The members of Pleione (Orchidaceae) are popular worldwide for their ornamental appeal and medicinal properties. Pleione bulbocodioides , a CITES Appendix II-listed species, has been traditionally used in dermatological therapies but remains pharmacologically understudied. In this study, the in vitro anti-inflammatory effects of extracts from artificially cultivated P. bulbocodioides were investigated. We found the P. bulbocodioides extract (PE) significantly suppressed TNF-α/IFN-γ-induced expression of IL-6, IL-1β, CCL5, CCL8, CXCL8, CXCL3, and TMEM173 (STING) genes in both HaCaT cells and NHEKs. Transcriptomic analysis and Western blotting confirmed the inhibitory effects on STING/NF-κB signaling pathway of PE. And phytochemical characterization identified militarine and batatasin III as principal bioactive constituents responsible for STING/NF-κB pathway inhibition by PE. PE also demonstrated comparable anti-inflammatory efficacy in LPS-induced RAW 264.7 macrophages and SLS-irritated 3D reconstructed human epidermis. Thus, these findings indicate the potential of PE as a natural anti-inflammatory therapeutic or skincare ingredient for dermatological applications.
Militarine, a natural glucosyloxybenzyl 2-isobutylmalate, isolated fromBletilla striata, was reported with a prominent neuroprotective effect recently. The limited information on the metabolism of militarine impedes comprehension of its biological actions and pharmacology. This study aimed to investigate the metabolite profile and the distribution of militarine in vivo, which help to clarify the action mechanism further. A total of 71 metabolites (57 new metabolites) in rats were identified with a systematic method by ultra-high-performance liquid chromatography combined with quadrupole time-of-flight tandem mass spectrometry (UPLC-Q-TOF-MS/MS). The proposed metabolic pathways of militarine include hydrolyzation, oxidation, glycosylation, esterification, sulfation, glucuronidation and glycine conjugation. Militarine and its metabolites were distributed extensively in the treated rats. Notably, six metabolites of militarine were identified in cerebrospinal fluid (CSF), which were highly consistent with the metabolites after oral administration of gastrodin in rats. Among the metabolites in CSF, five of them were not reported before. It is the first systematic metabolic study of militarine in vivo, which is very helpful for better comprehension of the functions and the central nervous system (CNS) bioactivities of militarine. The findings will also provide an essential reference for the metabolism of other glucosylated benzyl esters of succinic, malic, tartaric and citric acids.Keywords:militarine;metabolite identification;metabolic profiles;UPLC-Q-TOF-MS/MS
危险品化学品经营许可证（带存储）