Difference in microbial community and taste compounds between Mucor-type and Aspergillus-type Douchi during koji-making.

Douchi has attracted people's attention because of its unique taste and rich health function. The microbes participated in the koji-making process contribute to taste compounds of Douchi. However, the majority of studies on Douchi focused on their functional components and the microbial community in single type of Douchi during koji-making so far.

Total Synthesis of Mycalisine B.

The first total synthesis of the marine nucleoside Mycalisine B-a naturally occurring and structurally distinct 4,5-unsaturated 7-deazapurine nucleoside-has been accomplished in 10 linear steps with 27.5% overall yield from commercially available 1,2,3,5-tetra--acetyl-ribose and tetracyanoethylene. Key steps of the approach include: (1) I catalyzed acetonide formation from 1,2,3,5-tetra--acetylribose and acetone at large scale; (2) Vorbrüggen glycosylation using -benzoyl-5-cyano-6-bromo-7-pyrrolo[2,3-]pyrimidine as a nucleobase to avoid formation of -3 isomer; (3) mild and scalable reaction conditions.

Functional Genomics of : Strategies and Progress.

has been used for the production of traditional fermentation and has promising potential to produce primary and secondary metabolites. Due to the tough cell walls and high drug resistance of , functional genomic characterization studies are relatively limited. The exploitation of selection markers and genetic transformation methods are critical for improving fermentative strains.

Highly fluorescent triazolopyridine-thiophene D-A-D oligomers for efficient pH sensing both in solution and in the solid state.

Conjugated fluorophores have been extensively used for fluorescence sensing of various substances in the field of life processes and environmental science, due to their noninvasiveness, sensitivity, simplicity and rapidity. Most existing conjugated fluorophores exhibit excellent light-emitting performance in dilute solutions, but their properties substantially decrease or even completely vanish due to severe aggregation quenching in the solid state. Herein, we synthesize a series of triazolopyridine-thiophene donor-acceptor-donor (D-A-D) type conjugated molecules with high absolute fluorescence quantum yields (ΦF) ranging from 80% to 89% in solution.

Edible fungi-assisted harvesting system for efficient microalgae bio-flocculation.

Conventional flocculants, commonly used to improve harvesting efficiency, can contaminate the broth and cause microalgae not suitable for food or feed production. In the present study, Pleurotus ostreatus, an edible fungal strain, was developed to improve the harvesting efficiency of microalgae. The results show that Pleurotus ostreatus pellets cultured under 100 rpm agitation resulted in higher harvesting efficiency than pellets cultured under 0 rpm and 150 rpm agitation.

Heterologous expression and functional characterization of the ligand-binding domain of oxysterol-binding protein from Aspergillus oryzae.

Oxysterol-binding proteins (OSBPs) comprise a family of sterol-binding proteins. In this study, we focused on AoOSBP1, one of the five OSBP proteins identified from the industrial fungus Aspergillus oryzae. The temporal expression pattern analysis showed that the expression of AoOSBP1, in both gene and protein levels, was stably expressed throughout the developmental stages, while was upregulated during the accelerated growth stage.

Design, synthesis and biological evaluation of novel 4-anlinoquinazoline derivatives as EGFR inhibitors with the potential to inhibit the gefitinib-resistant nonsmall cell lung cancers.

A series of quinazoline derivatives with benzylidene hydrazine carboxamide were designed and synthesised as EGFR inhibitors. Most compounds exhibited exceptional anti-proliferative activity against A549, HepG2, MCF-7 and H1975 cells. Furthermore, six compounds demonstrated excellent inhibition activity against EGFR with the IC value both less than 2 nM.

An Expeditious Total Synthesis of 5'-Deoxy-toyocamycin and 5'-Deoxysangivamycin.

In present paper, an expeditious total synthesis of naturally occurring 5'-deoxytoyocamycin and 5'-deoxysangivamycin was accomplished. Because of the introduction of a benzoyl group at -6 of 4-amino-5-cyano-6-bromo-pyrrolo[2,3-]pyrimidine, a Vorbrüggen glycosylation with 1,2,3-tri--acetyl-5-deoxy-β-D-ribofuranose afforded a completely regioselective -9 glycosylation product, which is unambiguously confirmed by X-ray diffraction analysis. All of the involved intermediates were well characterized by various spectra.

Dissecting the Role of Juvenile Hormone Binding Protein in Response to Hormone and Starvation in the Cotton Bollworm, Helicoverpa armigera (Hübner) (Lepidoptera: Noctuidae).

Juvenile hormone (JH) regulates many physiological processes in insect development, diapause, and reproduction. Juvenile hormone binding protein (JHBP), the carrier partner protein of JH, is essential for the balance of JH titer to regulate the metamorphosis and development of insect. In this study, two JHBP genes were identified from Helicoverpa armigera (Hübner) (Lepidoptera: Noctuidae), namely HaJHBP1 and HaJHBP2.

