• 제목/요약/키워드: suppressing activity

검색결과 446건 처리시간 0.03초

Preparation of Benzoyloxy Benzophenone Derivatives and Their Inhibitory Effects of ICAM-1 Expression

  • Kwon, Eun-Mi;Kim, Cheol-Gi;Goh, Ah-Ra;Park, Jin-Seu;Jun, Jong-Gab
    • Bulletin of the Korean Chemical Society
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    • 제33권6호
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    • pp.1939-1944
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    • 2012
  • Benzoyloxy benzophenone derivatives were prepared in 3 steps including DCC coupling, Fries rearrangement and esterification from benzoic acids in 24-89% total yields. Among the prepared 12 benzophenone analogues 1a-1l, the compound 1b having three chloro groups at the para position showed maximum inhibitory effects of ICAM-1 expression but, 1a which have no substituents at all showed no inhibitory activity. This study provides the evidences that benzoyloxy benzophenone derivative, 1b may exert its anti-inflammatory activity by suppressing IFN-${\gamma}$-induced ICAM-1 expression.

Antioxidant Activity and Inhibitory Effects on Oxidative DNA Damage of Callus from Abeliophyllum distichum Nakai

  • Jang, Tae Won;Park, Jae Ho
    • 한국자원식물학회지
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    • 제31권3호
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    • pp.228-236
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    • 2018
  • In this study, we evaluated the antioxidant activity and protective effects against oxidative DNA damage of the ethyl acetate fraction from the callus of Abeliophyllum distichum Nakai (ECA). Callus of A. distichum was induced on MS medium containing NAA (1 mg/L) and 2,4-D (1 mg/L), and a sufficient amount was obtained for the extraction by subculture. Acteoside was analyzed and quantified (0.39 mg/g callus) from ECA using the high-performance liquid chromatography-photodiode array detector method. ECA showed very high antioxidative activity as revealed by DPPH and ABTS scavenging assays. The $IC_{50}$ values were 12.4 and $6.8{\mu}g/ml$, respectively. ECA showed protective effects against oxidative DNA damage evaluated by using ${\Psi}X-174$ RF I plasmid DNA. It also inhibited DNA damage by suppressing the oxidative stress-induced protein and mRNA levels of ${\gamma}$-H2AX and p53 in NIH/3T3 cells. In conclusion, ECA protects against oxidative DNA damage through its powerful antioxidant activity.

Antioxidant and Skin Anti-Aging Effects of Marigold Methanol Extract

  • Kang, Chul Ho;Rhie, Sung Ja;Kim, Young Chul
    • Toxicological Research
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    • 제34권1호
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    • pp.31-39
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    • 2018
  • The objective of this study was to evaluate the antioxidant and anti-aging effects of marigold methanol extract (MGME) in human dermal fibroblasts. Total polyphenolic and flavonoid contents in MGME were 74.8 mg TAE (tannic acid equivalent)/g and 85.6 mg RE (rutin equivalent)/g, respectively. MGME ($500{\mu}g/mL$) increased 1,1-diphenyl-2-picryl hydrazyl (DPPH) and 2,2'-azino-3-ethylbenzothiazoline-6-sulfonic acid (ABTS) radical-scavenging, and superoxide dismutase (SOD)-like antioxidant activities by 36.5, 54.7, and 14.8%, respectively, compared with the control. At $1,000{\mu}g/mL$, these activities increased by 63.7, 70.6, and 20.6%, respectively. MGME ($100{\mu}g/mL$) significantly increased the synthesis of type 1 procollagen by 83.7% compared with control treatment. It also significantly decreased Matrix Metalloproteinase-2 (MMP-2) activity and MMP-1 mRNA expression by 36.5% and 69.5%, respectively; however, it significantly increased laminin-5 mRNA expression by 181.2%. These findings suggest that MGME could protect human skin against photo-aging by attenuating oxidative damage, suppressing MMP expression and/or activity as well as by stimulating collagen synthesis.

적백하오관중탕 약침액이 노화 흰쥐 비장세포의 면역활성에 미치는 영향 (The Effect of Jeokbaekhaogwanjung-tang Herbal Acupuncture Solution on the Immune Activity of Spleen Cells of Aged Rats)

  • 이현석;최강민;임윤경
    • 대한한의학회지
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    • 제37권1호
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    • pp.90-100
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    • 2016
  • Objectives: The purpose of this study was to investigate the effect of Jeokbaekhaogwanjung-tang (JGT) distillate on the immune activity of spleen cells of aged rats. Methods: Spleen cells of 10w, 52w 72w old SD rats were cultured and treated with JGT distillate and the levels of IL-2, IL-4, IL-10 and IFN-${\gamma}$ were measured. Results: 1. The levels of IL-2 and IFN-${\gamma}$ in the spleen cells of 52w old rats were significantly decreased by JGT treatment. 2. The level of IFN-${\gamma}$ in the spleen cells of 72w old rats were significantly decreased by JGT treatment. Conclusion: These results suggest that Jeokbaekhaogwanjung-tang distillate has an immune regulative effect by way of suppressing the change of immune activity caused by aging in rats.

