Marine-derived antidiabetic compounds: an insight into their sources, chemistry, SAR, and molecular mechanisms

Natural Bioactive Compounds from Marine Invertebrates That Modulate Key Targets Implicated in the Onset of Type 2 Diabetes Mellitus (T2DM) and Its Complications

“…Although the marine world is evolving as a remarkable source of antidiabetic agents, so far, the therapeutic benefits in the context of T2DM have been demonstrated in vivo for Although the marine world is evolving as a remarkable source of antidiabetic agents, so far, the therapeutic benefits in the context of T2DM have been demonstrated in vivo for a limited number of compounds. Among these, most are compounds derived from macroalgae, such as fucosterol and phlorotannins, or algal extracts, which are natural matrices that are already known as valuable nutraceuticals [139]. Among the invertebrate-derived bioactive compounds with antidiabetic potential, the most advanced compound is the PTP1B inhibitor dysidine (2), which is currently in preclinical trials for the treatment of diabetes [140].…”

“…There are few examples of marine metabolites from invertebrates that express inhibitory activity against α-amylase. The bioassay0guided fractionation of the Mediterranean Sea sponge Hemimycale collumella led to the identification of a series of bioactive compounds: In particular, the glycosides 2,3-O-hexahydroxydiphenoyl-(α/β)-glucose (137) and gentisic acid 2-O-β-glucoside (138) were isolated from the water extract; quercetin-3-O-β-glucopyranoside (139), kaempferol 3-O-β-glucopyranoside (140), and isorhamnetin 3-O-β-glucopyranoside (141) were isolated from the butanol soluble material; gallic acid (142) was isolated from an ethyl acetate extract, and gallic acid-3-methyl ether (143) was isolated from a dichloromethane fraction (Figure 29). All of the isolated compounds (137)(138)(139)(140)(141)(142)(143) were tested against the α-amylase enzyme at 600 µg/mL, and all of them exerted a strong inhibition.…”

“…The bioassay0guided fractionation of the Mediterranean Sea sponge Hemimycale collumella led to the identification of a series of bioactive compounds: In particular, the glycosides 2,3-O-hexahydroxydiphenoyl-(α/β)-glucose (137) and gentisic acid 2-O-β-glucoside (138) were isolated from the water extract; quercetin-3-O-β-glucopyranoside (139), kaempferol 3-O-β-glucopyranoside (140), and isorhamnetin 3-O-β-glucopyranoside (141) were isolated from the butanol soluble material; gallic acid (142) was isolated from an ethyl acetate extract, and gallic acid-3-methyl ether (143) was isolated from a dichloromethane fraction (Figure 29). All of the isolated compounds (137)(138)(139)(140)(141)(142)(143) were tested against the α-amylase enzyme at 600 µg/mL, and all of them exerted a strong inhibition. Indeed, compound 141 was the most active in the series, with a percent of inhibition of 25.3 ± 5.8, followed by compound 139 with 32.4 ± 6.5, compound 143 (52.0 ± 8.7), compound 140 (59.2 ± 5.4), compound 138 (72.4 ± 6.2), gallic acid (76.2 ± 5.9) and, at last, compound 137, with a percent of inhibition of 80 ± 5.1 [98].…”

Metabolites extracted from microorganisms as potential inhibitors of glycosidases (α-glucosidase and α-amylase): A review

“…The marine environment has not been fully explored, and metabolites of marine microbial origins have a more important role in drug discovery ( Pathak et al, 2022 ). These natural products from marine microorganisms have various bioactivities, such as anti-bacterial ( Yang et al, 2018 ), anti-fungal ( Sangkanu et al, 2021 ), anti-viral ( Richard et al, 2018 ), anti-parasitic ( Santos et al, 2019 ), anti-tumor ( Yan et al, 2020 ), and anti-diabetic properties ( Elaiyaraja et al, 2018 ).…”