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1

Roulland, Emmanuel, Emmanuel Bertounesque, Christiane Huel, and Claude Monneret. "Synthesis of picropodophyllin homolactone." Tetrahedron Letters 41, no. 35 (2000): 6769–73. http://dx.doi.org/10.1016/s0040-4039(00)01136-9.

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2

Roulland, Emmanuel, Emmanuel Bertounesque, Christiane Huel, and Claude Monneret. "ChemInform Abstract: Synthesis of Picropodophyllin Homolactone." ChemInform 31, no. 45 (2000): no. http://dx.doi.org/10.1002/chin.200045231.

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3

Wen, Pu Hong. "Kinetic Investigation of Thermal Decomposition Reactions of Podophyllic Acid and Picropodophyllic Acid." Advanced Materials Research 391-392 (December 2011): 1230–34. http://dx.doi.org/10.4028/www.scientific.net/amr.391-392.1230.

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The thermal behavior and thermal decomposition kinetic parameters of podophyllic acid and picropodophyllic acid in a temperature-programmed mode have been investigated by means of DSC and TG-DTG. The kinetic model functions in differential and integral forms of the thermal decomposition reactions mentioned above for leading stage were established. The kinetic parameters of the apparent activation energy Ea and per-exponential factor A were obtained from analysis of the TG-DTG curves by integral and differential methods. The most probable kinetic model function of the decomposition reaction in
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4

Guo, Hong Zhu, De An Guo, Xue Yan Fei, Ya Jun Cui, and Jun Hua Zheng. "Biotransformation of Podophyllotoxin to Picropodophyllin by Microbes." Journal of Asian Natural Products Research 1, no. 2 (1998): 99–102. http://dx.doi.org/10.1080/10286029808039850.

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5

Ohshima-Hosoyama, Sachiko, Tohru Hosoyama, Laura D. Nelon, and Charles Keller. "IGF-1 receptor inhibition by picropodophyllin in medulloblastoma." Biochemical and Biophysical Research Communications 399, no. 4 (2010): 727–32. http://dx.doi.org/10.1016/j.bbrc.2010.08.009.

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6

Wu, Qi, Ai-Ling Tian, Guido Kroemer, and Oliver Kepp. "Autophagy induction by IGF1R inhibition with picropodophyllin and linsitinib." Autophagy 17, no. 8 (2021): 2046–47. http://dx.doi.org/10.1080/15548627.2021.1936934.

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7

Berkowitz, David B., Sungjo Choi, and Jun-Ho Maeng. "Enzyme-Assisted Asymmetric Total Synthesis of (−)-Podophyllotoxin and (−)-Picropodophyllin." Journal of Organic Chemistry 65, no. 3 (2000): 847–60. http://dx.doi.org/10.1021/jo991582+.

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8

Pohmakotr, Manat, Taweechote Komutkul, Patoomratana Tuchinda, Samrarn Prabpai, Palangpon Kongsaeree, and Vichai Reutrakul. "Syntheses of (±)-thuriferic acid ethyl ester, its analogues and (±)-picropodophyllone." Tetrahedron 61, no. 22 (2005): 5311–21. http://dx.doi.org/10.1016/j.tet.2005.03.069.

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9

Pullin, Robert D. C., Jonathan D. Sellars, and Patrick G. Steel. "Silenes in organic synthesis: a concise synthesis of (±)-epi-picropodophyllin." Organic & Biomolecular Chemistry 5, no. 19 (2007): 3201. http://dx.doi.org/10.1039/b710370k.

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10

Colón, Eugenia, Farasat Zaman, Magnus Axelson, et al. "Insulin-Like Growth Factor-I Is an Important Antiapoptotic Factor for Rat Leydig Cells during Postnatal Development." Endocrinology 148, no. 1 (2007): 128–39. http://dx.doi.org/10.1210/en.2006-0835.

