• BMB Reports
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• 제53권7호
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• pp.379-384
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• 2020

Exposure to Ultraviolet (UV) light induces photoaging of skin, leading to wrinkles and sunburn. The perennial herb Humulus japonicus, widely distributed in Asia, is known to have anti-inflammatory, antimicrobial, and antioxidant effects. However, the physiological activities of isolated compounds from H. japonicus have rarely been investigated. This study focused on the isolation of active compounds from H. japonicus and the evaluation of their effects on photoaging in UVB-irradiated human fibroblast (Hs68) cells. When the extract and four fractions of H. japonicus were treated respectively in UVB-irradiated Hs68 cells to investigate anti-photoaging effects, the ethyl acetate (EtOAc) fraction showed the strongest inhibitory effect on MMP1 secretion. From EtOAc fraction, we isolated luteolin-8-C-glucoside (1), apigenin-8-C-glucoside (2), and luteolin-7-O-glucoside (3). These compounds suppressed UVB-induced MMP-1 production by inhibiting the phosphorylation of the mitogen-activated protein kinases (MAPKs) and activator protein-1 (AP-1). When the antioxidant activity of the compounds were estimated by conducting western blot, calculating the bond dissociation energies of the O-H bond (BDE) at different grade, and measuring radical scavenging activity, we found luteolin-8-C-glucoside (1) showed the strongest activity on the suppression of UVB-induced photoaging. These results demonstrate the inhibitory effect of three flavone glycosides derived from H. japonicus on MMP-1 production, MAPK and AP-1 signaling, and oxidative stress; this could prove useful in suppressing UVB induced photoaging.

• Journal of Oral Medicine and Pain
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• 제32권2호
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• pp.151-156
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• 2007

구강 내에서의 피톤치드는 항균효과를 통하여 입냄새 발생균을 줄여줄 뿐 만 아니라 발생된 휘발성 황화합물과 반응하여 생겨진 입냄새성분을 액체상태에서 침전시킴으로써 냄새제거를 할 수 있게 하는 기능을 가지고 있어, 미생물학적으로나 화학적으로 탁월한 냄새제거의 기능을 가지고 있다. 이에 본 실험에서는 ferrous sulfate를 사용하여 피톤치드에 의한 입냄새 성분인 휘발성 황화합물의 냄새제거작용을 증명함으로써 발전된 새로운 입냄새 치료 방법을 개발하고자 한 바, 아래와 같은 유의성 있는 결과를 얻었다. 1. 타액에 피톤치드 첨가 후의 침전에 의한 흡광도의 평균값과 타액자체만의 침전에 의한 흡광도의 평균값의 차이는 0.849이었다. 2. 증류수에 피톤치드 첨가했을 때 침전에 의한 흡광도의 평균값과 증류수 자체만의 침전에 의한 흡광도의 평균값의 차이는 0.701이었다. 3. 증류수에 피톤치드의 유무에 의한 평균값 차이(0.701)보다 타액 내 피톤치드의 유무에 의한 평균값의 차이(0.849)가 더 크므로 피톤치드는 타액 내에서 황화합물과 작용하여 더 많은 침전물을 발생시켰다. 이상의 결과로 보아, 본 연구에서 사용한 피톤치드는 타액 내의 입냄새물질인 황화합물과 반응하여 액체 상태에서 효과적으로 냄새제거작용을 수행할 수 있으므로, 인체에 부작용이 없는 한계 내에서 치약뿐 만 아니라 구강세척제 등의 구강용품에 첨가하여 임상에서 적극적으로 사용할 수 있을 것으로 생각된다.

