podophyllotoxin

Summary

Summary: A lignan (LIGNANS) found in PODOPHYLLIN resin from the roots of PODOPHYLLUM plants. It is a potent spindle poison, toxic if taken internally, and has been used as a cathartic. It is very irritating to skin and mucous membranes, has keratolytic actions, has been used to treat warts and keratoses, and may have antineoplastic properties, as do some of its congeners and derivatives.

Top Publications

  1. Liu J, Sang C, Xu X, Zhang L, Yang X, Hui L, et al. Synthesis and cytotoxic activity on human cancer cells of carbamate derivatives of 4?-(1,2,3-triazol-1-yl)podophyllotoxin. Eur J Med Chem. 2013;64:621-8 pubmed publisher
    Carbamate derivatives of 4?-(1,2,3-triazol-1-yl)podophyllotoxin were synthesized by means of click chemistry, and their cytotoxicities against human cancer cell lines HL-60, A-549, HeLa, and HCT-8 were evaluated...
  2. Colón E, Zaman F, Axelson M, Larsson O, Carlsson Skwirut C, Svechnikov K, et al. Insulin-like growth factor-I is an important antiapoptotic factor for rat leydig cells during postnatal development. Endocrinology. 2007;148:128-39 pubmed
    ..Inhibition of IGF-IR by picropodophyllin decreases the survival of Leydig cells, both in the presence and absence of IGF-I, demonstrating that signaling via the IGF-IR plays an important role in Leydig cell survival. ..
  3. Kushwaha R, Bhattacharya A, Singh B, Singh R. Factors affecting podophyllotoxin yield in the ex situ grown Podophyllum hexandrum, an endangered alpine native of the western Himalayas. J Nat Med. 2012;66:1-7 pubmed publisher
    This study reports an appreciable yield of podophyllotoxin (PDT) in P. hexandrum plants grown ex situ under polyhouse conditions of a temperate locale...
  4. Bala M, Goel H. Radioprotective effect of podophyllotoxin in Saccharomyces cerevisiae. J Environ Pathol Toxicol Oncol. 2004;23:139-44 pubmed
    Recent reports showed that whole extract of Podophyllum hexandrum was radioprotective in mice. Podophyllotoxin is one of the major constituents of the whole extract of Podophyllum...
  5. Liu Y, Zhao C, Li H, Yu M, Gao J, Wang L, et al. Cytotoxicity and apoptosis induced by a new podophyllotoxin glucoside in human hepatoma (HepG2) cells. Can J Physiol Pharmacol. 2010;88:472-9 pubmed publisher
    4-Demethylepipodophyllotoxin 7'-O-beta-D-glucopyranoside (4' DPG), a new podophyllotoxin glucoside with a chemical structure similar to that of 4-demethylpicropodophyllotoxin 7'-O-beta-D-glucopyranoside (4DPG), was isolated from the ..
  6. Barret J, Kruczynski A, Vispé S, Annereau J, Brel V, Guminski Y, et al. F14512, a potent antitumor agent targeting topoisomerase II vectored into cancer cells via the polyamine transport system. Cancer Res. 2008;68:9845-53 pubmed publisher
    ..This work supports the clinical development of F14512 as a novel targeted cytotoxic drug and sheds light on the concept of selective delivery of drugs to tumor cells expressing the PTS. ..
  7. Berim A, Ebel R, Schneider B, Petersen M. UDP-glucose:(6-methoxy)podophyllotoxin 7-O-glucosyltransferase from suspension cultures of Linum nodiflorum. Phytochemistry. 2008;69:374-81 pubmed
    Cell cultures of Linum species store 6-methoxypodophyllotoxin (MPTOX), podophyllotoxin (PTOX) and related lignans as O-glucosides...
  8. Vasilcanu R, Vasilcanu D, Rosengren L, Natalishvili N, Sehat B, Yin S, et al. Picropodophyllin induces downregulation of the insulin-like growth factor 1 receptor: potential mechanistic involvement of Mdm2 and beta-arrestin1. Oncogene. 2008;27:1629-38 pubmed
    ..All together these data suggest that PPP downregulates IGF-1R by interfering with the action of beta-arrestin1/MDM2 as well as the achieved receptor downregulation contributes to the apoptotic effect of PPP. ..
