Four new octanuclear Ru(II) cages (OC-1-OC-4) were synthesized from dinuclear p-cymene ruthenium(II) acceptors [Ru₂(μ-η⁴-C₂O₄)(CH₃OH)₂(η⁶-p-cymene)₂](O₃SCF₃)₂ (A₁), [Ru₂(μ-η⁴-C₆H₂O₄)(CH₃OH)₂(η⁶-p-cymene)₂](O₃SCF₃)₂ (A₂), [Ru₂(dhnq)(H₂O)₂(η⁶-p-cymene)₂](O₃SCF₃)₂ (A₃), and [Ru₂(dhtq)(H₂O)₂(η⁶-p-cymene)₂](O₃SCF₃)₂ (A₄) separately with a tetradentate pyridyl ligand (L₁) in methanol using coordination-driven self-assembly [L₁= N,N,N',N'-tetra(pyridin-4-yl)benzene-1,4-diamine]. The octanuclear cages are fully characterized by various spectroscopic techniques including single-crystal X-ray diffraction analysis of OC-4. The self-assembled cages show strong in vitro anticancer activity against human lung adenocarcinoma A549 and human cervical cancer HeLa cell lines as observed from the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Of all the octanuclear cages, OC-3 exhibits remarkable anticancer activity against both cancer cell lines and is more active than that reported for cisplatin. The excellent anticancer activity of OC-3 and OC-4 highlights the importance of the synergistic effects of the spacer component of the dinuclear p-cymene Ru(II) acceptor clips.

2010-01-01·International journal of toxicology4区 · 医学

14-Day Repeat-Dose Oral Toxicity Evaluation of Oxazyme in Rats and Dogs

4区 · 医学

Article

作者: Meschter, Carol L. ; Cowley, Aaron B. ; Dean, Robin R. ; Ghoddusi, Majid ; Sidhu, Harmeet ; Poage, Duane W. ; Li, Qing-Shan

Oxazyme (OC4) is an orally administered formulation that has as an active component a recombinant mutant form of Bacillus subtilis oxalate decarboxylase (OxDC) enzyme C383S, designed to degrade dietary oxalate in the stomach. Fourteen-day repeat-dose studies were conducted in rats and dogs to evaluate toxicity and determine a no observed adverse effect level (NOAEL). Animals were administered OC4 by oral gavage twice daily for 14 consecutive days. Reversibility, progression, and delayed appearance of any observed changes were evaluated in a subset of animals that underwent a recovery of 7 days following 14 days of control or test-article. There were no test-article-related adverse effects or deaths in either species. Results indicate that the NOAEL under the conditions used in the studies was 720.8 mg/kg/d in rats and 187.2 mg/kg/d in dogs, the high dose tested in each species.

Marine drugs2区 · 医学

Cytotoxic, Anti-Migration, and Anti-Invasion Activities on Breast Cancer Cells of Angucycline Glycosides Isolated from a Marine-Derived Streptomyces sp.

2区 · 医学

ArticleOA

作者: Li, Xia ; Lu, Dan-Dan ; Lin, Shi-Qi ; Qu, Xin-Ying ; Liu, Ling ; Peng, Ai-Hong ; Du, Qian-Qian ; Ren, Jin-Wei ; Xie, Wei-Dong ; Li, Er-Wei

Four angucycline glycosides were previously characterized from marine-derived Streptomyces sp. OC1610.4. Further investigation of this strain cultured on different fermentation media from that used previously resulted in the isolation of two new angucycline glycosides, vineomycins E and F (1–2), and five known homologues, grincamycin L (3), vineomycinone B2 (4), fridamycin D (5), moromycin B (7), and saquayamycin B1 (8). Vineomycin F (2) contains an unusual ring-cleavage deoxy sugar. All the angucycline glycosides isolated from Streptomyces sp. OC1610.4 were evaluated for their cytotoxic activity against breast cancer cells MCF-7, MDA-MB-231, and BT-474. Moromycin B (7), saquayamycin B1 (8), and saquayamycin B (9) displayed potent anti-proliferation against the tested cell lines, with IC50 values ranging from 0.16 to 0.67 μM. Saquayamycin B (9) inhibited the migration and invasion of MDA-MB-231 cells in a dose-dependent manner, as detected by Transwell and wound-healing assays.

100 项与 OC-4 相关的药物交易

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