• 한국환경과학회지
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• 제20권10호
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• pp.1221-1232
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• 2011

We investigated the toxic effects of difenoconazole on the development in the African clawed frog, Xenopus laevis. To test the toxic effects, frog embryo teratogenesis assays using Xenopus were performed. Embryos were exposed to various concentrations of difenoconazole (0-30 ${\mu}M$). $LC_{100}$ for difenoconazole was 30 ${\mu}M$, and the $LC_{50}$ determined by probit analysis was 27.19 ${\mu}M$. Exposure to difenoconazole concentrations ${\geq}$5 ${\mu}M$ resulted in 10 different types of severe external malformation. Histological examinations revealed dysplasia of the eye, heart, liver, somatic muscle, and swelling of the pronephric ducts. The tissue-specific toxic effects were investigated with an animal cap assay. Blood cells were normally induced at a high frequency by mSCF and activin A. However, the induction of blood cells was strongly inhibited by the addition of difenoconazole. Electron micrographs of tested embryos showed the degeneration of somatic muscle and the shrinkage of microvilli on pronephric duct. The gene expression of cultivated animal cap explants was investigated by reverse transcriptase-polymerase chain reaction (RT-PCR). It revealed that the expression of the blood-specific marker(${\beta}$-globin II) and muscle-specific marker (XMA) were more strongly inhibited than the neural-specific marker(XEn2) by the addition of difenoconazole.

• Current Research on Agriculture and Life Sciences
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• 제7권
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• pp.33-40
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• 1989

Imidazole계(系) 농약(農藥)인 prochloraz와 triazole계(系)인 triadimefon의 사과나무 부란병균(腐爛病菌)(Valsa ceratosperma)에 대한 항균력(抗菌力) 및 지방산(脂肪酸)의 조성변화(組成變化)에 미치는 영향(影響)을 조사(調査)한 결과(結果)는 다음과 같다. 균(菌)이 생육(生育)하고 있는 PS액체배지(液體培地)에 두 약제(藥劑)를 각각(各各) 처리(處理)하였을 때의 $I_{50}$값은 prochloraz의 경우는 1~5ppm이었고 triadimelon은 5~10ppm이었으며 prochloraz의 저해능(沮害能)이 다소 높았다. 균사(菌絲)의 현미경(顯微鏡) 관찰결과(觀察結果) 약제(藥劑) 처리구(處理區)에서는 모두 균사(菌絲)의 이상생육현상(異常生育現象)이 관찰(觀察)되었다. 균체(菌體)에 약제(藥劑)를 처리(處理)함으로 인해서 지질(脂質)의 변화(變化)를 조사(調査)한 결과(結果) 균체중(菌體中)의 총지질(總脂質) 및 지방산(脂肪酸)의 함량변화(含量變化)는 없는 것으로 나타났다.

• Journal of Chest Surgery
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• 제46권1호
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• pp.14-21
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• 2013

Background: Reactive oxygen species (ROS) are known to be related to cardiovascular diseases. Many studies have demonstrated that angiotensin-converting enzyme inhibitors have beneficial effects against ROS. We investigated the antioxidant effect of captopril and enalapril in nitric oxide mediated vascular endothelium-dependent relaxations. Materials and Methods: Isolated rabbit abdominal aorta ring segments were exposed to ROS by electrolysis of the organ bath medium (Krebs-Henseleit solution) after pretreatment with various concentrations (range, $10^{-5}$ to $3{\times}10^{-4}$ M) of captopril and enalapril. Before and after electrolysis, the endothelial function was measured by preconstricting the vessels with norepinephrine ($10^{-6}$ M) followed by the cumulative addition of acetylcholine (range, $3{\times}10^{-8}$ to $10^{-6}$ M). The relevance of the superoxide anion and hydrogen peroxide scavenging effect of captopril and enalapril was investigated using additional pretreatments of diethyldithiocarbamate (DETCA, 0.5 mM), an inhibitor of Cu/Zn superoxide dismutase, and 3-amino-1,2,4-triazole (3AT, 50 mM), an inhibitor of catalase. Results: Both captopril and enalapril preserved vascular endothelium-dependent relaxation after exposure to ROS in a dose-dependent manner (p<0.0001). Pretreatment with DETCA attenuated the antioxidant effect of captopril and enalapril (p<0.0001), but pretreatment with 3AT did not have an effect. Conclusion: Both captopril and enalapril protect endothelium against ROS in a dose-dependent fashion in isolated rabbit abdominal aortas. This protective effect is related to superoxide anion scavenging.

