• Environmental Analysis Health and Toxicology
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• 제13권1_2호
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• pp.1-9
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• 1998

The ROS-producing potency of chromium compounds of several oxidation states were determined in the H4 cells. $K_2Cr_2O_7$ as Cr (VI), synthetic Cr (V) compounds and Cr (III) as TPP produced high level of ROS. However, ROS values of Cr-picolinate as Cr (III), CrCl$_2$, CrCI$_2$, were almost equal to the control. The effects of physiological antioxidants compounds which react with free radicals were examined for their effects on chromate-induced production of reactive oxygen species (ROS) in A549 cells after the addition of $K_2Cr_2O_7$. The compounds used were vitamin C (ascorbate), vitamin E ($\alpha$-tocopherol), superoxide dismutase (SOD) and catalase. The preincubation of ascorbate (200uM) with A549 cells for 20hr resulted in a significant reduction of hexavalent chromate(100uM) induced ROS. However, there is no effects of preincubation of the cells with vitamin E succinate (10 and 20uM, 20hr) on the ROS production. Also, the effects of Cr (VI) on the cell cycle of A549 cells was measured by adding the DNA intercalating agent, propidium iodide. S phase of the cell cycle was increased by the chromium (VI) compounds up to 20uM indicating toxicity or possible mitogenic action of the cell. The shoulder in Go/G1 phase at 20uM Cr (VI) with 24 hr treatment indicates apoptosis.

• 약학회지
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• 제49권1호
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• pp.68-73
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• 2005

Epi-xanthatin analogs containing hydrophilic substituents such as carboxylic acid, alcohol, morpholine, amino acid, and glucose derivatives were synthesized and their in vitro cytotoxicity and in vivo antitumor activity were evaluated. The target compounds were generally cytotoxic against tumor cell lines of human origin with $ED_{50}$ values of $0.1{\sim}30{\mu}g/ml$, except the highly hydrophilic analog 6 containing aspartic acid. Contrary to the potent cytotoxicity weakly hydrophilic analogs 2 and 8 were not active in vivo, or even toxic to the test animals. As a result, hydrophilic analog of epi-xanthatin did not show in vitro cytotoxicity and hydrophobic analogs did not show in vivo antitumor activity, thus it is presumed that amphiphilic analogs or those with medium hydrophilicity would exhibit the antitumor potency in vivo.

• 대한본초학회지
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• 제39권4호
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• pp.11-17
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• 2024

Objective : The purpose of this dissertation is to make a list of the Rhodophyta growing naturally in the Korean coastal waters, and to carry out a survey on the current distribution status to investigate the Bangiaceae which can be used as medicinal herbs. Methods : References and research papers about herbology published at home and abroad were examined. Results : A list was made about Bangiaceae plant which were cultivated or grew naturally in Korea, after investigated the data on domestic and foreign Bangiaceae plants. Out of those lists, serviceable plants were selected , their distributions were analysed. 1. A total of 2 genera and 18 species of Bangiaceae were found in the Korean coastal waters among which 1 genera and 4 species(approximately 22%) were medicinal plants. 2. Out of the 18 species of Bangiaceae 16 species belonged to Porphyra, and out of the 4 species of medicinal plants 4 species belonged to Porphyra. 3. Among the medicinal parts 4 species belonged to algae species had cold property, and had salty and sweet flavors. 4. 4 species had the efficacy of Lung, Spleen and bladder meridian had the potency of soften hardness, which helps to remove hard clots generated, cure phlegm in human body. 5. No toxic drugs were detected. Conclusion : There were totaled to 18 genera and 2 species in Bangiaceae in Korea and among them medicinal plants are 1 genera, 4 species, some 22% in total.

