Vincent Gullo | Drew University (original) (raw)
Papers by Vincent Gullo
The Journal of Antibiotics
ruber3). Independently, the same compound (named mevinolin) was isolated by ALBERTS et al.1) from... more ruber3). Independently, the same compound (named mevinolin) was isolated by ALBERTS et al.1) from Aspergillus terreus. 4a, 5-Dihydromevinolin (Fig. 2)* was also isolated from the same culture.5) All of these five structurally-related entities are potent competitive inhibitors of 3-hydroxy-3-methylglutaryl (HMG)-CoA reductase (EC 1.1.1.34)2-1), the rate-limiting enzyme in cholesterol synthesis, with mevinolin being the most potent. However, compactin is the most extensively studied. Its hypocholesteremic acitivity in several animal species including human subjects has been demonstrated8~12) and a review of its pharmacology was also publi-shed13). In our search for new microbial metabolites having HMG-CoA reductase inhibition and ultimately hypocholesteremic activities, we have regrown P. citrinum in our laboratories and discovered a new component, designated as 4a,5dihydrocompactin. This new compound apparently cannot be derived from compactin stereospecifically without lengthy chemical conversions. The present communication describes the isolation, physical and chemical properties of this unique compound. The inhibition of HMG-CoA reductase is also described.
The Journal of Antibiotics
ChemInform, 2008
Sch 213766, a Novel Chemokine Receptor CCR-5 Inhibitor from Chaetomium globosum. -(I) exhibits an... more Sch 213766, a Novel Chemokine Receptor CCR-5 Inhibitor from Chaetomium globosum. -(I) exhibits an IC 50 value of 8.6 μM in the CCR-5 receptor in vitro binding assay. -(YANG*, S.-W.; MIERZWA, R.; TERRACCIANO, J.; PATEL, M.; GULLO, V.; WAGNER, N.; BAROUDY, B.; PUAR, M.; CHAN, T.-M.; CHU*, M.; J. Antibiot. 60 (2007) 8, 524-528; Schering-Plough Res. Inst., Kenilworth, NJ 07033, USA; Eng.) -H. Haber 05-217
The Journal of Antibiotics, 1993
A novel natural product (1), with antifungal activity was isolated from the culture broth of an a... more A novel natural product (1), with antifungal activity was isolated from the culture broth of an actinomadurae. The active compoundwas separated from broth by w-butanol extraction and purified by silica gel and multicoil counter current chromatography. Physico-chemical data suggested the structure of this compoundto be a novel macrolactam disaccharide related to Sch 38518 (3). The structure wasdetermined by spectroscopic studies on the acetate derivative. It wasactive against Candida spp. (MIC's, 4~64/jg/ml) but less active than the monosaccharide, Sch 38518 (MIC's, l~16iig/ml).
ChemInform, 2010
ABSTRACT ChemInform is a weekly Abstracting Service, delivering concise information at a glance t... more ABSTRACT ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Cheminform, 2010
ABSTRACT ChemInform is a weekly Abstracting Service, delivering concise information at a glance t... more ABSTRACT ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Tetrahedron Letters, 1994
Sch 49210, Sch 53514 and Sch 53516 have been isolatedfiom a fungal culture, and identified by ana... more Sch 49210, Sch 53514 and Sch 53516 have been isolatedfiom a fungal culture, and identified by analysis of 20 NMR data Tbo diocetyhtion derivatives Sch SMIS and Sch 53517 have been synthesized These compounds demonstrate inhibitory activity of phospholipase D (PLB), and display potent activity in the antitumor invasion chamber assay.
Tetrahedron Letters, 1997
Journal of Natural Products, 2003
A novel primase inhibitor, Sch 642305 (1), was isolated from the fermentation broth of the fungal... more A novel primase inhibitor, Sch 642305 (1), was isolated from the fermentation broth of the fungal culture Penicillium verrucosum. The structure of 1 was elucidated on the basis of MS and NMR spectroscopic data as a new and unusual bicyclic 10-membered macrolide. The absolute configuration of the asymmetric centers was determined by X-ray crystallographic analysis of the p-bromobenzoate derivative (3). Compound 1 exhibited inhibitory activity against bacterial DNA primase enzyme with an EC(50) of 70 microM.
