A growing body of evidence indicates that glycosylated natural products have become vital platforms for the development of many existing first-line drugs. This review covers 205 new glycosides over the last 22 years (1997–2018), from marine microbes, including bacteria, cyanobacteria, and fungi. Herein, we discuss the structures and biological activities of these compounds, as well as the details of their source organisms.

Eight new compounds, sinulolides A–H (1–8), along with two known compounds, α-methoxy-2,3-dimethyl-butenolide (9) and sinularone D (10), were isolated from the soft coral Sinularia sp. The structures of these compounds were elucidated on the basis of extensive spectroscopic analysis. The absolute configurations were determined on the basis of electronic circular dichroism (ECD) data analysis. Compounds 5 and 10 exhibited moderate effects for the inhibition of NF-κB activation.

A new macrodiolide, mangrovlide A (1) and two new polycyclic chromones, penixanthones C (2) and D (3), as well as four other known compounds (4–7), have been isolated from the mangrove sediment derived fungus Penicillium sp. SCSIO041218, cultured in the 0.25% NaCl rice substrate. The structures of the new compounds were determined by analysis of the NMR and MS spectroscopic data. Compound 1 possesses a 10-membered macrodiolide unit, while 2 and 3 are chromones with an unprecedented 6/6/6/5 polycyclic skeleton. Compounds 1–7 were evaluated for their cytotoxicities, while all the compounds displayed weak or no activity.

Butyrolactone I (BTL-I), a butenolide compound isolated from land or marine-derived fungi, has been reported to show diverse activities. To further study the pharmaceutical potential of BTL-I, transcriptome and bioinformatics analysis of BTL-I treated HepG2 cells were taken. BTL-I was revealed with lipid metabolism regulatory activity and confirmed by increasing the mRNA expression of related genes, such as LXRα and its target gene UGT1A1. However, the obvious chemical carcinogenesis of BTL-I was also disclosed. BTL-I could significantly increase the mRNA and protein levels of oncogenes such as CYP1A1. Molecular docking of BTL-I and its analogs were performed to understand the active or toxic effects. Although BTL-I showed attractive activities, enough attention must be paid to its adverse effects in its further development. Graphical Abstract