ABSTRACT
Shikonin, the main active ingredient of Lithospermum, and its derivatives have been proved to have antitumor effects, and the anti-tumor mechanisms involve multiple targets. Based on recent literatures, this review focuses on the antitumor effects and its mechanisms. More emphases are given on the aspects of induction of apoptosis, induction of necrosis, acting on matrix metalloproteinase, acting on the protein tyrosine kinase and antiangiogenesis. The current status and problems of shikonin derivatives in antitumor effects are simply summarized and lookout for the development of antitumor drugs with shikonin as leading compounds.
Subject(s)
Humans , Antineoplastic Agents, Phytogenic , Pharmacology , Therapeutic Uses , Apoptosis , Cell Line, Tumor , Drugs, Chinese Herbal , Pharmacology , Therapeutic Uses , Lithospermum , Chemistry , Matrix Metalloproteinase 9 , Metabolism , Naphthoquinones , Pharmacology , Therapeutic Uses , Necrosis , Neoplasms , Drug Therapy , Metabolism , Pathology , Neovascularization, Pathologic , Plants, Medicinal , Chemistry , Protein-Tyrosine Kinases , Metabolism , Reactive Oxygen Species , MetabolismABSTRACT
Multi-drug resistance (MDR) of cancer cells is a major cause of failure in chemotherapy. To the majority of anti-cancer drugs, tumor cells are able to generate a multi-drug resistance; but there is no common views on the mechanism of MDR. This review summarizes the use of drug delivery system based on nanoparticles to overcome MDR in recent years. Three kinds including non-modified, ligand-modified and multifunctional drug delivery systems are described. Especially, the mechanism of reversing MDR based on nanoparticles is covered. Through efficiently offsetting and antagonizing the action of pumping drugs out of the tumor cells, drug delivery system based on nanoparticles can increase the concentration of the drug in tumors, while reduce the side effects on normal cells and overcome multi-drug resistance. The use of drug-loaded nanoparticles, which combines nanotechnology with the strategy of active and passive targeting administration, has shown significant prospect improving cancer therapy.
Subject(s)
Animals , Humans , Antineoplastic Agents , Therapeutic Uses , Drug Delivery Systems , Methods , Drug Resistance, Multiple , Drug Resistance, Neoplasm , Nanoparticles , Therapeutic Uses , Neoplasms , Drug TherapyABSTRACT
<p><b>OBJECTIVE</b>To test the dissolution rate of silymarin dropping pill as well as to be compared with other three commercial products of the silymarin.</p><p><b>METHOD</b>By UV spectrophotometry, we studied the dissolution conditions of silymarin dropping pill and compared its dissolution rate with Yiganling tablets (film-coating, sugar-coating) and Legalon capsule which are available in the market.</p><p><b>RESULT</b>The dissolution parameters T50 and Td of silymarin dropping pill, Yiganling tablet (film-coating), Yiganling tablet (sugar-coating) and Legalon capsule are 6.78, 9.85 min, 51.01, 73.78 min, 74.35, 86.97 min and 53.10, 72.65 min.</p><p><b>CONCLUSION</b>The dissolution rate of silymarin dropping pill is superior to that of two kinds of Yiganling tablets and Legalon capsule.</p>