Anti-Inflammatory and Antibacterial Activity Constituents from the Stem of Cinnamomum validinerve

One new dibenzocycloheptene, validinol (1), and one butanolide firstly isolated from the natural source, validinolide (2), together with 17 known compounds were isolated from the stem of Cinnamomum validinerve. Among the isolates, lincomolide A (3), secosubamolide (7), and cinnamtannin B1 (19) exhibited potent inhibition on both superoxide anion generation (IC50 values of 2.98 &plusmn
0.3 &micro
M, 4.37 &plusmn
0.38 &micro
M, and 2.20 &plusmn
M, respectively) and elastase release (IC50 values of 3.96 &plusmn
0.31 &micro
M, 3.04 &plusmn
0.23 &micro
M, and 4.64 &plusmn
0.71 &micro
M, respectively) by human neutrophils. In addition, isophilippinolide A (6), secosubamolide (7), and cinnamtannin B1 (19) showed bacteriostatic effects against Propionibacterium acnes in in vitro study, with minimal inhibitory concentration (MIC) values at 16 &mu
g/mL, 16 &mu
g/mL, and 500 &mu
g/mL, respectively. Further investigations using the in vivo ear P. acnes infection model showed that the intraperitoneal administration of the major component cinnamtannin B1 (19) reduced immune cell infiltration and pro-inflammatory cytokines TNF-&alpha
and IL-6 at the infection sites. The results demonstrated the potential of cinnamtannin B1 (19) for acne therapy. In summary, these results demonstrated the anti-inflammatory potentials of Formosan C. validinerve during bacterial infections.