• International Journal of Oral Biology
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• 제36권1호
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• pp.7-11
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• 2011

Ursolic acid is a triterpenoid compound present in many plants. This study examined the antimicrobial activity of ursolic acid against mutans streptococci (MS) isolated from the Korean population. The antimicrobial activity was evaluated by the minimum inhibitory concentration (MIC) and time kill curves of MS. The cytotoxicity of ursolic acid against KB cells was tested using an MTT assay. The $MIC_{90}$ values of ursolic acid for Streptococcus mutans and Streptococcus sobrinus isolated from the Korean population were $2 {\mu}g$/ml and $4 {\mu}g$/ml, respectively. Ursolic acid had a bactericidal effect on S. mutans ATCC $25175^T$ and S. sobrinus ATCC $33478^T$ at > $2 \;{\times}\; MIC (4 {\mu}g$/ml) and $4 \;{\times}\; MIC (8 {\mu}g$/ml), respectively. Ursolic acid had no cytotoxic effect on KB cells at concentrations at which it exerted antimicrobial effects. The results suggest that ursolic acid can be used in the development of oral hygiene products for the prevention of dental caries.

• Molecules and Cells
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• 제38권3호
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• pp.273-278
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• 2015

The induction of angiogenesis is a crucial step in tumor progression, and therefore, efficient inhibition of angiogenesis is considered a powerful strategy for the treatment of cancer. In the present study, we report that the lipophilic antimicrobial peptides from EML-CAP3, a new endophytic bacterial strain isolated from red pepper leaf (Capsicum annuum L.), exhibit potent antiangiogenic activity both in vitro and in vivo. The newly obtained antimicrobial peptides effectively inhibited the proliferation of human umbilical vein endothelial cells at subtoxic doses. Furthermore, the peptides suppressed the in vitro characteristics of angiogenesis such as endothelial cell invasion and tube formation stimulated by vascular endothelial growth factor, as well as neovascularization of the chorioallantoic membrane of growing chick embryos in vivo without showing cytotoxicity. Notably, the angiostatic peptides blocked tumor cell-induced angiogenesis by suppressing the expression levels of hypoxia-inducible $factor-1{\alpha}$ and its target gene, vascular endothelial growth factor (VEGF). To our knowledge, our findings demonstrate for the first time that the antimicrobial peptides from EML-CAP3 possess antiangiogenic potential and may thus be used for the treatment of hypervascularized tumors.

• 한국자기공명학회논문지
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• 제15권1호
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• pp.1-13
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• 2011

9Pbw2 is a 9-mer analog of protaetiamycine derived from the larvae of the beetle Protaetia brevitarsis. Previously, we designed four 9-mer peptide analogues to optimize the balance between the hydrophobicity and cationicity of the peptides and to increase bacterial cell selectivity. Among them, 9Pbw2 has high antibacterial activity without cytotoxicity. The results obtained in previous study suggest that the bactericidal action of 9Pbw2 may be attributed to the inhibition of the functions of intracellular components after penetration of the bacterial cell membrane. In order to understand structure-activity relationships, we determined the three-dimensional structure of 9Pbw2 in 200 mM DPC micelle by NMR spectroscopy. 9Pbw2 has one hydrophobic turn helix from $Trp^3$ to $Arg^8$ and positively charged residues at the N- and C-terminus. This result suggested that positively charged residues from position at the C-terminus in 9Pbw2 may be important for the primary binding to the negatively charged phospholipid head groups in bacterial cell membranes and hydrophobic residues in the middle portion face toward the acyl chains of the hydrophobic lipid in the bacterial cell membrane.

• 한국식품영양과학회지
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• 제34권6호
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• pp.765-770
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• 2005

