BackgroundThe pimprinine family of compounds represent very important and promising microbial metabolites for drug discovery. However, their ability in inhibiting viral infections has not yet been tested.MethodsThe antiviral activity of the pimprinine family of compounds was evaluated by determining the cytopathic effect (CPE), cell viability or plaque-forming unit (PFU), and virus yield. The mechanism of action against EV71 was determined from the virucidal activity, and effective stage and time-of-addition assays. The effects on EV71 replication were evaluated further by determining viral RNA synthesis, protein expression and cells apoptosis using the SYBR Green assays, immunofluorescence assays and flow cytometric assays, respectively.ResultsPimprinethine, WS-30581 A and WS-30581 B inhibited EV71-induced CPE, reduced progeny EV71 yields, as well as prevented EV71-induced apoptosis in human rhabdomyosarcoma (RD) cells. These compounds were found to target the early stages of the EV71 replication in cells including viral RNA replication and protein synthesis. They also showed antiviral activity against ADV-7, and were slightly active against CVB3, HSV-1 and H1N1 with a few exceptions. Pimprinine was slightly active or inactive against all the viruses tested. The mechanisms by which these compounds act against the viruses tested may be similar to that demonstrated for EV71.ConclusionThe data described herein demonstrate that the pimprinine family of compounds are inhibitors effective against the replication of EV71 and ADV-7, so they might be feasible therapeutic agents for the treatment of viral infections.
Two new 32-membered macrolide compounds, named Novonestmycins A (1) and B (2), were isolated from the soil strain Streptomyces phytohabitans HBERC-20821. Their structures were elucidated by using spectroscopic methods, including 1D, 2D-NMR and MS spectrometry. The two compounds showed strong activities against the phytophathogenic fungi Corynespora cassiicola, Rhizoctonia solani and Septoria nodorum, with MIC values of 0.78, 0.39 and 0.78 μg ml(-1), respectively. In addition, the two compounds exhibited potent inhibitory activities against four different human tumor cell lines as well as one 5-FU-resistant human hepatocellular carcinoma cell line, with IC50 of 0.15-0.48 μg ml(-1) and 0.24-1.34 μg ml(-1), respectively.
Weeds had caused significant loss for crop production
in the process
of agriculture. Herbicides have played an important role in securing
crop production. However, the high reliance on herbicides has led
to environmental issues as well as the evolution of herbicide resistance.
Thus, there is an urgent need for new herbicides with safer toxicological
profiles and novel modes of action. Actinomycetes produce very diverse
bioactive compounds, of which some show potent biopesticidal activity.
The herbicidal secondary metabolites from actinomycetes can be classified
into several groups, such as amino acids, peptides, nucleosides, macrolides,
lactones, amide, amines, etc., some of which have been successfully
developed as commercial herbicides. The structure diversity and evolved
biological activity of secondary metabolites from actinomycetes can
offer opportunities for the development of both directly used bioherbicides
and synthetic herbicides with new target sites, and thus, this review
focuses on the structure, herbicidal activity, and modes of action
of secondary metabolites from actinomycetes.
Steroids are classes of natural products widely distributed in nature, which have been demonstrated to exhibit broad biological functions, and have also attracted increasing interest from bioorganic and pharmaceutical researches. In order to develop novel chemical entities as potential cytotoxic agents, a series of steroidal isatin conjugations derived from epiandrosterone and androsterone were efficiently prepared and characterized, and all these obtained compounds were screened for their potential cytotoxic activities. The preliminary bioassay indicated that most of the newly synthesized compounds exhibited good cytotoxic activities against human gastric cancer (SGC-7901), melanoma (A875), and hepatocellular liver carcinoma (HepG2) cell lines compared with 5-fluorouracil (5-FU), which might be considered as promising scaffold for further development of potential anticancer agents.
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