• 제목/요약/키워드: New and known compounds

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Di- and Sesqui-Terpenoids Isolated from the Pods of Sindora sumatrana and Their Potential to Inhibit Lipopolysaccharide-Induced Nitric Oxide Production

  • Jang, Dae-Sik;Min, Hye-Young;Jeong, Yeon-Hee;Lee, Sang-Kook;Seo, Eun-Kyoung
    • Archives of Pharmacal Research
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    • 제27권3호
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    • pp.291-294
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    • 2004
  • Activity-guided fractionation of the n-hexane and ${CHCl_3}-soluble$ fractions of Sindora sumatrana using a bioassay based on the inhibition of lipopolysaccharide (LPS)-induced nitric oxide (NO) production by inducible nitric oxide synthase (iNOS) in murine macrophage RAW 264.7 cells led to the isolation of the known compound, $(+)-7{\beta}-acetoxy-15,16-epoxy-3$, 13(16), 14-clero-datriene-18-oic acid (2) as an active constituent. In addition, a new trans-clerodane diterpenoid, (+)-2-oxokolavenic acid (1), together with six known compounds, (+)-3, 13-clerodadiene-16,15-olide-18-oic acid (3), $(+)-7{\beta}-acetoxy-3$,13-clerodadiene-16,15-olide-18-oic acid (4), $(+)-7{\beta}-acetoxy-16-hydroxy-3$,13-clerodadiene-16, 15-olide-18-oic acid (5), ${\beta}-caryophyllene$ oxide (6), $clovane-2{\beta},9{\beta}-diol (7),{\;}and{\;}caryolane-1,9{\beta}-diol$ (8) were isolated and found to be inactive. The structure of compound 1 was determined using physical and spectroscopic methods such as 1D and 2D-NMR experiments. The known compounds 2-8 were identified by the spectroscopic data and by comparison with the published values. Of eight isolates (1-8), only compound 2 exhibited an iNOS inhibitory activity with $IC_{50}$/ value of $51.6{\;}\mu\textrm{m}M$.

시뮬레이션 프로그램을 이용한 신규 차량의 인테리어 물질에 따른 VOC와 폼알데히드의 농도 변화에 관한 연구 (A Study on the Concentration Variations of VOCs and Formaldehyde on the Type of Interior Materials of New Vehicles by Simulation Program)

  • 이영섭;김인범;고원경
    • 한국안전학회지
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    • 제27권3호
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    • pp.89-95
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    • 2012
  • The concentrations of Volatile Organic Compounds(VOCs) and Formaldehyde(HCHO) for interior materials of new vehicles are estimated and recognized by using the simulation program known as IAQx. The concentrations of contaminants are estimated and evaluated by the ventilation rates of new domestic vehicles and the required ventilation rates for new vehicles are estimated through the given contaminant data. This study is conducted to compare the ventilation rates for the contaminants between the discontinuously ventilated new vehicles and the continuously ventilated new vehicles using the simulation program. The equation of ventilation rate of new vehicles is acquired to be able to lower initial concentrations below the standard level under different conditions for both business and personal commuting.

백렴으로부터 항산화 물질의 분리와 자외선이 조사된 사람 섬유아세포의 Matrix Metalloproteinase-1 발현에 미치는 영향 (Antioxidant Constituents from Melothria heterophylla; Regulation of Matrix Metalloproteinase-1 Expression in Ultraviolet A-irradiated Human Dermal Fibroblasts)

