• Title/Summary/Keyword: Antifungal compound

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Marine Algicolous Endophytic Fungi - A Promising Drug Resource of the Era

  • Sarasan, Manomi;Puthumana, Jayesh;Job, Neema;Han, Jeonghoon;Lee, Jae-Seong;Philip, Rosamma
    • Journal of Microbiology and Biotechnology
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    • v.27 no.6
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    • pp.1039-1052
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    • 2017
  • Endophytic fungi have currently been acknowledged as the most promising source of bioactive compounds for drug discovery, and considerable progress has been made in exploring their diversity, species richness, and bioprospecting. Fungal endophytes from unique environmental settings offer a pool of potentially useful medicinal entities. Owing to the constant stresses imposed on macroalgae by marine environments, it is believed that algae and their associated endophytic symbionts represent a good source of structurally diverse bioactive secondary metabolites. Despite the proven significance of active metabolites of algal endophytes, little have been exploited. This review highlights the latest discoveries in algicolous endophytic research, with particular focus on the bioactive metabolites from algal endophytes. Compounds are classified according to their reported biological activities, like anticancer, antibacterial, antifungal, and antioxidant properties. Present experimental evidence suggests that a majority of the bioactive metabolites were reported from Phaeophyceae followed by Rhodophyceae and Chlorophyceae. An intensive search for newer and more effective bioactive metabolites has generated a treasure trove of publications, and this review partially covers the literature published up to 2016.

Isolation and Biological Activity of $Resveratrol-3-O-{\beta}-D-Glucoside$ in Transgenic Rehmannia glutinosa L. Transformed by Peanut Resveratrol Synthase Gene (RS3)

  • Lim, Jung-Dae;Yang, Deok-Chun;Yun, Song-Joong;Chung, Ill-Min;Sung, Eun-Soo;Kim, Myong-Jo;Heo, Kweon;Yu, Chang-Yeon
    • Korean Journal of Medicinal Crop Science
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    • v.12 no.5
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    • pp.406-414
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    • 2004
  • Resveratrol, which is both a phytoalexin with antifungal activity and a phytochemical associated with reduced cancer risk and reduced cardiovascular disease, is synthesized in a limited number of plant species including peanut. Resveratrol synthesis is catalyzed by the enzyme stilbene synthase including resveratrol synthase (RS). Resveratrol synthase gene (RS3) obtained from peanut, Arachis hypogaea, Fabaceae has been transferred into chinese foxglove, Rehmannia glutinosa by using Agrobacterium mediated transformation. RS t-DNA introduced to chinese foxglove (R. glutinosa L) by transformation and its reaction product, $resveratrol-3-O-{\beta}-D-glucoside$ was isolated and characterized using HPLC. Also its biological effects was tested in inhibition of the lipid peroxidation of mouse LDL by glycosylated stilbenes derivatives obtained from transgenic plants. $Resveratrol-3-O-{\beta}-D-glucoside$ isolated from transgenic R. glutinosa L. showed antimicrobial activity of the growth inhibition zone against Escherichia coli and Salmonella typhimurium. Therefore, this compound can be contributed to be useful as a phytoalexin for plant health as well as a phytochemical for human health.

Defense Response and Suppression of Phytophthora Blight Disease of Pepper by Water Extract from Spent Mushroom Substrate of Lentinula edodes

