• Korean Journal of Acupuncture
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• v.23 no.3
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• pp.123-131
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• 2006

목 적 : 과산화수소는 산화적 스트레스를 통해 아폽토시스를 유도하는 것으로 알려져 있다. 본 논문에서는 과산화수소로 유발된 신경아세포종 아폽토시스 과정에서 호도약침액의 효과를 관찰하였다. 방 법 : 과산화수소로 인한 신경아세포종의 아폽토시스에서 호도약침액의 효과를 알아보기 위해 배양 중인 신경아세포종에 과산화수소를 처리하고, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide(MIT)분석법, 4,6-diamidino-2-phenylindole (DAPI) 염색법, reverse transcription-polymerase chain reaction (RT-PCR), western blotting의 방법으로 확인하였다. 결 과 : 과산화수소로 인한 신경아세포종의 아폽토시스에서 호도약침액을 처리한 결과, 약침액을 처리한 세포의 생존이 약 30% 정도 증가하고, 핵 응축과 단편화를 막아주며, CASP3와 BAX단백질의 발현이 감소되었다. 결 론 : 이러한 결과로 호도약침액이 과산화수소로 인한 신경아세포종의 아폽토시스과정에서 보호효과를 나타내는 것으로 사료된다.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1994.04a
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• pp.287-287
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• 1994

In the present study, it was aimed to asses the possibility that calcitonin gene-related peptide (CGRP) released in response to transient hypotension may contribute to the reflex autoregulation of cerebral blood flow as a putative modulator. Changes in pial arterial diameter (mean, 33.0 ${\pm}$ 1.1 $\mu\textrm{m}$) with changes in systemic arterial blood pressure (mean, 101.9 ${\pm}$ 2.7 mmHg) were observed directly through a closed cranial window in anesthetized normotensive rats. Image of the pial vessels was captured with a stereoscope connected to a CCD video camera and the diameter was measured with a microscaler. In the capsaicin-treated rats (one day prior to experiment, 50 nmol capsaicin injected intracisternally), both vasodilater and vasoconstrictor responses evoked by a transient hypotension and the reverse of blood pressure were markedly attenuated or almost abolished. When changes in pial arterial diameter were plotted as a function of changes in blood pressure, the slopes of both regression lines (for vasodilators and vasoconstrictors ) were markedly reduced. Similar reductions were evidenced under treatment wi th the CGRP antibody serum (1:1,000) and following CGRP receptor desensitization. However, the autoregulatory mechanics were neither affected by treatment wi th spantide (1 ${\mu}$M), substance P antagonist, nor by substance P receptor desensitization. Suffusion wi th mock cerebrospinal fluid containing CGRP and cromakalim caused a vasodilatation in a concentration-dependent manner, respectively and their effects were antagonized by glibenclamide. Substance P produced a vasodilatation, which was, however, little affected by glibenclamide. These observations indicate that the CGRP released from the perivascular sensory fibers in response to a hypotension is implicated in the modulation of the autoregulation of cerebral blood flow.

• Biomolecules & Therapeutics
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• v.22 no.6
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• pp.525-531
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• 2014

In the present study, we investigated whether apigenin significantly affects tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$)-induced production and gene expression of MUC5AC mucin in airway epithelial cells. Confluent NCI-H292 cells were pretreated with apigenin for 30 min and then stimulated with TNF-${\alpha}$ for 24 h or the indicated periods. The MUC5AC mucin gene expression and mucin protein production were measured by reverse transcription - polymerase chain reaction (RT-PCR) and enzyme-linked immunosorbent assay (ELISA), respectively. Apigenin significantly inhibited MUC5AC mucin production and down-regulated MUC5AC gene expression induced by TNF-${\alpha}$ in NCI-H292 cells. To elucidate the action mechanism of apigenin, effect of apigenin on TNF-${\alpha}$-induced nuclear factor kappa B (NF-${\kappa}B$) signaling pathway was also investigated by western blot analysis. Apigenin inhibited NF-${\kappa}B$ activation induced by TNF-${\alpha}$. Inhibition of inhibitory kappa B kinase (IKK) by apigenin led to the suppression of inhibitory kappa B alpha ($I{\kappa}B{\alpha}$) phosphorylation and degradation, p65 nuclear translocation. This, in turn, led to the down-regulation of MUC5AC protein production in NCI-H292 cells. Apigenin also has an influence on upstream signaling of IKK because it inhibited the expression of adaptor protein, receptor interacting protein 1 (RIP1). These results suggest that apigenin can regulate the production and gene expression of mucin through regulating NF-${\kappa}B$ signaling pathway in airway epithelial cells.

• Toxicological Research
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• v.29 no.3
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• pp.217-219
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• 2013

Hypertension is a serious health problem due to high frequency and concomitant other diseases including cardiovascular and renal dysfunction. Olmesartan cilexetil is a new antihypertensive drug associated with angiotensin II receptor antagonist. This study was conducted to evaluate the mutagenicity of olmesartan cilexetil by bacterial reverse mutation test using Salmonella typhimurium (TA100, TA1535, TA98, and TA1537) and Escherichia coli (WP2 uvrA). At the concentrations of 0, 62, 185, 556, 1667, and 5000 ${\mu}g$/plate, olmesartan cilexetil was negative in both Salmonella typhimurium and Escherichia coli regardless of presence or absence of metabolic activation system (S9 mix). These results demonstrate that olmesartan cilexetil does not induce bacterial reverse mutation.

• Archives of Pharmacal Research
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• v.29 no.6
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• pp.431-458
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• 2006

As we approach the completion of the first 25 years of the human immunodeficiency virus(HIV) epidemic, there have been dramatic improvements in the care of patients with HIV infection. These have prolonged life and decreased morbidity. There are twenty currently available antiretrovirals approved in the United States for the treatment of this infection. The medications, including their pharmacokinetic properties, side effects, and dosing are reviewed. In addition, the current approach to the use of these medicines is discussed. We have included a section addressing common comorbid conditions including hepatitis B and C along with tuberculosis.

