HPLC profile analysis of hepatoprotective oleanene-glucuronides in Puerariae Flos.

In order to confirm the constitution of hepatoprotective oleanene glucuronide (OG), HPLC profile analyses of the total OG fractions of both Puerariae Thomsonii Flos (the flowers of Pueraria thomsonii) and Puerariae Lobatae Flos (the flowers of P. lobata) were performed. No remarkable difference in the HPLC profiles with respect to OGs in the flowers was shown, in contrast to those of the roots. By repeated chromatography of the total OG fraction of Puerariae Thomsonii Flos, soyasaponin I (1), kaikasaponin III (2) and kakkasaponin I (3), which had been already isolated from Puerariae Lobatae Flos, were obtained. The hepatoprotective activity of 2 towards immunologically induced liver injury was significantly more effective than that of 1. This information supported previously obtained structure-hepatoprotective relationship data which was measured on another model. The structure-activity relationship information which suggested that the hydroxymethyl group of the galactosyl unit would enhance the hepatoprotective activity was also substantiated.

[Pharmacological studies on small peptide fraction derived from soybean. The effects of small peptide fraction derived from soybean on fatigue, obesity and glycemia in mice].

The present research was an attempt to determine the pharmacological actions as for anti-fatigue, anti-obesity and hypoglycemia of small peptide isolated from soybean in mice. Small peptide administration prevented the decrease in sporting movement induced by concussion stress for 3 h in mice. In addition, it should be noted that the recovery rate of fatigue in 60 min after small peptide administration was over one hundred percentage in comparison with that after pretreatment, while the equivalent dose administration of amino acid mixture with the same small peptide amino acid composition did not prevent the decrease in sporting movement. In gold-thioglucose (500 mg/kg (i.p.))-induced obese mouse body weight gain, liver weight and body lipid level around uterine were significantly reduced by the chronic oral administration of small peptide (200, 1000 mg/kg). Administration in 1000 mg per kg of small peptide significantly lowered hyperglycemia in 30 and 120 min after glucose (3 g/kg (p.o.)) administration, whereas the equivalent amino acid mixture showed no effect. In conclusion, it suggested that small peptide isolated from soybean might have some pharmacological effects of anti-fatigue, anti-obesity, and hypoglycemia.

[Pharmacological studies on puerariae flos. II. The effects of puerariae flos on alcohol-induced unusual metabolism and experimental liver injury in mice].

The present study was designed to examine the effects of methanolic extract (PE-ME), isoflavonoid fraction (PF-IF), triterpenoid saponin fraction (PF-SP) and N-acyl-N1-glucosyl-tryptophan (PF-P) isolated from puerariae flos on alcohol-induced unusual metabolism (as for glucose (BG), triglyceride (TG), and urea nitrogen (BUN) level in blood) and experimental liver injury (model: CCl4- and high fatty food induced) in mice. These alcohol-induced increasing responses were inhibited by the extracted and refined substances from puerariae flos. In short, PF-ME (4500 mg/kg) and PF-P (400 mg/kg) inhibited an increase in BG level induced by alcohol, whereas PF-IF (1000 mg/kg) and PF-SP (1000 mg/kg) did not. Similary, PF-ME and PF-SP inhibited an increase in TG induced by alcohol, whereas PF-IF did not. In addition, PF-IF and PF-SP inhibited increasing BUN level. Still more, PF-IF and PF-SP significantly inhibited an increase in gulutamate oxalacetate transaminase or gulutamate pyruvate transaminase level induced by high-fatty food and CCl4 in control animals. Especially PF-IF (250 mg/kg) administration showed a remarkable effect (inhibition: 76.3%) in control animals. These results suggested that puerariae flos or its combination drugs may be a useful drug as a traditional medicinal system for counteraction to drinking.

[Pharmacological studies on puerariae flos. I. The effects of puerariae flos on alcoholic metabolism and spontaneous movement in mice].

In the general rule, Puerariae Flos or it's combination drugs are used in traditional medicinal system for counteraction to drinking among Japanese and Chinese therapy. One of such drugs is Kakkakaiseito. Here we report the results of investigation on some pharmacological actions including alcoholic metabolism. The experiments were carried out to confirm its actual effect on alcohol, acetaldehyde and ketone body metabolism in the blood and the alteration of behaviour pattern of mice. Drugs used in this study were methanolic extract (PF-ME), isoflavonoid fraction (PF-IF) and triterpenoid saponin fraction (PF-SP) isolated from Puerariae Flos. Each drug was orally administrated to mice. These results were shown as follows: the concentrations of blood alcohol and acetaldehyde decreased more after the treatment with PF-IF (800 mg/kg) than those of the control group. This fact was evidenced remarkable effects with area under the blood concentration-time curve, mean residence time, and variance residence time and values on the moment analysis. However, a reduction effect was not recognized by the treatment with PF-SP (1000 mg/kg). Moreover, PF-ME and PF-IF suppressed the increment of spontaneous movement induced by alcohol administration, whereas PF-SP did not prevent the decrease in the increment caused by alcohol administration. These results support the basis that Puerariae Flos or its combination drugs is used in a traditional medicinal system for counteraction to drinking. However, further investigation is necessary.