• 제목/요약/키워드: EC_{50}

검색결과 1,253건 처리시간 0.036초

청태전과 녹차 추출물의 이화학적 성분과 생리 활성 (Physical and Chemical Ingredients Components and Physiological Activity of Chungtaejeon and Green Tea Extracts)

  • 박용서;이미경;유현희;허북구
    • 동아시아식생활학회지
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    • 제18권3호
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    • pp.391-396
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    • 2008
  • This study was carried out to help restore and spread broaden the consumption of Chungtaejeon, a our traditional tea, Chungtaejeon in Korea, and as well as to gather the basic data on Chutaejeon tea. We have also compared the various ingredients components and physiological activities of Chungtaejeon tea extracts with that of green tea extracts. According to the results, the total phenol contents in of the Chungtaejeon and green tea extracts were 90.56 and 98.70 mg/100 mL, respectively, and their tannin contents levels in Chungtaejeon and green tea extracts were 214.14 mg/100 mL and 259.60 mg/100 mL, respectively, showing a difference in content. The catechin contents of the Chetaejeon and green tea extracts were in the order of EGC($15.80{\sim}16.50\;mg/100mL$), EGCG($10.40{\sim}10.60\;mg/100 mL$), and ECG($9.55{\sim}9.88\;mg/100 mL$), however, with the exception of EC(7.86 mg/100 mL) in the green tea extracts, there were not significant differences between that in them Chetaejeon and green tea extracts. Quercetin was the main flavonoid ingredient component in those both the Chungtaejeon and green tea extracts was quercetin, at levels of 0.08 mg/100 mL and 0.06 mg/100 mL and its contents in Chungtaejeon and green tea extracts were 0.08 mg/100 mL and 0.06 mg/100 mL, respectively. The primary amino acid in both tea extracts was theanine main amino acid at levels of, theanine contents were most increased in 8.02 mg/100mL and 10.80 mg/100 mL, respectively, Chungtaejeon tea extracts by 8.02 mg/100 mL and green tea extracts by 10.80 mg/100 mL. And the arginine contents of the Chungtaejeon and green tea extracts in Chungtaejeon and green tea extracts were 1.78 mg/100 mL and 1.86 mg/100 mL, respectively. In terms of mineral composition, potassium content was highest contents in the Chungtaejeon and green tea extracts by 19.80 and 18.04 mg/100 mL, respectively. Finally, the Chungtaejeon tea extracts offered the greatest anti-oxidation and ACE inhibition activities were most increased in the Chungtaejeon tea extracts, and the green tea extracts showed the highest level of nitrite radical scavenging activity at 90% was extremely much increased in the green tea extracts by 90%.

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Guinea Pig 기도상피세포가 기도 평활근 수축에 미치는 영향 (Influence of the Epithelium on the Contraction of Guinea Pig Isolated Tracheal Smooth Muscle)

  • 권오정;조상헌;박인원;김영환;한성구;심영수;김건열;한용철;서석효;김기환
    • Tuberculosis and Respiratory Diseases
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    • 제38권1호
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    • pp.8-15
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    • 1991
  • It has been well known that the integrity of airway epithelium is important in development of bronchial hyperreactivity and bronchial asthma. But the mechanisms involved are still unclear. To evaluate that airway epithelium is able to modulate the contraction of guinea pig tracheal smooth muscle, we investigated the responsiveness of intact and epithelium-denuded tracheal strips to histamine and acetylcholine. And to evaluate whether cyclooxgenase products play a role in this modulatory mechanism, we also investigated the effect of indomethacin pretreatment on the tracheal responsiveness to histamine. Results were as follows: 1) In guinea pig tracheal smooth muscle the presence of airway epithelium significantly reduced the response to histamine. 2) In the presence of indomethacin dose-response curves and $EC_{50}$ values were similar between intact and epithelium-denuded tracheal strips, that is, indomethacin abolished the influence of epithelium on the contracion of tracheal smooth muscle. 3) The response of tracheal smooth muscle to acetylcholine was similar both in the presence and absence of epithelium. These results suggest that airway epithelium of guinea pig may generate an inhibitory signal to decrease the response of tracheal smooth muscle to histamine and cyclooxygenase products may contrbute to the modulation of airway epithelium on the contracion of tracheal smooth muscle.