Journal of Natural Products, 2009
Journal of Natural Products, 2006
Two novel chemokine receptor CCR-5 inhibitors, Sch 210971 (1) and Sch 210972 (2), were isolated f... more Two novel chemokine receptor CCR-5 inhibitors, Sch 210971 (1) and Sch 210972 (2), were isolated from the fungal fermentation broth of Chaetomium globosum by normal- and reversed-phase HPLC purifications. The structure determination of 1 and 2 was accomplished on the basis of UV, MS, and NMR spectral data analyses including COSY, NOESY, HMQC, and HMBC experiments. The structure and relative configuration of 2 were determined unequivocally by X-ray crystallographic analysis. The major component 2 demonstrated a potent inhibitory activity of IC(50) = 79 nM in the CCR-5 receptor in vitro binding assay.
Journal of Natural Products, 1995
The structures of two novel muscarinic receptor antagonists, 1 and 2, were determined by their sp... more The structures of two novel muscarinic receptor antagonists, 1 and 2, were determined by their spectral data and high-resolution mass measurements of their degradation products. Both are aliphatic long-chain compounds and contain amide and keto functionalities. The major microbial metabolite [1] contains three terminal guanidino groups and the minor compound [2] has two terminal guanidino groups.
Journal of Industrial Microbiology & Biotechnology, 2006
Natural product compounds are the source of numerous therapeutic agents. Recent progress to disco... more Natural product compounds are the source of numerous therapeutic agents. Recent progress to discover drugs from natural product sources has resulted in compounds that are being developed to treat cancer, resistant bacteria and viruses and immunosuppressive disorders. Many of these compounds were discovered by applying recent advances in understanding the genetics of secondary metabolism in actinomycetes, exploring the marine environment and applying new screening technologies. In many instances, the discovery of a novel natural product serves as a tool to better understand targets and pathways in the disease process. This review describes recent progress in drug discovery from natural sources including several examples of compounds that inhibit novel drug targets.
Journal of Industrial Microbiology, 1991
Summary Sch 40873, a novel antifungal compound isolated from the fermentation broth of anActinoma... more Summary Sch 40873, a novel antifungal compound isolated from the fermentation broth of anActinomadura spp. was discovered in an assay designed to detect compounds with preferential activity against the invasive mycelial form ofCandida albicans. The geometric mean MIC of Sch 40873 against sevenCandida spp. in Sabouraud dextrose broth (yeast phase) was =58 µg/ml and in Eagles minimum essential medium (mycelial
The Journal of Antibiotics, 2009
The Journal of Antibiotics, 2006
A new hydrogenated azaphilone Sch725680 (1) was isolated and identified from the culture of an As... more A new hydrogenated azaphilone Sch725680 (1) was isolated and identified from the culture of an Aspergillus sp. The structure elucidation of 1 was achieved based on extensive NMR spectroscopic analyses. Compound 1 showed inhibitory activity against Saccharomyces cerevisiae (PM503) and Candida albicans (C43) with MICs of 8 and 64 mg/ml, respectively.
The Journal of Antibiotics, 2006
A new 5-alkenylresorcinol Sch725681 (1) was isolated and identified from the culture of an Asperg... more A new 5-alkenylresorcinol Sch725681 (1) was isolated and identified from the culture of an Aspergillus sp. The structure elucidation of 1 was accomplished based on extensive NMR spectroscopic analyses. Compound 1 showed inhibitory activity against Saccharomyces cerevisiae (PM503) and Candida albicans (C43) with MICs of 16 and 64 mg/ml, respectively.
The Journal of Antibiotics, 2005
A new microbial metabolite Sch 725424 (1) was isolated from the culture of Kitasatospora sp. The ... more A new microbial metabolite Sch 725424 (1) was isolated from the culture of Kitasatospora sp. The structure elucidation of 1 was accomplished based on NMR spectroscopic analyses as well as extensive structure elucidation of its dehydration product Sch 725428 (2). Compound 1 showed inhibitory activity against Staphylococcus aureus with MIC values 1ϳ2 m g/ml, and also displayed weak antifungal activity against Saccharomyces cerevisiae (PM503) with an MIC 32 mg/ml.
