN), hexane extracts and isolated pure terpenoidal compound Lupeol from the leaves of Teclea nobilis, Delile (TN), on inflammation induced by carrageenan an implantation of cotton pellets in rats; the nociceptive response using writhing and tail flick tests and the antipyretic activity in yeast-induced fever were examined in mice. Oral administration of TN extracts at doses of 150 and 300 mg/ks and lupeol 5 and 10 mg/kg showed a significant anti-inflammatory activity in rats. The extracts of TN and lupeol significantly decreased the number of contractions and stretchings induced by acetic acid and heat-induced pain in mice. The antipyretic effect of extracts and lupeol was also found to be significant. The behavioral observation of animals showed that the hexane extract and lupeol caused CNS depressant activity and did not produce any toxic or lethal effects in animals at various dose levels. The results suggest that the Teclea nobilis extracts and lupeol possesses anti-inflammatory, analgesic and antipyretic activities.

• 한국작물학회:학술대회논문집
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• 한국작물학회 2022년도 추계학술대회
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• pp.253-253
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• 2022

Codonopsis lanceolata (C. lanceolata) has been widely used in East Asia as a traditional medicine to treat various diseases such as bronchitis, convulsions, cough, obesity, and hepatitis. C. lanceolata belonging to Campanulaceae contains bioactive compounds such as polyphenols, saponins, and steroids. However, despite the pharmacological significance of C. lanceolata, the genetic information of this plant is limited and there are few studies of its transcriptome. In this study, we constructed a unigene set of C. lanceolata using Pac-Bio sequencing. Furthermore, the reads generated from Pac-bio and Illumina sequencing were mixed and assembled using rnaSPAdes. All genes involved in the triterpenoid pathway, a major bioactive compounds of C. lanceolata, were searched from the two unigene sets and the expression profiles of these genes were analyzed. The results showed that lupeol, beta-amyrin, and dammarenediol synthesis genes were activated in the leaves and roots of C. lanceolata. In particular, the expression of genes related to lupeol synthesis was relatively high, suggesting that the main triterpenoid of C. lanceolata is lupeol. Transcriptome studies related to lupeol synthesis in C. lanceolata have been rarely reported. Lupeol has been reported to have pharmacological effects such as anti-inflammatory, anti-cancer, and anti-bacterial. This study suggests the importance of C. lanceolata as a lupeol producing plant.

• 대한본초학회지
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• 제32권5호
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• pp.27-38
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• 2017

Objective : In the present study, we examined whether Canavalia gladiata D.C. (CG) and Arctium lappa L., Redix (AL) mixture (CGAL), their components, lupeol and chicoric acid, regulate immune system and suppress the tumor in vitro and in vivo. Methods : LPS-induced reactive oxygen species (ROS) and nitric oxide (NO) were measured after treatment with CG extract (CGE), CGAL, lupeol, chicoric acid and lupeol and chicoric acid mixture (lupeol+CA) in Raw264.7 cell. To determine the effect of CGE on immune responses, immune cell population and IgG production were assessed in mice. To investigate the effect of CGAL and their component on anti-tumor activity, tumor volume and weight were measured, cell cycles and immune cell population were analyzed in MC38 injected tumor bearing mice. Also, NK cell activity was determined in splenocyte isolated from tumor bearing mice. Results : CGE, CGAL, lupeol, chicoric acid and lupeol+CA decreased the LPS-induced ROS and NO production without cell toxicity in RAW264.7 cells. CGE increased the immune cell populations of $CD4^+T$, $CD8^+T$ and macrophages in various immune organ of mice. In tumor bearing mice, CGAL, lupeol, chicoric acid and lupeol+CA suppressed tumor volume and weight. In cell cycle analysis, they decreased the percentages of S phase. In addition, CGAL, lupeol, chicoric acid and lupeol+CA immune cell populations of $CD4^+T$, $CD8^+Tcell$, NK cell and macrophage in tumor as well as NK cell activity. Conclusion : CGAL and its compounds may enhance immune responses and suppress tumor growth, and may be capable of developing health functional foods.

• Tuberculosis and Respiratory Diseases
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• 제78권3호
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• pp.210-217
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• 2015

