• 제목/요약/키워드: 7 against 3

검색결과 4,874건 처리시간 0.029초

Prediction of the Antagonistic Activity of Aryl Benzyl Ethers against LTD4 by Using 3D-CoMFA Model Developed with Pranlukast Analogues

  • Kim, Jin-young;Lee, Mi-ryung;Kang, Seock-yong;Park, Jin-a;Lim, Yoong-ho;Koh, Dong-soo;Park, Kwan-Ha;Chong, You-hoon
    • Bulletin of the Korean Chemical Society
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    • 제27권7호
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    • pp.1025-1030
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    • 2006
  • A 3D-CoMFA model with pranlukast analogues was constructed, which could be applied to predict the antagonistic activity of aryl benzyl ether analogues against LTD4. Molecular modeling and 3D-CoMFA studies were performed on 78 pranlukast analogues and 14 aryl benzyl ethers to evaluate the antagonistic behavior of aryl benzyl ethers and provide information for further modification of this kind of compounds. The aryl benzyl ether core was found to be in excellent three dimensional match with the central planar moiety of pranlukast analogues, and the pranlukast 3D-CoMFA model could be successfully applied to predict the biological activity of aryl benzyl ether analogues.

Biological Activities of Methyl-4-[[(2E)-3,7-dimethyl-oxy]-3-hydroxybenzoate

  • Baek, Seung-Hwa;Oh, Hyun-Ju;Lim, Jin-A;Chun, Hyun-Ja;Lee, Hyun-Ok;Ahn, Jong-Woong;Perry, Nigel B.;Kim, Hyung-Min
    • Bulletin of the Korean Chemical Society
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    • 제25권2호
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    • pp.195-197
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    • 2004
  • Methyl-4-[[(2E)-3,7-dimethyl-2,6-octadienyl]oxy]-3-hydroxybenzoate (5) has been identified from the New Zealand liverwort Trichocolea hatcheri (T. hatcheri) on the basis of spectroscopic evidence. This compound was tested for its growth inhibitory effects against tumor cell lines, using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay. It showed growth inhibition activity against Staphylococcus epidermidis (MIC, 1,000 ${\mu}$g/mL). These results suggest that compound 5 possesses antitumoral , antimicrobial and antioxidative activities.

The issue of vaccine refusal: the study of a risky behavior

  • Mikhail Osadchuk;Yuliya Tikhonova;Mariya Krivetskaya
    • Clinical and Experimental Vaccine Research
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    • 제12권3호
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    • pp.216-223
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    • 2023
  • Purpose: Influenza is the most common seasonal infectious disease that causes permanent social, economic, and medical problems worldwide. Therefore, the most effective way to prevent influenza is through vaccines. The aim of this study is to identify the influence of factors that determine the refusal of influenza vaccine among three subjects groups. Materials and Methods: A survey was conducted amongst the three high-risk groups in 2018-2019 (Moscow, Russia). The survey involved 1,620 parents and pregnant women (group 1), 324 doctors (group 2), and 433 students (group 3). Poor vaccine uptake was observed among respondents in all three groups. Results: According to the survey results, only 22.2% of children and 13.8% of adults were vaccinated against influenza. Group 2 showed increased rates with 36.7% of vaccinated adults and 58.7% of children. The lowest adherence to annual vaccinations was recorded in group 3 (only 17.3%). There is also a negative correlation between adherence to vaccination and smoking (-0.66), unhealthy diet (-0.73), poor oral hygiene (-0.61), and insufficient awareness of the need for influenza vaccine as well (-0.81). Conclusion: Thus, a general lack of vaccination awareness has a fundamental role in forming a negative attitude toward influenza vaccine. It is necessary to conduct research to promote vaccination against influenza to improve vaccine uptake among high-risk groups, particularly students.