• Biomolecules & Therapeutics
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• v.8 no.3
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• pp.248-254
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• 2000

(R)-JG-381, a R form of alkylglycidic acid derivative, was examined for mutagenicity in the reverse mutation test on bacteria, chromosomal aberration test on cultured mammalian cells and micronucleus test in mice. In the reverse mutation test on bacteria using Salmonella typhimurium strain TA98, TA100, TA102, TA1535, TA1537 with or without a metabolic activation system (S9 mix), (R)-JG-381 did not affect the revertant colonies but significantly increased revertant colonies in one test strain, TA98, compared with the vehicle control. In the chromosomal aberration (CA) test using cultured Chinese Hamster Lung fibroblast(CHL) cells, the number of aberrant cells was clot increased in the presence or absence of 59 mix at concentration of the (R)-JG-381 0.025 $\mu$l/m1 to 0.1 $\mu$l/m1, compared with vehicle control. In the micronucleus (MN) test, micronucleated polychromatic erythrocytes in the (R)-JG-381-treated mice were not different from those of the vehicle-treated mice.

• Biomolecules & Therapeutics
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• v.3 no.3
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• pp.210-216
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• 1995

Partially purified water-soluble extract mixture from Ricini and Coptidis (named as RIC) showed to be a potent inhibitor of human immunodeficiency virus-1 (HIV-1) replication. RIC was evaluated for in vitro anti-HIV activity using SupTl and H9 cells infected by a recombinant virus (pSVCAT) containing chloramphenicol acetyltransferase (CAT) gene substituted for nef gene in the HIV-1 genome. RIC inhibited syncytiaformation of SupTl cells with a half maximal effective concentration, $IC_{50}$/, of 2.5 $\mu\textrm{g}$/mι and showed marked inhibition of CAT activity in the infected H9 cells and also suppressed reverse transcriptase (RT) activity in the supernatant of the infected H9 culture. However, RIC did not inhibit the activity of reverse transcriptase directly when it was mixed with the enzyme or with viral particles. Berberine, one of components of RIC, also showed similar anti-HIV activity as RIC did. The data suggest that there are active ingredients which mediate anti-HIV activity in RIC.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1994.04a
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• pp.262-262
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• 1994

Ras oncogene의 산물로서 대부분의 암조직이나 transformed human cell에서 거의 공통적으로 발견되는 p21 단백질은 C-terminal processing에 의해 먼저 C-terminal cysyeine에 palmition 된 후 carboxylmethylation 된다. Palmitation은 transforming activity의 요건인 세포막에 대한 친화력을 유지시키기 위한것으로 추측되며, cysteine residue의 carboxylmethylation의 의미는 아직 확실히 밝혀지고 있지 않으나 세포막에 대한 친화력을 증가 시키는 것으로 추측되고있다. 본 연구에서는 S-Farnesylcysteine Methyltransferase의 기질로서 N-acetyl-S-trans, trans-farnesyl-L-cysteine(AFC)을 합성하였으며, 본 실험실에서 계속 연구하여 온 돼지 간장으로 부터 정제한 천연 단백성 Methylation Inhibitor의 S-Farnesylcysteine Methyltransferase 활성에 대한 억제효과를 검색하였다. 천연 단백성 Methylation Inhibitor는 돼지 간조직의 soluble fraction을 열처리하여 Sephadex G-25 column chromatngraphy한 후 reverse phase HPLC로 정제하였다. 본 inhibitor는 약 10개의 아미노산으로 구성된 peptide성 천연물질로 분자량은 1,400 Da 으로서 합성한 AFC를 기질로 하였을 때, 흰쥐 뇌 조직내 S-Farnesylcysteine methyltransferase에 대한 $IC_{50}$/은 0,82 $\times$ $10^{-6}$ M이었으며 또한 human cancer cell line의 S-Farnesylcysteine Methyltransferase에 대해서도 현저한 저해효과를 나타내었다.

• The Korean Journal of Physiology and Pharmacology
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• v.6 no.2
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• pp.121-125
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• 2002

The pathophysiological implications of aldosterone and adrenomedullin in the cardiac ventricular hypertrophy were examined. Male Sprague-Dawley rats were treated with deoxycorticosterone acetate (DOCA)-salt and monocrotaline (MCT) to selectively elicit left and right ventricular (LV, RV) hypertrophy, respectively. The mRNA expression of aldosterone synthase and adrenomedullin in LV and RV was determined by reverse transcription-polymerase chain reaction. The expression of aldosterone synthase and adrenomedullin was increased in LV, while not altered significantly in RV of DOCA-salt-treated rats. On the contrary, the expression was not significantly altered in LV, but increased in RV of MCT-treated rats. The enhanced expression of aldosterone synthase may be causally related with the development of ventricular hypertrophy, and the increased expression of adrenomedullin may act as a counter-regulatory mechanism.

• Proceedings of the Korean Society of Applied Pharmacology
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• 2003.11a
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• pp.105-105
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• 2003

A rapid and reproducible high performance liquid chromatographic assay of prazosin in human plasma was developed. After addition of internal standard (IS, terazosin hydrochloride) and alkalization of the plasma, the drug and IS were extracted into t-butylmethylether. The organic phase was back-extracted into 0.05% phosphoric acid and 50 ${\mu}\ell$ of the acid solution was injected into a reverse-phase C18 column with a mobile phase consisting of water : acetonitrile : triethylamine = 75 : 25 : 0.1 (pH 5.0). The samples were detected utilizing a fluorescence detector. A