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Differential Effects of Ginsenoside Metabolites on HERG K+ Channel Currents

  • Choi, Sun-Hye;Shin, Tae-Joon;Hwang, Sung-Hee;Lee, Byung-Hwan;Kang, Ji-Yeon;Kim, Hyeon-Joong;Oh, Jae-Wook;Bae, Chun-Sik;Lee, Soo-Han;Nah, Seung-Yeol
    • Journal of Ginseng Research
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    • 제35권2호
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    • pp.191-199
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    • 2011
  • The human ether-a-go-go-related gene (HERG) cardiac $K^+$ channels are one of the representative pharmacological targets for development of drugs against cardiovascular diseases such as arrhythmia. Panax ginseng has been known to exhibit cardioprotective effects. In a previous report we demonstrated that ginsenoside $Rg_3$ regulates HERG $K^+$ channels by decelerating deactivation. However, little is known about how ginsenoside metabolites regulate HERG $K^+$ channel activity. In the present study, we examined the effects of ginsenoside metabolites such as compound K (CK), protopanaxadiol (PPD), and protopanaxatriol (PPT) on HERG $K^+$ channel activity by expressing human a subunits in Xenopus oocytes. CK induced a large persistent deactivatingtail current ($I_{deactivating-tail}$) and significantly decelerated deactivating current decay in a concentration-dependent manner. The $EC_{50}$ for persistent $I_{deactivating-tail}$ was $16.6{\pm}1.3$ ${\mu}M$. In contrast to CK, PPT accelerated deactivating-tail current deactivation. PPD itself had no effects on deactivating-tail currents, whereas PPD inhibited ginsenoside $Rg_3$-induced persistent $I_{deactivating-tail}$ and accelerated HERG $K^+$ channel deactivation in a concentration-dependent manner. These results indicate that ginsenoside metabolites exhibit differential regulation on Ideactivating-tail of HERG $K^+$ channel.

검정콩 안토시아닌의 항산화 및 암세포독성 (Antioxidant Activity and Cytotoxicity on Human Cancer Cells of Anthocyanin Extracted from Black Soybean)

  • 김용호;김동선;우성식;김현희;이영상;김희선;고광오;이석기
    • 한국작물학회지
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    • 제53권4호
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    • pp.407-412
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    • 2008
  • 검정콩 안토시아닌의 항산화력과 암세포독성을 분석한 결과는 다음과 같다. 1. 안토시아닌 함량은 일품검정콩이 공시재료 중 가장 높게 나타났으며, 특히 C3G 함량은 타 계통보다 2배 이상 높았다. 2. 안토시아닌을 분획한 후 각각의 pigment로 항산화 효과를 분석한 결과 TEAC 법과 DPPH법 모두 C3G, D3G, 및 Pt3G의 효과가 인정되었으며, C3G와 D3G의 항산화력이 높게 나타났다. 일품검정콩과 재래속청간 품종 비교에서는 일품검정콩이 3가지 분획 모두 재래속청 보다 항산화 효과가 높았으며, 이는 TEAC 법과 DPPH법 공히 같은 경향이었다. 3. 인간 암세포인 Jurkat T 세포와 MCF-7 세포에 안토시 아닌 개별색소(C3G, D3G 및 Pt3G)를 $100{\sim}500\;{\mu}g/mL$ 농도로 처리하고 암세포에 대한 독성을 관찰한 결과, 3가지 시험물질 모두 두 가지 암 세포에서 세포독성 효과를 나타내었다. 이와 같은 결과는 검정콩 안토시아닌이 여러 가지 생리활성 효과를 가지고 있음을 나타내는 결과로 판단된다.

Signal Transduction of Eel Luteinizing Hormone Receptor (eelLHR) and Follicle Stimulating Hormone Receptor (eelFSHR) by Recombinant Equine Chorionic Gonadotropin (rec-eCG) and Native eCG