  9. Miao R, Han Y, An L, Yang J, Wang Q. Seleno-podophyllotoxin derivatives induce hepatoma SMMC-7721 cell apoptosis through Bax pathway. Cell Biol Int. 2008;32:217-23 pubmed
    b>Podophyllotoxin is a well known anti-tumor chemical, but because of its strong side effects much effort has been paid to reduce cytotoxicity by modifying its structure...

More Information

Publications62

  1. Ma Y, Fang S, Li H, Han C, Lu Y, Zhao Y, et al. Biological evaluation and molecular modelling study of podophyllotoxin derivatives as potent inhibitors of tubulin polymerization. Chem Biol Drug Des. 2013;82:12-21 pubmed publisher
    Microtubules are considered as important targets of anticancer therapy. Podophyllotoxin and its structural derivative are major microtubule-interfering agents with potent anticancer activity...
  2. Chen J, Tang Y, Li W, Chiou Y, Shieh J, Wang Y. A synthetic podophyllotoxin derivative exerts anti-cancer effects by inducing mitotic arrest and pro-apoptotic ER stress in lung cancer preclinical models. PLoS ONE. 2013;8:e62082 pubmed publisher
    Some potent chemotherapy drugs including tubulin-binding agents had been developed from nature plants, such as podophyllotoxin and paclitaxel...
  3. Komericki P, Akkilic Materna M, Strimitzer T, Aberer W. Efficacy and safety of imiquimod versus podophyllotoxin in the treatment of anogenital warts. Sex Transm Dis. 2011;38:216-8 pubmed publisher
    ..Despite the fact, that imiquimod and podophyllotoxin represent common topical agents, direct comparative studies lack...
  4. Economou M, Wu J, Vasilcanu D, Rosengren L, All Ericsson C, van der Ploeg I, et al. Inhibition of VEGF secretion and experimental choroidal neovascularization by picropodophyllin (PPP), an inhibitor of the insulin-like growth factor-1 receptor. Invest Ophthalmol Vis Sci. 2008;49:2620-6 pubmed publisher
    ..PPP reduces IGF-1-dependent VEGF expression and CNV in vivo. Accordingly, IGF-1R inhibitors may be useful tools in the treatment of conditions associated with CNV, including neovascular AMD. ..
  5. Chattopadhyay S, Bisaria V, Panda A, Srivastava A. Cytotoxicity of in vitro produced podophyllotoxin from Podophyllum hexandrum on human cancer cell line. Nat Prod Res. 2004;18:51-7 pubmed
    b>Podophyllotoxin was produced by cell culture of Podophyllum hexandrum under in vitro culture conditions. A maximum of 4.26 mg/L of podophyllotoxin was produced when P. hexandrum was cultivated in 3 L stirred tank bioreactor...
  6. Stromberg T, Ekman S, Girnita L, Dimberg L, Larsson O, Axelson M, et al. IGF-1 receptor tyrosine kinase inhibition by the cyclolignan PPP induces G2/M-phase accumulation and apoptosis in multiple myeloma cells. Blood. 2006;107:669-78 pubmed
    ..In addition, the expression of mcl-1 and survivin was reduced. Taken together, we suggest that interfering with the IGF-1 RTK by using the cyclolignan PPP offers a novel and selective therapeutic strategy for MM. ..
  7. Lv M, Xu H. Recent advances in semisynthesis, biosynthesis, biological activities, mode of action, and structure-activity relationship of podophyllotoxins: an update (2008-2010). Mini Rev Med Chem. 2011;11:901-9 pubmed
    b>Podophyllotoxin, one of the well-known naturally occurring aryltetralin lignans, has been used as the lead-compound for the preparation of potent anticancer agents, such as etoposide, teniposide, and etopophos...
  8. Yousefzadi M, Sharifi M, Behmanesh M, Ghasempour A, Moyano E, Palazon J. Salicylic acid improves podophyllotoxin production in cell cultures of Linum album by increasing the expression of genes related with its biosynthesis. Biotechnol Lett. 2010;32:1739-43 pubmed publisher
    Treatment of Linum album cell cultures with 10 ?M salicylic acid (SA) for 3 days improved podophyllotoxin (PTOX) production up to 333 ?g/g dry weight (DW): over three times that of the control cultures...
