ABSTRACT
Objective: To confirm the structure and preferential conformation of the Schiff base of gossypol with 1, 3, 4, 6-tetra-O-acetyl-β-D-glucosamine and explore its anti-HIV-1 activity.Methods: The Schiff base of gossypol with 11, 3, 4, 6-tetra-O-acetyl-β-D-glucosamine was synthesized and identified by FT-IR, NMR spectroscopy and the PM6 semi-classical calculation.The inhibitory activity of the novel compound against the laboratory-adapted HIV-1IIIB strain was examined using the HIV-1IIIB/TZM-bl indicator cell culture system.Results: The 1H and 13C-NMR signals of the new Schiff base were assigned.The PM6 semi-classical calculation indicated that enamine-enamine tautomeric form of the new Schiff base was more stable,which was stabilized by the intramolecular hydrogen bonds.The anti-HIV-1 test showed that the compound could block the entry of HIV-1IIIB into the target cells.Conclusion: The Schiff base of gossypol with 1, 3, 4, 6-tetra-O-acetyl-β-D-glucosamine exhibits enamine-enamine tautomeric form in solution, which shows potential anti-HIV-1 activity.
ABSTRACT
Objective:To explore novel compounds with anti-EV71 activity. Methods: A series of oligopeptides were designed based on the active groove of the EV71 3C protease using molecular simulation technology. Furthermore, some oligopeptides were syn-thesized and tested for the inhibition ability against EV71 in vitro. Results:Pentapeptides had higher binding affinity to the EV71 3C protease than the other oligopeptides, such as compounds 25 and 16. Therefore, compounds 25 and 16 were synthesized and tested in vitro for the anti-EV71 activity, and compound 25 exhibited potent anti-EV71 activity(EC50 =1. 36 μmol·L-1, CC50 =211. 94 μmol ·L-1, SI=155. 84), while compound 16 had no evident effect on EV71. Conclusion: It is worthy of further investigation on com-pound 25 as a novel scaffold of anti-EV71inhibitor.
ABSTRACT
Background and purpose: Regional lymph node metastasis was significantly associated with the prognosis of patients with non-small cell lung cancer (NSCLC). This study was designed to compare paclitaxel liposome plus cisplatin (LP) with gemcitabine and cisplatin (GP) in patients with regional lymph node metastasis of advanced NSCLC as a ifrst-line treatment. Methods:A total of 55 patients were randomly assigned to receive either liposomal paclitaxel (175 mg/m2) and cisplatin (75 mg/m2) or gemcitabine (1 000 mg/m2) and cisplatin (75 mg/m2) every 3 weeks. Results:Objective response rate (ORR) of lung primary foci was 37.9%in the LP arm and 30.8%in the GP arm (P>0.05) and the disease control rate (DCR) was 91.3%and 80.8%respectively (P>0.05);ORR of regional metastasis lymph node was higher in the LP arm (44.8%vs 15.4%, P0.05). Conclusion: Liposomal paclitaxel plus cisplatin is superior to gemcitabine plus cisplatin with less toxicity and better tolerated, it deserves further research and clinic application for patients with regional lymph node metastasis of advanced NSCLC.