Germacrane Sesquiterpene Esters from<i>Salvia roborowskii</i>

Osteolytic bone diseases are commonly presented with enhanced osteoclast formation and bone resorption. Sesquiterpene lactone natural compounds have been found to possess anti-inflammatory and immune-modulation effects. Here, we identified three germacrane sesquiterpenes using computer-based virtual screening for the structural similarity with sesquiterpene lactone, parthenolide. We showed that natural germacrane sesquiterpene compounds A, B, and C inhibit osteoclast formation and bone resorption in a dose-dependent manner, with relative potency compound A > compound C > compound B based on their equimolar concentrations. Mechanistic studies by Luciferase reporter gene assay and Western blot analysis showed that germacrane sesquiterpene compound A inhibits RANKL-induced activation of NF-κB and IκBα degradation. This study reveals that natural germacrane sesquiterpene compounds are inhibitors for osteoclast formation and bone resorption, and provides evidence that naturally-occurring compounds might be beneficial as alternative medicine for the prevention and treatment of osteolysis.

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“…Other Names: 3β,6β,8α-Triacetyl-4β,5α-epoxy-1-oxogermacr-10(14)-ene isolated from Germacrane sesquiterpene esters from salvia roborowskii [ 20 ].…”

Section: Methodsmentioning

confidence: 99%

Natural Germacrane Sesquiterpenes Inhibit Osteoclast Formation, Bone Resorption, RANKL-Induced NF-κB Activation, and IκBα Degradation

Qin

Ang

Dai

et al. 2015

IJMS

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Two New Sesquiterpenes from Salvia roborowskiiMaxim

Liu¹,

Li²,

Shi³

et al. 2009

Helvetica Chimica Acta

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Two new sesquiterpenes, (1b,3b,4a,5a,6a,8a)-guai-10(14)-ene-3,4,6,8-tetrol 3,6,8-triacetate (1) and (3b,4a,6a,8b,9b,10a)-8-(acetyloxy)-3,4 : 9,10-diepoxygermacr-7(11)-eno-12,6-lactone (2) were isolated from the EtOH extract of Salvia roborowskii Maxim. Their structures were established by spectroscopic methods, including one-and two-dimensional NMR techniques, and the relative configurations of these compounds were determined on the basis of NOE experiments.

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