• 한국대기환경학회지
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• 제8권1호
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• pp.13-19
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• 1992

This study was conducted to determine the efficacy of using uniconazole,[(E)-1-(4-chlorophenyl)-4,4-dimethyl-2-(1,2,4-triazole-1-yl)-1-penten-3-ol)] as a phytoprotectant against $SO_2$ injury in snap been (Phaseolus vulgaris L. 'Strike'). Thirteen days prior to $SO_2$ fumigation, plants were given a 100 ml soil drench of uniconazole solution at concentrations of 0.02, 0.10, 0.25 and 0.50 mg/pot. All four uniconazole concentrations were significantly effective in providing protection against $SO_2$ exposure(3 h at 1.5 ppm), but uniconazole treatment above 0.02 mg/pot severely reduced stem elongation, leaf enlargement, flowering date and pod number and weight. Uniconazole treatment had little or no effect on stomatal conductance but reduced transpiration rate on a whole plant basis by nearly 40%. This may reflect an alteration in canopy structure by reducing stem elongation and leaf enlargement. Although uniconazole did not increase the activities of superoxide dismutase(SOD) and peroxidase(POD) in non-$SO_2$-fumigated plants, it significantly increased those enzyme activities in $SO_2$-fumigated plants. Chlorophyll concentration on the basis of unit area was increased 50-60% by uniconazole. However, the difference was not detected on the basis of dry weight. $SO_2$ increased variable chlorophyll fluorescence (Fv) 48% after 1.5 h of exposure in non-uniconazole treated plants but decreased Fv in the plants after 3 h of exposure. By appliing uniconazole, it was possible to maintain high Fv values in the latter group of plants. These results suggest that the phytoprotective effects of uniconazole are related to its growth-retarding properties as an anti-gibberellin as well as the increase of activites of free radical scavengers such as SOD and POD.

• 농약과학회지
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• 제2권2호
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• pp.108-112
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• 1998

Hexaconazole의 처리가 수박의 생육 및 박의 ethylene 발생에 미치는 영향을 검토한 결과를 하면 다음과 같다. 약제처리 방법에 따른 수박 생장의 억제효과는 경엽처리가 현저하게 효과적인데 반하여 토양관주 처리에서는 효과가 없거나 미미하였다. Hexaconazole 경엽처리시 수박생장은 약제처리 7일후에는 농도가 높으면 높을수록 신장, 마디수가 억제된 반면 약제처리 42일후에는 무처리와 차이가 없었다. Hexaconazole 처리시 수박의 암꽃 착화위치는 착과부위인 제 2번 암꽃까지의 길이생장 및 마디수에는 아무런 영향이 없었고, 측지길이에 미치는 영향은 제 2, 제 3마디에서 현저하게 억제되었는데 이는 처리시기와 밀접한 관련이 있을 것으로 판단된다. Hexaconazole 처리시 박의 ethylene 발생량은 처리농도가 높을수록 ethylene 발생량이 증가하는 경향을 보였으며 약제처리 5일까지는 계속 증가하다가 이후 감소하였다.