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The present investigation examines the influence of IGF-I and the role of IGF-I receptor (IGF-IR) in the apoptosis/survival of Leydig cells. Immunohistochemical analysis of the rat testis at different ages revealed that the level of the phosphorylated IGF-IR increases from birth to d 20 of postnatal life, remaining high in the adult testis. Western blotting revealed that this level is higher in Leydig cells isolated from 40-d-old than from 10- or 60-d-old rats. Application of the terminal deoxyribonucleotidyl transferase-mediated deoxyuridine triphosphate nick end labeling assay revealed that
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11

Zhao, Jing, Yajing Wang, and Libiao Luan. "Star-Shaped Polycaprolactone-Polyethyleneglycol Copolymer Micelle-Like Nanoparticles for Picropodophyllin Delivery." Journal of Biomedical Nanotechnology 10, no. 8 (2014): 1627–34. http://dx.doi.org/10.1166/jbn.2014.1835.

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12

Hashemi, Jamileh, Claire Worrall, Daiana Vasilcanu, et al. "Molecular Characterization of Acquired Tolerance of Tumor Cells to Picropodophyllin (PPP)." PLoS ONE 6, no. 3 (2011): e14757. http://dx.doi.org/10.1371/journal.pone.0014757.

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13

Lu, Xiaosheng, Ledan Wang, Jie Mei, et al. "Picropodophyllin inhibits epithelial ovarian cancer cells in vitro and in vivo." Biochemical and Biophysical Research Communications 435, no. 3 (2013): 385–90. http://dx.doi.org/10.1016/j.bbrc.2013.04.097.

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14

Berkowitz, David B., Sungjo Choi, and Jun-Ho Maeng. "ChemInform Abstract: Enzyme-Assisted Asymmetric Total Synthesis of (-)-Podophyllotoxin and (-)-Picropodophyllin." ChemInform 31, no. 23 (2010): no. http://dx.doi.org/10.1002/chin.200023243.

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15

FENG, XIAOYING, EIMAN ALEEM, YINGBO LIN, MAGNUS AXELSON, OLLE LARSSON, and THOMAS STRÖMBERG. "Multiple antitumor effects of picropodophyllin in colon carcinoma cell lines: Clinical implications." International Journal of Oncology 40, no. 4 (2011): 1251–58. http://dx.doi.org/10.3892/ijo.2011.1281.

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16

Wu, Xuping, Linda Sooman, Malin Wickström, et al. "Alternative Cytotoxic Effects of the Postulated IGF-IR Inhibitor Picropodophyllin In Vitro." Molecular Cancer Therapeutics 12, no. 8 (2013): 1526–36. http://dx.doi.org/10.1158/1535-7163.mct-13-0091.

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17

Yin, Shu-Cheng, Wei Guo, and Ze-Zhang Tao. "Picropodophyllin inhibits tumor growth of human nasopharyngeal carcinoma in a mouse model." Biochemical and Biophysical Research Communications 439, no. 1 (2013): 1–5. http://dx.doi.org/10.1016/j.bbrc.2013.08.050.

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18

Vitale, Maxime, Guillaume Prestat, David Lopes, et al. "New Picropodophyllin Analogs via Palladium-Catalyzed Allylic Alkylation−Hiyama Cross-Coupling Sequences." Journal of Organic Chemistry 73, no. 15 (2008): 5795–805. http://dx.doi.org/10.1021/jo800707q.

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19

Ogiku, Tsuyoshi, Shin-ichi Yoshida, Tooru Kuroda, Masami Takahashi, Hiroshi Ohmizu, and Tameo Iwasaki. "Syntheses of Aryltetralin Lignans: Concise Syntheses of (±)-Isopodophyllotoxone, (±)-Picropodophyllone and Their Related Compounds." Bulletin of the Chemical Society of Japan 65, no. 12 (1992): 3495–97. http://dx.doi.org/10.1246/bcsj.65.3495.

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20

TOMIZAWA, MINORU, FUMINOBU SHINOZAKI, YASUFUMI MOTOYOSHI, TAKAO SUGIYAMA, SHIGENORI YAMAMOTO, and MAKOTO SUEISHI. "Picropodophyllin and sorafenib synergistically suppress the proliferation and motility of hepatocellular carcinoma cells." Oncology Letters 8, no. 5 (2014): 2023–26. http://dx.doi.org/10.3892/ol.2014.2484.

