• Title/Summary/Keyword: active agent

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P-Glycoprotein Inhibitory Activity of Indonesian Medicinal Plants in Human Breast Cancer Cells

  • Kim, Hyang-Rim;Chung, Soo-Yeon;Jeong, Yeon-Hee;Go, Eun-Jung;Han, Ah-Reum;Kim, Na-Hyung;Sung, Min-Kyung;Song, Gi-Na;Jang, Jung-Ok;Nam, Joo-Won;Lee, Hwa-Jeong;Seo, Eun-Kyoung
    • Natural Product Sciences
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    • 제10권6호
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    • pp.268-271
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    • 2004
  • In order to examine their effects on the P-glycoprotein (P-gp) activity in human breast cancer cells, MCF-7/ADR, one hundred Indonesian plant extracts were screened. Among them, the five chloroform extracts of Calotropis gigantea, Curcuma aeruginosa, Merremia mammosa, Sindora sumatrana, and Zingiber cassumunar, showed the most potent P-gp inhibitory activity. When each of these extracts was treated together with the anticancer agent, daunomycin, they increased the cytotoxic activity of daunomycin up to $IC_{50}$ values of less than $6.62\;{\mu}M$, which is a value with a positive control, verapamil. Also, other 15 plant extracts exhibited significant P-gp inhibitory activity with $IC_{50}$ values between 6.62 and $13.20\;{\mu}M$. These prospective samples will be subjected to further laboratory phytochemical investigation to find active principles.

해김사(海金沙)가 Rat의 전립선비대에 미치는 영향 (The Effects of Lygodium japonicum on Experimental Rat Model of Benign Prostatic Hyperplasia)

  • 이두현;이장식;김용성
    • 대한한방내과학회지
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    • 제31권3호
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    • pp.457-466
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    • 2010
  • Objective : In benign prostatic hyperplasia, dihydrotestosterone acts as a potent cellular androgen and promotes prostate growth. Inhibiting enzyme $5{\alpha}$-reductase that is involved in the conversion of testosterone to the active form dihydrotestosterone reduces this excessive prostate growth. The mechanism on benign prostatic hyperplasia is substantiating evidence to support the clinical value in the evaluation of therapeutic efficacy. In this study, we investigated the effects of Lygodium japonicum on cyto-pathological alterations and expression of $5{\alpha}$-reductase in the rat model of benign prostatic hyperplasia induced by castration and testosterone treatment. Methods : Sprague-Dawley rats were treated with testosterone after castration for induction of experimental benign prostatic hyperplasia, which is similar to human benign prostatic hyperplasia in histopathological profiles. Lygodium japonicum as an experimental specimen, and finasteride as a positive control, were administered orally. The prostates were evaluated by histopathological changes and testosterone levels. Also, the prostates were observed by hematological alterations of AST, ALT, ${\gamma}$-GTP, BUN and creatinine. Results : The rats treated with Lygodium japonicum showed a diminished range of luminal cell and duct epithelial cell damage. The stromal elements and connective tissue proliferation of Lygodium japonicum treated group as compared to the control group decreased. Conclusions : These findings suggest that Lygodium japonicum may protect the glandular epithelial cells. We concluded that Lygodium japonicum could be a useful remedy agent for treating the benign prostatic hyperplasia.

Protective Effect of Lonicerae Flos Aqueous Extracts on a Pressure Overload-induced Heart Failure Model

  • Shin, Jae-wook;Jang, Woo-seok;Baek, Kyung-min
    • 대한한방내과학회지
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    • 제38권6호
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    • pp.877-890
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    • 2017
  • Objectives: Lonicerae flos (LF), a dried flower part of Lonicera japonica Thunb., has been widely used in Korean medicine as anti-inflammatory and antioxidative agent. The purpose of this study was to determine the cardioprotective effects of LF, through potential antioxidant effects, on the pressure overload (PO)-induced heart failure (HF) in C57BL/6 mice after transverse aortic constriction (TAC) surgery. Methods: Resveratrol (10 mg/kg body weight) or LF (125, 250 or 500 mg/kg body weight) was orally administered, once daily for 14 days, starting 14 days after TAC surgery. Changes in the mortality, body weights, heart weights, histopathology of the heart, and antioxidant defense systems of the heart were analyzed. Results: Marked and noticeable increases of heart weights, mortalities, and hypertrophic, focal, and lytic fibrotic histological changes in the LVs were observed, with destruction of heart antioxidant defense systems after surgery. However, HF signs, induced by TAC surgery through PO, and destruction of heart antioxidant defense systems were significantly and dose-dependently inhibited by 14 days of maintained oral treatment with LF 500, 250 or 125 mg/kg. Treatment with 250 mg/kg LF was comparable to treatment with 10 mg/kg resveratrol. Conclusions: The results in this study suggest that oral administration of LF favorably relieves PO-induced HF following TAC, through increase of heart antioxidant defense systems. The overall effects of 250 mg/kg LF were similar to those of 10 mg/kg resveratrol. More detailed mechanistic studies should be conducted in the future, with screening of the biologically active compounds in LF.

