Project description:Scopolia tangutica (S. tangutica) is a traditional Chinese medicinal plant used for antispasmodics, anesthesia, analgesia and sedation. Its pharmacological activities are mostly associated with the antagonistic activity at muscarinic acetylcholine receptors (mAchRs) of several known alkaloids such as atropine and scopolamine. With our recent identification of four hydroxycinnamic acid amides from S. tangutica, we hypothesized that this plant may contain previously unidentified alkaloids that may also contribute to its in vivo effect. Herein, we used a bioassay-guided multi-dimension separation strategy to discover novel mAchR antagonists from S. tangutica. The core of this approach is to use label-free cell phenotypic assay to first identify active fractions, and then to guide purification of active ligands. Besides four tropanes and six cinnamic acid amides that have been previously isolated from S. tangutica, we recently identified two new tropanes, one new cinnamic acid amide, and nine other compounds. Six tropane compounds purified from S. tangutica for the first time were confirmed to be competitive antagonists of muscarinic receptor 3 (M3), including the two new ones 8 and 12 with IC50 values of 1.97 μM and 4.47 μM, respectively. Furthermore, the cinnamic acid amide 17 displayed 15-fold selectivity for M1 over M3 receptors. These findings will be useful in designing lead compounds for mAchRs and elucidating mechanisms of action of S. tangutica.

| S-EPMC5384254 | biostudies-literature

The complete chloroplast genome of <i>Prunus tangutica</i> (Batal.) Korsh.

Project description:The complete cp genome of Prunus tangutica is 158,131 bp in length, exhibits a typical quadripartite structural organization, consisting of a large single copy (LSC) region of 86,266 bp, two inverted repeats (IR) regions of 26,389 bp, and a small single copy (SSC) region of 19,087 bp. The cp genome contains 131 complete genes, including 86 protein-coding genes (86 PCGs), 8 ribosomal RNA genes (8 rRNAs), and 37 tRNA genes (37 tRNAs). Most genes occur in a single copy, while 19 genes occur in double, including 4 rRNAs (4.5S, 5S, 16S, and 23S rRNA), 7 tRNAs (trnA-UGC, trnI-GAU, trnL-CAA, trnI-CAU, trnN-GUU, trnR-ACG, and trnV-GAC), and 5 PCGs (rps7, ndhB, ycf2, rpl2 and rpl23). The overall GC content of cp DNA is 36.7%, the corresponding values of the LSC, SSC, and IR regions are 34.6%, 30.1%, and 42.6%, respectively. Further, the phylogenetic analysis suggested that the P. tangutica was closely related to Prunus tenella. The results of P. tangutica will lay a foundation for further research.

| S-EPMC8788344 | biostudies-literature

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