Planta Med 2013; 79 - PI53
DOI: 10.1055/s-0033-1352142

Anti-inflammatory effects of triterpene saponins from Kalopanax pictus

S Yang 1, T Quang 1, N Ngan 1, H Yoon 1, Y Kim 1, J Kang 1
  • 1College of Pharmacy, Chungnam National University, Daejeon 305 – 764, Korea

Phytochemical study of the stem bark of Kalopanax pictus Nakai resulted in the isolation of 23 oleanane-type triterpenes and saponins, including eight new (1 – 5 and 16 – 18), and 15 known compounds (6 – 15 and 19 – 23). Their structures were identified by spectroscopic and chromatographic data. For the quantitation of saponins, the HPLC-ELSD system was used. The HPLC analysis was achieved on an Optimapak C18 column (4.6 mm x 250 mm, 5 µm, RStech Corp, Korea). The mobile phase consisted of solvent A (water) and solvent B (acetonitrile) was used in gradient elution: 0 min, 30% B; 15 min, 50% B; 20 min, 100% B and held at 100% for 10 min at the flow rate of 0.50 mL/min. The chromatograms were monitored at the following ELSD conditions: temperature 65oC, gas pressure at 2.0 bar. The results showed that the content of kalopanaxsaponin B, kalopanaxsaponin C and sieboldianoside A were in the range of 0.61˜27.77 mg/g, 0.99˜26.83 mg/g and 1.56˜16.75 mg/g in KC samples, respectively.

Seventeen of the compounds (1 – 5, 7 – 12, 14, 16, 17, 20, 21, and 23) significantly inhibited TNFα-induced NF-kB transcriptional activity in HepG2, with IC50 values ranging of 0.6 – 16.4µM. Compounds 9, 11, 12, 14, 16 – 18, 20, 21, and 23 upregulated PPARs transcriptional activity in HepG2, with EC50 values of 0.2 – 15.5 mM. Compounds 14, 15, 19, and 21 showed significant PPARa transactivational activity, with EC50 values of 17.3, 8.0, 7.8, and 10.3 mM, respectively. Compounds 14, 17, 19, and 20 – 22 exhibited PPARg dose-dependent transactivational activity, with EC50 values of 16.3, 14.7, 15.5, 14.8, 10.9, and 17.1 mM, whereas compounds 14 and 21 significantly upregulated PPARβ(d) transcriptional activity, with EC50 values of 17.7 and 15.7 mM, respectively. These results provide a scientific support for the use of the stem bark of K. pictus Nakaiand warrant further studies to develop new agents for the prevention and treatment of the inflammatory and metabolic diseases.

Fig. 1: Structures of isolated compounds