• Title/Summary/Keyword: in vivo antifungal activity

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Synthesis and antifungal activities of 4-[5-(2-cyclopropylaminopyrimidin-4-yl)-4-arylthiazol-5-yl]piperidine derivatives on Phytophthora capsici (4-[5-(2-cyclopropylaminopyrimidin-4-yl)-4-arylthiazol-5-yl] piperidine 유도체들의 합성과 고추역병균에 대한 살균활성)

  • Nam, Seok-Woo;Lee, Gyung-Rak;Kim, Tae-Joon;Chung, Bong-Jin;Choi, Won-Sik
    • The Korean Journal of Pesticide Science
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    • v.16 no.1
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    • pp.1-10
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    • 2012
  • Fungicidal activities against phytopathogenic fungi of diarylthiazole compound of 4-[5-(2-cyclopropylaminopyrimidin-4-yl)-4-(4-fluorophenyl)thiazol-5-yl]-1-methylpiperidine (I) have been determined to be excellent and compound I was used as the leading compounds in this study. Furthermore, the compound was synthesized by reacting them with five functional groups, 4-fluoro-3-methylphenyl, 4-fluoro-3-chlorophenyl, 4-chloro-2-fluorophenyl, 4-bromo-3-methylphenyl and 2,4-dichlorophenyl groups instead of 4-fluorophenyl group. Also, 2-amino-, 2-(N-ethoxycarbonyl)piperidin-4-yl-, and 2-piperidin-4-yl-thiazole were introduced as the leads instead of 2-N-methylpiperidine-4-yl-thiazol of compound I. VIII-1~VIII-5 and XIII-1~XV-5 compounds were newly synthesized and their structures were confirmed by $^1H$-NMR-spectrum. The fungicidal activities of all the synthesized compounds against Phytophthora capsici were examined using the whole plant method. Among the VIII-1~VIII-5 and XIII-1~XV-5 chemicals, XIV-3 showed the most potent antifungal activity in vivo. While the $EC_{50}$ and $EC_{90}$ values of the commercial fungicide dimethomorph and I were $4.26{\pm}0.02$, $14.72{\pm}0.05$ and $1.01{\pm}0.11$, $6.31{\pm}0.09mM$, those of 4-[5-(2-cyclopropylaminopyrimidin-4-yl)-4-(4-chloro-2-fluorophenyl)thiazol-5-yl]-1-methylpiperidine (XIV-3) was $0.98{\pm}0.21$ and $5.85{\pm}0.05mM$. Therefore, XIV-3 can be considered as a viable candidate for the control of plant diseases caused by P. capsici, and further studies will be conducted on the mode of action XIV-3.

Control of Botrytis cinerea and Postharvest Quality of Cut Roses by Electron Beam Irradiation (전자빔 조사에 따른 잿빛곰팡이병원균 방제효과와 절화 장미의 수확 후 품질)

  • Kwon, Song;Choi, Gyung Ja;Kim, Ki Sun;Kwon, Hye Jin
    • Horticultural Science & Technology
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    • v.32 no.4
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    • pp.507-516
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    • 2014
  • The present study was conducted to determine the effect of electron beam irradiation on control of Botrytis cinerea and postharvest quality of cut roses. Electron beam doses of 0.1, 0.2, 0.4, 0.6, 0.8, 1, 2, 10, and 20 kGy were applied with a 10-MeV linear electron beam accelerator (EB Tech, Korea). Electron beams inhibited spore germination and mycelial growth of B. cinerea with increasing irradiation doses. Conidia of B. cinerea were more tolerant to irradiation than were mycelia: the effective irradiation doses for 50% inhibition ($ED_{50}$) of spore germination and mycelial growth were 2.02 kGy and 0.89 kGy, respectively. In addition, electron beam irradiation was more effective in reducing mycelial growth of B. cinerea at $10^{\circ}C$ than at $20^{\circ}C$. Analysis of in vivo antifungal activity revealed that elevated irradiation doses exhibited increased control efficacy for tomato gray mold. Flower longevity and fresh weight of cut roses decreased when the irradiation dose was increased. In addition, flower bud opening tended to be inhibited in a dose-dependent manner. Although 'Decoration', 'Il se Bronze', 'Queen Bee', and 'Revue' roses tolerated and maintained overall postharvest quality up to 0.4 kGy, 'Vivian' did not, demonstrating that the irradiation sensitivity of cut roses varies according to cultivar.