  • 조영호;김진희;심관섭;이범천;표형배
    • 대한화장품학회지
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    • 제31권4호
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    • pp.323-327
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    • 2005
  • 노화에 미치는 자외선의 영향에 대해 많은 연구가 진행되어 왔지만, 천연물에 대한 연구는 별로 알려진 것이 없다. MMPs는 광노화 과정에 매우 중요한 역할을 하는 것으로 알려져 있다. 본 연구에서는 MMP-1의 발현과 활성 및 항산화 효과에 미치는 $1,2,4,6-tetra-O-galloyl-{\beta}-{_D}-glucopyranose$와 3,4,5-trihydroxybenzoic acid의 효과를 측정하였다. 이들 화합물은 박과의 백렴으로부터 분리하였으며, 자유 라디칼과 활성산소 소거활성이 매우 높은 것으로 나타났다. 이들 화합물의 DPPH 라디칼과 활성산소를 50% 소거하는 활성$(SC_{50})$은 각각 $3.9{\mu}M,\;13.3{\mu}M,\;4.3{\mu}M,\;4.0{\mu}M$로 나타났다. 또한, 이들 화합물은 단백질 수준에서의 MMP-1 발현 및 활성을 처리농도 의존적으로 저해하였지만, 유전자 수준에서는 저해활성이 없는 것으로 나타났다 따라서, 이들 화합물은 단백질 수준에서의 우수한 MMP-1 발현 저해능과 높은 항산화 활성을 가지는 것을 알 수 있다. 결론적으로 이들 화합물은 새로운 항노화 소재로 적용될 수 있을 것으로 기대된다

Anti-inflammatory and PPAR Subtypes Transactivational Activities of Phenolics and Lignans from the Stem Bark of Kalopanax pictus

  • Quang, Tran Hong;Ngan, Nguyen Thi Thanh;Minh, Chau Van;Kiem, Phan Van;Nhiem, Nguyen Xuan;Tai, Bui Huu;Thao, Nguyen Phuong;Luyen, Bui Thi Thuy;Song, Seok-Bean;Kim, Young-Ho
    • Bulletin of the Korean Chemical Society
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    • 제32권11호
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    • pp.4049-4054
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    • 2011
  • A new compound, kalopanaxin F (3), and 11 known compounds (1, 2, 4-12), were isolated from the stem bark of Kalopanax pictus. Their structures were elucidated on the basis of chemical and spectroscopic methods. Five of the compounds (2, 3, 5, 6, and 12) significantly inhibited $TNF{\alpha}$-induced NF-${\kappa}B$ transcriptional activity in HepG2 cells in a dose-dependent manner, with $IC_{50}$ values ranging from 6.2 to 9.1 ${\mu}M$. Furthermore, the transcriptional inhibitory function of these compounds was confirmed based on decreases in COX-2 and iNOS gene expression in HepG2 cells. Compounds 3-7, 9, and 12 significantly activated the transcriptional activity of PPARs dose-dependently, with $EC_{50}$ values ranging from 4.1-$12.7{\mu}M$. Compounds 4 and 5 exhibited $PPAR{\alpha}$, $PPAR{\gamma}$, and $PPAR{\beta}({\delta})$ transactivational activities in a dose-dependent manner, with $EC_{50}$ values of 16.0 and 17.0, 8.7 and 16.5, 26.2 and 26.3 ${\mu}M$, respectively.

열가소성 수지의 단량체 분석 및 유해성 분류 (Analysis and hazard classification for the monomers in thermoplastic resins)

  • 이권섭;조지훈;최진희;최성봉;이종한;양정선
    • 한국산업보건학회지
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    • 제17권4호
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    • pp.322-334
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    • 2007
  • This study covers the investigation of the actual condition in the workplace to produce plastics products using synthetic resins and the investigation on the trends amount of the domestic production of thermoplastic resins. To analyze the monomers included in thermoplastic resins frequently used in the workplace, we analyzed thermal characteristics for test compounds using thermogravimetric analysis and did the qualitative analysis using Pyrolyzer GC-MSD & TDS GC-MSD. And then we classified the health hazard of monomers based on GHS classification criteria using information toxicity & carcinogenicity. The number of the workplace to produce plastics products among all domestic manufacturers of 73,884 was 4,391 (5.94%). The number of workers to produce plastics products among all workers of 2,522,750 in all domestic manufacturers was 104,971 (4.16%). The amount of production per year for thermoplastic resins is in the order of PP, HDPE, LDPE, PVC, ABS, PS and such compounds was producing over 1 Million ton per year each. The classification result based on GHS classification criteria for 22 main compounds included thermoplastic resins says 2 compounds of acrylonitrile, naphthalene are in Acute oral category 3 and benzene is in Acute dermal category 1. The classification results of health hazard of carcinogenicity based on IARC & ACGIH carcinogen classification says 2 compounds of benzene, vinyl chloride are in category 1A (known to be human carcinogens).

