scholarly journals Simplification of Natural β-Carboline Alkaloids to Obtain Indole Derivatives as Potent Fungicides against Rice Sheath Blight

Molecules ◽  
2020 ◽  
Vol 25 (5) ◽  
pp. 1189
Author(s):  
Jie Zeng ◽  
Zhijun Zhang ◽  
Qi Zhu ◽  
Zhiyan Jiang ◽  
Guohua Zhong
Keyword(s):  
Mode Of Action ◽  
Fungicidal Activity ◽  
Sheath Blight ◽  
Environmentally Benign ◽  
Indole Derivatives ◽  
Rice Sheath Blight ◽  
Structural Alterations ◽  
Validamycin A ◽  
In Vivo Bioassay

The increasing resistance of rice sheath blight caused by Rhizoctonia solani highlights the need for highly effective and environmentally benign agents. Natural β-carboline alkaloids were simplified to obtain a series of indole derivatives, and their fungicidal activity and preliminary mode of action against R. solani were also evaluated. The initial hit indole (7) displayed significant fungicidal activity with an EC50 value of 25.56 μg/mL, and was selected for further optimization. Importantly, compound 55, the most active compound, had an EC50 value of 0.62 μg/mL, and approximately 300-fold more potent than validamycin A (EC50 = 183.00 μg/mL). In vivo bioassay also demonstrated that compound 55 showed better fungicidal activities than validamycin A. Moreover, the mechanism studies revealed that compound 55 not only caused remarkable morphological and structural alterations of R. solani hyphae, but also induced the loss of mitochondrial membrane potential and interfered with DNA synthesis. Therefore, compound 55 showed superior fungicidal activity against R. solani, and the elucidated mode of action supported the potential application of compound 55 against rice sheath blight.

scholarly journals Evolution from Natural β-Carboline Alkaloids to Obtain 1,2,4,9-tetrahydro-3-thia-9-aza-fluorene Derivatives as Potent Fungicidal Agents against Rhizoctonia solani

2018 ◽  
Vol 19 (12) ◽  
pp. 4044 ◽  
Author(s):  
Junmin Xi ◽  
Zhijun Zhang ◽  
Qi Zhu ◽  
Guohua Zhong
Keyword(s):  
Rhizoctonia Solani ◽  
Fungicidal Activity ◽  
Sheath Blight ◽  
Potential Candidate ◽  
Oxygen Species ◽  
Rice Sheath Blight ◽  
Validamycin A ◽  
Rice Disease

Rice sheath blight, caused by Rhizoctonia solani, is a globally important rice disease and the increasing resistance of this pathogen highlights the need for new active compounds against rice sheath blight. In this study, natural β-carboline alkaloids were optimized to obtain a series of 1,2,4,9-tetrahydro-3-thia-9-aza-fluorene derivatives and evaluated for their fungicidal activity and mode of action against R. solani. Of these compounds, 18 exhibited significant in vitro fungicidal activity against R. solani, with an EC50 value of 2.35 μg/mL, and was more active than validamycin A. In vivo bioassay also demonstrated that 18 displayed superior protective and curative activities as compared to validamycin A. Mechanistically, 18 not only induced the loss of mitochondrial membrane potential and accumulation of reactive oxygen species, but also interfered with DNA synthesis. Therefore, compound 18 displayed pronounced in vitro and in vivo fungicidal activity against R. solani and could be used as a potential candidate for the control of rice sheath blight.

scholarly journals In vitro and in vivo antifungal properties of silver nanoparticles against Rhizoctonia solani , a common agent of rice sheath blight disease

2016 ◽  
Vol 11 (3) ◽  
pp. 236-240 ◽  
Author(s):  
Meysam Soltani Nejad ◽  
Gholam Hosein Shahidi Bonjar ◽  
Mehrdad Khatami ◽  
Abbas Amini ◽  
Sonia Aghighi
Keyword(s):  
Silver Nanoparticles ◽  
Rhizoctonia Solani ◽  
Sheath Blight ◽  
Rice Sheath Blight ◽  
Sheath Blight Disease ◽  
Antifungal Properties ◽  
Blight Disease

scholarly journals Fungicidal Activity and Mechanism of Action of Glabridin from Glycyrrhiza glabra L.

2021 ◽  
Vol 22 (20) ◽  
pp. 10966
Author(s):  
Anping Li ◽  
Zhongmin Zhao ◽  
Shaoyong Zhang ◽  
Zhijun Zhang ◽  
Yanping Shi
Keyword(s):  
Reactive Oxygen Species ◽  
Membrane Potential ◽  
Mitochondrial Membrane ◽  
Fungicidal Activity ◽  
Phytopathogenic Fungi ◽  
Glycyrrhiza Glabra ◽  
Oxygen Species ◽  
Glycyrrhiza Glabra L ◽  
In Vivo Bioassay

