Background:
Marine sponges provided a great source of natural products with promising
biological activity. This study was aimed to investigate the chemical constituents of methanol extracts
of selected Indonesian marine sponges (Callyspongia sp., Clathria sp., Melophlus sarasinorum,
and Xestospongia sp.), collected from the Saponda Islands, Southeast Sulawesi, Indonesia as
well as to evaluate their antimicrobial and antioxidant activities.
Methods:
LCMS/MS analysis used to identify the compounds. Agar well diffusion and DPPH
assays were used to evaluate the antimicrobial and antioxidant activities.
Results:
Chemical screening reported alkaloids, terpenoids, steroids, and saponins from all investigated
sponges. The LC-MS/MS analysis identified various compounds which mainly contained steroids.
Antimicrobial activity (against Bacillus subtilis, Escherichia coli, Salmonella enterica, and
Candida albicans) was only shown by the Xestospongia sp. extract. Meanwhile, extracts of M.
sarasinorum, Xestospongia sp., and Callyspongia sp. exhibited potent radical scavenging activity.
Conclusion:
The study concluded that the selected sponges could provide various groups of
compounds. Methanol extracts of these sponges could be used as sources of antimicrobial and
antioxidant agents.
Two geranylated and methylated flavonol derivatives, macarhizinoidins A (1) and B (2), along with a known phenolic compound methyl 4-isoprenyloxycinnamate (3), have been isolated from the methanol extract of the leaves M. rhizinoides. The structures of these compounds were identified based on their spectroscopic data. On cytotoxic evaluation against murine leukemia P-388 cells, compounds 1-2 showed IC 50 values of 11.4 and 13.9 μM, respectively, while compound 3 was inactive.
The antidiabetic activity test through a mechanism of inhibition of α-glucosidase enzyme was studied against ethanol, n-hexane, ethyl acetate and n-butanol fractions of ethanol extract of Artocarpus altilis (Parkinson) Fosberg (Moraceae) leaves and four flavonoid compounds isolated from ethyl acetate extracts of A. altilis. Ethyl acetate fraction has strongest antidiabetic activity compared to ethanol, n-hexane, and n-butanol fractions with IC50values5.98,6.79, 440.18and14.42μg/mL, respectively. Four flavonoid compounds (1-(2,4-dihydroxyphenyl)-3-[8-hydroxy-2-methyl-2-(4-methyl-3-pentenyl)-2H-1-benzopyran-5-yl]-1-propanone (AC-31), 2-geranyl-2',3,4,4'-tetrahydroxy dihydrochalcone (AC-51), 8-geranyl-4',5,7-trihydroxyflavone (AC-33) andcyclocommunol (AA-3), have been isolated from ethylacetate fraction. AC-31 was the strongest antidiabetic compound compared to AC-51, AC-33 and cyclocommunolwithIC50values are 15.73, 24.41,49.49,and72.20μg/mL. Kineticstudies of AC-31 using Lineweaver-Burk method showed that inhibition mechanism of enzymeα-glucosidase was anon-competitivetype.
Myristica fatua Houtt. is one of the endemic plants growth in Wallace region. Isolation of the secondary metabolite compounds from the ethyl acetate fraction of the bark of Myristica fatua Houtt. has been done using some chromatography techniques afforded two resorcinol compounds, malabaricone C (1), and malabaricone B (2). The structures of 1-2 were determined using spectroscopic techniques, including mass spectrometry, 1D-NMR and 2D-NMR. Both compounds showed in vitro cytotoxic activity against the breast carcinoma cancer cell lines MCF-7 using alamar blue assay method, with IC 50 of 2.38 and 0.71 μg/mL, respectively.
Use of α-glucosidase inhibitorsis one of the therapeutic approaches for decreasing postprandial hyperglycemia. Sulochrin (1) from Aspergillus terreus as well as two synthetic sulochrin derivatives were assessed for antidiabetic activity against yeast and rat intestine α-glucosidase. Sulochrin showed potential inhibition against yeast α-glucosidase, through a non-competitive mode with an IC 50 value of 133.79 µM, and rat intestine α-glucosidase by uncompetitive mode with an IC 50 value of 144.59 µM.. Two synthetic derivatives of sulochrin were also prepared by bromination which resulted in dibromosulochrin (2) and tribromo-sulochrin (3). Preliminary SAR studies of sulochrin derivatives revealed that the yeast α-glucosidase inhibitory activity of compound 2 and 3 increased than 1 due to substitution of hydrogen atom with bromine with IC 50 values of 122.65 and 49.08 µM, respectively. However, the inhibitory activity against rat intestine α-glucosidase of 2 and 3 was decreased compared to 1. To the best our knowledge, this is the first report of structure-activity relationship of sulochrin and its derivatives as α-glucosidase inhibitors. These results suggested that sulochrin can potentially be used as a lead compound to develop new α-glucosidase inhibitor from microorganisms.
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