  • Kang, Dae-Sun;Min, Kyong-Jin;Kwak, A-Min;Lee, Sang-Yeop;Kang, Hee-Wan
    • The Plant Pathology Journal
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    • v.33 no.3
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    • pp.264-275
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    • 2017
  • The spent mushroom substrate (SMS) of Lentinula edodes that was derived from sawdust bag cultivation was used as materials for controlling Phytophthora blight disease of pepper. Water extract from SMS (WESMS) of L. edodes inhibited mycelial growth of Phytophthora capsici, suppressed Phytophthora blight disease of pepper seedlings by 65% and promoted growth of the plant over 30%. In high performance liquid chromatography (HPLC) analysis, oxalic acid was detected as the main organic acid compound in WESMS and inhibited the fungal mycelium at a minimum concentration of 200 mg/l. In quantitative real-time PCR, the transcriptional expression of CaBPR1 (PR protein 1), CaBGLU (${\beta}$-1,3-glucanase), CaPR-4 (PR protein 4), and CaPR-10 (PR protein 10) were significantly enhanced on WESMS and DL-${\beta}$-aminobutyric acid (BABA) treated pepper leaves. In addition, the salicylic acid content was also increased 4 to 6 folds in the WESMS and BABA treated pepper leaves compared to water treated leaf sample. These findings suggest that WESMS of L. edodes suppress Phytophthora blight disease of pepper through multiple effects including antifungal activity, plant growth promotion, and defense gene induction.

Isolation of Antimicrobial Active Substance from Aristolochia tagala Champ. against Sclerotial Rot (Sclerotinia sclerotiorum) (이엽마두령(Aristolochia tagala Champ.)추출물로부터 균핵병 병원균(Sclerotinia sclerotiorum)에 대한 항균 활성물질 탐색)

  • Kim, Hyun-Sang;Shon, Jinhan;Choi, Yong-Hwa
    • Korean Journal of Organic Agriculture
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    • v.23 no.4
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    • pp.951-962
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    • 2015
  • To develop environment-friendly agricultural products with anti-microbial activity against Sclerotinia sclerotiorum as a pathogen of sclerotium disease, Aristolochia tagala Champ. was extracted by methanol and its extract was fractionated into several solvent fractions. The chloroform fraction, which showed the highest antimicrobial activity, was separated by column chromatography and obtained forty three subfractions. The forty three fractions were searched the anti-fungal activities by bioassay. The most active No. 26 subfraction was analyzed by GC-MS. Each mass spectra, corresponding to each peak of chromatogram, was compared to MS database of Wiley library. As a result, 2,4-di-tetra-butyl-phenol, 2-mono-palmitin, 1-mono-stearin were profiled as maine compounds in No. 26 subfraction. Bioassay using commercial 1-mono-stearin to test for the anti-microbial activity conformed the antimicrobial active compound. In conclusion, 1-mono-stearin identified from Aristolochia tagala Champ. was antimicrobial chemical against Sclerotinia sclerotiorum.

A Randomized Active Controlled Clinical Trial to Evaluate Safety and Efficacy of a Topical Unani Formulation Marham Kharish Jadeed in the Management of Qūbā (Tinea Corporis)

  • Aaliya, Aaliya;Nawab, Mohammad;Kazmi, M.H.;Ayyub, Sana
    • CELLMED
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    • v.10 no.3
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    • pp.22.1-22.7
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    • 2020
  • Introduction: Qūbā (Tinea Corporis) is a very common disease widely prevalent worldwide. 20 - 25 % individuals suffer for this stubborn disease. Unani System of Medicine offers its treatment. There are many pharmacopoeial formulations indicated for various types of dermatophytic infections. In this study clinical efficacy and safety of the topical Unani formulation Marham Kharish Jadeed (a compound drug in the dosage form of an ointment) was assessed and compared with a standard conventional medicine. Materials and methods: A clinical study was conducted on 60 participants of qūbā randomized into test and control groups (n=30 in each group). The participants were clinically diagnosed and confirmed by microscopy of skin scrapings. The efficacy of the Unani formulation was assessed in terms of TSS score and elimination of fungal elements from the skin lesions. The data collected were analyzed statistically. Results and discussion: The study showed that the Unani formulation had comparatively better efficacy clinically than conventional medicine Terbinafine hydrochloride 1% cream in terms of reduction of itching, erythema, scaling, peripheral raised margins of the lesion comparing to baseline. In this study, 27 participants in test group and 18 participants in control group were completely cured (≥75% reduction in TSS Score with Mycological Cure) after 4 weeks of treatment. The efficacy of the Unani formulation was found significant statistically. The individual drugs of the formulations having analgesic (Musakkin), blood purifier (Muṣaffi-i-Dam), demulcent (Mulaṭṭif), antifungal (Qātil-i-fafūndῑ), detergent (Jālῑ), refrigerant (Mubarrid) and antiseptic (Dāfi'-i-'Ufūnat) properties might be responsible for the efficacy of Unani formulation. Conclusion: The findings of the study suggested that the Unani formulation was found effective and safe in the management of qūbā. No local and systemic adverse effect was reported during the study.

