A new antitumor antibiotic, spergualin: Isolation and antitumor activity.

Takeuchi, Tomio; Iinuma, Hisae; Kunimoto, Setsuko; Masuda, Tohru; Ishizuka, Masaaki; Takeuchi, Mieko; Hamada, Masa; Naganawa, Hiroshi; Kondo, Shinichi; Umezawa, Hamao

doi:10.7164/antibiotics.34.1619

Cited by 197 publications

(61 citation statements)

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“…It is a synthetic derivative of spergualin, originally isolated from Bacillus laterosporus, and it differs from other immunosuppressive agents both structurally and mechanistically (2). DSG has been shown to bind certain heat shock proteins (hsp), such as heat shock cognate protein (hsc)70 and hsp90, and to partially inhibit the nuclear transport of the transcription factor, NF-B (3)(4)(5).…”

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confidence: 99%

The Immunosuppressive Agent 15-Deoxyspergualin Functions by Inhibiting Cell Cycle Progression and Cytokine Production Following Naive T Cell Activation

Holcombe

Mellman

Janeway

et al. 2002

The Journal of Immunology

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Immunosuppressive agents are commonly used in the prevention of graft rejection following transplantation and in the treatment of autoimmunity. In this study, we examined the immunosuppressive mechanism of the drug 15-deoxyspergualin (DSG), which has shown efficacy in the enhancement of graft survival and in the treatment of autoimmunity. Using a murine model of chronic relapsing and remitting experimental autoimmune encephalomyelitis, we were able to demonstrate that DSG both delayed and reduced the severity of experimental autoimmune encephalomyelitis. Subsequent in vitro studies to examine the mechanism of immune suppression showed that DSG was not able to inhibit early activation of naive CD4 T cells, but DSG did effectively inhibit the growth of naive CD4 T cells after activation. An analysis of cell proliferation and cell cycle showed that DSG treatment led to a block in cell cycle progression 2–3 days following Ag stimulation. In addition, DSG treatment inhibited the production of IFN-γ by Th1 effector T cells. These studies suggest that CD4 T cells are a predominant target for DSG and the immunosuppressive effects of the drug may result from reduced CD4 T cell expansion and decreased polarization into IFN-γ-secreting Th1 effector T cells in the induction of certain autoimmune disorders.

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The Immunosuppressive Agent 15-Deoxyspergualin Functions by Inhibiting Cell Cycle Progression and Cytokine Production Following Naive T Cell Activation

Holcombe

Mellman

Janeway

et al. 2002

The Journal of Immunology

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“…15-Deoxy derivative of spergualin with 7-guanidinoheptanoic acid [134] was found to be more potent in antitumor activity (Takeuchi et al, 1981;Umezawa et al, 1981;Umezawa et al, 1987).…”

Section: Lydiamycinsmentioning

confidence: 99%

Paradigm Shifts in Fungal Secondary Metabolite Research: Unusual Fatty Acids Incorporated into Fungal Peptides

Dembitsky¹

2017

Int. J. Curr. Res. Biosci. Plant Biol.

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A b s t r a c t A r t i c l e I n f oThis review is a comprehensive survey of unique, unusual, and rare fatty acids incorporated into natural marine and terrestrial peptides obtained from fungi, fungal endophytes, lichenized ascomycetes, basidiomycetes, and actinomycetes. Lots of fungal peptides display important biological activities of interest, which includes antitumor, antibacterial, antimicrobial, antifungal, phototoxic, HIV inhibitory, immunosuppressive properties, and other pharmacological activities. There is no doubt that they are of great importance, especially in medicinal chemistry and/or pharmaceutical application. This review presents structures of more than 150 fatty acids, incorporated into marine and terrestrial fungal lipopeptides.

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“…Deoxyspergualin (DSG) was isolated in the 1980's from the Bacillus laterosporus found in Japanese fields (Takeuchi et al 1981). It was initially expected to be an antitumor antibiotic, but it also had special immunosuppressive effects.…”

confidence: 99%

Usage of Deoxyspergualin on Steroid-Resistant Acute Rejection in Living Donor Liver Transplantation

Kawagishi

Satoh

Enomoto

et al. 2006

Tohoku J. Exp. Med.

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A new antitumor antibiotic, spergualin: Isolation and antitumor activity.

Cited by 197 publications

References 1 publication

The Immunosuppressive Agent 15-Deoxyspergualin Functions by Inhibiting Cell Cycle Progression and Cytokine Production Following Naive T Cell Activation

The Immunosuppressive Agent 15-Deoxyspergualin Functions by Inhibiting Cell Cycle Progression and Cytokine Production Following Naive T Cell Activation

Paradigm Shifts in Fungal Secondary Metabolite Research: Unusual Fatty Acids Incorporated into Fungal Peptides

Usage of Deoxyspergualin on Steroid-Resistant Acute Rejection in Living Donor Liver Transplantation

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