OBJECTIVETo study the scientific theory on detoxification (attenuation) of Stellera chamaejasme (ScL) by processing and the impact on drug effect of ScL before and after being processed with vinegar.

METHODThe difference in ingredients of ScL before and after being processed vinegar was compared by using PHLC-MS technique. A subcutaneously transplanted tumor model of H22 hepatoma was established to compare the lethal effect and weight change between tumor-loaded mice and normal mice. After consecutive oral administration in tumor-loaded mice, the impacts on tumors and immune organs were compared before and after being processed with vinegar. Luciferase Report Gene was employed to investigate the target genes TGF-beta, AP1 and NF-kappaB.

RESULTThe LD50 (median fatal dose) of extract Zp1102 exhibited higher than that of the processed one Zp1103, that is 9. 89 g x kg(-1) vs. 16.85 g x kg(-1). According to the test, Zp1102 showed more effective anti-tumor activities in vivo than that of Zp1103 in a same dosage, with the tumor inhibitory rate 36.24% (P < 0.01) at the dosage of2 g x kg(-1) and 34.40% (P < 0.05) at the dosage of 1 g x kg(-1). At the dosage of 1 g x kg(-1), Zp1102 showed a tumor inhibitory rate of 34.52% (P < 0.05), much higher from 21.55% in Zp1103. Both Zp1102 and Zp1103 had basically no impact on the report gene NF-kappaB, besides that Zp1102 up-regulated the report gene after increase in NF-kappaB concentration and down-regulated TGF-beta, but Zp1103 can only up-regulate NF-kappaB expression without any impact on TGF-beta.

CONCLUSIONProcessed ScL extracts show less toxic than unprocessed extracts and slight reduction in anti-tumor activity, which may be related to the regulation of transforming growth factor TGF-beta.