• Title/Summary/Keyword: in vitro activity

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The EphA8 Receptor Phosphorylates and Activates Low Molecular Weight Phosphotyrosine Protein Phosphatase in Vitro

  • Park, Soo-Chul
    • BMB Reports
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    • v.36 no.3
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    • pp.288-293
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    • 2003
  • Low molecular weight phosphotyrosine protein phosphatase (LMW-PTP) has been implicated in modulating the EphB1-mediated signaling pathway. In this study, we demonstrated that the EphA8 receptor phosphorylates LMW-PTP in vitro. In addition, we discovered that mixing these two proteins leads to EphA8 dephosphorylation in the absence of phosphatase inhibitors. Finally, we demonstrated that LMW-PTP, modified by the EphA8 autokinase activity, possesses enhanced catalytic activity in vitro. These results suggest that LMW-PTP may also participate in a feedback-control mechanism of the EphA8 receptor autokinase activity in vivo.

Preliminary Study on the Antisnake Venom Activity of Alcoholic Root Extract of Clerodendrum viscosum (Vent.) in Naja naja Venom

  • Lobo, Richard;Punitha, I.S.R.;Rajendran, K.;Shirwaikar, Arun;Shirwaikar, Annie
    • Natural Product Sciences
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    • v.12 no.3
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    • pp.153-156
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    • 2006
  • The antisnake venom activity of Clerodendrum viscosum Vent. (Fam. Verbenaceae), a plant traditionally used in India for the treatment of snake bite was evaluated by in vitro and in vivo methods. While in vitro studies were performed using human blood, in vivo studies were carried out using mice administered three different i.p doses of the extract, 5 min before the administration of Naja naja snake venom. The results of the in vitro studies showed that the extract probably interacts with but does not stabilize membrane protein. In the in vivo studies the extract showed significant antisnake venom activity, which may be attributed to its possible interference with the acetylcholine receptor sites. Hence the present investigation justifies the traditional use of Clerodendrum viscosum (C. viscosum) as antisnake venom.

The anti-platelet activity of panaxadiol fraction and panaxatriol fraction of Korean Red Ginseng in vitro and ex vivo

  • Yuan Yee Lee;Yein Oh;Min-Soo Seo;Min-Goo Seo;Jee Eun Han;Kyoo-Tae Kim;Jin-Kyu Park;Sung Dae Kim;Sang-Joon Park;Dongmi Kwak;Man Hee Rhee
    • Journal of Ginseng Research
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    • v.47 no.5
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    • pp.638-644
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    • 2023
  • Background: The anti-platelet activity of the saponin fraction of Korean Red Ginseng has been widely studied. The saponin fraction consists of the panaxadiol fraction (PDF) and panaxatriol fraction (PTF); however, their anti-platelet activity is yet to be compared. Our study aimed to investigate the potency of anti-platelet activity of PDF and PTF and to elucidate how well they retain their anti-platelet activity via different administration routes. Methods: For ex vivo studies, Sprague-Dawley rats were orally administered 250 mg/kg PDF and PTF for 7 consecutive days before blood collection via cardiac puncture. Platelet aggregation was conducted after isolation of the washed platelets. For in vitro studies, washed platelets were obtained from Sprague-Dawley rats. Collagen and adenosine diphosphate (ADP) were used to induce platelet aggregation. Collagen was used as an agonist for assaying adenosine triphosphate release, thromboxane B2, serotonin, cyclic adenosine monophosphate, and cyclic guanosine monophosphate (cGMP) release. Results: When treated ex vivo, PDF not only inhibited ADP and collagen-induced platelet aggregation, but also upregulated cGMP levels and reduced platelet adhesion to fibronectin. Furthermore, it also inhibited Akt phosphorylation induced by collagen treatment. Panaxadiol fraction did not exert any antiplatelet activity in vitro, whereas PTF exhibited potent anti-platelet activity, inhibiting ADP, collagen, and thrombin-induced platelet aggregation, but significantly elevated levels of cGMP. Conclusion: Our study showed that in vitro and ex vivo PDF and PTF treatments exhibited different potency levels, indicating possible metabolic conversions of ginsenosides, which altered the content of ginsenosides capable of preventing platelet aggregation.

