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NMR, LC-MS Characterization of Rydingia michauxii Extracts, Identification of Natural Products Acting as Modulators of LDLR and PCSK9.

Abstract
Rydingia michauxii (Briq.) Scheen and V.A.Albert (Lamiaceae) is used in Iranian traditional medicine to treat malaria, diabetes, hyperlipidemia, rheumatism and cardiovascular diseases. NMR and LC-DAD-MSn analyses were used to establish extract composition and phenylethanoid, flavonoid glycosides, lignans, labdane diterpenes and iridoids were identified and quantified. The main constituents were isolated, and structures were elucidated based on NMR, polarimetric and MS measurements. A new natural compound, ent-labda-8(17),13-dien-18-glucopyranosyl ester-15,16-olide is described here. The effects of ent-labda-8(17),13-dien-18-oic acid-15,16-olide (1), ent-labda-8(17),13-dien-18-glucopyranosyl es-ter-15,16-olide (2), antirrhinoside (3), echinacoside (4), verbascoside (5), and apigenin 6,8-di-C-glucoside (6), on the low-density lipoprotein receptor (LDLR) and proprotein convertase subtilisin/kexin type 9 (PCSK9), were studied in the human hepatocarcinoma cell line Huh7. Among the six constituents, (3) showed the strongest induction of the LDLR (3.7 ± 2.2 fold vs. control) and PCSK9 (3.2 ± 1.5 fold vs. control) at a concentration of 50 µM. The in vitro observations indicated a potential lipid lowering activity of (3) with a statin-like mechanism of action.
AuthorsStefania Sut, Aminallah Tahmasebi, Nicola Ferri, Irene Ferrarese, Ilaria Rossi, Giovanni Panighel, Maria Giovanna Lupo, Filippo Maggi, Akbar Karami, Stefano Dall'Acqua
JournalMolecules (Basel, Switzerland) (Molecules) Vol. 27 Issue 7 (Mar 30 2022) ISSN: 1420-3049 [Electronic] Switzerland
PMID35408655 (Publication Type: Journal Article)
Chemical References
  • Biological Products
  • Plant Extracts
  • Receptors, LDL
  • PCSK9 protein, human
  • Proprotein Convertase 9
Topics
  • Biological Products (pharmacology)
  • Chromatography, Liquid
  • Humans
  • Iran
  • Lamiaceae (metabolism)
  • Liver Neoplasms
  • Plant Extracts (pharmacology)
  • Proprotein Convertase 9 (metabolism)
  • Receptors, LDL (metabolism)
  • Tandem Mass Spectrometry

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