• 한국식품영양학회지
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• 제30권2호
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• pp.181-190
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• 2017

Functional foods are of great significance since our society is accelerating into aging. An aging society has many physiological metabolic diseases such as hypertension, diabetes, heart disease, cancer, dementia and geriatric diseases. Fundamental treatments for the elderly are almost impossible and the social burden is heavy. If these diseases can be prevented or alleviated by improving dietary habits using functional foods, the significance would be very large. Pomegranate has been found to have 124 different kinds of phytochemicals. Polyphenols have a wide range of protective effects including various physiological metabolic diseases and cancers. It is necessary to develop functional foods such as preservatives and food extenders which can contribute to food safety, required in the food industry, by using such bioactive substances. Pomegranates have been reported to decrease the impact of many serious illnesses. There is a considerable amount of bioactive substances in the peel of a pomegranate, which has potent anticancer, antioxidant, antimicrobial and anti-apoptotic properties. Unfortunately, the peel is typically discarded after processing. Despite knowledge regarding the bioactive substances in the pomegranate peel and peel extracts, including their functionality and diversity, the knowledge is not well known by consumers in general. The aim of this study was to review up to date research trends for processing and developing new functional foods by utilizing nutritional functional substances, favourite food materials, and materials for processing food contained in pomegranate peels and pomegranate peel extracts. This study will summarize the data found in pomegranate peel and pomegranate peel extract literature mainly recently published in Science Direct. There are polyphenolic compounds (ellagitannins, punicalagin, proanthocyanidin, flavonoids, polysaccharides, etc.) in the fruit peel, making up about 50% of the pomegranate's weight. The polyphenol content of a pomegranate fruit peel is 149.91 mg/g, which is about 100 times higher than the juice. Paying attention to the fact that the ellagitannin content (14.22 mg/g) in the fruit peel is also twice as high as that of the fruit juice and seeds, that confirms the possibility of utilizing the peel as a food ingredient capable of developing new, functional bioactive foods.

• 한국미생물·생명공학회지
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• 제26권5호
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• pp.379-386
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• 1998

본 연구에서는 천연 항균물질의 개발 이용을 위해 황기 종자로부터 인체에 무해한 천연 항균 단백질을 ion exchange chromatography 및 gel filteration을 이용하여, 순수 분리하고 특성을 조사하였다. 황기종자로부터 추출한 천연 항균 단백질은 Aspergillus ocraceus, Penicillium expensum, P. digitatum, Botrytis cineria의 포자 발아 및 효모인 Candida albicans의 생육을 현저하게 저해하였으며 ammonium sulfate 포화도가 0.4일 때 단백질의 침전량이 122.6 $\mu\textrm{g}$/$m\ell$로 가장 많았고 항균력도 15.2 mm로 가장 높게 나타났다. 강력한 cation exchange chromatography인 Mono-S를 이용하여 FPLC에서 단백질을 분획하였을때 첫번째 peak에서 분획된 단백질군이 항균력을 보였으며 Superose 12HR gel filteration column을 이용하여 2차 분획 하였을 때 분자량이 19 kDa되는 단일 단백질만을 순수분리 할 수 있었다. 전기 영동한 polyacrylamide gel위에 곰팡이 포자를 중층하는 bio autography로 19 kDa 단백질 band의 항균력을 직접 확인하였으며 분리된 항균 단백질의 아미노 말단의 아미 노산 22잔기를 sequencing하고 thaumatin 및 zeamatin 유사 단백질들과 상동성을 측정한 결과 50%내외의 homology를 나타내었다. 분리된 항균 단백질은 곰팡이 균사가 성장하는 선단부위에 가장 먼저 침투하여 channel을 형성함으로 osmolysis를 일으켜 곰팡이의 생육을 억제하는 것으로 추측할 수 있었다.

• Journal of Microbiology and Biotechnology
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• 제27권6호
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• pp.1039-1052
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• 2017

Endophytic fungi have currently been acknowledged as the most promising source of bioactive compounds for drug discovery, and considerable progress has been made in exploring their diversity, species richness, and bioprospecting. Fungal endophytes from unique environmental settings offer a pool of potentially useful medicinal entities. Owing to the constant stresses imposed on macroalgae by marine environments, it is believed that algae and their associated endophytic symbionts represent a good source of structurally diverse bioactive secondary metabolites. Despite the proven significance of active metabolites of algal endophytes, little have been exploited. This review highlights the latest discoveries in algicolous endophytic research, with particular focus on the bioactive metabolites from algal endophytes. Compounds are classified according to their reported biological activities, like anticancer, antibacterial, antifungal, and antioxidant properties. Present experimental evidence suggests that a majority of the bioactive metabolites were reported from Phaeophyceae followed by Rhodophyceae and Chlorophyceae. An intensive search for newer and more effective bioactive metabolites has generated a treasure trove of publications, and this review partially covers the literature published up to 2016.