  9. You Y. Podophyllotoxin derivatives: current synthetic approaches for new anticancer agents. Curr Pharm Des. 2005;11:1695-717 pubmed
    b>Podophyllotoxin is an antimitotic natural product. Its inhibitory activity on cell growth led to the development of the clinically valuable anticancer agents, etoposide, teniposide and the water-soluble prodrug, etoposide phosphate...
  10. Zhang Q, Jiang M, Zhao C, Yu M, Zhang H, Ding Y, et al. Apoptosis induced by one new podophyllotoxin glucoside in human carcinoma cells. Toxicology. 2005;212:46-53 pubmed
    4-Demethyl-picropodophyllotoxin 7'-O-beta-D-glucopyranoside (4DPG), a new podophyllotoxin glucoside, was isolated from the rhizomes of Sinopodophyllum emodi (Wall.) Ying and showed cytotoxic effects in human carcinoma cells...
  11. Economou M, Andersson S, Vasilcanu D, All Ericsson C, Menu E, Girnita A, et al. Oral picropodophyllin (PPP) is well tolerated in vivo and inhibits IGF-1R expression and growth of uveal melanoma. Invest Ophthalmol Vis Sci. 2008;49:2337-42 pubmed publisher
    ..PPP decreased VEGF expression in the OCM-1 (P = 0.006) and OCM-8 (P = 0.01) tumors. Oral PPP was well tolerated in vivo, caused total growth inhibition of uveal melanoma xenografts, and decreased VEGF levels in the tumors. ..
  12. Nadeem M, Palni L, Kumar A, Nandi S. Podophyllotoxin content, above- and belowground biomass in relation to altitude in Podophyllum hexandrum populations from Kumaun region of the Indian Central Himalaya. Planta Med. 2007;73:388-91 pubmed
    ..features of Podophyllum hexandrum Royle, a 'critically endangered' medicinal herb and a source of podophyllotoxin, were studied in populations growing in different parts of the Kumaun region of the Indian Central Himalaya...
  13. Jiang R, Zhou J, Hon P, Li S, Zhou Y, Li L, et al. Lignans from Dysosma versipellis with inhibitory effects on prostate cancer cell lines. J Nat Prod. 2007;70:283-6 pubmed
    A new monoepoxylignan, dysosmarol (1), along with eight known compounds, podophyllotoxin (2), 4'-demethylpodophyllotoxin (3), deoxypodophyllotoxin (4), 4'-demethyldeoxypodophyllotoxin (5), diphyllin (6), kaempferol, quercetin, and beta-..
  14. Menu E, Jernberg Wiklund H, Stromberg T, De Raeve H, Girnita L, Larsson O, et al. Inhibiting the IGF-1 receptor tyrosine kinase with the cyclolignan PPP: an in vitro and in vivo study in the 5T33MM mouse model. Blood. 2006;107:655-60 pubmed
    ..These data suggest that the IGF-1RTK inhibitor PPP possesses a marked antitumor activity and strongly points to the possibility of using IGF-1R inhibitors in the treatment of MM. ..
  15. Baldi A, Srivastava A, Bisaria V. Improved podophyllotoxin production by transformed cultures of Linum album. Biotechnol J. 2008;3:1256-63 pubmed publisher
    Various cell and hairy root cultures of L. album were developed and analyzed for podophyllotoxin content. Transformed callus and hairy root cultures developed from infection of stem portions of in vitro-germinated L...
  16. Shin S, Yong Y, Kim C, Lee Y, Lim Y. Deoxypodophyllotoxin induces G2/M cell cycle arrest and apoptosis in HeLa cells. Cancer Lett. 2010;287:231-9 pubmed publisher
  17. Castro M, Miguel del Corral J, Gordaliza M, Garcia P, Gómez Zurita M, García Grávalos M, et al. Synthesis and biological evaluation of new selective cytotoxic cyclolignans derived from podophyllotoxin. J Med Chem. 2004;47:1214-22 pubmed
    b>Podophyllotoxin and some of its derivatives are cyclolignans currently used for removing warts and in the clinical treatment of malign neoplasms...