본 연구에서는 미역귀를 추출, 각 용매 별로 분획 하여 항균효과와 암세포 성장억제 및 QR유도활성 효과 등의 생리활성을 연구하였다. 미역은 일반적으로 콜레스테를 배출 작용, 중금속(Cd) 및 방사능 물질(Sr)의 체내 흡수 억제, 배출 작용과 정장 작용이 있으므로 식이섬유 식품으로서 효과가 많다. 미역의 뿌리부분이며 식품개발품으로 소외되고 있는 미역귀를 이용하여 식중독 및 식품부패 원인균 등을 이용한 항균활성을 측정해 보았으며 특히 식중독원인균인 Staphylococus aureous에 시료의 UPMM층의 항균효과가 보였고 단백질 식품부패균인 Serratia marcescens에는 UPMB와 UPMM, UPMH 등에서 전반적으로 항균효과가 보였다. 또 4종의 인체 암 세포주 HeLa, HT-29, MCF-7 및 HepG2에 대한 암세포 성장억제 실험을 한 결과 사용한 4종의 암세포주에서 모두 정도의 차이는 있으나 시료첨가 농도에 의존적으로 성장 저지 효과가 나타났다. 특히 시료의 methanol 분획층인 UPMM에서 괄목할 만한 높은 효과를 나타내었으며 HeLa, HT-29 및 HepG2세포에서는 UPMM의 농도를 $500\mu g/mL$ 첨가 시 이미 97.71, 98.63 및 $90.32\%$의 높은 암세포 성장 억제 효과를 나타내었다. 한편, 사용한4가지 암세포주 중 유일하게 quinone reductase를 가지고 있는 HepG2를 이용한 quinone reductase 유도 활성여부를 측정한 결과 UPMH의 첨가농도 $320\mu g/mL$에서 대조군보다 2.36배의 높은 QR유도효과를 나타내었다. 이와 같은 실험결과에서 식품이나 건강 및 약리적 효과가 있는 식품으로 알려진 미역귀의 기능성 식품으로서의 개발이 기대되어진다.

• Mycobiology
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• 제36권3호
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• pp.173-177
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• 2008

The crude ethanol extracts (stem and fruits), their fractions and two triterpenes, $\beta$-Amyrin and 12-Oleanene 3$\beta$, 21$\beta$-diol, isolated as a mixture from the chloroform soluble fraction of an ethanolic extract of Duranta repens stem, were evaluated for antibacterial, antifungal activities by the disc diffusion method and cytotoxicity by brine shrimp lethality bioassay. The structures of the two compounds were confirmed by IR, $^1H$-NMR, $^{13}C$-NMR and LC-MS spectral data. The chloroform soluble fraction of stem and ethanol extract of fruits possess potent antishigellosis activity and also exhibited moderate activity against some pathogenic bacteria and fungi but the isolated compound 1 (mixture of $\beta$-Amyrin and 12-Oleanene 3$\beta$, 21$\beta$-diol) showed mild to moderate inhibitory activity to microbial growth. The minimum inhibitory concentrations (MICs) of the extracts (stem and fruits), their fractions and compound 1 were found to be in the range of 32$\sim$128 ${\mu}g/ml$. The chloroform soluble fractions of stem and ethanol extract of fruit showed significant cytotoxicity with $LC_{50}$ value of 0.94 ${\mu}g/ml$ and 0.49 ${\mu}g/ml$, respectively against brine shrimp larvae.

• 한국유기농업학회지
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• 제22권3호
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• pp.469-481
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• 2014

본 연구진은 신규 미생물인 Nocardia sp. CS682 균주에서 항균물질인 nargenicin을 확보하고, 그 유도체 5종을 확보하여 그람양성, 음성 및 다약제 내성균에 대한 항균 효능 및 LPS로 자극된 대식세포에서의 nitric oxide 생성 억제능을 확인하였다. Nargenicin 유도체들은 nargenicin 및 vancomycin에 비교하여 우수한 항균 활성을 보여주었으며, compound 4 및 5는 광범위한 항균 효능 외에 nitric oxide 생성 억제능을 보여 항균-항염효과를 가지는 dual effector로써 감염, 면역 질환에 응용 가능성을 시사하였다. Nargenicin 유도체들은 향후 염증반응에서의 면역 조절 기작에 대한 추가 연구가 필요할 것으로 사료된다.

• 한국자원식물학회:학술대회논문집
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• 한국자원식물학회 2018년도 춘계학술발표회
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• pp.94-94
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• 2018

The gold (LC-AuNPs) and silver (LC-AgNPs) nanoparticles were rapidly synthesized by fruit extract of Lycium chinense within 1.15 and 25 min respectively in an eco-friendly way. The synthesized nanoparticles confirmed by relevant surface plasmon resonance peaks for gold and silver nanoparticles at 536 and 480 nm, respectively. FE-TEM results revealed that LC-AuNPs were 20-50 nm and LC-AgNPs were 50-100 nm. The maximum distribution of gold, silver elements and the crystallographic nature of synthesized were confirmed using EDX, elemental mapping and XRD. LC-AgNPs showed inhibitory activity against pathogenic microorganisms such as E. coli and S. aureus, whereas LC-AuNPs did not show inhibitory activity. The LC-AgNps nanoparticles exhibited significant cytotoxicity to human breast cancer MCF7 cell line and less cytotoxicity to non-diseased RAW264.7 (murine macrophage) cells whereas LC-AuNps showed minimal toxicity to both cell lines. In-depth research on this rapid, facile and greenery nanoparticles may play a potential role in biomedical applications.