• 대한환경공학회지
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• 제27권6호
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• pp.606-613
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• 2005

본 연구에서는 실내공기 중 포름알데히드를 측정하기 위해 세 가지 다른 반응의 흡광광도법(비색분석)을 응용한 뱃지형 확산측정기를 평가하였다. 흡수여지의 세척방법을 비교한 결과 사용된 세척용액의 종류에 관계없이 세척하지 않은 경우 보다 양호한 세척효과가 나타났다. 각 측정방법에서 사용될 흡수액의 농도는 시료채취율을 기준으로 정하였다. 평가된 공시험 값은 측정방법별로 15% 이내의 편차를 가진 것으로 나타나 대체적으로 안정적인 것으로 나타났다. 확산측정기의 재현성은 MBTH법이 상대표준편차 10% 이내로 가장 양호하며, 채취된 포름알데히드 양과 시간가중평균농도와의 상관관계는 세 가지 측정방법 모두 양호한 것으로 나타났다. 검출한계 및 정량한계는 시료채취율이 가장 좋은 MBTH법이 다른 측정방법과 비교하여 가장 낮게 나타나 시료채취율이 가장 크고 정량한계가 낮은 측정방법일수록 포름알데히드 측정에 요구되는 측정시간이 감소되는 것으로 나타났다.

• 한국환경과학회지
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• 제21권12호
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• pp.1435-1447
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• 2012

The present study was conducted to determine the effect of hexaconazole (HEX), a triazole fungicide, on the growth, yield, photosynthetic response and antioxidant potential in cucumber (Cucumis sativus L.) plants subjected to UV-B stress. UV-B radiation and HEX were applied separately or in combination to cucumber seedlings. The growth parameters were significantly reduced under UV-B treatment, however, this growth inhibition was less in HEX treated plants. HEX caused noticeable changes in plant morphology such as reduced shoot length and leaf area, and increased leaf thickness. HEX was quite persistent in inhibiting shoot growth by causing a reduction in shoot fresh and dry weight. HEX noticeably recovered the UV-B induced inhibition of biomass production. Significant accumutation in anthocyanin and flavonoid pigments in the leaves occurred as a result of HEX or UV-B treatments. HEX permitted the survival of more green leaf tissue preventing chlorophyll content reduction and higher quantum yield for photosystemII under UV-B exposure. HEX treatment induced a transient rise in ABA levels in the leaves, and combined application of HEX and UV-B showed a significant enhancement of ABA content which activates $H_2O_2$ generation. UV-B exposure induced accumulation of $H_2O_2$ in the leaves, while HEX prevented UV-B induced increase in $H_2O_2$, indicating that HEX serves as an antioxidant agent able to scavenge $H_2O$ to protect cells from oxidative damage. An increase in the ascorbic acid was observed in the HEX treated cucumber leaves affecting many enzyme activities by removing $H_2O_2$ during photosynthetic processes. The activities of antioxidant enzymes including catalase(CAT), ascorbate peroxidase(APX), superoxide dismutase(SOD) and peroxidase(POD) in the leaves in the presence of HEX under UV-B stress were higher than those under UV-B stress alone. These findings suggest that HEX may participate in the enhanced tolerance to oxidative stress. From these results it can be concluded that HEX moderately ameliolate the effect of UV-B stress in cucumber by improving the components of antioxidant defense system.

• 한국임상약학회지
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• 제28권3호
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• pp.181-187
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• 2018

