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Bicyclol, an innovative hepatoprotective drug, was approved by the Chinese National Medical Products Administration (NMPA) in 2001 to treat Hepatitis B and drug-induced liver injury. Two active metabolites of bicyclol have been identified as M2 and M3. To evaluate the impact on drug safety and efficacy of possible drug-drug interactions (DDIs) associated with these metabolites, a sufficient quantity of these metabolites is required. Herein, we report a concise novel route for the synthesis of M2 and M3 using the Suzuki-Miyaura coupling as the key step. Furthermore, we complete the gram-scale syntheses of M2 and M3. [ABSTRACT FROM AUTHOR]

The novel protein elicitor GP1pro is the protein component of glycoprotein GP‐1 isolated and identified from Streptomyces kanasensis ZX01. GP1pro induces the production of reactive oxygen species (ROS) and a hypersensitive response (HR), along with the accumulation of resistance‐related genes and secondary metabolites. It ultimately regulates plant defence responses. Further analysis revealed that GP1pro interacts with the PIP2‐family aquaporin protein NbPIP2;4 on the plant plasma membrane (PM) in Nicotiana benthamiana. PM localization is necessary for inducing GP1pro resistance. These results demonstrate that NbPIP2;4 acts as a H2O2 transporter to positively regulate plant immunity and ROS accumulation. In summary, this study elucidates a conserved and novel pathway caused by GP1pro to initiate host cellular defences by targeting the plant aquaporin protein NbPIP2;4 and transporting apoplast‐to‐cytoplast H2O2 to regulate plant immunity. Summary Statement: We found a protein elicitor from actinomycetes that interacts with the tobacco aquaporin NbPIP2;4 to regulate plant immunity and enhance tobacco disease resistance. This provides a basis for the development of protein elicitors for green plant protection strategies. [ABSTRACT FROM AUTHOR]

Myxobacteria are part of the phylum Myxococcota, encompassing four orders. Most of them display complex lifestyles and broad predation profiles. However, metabolic potential and predation mechanisms of different myxobacteria remains poorly understood. Herein, we used comparative genomics and transcriptomics to analyze metabolic potentials and differentially expressed gene (DEG) profiles of Myxococcus xanthus monoculture (Mx) compared to coculture with Escherichia coli (MxE) and Micrococcus luteus (MxM) prey. The results showed that myxobacteria had conspicuous metabolic deficiencies, various protein secretion systems (PSSs) and the common type II secretion system (T2SS). RNA-seq data demonstrated that M. xanthus overexpressed the potential predation DEGs, particularly those encoding T2SS, the tight adherence (Tad) pilus, different secondary metabolites (myxochelin A/B, myxoprincomide, myxovirescin A1, geosmin and myxalamide), glycosyl transferases and peptidase during predation. Furthermore, the myxalamide biosynthesis gene clusters, two hypothetical gene clusters and one arginine biosynthesis clusters were highly differential expressed in MxE versus MxM. Additionally, homologue proteins of the Tad (kil) system and five secondary metabolites were in different obligate or facultative predators. Finally, we provided a working model for exhibiting multiple predatory strategies when M. xanthus prey on M. luteus and E. coli. These results might spur applicationoriented research on the development of novel antibacterial strategies. [ABSTRACT FROM AUTHOR]

As the most abundant and bioactive constituent in vine tea (Ampelopsis grossedentata), dihydromyricetin possesses numerous biological activities. A rapid profiling and identification method for dihydromyricetin metabolites in rats after the oral administration has been established using ultra‐high‐performance liquid chromatography‐Q‐Exactive Orbitrap mass spectrometry coupled with multiple data‐mining methods. Herein, an efficient analytical strategy characterized by a parallel reaction monitoring mode combining diagnostic fragment ions filtering techniques was developed for the comprehensive identification of dihydromyricetin metabolites in rat plasma, urine, and feces. And then, the biotransformation pathways of dihydromyricetin were further revealed. As a result, a total of 49 metabolites were finally identified by comparing diagnostic fragment ions, chromatographic retention times, neutral loss fragment ions, and accurate mass measurement with those of the dihydromyricetin reference standard. These metabolites were presumed to be dominantly generated through hydroxylation, dehydroxylation, methylation, reduction, sulfation, decarbonylation, glucuronidation, glucosylation, and their composite reactions. In a word, our present results not only supplied a solid foundation to better understand the action mechanism of dihydromyricetin, but also provided some models for the metabolism study of the other compounds in traditional Chinese medicines or natural plants. [ABSTRACT FROM AUTHOR]