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21

OGIKU, T., S. YOSHIDA, T. KURODA, M. TAKAHASHI, H. OHMIZU, and T. IWASAKI. "ChemInform Abstract: Syntheses of Aryltetralin Lignans: Concise Syntheses of (.+-.)- Isopodophyllotoxone, (.+-.)-Picropodophyllone and Related Compounds." ChemInform 24, no. 15 (2010): no. http://dx.doi.org/10.1002/chin.199315280.

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22

Wong Te Fong, Anne-Christine, Thomas R. Eykyn, Harry G. Parkes, et al. "Abstract B61: Picropodophyllin (PPP) increases glucose metabolism and lactate production in paediatric glioblastoma cells." Clinical Cancer Research 18, no. 10 Supplement (2012): B61. http://dx.doi.org/10.1158/1078-0432.mechres-b61.

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23

Meresse, Philippe, Claude Monneret та Emmanuel Bertounesque. "Synthesis of podophyllotoxin analogues: δ-lactone-containing picropodophyllin, podophyllotoxin and 4′-demethyl-epipodophyllotoxin derivatives". Tetrahedron 60, № 11 (2004): 2657–71. http://dx.doi.org/10.1016/j.tet.2004.01.017.

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24

Lemaire, Miguel, Charlotte Fristedt, Prasoon Agarwal, et al. "The HDAC Inhibitor LBH589 Enhances the Antimyeloma Effects of the IGF-1RTK Inhibitor Picropodophyllin." Clinical Cancer Research 18, no. 8 (2012): 2230–39. http://dx.doi.org/10.1158/1078-0432.ccr-11-1764.

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25

Zhang, Qi, Jing Pan, Ronald A. Lubet, Yian Wang, and Ming You. "Targeting the insulin-like growth factor-1 receptor by picropodophyllin for lung cancer chemoprevention." Molecular Carcinogenesis 54, S1 (2014): E129—E137. http://dx.doi.org/10.1002/mc.22206.

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26

Bieghs, Liesbeth, Susanne Lub, Karel Fostier, et al. "The IGF-1 receptor inhibitor picropodophyllin potentiates the anti-myeloma activity of a BH3-mimetic." Oncotarget 5, no. 22 (2014): 11193–208. http://dx.doi.org/10.18632/oncotarget.1933.

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27

Dong, Lin, Meirong Du, and Qianzhou Lv. "Picropodophyllin inhibits type I endometrial cancer cell proliferation via disruption of the PI3K/Akt pathway." Acta Biochimica et Biophysica Sinica 51, no. 7 (2019): 753–60. http://dx.doi.org/10.1093/abbs/gmz055.

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Abstract The type-I insulin-like growth factor receptor (IGF-IR) is overexpressed in endometrial cancer. High IGF-IR expression was considered as an important prognostic factor for tumor progression. The purpose of this study was to investigate the role and molecular mechanism of IGF-IR inhibitor picropodophyllin (PPP) in the growth and development of endometrial cancer. High expression of IGF-IR was observed in endometrial cancer tissues, as well as in ECC-1 and KLE cell lines. PPP suppressed the number of clones of ECC-1 and KLE cell lines; however, it had no significant effect on HEC-1-A ce
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28

Yoshida, Shin-ichi, Takeshi Yamanaka, Tutomu Miyake, Yasunori Moritani, Hiroshi Ohmizu, and Tameo Iwasaki. "Asymmetric syntheses of lignans utilizing novel diastereoselective Michael addition of cyanohydrin: Syntheses of (+)-fargesin and (−)-picropodophyllone." Tetrahedron 53, no. 28 (1997): 9585–98. http://dx.doi.org/10.1016/s0040-4020(97)00643-1.

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29

Yin, S., A. Girnita, T. Stromberg, et al. "Targeting the insulin-like growth factor-1 receptor by picropodophyllin as a treatment option for glioblastoma." Neuro-Oncology 12, no. 1 (2009): 19–27. http://dx.doi.org/10.1093/neuonc/nop008.