적조생물 살조세균 탐색 II. 적조생물 Prorocentrum micans 살조세균 Pseudomonas sp. LG-2의 분리와 살조특성 (Isolation of Marine Bacteria Killing Red Tide Microalgae II. Isolation and Algicidal Properties of Pseudomonas sp. LG-2 Possessing Killing Activity for Dinoflagellate, Prorocentrum micans)

  • 이원재;박영태
    • 한국수산과학회지
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    • 제31권6호
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    • pp.852-858
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    • 1998
  • 1996년 7월 마산만의 해수를 0.8 $\mu$m filter에 여과한 여과액과 f/2배지에서 배양한 P. micans와의 혼합배양액에서 P. micans를 사멸시키는 해양세균을 분리하였다. 분리균의 형태학적 및 생화학적 검사와 균체지방산을 분석하여 동정한 결과 Pseudomonas 속으로 동정되어 Pseudomonas sp. LG-2로 명명하였으며, 그 살조특성을 조사한 결과는 아래와 같다. Pseudomonas sp. LG-2의 개체수와 배양여과액의 농도가 높을수록 P. micans의 사멸효과가 높게 나타났다. $1.3\times10^5,\;1.3\times10^6$ cells/ml의 농도로 접종한 시험관의 P. micans는 급격히 감소하여 배양 7일 후에는 $10^2$ cells/ml 이하로 사멸되었다. 또한, 배양석과액의 최종농도가 $30\%$일 경우에는 급격히 감소하여 배양 3일 후 거의 사멸하였다. Pseudomonas sp. LG-2의 성장시기에 따른 배양여과액의 사멸효과는 잠복기의 경우 P. micans의 성장에 큰 영향을 미치지 않았으나, 대수증식기 중기의 배양여과액은 접종 5일 후 P. micans의 개체수를 1/2로 감소시켰으며, 정상기의 배양여과액은 접종 후 급격히 감소시켜 배양 3일 후 대부분 사멸시켰다. Alexandrium tamarense, Prorocentrum micans, Scrippsiella trochoidea, Gymnodinium sanguineum, Cochlodinium polykrikoides의 5종의 적조원인 편모조류에 대한 Pseudomonas sp. LG-2의 살조특이성은 P. micans와 S. trochoidea에 살조효과를 나타내었다.

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각종 변이원에 대한 쇠비름 추출물의 돌연변이 억제 효과 (Inhibitory Effects of Poturaca oleracea L. Extract on the Mutagenicity of Various Mutagen)

  • 최근표;정성원;김은정;함승시
    • 동아시아식생활학회지
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    • 제7권4호
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    • pp.527-537
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    • 1997
  • This study was performed to determine the effects of antimutagenicity of Porturaca oleracea L. in Korea. In Ames test, the ethanol extract of Poturaca oleracea L. inhibited mutagenic activity of N-methyl-N'-nitro-N-nitrosoguanidine(MNNG), , 4-nitroquinoline-1-oxide(4NQO), benzo($\alpha$)pyrene (B($\alpha$)P) and 3-amino-1,4-dimethyl-5H-pyrido-(4,3-b)indole (Trp-P-1) in Salmonella typhimurium TA98 and TA100. But hot-water extract Poturaca oleracea L. only Inhibited mutagenic activity of MNNG in Salmonella typhimurium TA100, On 4NQO, the ethanol extract 100-1,600$\mu\textrm{g}$/plate of Porturaca oleracea L. showed a slight inhibitory effect of 13-48%, 4-47% in TA98 and TA100, respectively, but on MNNG, it showed higher inhibitory effect of 6-86% in TA100, And the treatment of 1,600$\mu\textrm{g}$/plate of ethanol extract of Porturacea L. had strong antimutagenicity with 74-87% inhibition against TA98 and TA100 induced by B(a)P and with 85-93% inhibition against TA98 and TA100 induced by Trp-P-1. The ethanol extract was fractionated with ether. chloroform, ethylacetate, butanol and water. Among them, most of the fraction except water fraction showed strong antimutagenicity effects against mutation induced by 4-NQO, MNNG, B(a)P and Trp-P-1. Chloroform fraction had strong antimutagenicity with 91% inhibition against TA100 induced by MNNG, diethyl etherfraction had strong antimutagenicity with 92%, 98% inhibition against TA98 and TA100 induced by 4NQO, Chloroform fraction had strong antimutagenicity with 97% inhibition against TA100 induced by B (a)P and diethyl etherfraction had strong antimutagenicity with 98% inhibition against both strain Induced by Trp-P-1, respectively.