Differential Expression and Stability of Endogenous Nuclear Factor E2-related Factor 2 (Nrf2) by Natural Chemopreventive Compounds in HepG2 Human Hepatoma Cells

  • Jeong, Woo-Sik;Keum, Young-Sam;Chen, Chi;Jain, Mohit R.;Shen, Guoxiang;Kim, Jung-Hwan;Li, Wenge;Kong, Ah-Ng Tony
    • BMB Reports
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    • 제38권2호
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    • pp.167-176
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    • 2005
  • Nuclear factor-E2-related factor 2 (Nrf2) is known as a key regulator of ARE-mediated gene expression and the induction of Phase II detoxifying enzymes and antioxidant enzymes, which is also a common property of many chemopreventive agents. In the present study, we investigated the regulatory role of different chemopreventive agents including sulforaphane (SUL), allyl isothiocyanate (AITC), indole-3-carbinol (I3C), and parthenolide (PTL), in the expression and degradation of Nrf2 and the induction of the antioxidant enzyme HO-1. SUL strongly induced Nrf2 protein expression and ARE-mediated transcription activation, retarded degradation of Nrf2 through inhibiting Keap1, and thereby activating the transcriptional expression of HO-1. AITC was also a potent inducer of Nrf2 protein expression, ARE-reporter gene and HO-1 but had little effect on delaying the degradation of Nrf2 protein. Although PTL and I3C could induce ARE reporter gene expression and Nrf2 to some extent, they were not as potent as SUL and AITC. However, PTL dramatically induced the HO-1 expression, which was comparable to SUL, while I3C had no effect. In addition, when treated with SUL and PTL, inhibition of proteasome by MG132 did not cause additional accumulation of Nrf2, suggesting the involvement of other degradation mechanism(s) in the presence of these compounds such as SUL and PTL. In summary, the results of our current study indicated that different chemopreventive compounds have different regulatory properties on the accumulation and degradation of Nrf2 as well as the induction of cellular antioxidant enzyme HO-1.

A New Stilbene Dimer and Other Chemical Constituents from Monanthotaxis littoralis with Their Antimicrobial Activities

  • Dongmo, Arnaud Joseph Nguetse;Ekom, Steve Endeguele;Tamokou, Jean-de-Dieu;Tagousop, Cyrille Ngoufack;Harakat, Dominique;Voutquenne-Nazabadioko, Laurence;Ngnokam, David
    • Natural Product Sciences
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    • 제26권4호
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    • pp.317-325
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    • 2020
  • A new dimer stilbene [Monalittorin (1)] and ten known compounds [engeletin (2), aurantiamide acetate (3), lupeol (4), friedelin (5), quercetin (6), tiliroside (7), rutoside (8), astragalin (9), isoquercitrin (10) and quercimeritroside (11)] have been isolated from the leaves of Monanthotaxis littoralis (Annonaceae). The structures of these compounds were established by interpretation of their data, mainly, HR-TOFESIMS, 1-D NMR (1H and 13C) and 2-D NMR (1H-1H COSY, HSQC, HMBC and NOESY) and by comparison with the literature. The evaluation of their antimicrobial activities against three bacteria (Staphylococcus aureus ATCC 25923, Escherichia coli S2 (1) and Pseudomonas aeruginosa PA01) and three fungal strains (Candida albicans ATCC10231, Candida tropicalis PK233 and Cryptococcus neoformans H99) using broth micro dilution method, showed the largest antimicrobial activities of EtOAc fraction and compounds 1, 5, 6, 8 and 11 (MIC = 8 - 64 ㎍/mL). In addition, EtOAc fraction presented synergistic effect with Vancomycin and fluconazole against the tested microorganisms.