In vitro antimicrobial activity of Korean propolis against fish pathogenic bacteria (Propolis의 어류 병원성 세균에 대한 in vitro 항균 효과)

  • Heo, Gang-Joon;Won, Tae-Gyeong;Shin, Gee-Wook
    • Korean Journal of Veterinary Service
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    • v.38 no.2
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    • pp.65-70
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    • 2015
  • The present study was to investigate in vitro antimicrobial effects of propolis against six different fish bacterial pathogens, Aeromonas hydrophila, Edwardsiella tarda, Vibrio vulnificus, V. parahaemolyticus, A. salmonicida subsp. masoucida, A. salmonicida subsp. salmonicida) using minimum inhibitory concentration (MIC) and minimum bacteriocidal concentration (MBC) tests. In the results, propolis exhibited antimicrobial activity against all bacteria used in the present study, but there was no marked difference in bacterial species except Vibrio species. Collectively, propolis was thought to be an usefulness antimicrobial substance for controlling bacterial diseases in the fish industry.

A Study on the Antimicrobial Activity and in vitro Cytotoxicity of UVB Sunscreen Chemicals in Cosmetic Products (UVB 자외선 차단제의 항균력 및 피부자극에 관한 연구)

  • 최종완;허윤석;손근욱
    • Proceedings of the SCSK Conference
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    • 1992.09a
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    • pp.46-68
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    • 1992
  • To investigate the effect on the antimicrobial activity against S.aureus ATCC 6538, E.coli KCTC 1039 and cell toxic level against transformed mouse fibroblast L929 in formula added with various concentrations of UVB blockers commonly used in cosmetic products, these experiments were carried out by preservative efficacy testing methods and in vitro cytotoxicity methods. The results obtained were as follow ; 1) Octyl Dimethyl PABA had a broad antibacterial spectrum against the Gram (+) and the Gram(-) bacteria at 5.84 % concentration, but not Octyl Methoxycinnamate. 2) Antibacterial activity was decreased in a combined UVB blocker system of squalane base. Especially, Octyl Dimethyl PABA was inactivated by Octyl Methoxycinnamate at 5.84% concentration to a large extents , but not 4-Methylbenzylidene Camphor. 3) Within in vitro cytotoxicity by use of mouse fibroblast L929 on UV-B blockers, NR assay was more excellent than MTT assay on quantitative

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Hepatoprotective activity of terpenoids and terpenoid fractions of Scoparia dulcis L

  • Krishnamurthy, Praveen Thaggikuppe;Bajaj, Jitendra;Sharma, Abhishek;Manimaran, Sellappan;Ravanappa, Prashantha Kumar Bommenahalli;Pottekad, Vijayan
    • Advances in Traditional Medicine
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    • v.10 no.4
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    • pp.263-270
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    • 2010
  • Scoparia dulcis L. is widely used in the traditional system of medicine for treating liver ailments. In the present study the terpenoids and terpenoid fractions isolated from 1:1:1 petroleum ether, diethyl ether and methanol (PDM) extract of Scoparia dulcis L. were tested for their in vitro 1, 1-Diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity. Selected samples from the assay were further tested for their in vitro hepatoprotective activity against $CCl_4$ induced hepatotoxicity in freshly isolated rat hepatocytes. In the in vitro antioxidant study, fractions 7, 11, 13, 14, and 15 and PDM extract show the DPPH radical scavenging activity. The phytochemical screening of all these fractions show the presence of terpenoids. In the in vitro hepatoprotective study all these fractions and the PDM extract significantly prevent the $CCl_4$ induced changes in the aspartate aspartate amino transferase, alanine amino transferase and alkaline phosphatase levels (p < 0.05). The above results are comparable with the standard, silymarin. The results of the study indicate that, the PDM extract of Scoparia dulcis L. possesses potential hepatoprotective activity and this may be attributed to its free radical scavenging potential, which in turn may be attributed to the presence of terpenoids.

Effects of Calendula Officinalis L. Extract on the Activation of Murine Lymphocytes and Macrophages (금잔화 추출물이 생쥐의 임파구 및 대식세포의 활성에 미치는 영향)

  • Eun, Jae-Soon
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.23 no.4
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    • pp.825-830
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    • 2009
  • The purpose of this research was to investigate the effects of Calendula officinalis extract (CE) on the activation of murine lymphocytes and macrophages. CE was administered p.o. once a day for 7 days at the concentration of 500 mg/kg. The administration of CE increased the viability of thymocytes, but decreased the viability of splenocytes. Also, CE increased the viability of thymocytes and splenocytes at the concentration of $5{\mu}g$/ml in vitro. The administration of CE did not affect the population of thymic $CD4^+$/$CD8^+$ cells and splenic $CD4^+$/$CD8^+$ cells. Furthermore, the administration of CE enhanced the phagocytic activity of peritoneal macrophages, but decreased the phagocytic activity in vitro. CE decreased the production of nitric oxide from peritoneal macrophages in vivo and in vitro system. These results suggest that CE enhance of cell viability by a direct influence on thymocytes and phagocytic activity by an indirect influence on peritoneal macrophages.

