A number of podophyllotoxin derivatives (3A-3J) had been designed and synthesized, and their biological activities were evaluated in this study. Moreover, the antiproliferation activities of these compounds against four human cancer cell lines (HepG2, HeLa, A549, and MCF-7) were also tested. The results indicated that the most promising compound 3D displayed potent inhibitory activity over the four human cancer cell lines and was further demonstrated to have potent tubulin polymerization inhibitory effects without damaging the non-cancer cells. Additionally, 3D was verified to effectively interfere with tubulin and could prevent the mitosis of cancer cells, leading to cell cycle arrest and eventually inducing apoptosis in a dose- and time-dependent manner. Moreover, the Western blotting and siRNA results showed that Bcl-2 was downregulated in HepG2 cells treated with 3D. Finally, the molecular docking simulation results revealed that 3D could fit well in the colchicine-binding pocket. Taken together, this study has provided certain novel antitubulin agents for possible cancer chemotherapy.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1002/cbdv.201800289 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Design, synthesis and activity evaluation of reduction-responsive anticancer peptide temporin-1CEa drug conjugates.
Bioorg Chem
January 2025
Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China. Electronic address:
Membranes that destroy anticancer peptides can bind to negatively charged cancer cell membranes through electrostatic interactions, destroying their functions and leading to cancer cell necrosis. Temporin-1CEa, obtained from the skin secretions of the Chinese frog Rana chensinensis, is an anticancer peptide with 17 amino acid residues that exhibits concentration-dependent cytotoxicity against a variety of cancer cell lines, although it has no obvious cytotoxicity to normal HUVECs. In this work, we designed and synthesized 12 derivative peptides through double-cysteine scanning of temporin-1CEa-truncated peptides.
View Article and Find Full Text PDFComprehensive Biotechnological Strategies for Podophyllotoxin Production from Plant and Microbial Sources.
Planta Med
January 2025
Department of Biotechnology, Thapar Institute of Engineering and Technology, Patiala, Punjab, India.
Podophyllotoxin is derived from plant sources and exhibits strong anticancer activity. However, limited natural availability and environmental impacts from traditional extraction methods drive the search for alternative production approaches. This review explores diverse strategies for sustainable podophyllotoxin synthesis, including biosynthesis, semi-synthesis, and biotransformation.
View Article and Find Full Text PDFCurrent developments in PI3K-based anticancer agents: Designing strategies, biological activity, selectivity, structure-activity correlation, and docking insight.
Bioorg Chem
January 2025
Integrated Drug Discovery Centre, Department of Pharmaceutical Chemistry, Acharya & BM Reddy College of Pharmacy, Bengaluru 560107, Karnataka, India.
Article Synopsis
- The phosphatidylinositol-3 kinase (PI3K) pathway is crucial in various cancers, making it an attractive target for cancer therapies due to its role in cell survival and metastasis.
- Mutations or overexpression in PI3K genes (PIK3CA, PIK3CB, PIK3CD, PIK3CG) lead to treatment failures, prompting ongoing clinical trials of PI3K inhibitors to combat drug resistance.
- Many PI3K inhibitors have faced withdrawal due to safety concerns, but research continues on promising compounds with unique scaffolds to improve therapy efficacy and safety.
Cost-effectiveness analysis of benmelstobart, anlotinib, and chemotherapy in extensive-stage small-cell lung cancer.
Front Immunol
December 2024
Department of Emergency Medicine, Mindong Hospital Affiliated to Fujian Medical University, Ningde, China.
Background: The ETER701 trial assessed the efficacy and safety of benmelstobart combined with anlotinib plus etoposide/cisplatin (BEN-AL-EC) as a first-line therapy for extensive-stage small-cell lung cancer (ES-SCLC). Results indicated that BEN-AL-EC, when compared with placebo in combination with etoposide/cisplatin (PLB-EC), significantly enhanced both progression-free and overall survival rates, while demonstrating an acceptable safety profile among patients with ES-SCLC. However, BEN-AL-EC is expensive, necessitating its cost-effectiveness analysis.
View Article and Find Full Text PDFFrom Plant to Patient: A Historical Perspective and Review of Selected Medicinal Plants in Dermatology.
JID Innov
January 2025
Department of Dermatology, Emory University School of Medicine, Atlanta, Georgia, USA.
Skin conditions are a common health concern faced by patients of all ages. For thousands of years, plants have been used to treat various skin conditions, including acne, vitiligo, and psoriasis, to name a few. Today, with increasing patient preference for natural therapies, modern medicine is now more than ever incorporating age-old knowledge of herbal remedies useful in treating skin conditions into modern-day treatments.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!