The Journal of Antibiotics
ruber3). Independently, the same compound (named mevinolin) was isolated by ALBERTS et al.1) from... more ruber3). Independently, the same compound (named mevinolin) was isolated by ALBERTS et al.1) from Aspergillus terreus. 4a, 5-Dihydromevinolin (Fig. 2)* was also isolated from the same culture.5) All of these five structurally-related entities are potent competitive inhibitors of 3-hydroxy-3-methylglutaryl (HMG)-CoA reductase (EC 1.1.1.34)2-1), the rate-limiting enzyme in cholesterol synthesis, with mevinolin being the most potent. However, compactin is the most extensively studied. Its hypocholesteremic acitivity in several animal species including human subjects has been demonstrated8~12) and a review of its pharmacology was also publi-shed13). In our search for new microbial metabolites having HMG-CoA reductase inhibition and ultimately hypocholesteremic activities, we have regrown P. citrinum in our laboratories and discovered a new component, designated as 4a,5dihydrocompactin. This new compound apparently cannot be derived from compactin stereospecifically without lengthy chemical conversions. The present communication describes the isolation, physical and chemical properties of this unique compound. The inhibition of HMG-CoA reductase is also described.
The Journal of Antibiotics
ChemInform, 2008
Sch 213766, a Novel Chemokine Receptor CCR-5 Inhibitor from Chaetomium globosum. -(I) exhibits an... more Sch 213766, a Novel Chemokine Receptor CCR-5 Inhibitor from Chaetomium globosum. -(I) exhibits an IC 50 value of 8.6 μM in the CCR-5 receptor in vitro binding assay. -(YANG*, S.-W.; MIERZWA, R.; TERRACCIANO, J.; PATEL, M.; GULLO, V.; WAGNER, N.; BAROUDY, B.; PUAR, M.; CHAN, T.-M.; CHU*, M.; J. Antibiot. 60 (2007) 8, 524-528; Schering-Plough Res. Inst., Kenilworth, NJ 07033, USA; Eng.) -H. Haber 05-217
The Journal of Antibiotics, 1993
A novel natural product (1), with antifungal activity was isolated from the culture broth of an a... more A novel natural product (1), with antifungal activity was isolated from the culture broth of an actinomadurae. The active compoundwas separated from broth by w-butanol extraction and purified by silica gel and multicoil counter current chromatography. Physico-chemical data suggested the structure of this compoundto be a novel macrolactam disaccharide related to Sch 38518 (3). The structure wasdetermined by spectroscopic studies on the acetate derivative. It wasactive against Candida spp. (MIC's, 4~64/jg/ml) but less active than the monosaccharide, Sch 38518 (MIC's, l~16iig/ml).
ChemInform, 2010
ABSTRACT ChemInform is a weekly Abstracting Service, delivering concise information at a glance t... more ABSTRACT ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Cheminform, 2010
ABSTRACT ChemInform is a weekly Abstracting Service, delivering concise information at a glance t... more ABSTRACT ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Tetrahedron Letters, 1994
Sch 49210, Sch 53514 and Sch 53516 have been isolatedfiom a fungal culture, and identified by ana... more Sch 49210, Sch 53514 and Sch 53516 have been isolatedfiom a fungal culture, and identified by analysis of 20 NMR data Tbo diocetyhtion derivatives Sch SMIS and Sch 53517 have been synthesized These compounds demonstrate inhibitory activity of phospholipase D (PLB), and display potent activity in the antitumor invasion chamber assay.
Tetrahedron Letters, 1997
Journal of Natural Products, 2003
A novel primase inhibitor, Sch 642305 (1), was isolated from the fermentation broth of the fungal... more A novel primase inhibitor, Sch 642305 (1), was isolated from the fermentation broth of the fungal culture Penicillium verrucosum. The structure of 1 was elucidated on the basis of MS and NMR spectroscopic data as a new and unusual bicyclic 10-membered macrolide. The absolute configuration of the asymmetric centers was determined by X-ray crystallographic analysis of the p-bromobenzoate derivative (3). Compound 1 exhibited inhibitory activity against bacterial DNA primase enzyme with an EC(50) of 70 microM.
