Callypyrones from marine Callyspongiidae sponge Callyspongia diffusa: antihypertensive bis-c-pyrone polypropionates attenuate angiotensin-converting enzyme
CMFRI Repository
View Archive InfoField | Value | |
Relation |
http://eprints.cmfri.org.in/15394/
https://www.tandfonline.com/doi/abs/10.1080/14786419.2020.1837819?journalCode=gnpl20 10.1080/14786419.2020.1837819 |
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Title |
Callypyrones from marine Callyspongiidae sponge Callyspongia diffusa: antihypertensive bis-c-pyrone polypropionates attenuate angiotensin-converting enzyme |
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Creator |
Chakraborty, Kajal
Francis, Prima |
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Subject |
Bioactive compounds
Biochemical composition Biochemistry |
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Description |
Angiotensin I-converting enzyme (ACE) catalyses the biosynthesis of angiotensin II, a potent blood vessel constrictor, from angiotensin I, and ACE inhibitors were recognised as medications for hypertension. Undescribed bis-c-pyrone polypropionate compounds, callypyrones A and B were purified from the organic extract of Callyspongiidae sponge species Callyspongia diffusa by repeated chromatographic purification. Callypyrone A exhibited significantly greater attenuation potential against ACE (IC50 0.48 mM) than that displayed by callypyrone B (IC50 0.57 mM) and showed comparable activity with standard ACE inhibitor captopril (IC50 0.36 mM). Higher electronic parameters of callypyrone A (topological surface area of 108.36) combined with balanced hydrophilic-lipophilic parameter (octanol–water coefficient, log Pow 1.9), as deduced from the structure–activity relationship analyses, could further indicate the improved ligand–receptor interactions resulting in its prospective ACE inhibitory activity. In silico docking analyses of the callypyrones with ACE recorded lowest binding energy (–12.58 kcal mol-1 ) for callypyrone A, which further supported the antihypertensive potential of the compound |
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Publisher |
Taylor and Francis
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Date |
2020
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Type |
Article
PeerReviewed |
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Format |
text
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Language |
en
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Identifier |
http://eprints.cmfri.org.in/15394/1/Natural%20product%20research_2020_Kajal%20Chakraborty_Callypyrones.pdf
Chakraborty, Kajal and Francis, Prima (2020) Callypyrones from marine Callyspongiidae sponge Callyspongia diffusa: antihypertensive bis-c-pyrone polypropionates attenuate angiotensin-converting enzyme. Natural Product Research. pp. 1-12. |
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