• 농약과학회지
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• 제7권1호
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• pp.45-50
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• 2003

Procarbamate계 살충제인 benfuracarb의 산화효소계에 의한 활성화 과정과 이 과정을 통하여 생성되는 독성 대사물의 전환 정도를 확인하고자 수행되었다. Acetylcholinesterase(AChE) 에 대한 henfuracarb의 이 분자속도저해상수$(k_i)$가 $1.1\times10^3\;M^{-1}\;min^{-1}$로 매우 낮은 저해력을 보인 바, 이 약제가 체내에서 독성을 발현하기 위해서는 활성화 과정이 필수적임을 가정할 수 있었다. Benfuracarb의 활성화 과정에 관여하는 cytochrome $P_{450}$의 역할을 in vitro 에서 관찰하기 위하여 AChE/MFO coupling system을 사용하였다. AChE/MFO coupling system에서 AChE에 대한 저해력은 NADPH가 처리된 oxidase system이 NADPH 가 결핍된 대조구에 비하여 약 10배정도 증가하였으며, oxidase+PBO system 에서는 약간의 저해력 감소 경향이 관찰되었다. 생쥐에 henfuracarb을 처리한 후 brain AChE 활성을 조사해 본 결과 henfuracarb만 처리한 benfuracarb 처리구에서의 $I_{50}$은 22.7mg $kg^{-1}$이었으며, PBO를 전처리 한 후 henfuracarb을 처리한 benfuracarb+PBO 처리구에서는 $I_{50}$이 >100mg $kg^{-1}$으로 저해정도가 급격히 경감되어 benfuracarb의 활성화 과정에 cytochrome $P_{450}$이 관련되어 있음을 확인할 수 있었다. Microsomal oxidase system 을 이용하여 henfuracarb이 독성 대사물인 carbofuran으로 전환되는 정도를 관찰하였다. Oxidase system 에서는 처리된 benfuracarb의 58.0%가 carbofuran으로 전환되었지만, oxidase+PBO system에서 1.7%만 생성되어 benfuracarb의 활성화과정에 산화효소인 cytochrome $P_{450}$의 역할이 중요함을 확인할 수 있었다. 본 연구를 통하여 benfuracarb의 독성 발현에 관여하는 주된 독성 대사물은 carbofuran이며, 이 활성화 과정 에 cytochrome $P_{450}$이 중요한 역할을 하는 것으로 확인되었다.

• 농약과학회지
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• 제2권2호
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• pp.10-15
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• 1998

Carbofuran 및 N-dimethoxyphosphinothioyl carbofuran (PSC)의 AChE에 대한 이분자 저해 속도상수(bimolecular inhibition rate constant, $k_{i}$)를 관찰하였다. Carbofuran은 $7.7{\times}10^{5}\;M^{-1}{\cdot}min^{-1}$으로 높은 저해효과를 보이고 있는 반면, PSC는 $1.2{\times}10^{3}\;M^{-1}{\cdot}min^{-1}$으로 carbofuran에 비하여 AChE에 대한 저해력이 600배 정도 낮은 저해력을 갖고 있는 것으로 관찰되어 독성발현을 위하여 활성화 과정이 필요한 것으로 확인되었다. AChE/mixed function oxidase(mfo) coupling system을 이용한 microsomal oxidative activation 실험에서 PSC의 AChE에 대한 저해력이 control에 비하여 NADPH가 첨가된 oxidase 처리구에서 800배 더 강하게 나타났으며, cytochrome $P_{450}$의 저해제를 첨가한 oxidase+PBO 처리구에서는 control의 저해 경향과 유사하였다. 또한 생쥐 뇌 AChE에 대한 PSC의 $I_{50}$은 28 mg/kg인 반면 PBO를 전처리하였을 경우 $I_{50}$은 57 mg/kg으로 나타나 cytochrome $P_{450}$ 저해제로 인하여 PSC의 저해력이 2배정도 감소된 것을 관찰할 수 있었고, PSC는 독성발현을 위하여 활성화 과정을 거쳐야 하며, 이 과정에서 cytochrome $P_{450}$ 이 작용함을 확인할 수 있었다. PSC와 MCPBA를 반응시켜 산화 과정을 통하여 생성된 독성대사물을 분석한 결과 반응산물의 약 55%가 carbofuran임을 확인할 수 있었다. 본 연구를 통하여 PSC의 활성화 과정을 통한 독성발현에 cytochrome $P_{450}$이 중요한 역할을 하는 효소임을 확인할 수 있었고, PSC의 산화적 활성화 과정을 통한 주된 독성대사물이 carbofuran임을 확인할 수 있었다.