Journal of Natural Products, 2009
Journal of Natural Products, 2006
Two novel chemokine receptor CCR-5 inhibitors, Sch 210971 (1) and Sch 210972 (2), were isolated f... more Two novel chemokine receptor CCR-5 inhibitors, Sch 210971 (1) and Sch 210972 (2), were isolated from the fungal fermentation broth of Chaetomium globosum by normal- and reversed-phase HPLC purifications. The structure determination of 1 and 2 was accomplished on the basis of UV, MS, and NMR spectral data analyses including COSY, NOESY, HMQC, and HMBC experiments. The structure and relative configuration of 2 were determined unequivocally by X-ray crystallographic analysis. The major component 2 demonstrated a potent inhibitory activity of IC(50) = 79 nM in the CCR-5 receptor in vitro binding assay.
Journal of Natural Products, 1995
The structures of two novel muscarinic receptor antagonists, 1 and 2, were determined by their sp... more The structures of two novel muscarinic receptor antagonists, 1 and 2, were determined by their spectral data and high-resolution mass measurements of their degradation products. Both are aliphatic long-chain compounds and contain amide and keto functionalities. The major microbial metabolite [1] contains three terminal guanidino groups and the minor compound [2] has two terminal guanidino groups.
Journal of Industrial Microbiology & Biotechnology, 2006
Natural product compounds are the source of numerous therapeutic agents. Recent progress to disco... more Natural product compounds are the source of numerous therapeutic agents. Recent progress to discover drugs from natural product sources has resulted in compounds that are being developed to treat cancer, resistant bacteria and viruses and immunosuppressive disorders. Many of these compounds were discovered by applying recent advances in understanding the genetics of secondary metabolism in actinomycetes, exploring the marine environment and applying new screening technologies. In many instances, the discovery of a novel natural product serves as a tool to better understand targets and pathways in the disease process. This review describes recent progress in drug discovery from natural sources including several examples of compounds that inhibit novel drug targets.
Journal of Industrial Microbiology, 1991
Summary Sch 40873, a novel antifungal compound isolated from the fermentation broth of anActinoma... more Summary Sch 40873, a novel antifungal compound isolated from the fermentation broth of anActinomadura spp. was discovered in an assay designed to detect compounds with preferential activity against the invasive mycelial form ofCandida albicans. The geometric mean MIC of Sch 40873 against sevenCandida spp. in Sabouraud dextrose broth (yeast phase) was =58 µg/ml and in Eagles minimum essential medium (mycelial
The Journal of Antibiotics, 2009
The Journal of Antibiotics, 2006
A new hydrogenated azaphilone Sch725680 (1) was isolated and identified from the culture of an As... more A new hydrogenated azaphilone Sch725680 (1) was isolated and identified from the culture of an Aspergillus sp. The structure elucidation of 1 was achieved based on extensive NMR spectroscopic analyses. Compound 1 showed inhibitory activity against Saccharomyces cerevisiae (PM503) and Candida albicans (C43) with MICs of 8 and 64 mg/ml, respectively.
The Journal of Antibiotics, 2006
A new 5-alkenylresorcinol Sch725681 (1) was isolated and identified from the culture of an Asperg... more A new 5-alkenylresorcinol Sch725681 (1) was isolated and identified from the culture of an Aspergillus sp. The structure elucidation of 1 was accomplished based on extensive NMR spectroscopic analyses. Compound 1 showed inhibitory activity against Saccharomyces cerevisiae (PM503) and Candida albicans (C43) with MICs of 16 and 64 mg/ml, respectively.
The Journal of Antibiotics, 2005
A new microbial metabolite Sch 725424 (1) was isolated from the culture of Kitasatospora sp. The ... more A new microbial metabolite Sch 725424 (1) was isolated from the culture of Kitasatospora sp. The structure elucidation of 1 was accomplished based on NMR spectroscopic analyses as well as extensive structure elucidation of its dehydration product Sch 725428 (2). Compound 1 showed inhibitory activity against Staphylococcus aureus with MIC values 1ϳ2 m g/ml, and also displayed weak antifungal activity against Saccharomyces cerevisiae (PM503) with an MIC 32 mg/ml.