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Elucidation of the Inhibitory Mechanisms of Nipponoparmelia laevior Lichen Extract against Influenza A (H1N1) Virus through Proteomic Analyses

  • Cuong, Tran Van;Cho, Se-Young;Kwon, Joseph;Kim, Duwoon
    • Journal of Microbiology and Biotechnology
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    • 제29권7호
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    • pp.1155-1164
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    • 2019
  • Lichens contain diverse bioactive secondary metabolites with various chemical and biological properties, which have been widely studied. However, details of the inhibitory mechanisms of their secondary metabolites against influenza A virus (IAV) have not been documented. Here, we investigated the antiviral effect of lichen extracts, obtained from South Korea, against IAV in MDCK cells. Of the lichens tested, Nipponoparmelia laevior (LC24) exhibited the most potent inhibitory effect against IAV infection. LC24 extract significantly increased cell viability, and reduced apoptosis in IAV-infected cells. The LC24 extract also markedly reduced (~ 3.2 log-fold) IAV mRNA expression after 48 h of infection. To understand the antiviral mechanism of LC24 against IAV, proteomic (UPLC-$HDMS^E$) analysis was performed to compare proteome modulation in IAV-infected (V) vs. mock (M) and LC24+IAV (LCV) vs. V cells. Based on Ingenuity Pathway Analysis (IPA), LC24 inhibited IAV infection by modulating several antiviral-related genes and proteins (HSPA4, HSPA5, HSPA8, ANXA1, ANXA2, $HIF-1{\alpha}$, AKT1, MX1, HNRNPH1, HNRNPDL, PDIA3, and VCP) via different signaling pathways, including $HIF-1{\alpha}$ signaling, unfolded protein response, and interferon signaling. These molecules were identified as the specific biomarkers for controlling IAV in vitro and further confirmation of their potential against IAV in vivo is required. Our findings provide a platform for further studies on the application of lichen extracts against IAV.

Flavopiridol 유도체에 의한 유방암 MCF-7 세포의 저해 활성에 관한 구조와 활성과의 관계 (QSAR on the Inhibition Acticity of Flavopiridol Analogues against Breast Cancer MCF-7)

  • 성민규;주성모;송아름;성낙도
    • Applied Biological Chemistry
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    • 제50권3호
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    • pp.147-153
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    • 2007
  • 새로운 유방암의 억제 물질을 탐색하고 설계하기 위하여 flavopiridol 유도체의 치환기($R_1{\sim}R_2$) 변화에 따른 유방암 유발세포 MCF-7의 저해활성에 관한 2D-QSAR 및 분자 홀로그래피적인 QSAR을 분석하였다. 2D-QSAR 모델(1)로부터 분자는 분산력으로 그리고 치환기는 입체장애를 유발하는 요인으로 작용하였으며 질량(MS)보다 굴절율(MR)상수가 저해활성에 크게 기여하였다. 그리고 2D-QSAR 모델(2)로부터는 MR상수의 적정값. $(MR)_{opt.}$= 126$Cm^3/mol$을 가지는 치환기의 저해활성이 가장 높을 것으로 예상되었다. 또한, 최적의 HQSAR 모델은 분자 조각의 크기($7{\sim}10$) 조건에서 예측성($q^2$= 0.583)과 상관성($r^2$= 0.982)이 매우 양호하였으며 기여도로부터 flavopiridol 분자내 A고리의 $C_8$원자에 결합된 수소원자나 hydroxyl-기보다 $C_9$원자 부분의 imino 골격이 저해활성에 기여하였다. 결과적으로 치환기들에 의한 분산력이 유방암 유발 세포 MCF-7의 저해활성에 크게 관여하는 주요인이었다.