Changes in Antioxidant Activity and Total Phenolic Content of Water Spinach (Ipomoea aquatic Forsk.) under In Vitro Biomimicking System

  • Lee, A-Young;Kim, Young-Suk;Shim, Soon-Mi
    • Food Engineering Progress
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    • v.14 no.4
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    • pp.342-345
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    • 2010
  • The purpose of current study was to examine bioaccessibility of antioxidant activity and total phenolic content in each part of water spinach (Ipomoea aquatic Forsk.). In vitro biomimicking system simulated human digestive fluid was employed in order to measure bioavailable anti-oxidative effect and phenolic content. Antioxidant activity and total phenolic content was measured by using the DPPH method and the Folin-Ciocalteu assay, respectively. Stem of water spinach had a higher DPPH free radical scavenging effect (5.43 mg/mL for $IC_{50}$) than leaf (5.95 mg/mL for $IC_{50}$), while leaf had a greater level of total phenolic content (287.45 ${\mu}g$ GAE/mL) than stem (216.45 ${\mu}g$ GAE/mL). Bioaccessible antioxidant capacity and digestive stability of total phenolic content showed a similar pattern to what found in raw materials. Our result also indicated that total phenolic content was not found to be a major marker for prediction of antioxidant activity. It is plausible that other constituents such as vitamin E and C in water spinach could be contributors for antioxidant activities.

Screening of Anticancer Potential of Celecoxib and its Derivatives (셀레콕시브 및 그 합성유도체들의 항암활성 스크리닝)

  • Park, Jeong-Ran;Kang, Jin-Hyoung;Kuh, Hyo-Jeong;Noh, Ji-Young;Ryu, Hyung-Chul;Park, Sang-Wook;Ko, Dong-Hyun;Cho, Il-Hwan;Lee, Joo-Y.;Hwang, Daniel-H.;Kim, In-Kyung
    • Journal of Pharmaceutical Investigation
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    • v.33 no.2
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    • pp.105-112
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    • 2003
  • Selective COX (cyclooxygenase)-2 inhibitors including celecoxib have been shown to induce apoptosis and cell cycle changes in various tumor cells. New inhibitors are recently being developed as chemomodulating agents. We evaluated celecoxib and screened 150 synthetic compounds for anti-proliferative activities in vitro. Effects of celecoxib on COX activity, cell growth, cell cycle distribution, and apoptosis induction were determined in A549 COX-2 overexpressing human non-small cell lung cancer (NSCLC) cells. The COX inhibition of celecoxib increased with concentration up to 82% at $1\;{\mu}M$ after 24 hr exposure. Forty ${\mu}M$ and $50\;{\mu}M$ of ce1ecoxib induced $G_1$ arrest, and TUNEL-positive apoptotic cells, respectively. Among 150 compounds, several compounds were selected for having greater COX-2 inhibitory activity and higher selectivity than celecoxib with growth inhibitory activity. Celecoxib showed concentration-dependent COX inhibitory activity, and ability to induce cell cycle arrest and apoptosis in human NSCLC cells in vitro. Among synthetic analogues screened, several compounds showed promising in vitro activity as COX-2 inhibitory anticancer agents, which warrant further evaluation in vitro and in vivo.

$\beta$-Lactamase Inhibitory Activity and Comparative Activity of Sulbactam Derivatives Combined with $\beta$-Lactam Antibiotics (Sulbactam 유도체의 베타락타마제 효소억제력과 베타락탐항생제 병용시 활성비교)

  • 임채욱;박희석;김용현;임철부
    • YAKHAK HOEJI
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    • v.46 no.6
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    • pp.387-391
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    • 2002
  • In vitro $\beta$-lactamase inhibitory activity of 6-exomethylene sulbactam compounds (CH-120, 130, 140, 145, 150, 155) was compared with clavulanic acid, sulbactam and tazobactam. The inhibitory activity of CH-140 was stronger than sulbactam and clavulanic acid against Type II, III, IV, TEM enzymes and stronger than tazobactam against Type IV enzyme. The inhibitory activity of CH-145 was stronger than sulbactam and clavulanic acid against Type I, II, III, IV, TEM enzymes and stronger than tazobactam against Type III, IV enzymes. The in vitro antimicrobial activity of CH-140 and CH-145 combined with piperacillin and ceftriaxone was compared with the sulbactam and tazobactam against $\beta$-lactamase producing 31 strains. But, synergistic activity of CH-140 and CH-145 was inferior to tazobactam.