세척을 통한 중금속(Cd, Zn)으로 오염된 토양의 정화 (Remediation of Heavy Metal Contaminated Soil by Washing Process)

  • 백정선;현재혁;조미영;김수정
    • 한국토양환경학회지
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    • 제5권1호
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    • pp.45-54
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    • 2000
  • 본 연구는 중금속(Zn, Cd)으로 오염된 토양을 여러 세척 용제(물, mineral acid, chelating agent, organic acld)를 가지고 탈착시켜 제거하는 실험으로 pH와 농도에 따라 회분식과 연속식 실험을 병행하였다. 물과 NaOH에 의한 세척 효과는 거의 없는 것으로 나타났으며 HCI, EDTA, Oxalic acid에 의한 세척 효과는 매우 높게 나타났다. HCI에 의한 세척효과가 가장 높은 이유는 낮은 pH에 의한 중금속의 이온화 현상에 의한 것으로 사료되며 EDTA, Oxalic acid의 효과가 높은 것은 용해도를 증가시켜 중금속 이온과 많은 착물을 형성하기 때문이다. 또한 Zn이 Cd보다 대체적으로 탈착율이 좋았으며 일반적으로 제거 경향은 pH가 낮을수록, 세척 용제의 농도가 높을수록 탈착율이 증가하였다. 중금속으로 오염된 토양 복원시 Zn의 세척 용제로는 HCI 과 EDTA를, Cd의 세척 용제로는 HCI과 Oxalic acid를 가지고 세척을 함으로써 효과적으로 정화되는 것을 알 수 있었다.

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Purification and Characterization of a Novel Fibrinolytic Enzyme from Culture Supernatant of Pleurotus ostreatus

  • Liu, Xiao-Lan;Zheng, Xi-Qun;Qian, Peng-Zhi;Kopparapu, Narasimha-Kumar;Deng, Yong-Ping;Nonaka, Masanori;Harada, Naoki
    • Journal of Microbiology and Biotechnology
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    • 제24권2호
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    • pp.245-253
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    • 2014
  • A fibrinolytic enzyme was produced by an edible mushroom of Pleurotus ostreatus using submerged culture fermentation. The enzyme was purified from the culture supernatant by applying a combination of freeze-thaw treatment, ammonium sulfate precipitation, hydrophobic interaction, and gel filtration chromatographies. The enzyme was purified by a 147-fold, with a yield of 7.54%. The molecular masses of the enzyme an determined by gel filtration and SDS-PAGE were 13.6 and 18.2 kDa, respectively. The isoelectric point of the enzyme was 8.52. It hydrolyzed fibrinogen by cleaving the ${\alpha}$ and ${\beta}$ chains of fibrinogen followed by the ${\gamma}$ chains, and also activated plasminogen into plasmin. The enzyme was optimally active at $45^{\circ}C$ and pH 7.4. The enzyme activity was completely inhibited by EDTA, whereas protease inhibitors of TPCK, SBTI, PMSF, aprotinin and pepstatin showed no inhibition on its activity. The partial amino acid sequences of the enzyme as determined by Q-TOF2 were ATFVGCSATR, GGTLIHESSHFTR, and YTTWFGTFVTSR. These sequences showed a high degree of homology with those of metallo-endopeptidases from P. ostreatus and Armillaria mellea. The purified enzyme can also be applied as a natural agent for oral fibrinolytic therapy or prevention of thrombosis.