  • Byambaragchaa, Munkhzaya;Lee, So-Yun;Kim, Dae-Jung;Kang, Myung-Hwa;Min, Kwan-Sik
    • 한국발생생물학회지:발생과생식
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    • 제22권1호
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    • pp.55-64
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    • 2018
  • Previous studies showed that recombinant equine chorionic gonadotropin ($rec-eCG{\beta}/{\alpha}$) exhibits both follicle-stimulating hormone (FSH) and luteinizing hormone (LH)-like activities in rat LHR- and FSHR-expressing cells. In this study, we analyzed signal transduction by eelFSHR and eelLHR upon stimulation with $rec-eCG{\beta}/{\alpha}$ and native eCG. The cyclic adenosine monophosphate (cAMP) stimulation in CHO-K1 cells expressing eelLHR was determined upon exposure to different doses (0-1,450 ng/mL) of $rec-eCG{\beta}/{\alpha}$ and native eCG. The $EC_{50$ values of $rec-eCG{\beta}/{\alpha}$ and native eCG were 172.4 and 786.6 ng/mL, respectively. The activity of $rec-eCG{\beta}/{\alpha}$ was higher than that of native eCG. However, signal transduction in the CHO PathHunter Parental cells expressing eelFSHR was not enhanced by stimulation with both agonist $rec-eCG{\beta}/{\alpha}$ and native eCG. We concluded that $rec-eCG{\beta}/{\alpha}$ and native eCG were completely active in cells expressing eelLHR, similar to the activity in the mammalian cells expressing LHRs. However, $rec-eCG{\beta}/{\alpha}$ and native eCG did not invoke any signaling response in the cells expressing eelFSHR. These results suggest that eCG has a potent activity in cells expressing eelLHR. Thus, we also suggest that $rec-eCG{\beta}/{\alpha}$ can induce eel maturation by administering gonadotropic reagents (LH), such as salmon pituitary extract.

Nematicidal Activity of Kojic Acid Produced by Aspergillus oryzae against Meloidogyne incognita

  • Kim, Tae Yoon;Jang, Ja Yeong;Jeon, Sun Jeong;Lee, Hye Won;Bae, Chang-Hwan;Yeo, Joo Hong;Lee, Hyang Burm;Kim, In Seon;Park, Hae Woong;Kim, Jin-Cheol
    • Journal of Microbiology and Biotechnology
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    • 제26권8호
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    • pp.1383-1391
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    • 2016
  • The fungal strain EML-DML3PNa1 isolated from leaf of white dogwood (Cornus alba L.) showed strong nematicidal activity with juvenile mortality of 87.6% at a concentration of 20% fermentation broth filtrate at 3 days after treatment. The active fungal strain was identified as Aspergillus oryzae, which belongs to section Flavi, based on the morphological characteristics and sequence analysis of the ITS rDNA, calmodulin (CaM), and β-tubulin (BenA) genes. The strain reduced the pH value to 5.62 after 7 days of incubation. Organic acid analysis revealed the presence of citric acid (515.0 mg/kg), malic acid (506.6 mg/kg), and fumaric acid (21.7 mg/kg). The three organic acids showed moderate nematicidal activities, but the mixture of citric acid, malic acid, and fumaric acid did not exhibit the full nematicidal activity of the culture filtrate of EML- DML3PNa1. Bioassay-guided fractionation coupled with 1H- and 13C-NMR and EI-MS analyses led to identification of kojic acid as the major nematicidal metabolite. Kojic acid exhibited dose-dependent mortality and inhibited the hatchability of M. incognita, showing EC50 values of 195.2 μg/ml and 238.3 μg/ml, respectively, at 72 h post-exposure. These results suggest that A. oryzae EML-DML3PNa1 and kojic acid have potential as a biological control agent against M. incognita.

생물검정법을 이용한 하수슬러지 장기연용 토양의 독성평가 (Toxicity Assessment of the Soil by Bioassay Following a Long-Term Application of Sewage Sludge)