• Advances in Traditional Medicine
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• 제8권4호
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• pp.339-348
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• 2008

Butea frondosa has been used traditionally as a topical formulation in the treatment of many diseases and disorders. Two compounds [BF-1 (crystalline flavonol quercetin) and BF-2 (tannin) from ethyl acetate fraction of ethanolic extract] were isolated from the bark of Butea frondosa. The stereostructures of the compounds were determined on the basis of chemical and physicochemical evidence. BF-1 and BF-2 were screened in vitro for possible antibacterial property against 112 bacteria comprising 3 genera of Gram-positive and 12 genera of Gram-negative types. It was found that both BF-1 and BF-2 exhibited inhibitory activity against several bacteria. Most of these strains were inhibited by BF-1 at $50-200\;{\mu}g/ml$, while BF-2 ($MIC_{50}$ $400\;{\mu}g/ml$) was much less active. The bacteria could be arranged in the decreasing order of sensitivity towards BF-1 in the following manner: S. aureus, Bacillus spp., Salmonella spp., Vibrio spp., Shigella spp., E. coli and Pseudomonas spp. The $MIC_{50}$ of the compound was $50\;{\mu}g/ml$ while the $MIC_{90}$ was $100\;{\mu}g/ml$. The decreasing order of sensitivity towards BF-2 was V. cholerae, Bacillus spp., S. aureus, V. parahaemolyticus, Salmonella spp. and Proteus spp. BF-1 was bactericidal in action. In vivo studies with this extract showed that it could offer statistically significant protection (p < 0.01) to mice challenged with a virulent bacterium. The inhibitory activity of Butea frondosa against Gram-positive and Gram-negative bacteria indicates its usefulness in the treatment of common bacterial infections. The potentiality of BF-1 as an antibacterial agent may be confirmed further by pharmacological studies.

• Asian Pacific Journal of Cancer Prevention
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• 제16권17호
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• pp.7641-7651
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• 2015

It has been shown previously that nutritional supplements rich in polyphenolic compounds play a significant role in prostate cancer chemoprevention. Propolis is a natural, resinous hive product that has several pharmacological activities including antimicrobial, antioxidant, anti-inflammatory, and antitumoral activities. The aim of this study was to compare the cytotoxic, antioxidant and antitumoral activities of an ethanolic extract of Egyptian propolis (EEP) in vitro with an established chemotherapeutic drug such as doxorubicin (DOX), and the effects of their combination against the PC3 human prostate cancer cell line. Cellular viability and $IC_{50}$ levels with EEP, DOX and their (v/v) combination were detected by sulphorhodamine-B (SRB) assay after incubation of PC3 cells for 72h with different doses (0, 0.01, 0.1, 1, 10 and $100{\mu}g/ml$). Two selected doses of $IC_{50}$ and $IC_{25}$ were applied to cells for 24h for antitumor evaluation assay of treatment compounds. EEP and its (v/v) combination with DOX showed significant antitumor potential besides high antioxidant properties of superoxide dismutase (SOD), total antioxidant capacity (TAC), catalase (CAT), nitric oxide (NO) and reduced glutathione (GSH) levels when compared with the control untreated cells. DNA fragmentation assay and semi quantitative RT-PCR analyses for p53 and Bax genes showed that EEP activated cellular apoptosis and increased the mRNA expression levels more than other treatment. In conclusion, EEP alone or in combination with DOX at both doses used here showed greater antioxidant, antiproliferative and apoptotic effects against the PC3 cell lines as compared to treatment with DOX alone. Therefore, EEP could be considered as a promising candidate for prostate cancer chemotherapy.

