ABSTRACT
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.
Subject(s)
Secondary Metabolism , Xestospongia/chemistry , AnimalsABSTRACT
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.
Subject(s)
Antineoplastic Agents/pharmacology , Hydroxamic Acids/pharmacology , Indoles/pharmacology , Lung Neoplasms/drug therapy , Animals , CD13 Antigens/antagonists & inhibitors , CD13 Antigens/metabolism , Cell Line, Tumor , Cell Movement/drug effects , Dose-Response Relationship, Drug , Drug Synergism , Female , Fluorouracil/pharmacology , Inhibitory Concentration 50 , Leucine/analogs & derivatives , Leucine/pharmacology , Lung Neoplasms/secondary , Mice , Tumor Burden/drug effects , Xenograft Model Antitumor AssaysABSTRACT
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.
Subject(s)
Anti-Infective Agents/pharmacology , Antineoplastic Agents/pharmacology , Macrolides/pharmacology , Resorcinols/pharmacology , Animals , Anti-Infective Agents/chemical synthesis , Anti-Infective Agents/isolation & purification , Anti-Infective Agents/metabolism , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/isolation & purification , Antineoplastic Agents/metabolism , Humans , Macrolides/chemical synthesis , Macrolides/isolation & purification , Macrolides/metabolism , Molecular Structure , Resorcinols/chemical synthesis , Resorcinols/isolation & purification , Resorcinols/metabolism , Structure-Activity RelationshipABSTRACT
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.
Subject(s)
Biological Products/pharmacology , Disulfides/pharmacology , Protein Tyrosine Phosphatase, Non-Receptor Type 1/antagonists & inhibitors , Thiosulfonic Acids/chemical synthesis , Thiosulfonic Acids/pharmacology , Biological Products/chemical synthesis , Biological Products/chemistry , Disulfides/chemical synthesis , Disulfides/chemistry , Dose-Response Relationship, Drug , Humans , Models, Molecular , Molecular Structure , Protein Tyrosine Phosphatase, Non-Receptor Type 1/metabolism , Structure-Activity Relationship , Thiosulfonic Acids/chemistryABSTRACT
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.