  • 남재작;이승환;권순익;홍석영;임동규;고문환;송범헌
    • 한국환경농학회지
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    • 제23권4호
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    • pp.258-263
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    • 2004
  • 생물검정법에 의한 토양 내 독성평가의 유용성을 확인하기 위해 두 종류의 하수슬러지를 7년간 연용한 토양을 $Microtox^{(R)}$ 생물검정법과 상추종자 뿌리 신장법을 사용하여 독성을 평가하였다. 이 방법들은 하수오니의 종류나 시용량에 따른 토양의 독설 정도를 잘 평가 할 수 있었다. 상추종자 뿌리 신장법은 특별한 장비나 복잡한 처리 없이도 유의성 있는 결과를 구할 수 있었고 $Microtox^{(R)}$ 검정법은 전반적으로 재현성과 감도에서 유의성이 있었으며 또한 유기화합물에 대한 종합적인 평가도 가능하였다. 하수오니와 같이 다양한 화합뭍이 혼재되어 있는 유기성 자원의 토양 시용시 기존의 제한된 화학성분의 토양 분석법만으로는 독성평가에 한계가 있고 또 개별적으로는 별 영향이 없더라도 여러 화합물이 복합적으로 존재할 때 나타나는 독성작용에 대한 평가는 더욱이 어렵다. 그러므로 이러한 영향을 종합적으로 평가할 수 있는 생물검정법이 토양의 독성평가에서 화학분석법을 보완하는 평가방법으로서의 중요성은 충분하다고 할 수 있다. 그리고 생물독성법의 유용성을 높이기 위해서는 생물검정법의 시료 추출방법 개선과 실험의 재현성을 높이기 위한 노력이 필요하리라 생각된다. 따라서 이런 생뭍검정법의 많은 제약에도 불구하고 환경의 종합적인 평가에 있어서 생물검정법의 중요성은 대단히 크며 직접적으로 생물을 이용하는 방법뿐만 아니라 유전독성 평가방법 등 다양한 방법들이 환경독성 평가에 응용될 수 있을 것으로 판단된다.

Comparison of Inodilator Effect of Higenamine, YS49, YS51, Tetrahydroisoquinoline Analogs, and Dobutamine in the Rat

  • Chong, Won-Seog;Lee, Young-Soo;Kang, Young-Jin;Lee, Duck-Hyung;Ryu, Jae-Chun;Yun-Choi, Hye-Sook;Chang, Ki-Churl
    • The Korean Journal of Physiology and Pharmacology
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    • 제2권3호
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    • pp.323-330
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    • 1998
  • Tetrahydroisoquinoline (THI) alkaloids can be considered as cyclized derivatives of simple phenylethylamines. Many of them, especially with 6,7-disubstitution, demonstrate a relatively high affinity for catecholamines. Present study examines the pharmacological action of limited series of THI, using rats' isolated atria and aorta. In addition, a $[^3H]$ prazosin displacement binding study with THI compounds was performed, using rat brain homogenates to investigate whether these probes have ?${\alpha}$-adrenoceptor affinity. We also compared the vascular relaxation potency of these probes with dobutamine. YS 49, YS 51, higenamine and dobutamine, concentration-dependently, relaxed endothelium-denuded rat thoracic aorta precontracted with phenylephrine (PE, 0.1 ${\mu}M$) in which $pEC_{50}$ were $5.56{\pm}0.32$ and $5.55{\pm}0.21$, $5.99{\pm}1.16$ and $5.57{\pm}0.34$, respectively. These probes except higenamine also relaxed KCl (65.4 mM)-contracted aorta. In isolated rat atria, all THIs and dobutamine increased heart rate and contractile force. In the presence of propranolol, the concentration response curves of YS 49 and YS 51 shifted to the right and resulted in $pA_2$ values of $8.07{\pm}0.84$ and $7.93{\pm}0.11$, respectively. The slope of each compound was not deviated from unity, indicating that these chemicals are highly competitive at the cardiac ?${\beta}-adrenoceptors$. YS 49, YS 51, and higenamine showed ?${\alpha)-adrenoceptor$ affinity in rat brain, in which the dissociation constant $(K_i)$ was 2.75, 2.81, and 1.02 ${\mu}M$, respectively. It is concluded, therefore, that THI alkaloids have weak affinity to ${\alpha)_1-adrenoceptor$ in rat aorta and brain, respectively, while these probes show relatively high affinity for cardiac ${\beta}-adrenoceptors$. Thus, these chemicals may be useful in the treatment of congestive heart failure.