Antifungal Activity of Crude Extract Compound from Rhus verniciflua Against Anthracnose Fungi (Collectotrichum spp.) of Red-Pepper (고추 탄저병균에 대한 옻나무 추출물의 항진균 효과)

  • Song, Chi-Hyoun;Chung, Jong-Bae;Jeong, Byoung-Ryong;Park, Se-Young;Lee, Yong-Se
    • Korean Journal of Environmental Agriculture
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    • v.31 no.1
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    • pp.60-67
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    • 2012
  • BACKGROUND: Anthracnose disease caused by Collectotrichum spp. is one of the most important worldwide devastating diseases in red pepper plants. Fungicides using plant extracts have several advantages, compared to synthetic chemical fungicides, because they are naturally occurring compounds, are usually safe for agricultural environment and are used for producing highly valuable agricultural products. Efforts for seeking an anti-fungal activities using naturally occurring compounds were mostly conducted from medicinal plant extracts. Sap of Rhus verniciflus was known to have healing effects on several human diseases. Recently, the extracts of Rhus verniciflus were actively tested for anti-cancer, anti-oxidative, and anti-fungal effects. In this study, the extract of Rhus verniciflus was tested for anti-fungal activity against Colletotrichum spp., which cause anthracnose in red-pepper. METHODS AND RESULTS: After neutralizing extracts of Rhus verniciflus (urushiol contents 70%) with autoclave, the crude extracts were used to investigate inhibitory effects for mycelial growth and spore germination of Colletotrichum spp. on PDA media. The mycelial growth and spore germination of Colletotrichum spp. were inhibited 18-39% and over 50% in response to crude extract of R. verniciflus (1.0 mg/mL). After spraying the extracts at the same concentrations above and then artificially inoculating Colletotrichum spp. on blue and red-pepper fruits, in vitro inhibition effects were examined. At 1.0 mg/mL, the crude extract of R. verniciflus showed inhibition activity in anthracnose incidence on blue- and red-pepper as 68.1-75.0%, through a artificial inoculation of Colletotrichum spp. in a laboratory. For in vivo inhibitory effects, the extracts (1.0, 0.1, and 0.01 mg/mL) were treated on red-pepper plants grown in green house 3 times at the interval of 1 week. Then inhibitory effects were determined by counting diseased fruits at 1 week after final treatment. The incidence of anthracnose was inhibited over 60% in the greenhouse by treatment of crude extract of R. verniciflus (1.0 mg/mL). CONCLUSION(s): Extracts of Rhus verniciflus were shown to have inhibitory effects on mycelial growth, spore germination of Colletotrichum spp. in vitro and on occurrence of anthracnose on pepper fruit in green house.

Chitinase of Multifunctional Antagonistic Bacterium Bacillus amyloliquefaciens 7079 against Phy-tophathogenic fungi (식물병원진균을 길항하는 chitinase 생산성 생물방제균 Bacillus amyloliquefaciens 7079의 선발과 chitinase 생산조건)

  • 한옥경
    • Microbiology and Biotechnology Letters
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    • v.29 no.3
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    • pp.142-148
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    • 2001
  • An indigenous antagonistic bacterium Bacillus sp. 7079 was isolated from a local soil sampled at Kyongju area in Korea . The strain has strong antagonistic ability which was originated from multifunctional mechanisms of chitinase and antibiotic and is a powerful antagonistic biocontrol agent against red-pepper rotting fungus Phytophthora capsici and Wilt fungus Fusarium oxysporum. The chitinase might degrade the cell wasll for Fusarium species. The selected Bacilus sp. 7079 was identified as a Bacillus amyloliquefaciens 7079. The maximal production of the chitinase from B, amyloliquefaciens 7079 were obtained in chitin-yeast extract medium containing 0.7%, $K_2$$HPO_4$, $0.2KH_2$$PO_4$, 0.1% ($NH_4$)$_2$$SO_4$, 0.05% sodium cirate, 0.01% $MgSO_4$$7H_2$O, 0.1% yeast extract and 0.1% colloidal chitin after cultivation of 3 days at pH 7.0 and $30^{\circ}C$. The best carbon and nitrogen sources for the production of the chitinase from B amyloliquefaciens 7079 were determined to be 0.1% colloi- dal chitin and 0.15% proteose peptone NO 3 respectively, The antagonistic activity of B amyloliquefaciens 7079 was confirmed using P. capsici by in vivo pot test with red-pepper plant.

