Twenty natural stilbenoids (1-20), including seven new stilbenoids (2, 4-7, 19, 20) and thirteen known stilbenoids (1, 3, 8-18), were isolated from the stem barks of Acanthopanax leucorrhizus, and six modified stilbenoid derivatives (1a, 2a, 4a, 4b, 7a and 17a) were obtained via methylation, demethylation and isopentenylation of the corresponding isolates (1, 2, 4, 7 and 17). These stilbenoids were structurally characterized by comprehensive analysis of their spectroscopic data and comparison with literature information, and evaluated for their cytotoxic activities against three human tumor cell lines (leukemia HL-60, hepatoma SMMC-7721 and breast carcinoma MCF-7) in vitro by MTT assay. The results showed that compounds 1a, 4a and 4b showed potent selective cytotoxicity against SMMC-7721 (IC=10.16±1.95μM and 9.76±1.32μM) and MCF-7 (IC=10.72±2.78μM) cell lines. The cytotoxic evaluation of these structurally modified stilbenoid derivatives have led to the establishment of a structure-activity relationship.
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http://dx.doi.org/10.1016/j.fitote.2017.11.007 | DOI Listing |
Chem Biodivers
December 2024
Wuyi University, School of Pharmacy and Food Engineering, Yingbin Street NO.99, 529020, Jiangmen, CHINA.
Long-term use of naproxen can lead to serious side effects. Inspired by the biological activity of cinnamic acid, a series of cinnamic acid derivatives containing naproxen were designed, synthesized and explored their anti-inflammatory activities and mechanism in vitro. Our results indicated that all of naproxen derivatives showed more significant inhibition against lipopolysaccharide (LPS)-induced nitric oxide (NO) production and had lower degree of cytotoxicity than that of naproxen.
View Article and Find Full Text PDFEClinicalMedicine
January 2025
Canadian Cancer Trials Group, Queen's University, Kingston, ON, Canada.
Background: Dual inhibition of cytotoxic T-lymphocyte associated protein 4 (CTLA-4) and programmed death ligand 1 (PD-L1) has been shown to be an effective treatment strategy in many cancers. We sought to determine the objective response rate of combination durvalumab (D) plus tremelimumab (TM) in parallel cohorts of patients with carefully selected rare cancer types in which these agents had not previously been evaluated in phase II trials and for which there was clinical or biological rationale for dual immune checkpoint inhibitor therapy to be active.
Methods: We designed a multi-centre, non-blinded, open-label phase II basket trial with each of the following 8 rare cancers considered a separate phase II trial: salivary carcinoma, carcinoma of unknown primary (CUP) with tumour infiltrating lymphocytes and/or expressing PD-L1, mucosal melanoma, acral melanoma, osteosarcoma, undifferentiated pleomorphic sarcoma, clear cell carcinoma of the ovary (CCCO) or squamous cell carcinoma of the anal canal (SCCA).
Appl Sci (Basel)
January 2024
Department of Microbiology and Medical Zoology, University of Puerto Rico School of Medicine, San Juan 00921, Puerto Rico.
Gracilioether M () and 11,12-dihydrogracilioether M (), two polyketides with a [2(5H)-furanylidene]ethanoate moiety, along with known plakortone G () and its new naturally occurring derivative 9,10-dihydroplakortone G (), were isolated from the Caribbean marine sponge . The structures and absolute configuration of , , and were characterized by analysis of HRESIMS and NMR spectroscopic data, chemical derivatization, and side-by-side comparisons with published NMR data of related analogs. Compounds and and a mixture of and were evaluated for cytotoxicity against MCF-7 human breast cancer cells.
View Article and Find Full Text PDFArch Razi Inst
June 2024
Faculty of Pharmacy, Eastern Mediterranean University, Famagusta, Mersin 10, Turkey.
The present experimental study aimed to assess the wound healing and anti-inflammatory effects of green synthesized copper nanoparticles (CuNPs) by the methanol extract of (Boiss), as a plant with various pharmacological effects, such as anti-inflammatory and antimicrobial effects, in traditional and modern medicine. The precipitation approach was used for the green synthesis of CuNPs by mixing the methanol and copper sulfate solution. Cell viability and fibroblast proliferation assay were performed by MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide) assay.
View Article and Find Full Text PDFBMC Mol Cell Biol
December 2024
Department of Biochemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh, 11451, Saudi Arabia.
Cystic echinococcosis (CE) is a worldwide zoonotic public health issue. The reasons for this include a lack of specific therapy options, increasing antiparasitic drug resistance, a lack of control strategies, and the absence of an approved vaccine. The aim of the current study is to develop a multiepitope vaccine against CE by in-silico identification and using different Antigen B subunits.
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