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30

YOSHIDA, S., T. YAMANAKA, T. MIYAKE, Y. MORITANI, H. OHMIZU, and T. IWASAKI. "ChemInform Abstract: Asymmetric Syntheses of Lignans Utilizing Novel Diastereoselective Michael Addition of Cyanohydrin: Syntheses of (+)-Fargesin and (-)- Picropodophyllone." ChemInform 28, no. 50 (2010): no. http://dx.doi.org/10.1002/chin.199750276.

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31

Waraky, Ahmed, Karen Akopyan, Vendela Parrow, et al. "Picropodophyllin causes mitotic arrest and catastrophe by depolymerizing microtubules via Insulin-like growth factor-1 receptor-independent mechanism." Oncotarget 5, no. 18 (2014): 8379–92. http://dx.doi.org/10.18632/oncotarget.2292.

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32

Economou, Mario A., Sandra Andersson, Diana Vasilcanu, et al. "Oral Picropodophyllin (PPP) Is Well Tolerated In Vivo and Inhibits IGF-1R Expression and Growth of Uveal Melanoma." Investigative Opthalmology & Visual Science 49, no. 6 (2008): 2337. http://dx.doi.org/10.1167/iovs.07-0819.

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33

Economou, Mario A., Sandra Andersson, Diana Vasilcanu, et al. "Oral picropodophyllin (PPP) is well tolerated in vivo and inhibits IGF-1R expression and growth of uveal melanoma." Acta Ophthalmologica 86, esis4 (2008): 35–41. http://dx.doi.org/10.1111/j.1755-3768.2008.01184.x.

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34

Jiang, Li-hua, Nian-yun Yang, Xiao-lin Yuan та ін. "Microarray Analysis of mRNA and MicroRNA Expression Profile Reveals the Role ofβ-Sitosterol-D-glucoside in the Proliferation of Neural Stem Cell". Evidence-Based Complementary and Alternative Medicine 2013 (2013): 1–12. http://dx.doi.org/10.1155/2013/360302.

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Neural stem cells (NSCs) are self-regenerating cells, but their regenerative capacity is limited. The present study was conducted to investigate the effect ofβ-sitosterol-D-glucoside (BSSG) on the proliferation of hippocampal NSCs and to determine the corresponding molecular mechanism. Results of CCK-8 assay showed that BSSG significantly increased NSC proliferation and the effectiveness of BSSG was similar to that of basic fibroblast growth factor and epidermal growth factor. mRNA expression profiling showed that 960 genes were differentially expressed after NSCs were treated with BSSG. Among
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35

Conti, Laura, Gabriella Regis, Angela Longo та ін. "In the absence of IGF-1 signaling, IFN-γ suppresses human malignant T-cell growth". Blood 109, № 6 (2006): 2496–504. http://dx.doi.org/10.1182/blood-2006-07-034231.

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Abstract Several approaches to target insulin-like growth factor-1 (IGF-1) signaling have resulted in the inhibition of the growth of a broad range of tumor cells. Malignant T cells are insensitive to the antiproliferative effects of the interferon-γ (IFN-γ)/signal transducer and activator of transcription 1 (STAT1) pathway because of the IGF-1–dependent internalization of the IFN-γR2 signaling chain. Here we show that human malignant T cells are also resistant to the growth inhibitory effect of both the IGF-1 receptor–specific inhibitor picropodophyllin (PPP) and retrovirus-mediated gene tran
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36

Gong, Wan, Naidan Zhang, Gang Cheng, et al. "Rehmannia glutinosa Libosch Extracts Prevent Bone Loss and Architectural Deterioration and Enhance Osteoblastic Bone Formation by Regulating the IGF-1/PI3K/mTOR Pathway in Streptozotocin-Induced Diabetic Rats." International Journal of Molecular Sciences 20, no. 16 (2019): 3964. http://dx.doi.org/10.3390/ijms20163964.