방사선(放射線) 조사(照射)가 숙성(熟成)시킨 감자 괴경(塊莖) 박편(薄片)에서 Invertase, 핵산(核酸) 및 호흡작용(呼吸作用)의 발달(發達)에 미치는 영향(影響) (Effects of Ionizing Radiation on Development of Invertase Activity, Nucleic Acids, and Respiratory Activity in Aging Potato Tuber Slices)

  • 이미순;김홍열;홍영표
    • 한국식품과학회지
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    • 제5권3호
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    • pp.157-162
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    • 1973
  • 무균(無菌) 상태하에서 습윤한 여지위에 숙성(熟成)시킨 감자 괴경 박편(塊莖 薄片) $(1mm{\times}1.5cm)$을 재료로 방사선(放射線)의 작용기작(作用幾作)연구를 행하였다. Invertase, 핵산 및 호흡작용의 time courses를 결정하고 이들 세작용의 방사선(放射線)에 대한 민감도를 측정하였다. 세 작용 중 어느 것도 세포분열을 억제하는 선량에서 심하게 억제되지 않았다. $^3H-thymidine$의 incorporation 결과는 방사선(放射線)의 작용부위가 mitosis나 $G_2$ period에 존재할지도 모른다는 것을 암시한다.

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Comparison of the antioxidant and anti-inflammatory activities of leaf extracts from grain amaranths (Amaranthus spp.)

  • Ji, Hyo Seong;Kim, Gayeon;Ahn, Min-A;Chung, Jong-Wook;Hyun, Tae Kyung
    • Journal of Plant Biotechnology
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    • 제49권1호
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    • pp.99-105
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    • 2022
  • This study assessed the antioxidant and anti-inflammatory activities of leaf extracts from grain amaranths (Amaranthus spp.). Among all the extracts, the ethanol extract of Amaranthus cruentus leaves (Ar) exhibited the highest antioxidant activity, including the DPPH free radical scavenging activity and ORAC. In addition, Ar strongly inhibited nitric oxide production by suppressing the MEK/ERK signaling pathway in lipopolysaccharide-stimulated RAW264 murine macrophages. HPLC analysis revealed 13 polyphenolic compounds in the leaf extracts of grain amaranth and indicated that Ar contained more rutin than the other extracts. Taken together, these results show the impact of species diversity on the phytochemical contents and bioactivities of plant extracts and suggest that the nonedible parts, such as leaves, of A. cruentus should be considered for use as crude drugs and dietary health supplements.

Epigallocatechin-3-gallate Inhibits Tax-dependent Activation of Nuclear Factor Kappa B and of Matrix Metalloproteinase 9 in Human T-cell Lymphotropic Virus-1 Positive Leukemia Cells

  • Harakeh, Steve;Diab-Assaf, Mona;Azar, Rania;Hassan, Hani Mutlak Abdulla;Tayeb, Safwan;Abou-El-Ardat, Khalil;Damanhouri, Ghazi Abdullah;Qadri, Ishtiaq;Abuzenadah, Adel;Chaudhary, Adeel;Kumosani, Taha;Niedzwiecki, Aleksandra;Rath, Mathias;Yacoub, Haitham;Azhar, Esam;Barbour, Elie
    • Asian Pacific Journal of Cancer Prevention
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    • 제15권3호
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    • pp.1219-1225
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    • 2014
  • Epigallocatechin-3-gallate (EGCG) is the most abundant polyphenol molecule from green tea and is known to exhibit antioxidative as well as tumor suppressing activity. In order to examine EGCG tumor invasion and suppressing activity against adult T-cell leukemia (ATL), two HTLV-1 positive leukemia cells (HuT-102 and C91-PL) were treated with non-cytotoxic concentrations of EGCG for 2 and 4 days. Proliferation was significantly inhibited by 100 ${\mu}M$ at 4 days, with low cell lysis or cytotoxicity. HTLV-1 oncoprotein (Tax) expression in HuT-102 and C91-PL cells was inhibited by 25 ${\mu}M$ and 125 ${\mu}M$ respectively. The same concentrations of EGCG inhibited NF-kB nuclearization and stimulation of matrix metalloproteinase-9 (MMP-9) expression in both cell lines. These results indicate that EGCG can inhibit proliferation and reduce the invasive potential of HTLV-1-positive leukemia cells. It apparently exerted its effects by suppressing Tax expression, manifested by inhibiting the activation of NF-kB pathway and induction of MMP-9 transcription in HTLV-1 positive cells.