Gene transcription profiling of Aspergillus oryzae 3.042 treated with ergosterol biosynthesis inhibitors.

Ergosterol, a unique component of fungal cells, is not only important for fungal growth and stress responses but also holds great economic value. Limited studies have been performed on ergosterol biosynthesis in Aspergillus oryzae, a safe filamentous fungus that has been used for the manufacture of oriental fermented foods. This study revealed that the ergosterol biosynthesis pathway is conserved between Saccharomyces cerevisiae and A.

A Dual Selection Marker Transformation System Using for the Industrial 3.042.

Currently, the genetic modification of is mainly dependent on protoplastmediated transformation (PMT). In this study, we established a dual selection marker system in an industrial 3.042 strain by using -mediated transformation (ATMT).

Synthesis, characterization, DNA binding, topoisomerase I inhibition and antiproliferation activities of three new functionalized terpyridine platinum(II) complexes.

Three new platinum(II) complexes with pendent morpholine were synthesized, namely complex 1 ([Pt(L)Cl]CFSO), complex 2 ([Pt(L)(NH)](CFSO)) and complex 3 ([Pt(L)(PPh)](CFSO)), where L = 4'-[4-(4-morpholinobutyloxy)phenyl]-2,2':6',2″-terpyridine and PPh = triphenylphosphine. The detailed molecular structures of complex 3, L and its precursor L' (1,4'-[4-(4-bromobutyloxy)phenyl]-2,2':6',2″-terpyridine) were determined by single crystal X-ray diffraction. An evaluation of in vitro cytotoxicity for both ligand and complexes was performed by methyl thiazolyl tetrazolium (MTT) assay in three cancer cell lines and normal cells as the control, respectively.

Polysaccharides from Portulaca oleracea L. regulated insulin secretion in INS-1 cells through voltage-gated Na channel.

The present study was undertaken to determine the involvement of voltage-gated Na channel (VGSC) and other mechanism related to insulin secretion in polysaccharides from Portulaca oleracea L. (POP)-induced secretion of insulin from insulin-secreting β-cell line cells (INS-1) cells. Our results showed that the concentration of insulin both in culture medium and inside INS-1 cells were increased under the existing of different concentration of glucose by POP or TTX, respectively.

Design, synthesis and biological evaluation of AZD9291 derivatives as selective and potent EGFR inhibitors.

Third-generation epidermal growth factor receptor (EGFR) inhibitors are still the main drugs for the treatment of advanced non-small cell lung cancer (NSCLC), and these drugs have achieved remarkable clinical efficacy. However, there are still many patients suffering from drug-resistant mutations and drug side effects caused by NSCLC. In this study, guided by the molecular simulation, we applied a structure-based drug design strategy (SBDD) and optimized the structure to obtain a series of potent and selective EGFR inhibitors.

Discovery of novel quinazoline derivatives bearing semicarbazone moiety as potent EGFR kinase inhibitors.

Aimed at discovering effective EGFR inhibitors, six series of quinazoline derivatives bearing a semicarbazone moiety were designed, synthesized and evaluated in different cancer cell lines (A549, HepG2, MCF-7 and PC-3). Most of the selected compounds showed remarkable cytotoxicity with IC values reaching the nanomole range. Further, the inhibition efficacy of 11 compounds against EGFR kinases was tested, which demonstrated excellent IC values in nanomolar level.

Targeted folate-conjugated pluronic P85/poly(lactide-co-glycolide) polymersome for the oral delivery of insulin.

Aim: To explore the better efficacy of targeted folic acid (FA)-Pluronic 85-poly(lactide-co-glycolide) (FA-P85-PLGA) polymersome in oral insulin delivery.

Materials & Methods: The cytotoxicity of the polymers, in vitro qualitative and quantitative cellular uptake and the internalization mechanism of insulin-loaded FA-P85-PLGA and PLGA-P85-PLGA polymersomes were studied with the human colon adenocarcinoma cells (Caco-2 cells). Their pharmacodynamics and pharmacokinetics properties were also studied with diabetic rats.

Genome-wide identification of the fatty acid desaturases gene family in four Aspergillus species and their expression profile in Aspergillus oryzae.

Fatty acid desaturases play a key role in producing polyunsaturated fatty acids by converting single bonds to double bonds. In the present study, a total of 13, 12, 8 and 8 candidate fatty acid desaturases genes were identified in the Aspergillus oryzae, Aspergillus flavus, Aspergillus fumigatus and Aspergillus nidulans genomes through database searches, which were classified into five different subfamilies based on phylogenetic analysis. Furthermore, a comprehensive analysis was performed to characterize conserved motifs and gene structures, which could provide an intuitive comprehension to learn the relationship between structure and functions of the fatty acid desaturases genes in different Aspergillus species.