리튬이온이차전지에서 결정성 탄소재료가 탄소부극 특성에 미치는 영향 (The Effect of Crystalline Type of Carbonaceous Materials on Performance of the Carbon Anode for Lithium Ion Secondary Battery)

  • 김현중;이철태
    • 공업화학
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    • 제9권7호
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    • pp.1059-1064
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    • 1998
  • 본 연구는 리튬이온 이차전지용 탄소전극을 개발하기 위하여 다양한 종류의 흑연과 MCMB6-28을 대상으로 이루어졌다. 이들의 층간거리는 $3.358{\sim}3.363{\AA}$, BET 비 표면적은 $2.95{\sim}26.15m^2/g$이었다. 이들의 전기화학적 특성은 층간거리가 크고 적절한 크기의 BET 비 표면적을 가질 때 리튬의 삽입과 탈삽입 거동이 우수하였다. 다양한 결정성계 탄소전극 활물질에 도전재로 KJ-Black을 0, 3, 5wt% 첨가하였을 때 도전제의 함량이 많을수록 전극과 전해질의 계면저항은 작아지나 3wt%를 첨가하였을 때 우수한 가역성을 보였다. 정전류 충 방전 시 인가되는 전류밀도를 증가시킴에 따라 탄소부극의 방전용량은 작아졌다.

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Growth Responses of seven Intestinal Bacteria Against Phellodendron amurense Root-Derived Materials

  • Kim, Min-Jeong;Lee, Sang-Hyun;Cho, Jang-Hee;Kim, Moo-Key;Lee, Hoi-Seon
    • Journal of Microbiology and Biotechnology
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    • 제13권4호
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    • pp.522-528
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    • 2003
  • The growth responses of Phellodendron amurense root-derived materials against seven intestinal bacteria were examined, using an impregnated paper disk agar diffusion method and spectrometric method under $O_2$-free condition. The biologically active constituent of the P. amurense root extract was characterized as berberine chloride ($C_{20}H_{18}NO_{41}Cl$) using various spectroscopic analyses. The growth responses varied depending on the bacterial strain, chemicals, and dose tested. At 1 mg/disk, berberine chloride strongly inhibited the growth of Clostridium perfringens, and moderately inhibited the growth of Escherichia coli and Streptococcus mutans without any adverse effects on the growth of three lactic acid-bacteria (Bifidobacterium bifidum, B. longum, and Lactobacillus acidophilus). The structure-activity relationship revealed that berberine chloride exhibited more growth-inhibiting activity against C. perfringens, E. coli, and S. mutans than berberine iodide and berberine sulfate. These results, therefore, indicate that the growth-inhibiting activity of the three berberines was much more pronounced as chloridated analogue than iodided and sulphated analogues. As for the morphological effect caused by 1 mg/disk of berberine chloride, most strains of C. perfringens were damaged and killed, indicating that berberine chloride showed a strong inhibition against C. perfringens. As naturally occurring growth-inhibiting agents, the P. amurense root-derived materials described could be useful as a preventive agent against diseases caused by harmful intestinal bacteria such as clostridia.

Biochemical Characterization of $\small{L}$-Asparaginase in NaCl-Tolerant Staphylococcus sp. OJ82 Isolated from Fermented Seafood

  • Han, Sangwon;Jung, Jaejoon;Park, Woojun
    • Journal of Microbiology and Biotechnology
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    • 제24권8호
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    • pp.1096-1104
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    • 2014
  • $\small{L}$-Asparaginase from gram-positive bacteria has been poorly explored. We conducted recombinant overexpression and purification of $\small{L}$-asparaginase from Staphylococcus sp. OJ82 (SoAsn) isolated from Korean fermented seafood to evaluate its biotechnological potential as an antileukemic agent. SoAsn was expressed in Escherichia coli BL21 (DE3) with an estimated molecular mass of 37.5 kDa, determined using sodium dodecyl sulfate-polyacrylamide gel electrophoresis. Consistent with asparaginases in gram-negative bacteria, size-exclusion chromatography determined SoAsn as a homodimer. Interestingly, the optimal temperature of SoAsn was $37^{\circ}C$ and over 90% of activity was retained between $37^{\circ}C$ and $50^{\circ}C$, and its thermal stability range was narrower than that of commercial E. coli $\small{L}$-asparaginase (EcAsn). Both SoAsn and EcAsn were active between pH 9 and 10, although their overall pH-dependent enzyme activities were slightly different. The $K_m$ value of SoAsn was 2.2 mM, which is higher than that of EcAsn. Among eight metals tested for enzyme activity, cobalt and magnesium greatly enhanced the SoAsn and EcAsn activity, respectively. Interestingly, SoAsn retained more than 60% of its activity under 2 M NaCl condition, but the activity of EcAsn was reduced to 48%. Overall, the biochemical characteristics of SoAsn were similar to those of EcAsn, but its kinetics, cofactor requirements, and NaCl tolerance differed from those of EcAsn.

