Estrogenic activity of the dichloromethane extract from Pueraria mirifica.

Pueraria mirifica and its extracts are widely used as the ingredient(s) in many rejuvenating products. Up to now, the extract of P. mirifica roots that has been used in most studies, is the alcoholic extract. In the present study, we investigated the estrogenic activity using uterotropic and MCF-7 cell proliferation models of the dichloromethane extract as well as the water extract which was obtained from partitioning the ethanolic extract. The results indicated that among the three extracts, i.e. the ethanolic extract (PM1), the water extract (PM2) and dichloromethane extract (PM3), PM3 exhibited the most potent estrogenic activity in both models, followed by PM1. The extracts produced uterotropic activity associated with the increase of water content while uterotropic activity of 17beta-estradiol was related to the increase of muscle mass. The two isoflavonoids, genistein and daidzein, were not the major active phytoestrogens involving the estrogenic activity of these extracts.

Anti-headlice activity of a preparation of Annona squamosa seed extract.

Various parts of Annona squamosa Linn. (custard apple) have long been used in Thai folk medicine. The effectiveness of organic solvent extracts of custard apple seeds and leaves against headlice has been reported. The present study is focused on the efficacy and stability of seed extract prepared as a cream. A petroleum ether extract of seeds was prepared as a 20% w/w oil in water cream and tested for anti-headlice activity in school girls. After a 3 hour-hair exposure to 20 g of freshly prepared custard apple cream, 95.34+/-1.96% of headlice were killed. This killing rate was higher than that obtaned from the control (cream base) or the standard drug (25% benzyl benzoate emulsion). The anti-headlice efficacy of the 6 and 12 month-storage preparations kept in a refrigerator and 12 month-storage at room temperature were 99.19+/-0.60%, 97.55+/-2.06% and 89.47+/-3.64%, respectively, which were not significantly different from that of the freshly prepared cream. This cream did not cause any irritant effect on the scalp or neck skin while benzyl benzoate emulsion produced burning sensation or redness. The results demonstrate that the petroleum ether extract of Annona squamosa seeds prepared as a cream is stable for at least 12 months. The custard apple cream may be, therefore, suitable for use as an alternative therapy against headlice.

Toxicological study of pyridoxal isonicotinoyl hydrazone: acute and subchronic toxicity.

Pyridoxal isonicotinoyl hydrazone (PIH) is a highly effective iron chelator. Acute toxicity testing was performed in mice and rats of both sexes, with 10 mice or rats/sex/group. The LD50 values of PIH in both species were 5 and 1 g/kg given orally and intraperitoneally, respectively. Microscopic examination of tissues from the highest oral dose (6 g/kg) animals that survived 7 days revealed fatty degeneration in the liver. Subchronic toxicity was tested in rats of both sexes, with 8 males and 8 females/group. PIH doses of 100, 400 and 800 mg/kg were given orally for 90 consecutive days. Water was given to the control group. Hematocrit and blood chemistries were analysed at weeks 3, 6, 10 and 13. There were no changes in hematocrit and BUN. PIH at doses of 800 mg/kg caused a significant increase in serum alkaline phosphatase and transaminase levels at week 13. Microscopic examination showed hepatic degeneration in a dose-related fashion. Vascular congestion of the kidney and spleen was also found. No histopathological changes were detected in sections from the stomach and intestine.

Effect of diazepam and phenobarbital sodium on postcoital contraceptive efficacy of ethinyl estradiol in rats.

Diazepam, a well known tranquilizer, and ethinyl estradiol have frequently been prescribed together in rape cases. These two drugs were reported to possess an opposite action on uterine motility. Phenobarbital, a typical enzyme inducer, has been prescribed together with ethinyl estradiol in some cases as a sedative-hypnotic. The present study was, therefore, designed to investigate the possible interferences of diazepam or phenobarbital sodium on postcoital contraceptive efficacy of ethinyl estradiol (4 micrograms/kg/day) in rats. All tested doses of diazepam (1, 2 and 4 mg/kg/day) or phenobarbital sodium (30 and 60 mg/kg/day) appear to have no effect on the efficacy of ethinyl estradiol when either of them was administered from D3 to D5 or from D1 to D5 of pregnancy. In addition, neither diazepam nor phenobarbital sodium at the highest doses used showed an effect on pregnancy.