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Selection and Mechanisms of Indigenous Antagonistic Microorganisms against Sheath Rot and Dry Rot Disease of Garlic (마늘 잎집썩음병과 마른썩음병을 길항하는 토착길항미생물의 선발 및 기작)

  • Jeong, Hee-Young;Lim, Jong-Hui;Kim, Byung-Keuk;Lee, Jung-Jong;Kim, Sang-Dal
    • Microbiology and Biotechnology Letters
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    • v.38 no.3
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    • pp.295-301
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    • 2010
  • Sheath rot and dry rot disease caused by Pseudomonas marginalis and Fusarium oxysporum were serious problems in garlic farmland. In this study, total of 160 indigenous antagonistic bacteria were isolated from 16 farmlands in Yeongcheon, Korea. Among these, 15 strains were able to inhibited P. marginalis and F. oxysporum. The 16s rDNA genes of the selected 15 strains were amplified and sequenced. The strains has strong antagonistic ability against garlic pathogens was achieved Bacillus subtilis YC82, B. vallismortis YC84, B. amyloliquefaciens YC240. The selected 3 strains tested for investigation of antifungal mechanisms further analyses; 3 strains of these validated for production of siderophore, ${\beta}$-glucanase and chitinase using CAS (chrome azurol S) blue agar, CMC-congo red agar and DNS method. The 3 strains were able to utilized insoluble phosphate as dertermined by vanado-molybdate method. The 3 strains verified for production of auxin and gibberellic acid using Salkowski test and holdbrook test. Also, 3 strains showed stimulation germination, stem growth promoting activity on the in vivo test. The 3 strains were able to effectively suppress P. marginalis and F. oxysporum causing sheath rot and dry rot diseases on the in vivo pot test.

Antifungal activity of pesticides to control dry rot and blue mold during garlic storage (마늘 저장 중 마름썩음병과 푸른곰팡이병 억제를 위한 농약의 살균활성)

  • You, Oh-Jong;Lee, Yong-Hoon;Jin, Yong-Duk;Kim, Jin-Bae;Hwang, Se-Gu;Han, Sang-Hyun;Kim, Jang-Eok
    • The Korean Journal of Pesticide Science
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    • v.11 no.4
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    • pp.331-338
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    • 2007
  • The major fungal diseases which effecting garlic storage are blue mold and dry rot, caused by Penicillium hirsutum and Fusarium oxysporum, respectively. In order to reduce the damage by the pathogenic fungi, here we report the effects of 11 fungicides tested to reduce spoilage during storage of garlics. In the in vitro antimicrobial activity test, the fungicides, diphenylamine, prochloraz and tebuconazole showed 0.3, 2.2, and 1.3 nun inhibition zone to F. oxysporium, and cyprodinil, diphenylamine, fenbuconazole, hexaconazole, penconazole, prochloraz, propiconazole, pyrimethanil and tebuconazole exhibited 0.2, 2.4, 0.8, 0.4, 1.2, 1.5, 1.2, 0.4 and 1.5 mm to P. hirsutum, respectively. To test the in vivo control effect, when the diphenylamine, prochloraz, and tebuconazole were treated by standard concentration, the fungal mycelium of F. oxysporium started to grow 5 days after inoculation, and 80, 63.3 and 83.3% of the inoculated cloves are infected 11 days after inoculation. When the tebuconazole were treated by standard concentration, the P. hirsutum was completely inhibited the growth of the fungi. In case of diphenylamine, penconazole and propiconazole treatment, the P. hirsutum was observed 7 days after inoculation and $20{\sim}23.3%$ of the cloves were infected 11 days after inoculation. When cyprodinil, prochloraz and pyrimethanil were treated, pathogens occurred 5 days after inoculation and $60{\sim}100%$ of the cloves infected 11 days after inoculation. Three fungicides such as diphenylamine, prochloraz and tebuconazole also suppressed remarkably the infection and growth of F. oxysporium and P. hirsutum on garlic when both of the pathogens are inoculated after the garlic cloves were dipped for 10 min in the suspension of each agrochemical. Overall, diphenylamine, prochloraz and tebuconazole showed effective control efficacy on dry rot and blue mold There was significant correlation between in vitro and in vivo assay in diphenylamine and prochloraz to F. oxysporum and cyprodinil, prochloraz and pyrimethanil to P. hirsutum.

