Clathriolide from marine demosponge Clathria (Thalysias) vulpina (Lamarck, 1814): previously undescribed macrocylic lactone with attenuating potential against angiotensin converting enzyme
2022
Chakraborty, Kajal | Francis, Prima
Angiotensin-I converting enzyme catalyses the rate-determined step of the conversion of angiotensin-I to angiotensin-II that narrows the blood vessels, and angiotensin-I converting enzyme inhibitors were recognised as important medications for hypertension-related diseases. Chemical investigation of angiotensin-I converting enzyme inhibitors from marine demospongiae Clathria (Thalysias) vulpina (family Microcionidae), resulted in a previously undescribed 22-membered macrocyclic lactone derivative, named as clathriolide. The studied compound showed potential angiotensin converting enzyme attenuation property (IC₅₀ 0.41 mM), which was comparable with the standard captopril (IC₅₀ 0.36 mM). Clathriolide revealed significantly greater antioxidant potentials against free radical species (IC₅₀ < 1 mM) in comparison with the standard α-tocopherol (IC₅₀ > 1.5 mM). Superior electronic characteristics (topological polar surface area > 100) coupled with relatively smaller binding energy and docking score of clathriolide with the aminoacyl residues of angiotensin-I converting enzyme (–11.5 and –12.2 kcal/mol, respectively) described its potential inhibitory property against angiotensin-I converting enzyme.
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