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Rehmanniae Radix Praeparata (RR, named as Shudihuang in traditional Chinese medicine), the steamed roots of Rehmannia glutinosa Libosch (Scrophulariaceae), has been demonstrated to have anti-diabetic and anti-osteoporotic activities. This study aimed to explore the protective effect and underlying mechanism of RR on diabetes-induced bone loss. It was found that RR regulated the alkaline phosphatase activity and osteocalcin level, enhanced bone mineral density, and improved the bone microarchitecture in diabetic rats. The catalpol (CAT), acteoside (ACT), and echinacoside (ECH) from RR increased
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37

WU, YONG-TAO, BAO-JUN WANG, SHENG-WU MIAO, and JIAN-JUN GAO. "Picropodophyllin inhibits the growth of Ewing's sarcoma cells through the insulin-like growth factor-1 receptor/Akt signaling pathway." Molecular Medicine Reports 12, no. 5 (2015): 7045–50. http://dx.doi.org/10.3892/mmr.2015.4266.

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38

Liao, Fenfang, Yongheng Chen, Qingqing Wu, et al. "Selective elimination of CML stem/progenitor cells by picropodophyllin in vitro and in vivo is associated with p53 activation." Biochemical and Biophysical Research Communications 579 (November 2021): 1–7. http://dx.doi.org/10.1016/j.bbrc.2021.09.029.

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39

Vasilcanu, R., D. Vasilcanu, L. Rosengren та ін. "Picropodophyllin induces downregulation of the insulin-like growth factor 1 receptor: potential mechanistic involvement of Mdm2 and β-arrestin1". Oncogene 27, № 11 (2007): 1629–38. http://dx.doi.org/10.1038/sj.onc.1210797.

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40

Kayacik, Nurcin, Hasan Kurter, Tolga Sever, Yasemin Basbinar, and Gizem Calibasi‑Kocal. "Picropodophyllin, an IGF‑1 receptor inhibitor, enhances oxaliplatin efficacy in chemoresistant colorectal cancer HCT116 cells by reducing metastatic potential." Oncology Letters 29, no. 5 (2025): 1–12. https://doi.org/10.3892/ol.2025.14966.

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41

Mo, Hai-Ying, Qi-Yao Wei, Qiu-Hua Zhong, et al. "Cytochrome P450 27C1 Level Dictates Lung Cancer Tumorigenicity and Sensitivity towards Multiple Anticancer Agents and Its Potential Interplay with the IGF-1R/Akt/p53 Signaling Pathway." International Journal of Molecular Sciences 23, no. 14 (2022): 7853. http://dx.doi.org/10.3390/ijms23147853.

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Cytochrome P450 enzymes (CYP450s) exert mighty catalytic actions in cellular metabolism and detoxication, which play pivotal roles in cell fate determination. Preliminary data shows differential expression levels of CYP27C1, one of the “orphan P450s” in human lung cancer cell lines. Here, we study the functions of CYP27C1 in lung cancer progression and drug endurance, and explore its potential to be a diagnostic and therapeutic target for lung cancer management. Quantitative real-time PCR and immunoblot assays were conducted to estimate the transcription and protein expression level of CYP27C1
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42

Menu, Eline, Helena Jernberg-Wiklund, Thomas Stromberg, 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 107, no. 2 (2006): 655–60. http://dx.doi.org/10.1182/blood-2005-01-0293.

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AbstractInsulin-like growth factor 1 (IGF-1) plays a pleiotropic role in multiple myeloma (MM), that is, in survival, proliferation, chemotaxis, and angiogenesis. Strategies targeting the IGF-1 receptor (IGF-1R) may therefore be important to develop efficient anti-MM agents. In this work we investigated the effect of an IGF-1R tyrosine kinase (IGF-1RTK) inhibitor (picropodophyllin or PPP) in the 5T33MM mouse model. In vitro data showed that PPP reduced IGF-1R autophosphorylation and downstream ERK activation, leading to inhibition of IGF-1–stimulated proliferation and vascular endothelial grow
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43

Takata, Sho, Hiromi Sakata-Haga, Hiroki Shimada, et al. "LIF–IGF Axis Contributes to the Proliferation of Neural Progenitor Cells in Developing Rat Cerebrum." International Journal of Molecular Sciences 23, no. 21 (2022): 13199. http://dx.doi.org/10.3390/ijms232113199.