Background: Posaconazole is a broad-spectrum triazole antifungal agent and the most recommended prophylactic antifungal agent for patients with acute myeloid leukemia (AML) undergoing induction chemotherapy. In this study, we evaluated the status and effectiveness of posaconazole as a prophylactic antifungal agent in pediatric patients receiving induction chemotherapy for AML. Methods: We retrospectively reviewed the electronic medical records of 36 pediatric patients with AML (between January 2013 and September 2017) at the Yonsei University Health System. Invasive fungal disease (IFD) was assessed as the primary endpoint of prophylactic antifungal effect. The secondary endpoints were incidence of fever, persistent fever despite the use of broad-spectrum antibiotics for 72 h, alteration of antifungal agent, intensive care unit admission, and death within 100 days. Results: Among the 36 patients, 18 patients used posaconazole, 12 were treated with suspension formula, and 6 of them were treated with tablets. Eighteen patients did not use antifungal agents prophylactically. The mean number of days of posaconazole administration was $26.8{\pm}16days$. IFD occurred in 2/18 (11.1%) patients in the no prophylaxis group and in 1/18 (5.6%) patients in the posaconazole group (p=0.49). Conclusion: Posaconazole is expected to be useful for the prevention of IFD in pediatric patients with AML undergoing induction chemotherapy. Prospective studies of the effectiveness of posaconazole prophylaxis should be conducted in more pediatric patients in the future.

• Current Research on Agriculture and Life Sciences
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• 제31권4호
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• pp.272-279
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• 2013

사과 중 triazole계 살균제 flusilazole 및 myclobutanil의 생물학적 반감기와 출하전 잔류허용기준을 산출하기 위해 안전사용기준에 근거한 기준량과 3배량의 약제를 살포하고 그 잔류량을 조사하였다. 시험기간 중 두 농약의 잔류량은 각각의 MRL 이하로 나타났으며, 사과 중 생물학적 반감기는 flusilazole의 경우 기준량 처리구에서 6.7일, 3배량 처리구에서 6.2일로 나타났다. 반면에 myclobutanil의 반감기는 기준량 처리구에서 13.3일, 3배량 처리구에서 24.8일로 나타나 flusilazole보다 더 긴 반감기를 가지는 것으로 조사되었다. First order kinetics에 근거한 감소지수식을 이용하여 산출된 각 농약의 감소상수는 flusilazole에 대하여 0.0513, myclobutanil에 대하여 0.0244이었으며, 산출된 감소상수들을 이용하여 출하 전 잔류허용기준(PHRL)을 계산한 결과, 안전사용기준을 준수한 농약살포를 가정하였을 때 flusilazole은 수확 일주일 전 0.43 mg/kg, myclobutanil은 같은 시기 0.59 mg/kg 이하로 잔류하면 수확 시 잔류농도가 MRL 이하로 잔류할 것으로 예측된다.

• Biomolecules & Therapeutics
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• 제26권5호
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• pp.494-502
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• 2018

Breast cancer is currently the most prevalent cancer in women, and its incidence increases every year. Azole antifungal drugs were recently found to have antitumor efficacy in several cancer types. They contain an imidazole (clotrimazole and ketoconazole) or a triazole (fluconazole and itraconazole) ring. Using human breast adenocarcinoma cells (MCF-7 and MDA-MB-231), we evaluated the effects of azole drugs on cell proliferation, apoptosis, cell cycle, migration, and invasion, and investigated the underlying mechanisms. Clotrimazole and ketoconazole inhibited the proliferation of both cell lines while fluconazole and itraconazole did not. In addition, clotrimazole and ketoconazole inhibited the motility of MDA-MB-231 cells and induced $G_1$-phase arrest in MCF-7 and MDA-MB-231 cells, as determined by cell cycle analysis and immunoblot data. Moreover, Transwell invasion and gelatin zymography assays revealed that clotrimazole and ketoconazole suppressed invasiveness through the inhibition of matrix metalloproteinase 9 in MDA-MB-231 cells, although no significant changes in invasiveness were observed in MCF-7 cells. There were no significant changes in any of the observed parameters with fluconazole or itraconazole treatment in either breast cancer cell line. Taken together, imidazole antifungal drugs showed strong antitumor activity in breast cancer cells through induction of apoptosis and $G_1$ arrest in both MCF-7 and MDA-MB-231 cells and suppression of invasiveness via matrix metalloproteinase 9 inhibition in MDA-MB-231 cells. Imidazole drugs have well-established pharmacokinetic profiles and known toxicity, which can make these generic drugs strong candidates for repositioning as antitumor therapies.