ABSTRACT
OBJECTIVE: To explore the efficient and economical synthesis method of asymmetric monocarbonyl curcumin ana-logues(AMCACs), design and sgnthesize a series of B19(1E, 4E)-1, 5-bis(2,3-dimethoxyphenyl) penta-1, 4-dien-3-one analogs to in- vestigate their anti-gastric cancer activities in vitro. METHODS: A series of asymmetric B19 analogues containing 2, 3-dimethoxyphenyl were designed via the combination principle of medicinal chemistry, and obtained a method for synthesizing intermediate (E)-2-(2, 3- dimethoxybenzylidene) cyclopentanone by one step catalyzed by L-proline. The targeted compounds were screened by MTT as-say, and colony cloning experiments were used to further verify its anti-gastric cancer activity in vitro. RESULTS: Ten novel target compounds were synthesized, and the structures were confirmed by LC-MS and 1H-NMR spectral analysis Among them, compound 6e had the highest inhibitory activity on the growth of gastric cancer cells SGC-7901 and BGC-823, whose IC50 were 9.80 and 13.50 μmol• L 1, respectively. CONCLUSION: L-proline could be used as a catalyst to synthesize asymmetric monocarbonyl curcumin analogues efficiently and economically Compound 6e could effectively inhibit the growth of gastric cancer cells in vitro, and its toxicity and inhibition mechanism of tumor cell growth need to be further studied.
ABSTRACT
Objective: To preliminarily ascertain the anti-gastric cancer active parts from the roots of Ferula ferulaeoide and to study its GC-MS fingerprint Methods: The inhibitory effects of different extraction from the roots of F. ferulaeoide on the cell proliferation of SGC-7901 cells were determined with MTT colorimetric method. GC-MS fingerprint of in vitro anti-gastric cancer active parts from F. ferulaeoide was investigated and analyzed by GC-MS and principal component analysis (PCA). Results: The chloroform extract showed the best inhibition on the growth of SGC-7901 cells. The method on GC-MS fingerprint of in vitro anti-gastric cancer active parts from F. ferulaeoide was established, showing 28 common characteristic peaks. The PCA demonstrated that the common peaks 1, 2, 4, 6, 7, 8, 9, 12, 21, 22, and 23 were connected closely with the in vitro anti-gastric cancer activity, and the seven compounds were 3-methoxy-1,2-propanediol, D-limonene, L-borneol acetate, terpinyl acetate, 1,5,9-undecatriene, 2,6,10-trimethyl, α-cedrene, and a-bergsmotene, β-cedrene, 8-epi-γ-eudesmol, γ-eudesmol, hinesol. Totally 28 common compounds of 10 batches of samples accounted for over 92% of the volatile contents, and the similarity of the GC-MS fingerprints from the 10 batches of samples was over 0.90. Conclusion: The chloroform extract from the roots of F. ferulaeoides with potential inhibitory effect on gastric cancer SGC-7901 cells is tentatively confirmed, and needs further to verify by animal cells in vivo. The method of GC-MS fingerprinting is rapid, simple, and accurate with good reproducibility and stability, and can be used to control the quality of active parts of F. ferulaeoides.