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In rodent models, leukemia inhibitory factor (LIF) is involved in cerebral development via the placenta, and maternal immune activation is linked to psychiatric disorders in the child. However, whether LIF acts directly on neural progenitor cells (NPCs) remains unclear. This study performed DNA microarray analysis and quantitative RT-PCR on the fetal cerebrum after maternal intraperitoneal or fetal intracerebral ventricular injection of LIF at day 14.5 (E14.5) and determined that the expression of insulin-like growth factors (IGF)-1 and -2 was induced by LIF. Physiological IGF-1 and IGF-2 leve
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44

Razuvaev, Anton, Bimma Henderson, Leonard Girnita, et al. "The cyclolignan picropodophyllin attenuates intimal hyperplasia after rat carotid balloon injury by blocking insulin-like growth factor-1 receptor signaling." Journal of Vascular Surgery 46, no. 1 (2007): 108–15. http://dx.doi.org/10.1016/j.jvs.2007.02.066.

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45

Economou, Mario A., Jiangmei Wu, Daiana Vasilcanu, et al. "Inhibition of VEGF Secretion and Experimental Choroidal Neovascularization by Picropodophyllin (PPP), an Inhibitor of the Insulin-like Growth Factor-1 Receptor." Investigative Opthalmology & Visual Science 49, no. 6 (2008): 2620. http://dx.doi.org/10.1167/iovs.07-0742.

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46

Economou, Mario A., Jiangmei Wu, Daiana Vasilcanu, et al. "Inhibition of VEGF secretion and experimental choroidal neovascularization by picropodophyllin (PPP), an inhibitor of the insulin-like growth factor-1 receptor." Acta Ophthalmologica 86, esis4 (2008): 42–49. http://dx.doi.org/10.1111/j.1755-3768.2008.01185.x.

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47

Wu, Qi, Ai-Ling Tian, Bei Li, et al. "IGF1 receptor inhibition amplifies the effects of cancer drugs by autophagy and immune-dependent mechanisms−." Journal for ImmunoTherapy of Cancer 9, no. 6 (2021): e002722. http://dx.doi.org/10.1136/jitc-2021-002722.

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BackgroundPharmacological autophagy enhancement constitutes a preclinically validated strategy for preventing or treating most major age-associated diseases. Driven by this consideration, we performed a high-content/high-throughput screen on 65 000 distinct compounds on a robotized fluorescence microscopy platform to identify novel autophagy inducers.ResultsHere, we report the discovery of picropodophyllin (PPP) as a potent inducer of autophagic flux that acts on-target, as an inhibitor of the tyrosine kinase activity of the insulin-like growth factor-1 receptor (IGF1R). Thus, PPP lost its aut
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48

E, Changyong, Jing Li, Dan Shao, et al. "The Insulin-Like Growth Factor-I Receptor Inhibitor Picropodophyllin-Induced Selective Apoptosis of Hepatocellular Carcinoma Cell Through a Caspase-Dependent Mitochondrial Pathway." Oncology Research Featuring Preclinical and Clinical Cancer Therapeutics 21, no. 2 (2014): 103–10. http://dx.doi.org/10.3727/096504013x13808175127324.

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49

Girnita, Ada, Charlotta All-Ericsson, Mario A. Economou, et al. "The insulin-like growth factor-I receptor inhibitor picropodophyllin causes tumor regression and attenuates mechanisms involved in invasion of uveal melanoma cells." Clinical Cancer Research 12, no. 4 (2006): 1383–91. http://dx.doi.org/10.1158/1078-0432.ccr-05-1106.

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50

Duan, Zhenfeng, Edwin Choy, David Harmon, et al. "Insulin-like growth factor-I receptor tyrosine kinase inhibitor cyclolignan picropodophyllin inhibits proliferation and induces apoptosis in multidrug resistant osteosarcoma cell lines." Molecular Cancer Therapeutics 8, no. 8 (2009): 2122–30. http://dx.doi.org/10.1158/1535-7163.mct-09-0115.

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