• Current Research on Agriculture and Life Sciences
• /
• v.7
• /
• pp.33-40
• /
• 1989

In order to elucidate the antifungal activity of prochloraz(imidazole) and triadimefon(triazole), the mycelia of the Valsa ceratosperma were treated with the compounds in vitro. Prochloraz applied to the target pathogen inhibited mycelial growth more than triadimefon. The concentration for the 50% inhibition of mycelial growth ($I_{50}$) was 1-5 ppm in treatment of prochloraz and 5-10 ppm in treatment of triadimefon. The mycelia of Valsa ceratosperma treated with low concentration of prochloraz and triadimefon were morphologically abnormal as observed with an optical microscope. Content of total lipid and fatty acids were not changed by the treatments of prochloraz and triadimefon, respectively, in liquid medium.

• Journal of Chest Surgery
• /
• v.46 no.1
• /
• pp.14-21
• /
• 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.

• Journal of Korean Society for Atmospheric Environment
• /
• v.8 no.1
• /
• pp.13-19
• /
• 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.

• The Korean Journal of Pesticide Science
• /
• v.2 no.2
• /
• pp.108-112
• /
• 1998

This studies were conducted to investigate the effects of hexaconazole on growth of watermelon(Citrullus lanatus Schrad) and ethylene evolution from gourd(Lagenaria siceraria Standl). While foliar application of hexaconazole exhibited inhibition effect, little or no inhibition was found in the plants treated with soil drench application. The plant height and number of internode in watermelon were significantly inhibited at 7 days after treatment(DAT), but no significant difference was found at 42 DAT. No significant difference was found in site of female flower setting when treated with hexaconazole. The length of branch was significantly inhibited at the 2nd or the 3rd internode. It was suggested that the inhibition of stem elongation was related with application timing of the chemical. Hexaconazole increased ethylene evolution more effectively at earlier stage of gourd, but after 5 DAT ethylene evolution was decreased.

• Journal of Korean Society of Environmental Engineers
• /
• v.27 no.6
• /
• pp.606-613
• /
• 2005

The badge-type diffusive sampler for the measurement of formaldehyde in indoor air using three types of colorimetric methods such as chromotrophic acid(CTA), 3-methyl-2-benzothiazolinone hydrazone(MBTH), and 4-amino-3-hydrazino-5-mercapto-1,2,4-triazole(AHMT) method. The washing of the collection filter with several cleaning solution was effected with satisfactory results, regardless of the types of cleaning solutions. The concentrations of absorbance solution in each colorimetric method were experimentally determined by considering the sampling rates. The variation blank values in each colorimetric method was below 15%. As compared with CTA and AHMT methods, the reproducibility of MBTH method was excellent and was below 10% relative standard deviation. The collected formaldehyde mass and time-weighted concentration had a good correlation (correlation coefficient > 0.93). The limit of detection and limit of quantitation, and minimum sampling time were closely correlated to the sampling rates for the measurement of formaldehyde in each method.

• Journal of Environmental Science International
• /
• v.21 no.12
• /
• pp.1435-1447
• /
• 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.

• Korean Journal of Clinical Pharmacy
• /
• v.28 no.3
• /
• pp.181-187
• /
• 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
• /
• v.31 no.4
• /
• pp.272-279
• /
• 2013

The dissipation patters of the triazole fungicides flusilazole and myclobutanil in apples were investigated to establish the biological half-lives and pre-harvest residue limits (PHRLs). The residual amounts of the fungicides sprayed with single or triple doses were below the maximum residue limits (MRL) for apples established by Ministry of Food and Drug Safety. The dissipation constants of the fungicides in the apples were 0.0513 for flusilazole and 0.0244 for myclobutanil meaning their biological half-lives were calculated as 6.2-6.7 days for flusilazole and 13.3-24.8 days for myclobutanil. The PHRLs calculated using the dissipation constants indicated that the residual amounts of flusilazole and myclobutanil in the apples at the harvesting date would be below the MRLs if their residual amounts were 0.43 and 0.59 mg/kg, respectively, at 7 days prior to harvesting the apples.

• Biomolecules & Therapeutics
• /
• v.26 no.5
• /
• pp.494-502
• /
• 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.

• Applied Chemistry for Engineering
• /
• v.17 no.6
• /
• pp.633-637
• /
• 2006

In this study, the efficient large-scale synthetic route for itraconazole, triazole antifungal agent, was developed. The original synthetic route for medicinal chemistry reported by Janssen Pharmaceutica was linear (14 linear steps) starting from 2,4-dichloroacetophenone with the total yield of 1.4%, and potential hazardous materials such as methanesulfonyl chloride ($CH_{3}SO_{2}Cl$), hydrogen gas, and sodium hydride (NaH) were used. Furthermore, the expensive 1-acetyl-4-(4-hydroxyphenyl)piperazine and palladium were used in this medicinal chemistry route, thus the manufacturing cost would be practically high. In order to improve the commercial route, we developed the process of 12 step convergent synthesis combining two intermediates which are roughly halves of itraconazole with the total yield of 12.0%, and hazardous materials and expensive reagents were excluded in this process, thus the manufacturing cost could be cut down to a great extent.