Francis, Prima and Chakraborty, Kajal (2022) Clathrolides A–B: previously undescribed macrocylic lactones from marine demosponge Clathria (Thalysias) vulpina (Lamarck, 1814) as potential antihypertensive leads attenuating angiotensin converting enzyme. Medicinal Chemistry Research, 30. pp. 1438-1451.
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Abstract
Biochemical investigation of bioactive compounds from the marine demospongiae Clathria (Thalysias) vulpina (Lamarck, 1814) (family Microcionidae) resulted in the isolation of two previously undescribed 22-membered macrocyclic lactone derivatives clathrolide A and B from its organic extract. Structural elucidation of the compounds were carried out using spectroscopic analysis. Clathrolide A exhibited greater antihypertensive (IC50 0.44 ± 0.02 mM), anti-inflammatory (IC50 0.74 ± 0.04 mM), anti-hyperglycemic (IC50 0.85 ± 0.01 mM), and antioxidant (IC50 0.70 ± 0.03 mM) activities compared to clathrolide B. Among various bioactivities, such as antihypertensive, anti-inflammatory, anti-hyperglycemic, and antioxidant properties, angiotensin converting enzyme attenuation potential of clathrolide A was found to be significantly greater, and comparable with the standard antihypertensive drug, captopril (IC50 0.36 ± 0.03 mM). Higher electronic properties (topological polar surface area 133.52) along with comparatively lesser docking score and binding energy of clathrolide A with the aminoacyl residues of angiotensin-I converting enzyme (−12.38 and −12.91 kcal/mol, respectively) recognized its prospective inhibitory property against the enzyme catalyzing the rate-limiting step to form the vasoconstrictor angiotensin-II
Item Type: | Article |
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Uncontrolled Keywords: | Clathria (Thalysias) vulpina (Lamarck, 1814) ; Clathrolides A–B ; 22-membered macrocyclic lactones ● Angiotensin-I converting enzyme ; In silico molecular docking |
Subjects: | Biochemistry > Bioactive compounds Biochemistry Fish Biotechnology |
Divisions: | CMFRI-Kochi > Marine Biotechnology, Fish Nutrition and Health Division Subject Area > CMFRI > CMFRI-Kochi > Marine Biotechnology, Fish Nutrition and Health Division CMFRI-Kochi > Marine Biotechnology, Fish Nutrition and Health Division Subject Area > CMFRI-Kochi > Marine Biotechnology, Fish Nutrition and Health Division |
Depositing User: | Arun Surendran |
Date Deposited: | 09 Sep 2021 09:07 |
Last Modified: | 26 Dec 2023 11:20 |
URI: | http://eprints.cmfri.org.in/id/eprint/13545 |
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