Category Ranking
98%
Total Visits
921
Avg Visit Duration
2 minutes
Citations
20
Article Abstract
Podophyllotoxin is a natural occurring aryltetralin lignin with pronounced cytotoxic activity. However, its clinical application for cancer treatment has been blocked due to its poor water solubility and selectivity. In this work, biotin as a tumor specific ligand was coupled with β-cyclodextrin and the resulting biotin modified β-cyclodextrin was used to complex with podophyllotoxin to improve its aqueous solubility and tumor selectivity. The solubility of β-cyclodextrin was greatly enhanced(>16 times) by conjugating with biotin. podophyllotoxin/ mono-6-biotin-amino-6-deoxy-β-cyclodextrin inclusion complex was prepared by freeze-drying method and the complex behavior between mono-6-biotin-amino-6-deoxy-β-cyclodextrin and podophyllotoxin was studied by water solubility, phase solubility, Job's plot, UV spectroscopy, Proton Nuclear Magnetic Resonance, Rotating-frame Overhauser Effect Spectroscopy, Powder X-ray diffraction and Scanning electron microscopy. The solubility of podophyllotoxin/ mono-6-biotin-amino-6-deoxy-β-cyclodextrin complex was greatly improved(9 times) compared with Podophyllotoxin. The stability constant of podophyllotoxin/ mono-6-biotin-amino-6-deoxy-β-cyclodextrin complex (K= 415.29 M) was 3.2 times that of podophyllotoxin/β-cyclodextrin complex. The possible inclusion mode of podophyllotoxin/mono-6-biotin-amino-6-deoxy-β-cyclodextrin complex was inferred from the Proton Nuclear Magnetic Resonance and Rotating-frame Overhauser Effect Spectroscopy. The cellular uptake study showed that the introduction of biotin increased the cellular uptake of rhodamine-B/mono-6-biotin-amino-6-deoxy-β-cyclodextrin complex. Moreover, cell cytotoxicity study showed that the antitumor activity of podophyllotoxin/ mono-6-biotin-amino-6-deoxy-β-cyclodextrin complex was more potent than podophyllotoxin/β-cyclodextrin complex and free podophyllotoxin. The superior water solubility and enhanced cytotoxicity suggested that the mono-6-biotin-amino-6-deoxy-β-cyclodextrin associated inclusion complex might be a potential and promising delivery system for hydrophobic chemotherapeutics such as podophyllotoxin.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.ejps.2021.105745 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Background: Angioimmunoblastic T-cell lymphoma (AITL) is a rare and aggressive form of peripheral T-cell lymphoma, accounting for 1 - 2% of non-Hodgkin lymphomas. Diagnosis is challenging, and there is no established standard first-line treatment. This case report highlights a rare progression from AITL to therapy-related acute myeloid leukemia (AML-pCT) following cytotoxic chemotherapy.
View Article and Find Full Text PDFA Case of Hepatosplenic Gamma Delta T Cell Lymphoma With Concomitant Bone Marrow Aplasia Following Azathioprine Therapy, Treatment Course and Review of the Literature.
Cancer Rep (Hoboken)
September 2025
Department of Oncology and Haematology, Klinikum Oldenburg and Faculty of Medicine, University of Oldenburg, Oldenburg, Germany.
Background: Hepatosplenic T-cell lymphoma (HSTCL) is a rare and aggressive subtype of peripheral T-cell lymphoma with a poor prognosis, primarily affecting young adult males, many with a background of immunosuppression or autoimmune disease.
Case: We present the case of a 27-year-old male previously treated with azathioprine who developed pancytopenia. Bone marrow biopsy revealed severe aplasia with partial infiltration by gamma-delta T-lymphocytes (Tγδ).
Mechanisms of podophyllotoxin-induced enterotoxicity: A multi-omics integration of gut microbiota, short-chain fatty acids, and inflammatory mediators.
Toxicology
September 2025
Luoyang key laboratory of transplantation and immunological studies for haematological diseases, Department of Clinical Laboratory, The First Affiliated Hospital, and College of Clinical Medicine of Henan University of Science and Technology, Luoyang 471003, China. Electronic address:
Podophyllotoxin (PPT), a lignan extracted from the roots and stems of Podophyllum species, exhibits significant enterotoxicity that limits its clinical application. However, its underlying mechanisms remain unclear. This study aimed to elucidate the mechanisms underlying PPT-induced enterotoxicity.
View Article and Find Full Text PDFNovel Aza-podophyllotoxin Derivative Inhibits Growth of Triple-Negative Breast Cancer.
ACS Omega
August 2025
Department of Cell, Developmental and Cancer Biology, Oregon Health & Science University, Portland, Oregon 97239, United States.
Triple-negative breast cancer (TNBC), the most aggressive type of breast cancer, has high rates of metastasis and recurrence and represents 15-20% of diagnosed breast cancer cases. Most women with TNBC experience recurrence following curative treatment for early-stage breast cancer. We have identified CET022, a novel small molecule, and shown that it inhibits TNBC growth and clonogenic potential in multiple cell lines (MDA-MB-231, MDA-MB-468, 4T1, and EMT6).
View Article and Find Full Text PDFEye Salvage and Vision Preservation in High-Risk Intraocular Retinoblastoma Patients: Long-Term Results From the Prospective Phase II AIEOP RTB 012 Study.
Cancer Med
September 2025
Onco-Hematology, Cell Therapy, Gene Therapies and Hemopoietic Transplant, Bambino Gesù Children's Hospital, IRCCS, Rome, Italy.
Introduction: This study presents the outcomes of high-risk group retinoblastoma (Rb) patients enrolled in the AIEOP RTB 012 Protocol.
Methods: Patients with intraocular unilateral Rb classified as group C/D according to "International Intraocular Retinoblastoma Classification" (IIRC), as well as those with bilateral Rb with at least one eye group C/D/E-IIRC, were treated with four cycles of carboplatin/etoposide combined with focal treatments. The primary endpoint was to evaluate ocular event-free survival (EFS) and overall survival (OS), where events were defined as the need for radiotherapy, eye enucleation, and second-line treatment.