Synthesis and antitumor evaluation of sophocarpine-cinnamic acid ester derivatives as potential antitumor agents / 中草药

Objective: To synthesize sophocarpine-cinnamic acid ester derivatives and evaluate the in vitro antitumor activities of the derivatives. Methods: Taking sophocarpine as the starting material, the target compounds were synthesized by oxidation, esterification, N-alkylation, reduction, condensation, hydrolysis, and salification. Their antitumor activities in vitro were evaluated for HeLa, HepG2 and A-549 by MTT assay. Results: Eleven sophocarpine-cinnamic acid ester derivatives were synthesized and the structures were characterized by 1H-NMR, 13C-NMR and HRMS. MTT assay showed that some derivatives exhibited good antitumor activities. Compound 5g showed good antitumor activity against three human tumor cell lines, which was better than that of the positive control drug, cisplatin. Conclusion: Some derivatives showed promising antitumor activities and compound 5g was worth further studying.

Multi-substituted N-phenyl-2, 2-dichloroacetamide analogues as anti-cancer drugs: design, synthesis and biological evaluation / 药学学报

Our earlier research has shown that mono-substituted N-phenyl-2, 2-dichloroacetamide exhibited much higher anti-cancer activity than the lead compound sodium dichloroacetate (DCA). In this paper, a variety of multi-substituted N-phenyl-2, 2-dichloroacetamides were synthesized and biologically evaluated. The results showed that 3, 5-disubstituted N-phenyl-2, 2-dichloroacetamide analogues had satisfactory potency. Among them, N-(3, 5-diiodophenyl)-2, 2-dichloroacetamide had an IC50 of 2.84 micromol x L(-1) against non-small cell lung cancer cell line A549 and could induce cancer cell apoptosis.

Curative effect of Xianling Qianggu koufuye on postmenopausal osteoporosis / 中国中药杂志

<p><b>OBJECTIVE</b>To study the curative effects of Xianling Qianggu koufuye (XLQG) on postmenopausal osteoporosis in ovariectomized female rats.</p><p><b>METHOD</b>Sixty female Sprague-dawley rats aged 12-months were used, 50 of them were ovariectomized and randomly divided into 5 groups: ovariectomized (OVX), OVX + Nylestriol, OVX + XLQG (high dose, middle dose, low dose), and the others were sham-operated group. Rats were treated with drugs starting at the 45 day after the operation for 90 days. Double in vivo fluorochrome labeling was administered to all rats. At the end-point of study, the blood was collected to detecte the contents of ALP and StrACP in serum, and the fourth lumar vertebra (LV4) and femur bone sections were cut and stained for bone histomorphometric analyses, biomechanical analyses and BMP analyses.</p><p><b>RESULT</b>XLQGKFY decreased greatly the StrACP content, increased BMP and bone stiffness, and improved the bone biomechanical property.</p><p><b>CONCLUSION</b>Xianling Qianggu koufuye has a curative effect on postmenopausal osteoporosis, which provides for clinical use.</p>