Podophyllum derivatives (CPH 82) compared with placebo in the treatment of rheumatoid arthritis.

The efficacy, tolerance, and safety of CPH 82 (semisynthetic lignan glycosides) (Conpharm AB) for patients with rheumatoid arthritis (RA) were assessed in a 12-week double-blind placebo-controlled study. Thirteen patients out of 15 in the CPH 82 group and 10 out of 15 in the placebo group completed the study. No improvement was seen in placebo treated patients. Patients treated with CPH 82 showed a statistically significant improvement in most clinical and immunological variables. Some patients treated with CPH 82 reported gastrointestinal discomfort (diarrhoea and abdominal pain).

Antitumor agents, 99. Synthetic ring C aromatized podophyllotoxin analogues as potential inhibitors of human DNA topoisomerase II.

Several ring C aromatized analogues of podophyllotoxin were synthesized for testing against human DNA topoisomerase II. The results indicate that aromatization of ring C gave rise to no inhibition of this enzyme at 200 microM. A comparison of the cytotoxicity among these compounds also demonstrates that a free hydroxyl group at C-4 contributes to significant cytotoxicity.

Determination of the aryltetralin lignan content of podophyllum resins and roots/rhizomes.

A simple, quantitatively reproducible method for determining the aryltetralin lignan content of the resins and roots/rhizomes of Podophyllum hexandrum and P. peltatum is described. The method confirms that P. hexandrum resins and roots/rhizomes contain approximately four times the quantity of lignans as do those of P. peltatum and also that there is a significant variation in the lignan content of P. hexandrum resins.

An investigation of the antiviral activity of Podophyllum peltatum.

The antiviral activity of an aqueous extract of Podophyllum peltatum was investigated. The extract was fractionated by reversed-phase chromatography, and podophyllotoxin was found to be the most active component in inhibiting the replication of measles and herpes simplex type I viruses. beta-Peltatin and desoxypodophyllotoxin produced marginal antiviral effects, while alpha-peltatin and picropodophyllotoxin were inactive at the levels tested.