In the present work we have studied a novel conjugate of DNA alkylating agent chlorambucil with podophyllotoxin, ligand colchicine binding site in tubulin. The target compound was obtained by Steglich esterification podophyllotoxin percentage yield 41%. Results biotesting carried out on carcinoma A549 cell line revealed that at concentration 2 μM caused full depolymerization microtubules withou...

Podophyllum hexandrum Royle, a rhizomatous perennial herb from the Berberidaceae family, is a highly reputed medicinal plant known for its lignan, podophyllotoxin. Podophyllotoxin and its semisynthetic derivativatives are potent anticancer agents. The semisynthetic analogues of podophyllotoxin are also used in the treatment of lung cancer, testicular cancer, neuroblastoma, hepatoma and other tu...

OBJECTIVES To evaluate the efficacy and cost effectiveness of self applied podophyllotoxin 0.5% solution and podophyllotoxin 0.15% cream, compared to clinic applied 25% podophyllin in the treatment of genital warts over 4 weeks. METHODS We conducted a randomised controlled trial in 358 immunocompetent men and women with genital warts of 3 months' duration or less. RESULTS In the principal a...

We have investigated the effects of podophyllotoxin on the dynamic properties of microtubules assembled from pure tubulin dimer. Excess podophyllotoxin causes the complete disassembly of microtubules, through formation of a tubulin-GTP-podophyllotoxin ternary complex with a dissociation rate constant of 160 s-1 at 37 degrees C, similar to that found upon extensive isothermal dilution in this bu...

INTRODUCTION Podophyllotoxin is the starting material for the semi-synthesis of the anti-cancer drugs etoposide, teniposide and etopophos. These compounds have been used for the treatment of lung and testicular cancers as well as certain leukemias. It is also the precursor to a new derivative CPH 82 that is being tested for rheumatoid arthritis in Europe, and it is the precursor to other deriva...

Two new aryltetralin-type lignans, isopodophyllotoxin 7'-O-beta-D-glucopyranosyl-(1-->6)-beta-D-glucopyranoside (1) and 4-demethyl-picropodophyllotoxin 7'-O-beta-D-glucopyranoside (2), along with eight known podophyllotoxin derivatives: 4-demethyl-podophyllotoxin 7'-O-beta-D-glucopyranoside (3), podophyllotoxin 7'-O-beta-D-glucopyranoside (4), deoxypodophyllotoxin (5), picropodophyllotoxin (6),...

OBJECTIVE To evaluate the efficacy-safety ratio of a new topical podophyllotoxin cream 0.5% compared with podophyllotoxin solution 0.5% (Condyline) in male patients with genital warts. METHODS In an observer-blinded controlled study a total of 136 and 133 wart lesions were treated with podophyllotoxin cream 0.5% and podophyllotoxin solution 0.5%, respectively. The preparations were applied tw...

The pharmaceutically important anticancer drugs etoposide and teniposide are derived from podophyllotoxin, a natural product isolated from roots of Podophyllum hexandrum growing in the wild. The overexploitation of this endangered plant has led to the search for alternative sources. Metabolic engineering aimed at constructing the pathway in another host cell is very appealing, but for that appr...

Podophyllotoxin is a natural lignan that is currently being used as a precursor to semi-synthetic anticancer drugs etoposide, teniposide, and etopophos. These compounds have been used for the treatment of lung and testicular cancers as well as certain leukemias (Stahelin and Wartburg 1991; Imbert 1998). The patent for the use of etoposide in such therapies expired in 1995 and since then, etopos...

The binding of [3H]podophyllotoxin to tubulin, measured by a DEAE-cellulose filter paper method, occurs with an affinity constant of 1.8 X 10(6) M-1 (37 degrees at pH 6.7). Like colchicine, approximately 0.8 mol of podophyllotixin are bound per mol of tubulin dimer, and the reaction is entropy-driven (43 cal deg-1 mol-1). At 37 degrees the association rate constant for podophyllotoxin binding i...