• Title/Summary/Keyword: In vivo antifungal activities

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Effective Antibacterial Action of Tat (47-58) by Increased Uptake into Bacterial Cells in the Presence of Trypsin

  • Jung, Hyun-Jun;Jeong, Kyu-Shik;Lee, Dong-Gun
    • Journal of Microbiology and Biotechnology
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    • v.18 no.5
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    • pp.990-996
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    • 2008
  • In a previous study, we found an antifungal effect on human pathogenic fungi by the cell-penetrating peptide Tat (47-58) derived from HIV-1. Tat (47-58) immediately entered into the fungal nucleus and affected some physiological changes on the intracellular condition. In this study, Tat (47-58) showed a broad spectrum of antibacterial activity against pathogenic bacteria including bacterial clinical isolates. To improve resistance against proteases for use in vivo, we synthesized an analog of Tat (47-58) by substituting the L-amino acid for the D-amino acid. The D-enantiomer of Tat (47-58) also exhibited a broad spectrum of antibacterial activity at almost the same level of L-Tat (47-58) concentration. Unlike L-Tat (47-58), D-Tat (47-58) showed a significant proteolytic resistance against all proteases tested and antimicrobial activities in the presence of trypsin. Moreover, D-Tat (47-58) inhibited MRSA infection in human HeLa cells whereas L-Tat (47-58) partially allowed MRSA infection, and the results were due to the proteolytic resistance of D-Tat (47-58).

Synthesis of Trifluoromethylated Dihydro-1,4-oxathiin Carboxanilides and Their Fungicidal Activity (삼불화메틸기가 포함된 디히드로-1,4-옥사티인 카르복스아닐리드 유도체의 합성과 살균 활성)

  • Nam, Kee-Dal;Kim, Jin-Cheol;Cho, Kwang-Yun;Hahn, Hoh-Gyu
    • Applied Biological Chemistry
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    • v.44 no.3
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    • pp.191-196
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    • 2001
  • ${\alpha},{\beta}$-Unsaturated carboxanilides 5 with trifluromethylated dihydro-1,4-oxathiins were synthesized for the development of new agrochemical fungicide. Chlorination of trifluoromethylated ${\beta}-keto$ ester 6 followed by the reaction with 1,2-mercaptoethanol gave intermediate 1,4-oxathiane 11. Without purification of 11, substitution of hydroxy group by chlorine, followed by dehydrochlorination of 10 in the presence of triethylamine afforded trifluoromethylated dihydro-1,4-oxathiin ethyl ester 9. Acylation of the hydroxy group of the carboxylic acid 12 followed by treatment of various amines gave the corresponding trifluoromethylated dihydro-1,4-oxathiin carboxamides 5. Antifungal screening (in vivo) of the synthesized compounds against typical plant diseases, which include rice blast, rice sheath blight, cucumber gray mold, tomato late blight, wheat leaf rust, and barley powdery mildew, was carried out. Where meta position of the phenyl group was substituted with isopropoxy or isopropyl group, excellent antifungal activities against rice sheath blight and wheat leaf rust were detected.

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Antifungal and Proteolytic Activity and Auxin Formation of Bacterial Strains Isolated from Highland Forest Soils of Halla Mountain (한라산 고지대 토양에서 분리한 미생물의 항균 및 단백질분해 활성, 오옥신 생산 특성)

  • Kim, Tack-Soo;Ko, Min-Jung;Lee, Se-Weon;Han, Ji-Hee;Park, Kyung-Seok;Park, Jin-Woo
    • The Korean Journal of Pesticide Science
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    • v.15 no.4
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    • pp.495-501
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    • 2011
  • Bacterial strains were isolated from forest soils of Halla mountain, Jeju island in Korea. The soil samples were collected at each altitude of 100m from 1,000 m above sea level. Total 398 strains were isolated and tested for their physiological characteristics of antagonistic and proteolytic activities, and auxin production. Among the isolates, 172 strains were selected as antifungal strains showing antagonistic activity against at least one of 8 plant fungal pathogens (Alternaria alternata, Botrytis cinerea, Collectotrichum acutatum, Fusarium oxysporum, Phytophthora capsici, Pythium ultimum and Sclerotinia sclerotiorum). In addition 203 strains for proteolytic activity and 26 strains for auxin production were characterized for further study. Je28-4 (Rhodococcus sp.) were showed 80% of control value against tomato gray mold in vivo. Thus, it is suggested that soil bacteria isolated from forest soils of Halla mountain can be important sources of bioactive compounds for improving plant growth or promising biocontrol agents.

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.