• The Korean Journal of Physiology and Pharmacology
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• 제17권6호
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• pp.517-523
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• 2013

Naphthyridine compounds are important, because they exhibit various biological activities including anticancer, antimicrobial, and anti-inflammatory activity. Some naphthyridines have antimitotic effects or demonstrate anticancer activity by inhibiting topoisomerase II. These compounds have been investigated as potential anticancer agents, and several compounds are now part of clinical trials. A series of naphthyridine derivatives were evaluated for their in vitro cytotoxic activities against human cervical cancer (HeLa), leukemia (HL-60), and prostate cancer (PC-3) cell lines using an MTT assay. Some compounds (14, 15, and 16) were more potent than colchicine against all three human cancer cell lines and compound (16) demonstrated potency with $IC_{50}$ values of 0.7, 0.1, and $5.1{\mu}M$, respectively. Comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) were used for quantitative structure-activity relationship (QSAR) molecular modeling of these compounds. We obtained accurate and predictive three-dimensional QSAR (3D-QSAR) models as indicated by the high PLS parameters of the HeLa ($q^2$, 0.857; $r^2$, 0.984; $r^2\;_{pred}$, 0.966), HL-60 ($q^2$, 0.777; $q^2$, 0.937; $r^2\;_{pred}$, 0.913), and PC-3 ($q^2$, 0.702; $q^2$, 0.983; $r^2\;_{pred}$, 0.974) cell lines. The 3D-QSAR contour maps suggested that the C-1 NH and C-4 carbonyl group of the naphthyridine ring and the C-2 naphthyl ring were important for cytotoxicity in all three human cancer cell lines.

• Bulletin of the Korean Chemical Society
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• 제24권10호
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• pp.1478-1484
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• 2003

CRAMP was identified from a cDNA clone derived from a mouse femoral marrow cells as a member of cathelicidin-derived antimicrobial peptide. Tertiary structure of CRAMP in TFE/$H_2O$ (1 : 1, v/v) solution has been determined by NMR spectroscopy previously and consists of two amphipathic $\alpha-helices$ from Leu4 to Lys10 and from Gly16 to Leu33. These two helices are connected by a flexible region from Gly11 to Gly16. Analysis of series of fragments composed of various portion of CRAMP revealed that an 18-residue fragment with the sequence from Gly16 to Leu33 (CRAMP-18) was found to retain antibacterial activity without cytotoxicity. The effects of two Phe residues at positions 14 and 15 of CRAMP-18 on structure, antibacterial activity, and interaction with lipid membranes were investigated by $Phe^{14,15}$ ${\rightarrow}$ Ala substitution (CRAMP-18-A) in the present study. Substitution of Phe with Ala in CRAMP-18 caused a significant reduction on antibacterial and membrane-disrupting activities. Tertiary structures of CRAMP-18 in 50% TFE/$H_2O$ (1 : 1, v : v) solution shows amphipathic ${\alpha}$-helix, from $Glu^2{\;}to{\;}Leu^{18}$, while CRAMP-18-A has relatively short amphipathic ${\alpha}$-helix from $Leu^4{\;}to{\;}Ala^{15}$. These results suggest that the hydrophobic property of $Phe^{14}{\;}and{\;}Phe^15$ in CRAMP-18 is essential for its antibacterial activity, ${\alpha}$-helical structure, and interactions with phospholipid membranes.

• Mycobiology
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• 제37권1호
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• pp.31-36
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• 2009

A phytochemical study on the flower of Calotropis gigantea (Linn.) using silica gel column chromatography and preparative thin layer chromatography, led to the first time isolation of Di-(2-ethylhexyl) phthalate (compound 1) and anhydrosophoradiol-3-acetate (compound 2). The structures of these compounds were confirmed by spectroscopic analyses (IR, HRTOFMS and NMR). The antibacterial and antifungal activities of ethyl acetate extract, compound 1 and compound 2 were measured using the disc diffusion method. Ethyl acetate extract and compound 1 presented better results than compound 2. The minimum inhibitory concentrations (MICs) of the extract and compounds were found to be in the range of $16{\sim}128{\mu}g/ml$. The cytotoxicity ($LC_{50}$) against brine shrimp nauplii (Artemia salina) were also evaluated and found to be 14.61 ${\mu}g/ml$ for ethyl acetate, 9.19 ${\mu}g/ml$ for compound 1 and 15.55 ${\mu}g/ml$ for compound 2.