Tobishi Pharmaceutical Co. Ltd.

Cernitin pollen-extract (Cernilton, CN) is a preparation made from eight kinds of pollen and has been used for various prostatic diseases in Japan and Europe. We reported previously that CN possessed a recovery action on the sex-hormone-induced nonbacterial prostatitis in rats. To clarify the possible mechanism of action of CN, we investigated the effects of CN on inflammatory cytokines (IL-1 beta, IL-6 and TNF-alpha) in the same model. Aged Wistar rats were castrated and injected 17 beta-estradiol (0.25 mg/kg/day, s.c.) for 30 days. CN (630 and 1,260 mg/kg, p.o.) or testosterone (2.5 mg/kg, s.c.) was administered for the last 14 days of the treatment of 17 beta-estradiol. In control rats, prostatic IL-6 and TNF-alpha contents were increased approximately 2-3 fold, and acinar glandular inflammation and stromal proliferation were found histopathologically, as compared with those of intact rats. On the other hand, CN decreased the increased contents of cytokines in a dose-dependent manner. The histopathological changes mentioned above were restored in rats treated with 1,260 mg/kg. Testosterone also ameliorated them significantly. These results indicate that CN has an anti-inflammatory action, and that the inhibitory effect of CN on the prostatic inflammatory cytokine is an important factor in its action.

The one-step transformation of 2- or 3-(1-hydroxylalkyl)-2, 3-dihydrobenzofurans, e.g., I, to the 2- or 3-acylbenzofurans, e.g., II, with N-bromosuccinimide was performed with good yields.The reaction is characterized to take place via the continuous bromination-dehydrobromination process.Yields are dependent on the solvent and the kind of additive compounds as a scavenger of the hydrogen bromide by-produced during the reaction.

An antitumor morphinan alkaloid, sinococuline (I), was isolated from the MeOH extract of C. trilobus.Its structure was determined by spectroscopic anal.The antitumor activity of I against sarcoma 180A and leukemia P388 is described.