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실험견에서 Metoprolol 약리효과의 약동/력학적 검토 (Pharmacokinetic/Pharmacodynamic Analysis of Metoprolol in Dogs)

  • 오동진;장인진;이경훈;임동석;김형기;신상구;박찬웅;신재국
    • 대한약리학회지
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    • 제31권2호
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    • pp.251-259
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    • 1995
  • Pharmacokinetics and pharmacodynamics of metoprolol, a selective beta-l blocker, were examined for 360 minutes after intravenous bolus administration of metoprolol to 6 dogs. Plasma concentration and excreted amount in the urine metoprolol were measured by liquid chromatography with fluorescence detection. PR interval and heart rate were measured by ECG monitoring. Blood pressure was monitored through intraarterial catheter in femoral artery and cardiac output by thermodilution method using Swan-Ganz catheter. To analyze the effect site concentration-response relationship, plasma concentration and pharmacological effects were simultaneously fitted to a two pharmacokinetic compartment linked to pharmacodynamic model with NONLIN program. Results are as follows. 1) The plasma concentration of metoprolol after intrvenous injection decreased biexponentially. The terminal half-life estimated was $1.33{\pm}0.40$ hours and the volume of distribution at steady state (Vdss) and the total body clearance were $1.04{\pm}0.4\;L/kg,\;6.55{\pm}2.21\;L/hr$, respectively. The central compartment volume of distribution and peripheral compartment volume of distribution were $0.35{\pm}0.14L/kg\;and\;0.69{\pm}0.34L/kg$. The renal clearance and intercompartment clearance were $0.53{\pm}0.25\;L/min\;and\;0.35{\pm}0.19\;L/min$. 2) Simulated biophase concentration-response curve shows hyperbolic relationship and the estimated concentration-effect relationship was best explained by Emax model when the prolongation of PR interval and the reduction of the heart rate were used as pharmacodynamic parameters. Emax and EC50 were estimated to be $26.3{\pm}4.7\;msec\;and\;88.8{\pm}82.3\;g/ml$ for PR interval, and $48.7{\pm}18.8\;beats/min\;and\;113.5{\pm}78.7\;ng/ml$ for heart rate, respectively. 3) The changes of cardiac output-effect site concentration relationship was best fitted by a linear model and the slope of the relationship was $0.005{\pm}0.003$. Diastolic blood pressure-effect site concentration relationship was also explained by the linear model and the slope of the relationship was $0.038{\pm}0.034$.

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Airway Smooth Muscle Sensitivity to Methacholine in Precision-Cut Lung Slices (PCLS) from Ovalbumin-induced Asthmatic Mice

  • Kim, Hae Jin;Kim, Yeryung;Park, Su Jung;Bae, Boram;Kang, Hye-Ryun;Cho, Sang-Heon;Yoo, Hae Young;Nam, Joo Hyun;Kim, Woo Kyung;Kim, Sung Joon
    • The Korean Journal of Physiology and Pharmacology
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    • 제19권1호
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    • pp.65-71
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    • 2015
  • Asthma is a chronic inflammatory disease characterized by airway hyperresponsiveness (AHR) and reversible airway obstruction. Methacholine (MCh) is widely used in broncho-provocation test to evaluate airway resistance. For experimental investigation, ovalbumin-induced sensitization is frequently used in rodents (Ova-asthma). However, albeit the inflammatory histology and AHR in vivo, it remains unclear whether the MCh sensitivity of airway smooth muscle isolated from Ova-asthma is persistently changed. In this study, the contractions of airways in precision-cut lung slices (PCLS) from control, Ova-asthma, and IL-13 overexpressed transgenic mice (IL-13TG) were compared by analyzing the airway lumen space (AW). The airway resistance in vivo was measured using plethysmograph. AHR and increased inflammatory cells in BAL fluid were confirmed in Ova-asthma and IL-13TG mice. In the PCLS from all three groups, MCh concentration-dependent narrowing of airway lumen (${\Delta}AW$) was observed. In contrast to the AHR in vivo, the $EC_{50}$ of MCh for ${\Delta}AW$ from Ova-asthma and IL-13TG were not different from control, indicating unchanged sensitivity to MCh. Although the AW recovery upon MCh-washout showed sluggish tendency in Ova-asthma, the change was also statistically insignificant. Membrane depolarization-induced ${\Delta}AW$ by 60 mM $K^+$ (60K-contraction) was larger in IL-13TG than control, whereas 60K-contraction of Ova-asthma was unaffected. Furthermore, serotonin-induced ${\Delta}AW$ of Ova-asthma was smaller than control and IL-13TG. Taken together, the AHR in Ova-asthma and IL-13TG are not reflected in the contractility of isolated airways from PCLS. The AHR of the model animals seems to require intrinsic agonists or inflammatory microenvironment that is washable during tissue preparation.