  18. Gilson R, Ross J, Maw R, Rowen D, Sonnex C, Lacey C. A multicentre, randomised, double-blind, placebo controlled study of cryotherapy versus cryotherapy and podophyllotoxin cream as treatment for external anogenital warts. Sex Transm Infect. 2009;85:514-9 pubmed publisher
    To compare the efficacy and safety of combination therapy with cryotherapy and podophyllotoxin 0.15% cream versus cryotherapy alone in the treatment of anogenital warts. A randomised, double-blind, multicentre controlled trial...
  19. van Fürden B, Humburg A, Fuss E. Influence of methyl jasmonate on podophyllotoxin and 6-methoxypodophyllotoxin accumulation in Linum album cell suspension cultures. Plant Cell Rep. 2005;24:312-7 pubmed
    The accumulation of podophyllotoxin (PTOX) and 6-methoxypodophyllotoxin (6MPTOX) was enhanced about twofold in the suspension culture of Linum album line 2-5 aH following the addition of methyl jasmonate (MeJas) to the cultivation medium,..
  20. Santos E, Lima L, David J, Martins L, Guedes M, David J. Podophyllotoxin and other aryltetralin lignans from Eriope latifolia and Eriope blanchetii. Nat Prod Res. 2011;25:1450-3 pubmed publisher
    Phytochemical investigation of the aerial parts of Eriope blanchetii and E. latifolia (Lamiaceae) yielded podophyllotoxin, as well as the aryltetralin lignans ?- and ?-peltatin and yatein...
  21. Vasilcanu D, Girnita A, Girnita L, Vasilcanu R, Axelson M, Larsson O. The cyclolignan PPP induces activation loop-specific inhibition of tyrosine phosphorylation of the insulin-like growth factor-1 receptor. Link to the phosphatidyl inositol-3 kinase/Akt apoptotic pathway. Oncogene. 2004;23:7854-62 pubmed
    ..PPP was proven not to interfere directly with Akt or any of its downstream molecules in the apoptotic pathway. ..
  22. Klinakis A, Szabolcs M, Chen G, Xuan S, Hibshoosh H, Efstratiadis A. Igf1r as a therapeutic target in a mouse model of basal-like breast cancer. Proc Natl Acad Sci U S A. 2009;106:2359-64 pubmed publisher
    ..PPP also was effective against xenografts of the human basal-like cancer cell line MDA-MB-231, which carries a KRAS(G13D) mutation. ..
  23. Magedov I, Manpadi M, Slambrouck S, Steelant W, Rozhkova E, Przheval skii N, et al. Discovery and investigation of antiproliferative and apoptosis-inducing properties of new heterocyclic podophyllotoxin analogues accessible by a one-step multicomponent synthesis. J Med Chem. 2007;50:5183-92 pubmed
    b>Podophyllotoxin has been extensively used as a lead agent in the development of new anticancer drugs...
  24. Zhao Y, Wang C, Wu Z, Fang J, Zhu L. Synthesis and antitumor activity of novel aroylthiourea derivatives of podophyllotoxin. Invest New Drugs. 2012;30:17-24 pubmed publisher
    A novel series of 4?-[(4-substituted) aroylthiourea] derivatives of podophyllotoxin were synthesized and their abilities to inhibit the growth of cancer cells were investigated by MTT assay...
  25. Menu E, Jernberg Wiklund H, De Raeve H, De Leenheer E, Coulton L, Gallagher O, et al. Targeting the IGF-1R using picropodophyllin in the therapeutical 5T2MM mouse model of multiple myeloma: beneficial effects on tumor growth, angiogenesis, bone disease and survival. Int J Cancer. 2007;121:1857-61 pubmed
    ..The present studies on the biological effects of PPP in the 5T2MM model constitute an important experimental platform for future therapeutic implementation. ..