Exogenous Lytic Activity of SPN9CC Endolysin Against Gram-Negative Bacteria

  • Lim, Jeong-A;Shin, Hakdong;Heu, Sunggi;Ryu, Sangryeol
    • Journal of Microbiology and Biotechnology
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    • 제24권6호
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    • pp.803-811
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    • 2014
  • Concerns over drug-resistant bacteria have stimulated interest in developing alternative methods to control bacterial infections. Endolysin, a phage-encoded enzyme that breaks down bacterial peptidoglycan at the terminal stage of the phage reproduction cycle, is reported to be effective for the control of bacterial pathogenic bacteria. Bioinformatic analysis of the SPN9CC bacteriophage genome revealed a gene that encodes an endolysin with a domain structure similar to those of the endolysins produced by the P1 and P22 coliphages. The SPN9CC endolysin was purified with a C-terminal oligo-histidine tag. The endolysin was relatively stable and active over a broad temperature range (from $24^{\circ}C$ to $65^{\circ}C$). It showed maximal activity at $50^{\circ}C$, and its optimum pH range was from pH 7.5 to 8.5. The SPN9CC endolysin showed antimicrobial activity against only gram-negative bacteria and functioned by cutting the glycosidic bond of peptidoglycan. Interestingly, the SPN9CC endolysin could lyse intact gram-negative bacteria in the absence of EDTA as an outer membrane permeabilizer. The exogenous lytic activity of the SPN9CC endolysin makes it a potential therapeutic agent against gram-negative bacteria.

인체 폐암세포주에 대한 키토산의 항암효과와 항암제 감수성에 미치는 영향 (Antitumor Effect and the Change of Chemosensitivity of Chitosan in Human Lung Cancer Cell Line)

  • 노숙령
    • Journal of Nutrition and Health
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    • 제31권4호
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    • pp.739-746
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    • 1998
  • This study was designed to investigated the antitumor effect and change chemosensitivity of chitosan in 2 kinds of humen lung cancer cell lines(NCI-H522, NCI-H596). To evaluate the antitumor effect and synergistic effectof chomosensitivity, MTT assay was used in vitro. then anticancer drugs used were 챤-platin , ectoposide, and adrimycin. The results of this study were as follows; Chitosan shwoed in antitumor effect on both NCI-H522 and NCI-H596. The lung cancer viability percent for NCI-H522 and NCL-H596 showed at the lowest levels of 5.31 and 5.33% when the concentration of chitosan was 25mg/$m\ell$ media and the exposure time of chitosan was 72 hours. ID50 value of chitosan on both NCI-H522 and NCI-H596 showed at the lowest levels of 14.07, 11.68 mg/$m\ell$ media when the exposure time of chitosan was 72 hours. the synergistic effect of chomosensitivity was better in NCI-H596 than in NCI0H522 . When the synergistic effect of chomosensitivity was shown according to the kind of the anticancer drugs, in case of NCI-H522 , in the concentration of 100$\mu\textrm{g}$/$m\ell$, ectoposide showed the highest synergistic effect of chomosensitivity and then was adrimycin In case of NCI-H596, in the concentration of 100$\mu\textrm{g}$/$m\ell$,, the order of the synergistic effect of chomosensitivity was ectoposide>adrimycin>cis-platin and in the concentration of 10$\mu\textrm{g}$/$m\ell$, ectoposide>cis-platin >adrimycin. It is concluded that chitosan is an active antitumor agent and is increased chomosensitivity though there is difference according to the kind and the concentration of anticancer drugs. But to be sued to lung cancer theraphy, further studies on toxicity, the mechanism of action, animal experiment are wanted.

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