International journal of molecular sciences, 2016-06, Vol.17 (6), p.747-747
2016
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- Autor(en) / Beteiligte
- Titel
- Synthesis, Biological Activity, and Apoptotic Properties of NO-Donor/Enmein-Type ent-Kauranoid Hybrids
- Ist Teil von
- International journal of molecular sciences, 2016-06, Vol.17 (6), p.747-747
- Ort / Verlag
- Switzerland: MDPI AG
- Erscheinungsjahr
- 2016
- Quelle
- Free E-Journal (出版社公開部分のみ）
- Beschreibungen/Notizen
- Herein, we reported on a series of synthetic nitric oxide-releasing enmein-type diterpenoid hybrids (9a-i). All the target compounds showed potent antibacterial activity against selected Gram-positive bacteria S. aureus and B. subtilis. The antiproliferative activity against human tumor K562, MGC-803, CaEs-17 and Bel-7402 cells, and human normal liver cells L-02 was tested and the structure activity relationships (SARs) were also concluded. Compounds 9b and 9d showed the best activity against S. aureus and B. subtilis with the same minimal inhibitory concentrations (MICs) of 4 and 2 μg/mL, respectively. The derivative 9f displayed IC50 values of 1.68, 1.11, 3.60 and 0.72 μM against the four cancer cell lines above and 18.80 μM against normal liver cells L-02; meanwhile, 9f also released a high level of NO at the time point of 60 min of 22.24 μmol/L. Furthermore, it was also found that 9f induced apoptosis via the mitochondria-related pathway and arrested cell cycle of Bel-7402 cells at S phase. These findings might be important to explore new chemical entities for the main causes of in-hospital mortality of S. aureus infection, combined with a solid tumor.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 1422-0067, 1661-6596eISSN: 1422-0067DOI: 10.3390/ijms17060747Titel-ID: cdi_doaj_primary_oai_doaj_org_article_d5e741ec72a04e38a29e2838430eaada
- Format
- –
- Schlagworte
- Anti-Bacterial Agents - chemical synthesis, Anti-Bacterial Agents - chemistry, Anti-Bacterial Agents - pharmacology, Antimicrobial agents, Antineoplastic Agents - chemical synthesis, Antineoplastic Agents - chemistry, Antineoplastic Agents - pharmacology, antiproliferative, Apoptosis, Bacillus subtilis - drug effects, Bacteria, Bacterial infections, Biological activity, Cancer, Cell cycle, Cell Line, Tumor, Cell Proliferation - drug effects, Chemistry, Diterpenes - chemical synthesis, Diterpenes - chemistry, Diterpenes - pharmacology, Dose-Response Relationship, Drug, Drug resistance, enmein-type, ent-kauranoid, Gram-positive bacteria, Humans, Laboratories, Microbial Sensitivity Tests, Molecular Structure, Mortality, Nitric oxide, Nitric Oxide - chemistry, NO-donor, Pharmaceuticals, Staphylococcus aureus, Staphylococcus aureus - drug effects, Structure-Activity Relationship