  26. Sehgal R, Roy S, Kumar V. Evaluation of cytotoxic potential of latex of Calotropis procera and podophyllotoxin in Allium cepa root model. Biocell. 2006;30:9-13 pubmed
    ..meristem model to evaluate the cytotoxic and anti-mitotic activities of latex of Calotropis procera (DL) and podophyllotoxin. Standard cytotoxic drug cyclophosphamide and non-cytotoxic drugs cyprohcptadine and aspirin served as ..
  27. Yousefzadi M, Sharifi M, Behmanesh M, Ghasempour A, Moyano E, Palazon J. The effect of light on gene expression and podophyllotoxin biosynthesis in Linum album cell culture. Plant Physiol Biochem. 2012;56:41-6 pubmed publisher
    b>Podophyllotoxin (PTOX) is a naturally occurring phenolic compound isolated as an active anti-tumor agent...
  28. Yang T, Qi S, Zhao N, Yang Y, Yuan H, Zhang B, et al. Induction of apoptosis through caspase-independent or caspase-9-dependent pathway in mouse and human osteosarcoma cells by a new nitroxyl spin-labeled derivative of podophyllotoxin. Apoptosis. 2013;18:727-38 pubmed publisher
    Previous study has found that a new nitroxyl spin-labeled derivative of podophyllotoxin, 4-[4"-(2",2",6",6"-tetramethyl-1"-piperidinyloxy)amino]-4'-demethyl-epipodophyllotoxin (GP7), can induce apoptosis in ..
  29. Puri S, Nazir A, Chawla R, Arora R, Riyaz Ul Hasan S, Amna T, et al. The endophytic fungus Trametes hirsuta as a novel alternative source of podophyllotoxin and related aryl tetralin lignans. J Biotechnol. 2006;122:494-510 pubmed
    ..This strategy promises to improve the production of these therapeutically important compounds at lower costs...
  30. Gordaliza M, Garcia P, del Corral J, Castro M, Gómez Zurita M. Podophyllotoxin: distribution, sources, applications and new cytotoxic derivatives. Toxicon. 2004;44:441-59 pubmed
    Several podophyllotoxin derivatives modified in the A, B, C, D and E rings were prepared from podophyllotoxin and methyl isoxazopodophyllic acid and evaluated for their cytotoxicity on several neoplastic cell lines...
  31. Kumar A, Kumar V, Alegria A, Malhotra S. Synthetic and application perspectives of azapodophyllotoxins: alternative scaffolds of podophyllotoxin. Curr Med Chem. 2011;18:3853-70 pubmed
    b>Podophyllotoxin (1) has been known to possess anti-tumor activity and is still considered an important lead for research and development of antineoplastic agents...
  32. Zhang J, Zhang Z, Hui L, Chen S, Tian X. Novel semisynthetic spin-labeled derivatives of podophyllotoxin with cytotoxic and antioxidative activity. Bioorg Med Chem Lett. 2010;20:983-6 pubmed publisher
    A series of novel spin-labeled podophyllotoxin derivatives were synthesized by reacting the corresponding N-(1-oxyl-2,2,6,6-tetramethyl-4-piperidinyloxy carbonyl)-amino acids with 4beta-amino-4'-demethylepipodophyllotoxin...
  33. Afroz Alam M, Naik P. Molecular modelling evaluation of the cytotoxic activity of podophyllotoxin analogues. J Comput Aided Mol Des. 2009;23:209-25 pubmed publisher
    b>Podophyllotoxin and its structural derivatives, a class of tubulin polymerization inhibitors, have been the objective of numerous studies to prepare better and safer anti-cancer drugs...
  34. Chen H, Chang X, Du D, Liu W, Liu J, Weng T, et al. Podophyllotoxin-loaded solid lipid nanoparticles for epidermal targeting. J Control Release. 2006;110:296-306 pubmed
    ..of this study was to evaluate solid lipid nanoparticles as the topical carrier for epidermal targeting of podophyllotoxin (POD). The high pressure homogenization was employed to prepare drug-loaded solid lipid nanoparticles...
  35. Jin Y, Chen S, Tian X. Synthesis and biological evaluation of new spin-labeled derivatives of podophyllotoxin. Bioorg Med Chem. 2006;14:3062-8 pubmed
    In order to find compounds with superior bioactivity and less toxicity, a series of spin-labeled podophyllotoxin derivatives were synthesized and tested for the partition coefficients and cytotoxicity against P-388 and A-549...
