Eighteen new jatrophane diterpenoids,
euphoesulatins A–R
(1–18), and three known diterpenoids
(19–21) were isolated from Euphorbia esula. Compounds 1–7, 14, and 18 represent a rare type of jatrophane-type
diterpenoid containing a nicotinoyloxy group. The absolute configuration
of 1 was determined by X-ray crystallography. The compounds
were assayed for their antiosteoporotic activity in a bone-marrow-derived
macrophage cell line, and compounds 1, 8, and 10 significantly inhibited the formation of osteoclasts,
with IC50 values of 1.2, 3.5, and 2.3 μM, respectively.
These three compounds also dose-dependently reduced the activity of
nuclear factor activated T-cell cytoplasmic 1. This study reveals
the antiosteoporotic effects of jatrophane diterpenoids for the first
time.
Obesity is a chronic metabolic disease with an increasing worldwide prevalence and a major cause for development of many metabolic, cardiovascular, and chronic inflammatory diseases, such as type 2 diabetes mellitus (T2DM), dyslipidaemia, nonalcoholic fatty liver disease (NAFLD), hypertension, coronary heart disease, and stroke. 1 The increased mass
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