Ailanthoidol

J Cell Biochem. 2011 Dec;112(12):3816-23.

Ailanthoidol suppresses lipopolysaccharide-stimulated inflammatory reactions in RAW264.7 cells and endotoxin shock in mice.[Pubmed: 21826708]

The biological properties of Ailanthoidol, a neolignan from Zanthoxylum ailanthoides or Salvia miltiorrhiza Bunge, which is used in Chinese traditional herbal medicine, have not been evaluated.
METHODS AND RESULTS:
Here, we report that Ailanthoidol inhibits inflammatory reactions in macrophages and protects mice from endotoxin shock. Our in vitro experiments showed that Ailanthoidol suppressed the generation of nitric oxide (NO) and prostaglandin E(2) , as well as the expression of inducible NO synthase (iNOS) and cyclooxygenase (COX)-2 induced by lipopolysaccharide (LPS) in RAW264.7 cells. Similarly, Ailanthoidol inhibited the production of inflammatory cytokines induced by LPS in RAW264.7 cells, including interleukin (IL)-1β and IL-6. In an animal model, Ailanthoidol protected BALB/c mice from LPS-induced endotoxin shock, possibly through inhibition of the production of inflammatory cytokines and NO.
CONCLUSIONS:
Collectively, Ailanthoidol inhibited the production of inflammatory mediators and may be a potential target for treatment of various inflammatory diseases.

대한의생명과학회지, 2014, 20:62-69.

Anti-Adipogenic Activity of Ailanthoidol on 3T3-L1 Adipocytes.[Reference: WebLink]

Previous our study demonstrated that Ailanthoidol (3-deformylated 2-arylbenzo[b]furan), a neolignan from Zanthoxylum ailanthoides or Salvia miltiorrhiza Bunge, is a novel anti-inflammatory agent.
METHODS AND RESULTS:
In this investigation, we examined the anti-adipogenic effect of Ailanthoidol. Our data showed that Ailanthoidol suppressed lipid droplet formation and adipocyte differentiation in 3T3-L1 cells. Treatment of the 3T3-L1 adipocytes with Ailanthoidol resulted in an attenuation of the releases of leptin and interleukin-6. The expression of peroxisome proliferator-activated receptor (PPAR)γ and CCAAT/ enhancer-binding protein (C/EBP)α, the central transcriptional regulators of adipogenesis, was decreased by treatment with Ailanthoidol. Additionally, Ailanthoidol treatment increased the phosphorylation levels of 5" adenosine monophosphateactivated protein kinase.
CONCLUSIONS:
These results suggest that Ailanthoidol effectively suppresses adipogenesis and that it exerts its role mainly through the significant down-regulation of PPARγ and C/EBPα expression. Our findings provide important insights into the mechanisms underlying the anti-adipogenic activity of Ailanthoidol.

Oncol Rep. 2006 Oct;16(4):921-7.

Inhibitory effect of ailanthoidol on 12-O-tetradecanoyl-phorbol-13-acetate-induced tumor promotion in mouse skin.[Pubmed: 16969515]

Many components derived from dietary or medicinal plants showing antioxidant and anti-inflammatory potential have been found to possess chemopreventive properties. In our previous study, we achieved the total synthesis of Ailanthoidol (AT), a neolignan from Zanthoxylum ailanthoides or Salvia miltiorrhiza Bunge, which are used in Chinese traditional herbal medicine.
METHODS AND RESULTS:
In the present study, preliminarily, AT exhibited a radical quenching property by DPPH assay. Following this, we assessed the effect of AT on 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced oxidative stress and inflammation in female CD-1 mouse skin which was closely linked to tumor promotion. The topical application of AT (0.5-2.5 mM; 200 microl) reduced the formation of hydrogen peroxide and inhibited the myeloperoxidase (MPO) activity in the mouse skin when compared with that of the TPA-treated alone group. In addition, AT presented a suppression effect on the TPA-induced hyperplasia and leukocyte infiltration in the epidermis and edema of mouse ears. Furthermore, it showed that AT inhibited the TPA-induced expression of COX-2 protein and ornithine decarboxylase (ODC) activity in epidermis. Finally, AT was evaluated for its ability to inhibit the TPA-induced promotion in skin tumors of female CD-1 mice. Topical application of AT 5 min prior to TPA (5 nmol) three times weekly for 12 weeks to mice which were initiated with benzo[a]pyrene (B[a]P) inhibited the incidence of skin tumors in mice and the average number of tumors per mice as compared to TPA-treated alone.
CONCLUSIONS:
These results indicate that AT possesses potential as a chemopreventive agent against tumor promotion.