Recent progress regarding the bioactivities, biosynthesis and synthesis of naturally occurring resorcinolic macrolides.

Macrolides, which comprise a family of lactones with different ring sizes, belong to the polyketide class of natural products. Resorcinolic macrolides, an important subgroup, possess interesting structures and exhibit a wide variety of bioactivities, such as anti-tumor, anti-bacteria, and anti-malaria activities, etc. This review summarizes progress in isolation, bioactivity studies, biosynthesis, and representative chemical syntheses of this group of macrolides in recent decades, encompassing 63 naturally occurring macrolides published in 120 articles.

[Review on the secondary metabolites from Xestospongia sponges and their bioactivities].

The genus Xestospongia is one of the most widespread genera of sponges, containing abundant secondary metatolites with novel structures and potent bioactivities. The main structure types of secondary metatolites found in this genus are alkaloids, quinines, terpens, steroids, lipids, polyketones, etc. These metatolites exhibit a variety of bioactivities, such as cytotoxic, antibacterial and antiviral activities. This paper reviews the progress in the chemistry and pharmacological activities of the second metabolities from sponges of Xestospongia, especially for recent five years, with the aim for further research.

The first synthesis of natural disulfide bruguiesulfurol and biological evaluation of its derivatives as a novel scaffold for PTP1B inhibitors.

Bruguiesulfurol (1), a cyclic 4-hydroxy-dithiosulfonate isolated from mangrove plant Bruguiera gymnorrhiza, was concisely synthesized for the first time in four steps, and a series of its synthetic derivatives were evaluated for in vitro inhibitory effects on PTP1B and related PTPs. Some derivatives were found to have improved pharmacological profile compared with hit 1. Among them, 5a showed the potent selectivity towards PTP1B over other PTPs, including TCPTP, and 7j exhibited the strongest PTP1B inhibitory activity with an IC50 value of 4.54 µM.

The research progress of quantum dot lasers and photodetectors in China.

Self-assembled In(Ga)As/GaAs quantum dots (QDs), known as "artificial atoms" for their fully quantized electronic states, show unique physical properties and new prospects for applications. Based on the QDs, an increasing number of leading laboratories on the world engage in developing novel optoelectronic devices with special advantages over existing devices. This paper reviews the current research developments in self-assembled QD devices in China, covering QD lasers and inter sub-level QD photodetectors. QD devices in China are undergoing a rapid advance and have achieved the world's best results in terms of certain characteristics.

Preliminary detection of the anti­tumour activity of indoline­2,3­dione derivative DH­12a targeting aminopeptidase N.

Aminopeptidase N (APN) is important in tumour processes. The present study detected the anti­tumour activity of the novel APN inhibitor DH­12a, which is an indoline­2,3­dione derivative. In the present study, Bestatin, a clinical APN inhibitor was used as a positive control. The expression of APN in the ES-2 and 3AO cell lines were assessed using flow cytometry and the drug inhibition constants of DH­12a (Ki=13.15 µM) and Bestatin (Ki=16.57 µM) were assessed using a double reciprocal method of competitive inhibition. The in vitro effects of DH­12a on cell proliferation were assessed using a 3­(4,5­dimethyl­thiazol­2­yl)­2,5­diphenyl tetrazolium bromide assay on human cell lines of ES­2 (IC50=43.8 µM), A549 (inhibition rate=41.5% at 160 µM DH­12a), HL60 (inhibition rate=47.83% at 160 µM DH­12a) and 3AO (IC50=70.2 µM). The inhibition rates were consistently higher than those of Bestatin. The effects of DH­12a on cell migration (inhibition rates in ES­2 cells and 3AO cells were 56.4 and 76.5%, respectively at 15 µM) and invasion (inhibition rates in ES­2 cells and 3AO cells were 75.6 and 66.5%, respectively at 15 µM) were assessed using transwell plates. The in vivo effects of DH­12a on tumour proliferation and lung tumour metastasis were determined using an H22 xenograft mice model, where DH­12a was administered in combination with genotoxic 5­fluorouracil. The anti­tumour activities of DH­12a in vivo were also greater than those of Bestatin. In conclusion, the in vitro effects of DH­12a on tumour proliferation, migration and invasion were consistent with the in vivo effects. In addition, DH­12a exhibited greater anti­tumour properties compared with Bestatin.