  36. Vasilcanu D, Weng W, Girnita A, Lui W, Vasilcanu R, Axelson M, et al. The insulin-like growth factor-1 receptor inhibitor PPP produces only very limited resistance in tumor cells exposed to long-term selection. Oncogene. 2006;25:3186-95 pubmed
    ..2 and 0.5 microM. In conclusion, malignant cells develop no or remarkably weak resistance to the IGF-1R inhibitor PPP. ..
  37. Farkya S, Bisaria V, Srivastava A. Biotechnological aspects of the production of the anticancer drug podophyllotoxin. Appl Microbiol Biotechnol. 2004;65:504-19 pubmed
    The natural lignan podophyllotoxin, a dimerized product of two phenylpropanoid moieties which occurs in a few plant species, is a pharmacologically important compound for its anticancer activities...
  38. Girnita A, All Ericsson C, Economou M, Astrom K, Axelson M, Seregard S, et al. The insulin-like growth factor-I receptor inhibitor picropodophyllin causes tumor regression and attenuates mechanisms involved in invasion of uveal melanoma cells. Clin Cancer Res. 2006;12:1383-91 pubmed
    ..Targeting this receptor may therefore comprise a strategy to treat ongoing disease (today incurable) as well as a strategy to prevent development of metastases in patients with primary disease. ..
  39. Lacey C, Goodall R, Tennvall G, Maw R, Kinghorn G, Fisk P, et al. Randomised controlled trial and economic evaluation of podophyllotoxin solution, podophyllotoxin cream, and podophyllin in the treatment of genital warts. Sex Transm Infect. 2003;79:270-5 pubmed
    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...
  40. Li Q, Yan G, Ge T. A fragmentation study of podophyllotoxin and its 4'-demethyl-4beta-substituted derivatives by electrospray ionization ion-trap time-of-flight tandem mass spectrometry. Rapid Commun Mass Spectrom. 2007;21:2843-52 pubmed
    ..spectrometry (MS(1-9)) was used to determine the accurate masses and the fragmentation pathways of protonated podophyllotoxin (1) and its corresponding 4'-demethyl-4beta-substituted derivatives (2-4)...
  41. Eyberger A, Dondapati R, Porter J. Endophyte fungal isolates from Podophyllum peltatum produce podophyllotoxin. J Nat Prod. 2006;69:1121-4 pubmed
    The lignan podophyllotoxin (1) is highly valued as the precursor to clinically useful anticancer drugs. Substantial drug development of this compound class continues, including potential new use for inflammatory disease...
  42. Magedov I, Manpadi M, Rozhkova E, Przheval skii N, Rogelj S, Shors S, et al. Structural simplification of bioactive natural products with multicomponent synthesis: dihydropyridopyrazole analogues of podophyllotoxin. Bioorg Med Chem Lett. 2007;17:1381-5 pubmed
    ..and aliphatic aldehydes leads to the formation of dihydropyridopyrazole analogues of a cytotoxic lignan podophyllotoxin. This new heterocyclic scaffold-based library allows a drastic reduction of the structural complexity of the ..
  43. Kusari S, Zühlke S, Spiteller M. Chemometric evaluation of the anti-cancer pro-drug podophyllotoxin and potential therapeutic analogues in Juniperus and Podophyllum species. Phytochem Anal. 2011;22:128-43 pubmed publisher
    b>Podophyllotoxin, deoxypodophyllotoxin, demethylpodophyllotoxin and podophyllotoxone are four therapeutically potent secondary metabolites...
  44. Mustafa J, Khan S, Ma G, Walker L, Khan I. Synthesis and anticancer activities of fatty acid analogs of podophyllotoxin. Lipids. 2004;39:167-72 pubmed
    Derivatives of podophyllotoxin were prepared by coupling 10 FA with the C4-alpha-hydroxy function of podophyllotoxin...
  45. Kartal M, Konuklugil B, Indrayanto G, Alfermann A. Comparison of different extraction methods for the determination of podophyllotoxin and 6-methoxypodophyllotoxin in Linum species. J Pharm Biomed Anal. 2004;35:441-7 pubmed
    Three extraction methods for analysis of podophyllotoxin and its derivatives from Linum species were compared. No statistical difference on the percentage of recovery were found between the methods...
