Ecabet Sodium Hydrate

Selaginella moellendorffii miltiradiene synthase (SmMDS) is a unique bifunctional diterpene synthase (diTPS) that catalyses the successive cyclization of (E,E,E)‐geranylgeranyl diphosphate (GGPP) via (+)‐copalyl diphosphate (CPP) to miltiradiene, which is a crucial precursor of important medicinal compounds, such as triptolide, ecabet sodium and carnosol. Miltiradiene synthetic processes have been studied in monofunctional diTPSs, while the precise mechanism by which active site amino acids determine product simplicity and the experimental evidence for reaction intermediates remain elusive. In addition, how bifunctional diTPSs work compared to monofunctional enzymes is attractive for detailed research. Here, by mutagenesis studies of SmMDS, we confirmed that pimar‐15‐en‐8‐yl+ is an intermediate in miltiradiene synthesis. Moreover, we determined the apo‐state and the GGPP‐bound state crystal structures of SmMDS. By structure analysis and mutagenesis experiments, possible contributions of key residues both in class I and II active sites were suggested. Based on the structural and functional analyses, we confirmed the copal‐15‐yl+ intermediate and unveiled more details of the catalysis process in the SmMDS class I active site. Moreover, the structural and experimental results suggest an internal channel for (+)‐CPP produced in the class II active site moving towards the class I active site. Our research is a good example for intermediate identification of diTPSs and provides new insights into the product specificity determinants and intermediate transport, which should greatly facilitate the precise controlled synthesis of various diterpenes.

According to the PASS prediction, resin acids and rosin derivatives can exhibit protective activity with respect to mucous membranes (Pa 71-98%).Therefore, these substances can form the basis for drug development, which includes biotesting as a necessary step in biosafety assessment of drug candidates.Study of antibacterial activity by the disk diffusion method showed that the most toxic effect on E. coli and B. subtilis cells is characteristic of gum rosin, maleopimaric acid, and abietinol.Gum rosin exhibits fungicidal activity against C. tropicalis yeast. 12-Sulfodehydroabietic acid and its potassium salt affect the intensity of seed germination of Raphanus sativusL., and their toxicity is directly related to concentrationComplete inhibition of seed germination is observed at a concentration of 25 mg/mL.