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The amylase inhibitor montbretin A reveals a new glycosidase inhibition motif.
TLDR
X-ray structural analyses of the montbretin A-human α-amylase complex confirmed the importance of this core structure and revealed a novel mode of glycosidase inhibition wherein internal π-stacking interactions between the myricetin and caffeic acid organize their ring hydroxyls for optimal hydrogen bonding to the α- amylase catalytic residues D197 and E233.
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Synthesis and antimitotic/cytotoxic activity of hemiasterlin analogues.
TLDR
The antimitotic sponge tripeptide hemiasterlin and a number of structural analogues have been synthesized and evaluated in cell-based assays in order to explore the SAR for this promising anticancer drug lead.
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Cytotoxic peptides from the marine sponge Cymbastela sp.
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Glucose lowering effect of montbretin A in Zucker Diabetic Fatty rats
TLDR
Chronic oral administration of montbretin A was an effective glucose-lowering agent in the treatment of type 2 diabetes and improved the oxidative status of the fatty diabetic animals as well as attenuated markers for increased risk of cardiovascular complications associated with diabetes.
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Cytotoxic peptides hemiasterlin, hemiasterlin A and hemiasterlin B induce mitotic arrest and abnormal spindle formation
TLDR
The hemiasterlins probably exert their cytotoxic effect by inhibiting spindle microtubule dynamics, and are likely to have potential as antitumor drugs.
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New terpenoid metabolites from the skin extracts, an egg mass, and dietary sponges of the Northeastern Pacific dorid nudibranch Cadlinaluteomarginata
Chemical investigations of Cadlinaluteomarginata skin extracts, egg masses, and dietary sponges have led to the identification of the novel terpenoids cadlinaldehyde (30), spongian 32, seco-spongian…
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Total synthesis of (−)-hemiasterlin, a structurally novel tripeptide that exhibits potent cytotoxic activity
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Hemiasterlin methyl ester
The structure of the tripeptide hemiasterlin methyl ester, IUPAC name: methyl 2,5-dimethyl-4-{2-[3-methyl-2-methyl­amino-3-(N-methyl­benzo[b]pyrrol-3-…
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Total Synthesis of (-)-Hemiasterlin, a Structurally Novel Tripeptide That Exhibits Potent Cytotoxic Activity.
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New Terpenoid Metabolites from the Skin Extracts, an Egg Mass, and Dietary Sponges of the Northeastern Pacific Dorid Nudibranch Cadlina luteomarginata.
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