Applications of mass spectrometry in structural studies of bioactive compounds

doi:10.1098/rsta.1979.0075

Applications of mass spectrometry in structural studies of bioactive compounds

Philosophical Transactions of the Royal Society of London. Series A, Mathematical and Physical Sciences ◽

10.1098/rsta.1979.0075 ◽

1979 ◽

Vol 293 (1400) ◽

pp. 3-11

Keyword(s):

Mass Spectrometry ◽

Cell Proliferation ◽

Tissue Culture ◽

Nucleic Acids ◽

Bioactive Compounds ◽

Rat Liver ◽

Structural Studies

The paper describes the role played by mass spectrometry in structural studies of molluscicidal saponins from a plant; the adducts formed between 7,12-dimethylbenz[a]anthracene and nucleic acids upon tissue culture with rat liver; and the G2 factor, the first natural mitotic hormone that regulates cell proliferation.

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PROTECTIVE EFFECT OF POLYPEPTIDE AND AMINO ACIDS ON THE DEVELOPMENT OF THE NERVOUS TISSUE CULTURE IN THE PRESENCE OF CYCLOPHOSPHAMIDE

Токсикологический вестник ◽

10.36946/0869-7922-2017-2-22-26 ◽

2017 ◽

pp. 22-26

Author(s):

V. B. Dolgo-Saburov ◽

N. I. Chalisova ◽

L. V. Lyanginen ◽

E. S. Zalomaeva

Keyword(s):

Amino Acids ◽

Cell Proliferation ◽

Tissue Culture ◽

Protective Effect ◽

Organotypic Culture ◽

Inhibitory Effect ◽

Mustard Gas ◽

Synthesis Inhibitor ◽

Combined Administration ◽

The Central Nervous System

In an organotypic culture, an investigation was conducted into combined effects of cyclophosphamide DNA as synthesis inhibitor used to model a resorptive action of mustard gas, and cortexin polypeptide or each of 20 encoded amino acids on the development of cell proliferation in cerebral cortex explants of the rat. The combined administration of cyclophosphamide together with cortexin or with each of the 20 encoded amino acids, except glycine, showed suppression of the cytostatic agent inhibitory effect. Thus, cortexin and amino acids have a protective effect on cell proliferation in the tissue culture of the central nervous system under the action of mustardlike substances.

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Mass spectrometry‐based metabolomics unravel the transfer of bioactive compounds between rye and neighboring plants

Plant Cell & Environment ◽

10.1111/pce.14159 ◽

2021 ◽

Author(s):

Hossein Hazrati ◽

Inge S Fomsgaard ◽

Ling Ding ◽

Per Kudsk

Keyword(s):

Mass Spectrometry ◽

Bioactive Compounds

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A New Anti-Estrogen Discovery Platform Identifies FDA-Approved Imidazole Anti-Fungal Drugs as Bioactive Compounds against ERα Expressing Breast Cancer Cells

International Journal of Molecular Sciences ◽

10.3390/ijms22062915 ◽

2021 ◽

Vol 22 (6) ◽

pp. 2915

Author(s):

Manuela Cipolletti ◽

Stefania Bartoloni ◽

Claudia Busonero ◽

Martina Parente ◽

Stefano Leone ◽

...

Keyword(s):

Cell Proliferation ◽

Bioactive Compounds ◽

Estrogenic Activity ◽

Estrogen Receptor Α ◽

Breast Cancers ◽

Cellular Models ◽

Cancer Models ◽

17Β Estradiol ◽

Approved Drugs ◽

Anti Fungal

17β-estradiol (E2) exerts its physiological effects through the estrogen receptor α (i.e., ERα). The E2:ERα signaling allows the regulation of cell proliferation. Indeed, E2 sustains the progression of ERα positive (ERα+) breast cancers (BCs). The presence of ERα at the BC diagnosis drives their therapeutic treatment with the endocrine therapy (ET), which restrains BC progression. Nonetheless, many patients develop metastatic BCs (MBC) for which a treatment is not available. Consequently, the actual challenge is to complement the drugs available to fight ERα+ primary and MBC. Here we exploited a novel anti-estrogen discovery platform to identify new Food and Drug Administration (FDA)-approved drugs inhibiting E2:ERα signaling to cell proliferation in cellular models of primary and MBC cells. We report that the anti-fungal drugs clotrimazole (Clo) and fenticonazole (Fenti) induce ERα degradation and prevent ERα transcriptional signaling and proliferation in cells modeling primary and metastatic BC. The anti-proliferative effects of Clo and Fenti occur also in 3D cancer models (i.e., tumor spheroids) and in a synergic manner with the CDK4/CDK6 inhibitors palbociclib and abemaciclib. Therefore, Clo and Fenti behave as “anti-estrogens”-like drugs. Remarkably, the present “anti-estrogen” discovery platform represents a valuable method to rapidly identify bioactive compounds with anti-estrogenic activity.

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