Antibacterial and Antifungal Activities of a Naphthoquinone Derivative Isolated from the Fruits of Catalpa ovata G.$D_{ON}$

  • Kuk, Ju-Hee;Ma, Seung-Jin;Moon, Jae-Hak;Kim, Kil-Yong;Choi, Sang-Ho;Park, Keun-Hyung
    • Journal of Microbiology and Biotechnology
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    • v.12 no.5
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    • pp.858-863
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    • 2002
  • An antimicrobial compound was isolated from the MeOH extract of Catalpa ovata G.$D_{ON}$ fruits, and its structure was Identified as 4,9-dihydroxy-2,2-dimethyl-3,4-Uihydronaphtho[2,3-b]pyran-5,10-dione (HMNP). The antimicrobial activity of the Un was determined by measuring the dose-response inhibiton of microbial growth in liquid cultures and then compared with that of lapachol, a well known antimicrobial 1,4-naphthoquinone. The antimicrobial activity of the HMNP was more effective than that of lapachol over a wide range of test organisms. Gram-positive bacteria, yeast, and fungi ($IC_{50}$ $20-75\muM$) were found to be more sensitive to the HMNP than Cram-negative bacteria ($IC_{50}$ > $100\muM$). The HMNP also inhibited germination of spores of many fungi. The morphological defurmation of the fungal spores was induced by the treatment of HMNP, as illustrated by Scanning Electron Microscopy (SEM).

Synthesis of Some Biologically Active Halogenopurines (생물 활성이 있는 Halogenopurines의 합성)

  • Hu, Yu Lin;Liu, Xiang;Lu, Ming;Ge, Qiang;Liu, Xiao Bin
    • Journal of the Korean Chemical Society
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    • v.54 no.4
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    • pp.429-436
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    • 2010
  • A series of some biologically active halogenopurines were synthesized from commercially available guanine (1). The reaction of guanine with acetic anhydride yielded 2,9-diacetylguanine (2-1) by acetylation reaction. Further treatment of 2-1 with $POCl_3$ by PEG-2000 phase transfer catalysis furnished the important compound 3a, then 2-amino-6-halogenopurines (3b-d) were obtained through chlorine-exchange halogenations between KX and 3a by TPPB phase transfer catalyst. Further, 2-halogenopurines (2-2a-d, 4-2a-d, 5a-d) were efficiently prepared from 2-amino-6-substituted purines (1, 3a, 4-1) via a diazotization catalyzed by their corresponding CuX, and some new compounds 2-2a, 2-2c, 2-2d, 4-2c, 4-2d, 5b, 5c and 5d have been discovered. The structures of synthesized compounds were mainly established on the basis of their elemental analysis, $^1H$ NMR, as well as their mass spectral data. All the title compounds were screened for their antifungal activities, and some of the compounds showed promising activity.

A Synthesis of New Benzylimino-1,3-oxathioles and Their Fungicidal Activity (새로운 2-Benzoylimino-1,3-oxathiole 유도체의 합성 및 살균활성)

  • Nam, Kee-Dal;Shin, Sun-Ho;Mah, He-Duck;Lee, Seon-Woo;Cho, Kwang-Yun;Hahn, Hoh-Gyu
    • Applied Biological Chemistry
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    • v.45 no.3
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    • pp.157-161
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    • 2002
  • New 2-benzoylimino-1,3-oxathile derivatives 3 were synthesized and tested their fungicidal activities for the development of new agrochemical fungicide. Reaction of ${\gamma}-chloro-{\beta}-keto$ anilide derivative 5 with potassium thiocyanate followed by the treatment of acid catalyst gave cyclyzed 2-imino-1,3-oxathiole 3. New compound 3 reacted with benzoyl· chlorides to afford the corresponding 2-benzoylimino-1,3-oxathiole derivatives 7. 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. No significant fungicidal activities were shown of the synthesized compounds at 100 mg/l.