Ranunculin및 Protoanemonin의 합성법의 개선 및 세포독성 평가 (Modified Synthetic Method & Cytotoxic Activity of Ranunculin and Protoanemonin)

  • 방성철;김용;안병준
    • 약학회지
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    • 제48권2호
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    • pp.117-121
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    • 2004
  • Ranunculin, a potent cytotoxic component of P. koreana, was synthesized by reacting (s)-(-)-5-(hydroxymethyl)-2(5H)-furanone with 2,3,4,6-tetra-O-acetyl-$\alpha$-D-glucopyranosyl bromide and successive removal of the acetyl protecting group by 0.5 M HCl/MeOH. A new deacetylation process of the intermediate tetraacetylranunculin was deviced giving a yield of 83% of ranunculin. Protoanemonin, the cytotoxic structural moiety of ranunculin, was synthesized by dehydration of (s)-(-)-5-hydroxymethyl-2(5H)-furanone. Ranunculin showed a moderate cytototoxic activity against A-549 (ED$_{50}$=7.53 $\mu\textrm{g}$/$m\ell$), NIH3T (ED$_{50}$=13.6$\mu\textrm{g}$/$m\ell$), and SK-OV-3 (ED$_{50}$=17.5 $\mu\textrm{g}$/$m\ell$). Meanwhile, protoanemonin also exhibited moderate cytotoxicity against A-549 (ED$_{50}$=9.38 $\mu\textrm{g}$/$m\ell$), NIH3T (ED$_{50}$=13.8 $\mu\textrm{g}$/$m\ell$), and SK-OV-3 (ED$_{50}$=15.1 $\mu\textrm{g}$/$m\ell$). It was found that both of the synthetic products showed a potenter cytotoxicity against A-549.ainst A-549.

Synthesis and In Vitro Cytotoxicity of 1-Azanthraquinone-3-Carboxamides

  • Lee, Hee-Soon;Lee, Chang-Wook;Yang, Sung-Il
    • Archives of Pharmacal Research
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    • 제22권4호
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    • pp.380-383
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    • 1999
  • Five 1-azzanthraquinone-3-carboxamides were synthesized and evaluated in vitro cytotoxicity against four human cancer cell lines. The most active compound, 7b, exhibited cytotoxic activity comparable to doxorubicin.

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Isoetin 5'-Methyl Ether, A Cytotoxic Flavone from Trichosanthes kirilowii

  • Rahman, Md. Aziz Abdur;Moon, Surk-Sik
    • Bulletin of the Korean Chemical Society
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    • 제28권8호
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    • pp.1261-1264
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    • 2007
  • Bioassay-directed fractionations of the seed extracts of Trichosanthes kirilowii, have resulted in the isolation of two new compounds, 2-(4-hydroxy-3-methoxyphenyl)-3-(2-hydroxy-5-methoxyphenyl)-3-oxo-1-propanol (2) and isoetin 5'-methyl ether (5,7,2',4'-tetrahydroxy-5'-methoxyflavone) (3), together with two known compounds, 7-hydroxychromone (1) and 5,7,4'-trihydroxy-3',5'-dimethoxyflavone (tricin, 4). Their structures were characterized by spectroscopic analysis such as 2D-NMR, HRTOFMS, and UV. Compound 3 showed cytotoxicity against human lung cancer cell line A549, human skin melanoma SK-Mel-2, and mouse melanoma B16F1, with IC50 of 0.92, 8.0, and 7.23 μg/mL, respectively.