• Korean Journal of Pharmacognosy
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• v.33 no.2 s.129
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• pp.144-150
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• 2002

The methanol extracts of 132 herbal medicines were screened for the inhibitory activity against heparinase enzyme from Flavobacterium heparinum. Eleven medicinal plants, Amomum xanthiodides, Agrimonia pilosa, Paeonia lactiflora, Rubia cordifolia, Sanguisorba officinalis, Torrega grandis, Morus alba, Gleditsia sinensis, Crataegus pinnatifida, Cornus officinalis, Paeonia japonica showed potent inhibition on heparinase activity. The active substituents of those herbal medicine could be extracted into butanol fraction and the inhibitory compounds of Morus alba are now isolating.

• Journal of Microbiology and Biotechnology
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• v.30 no.1
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• pp.31-37
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• 2020

We previously identified a new heparinase inhibitor fungal metabolite, named CRM646-A, which showed inhibition of heparinase and telomerase activities in an in vitro enzyme assay and antimetastatic activity in a cell-based assay. In this study, we elucidated the mechanism by which CRM646-A rapidly induced nucleus condensation, plasma membrane disruption and morphological changes by increasing intracellular Ca²⁺ levels. Furthermore, PD98059, a mitogen-activated protein kinase (MEK) inhibitor, inhibited CRM646-A-induced nucleus condensation through ERK1/2 activation in rat 3Y1 fibroblast cells. We identified CRM646-A as a Ca²⁺ ionophore-like agent with a distinctly different chemical structure from that of previously reported Ca²⁺ ionophores. These results indicate that CRM646-A has the potential to be used as a new and effective antimetastatic drug.