الملخص
This study is to investigate the effect of Icogenin on and its mechanism in anti-metastasis of pancreatic cancer BxPC3 cells in vitro. Using transwell assay, the effects of Icogenin on the invasion of BxPC3 cells were measured. The abilities of cell motility and adhesion in BxPC3 cells were detected by MTT assay and wound healing assay, respectively. The MAPK signal pathway protein expressions were analyzed with Western blotting. Also, the activity of MMP2 was observed by zymography assay. Icogenin inhibited the abilities of motility, adhesion and invasion of pancreatic cancer BxPC3 cells in vitro (P < 0.05), in a dose-depended manner, and inhibited the secretion of MMP2 and phosphorylation of ERK. PD98059 and U0126 which were ERK inhibitors could suppress the abilities of invasion and metastasis of pancreatic cancer BxPC3 cells. It is concluded that Icogenin can inhibit the abilities of invasion and metastasis of pancreatic cancer in vitro by inhibiting the secretion of MMP2 and phosphorylation of ERK.
الموضوعات
Humans , Antineoplastic Agents, Phytogenic , Pharmacology , Cell Adhesion , Cell Line, Tumor , Cell Movement , Dose-Response Relationship, Drug , Dracaena , Chemistry , Extracellular Signal-Regulated MAP Kinases , Metabolism , Matrix Metalloproteinase 2 , Bodily Secretions , Mitogen-Activated Protein Kinase Kinases , Metabolism , Neoplasm Invasiveness , Pancreatic Neoplasms , Metabolism , Pathology , Phosphorylation , Saponins , Pharmacology , Signal Transduction , Steroids , Pharmacologyالملخص
The derivatives of (9S)-9-hydroxyl-12-methylene erythromycin A were synthesized by using erythromycin A as a starting material. An intermediate (9S)-9,11-O-isopropylidene-6-O-allyl-2' ,4"-O-bis(benzoyl)-12,21-anhydro erythromycin A 12 was obtained. The antibacterial activity in vitro of two compounds, 6 and 11, was tested. The preliminary biological test showed that two compounds exhibited less potent antibacterial activity in vitro.
الموضوعات
Anti-Bacterial Agents , Chemistry , Pharmacology , Erythromycin , Chemistry , Pharmacology , Microbial Sensitivity Tests , Molecular Structure , Staphylococcus aureus , Staphylococcus epidermidis , Streptococcus pneumoniaeالملخص
<p><b>AIM</b>To synthesizs of derivatives of (9S)-12-methylene erythromycin possessed potent antibacterial activity.</p><p><b>METHODS</b>Using erythromycin A as a starting material, via two intermediate compounds protected 12,21-dehydroerythromycin A and 6,7: 12,21-didehydro erythromycin A, several 9-O, 11-O-ethylidene compounds were obtained. During this process, benzyl and isopropyl have been selected as the protecting group. The structures of compounds obtained were confirmed with 13C NMR and MS-FAB. Their antibacterial activity in vitro was tested.</p><p><b>RESULTS</b>Eleven derivatives of erythromycin were synthesized. Five of them were unknown compounds.</p><p><b>CONCLUSION</b>The preliminary biological test showed that two target compounds exhibited less potent antibacterial activity in vitro.</p>
الموضوعات
Anti-Bacterial Agents , Pharmacology , Erythromycin , Pharmacology , Microbial Sensitivity Tests , Staphylococcus aureus , Staphylococcus epidermidis , Streptococcus pneumoniaeالملخص
Drug-resistance has become a challenging clinical problem. Ketolides, a new class of erythromycin derivatives, have shown promising effectiveness in killing drug-resistant bacteria. This article reviews recent development in synthesis of ketolides, with focus on the modification and synthesis of some important positions on erythromycin A cycles.