Antiviral Activity of Chrysin Derivatives against Coxsackievirus B3 in vitro and in vivo

  • Song, Jae-Hyoung;Kwon, Bo-Eun;Jang, Hongjun;Kang, Hyunju;Cho, Sungchan;Park, Kwisung;Ko, Hyun-Jeong;Kim, Hyoungsu
    • Biomolecules & Therapeutics
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    • 제23권5호
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    • pp.465-470
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    • 2015
  • Chrysin is a 5,7-dihydroxyflavone and was recently shown to potently inhibit enterovirus 71 (EV71) by suppressing viral 3C protease ($3C^{pro}$ activity. In the current study, we investigated whether chrysin also shows antiviral activity against coxsackievirus B3 (CVB3), which belongs to the same genus (Enterovirus) as EV71, and assessed its ability to prevent the resulting acute pancreatitis and myocarditis. We found that chrysin showed antiviral activity against CVB3 at $10{\mu}M$, but exhibited mild cellular cytotoxicity at $50{\mu}M$, prompting us to synthesize derivatives of chrysin to increase the antiviral activity and reduce its cytotoxicity. Among four 4-substituted benzyl derivatives derived from C(5) benzyl-protected derivatives 7, 9-11 had significant antiviral activity and showed the most potent activity against CVB3 with low cytotoxicity in Vero cells. Intraperitoneal injection of CVB3 in BALB/c mice with $1{\times}10^6TCID_{50}$ (50% tissue culture infective dose) of CVB3 induced acute pancreatitis with ablation of acinar cells and increased serum CXCL1 levels, whereas the daily administration of 9 for 5 days significantly alleviated the pancreatic inflammation and reduced the elevation in serum CXCL1 levels. Collectively, we assessed the anti-CVB3 activities of chrysin and its derivatives, and found that among 4-substituted benzyl derivatives, 9 exhibited the highest activity against CVB3 in vivo, and protected mice from CVB3-induced pancreatic damage, simultaneously lowering serum CXCL1 levels.

Effects of Brazilin on Induction of Immunological Tolerance by Sheep Red Blood Cells in C57BL/6 Female Mice

  • Mok, Myoung-Soo;Jeon, Sun-Duck;Yang, Kyoung-Mee;So, Dhong-Su;Moon, Chang-Kiu
    • Archives of Pharmacal Research
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    • 제21권6호
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    • pp.769-773
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    • 1998
  • Brazilin was examined for its effects on the induction of immunological tolerance. Brazilin was administered to C57BL/6 female mice for 2 consecutive days before the immunization with high dose SRBC (109 cells) which can produce immunological tolerance. Delayed type hypersensitivity, IgM plaque forming cells, ConA induced IL-2 production and mitogen- or antigen-induced proliferation of lymphocytes were measured as evaluation parameters. Administration of brazilin prior to immunization could keep the DTH and IL-2 production almost optimaly immunized levels. Brazilin also inhibited the elevation of non-specific suppressor cell activity. ConA induced proliferation of splenocytes in high dose SRBC immunized mice was significantly decreased by pretreatment of brazilin. And this might be one of the reason for augmentation of DTH by brazilin. However, IgM plaque forming cells were not affected by the treatment of brazilin. These results indicate that brazilin prevents the induction of mmunological tolerance caused by high dose SRBC by suppressing the elevation of suppressor cell activity and by inhibiting the decrease in IL-2 production in C57BL/6 female mice.

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조해(照海) 전침의 항산화 효과에 대한 실험적 연구 (Antioxidative Effects of Electro-acupuncture at $KI_6$ on Rats Treated with AAPH)

  • 김연미;이병렬;홍권의
    • Journal of Acupuncture Research
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    • 제25권1호
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    • pp.107-120
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    • 2008
  • Objectives : This study investigated the antioxidant effect of electro-acupuncture at $KI_6$ on rats treated with 2,2'-azobis(2-amidinopropane) dihydrochloride(AAPH). Methods : After electro-acupuncture at $KI_6$ on 48 rats that were given AAPH(50mg/kg) every day, the author observed several changes in weight, liver index, albumin, total bilirubin, LDL-cholesterol, LDH, glucose, GOT, GPT, SOD and catalase activity, and glutathione, NO, and MDA concentrations. Results : 1. In the $KI_6-EA$ group, the albumin level increased and LDL-cholesterol decreased compared with the control and holder groups. 2. In the $KI_6-EA$ group, SOD activity increased compared with the holder group, glutathione concentration increased compared with the control and holder groups, and catalase activity increased compared with the control group. 3. In the $KI_6-EA$ group, NO concentration decreased compared with the control and holder groups. Conclusions : This case shows that electro-acupuncture at $KI_6$ plays a significant antioxidant role by elevating defenses against cell toxicity caused by oxidative stress and suppressing oxidative injury.

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