TY - JOUR
T1 - Biological activity and safety of tripterygium extract prepared by sodium carbonate extraction
AU - Fang, Wei
AU - Peng, Fan
AU - Yi, Tao
AU - Zhang, Cong
AU - Wan, Chunxi
AU - Xu, Huibi
AU - Lam, Christopher Waikei
AU - Yang, Xiangliang
PY - 2012/9
Y1 - 2012/9
N2 - The commercial preparation named "Tripterygium glycosides" prepared by column chromatography has been used for the treatment of inflammatory and autoimmune diseases with significant efficacy but concurrent toxicity. The aim of this study was to reduce the toxicity of Tripterygium extracts, using cytotoxicity and anti-inflammatory activity of the three principal active components of Tripterygium wilfordii Hook. F. (TWHF) as guiding parameters. Column chromatography was replaced by sodium carbonate extraction for removing the acidic compounds and enriching epoxyditerpenoids and alkaloids in the extract. Results showed that the therapeutic index (IC 50/EC 50) on murine macrophage Raw 264.7 cells and rat mesangial HBZY-1 cells of the extract prepared by sodium carbonate extraction was significantly higher than that of Tripterygium glycosides (0.8 and 5.2 vs. 0.3 and 2.6, p < 0.05), while its cytotoxicity on human liver HL7702 cells was significantly lower (14.5 ± 1.4 vs. 6.8 ± 0.9, p < 0.05). Further acute oral toxicity experiments showed that the LD 50 value of this extract was 1,210 mg/kg compared to 257 mg/kg for Tripterygium glycosides. All the above results suggest that Tripterygium extract prepared by sodium carbonate extraction may represent a potentially optimal source of medicine with good therapeutic index.
AB - The commercial preparation named "Tripterygium glycosides" prepared by column chromatography has been used for the treatment of inflammatory and autoimmune diseases with significant efficacy but concurrent toxicity. The aim of this study was to reduce the toxicity of Tripterygium extracts, using cytotoxicity and anti-inflammatory activity of the three principal active components of Tripterygium wilfordii Hook. F. (TWHF) as guiding parameters. Column chromatography was replaced by sodium carbonate extraction for removing the acidic compounds and enriching epoxyditerpenoids and alkaloids in the extract. Results showed that the therapeutic index (IC 50/EC 50) on murine macrophage Raw 264.7 cells and rat mesangial HBZY-1 cells of the extract prepared by sodium carbonate extraction was significantly higher than that of Tripterygium glycosides (0.8 and 5.2 vs. 0.3 and 2.6, p < 0.05), while its cytotoxicity on human liver HL7702 cells was significantly lower (14.5 ± 1.4 vs. 6.8 ± 0.9, p < 0.05). Further acute oral toxicity experiments showed that the LD 50 value of this extract was 1,210 mg/kg compared to 257 mg/kg for Tripterygium glycosides. All the above results suggest that Tripterygium extract prepared by sodium carbonate extraction may represent a potentially optimal source of medicine with good therapeutic index.
KW - Active components
KW - Sodium carbonate extraction
KW - Toxicity
KW - Tripterygium wilfordii Hook. F.
UR - http://www.scopus.com/inward/record.url?scp=84866927709&partnerID=8YFLogxK
U2 - 10.3390/molecules170911113
DO - 10.3390/molecules170911113
M3 - Article
C2 - 22986922
AN - SCOPUS:84866927709
SN - 1420-3049
VL - 17
SP - 11113
EP - 11123
JO - Molecules
JF - Molecules
IS - 9
ER -