Glycyrrhiza glabra (Licorice) belongs to the Fabaceae family and its extracts have exhibited significant fungicidal activity against phytopathogenic fungi, which has mainly been attributed to the presence of phenolic compounds such as flavonoids, isoflavonoids and chalcones. In this study, a series of licorice flavonoids, isoflavonoids and chalcones were evaluated for their fungicidal activity against phytopathogenic fungi. Among them, glabridin exhibited significant fungicidal activity against ten kinds of phytopathogenic fungi. Notably, glabridin displayed the most active against Sclerotinia sclerotiorum with an EC50 value of 6.78 µg/mL and was 8-fold more potent than azoxystrobin (EC50, 57.39 µg/mL). Moreover, the in vivo bioassay also demonstrated that glabridin could effectively control S. sclerotiorum. The mechanism studies revealed that glabridin could induce reactive oxygen species accumulation, the loss of mitochondrial membrane potential and cell membrane destruction through effecting the expression levels of phosphatidylserine decarboxylase that exerted its fungicidal activity. These findings indicated that glabridin exhibited pronounced fungicidal activities against S. sclerotiorum and could be served as a potential fungicidal candidate.

Synthesis and Fungicidal Activity of (E)-5-[1-(4-Phenyl-2-oxo-1-oxaspiro[4.5]dec-3-en-3-yl)ethylidene]-2-aminoimidazolin-4-one Derivatives

Synthesis ◽  
2017 ◽  
Vol 49 (20) ◽  
pp. 4663-4669
Author(s):  
Zhao Yu ◽  
Tang Bo ◽  
Guan Aiying ◽  
Wang Weiwei ◽  
Zhang Zhenhua ◽  
...  
Keyword(s):  
1H Nmr ◽  
Fungicidal Activity ◽  
In Vitro Bioassay ◽  
In Vivo Bioassay

(E)-5-[1-(4-Phenyl-2-oxo-1-oxaspiro[4.5]dec-3-en-3-yl)eth­yl­idene]-2-aminoimidazolin-4-one derivatives, as novel fungicidal agents, are designed and synthesized in moderate to excellent yields in four steps from (1-hydroxycyclohexyl)(phenyl)methanone and diketene as the starting materials. The products are characterized by 1H NMR and HRMS (ESI) analysis. An in vivo bioassay shows that some of the products exhibit good to excellent inhibition against P. cubensis and C. lagenarium, whilst up to 94.7% inhibition against P. capsici and up to 78.1% inhibition against B. cinerea is demonstrated in the in vitro bioassay. EC50 values of 3.40 and 5.86 μg/mL are demonstrated against P. capsici and B. cinerea.

In-vivo topography of structural alterations of the anterior cingulate gyrus in schizophrenia

2007 ◽  
Vol 40 (05) ◽  
Author(s):  
T Zetzsche ◽  
UW Preuss ◽  
T Frodl ◽  
D Watz ◽  
G Schmitt ◽  
...  
Keyword(s):  
Anterior Cingulate ◽  
Cingulate Gyrus ◽  
Anterior Cingulate Gyrus ◽  
Structural Alterations

Insulinomimetic properties of trace elements and characterization of their in vivo mode of action

Diabetes ◽  
1990 ◽  
Vol 39 (10) ◽  
pp. 1243-1250 ◽  
Author(s):  
L. Rossetti ◽  
A. Giaccari ◽  
E. Klein-Robbenhaar ◽  
L. R. Vogel
Keyword(s):  
Trace Elements ◽  
Mode Of Action

scholarly journals A Peptide Found in Human Serum, Derived from the C-Terminus of Albumin, Shows Antifungal Activity In Vitro and In Vivo

2020 ◽  
Vol 8 (10) ◽  
pp. 1627
Author(s):  
Tecla Ciociola ◽  
Pier Paolo Zanello ◽  
Tiziana D’Adda ◽  
Serena Galati ◽  
Stefania Conti ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Human Serum ◽  
Fungicidal Activity ◽  
Galleria Mellonella ◽  
Serum Proteins ◽  
Morphological Alterations ◽  
C Terminus ◽  
Different Sources

The growing problem of antimicrobial resistance highlights the need for alternative strategies to combat infections. From this perspective, there is a considerable interest in natural molecules obtained from different sources, which are shown to be active against microorganisms, either alone or in association with conventional drugs. In this paper, peptides with the same sequence of fragments, found in human serum, derived from physiological proteins, were evaluated for their antifungal activity. A 13-residue peptide, representing the 597–609 fragment within the albumin C-terminus, was proved to exert a fungicidal activity in vitro against pathogenic yeasts and a therapeutic effect in vivo in the experimental model of candidal infection in Galleria mellonella. Studies by confocal microscopy and transmission and scanning electron microscopy demonstrated that the peptide penetrates and accumulates in Candida albicans cells, causing gross morphological alterations in cellular structure. These findings add albumin to the group of proteins, which already includes hemoglobin and antibodies, that could give rise to cryptic antimicrobial fragments, and could suggest their role in anti-infective homeostasis. The study of bioactive fragments from serum proteins could open interesting perspectives for the development of new antimicrobial molecules derived by natural sources.

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