Synthesis and antiproliferative activity of 6,7-disubstituted-4-phenoxyquinoline derivatives bearing the 1,8-naphthyridin-2-one moiety.

A series of 6,7-disubstituted-4-phenoxyquinoline derivatives bearing the 1,8-naphthyridin-2-one moiety were designed, synthesized and evaluated for their biological activities. The target compounds exhibited moderate to high antiproliferative activity against three cancer cell lines (A549, HepG2 and MCF-7) and several compounds (25, 27, 33, 37, 41, 43, 49 and 53) were evaluated for the activity against c-Met kinase. The most promising compound 33 (IC c-Met = 2.

Design and synthesis of novel pyrimido[5,4-d]pyrimidine derivatives as GPR119 agonist for treatment of type 2 diabetes.

We described the discovery and optimization of a novel series of pyrimidopyrimidine derivatives as G-protein coupled receptor 119 (GPR119) agonists against type 2 diabetes. Most designed compounds displayed significant GPR119 agonistic activities. Optimized analogues 15a and 21e exhibited highly potent agonistic activities with single digit EC values (2.

Neuroprotective effects of cordycepin inhibit Aβ-induced apoptosis in hippocampal neurons.

In Alzheimer's disease (AD), β-amyloid (Aβ) protein toxicity increases the formation of reactive oxygen species (ROS) and intracellular calcium levels, resulting in neuronal dysfunction, neurodegenerative disorders, and cell death. Cordycepin is a derivative of the nucleoside adenosine; also, it is speculated to exert neuroprotective effects against Aβ-induced oxidative toxicity in hippocampal neurons. In the present study, the fluorescence detection method and whole-cell patch-clamp recordings were used to study the neuroprotective effects against Aβ-induced toxicity in the primary hippocampal cultured neurons.

Design, Synthesis and Biological Evaluation of Novel Phenylsulfonylurea Derivatives as PI3K/mTOR Dual Inhibitors.

Five series of novel phenylsulfonylurea derivatives, ⁻, ⁻, ⁻, ⁻ and ⁻, bearing 4-phenylaminoquinoline scaffold were designed, synthesized and their IC values against four cancer cell lines (HepG-2, A549, PC-3 and MCF-7) were evaluated. Most compounds showed moderate cytotoxicity activity against the cancer cell lines. Structure⁻activity relationships (SARs) and pharmacological results indicated that introduction of 4-aminoquinoline scaffold and phenylsulfonylurea scaffold were beneficial for anti-tumor activity.

Design, Synthesis and Biological Evaluation of 6,7-Disubstituted-4-phenoxyquinoline Derivatives Bearing Pyridazinone Moiety as c-Met Inhibitors.

Deregulation of the receptor tyrosine kinase mesenchymal epithelial transition factor (MET) has been implicated in several human cancers and is an attractive target for small molecule drug discovery. Herein, a series of 6,7-disubstituted-4-phenoxyquinoline derivatives bearing pyridazinone derivatives were designed, synthesized and evaluated for their enzymatic inhibitory activity against c-Met kinase and cellular potency against A549, HepG2, and MCF-7 cell lines. Eight of them are equal to more active than positive control Foretinib against one or more cell lines and enzyme.

The Odorant Binding Protein 6 Expressed in Sensilla Chaetica Displays Preferential Binding Affinity to Host Plants Volatiles in .

The monophagous tea geometrid selectively feed on tea plants, requiring the specialized chemosensory system to forage for certain host. A deep insight into the molecular basis would accelerate the design of insect-behavior-modifying stimuli. In the present study, we focused on the odorant-binding protein 6 (EoblOBP6) with the high abundance in legs transcriptome of moths.

Design, synthesis, antiproliferative activity and docking studies of quinazoline derivatives bearing 2,3-dihydro-indole or 1,2,3,4-tetrahydroquinoline as potential EGFR inhibitors.

Eight series of quinazoline derivatives bearing 2,3-dihydro-indole or 1,2,3,4-tetrahydroquinoline were designed, synthesized and evaluated for the IC values against three cancer cell lines (A549, MCF-7 and PC-3). Most of the forty nine target compounds showed excellent antiproliferative activity against one or several cancer cell lines. The compound 13a showed the best activity against A549, MCF-7 and PC-3 cancer cell lines, with the IC values of 1.

Dissecting the role of Krüppel homolog 1 in the metamorphosis and female reproduction of the cotton bollworm, Helicoverpa armigera.

In insects, metamorphosis and reproduction are controlled by juvenile hormone (JH) and 20-hydroxyecdysone (20E). Krüppel homolog 1 (Kr-h1), a transcription factor, is regarded as a JH-early inducible gene responsible for the repression of metamorphosis. However, the role of Kr-h1 in reproduction of holometabolic insects is relatively less understood.