Inhibitory effects of environment-friendly materials and defense response signaling chemicals against anthracnose occurrence in Jujube (Zizyphus jujuba Miller)

  • Kim, Su Jun;Kim, Eun Su;Kim, Seung Heui;Yun, Hae Keun
    • Korean Journal of Agricultural Science
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    • v.45 no.3
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    • pp.365-378
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    • 2018
  • Anthracnose caused by Colletotrichum gloeosporioides, which is one of the major diseases of red dates, causes severe damages in jujube (Zizyphus jujuba Miller) production in Korea. This study was done to evaluate the inhibition of anthracnose occurrence and pathogen growth by the treatment of environment-friendly materials such as a Bordeaux mixture and loess-sulfur mixture and by defense-response signaling in jujube. The in vitro test of the environment-friendly materials and signaling molecules that were routinely applied did not exhibit any antifungal activities against the pathogen for jujube anthracnose. The Bordeaux mixture and loess-sulfur mixture at a two-fold concentration showed inhibition zones that were 16.0 and 20.3 mm in diameter, respectively. In the pathogen inoculation test with detached jujube tree leaves, while treatment with the environment-friendly materials diluted by half showed no inhibition of lesion development, they did show inhibition of lesion development when they were routinely applied to the leaves. In detached jujube fruits inoculated with the pathogen, better suppressive effects by the treatment of the environment-friendly materials were seen in the fruits at a young stage rather than in the ripening stage. The in vivo test with jujube trees in pots showed that the treatment of salicylic acid (1 mM) resulted in the best suppressive effects against lesion development. The results suggest that it is possible to manage the incidence of anthracnose by the treatment of environment-friendly materials such as the Bordeaux and loess-sulfur mixtures and signaling chemicals such as ethephon, hydrogen peroxide, methyl jasmonate, and salicylic acid in jujube trees and fruits. Consequently, these findings suggest that environment-friendly materials and defense response signaling molecules could be used as suitable candidates for sustainable agrochemicals to manage anthracnose in jujube production.

Application of Rhizobacteria for Plant Growth Promotion Effect and Biocontrol of Anthracnose Caused by Colletotrichum acutatum on Pepper

  • Lamsal, Kabir;Kim, Sang Woo;Kim, Yun Seok;Lee, Youn Su
    • Mycobiology
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    • v.40 no.4
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    • pp.244-251
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    • 2012
  • In vitro and greenhouse screening of seven rhizobacterial isolates, AB05, AB10, AB11, AB12, AB14, AB15 and AB17, was conducted to investigate the plant growth promoting activities and inhibition against anthracnose caused by Colletotrichum acutatum in pepper. According to identification based on 16S rDNA sequencing, the majority of the isolates are members of Bacillus and a single isolate belongs to the genus Paenibacillus. All seven bacterial isolates were capable of inhibiting C. acutatum to various degrees. The results primarily showed that antibiotic substances produced by the selected bacteria were effective and resulted in strong antifungal activity against the fungi. However, isolate AB15 was the most effective bacterial strain, with the potential to suppress more than 50% mycelial growth of C. acutatum in vitro. Moreover, antibiotics from Paenibacillus polymyxa (AB15) and volatile compounds from Bacillus subtilis (AB14) exerted efficient antagonistic activity against the pathogens in a dual culture assay. In vivo suppression activity of selected bacteria was also analyzed in a greenhouse with the reference to their prominent in vitro antagonism efficacy. Induced systemic resistance in pepper against C. acutatum was also observed under greenhouse conditions. Where, isolate AB15 was found to be the most effective bacterial strain at suppressing pepper anthracnose under greenhouse conditions. Moreover, four isolates, AB10, AB12, AB15, and AB17, were identified as the most effective growth promoting bacteria under greenhouse conditions, with AB17 inducing the greatest enhancement of pepper growth.

Efficacy of Chaetomium Species as Biological Control Agents against Phytophthora nicotianae Root Rot in Citrus

  • Phung, Manh Hung;Wattanachai, Pongnak;Kasem, Soytong;Poeaim, Supattra
    • Mycobiology
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    • v.43 no.3
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    • pp.288-296
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    • 2015
  • Thailand is one of the largest citrus producers in Southeast Asia. Pathogenic infection by Phytophthora, however, has become one of major impediments to production. This study identified a pathogenic oomycete isolated from rotted roots of pomelo (Citrus maxima) in Thailand as Phytophthora nicotianae by the internal transcribed spacer ribosomal DNA sequence analysis. Then, we examined the in vitro and in vivo effects of Chaetomium globosum, Chaetomium lucknowense, Chaetomium cupreum and their crude extracts as biological control agents in controlling this P. nicotianae strain. Represent as antagonists in biculture test, the tested Chaetomium species inhibited mycelial growth by 50~56% and parasitized the hyphae, resulting in degradation of P. nicotianae mycelia after 30 days. The crude extracts of these Chaetomium species exhibited antifungal activities against mycelial growth of P. nicotianae, with effective doses of $2.6{\sim}101.4{\mu}g/mL$. Under greenhouse conditions, application of spores and methanol extracts of these Chaetomium species to pomelo seedlings inoculated with P. nicotianae reduced root rot by 66~71% and increased plant weight by 72~85% compared to that in the control. The method of application of antagonistic spores to control the disease was simple and economical, and it may thus be applicable for large-scale, highly effective biological control of this pathogen.

