Marine natural products as inhibitors of cystathionine beta-synthase activity

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Abstract

A library consisting of characterized marine natural products as well as synthetic derivatives was screened for compounds capable of inhibiting the production of hydrogen sulfide (H2S) by cystathionine beta-synthase (CBS). Eight hits were validated and shown to inhibit CBS activity with IC50 values ranging from 83 to 187 μM. The majority of hits came from a series of synthetic polyandrocarpamine derivatives. In addition, a modified fluorogenic probe for H2S detection with improved solubility in aqueous solutions is reported.

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Acknowledgements

This work was supported by the American Heart Association grant 11GRNT7530023 to A.M.B. and award CA36622 from the National Institutes of Health to C.M.I.

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