Biphasic augmentation of alpha-adrenergic contraction by plumbagin in rat systemic arteries

  • Kim, Hae Jin;Yoo, Hae Young;Zhang, Yin Hua;Kim, Woo Kyung;Kim, Sung Joon
    • The Korean Journal of Physiology and Pharmacology
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    • v.21 no.6
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    • pp.687-694
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    • 2017
  • Plumbagin, a hydroxy 1,4-naphthoquinone compound from plant metabolites, exhibits anticancer, antibacterial, and antifungal activities via modulating various signaling molecules. However, its effects on vascular functions are rarely studied except in pulmonary and coronary arteries where NADPH oxidase (NOX) inhibition was suggested as a mechanism. Here we investigate the effects of plumbagin on the contractility of skeletal artery (deep femoral artery, DFA), mesenteric artery (MA) and renal artery (RA) in rats. Although plumbagin alone had no effect on the isometric tone of DFA, $1{\mu}M$ phenylephrine (PhE)-induced partial contraction was largely augmented by plumbagin (${\Delta}T_{Plum}$, 125% of 80 mM KCl-induced contraction at $1{\mu}M$). With relatively higher concentrations (>$5{\mu}M$), plumbagin induced a transient contraction followed by tonic relaxation of DFA. Similar biphasic augmentation of the PhE-induced contraction was observed in MA and RA. VAS2870 and GKT137831, specific NOX4 inhibitors, neither mimicked nor inhibited ${\Delta}T_{Plum}$ in DFA. Also, pretreatment with tiron or catalase did not affect ${\Delta}T_{Plum}$ of DFA. Under the inhibition of PhE-contraction with L-type $Ca^{2+}$ channel blocker (nifedipine, $1{\mu}M$), plumbagin still induced tonic contraction, suggesting $Ca^{2+}$-sensitization mechanism of smooth muscle. Although ${\Delta}T_{Plum}$ was consistently observed under pretreatment with Rho A-kinase inhibitor (Y27632, $1{\mu}M$), a PKC inhibitor (GF 109203X, $10{\mu}M$) largely suppressed ${\Delta}T_{Plum}$. Taken together, it is suggested that plumbagin facilitates the PKC activation in the presence of vasoactive agonists in skeletal arteries. The biphasic contractile effects on the systemic arteries should be considered in the pharmacological studies of plumbagin and 1,4-naphthoquinones.

Control Effects of Indole Isolated from Xenorhabdus nematophila K1 on the Diseases of Red Pepper (Xenorhabdus nematophila K1 유래물질 인돌의 고추 병해 방제 효과)

  • Jeon, Mi-Hyeon;Cheon, Won-Su;Kim, Yong-Gyun;Hong, Yong-Pyo;Yi, Young-Keun
    • Research in Plant Disease
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    • v.18 no.1
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    • pp.17-23
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    • 2012
  • Indole compound is a bacterial metabolite synthesized and released by an entomopathogenic bacterium, Xenorhabdus nematophila K1. The antibiotic activity was evaluated against plant pathogens, such as Phytophthora blight and anthracnose of red pepper. Indole significantly suppressed mycelial growth of Phytophthora blight and anthracnose pathogens. Under natural sunlight conditions, indole maintained the antifungal activity for at least sixty days. The activity was not affected under the condition of soil-water. When the indole suspension was applied to surface soil before transplanting of red pepper seedlings and was then regularly sprayed to the foliage of the plants with ten days interval, it resulted in significant reduction of the disease occurrences (Phytophthora blight, anthracnose, soft rot, and black mold) by about 30%. These results suggest that indole can be used to control Phytophthora blight and anthracnose of red pepper.