Structure-activity relationship study of novel evodiamine amino acid conjugates with potent anti-colorectal cancer efficacy.

Evodiamine has been a promising lead structure with broad-spectrum antitumor activity. Druggability optimization is the most challenging part of evodiamine-based lead-to-candidate campaign. Amino acids as building blocks for conjugates are widely incorporated into approved drug and drug candidates, demonstrating highly attractive druggability.

Discovery of 7-(1-methyl-1H-pyrazol-4-yl)-1,6-naphthyridine derivatives as potent inhibitors of rearranged during transfection (RET) and RET solvent-front mutants for overcoming selpercatinib resistance.

Rearranged during transfection kinase (RET) inhibition has been considered a promising therapeutic approach for treatment of a variety of cancers. However, the clinical therapeutic benefits of the second-generation RET inhibitor selpercatinib are greatly compromised by acquired resistance mediated by solvent-front mutations (e.g.

Identification of a novel 10-hydroxyevodiamine prodrug as a potent topoisomerase inhibitor with improved aqueous solubility for treatment of hepatocellular carcinoma.

Natural product evodiamine (Evo) and its synthetic derivatives represent an attractive dual Topo 1/2 inhibitors with broad-spectrum antitumor efficacy. However, the clinical applications of these compounds have been impeded by their poor aqueous solubility. Herein, a series of water-soluble 10-substituted-N(14)-phenylevodiamine derivatives were designed and synthesized.

Arbuscular mycorrhizal fungal communities in soils where astragalus had grown for 2 years were similar to those in the abandoned farmland.

Purpose: Astragalus-cultivated soils are enriched in arbuscular mycorrhizal fungi (AMF); however, the community changes of AMF between years in stragalus-cultivated soils are still unclear.

Methods: To illustrate this, using high-throughput amplicon sequencing and quantitative real-time PCR, we analyzed the AMF communities of the abandoned farmlands and interannual astragalus-cultivated soils for 1-, 2-, 3-, and 4-years, including community composition, dominant, core, specific and significantly fluctuating AMF, co-occurrence network, alpha diversity, and beta diversity.

Results: A total of 74 OTUs were classified into one phylum, Glomeromycota; one class, Glomeromycetes; four orders; four families; and six genera.

Astragalus-cultivated soil was a suitable bed soil for nurturing Angelica sinensis seedlings from the rhizosphere microbiome perspective.

Angelica sinensis (Oliv.) Diels is an important Chinese medicinal plant. A.

Rhizosphere bacterial and fungal communities during the growth of seedlings cultivated in an Alpine uncultivated meadow soil.

Background: seedlings are grown in alpine uncultivated meadow soil with rainfed agroecosystems to ensure the quality of after seedling transplantation. The aim was to investigate the rhizosphere bacterial and fungal communities during the growth stages of seedlings.

Methods: The bacterial and fungal communities were investigated by HiSeq sequencing of 16S and 18S rDNA, respectively.

Enhanced Heavy Metal Tolerance and Accumulation by Transgenic Sugar Beets Expressing Streptococcus thermophilus StGCS-GS in the Presence of Cd, Zn and Cu Alone or in Combination.

Phytoremediation is a promising means of ameliorating heavy metal pollution through the use of transgenic plants as artificial hyperaccumulators. A novel Streptococcus thermophilus γ-glutamylcysteine synthetase-glutathione synthetase (StGCS-GS) that synthesizes glutathione (GSH) with limited feedback inhibition was overexpressed in sugar beet (Beta vulgaris L.), yielding three transgenic lines (s2, s4 and s5) with enhanced tolerance to different concentrations of cadmium, zinc and copper, as indicated by their increased biomass, root length and relative growth compared with wild-type plants.

Characteristics of miniature Cheddar-type cheese made by microbial rennet from Bacillus amyloliquefaciens: a comparison with commercial calf rennet.

Miniature Cheddar-type cheeses were produced using microbial rennet from Bacillus amyloliquefaciens (milk-clotting enzyme [MCE]) or calf rennet (CAR). With the exception of pH, there were no significant differences in gross composition between MCE-cheese (MCE-C) and CAR-cheese (CAR-C). The pH value of CAR-C was significantly higher than that of MCE-C at 40 and 60 d of ripening.

Enhanced β-galactosidase production of Aspergillus oryzae mutated by UV and LiCl.

In order to breed a high-yield β-galactosidase-producing strain, Aspergillus oryzae was used as the parent strain and mutagenized with ultraviolet (UV) and UV plus lithium chloride (LiCl), respectively. After being mutagenized by UV, the β-galactosidase activity of mutant UV-15-20 reached 114.08 U/mL, which revealed a 49.

Enzyme inhibitor studies reveal complex control of methyl-D-erythritol 4-phosphate (MEP) pathway enzyme expression in Catharanthus roseus.

In Catharanthus roseus, the monoterpene moiety exerts a strong flux control for monoterpene indole alkaloid (MIA) formation. Monoterpene synthesis depends on the methyl-D-erythritol 4-phosphate (MEP) pathway. Here, we have explored the regulation of this pathway in response to developmental and environmental cues and in response to specific enzyme inhibitors.

Exploiting plants for glutathione (GSH) production: Uncoupling GSH synthesis from cellular controls results in unprecedented GSH accumulation.

Glutathione (GSH) is a key factor for cellular redox homeostasis and tolerance against abiotic and biotic stress (May et al., 1998; Noctor et al., 1998a).

BjMT2, a metallothionein type-2 from Brassica juncea, may effectively remove excess lead from erythrocytes and kidneys of rats.

The remedial effects of a plant metallothionein type-2 were observed from lead (Pb) injured rats. BjMT2 from Brassica juncea was expressed in Escherichia coli and purified by affinity chromatography, a purified BjMT2 protein was obtained which strongly reacted with the thiol reagent MBB (monobromobimane). The profiles of erythrocytes, renal tubules and glomerulus of kidney of rats suffered pathological changes from excess Pb were evidently improved by supplying the BjMT2.

Expression of BjMT2, a metallothionein 2 from Brassica juncea, increases copper and cadmium tolerance in Escherichia coli and Arabidopsis thaliana, but inhibits root elongation in Arabidopsis thaliana seedlings.

The protective function of a plant type-2 metallothionein was analysed after expression in Escherichia coli and in Arabidopsis thaliana seedlings. BjMT2 from Brassica juncea was expressed in E. coli as a TrxABjMT2 fusion protein.

Research advances on transgenic plant vaccines.

In recent years, with the development of genetics molecular biology and plant biotechnology, the vaccination (e.g. genetic engineering subunit vaccine, living vector vaccine, nucleic acid vaccine) programs are taking on a prosperous evolvement.