BACKGROUND: Studies have shown that basic fibroblast growth factor has effects on stimulating vessel regeneration and collateral reconstruction. However, administration was performed mostly by peripheral vein, left atrium or percutaneous coronary intervention, and it is difficult to achieve an effective therapeutic concentration in the local myocardium. OBJECTIVE: Based on the property of poly(D, I-lactic-coglycolic acid) (PLGA), to investigate outcomes of inducing neovascularization in the myocardium in combination of basic fibroblast growth factor (bFGF) by ensuring target release of protein growth factor in local tissue. METHODS: PLGA and bFGF were dissolved in dichloromethane. This liquid mixture was rolled into the form of a hollow tube (3.0 mm outer diameter, 2.8 mm inner diameter, 0.1 mm thick, 10 mm length) for further use. The middle third of the left anterior descending coronary artery of mini-swines was ligated, and the local myocardium became dark purple. After the successful establishment by abnormal regional wall motion in the cardiac apex at anterior wall using ultrasound, the mini-swines were assigned to channels and bare scaffolds (BS) group and channels and bFGF-incorporating scaffolds (FS) group. The scaffold was implanted in the myocardium using self-made hollow bit. At 6 weeks, the number of proliferative cells was quantified by immunohistochemical staining. New vessels were quantified utilizing Image-Pro Plus software package in both groups. Quantitative analysis of changes in mass defect percentage was performed by Emory Cardiac Toolbox software combined with single-photon-emission computed tomography. RESULTS AND CONCLUSION: At 6 weeks, number of proliferative cells and the density of new vessels were significantly increased in the FS group compared with BS group(P<0.001). Single-photon-emission computed tomography illustrates that MDP was significantly lower in the FS group compared with the BS group (P < 0.001). Results have suggested that PLGA scaffolds that incorporate bFGF were able to induce angiogenesis and enhance blood-flow perfusion.

Aim To search for colchicine derivatives which have high efficacy and low toxicity. Methods Colchicine was firstly converted into thiocolchicine, and then it was hydrolyzed to get 7-(N-deacetylthiocolchicine). At last, 7-(N-deacetylthiocolchicine) was amidated to get the target compounds. The chemical structure of these new derivatives was confirmed with 1H NMR, IR, MS, and HR-MS. The cytotoxicity of the compounds was tested by MTT assay. Their in vivo antitumor activity was evaluated against mice tumor H22 and U14. Results Twelve thiocolchicine derivatives are new compounds. Conclusion In vitro antitumor activity has showed that some of these thiocolchicines possessed cytotoxic activity superior to colchicine. However, in vivo antitumor activity indicated that these derivatives have poor efficacy in mice.