Pharmacokinetics of Compound D, the Major Bioactive Component of Zingiber cassumunar, in Rats.

Rhizomes of Zingiber cassumunar have been used for many years in traditional Thai medicine as an anti-inflammatory agent. The major bioactive component of this plant is Compound D [E-4-(3', 4'-dimethoxyphenyl)but-3-en-1-ol], which is a strong smooth muscle relaxant, and has antihistamine and anti-inflammatory actions. There is, however, incomplete information available for the pharmacokinetics of Compound D in mammals. In this study, we examined the pharmacokinetic profiles of Compound D in male Wistar rats. A standardized extract of Z. cassumunar containing 4 % w/w Compound D was administered intravenously at 25 mg/kg or by oral gavage at 25, 75, or 250 mg/kg to Wistar rats. Blood, tissues, urine, and feces were collected from 0 to 48 h after dosing and the level of Compound D was determined by liquid chromatography-tandem mass spectrometry. The concentration of Compound D ranged from 10-100 µg/L, reached a maximum approximately 0.15 h after oral dosing. Compound D exhibited an excellent tissue to plasma ratio, ranging from 1- to 1000 in several organs at 1-4 h after oral dosing. Less than 1 % of unchanged Compound D was excreted in the urine and feces. Further studies on tissue uptake and metabolite identification are required to obtain complete pharmacokinetic information and to develop appropriate dosing strategies of Compound D and the standardized extract of Z. cassumunar.

Anti-oxidant activities of Acanthopanax senticosus stems and their lignan components.

The antioxidant activities of Acanthopanax senticosus stems were evaluated in CCl4-intoxicated rats. The n-butanol fraction from the water extract of the stems, when pretreated orally at 200 mg/kg/day for 7 consecutive days in rats, was demonstrated to exhibit significant increases in antioxidant enzyme activities such as hepatic cytosolic superoxide dismutase, catalase and glutathione peroxidase by 30.31, 19.82 and 155%, respectively. The n-butanol fraction whereas showed a significant inhibition of serum GPT activity (65.79% inhibition) elevated with hepatic damage induced by CCl4-intoxication. Eleutheroside B, a lignan component, isolated from the n-butanol fraction was found to cause a moderate free radical scavenging effect on DPPH, its scavenging potency as indicated in IC50 value, being 58.5 microM. These results suggested that the stems of A. senticosus possess not only antioxidant but also hepatoprotective activities.

Percutaneous absorption of 3 organic solvents in the guinea pig (V). Effect of "accelerants".

The influence of "accelerants" on the percutaneous absorption of 3 organic solvents (butanol, toluene, 1,1,1-trichloroethane) was investigated in the guinea pig. DMSO in binary and ternary mixtures with various concentrations, the result of adding 0.1 M C18 fatty acids, and of pretreatment with DMSO and olive oil, were studied. Addition of DMSO (binary solutions) resulted in increased or decreased absorption of the solvents related to their water solubility. There was reduced absorption of toluene and trichloroethane in binary mixtures with DMSO, while DMSO in binary mixture with butanol gave a marked increase, with concentrations of 50 and 75%. Pretreatment with DMSO resulted in a decrease in the absorption of toluene and a marked increase in the absorption of butanol. The same tendency was seen when skin was pretreated with olive oil under occlusion. The results indicate that the effect of DMSO is related to the water solubility of the penetrant.