Isolation and Selection of Antagonistic Microbes for Biological Control of Zoysiagrass Large Patch Disease (한국잔디 갈색퍼짐병의 생물학적 방제를 위한 길항미생물의 분리 및 선발)

  • Ma, Ki-Yoon;Kwark, Soo Nyeon;Lee, Geung-Joo
    • Horticultural Science & Technology
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    • v.31 no.6
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    • pp.657-665
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    • 2013
  • A large patch disease caused by Rhizoctonia solani AG2-2 (IV) is a serious problem in Korean lawngrass (Zoysia japonica) sites including golf courses and sports fields in Korea. Antagonistic microorganisms against R. solani AG2-2 (IV) were isolated from various forest and crop soil sources in Southern Korea. Among the 61 isolates, I-009, FRIN-001-1, and YPIN-022 strains showing dramatic inhibition of the mycelial growth of R. solani AG2-2 (IV) in the pairing culture were selected as the most potential antagonistic microorganisms for this study. Based on the 16s RNA sequence comparison, I-009 and FRIN-001-1 isolates were identified as Bacillus spp., while YPIN-022 isolate belongs to the genus Pseudomonas. The greater inhibition (clear) zone between two edges of the selected and pathogenic microbes ranged from 11 to 15 mm in three selections, but the others averaged to 7 mm out of 30 mm distance. In another antifungal test using culture filtrate, those three isolates represented a range of 51.7 to 63.5% suppression potential. The selected isolates also inhibited significantly the stem-segment colonization by R. solani AG2-2 (IV) in vivo test by 28.1%, 43.0%, and 23.7% when inoculated with I-009, FRIN-001-1, and YPIN-022, respectively. The highest antagonistic activity for the large patch disease was demonstrated by the isolate FRIN-001-1, which will be useful for developing a bio-pesticide against Rhizoctonia.

Anti-inflammatory Effects of Illicium verum Hook. f. via Suppression of NFκB Pathway (NF-κB 억제를 통한 대회향(大茴香)의 항염증효능)

  • Keum, Soo Yeon;Park, Sang Mi;Jegal, Kyung Hwan;Hwangbo, Min;Cho, Il Je;Park, Chung A;Kim, Sang Chan;Jee, Seon Young
    • Herbal Formula Science
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    • v.24 no.4
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    • pp.243-257
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    • 2016
  • Objectives : Illicium verum Hook. f. has been known to possess antimicrobial, antioxidant, antifungal, anti-inflammatory, insecticidal, analgesic, sedative, convulsive activities, it has been rarely conducted to evaluate the immuno-biological activity. The present study was examined to evaluate the anti-inflammatory effects of the Illicium verum Hook. f. water extracts (IVE) in vivo and in vitro. Methods : Cell viability was measured by MTT assay. The relative levels of NO were measured with Griess reagent. iNOS, COX-2, $NF-{\kappa}B$ and target proteins were detected by immunoblot analysis, and levels of cytokines were analyzed by ELISA kit. Anti-edema effect was determined in the carrageenan (CA)-induced paw edema model in rats. Results : All dosages of IVE used in MTT assay had no significant cytotoxicity. The increases of NO production and iNOS expression were detected in LPS-treated cells compared with control. However, these increases were attenuated by treatment with IVE. Also, IVE reduced the elevated production of $TNF-{\alpha}$, $IL-1{\beta}$ and IL-6 by LPS. IVE inhibited the $p-I{\kappa}B$ and translocation of $NF-{\kappa}B$ to nuclear. Furthermore, IVE significantly inhibited the increases of hind paw swelling, skin thicknesses and inflammatory cell infiltrations induced by CA injection. Therefore, IVE will be favorably inhibited the acute edematous inflammations. Conclusion : These results provide evidences that anti-inflammatory effect of IVE is partly due to the reduction of some inflammatory mediators by suppression of $NF-{\kappa}B$ pathway.