  46. Duan Z, Choy E, Harmon D, Yang C, Ryu K, Schwab J, et al. Insulin-like growth factor-I receptor tyrosine kinase inhibitor cyclolignan picropodophyllin inhibits proliferation and induces apoptosis in multidrug resistant osteosarcoma cell lines. Mol Cancer Ther. 2009;8:2122-30 pubmed publisher
    ..Our data suggest that inhibition of IGF-IR with PPP offers a novel and selective therapeutic strategy for ostosarcoma, and at the same time, PPP is effective at reversing the drug-resistant phenotype in osteosarcoma cell lines. ..
  47. Chen S, Wang Y, Jin Y, Tian X, Zheng Y, Luo D, et al. Synthesis and anti-HIV-1 activities of novel podophyllotoxin derivatives. Bioorg Med Chem Lett. 2007;17:2091-5 pubmed
    In order to explore the range of biological activities of the podophyllotoxin compound class, a novel series of derivatives of podophyllotoxin, which were conjugates containing stavudine and different structural podophyllotoxin analogues,..
  48. Vasilcanu R, Vasilcanu D, Sehat B, Yin S, Girnita A, Axelson M, et al. Insulin-like growth factor type-I receptor-dependent phosphorylation of extracellular signal-regulated kinase 1/2 but not Akt (protein kinase B) can be induced by picropodophyllin. Mol Pharmacol. 2008;73:930-9 pubmed
    ..Thus, apart from inhibiting the receptor activity, PPP can induce IGF-1R ubiquitination and stimulate ERK in an Mdm2-dependent manner. This response could contribute to the apoptotic effect of PPP. ..
  49. Yin S, Girnita A, Stromberg T, Khan Z, Andersson S, Zheng H, et al. Targeting the insulin-like growth factor-1 receptor by picropodophyllin as a treatment option for glioblastoma. Neuro Oncol. 2010;12:19-27 pubmed publisher
    ..In vivo, PPP-treatment causes dramatic tumor regression not only in subcutaneous xenografts but also in intracerebral xenografts, indicating passage of PPP across the blood-brain barrier. ..
  50. Zhu R, Qin L, Wang M, Wu S, Wang S, Zhang R, et al. Preparation, characterization, and anti-tumor property of podophyllotoxin-loaded solid lipid nanoparticles. Nanotechnology. 2009;20:055702 pubmed publisher
    In an effort to develop an alternative formulation of podophyllotoxin suitable for drug release and delivery, podophyllotoxin-loaded solid lipid nanoparticles (PPT-SLNs) were constructed, characterized and examined for in vitro ..
  51. Qin L, Xue M, Wang W, Zhu R, Wang S, Sun J, et al. The in vitro and in vivo anti-tumor effect of layered double hydroxides nanoparticles as delivery for podophyllotoxin. Int J Pharm. 2010;388:223-30 pubmed publisher
    In this research, we intercalated anti-tumor drug podophyllotoxin (PPT) into layered double hydroxides (LDHs) and investigated the in vitro cytotoxicity to tumor cells, the cellular uptake and in vivo anti-tumor inhibition of PPT-LDH...
  52. Chen H, Bi W, Cao B, Yang Z, Chen S, Shang H, et al. A novel podophyllotoxin derivative (YB-1EPN) induces apoptosis and down-regulates express of P-glycoprotein in multidrug resistance cell line KBV200. Eur J Pharmacol. 2010;627:69-74 pubmed publisher
    Our group synthesized a new potent anti-tumor podophyllotoxin derivative, YB-1EPN. In our study, we found that it was more potent than etoposide (VP-16)...
  53. Marques J, Kim K, Lee C, Costa M, May G, Crow J, et al. Next generation sequencing in predicting gene function in podophyllotoxin biosynthesis. J Biol Chem. 2013;288:466-79 pubmed publisher
    Podophyllum species are sources of (-)-podophyllotoxin, an aryltetralin lignan used for semi-synthesis of various powerful and extensively employed cancer-treating drugs...