Effects of Medicinal Herb Extracts of Artemisia iwayomogi Kitamura and Angelica gigas Nakai on Disease Resistance in Olive Flounder Paralichthys olivaceus (한인진(Artemisia iwayomogi Kitamura)과 참당귀(Angelica gigas Nakai) 추출물이 넙치(Paralichthys olivaceus) 항병력에 미치는 영향)

  • Kim, Na Young;Lee, Nam-Sil;Jeon, Eun Ji;Seo, Jung Soo;Woo, Soo Ji;Kim, Myung Sug;Kang, So Young;Jung, Sung Hee
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.54 no.5
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    • pp.634-643
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    • 2021
  • Han In-jin (Artemisia iwayomogi Kitamura) and Cham Dang-gwi (Angelica gigas Nakai) exhibit antibacterial, antiparasitic, antifungal, and antiviral properties in vitro. In this study, mixture of the extracts of these two medicinal plants was absorbed on pellets. Thereafter, these pellets were fed to olive flounder Paralichthys olivaceus for 12 weeks at laboratory (1st experiment) and 24 weeks at field test (2nd experiment), and the immune activity and disease resistance properties of the extracts were examined. It was observed that lysozyme activities of plasma, spleen, and kidney improved after 12 weeks. Furthermore, when the olive flounders were artificially infected with bacterial pathogens, their cumulative mortality decreased in the group that was fed the extracts for 12 weeks compared to that in control group, and the relative percent survival also improved. This study concluded that mixture of Han In-jin and Cham Dang-gwi extracts provides disease resistance in vivo.

Antifungal Activity of Non-thermal Dielectric Barrier Discharge Plasma Against Clinical Isolates of Dermatophytes

  • Ali, Anser;Hong, Young June;Lee, SeungHyun;Choi, Eun Ha;Park, Bong Joo
    • Proceedings of the Korean Vacuum Society Conference
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    • 2014.02a
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    • pp.260-260
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    • 2014
  • Dermatophytes can invade in keratinized tissues and cause dermatophytosis [1] that rank among the most widespread and common infectious diseases world-wide. Although several systemically and topically administered drugs with activities against these fungi are available, still complete eradication of some of these infections, is difficult and relapses and remissions are often observed [2,3]. In addition, some people are allergic to many of the available drugs which add complications even more. Therefore, the search for novel, selective and more effective therapy is always required and it may help the clinicians to choose the correct treatment for their patients. Non-thermal plasmas primarily generate reactive species and recently have emerged as an efficient tool for medical applications including sterilization. In this study, we evaluated the ability of non-thermal dielectric barrier discharge (DBD) plasma for the inactivation of clinical isolates of Trichophyton genera, Trichophyton mentagrophytes (T. mentagrophytes) and Trichophyton rubrum (T. rubrum), which cause infections of nails and skin and, are two of the most frequently isolated dermatophytes [4]. Our results showed that DBD plasma has considerable time dependent inactivation potential on both T. mentagrophytes and T. rubrum in-vitro. Furthermore, the mechanisms for plasma based T. mentagrophytes and T. rubrum inactivation and planning for in-vivo future studies will be discussed.

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Beta-asarone Induces LoVo Colon Cancer Cell Apoptosis by Up-regulation of Caspases through a Mitochondrial Pathway in vitro and in vivo

  • Zou, Xi;Liu, Shen-Lin;Zhou, Jin-Yong;Wu, Jian;Ling, Bo-Fan;Wang, Rui-Ping
    • Asian Pacific Journal of Cancer Prevention
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    • v.13 no.10
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    • pp.5291-5298
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    • 2012
  • Beta-asarone is one of the main bioactive constituents in traditional Chinese medicine Acorus calamu. Previous studies have shown that it has antifungal and anthelmintic activities. However, little is known about its anticancer effects. This study aimed to determine inhibitory effects on LoVo colon cancer cell proliferation and to clarify the underlying mechanisms in vitro and in vivo. Dose-response and time-course anti-proliferation effects were examined by MTT assay. Our results demonstrated that LoVo cell viability showed dose- and time-dependence on ${\beta}$-asarone. We further assessed anti-proliferation effects as ${\beta}$-asarone-induced apoptosis by annexin V-fluorescein isothiocyanate/propidium iodide assay usinga flow cytometer and observed characteristic nuclear fragmentation and chromatin condensation of apoptosis by microscopy. Moreover, we found the apoptosis to be induced through the mitochondrial/caspase pathway by decreasing mitochondrial membrane potential (MMP) and reducing the Bcl-2-to-Bax ratio, in addition to activating the caspase-9 and caspase-3 cascades. Additionally, the apoptosis could be inhibited by a pan-caspase inhibitor, carbobenzoxy-valyl-alanyl-aspartyl-[O-methyl]-fluoromethylketone (Z-VAD-FMK). When nude mice bearing LoVo tumor xenografts were treated with ${\beta}$-asarone, tumor volumes were reduced and terminal deoxynucleotide transferase-mediated dUTP nick end labeling (TUNEL) assays of excised tissue also demonstrated apoptotic changes. Taken together, these findings for the first time provide evidence that ${\beta}$-asarone can suppress the growth of colon cancer and the induced apoptosis is possibly mediated through mitochondria/caspase pathways.