New Triterpenoids from the Fruits of Schisandra wilsoniana and Their Biological Activities

  • Gao, Xue-Mei;Li, Yun-Qi;Shu, Li-Dan;Shen, Yan-Qiong;Yang, Li-Ying;Yang, Liu-Meng;Zheng, Yong-Tang;Sun, Han-Dong;Xiao, Wei-Lie;Hu, Qiu-Fen
    • Bulletin of the Korean Chemical Society
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    • 제34권3호
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    • pp.827-830
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    • 2013
  • Investigation of an organic extract of the fruits Schisandra wilsoniana led to the isolation of two new highly oxygenated nortriterpenoids, named schilancidilactones V-W (1-2). Their structures were elucidated by spectroscopic evidence. Compounds 1-2 feature a double bond between C-7 and C-8 compared with related known nortriterpenoids isolated from the genus Schisandra. Compounds 1 and 2 were tested for their anti-HIV-1 activities and cytotoxicity. The results revealed that compounds 1 and 2 showed moderate anti-HIV-1 activities with $EC_{50}$ 3.05 and 2.87 ${\mu}g/mL$, respectively, and compound 1 showed high cytotoxicity against KB and MDA-MB-231 cell with $IC_{50}$ values of 3.18 and 5.22 ${\mu}M$, respectively.

Cytotoxic Isoflavanones from Uraria clarkei

  • Huang, Xiang-Zhong;Bai, Xi-Shan;Liang, Hui;Wang, Chao;Li, Wen-Juan;Guo, Jun-Ming;Jiang, Zhi-Yong
    • Bulletin of the Korean Chemical Society
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    • 제34권5호
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    • pp.1421-1424
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    • 2013
  • Two new isoflavanones, (3R) 5,7,3',4'-tetrahydroxy-2'-methoxyisoflavanone (1) and (3R) 5',8-di-(${\gamma}$,${\gamma}$-dimethylallyl)-2',5-dihydroxyl-4',7-dimethoxyl-isoflavanone (2), were isolated from Uraria clarkei, together with two known compounds dalbergioidin (3), 5,7-dihydroxy-2',4'-dimethoxyisoflavanone (4). The structures involving the absolute configuration of the new compounds were well elucidated by MS, IR, UV, CD, 1D and 2D NMR analyses. Cytotoxicity of the four compounds were assessed, results suggested that compound 2 possessed well cytotoxic activity, against the Hela, K562, and HL60 cell lines with $IC_{50}$ values of 28.0, 40.6 and $35.1{\mu}M$, respectively.

Acronyculatin P, A New Isoprenylated Acetophenone from the Stem Bark of Acronychia pedunculata

  • Tanjung, Mulyadi;Nurmalasari, Intan;Wilujeng, Aisyah Kanti;Saputri, Ratih Dewi;Rachmadiarti, Fida;Tjahjandarie, Tjitjik Srie
    • Natural Product Sciences
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    • 제24권4호
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    • pp.284-287
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    • 2018
  • A new isoprenylated acetophenone, acronyculatin P (1) as well as two known compounds, 3',5'-diisoprenyl-2',4'-dihydroxy-6'-methoxyphenylethanone (2) and 3'-isoprenyl-2',4',6'-trihydroxyphenylethanone (3) were isolated from the stem bark of Acronychia pedunculata (L.) Miq. The structures were determined by HRESIMS, 1D and 2D NMR. The inhibitory activity of the isoprenylated acetophenone derivatives against murine leukemia P-388 cells showed compound 1 moderate activity with $IC_{50}$ $15.42{\mu}M$.