Background: Adenophora triphylla var. japonica is empirically used for controlling airway inflammatory diseases in folk medicine. We evaluated the gene expression and production of mucin from airway epithelial cells in response to lupenone, lupeol and taraxerol derived from Adenophora triphylla var. japonica. Methods: Confluent NCI-H292 cells were pretreated with lupenone, lupeol or taraxerol for 30 minutes and then stimulated with tumor necrosis factor ${\alpha}$ (TNF-${\alpha}$) for 24 hours. The MUC5AC mucin gene expression and production were measured by reverse transcription-polymerase chain reaction and enzyme-linked immunosorbent assay, respectively. Additionally, we examined whether lupenone, lupeol or taraxerol affects MUC5AC mucin production induced by epidermal growth factor (EGF) and phorbol 12-myristate 13-acetate (PMA), the other 2 stimulators of airway mucin production. Results: Lupenone, lupeol, and taraxerol inhibited the gene expression and production of MUC5AC mucin induced by TNF-${\alpha}$ from NCI-H292 cells, respectively. The 3 compounds inhibited the EGF or PMA-induced production of MUC5AC mucin in NCI-H292 cells. Conclusion: These results indicated that lupenone, lupeol and taraxerol derived from Adenophora triphylla var. japonica regulates the production and gene expression of mucin, by directly acting on airway epithelial cells. In addition, the results partly explain the mechanism of of Adenophora triphylla var. japonica as a traditional remedy for diverse inflammatory pulmonary diseases.

• 생명과학회지
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• 제33권11호
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• pp.859-867
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• 2023

루페올은 5환성 트리테르펜의 일종으로 많은 질병에 치료 효과가 있는 것으로 보고되었으나, 인슐린 저항성에 미치는 영향은 명확하지 않다. 본 연구에서는 3T3-L1 지방세포에서 루페올의 IRS-1 인산화 억제능을 통해 인슐린 저항성 개선효과를 조사하였다. 3T3-L1 세포를 배양하고 TNF-α를 24시간 동안 처리하여 인슐린 저항성을 유도하였다. 서로 다른 농도의 루페올(15, 30 μM) 또는 100 nM의 rosiglitazone을 처리한 세포를 배양한 후, 용해된 세포를 이용하여 western blotting을 시행하였다. 실험결과 루페올은 지방세포에서 TNF-α에 의해 유발되는 인슐린 신호전달의 음성 조절자와 염증 활성화 단백질 kinase에 대한 개선 효과를 나타냈다. 인슐린 신호전달의 음성 조절자인 PTP-1B와 JNK의 활성 및 IKK와 염증활성화 단백질키나아제의 활성을 억제하였다. 또한, 루페올은 IRS-1의 serine 인산화는 하향 조절하고 tyrosine 인산화는 상향 조절하였다. 그 후, 하향 조절된 PI3K/AKT 경로가 활성화되고, GLUT 4의 세포막 전위가 자극되어, 결과적으로 인슐린 저항성이 유도된 3T3-L1 지방세포에서에서 세포내 포도당 흡수가 증가하였다. 본 연구결과, 루페올은 3T3-L1 지방세포에서 인슐린 신호전달 및 염증 활성화 단백질 kinsase들의 음성 조절인자를 억제하여, IRS-1의 serine 인산화를 하향 조절함으로써 TNF-α 유발 인슐린 저항성을 개선할 수 있을 것으로 사료된다.

• Asian Pacific Journal of Cancer Prevention
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• 제13권11호
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• pp.5753-5757
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• 2012

Apoptosis, also known as cell suicide or programmed cell death, removes unwanted and genetically damaged cells from the body. Evasion of apoptosis is one of the major characteristic features of rapidly proliferating tumor cells. Chemopreventive agents inhibit or suppress tumor formation through apoptotic induction in target tissues. The aim of the present study was to investigate the pro-apoptotic potential of lupeol during 7,12-dimethylbenz(a) anthracene (DMBA) induced hamster buccal pouch carcinogenesis. Topical application of 0.5% DMBA three times a week for 14 weeks in the buccal pouches of golden Syrian hamsters resulted in oral squamous cell carcinoma. The expression pattern of apoptotic markers was analyzed using immunohistochemistry (p53, Bcl-2, Bax) and ELISA reader (caspase 3 and 9). In the present study, 100% tumor formation with defects in apoptotic markerexpression pattern was noticed in hamsters treated with DMBA alone. Oral administration of lupeol at a dose of 50mg/kg bw completely prevented the formation oral tumors as well as decreased the expression p53 and Bcl-2, while increasing the expression of Bax and the activities of caspase 3 and 9. The present study thus indicated that lupeol might inhibit DMBA-induced oral tumor formation through its pro-apoptotic potential in golden Syrian hamsters.

• Archives of Pharmacal Research
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• 제25권5호
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• pp.617-620
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• 2002

Six compounds were isolated from the twigs of Ilex macropoda. Their structures were elucidated as betulinic acid, lupeol, betulone, betulin, erythrodiol and 11-oxo-erythrodiol by physicochemical and spectroscopic analysis. Among them, lupeol, betulone, erythrodiol and 11-oxo-erythrodiol were isolated for the first time from this plant.

• Natural Product Sciences
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• 제18권1호
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• pp.13-15
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• 2012

Three lupane type triterpenoids were isolated from the methanol extract of Pyrus pyrifolia fruit peel through repeated silica gel column chromatography. Based on the spectroscopic methods, their structures were determined to be lupeol (1), betulin (2), and betulinic acid (3).