• Parasites, Hosts and Diseases
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• 제47권3호
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• pp.213-218
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• 2009

Leishmaniasis is a neglected disease and endemic in developing countries. A lack of adequate and definitive chemotherapeutic agents to fight against this infection has led to the investigation of numerous compounds. The aim of this study was to investigate the effect of RT-01, an organotellurane compound presenting biological activities, in 2 experimental systems against Leishmania amazonensis. The in vitro system consisted of promastigotes and amastigotes forms of the parasite, and the in vivo system consisted of L.amazonensis infected BALB/c mice, an extremely susceptible mouse strain. The compound proved to be toxic against promastigotes and amastigotes. The study also showed that treatment with RT-01 produces an effect similar to that treatment with the reference antimonial drug, Glucantime, in L.amazonensis infected mice. The best results were obtained following RT-01 intralesional administration (720 ${\mu}g$/kg/day); mice showed significant delay in the development of cutaneous lesions and decreased numbers of parasites obtained from the lesions. Significant differences in tissue pathology consisted mainly of no expressive accumulation of inflammatory cells and wellpreserved structures in the skin tissue of RT-01-treated mice compared with expressive infiltration of infected cells replacing the skin tissue in lesions of untreated mice. These findings highlight the fact that the apparent potency of organotellurane compounds, together with their relatively simple structure, may represent a new avenue for the development of novel drugs to combat parasitic diseases.

• Toxicological Research
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• 제28권2호
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• pp.113-116
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• 2012

Various kinds of positive effects of green tea extracts had been studied for long time which included anti-inflammation, anti-aging, and cardiometabolic effects. Although topical steroid and non-steroidal calcineurin inhibitors may control clinical symptoms of allergic contact dermatitis, some of patients also present allergic reaction to these topical agents. Therefore, we have tried green tea extracts for managing this skin disorder with expectation of anti-inflammatory effect without potential side effects including skin irritation and toxic responses. The toxicity test of green tea extract also did not show any sign of irritation in the skin throughout the test period. Moderate severity of allergic contact dermatitis presented satisfactory clinical outcome at second week follow-up which was final visit of outpatient. This result mean that green tea extract has a positive effect for managing allergic contact dermatitis but its potency and efficacy seem to be so not strong enough to control moderate severity allergy skin lesion. In this pilot study, we were able to conclude that green tea cell extracts might be applied for potential anti-inflammatory soaking without skin toxicity.

• 한국미생물·생명공학회지
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• 제40권4호
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• pp.409-413
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• 2012

인돌리시딘(indolicidin)은 소의 호중구(bovine neutrophils)로 부터 분리된 13개의 아미노산 잔기로 이루어 지고, 트립토판(tryptophan)을 많이 함유한 항균 펩타이드(antimicrobial peptide)이다. 인돌리시딘은 강력한 항균활성과 더불어 mammalian cells에 대해 독성을 나타낸다. 본 연구에서는 인돌리시딘 보다 서열이 짧으며, 보다 증가된 원핵세포 선택성(박테리아세포에 대해 독성을 나타내지만 mammalian cells에 대해서는 독성을 나타내지 않음을 의미함)을 지닌 새로운 짧은 항균 펩타아드를 개발하기 위해, 몇 종의 인돌리시딘 유사체 펩타이드를 설계하고 합성하였다. 결과적으로, 인돌리시딘 보다 서열이 짧으며(10개의 아미노산 잔기로 이루어짐), 증가된 원핵세포선택성을 지닌 4종의 새로운 펩타이드(SI, SI-PA, SI-WF 및 SI-WL)를 개발하였다. 본 연구를 통하여 가장 높은 원핵세포선택성을 나타내는 인돌리시딘 유사체 펩타이드 SI의 항균활성에는 중앙부위에 위치하는 소수성 및 방향족 아미노산이 중요하며, 2군데의 프로린(proline) 잔기는 중요하지 않다는 것을 알았다. 인돌리시딘과 유사체 펩타이드에 대한 원핵세포 선택성은 SI>SI-PA>SI-WF>SI-WL>ID>SI-WA의 순서 이였다. 따라서, 본 연구에서 설계되고 합성한 4종의 인돌리시딘 유사체 펩타이드(SI, SI-PA, SI-WF 및 SI-WL)는 박테리아 감염의 치료제로서 개발될 수 있을 것이다.