Control effects of new triazoyl quinolines KSI-4315 and KSI-4317 against barley powdery mildew and wheat leaf rust (신규의 triazoyl quinoline 화합물 KSI-4315와 KSI-4317의 보리 흰가루병과 밀 붉은녹병에 대한 방제효과)

  • Choi, Gyung-Ja;Yon, Gyu-Hwan;Kim, Heung-Tae;Jang, Kyoung-Soo;Kim, Jin-Cheol;Lee, Seon-Woo;Pak, Chwang-Siek;Cho, Kwang-Yun
    • The Korean Journal of Pesticide Science
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    • v.7 no.4
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    • pp.302-309
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    • 2003
  • Disease control activities of 230 triazolyl quinoline derivatives were investigated against six plant diseases such as rice blast, rice sheath blight, tomato gray mold, tomato late blight, wheat leaf rust (WLR) and barley powdery mildew (BPM). New triazolyl quinolines, KSI-4315 and KSI-4317 exhibited a great in vivo control activities against WLR and BPM, and then were selected for further tests such as preventive, curative, systemic, and persistence against WLR and BPM. The KSI-4315 and KSI-4317 contained MeS moiety and MsO moiety in carbon 4-position, respectively. They possessed both preventive activity and curative activity against WLR and BPM. KSI-4317 showed the better control activity than KSI-4315 against BPM, while KSI-4315 represented the better antifungal activity against WLR. Good persistence of KSI-4315 and KSI-4317 were also observed against WLR and BPM. Persistence of KSI-4315 was similar to that of KSI-4317 on WLR, but KSI-4317 was superior to KSI-4315 on BPM in its persistence. Systemic disease control of KSI-4315 and KSI-4317 was investigated by examining translaminar activity from leaf-under-surface to leaf-upper-surface, systemic activities by leaf to leaf movement and the effect of drenching treatment. Systemicities of KSI-4315 and KSI-4317 were not observed in wheat, but KSI-4317 showed more predominant systemicity than KSI-4315 in barley. These results suggest that KSI-4317 would potentially control WLR and BPM in the fields.

Induction of Apoptosis and Antitumor Activity by Stichoposide D through the Generation of Ceramide in Human Leukemia Cells (Stichoposide D의 백혈병 세포주에서 세라마이드 생성을 통한 세포 사멸 유도 및 항암 작용)

  • Park, Eun-Seon;Yun, Seung-Hoon;Shin, Sung-Won;Kwak, Jong-Young;Park, Joo-In
    • Journal of Life Science
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    • v.22 no.6
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    • pp.760-771
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    • 2012
  • Marine triterpene glycosides are physiologically active natural compounds isolated from sea cucumbers(holothurians). It was demonstrated that they have a wide range of biological activities, including antifungal, cytotoxic, and antitumor effects. A previous study showed that stichoposide C (STC) isolated from Thelenota anax induces apoptosis through generation of ceramide by activation of acid sphingomyelinase (SMase) and neutral SMase in human leukemia cells. In this study, we investigated whether STD, a structural analog of STC, can induce apoptosis and examined the molecular mechanisms for its activity. It was found that STC and STD induce apoptosis in a dose- and time-dependent manner and lead to the activation of caspase-8, mitochondrial damage, activation of caspase-9, and activation of caspase-3 in K562 and HL-60 cells. STC activates acid SMase and neutral SMase, which results in the generation of ceramide. Specific inhibition of acid SMase or neutral SMase partially blocked STC-induced apoptosis, but not STD-induced apoptosis. In contrast, STD generates ceramide through the activation of ceramide synthase. Specific inhibition of ceramide synthase partially blocked STD-induced apoptosis, but not STC-induced apoptosis. Moreover, STC and STD markedly reduced tumor growth of HL-60 xenograft tumors and increased ceramide generation in vivo. These results indicate that STC and STD can induce apoptosis and have antitumor activity through the different molecular mechanisms, because they have a different sugar residue attached to aglycones. Thus, these results suggest that their actions are affected by a sugar residue attached to aglycones and they can be used as anticancer agents in the treatment of leukemia.