Seven benzylamino derivatives of podophyllotoxin 8a-8g were synthesized and their chemical structures were confirmed by IR, ¹H-NMR, (13)C-NMR and ESI-MS spectral analyses. Their abilities to inhibit the growth of cancer cells A549, HCT-116 and HepG2, were investigated by MTT assay. Compound 8b possessed the highest cytotoxicity on cancer cell lines with average IC(50) values of 3.8 µM. All we synthetic compounds were cytotoxic against three cancer cell lines at the micromolar range, indicating podophyllotoxin derivatives with structural modification of benzylamino possess potent antitumor activity.
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http://dx.doi.org/10.1002/ardp.201100095 | DOI Listing |
Bioorg Chem
December 2024
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 PDFPlanta Med
December 2024
Department ofBiotechnology, Thapar Institute of Engineering and Technology (Deemed to be University), Patiala, 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 PDFBioorg Chem
November 2024
Integrated Drug Discovery Centre, Department of Pharmaceutical Chemistry, Acharya & BM Reddy College of Pharmacy, Bengaluru 560107, Karnataka, India.
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 PDFJID 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.
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