• 동국한의학연구소논문집
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• 제1권
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• pp.209-236
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• 1992

The microculture XTT antiviral assay method is used to quantitate HIV-1 induced cytopathic effects as modulated by test substances. This relatively simple assay facilitated the safe and rapid determination of in vitro antiviral activity of selected chemicals as well as direct cytotoxicity. This experiment also confirmed that this system measures infection and subsequent viral replication in target cells and XTT formazan formations correlated with the accumulation of extracellular virions, as measured by quantitative HIV-1 induced syncytium foramtion. The present results with Glycyrrhizin using this in vitro culture system demonstrated that effective dose, EC50(the concentration at which increases XTT formazan production in infected cultures to 50% of that in untreated, uninfected controls) was 250ml. As comparison, AZT was included in this experiment and demonstrated that EC50 AZT of was 0.05g/ml, approximately 5,000 times more potent than Glycyrrhizin based on EC50 ratio's alone. However, this potency is limited by severe cytotoxicity of AZT, while Glycyrrhizin is approximately 16 times less toxic(IC50 of Glycyrrhizin 800 and AZT 51 g/ml). While AZT's anti-HIV-1 viral activity is mediated by inhibition of reverse transcriptase of the virus, Glycyrrhizin faild to demonstrate any inhibitory activity against reverse transcriptase. Further study is necessary in order to understand the precise mechanisms of Glycyrrhizin action against HIV-1 viruses. Althouth Glycyrrhizin is less effective antiviral agent than AZT, much less toxicity of Glycyrrhizin is desirable in terms of chronic treatment. Combination treatment of AZT and Glycyrrhizin may be therapeutically beneficial. Clinical effectiveness of two drug combination therapy for AIDS patient is unknown at this time. However, this experimental investigation presents the scientific rational basis for such therapeutic approach.

• 한국연초학회지
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• 제19권2호
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• pp.136-144
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• 1997

Cigarette smoking is known to suppress both 1-methy14-phenyl-155,Ltetrahydropy-ridine (MPTP)-induced parkinsonism and idiopathic Parkinson's disease (PD). However, the precise mechanism underlying its protective action against PD is not clearly elucidated yet. In order to find possible clue on the mechanism of protective action of smoking, we investigated the inhibitory effect of cigarette smoke components on rat brain mitochondria1 monoamine oxidase B (MAO-B), responsible enzyme for the activation of MPTP to its toxic metabolitesr and identified the components having an inhibitory potency on this enzyme from cigarette smoke. Total 31 eligible constituents including nicotine were selected from cigarette smoke condensates via solvents partitioning and silica gel chromatographic separation, and inhibitory potencies of 19 components on MAO-B were determined. Hydroquinone and methylcatechol, the phenolic components, showed the strongest inhibitory potencies on MAO-B activity in the components tested. 3,4-Dihydroxybenzylamino, myosmine and indole in basic fracton, eugenol in phenolic fraction, and farnesol in neutral fraction also inhibited the enzyme activity dose-dependently. Among tobacco alkaloids tested only myosmine was effective for the inhibition of this enzyme. These results suggest that the decrease in MAO-B activity by such components derived from cigarette smoke seems to be related to the suppression of MPTP-induced neurotoxicity and to the less incidence of Parkinson's disease in smokers than in nonsmokers.