• 분석과학
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• 제30권1호
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• pp.26-31
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• 2017

Background and purpose: This study was carried out to learn more about the potential prophylactic or antibacterial activity of the plant Acalypha indica against selective pathogenic bacteria. Experimental: The test organisms were Sarcina lutea IFO 3232, Bacillus subtilis IFO 3026, Pseudomonas denitrificans, Escherichia coli IFO 3007, Klebsiella pneumoniae ATTC 10031, Xanthomonas campestris IAM 1671, and Proteus vulgaris. Leaf, stem, and bud powder of Acalypha indica were dissolved in various solvents, and the extracts were tested for antimicrobial activity through the disc diffusion method. GC-MS profiling was performed to characterize active chemical compounds in the essential oil of Acalypha indica. Results: The ethanol extract showed the highest activity against all bacteria, while the petroleum ether extract yielded the highest zone of inhibition against Proteus vulgaris ($11.83{\pm}1.75mm$). The minimum inhibitory concentration (MIC) of the ethyl acetate extract against Bacillus subtilis was 16 µg/mL. Phytochemical screening by GC-MS revealed a total of 12 bioactive compounds. Conclusion: Extracts of Acalypha indica may be useful in formulating and synthesizing new antibacterial drugs.

• 공업화학
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• 제7권6호
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• pp.1096-1104
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• 1996

새로운 항균제 및 항종양제를 합성하기 위하여 norfloxacin(8) 또는 ciprofloxacin(9)이 pteroic acid의 C-9위치에 치환되고 C-2 위치에 아미노기 대신 $CH_3$기가 치환된 새로운 pteroic acid 유도체 13a와 13b를 합성하였다. 이는 출발 물질인 norfloxacin과 ciprofloxacin의 piperazine N-4 위치에 2-amino-3-cyano-5-chloro-methylpyrazine(20)을 결합하여 1-alkyl(ethyl, cyclopropyl)-6-fluoro-1,4-dihydro-4-oxo-7-[[4-N- (2-amino-3-cyanopyrazin-5-yl)methyl]piperazin-1-yl]-3-quinolinecarboxytic acid(12a, 12b)를 합성하였다. 이를 각각 acetamidine. HCl과 고리화시켜 C-2 위치에 아미노기 대신 $CH_3$기가 치환된 새로운 pteroic acid 유도체 135와 13b를 각각 76.2%와 82.8%의 수율로 합성하였다. 그리고 이들 화합물에 대한 항균활성의 측정은 Pseudomonas aeruginosa ATCC9027을 포함하여 Gram-positive와 Gram-negative bacteria에 대하여 검토한 결과 합성한 화합물 13a와 13b는 일반적으로 norfloxacin보다 낮은 항균활성을 나타냈다.

• Bulletin of the Korean Chemical Society
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• 제31권11호
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• pp.3304-3308
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• 2010

Condensation of 4-amino-5-mercapto-3-($\alpha$-naphthyl)-s-triazole (1) with cyanogen bromide gives 6-amino-3-($\alpha$-naphthyl)-s-triazolo[3,4-b]-1,3,4-thiadiazole (2) which on condensation with chloranil yields 3,9-di-($\alpha$-naphthyl)-6,14-dioxo-bis-(s-triazolo[3,4-b]-1,3,4-thiadiazolo[3,2-b]imidazo[4,5-b]cyclohexane]-5a,6a-diene) (3). 3-($\alpha$-naphthyl)-s-triazolo[3,4-b]-1,3,4-thiadiazolo[3,2-b]imidazo[4,5-b]quinoxaline (4) is obtained by a similar condensation of (2) with 2,3-dichloroquinoxaline. The reaction of (2) with $\alpha$-haloketones followed by bromination affords 7-aryl-3-($\alpha$-naphthyl)-imidazo[2,1-b]-1,3,4-thiadiazolo[2,3-c]-s-triazoles (5) and their 6-bromo analogues 6 respectively. The structures of all newly synthesized compounds were established on the basis of elemental analyses, IR, $^1H$-NMR. The antibacterial and antifungal activities of all newly synthesized compounds have also been evaluated.