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Synthesis of Ursolic Acid Derivatives and Their Inhibitory Activity against Prostate Cancer PC-3 Cells
ã€Abstract】 Ten ursolic acid derivatives were designed and synthesized by ursolic acid as the parent compound, and their structures were confirmed by IR, 1H NMR and MS techniques. Thiazole blue (MTT) colorimetric assay was used to investigate the inhibitory effect of the synthesized derivatives on the proliferation of human hepatoma cells HepG2 in vitro. The results showed that the tested derivatives all inhibited cell proliferation in a dose-dependent manner, of which derivative 9 The inhibitory effect was the strongest; the derivative 9 and the cells were treated for 24h, and then stained by Hoechst33342/PI, observed under inverted fluorescence microscope, and the high blue/low red fluorescence pattern of apoptosis appeared; flow cytometry was used to detect cell cycle. It was found that the cells were arrested in the S phase, and the blocking effect was enhanced with the increase of the drug concentration.
[Author]: School of Chemistry and Chemical Engineering, Fuzhou University; Zhengzhou Bosai Biotechnology Co., Ltd.;
ã€Key words】: Anti-cancer activity of ursolic acid derivatives [Fund]: Fujian Provincial Science and Technology Department Youth Talent Innovation Fund (2007F0347) Fujian Provincial Department of Education Class A Science and Technology Fund (JA08004) funded project [Category]: R914; R96
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Ursolic acid (UA), also known as ursolic acid and ursolic acid, is a pentacyclic triterpenoid. It is widely distributed in various plants such as loquat leaves, bearberry and Hedyotis diffusa in the form of free or combined with sugar [1]. Ursolic acid has many biological activities such as anti-HIV [2], anti-liver injury [3], anti-malaria [4], anti-inflammatory and antibacterial [5] and anti-cancer [6-8], especially its anti-cancer, The anticancer effect is taken seriously.
Ursolic acid is a triterpenoid compound found in natural plants. It has many biological effects such as sedative, anti-inflammatory, antibacterial, anti-diabetic, anti-ulcer, and lower blood sugar. Ursolic acid also has obvious antioxidant function. Therefore, it is widely used as a raw material for medicines and cosmetics. 1 liver, the role of anti-hepatitis clinical manifestations of ursolic acid significantly decreases rapidly alanine aminotransferase, serum transaminases, jaundice subsided, increase appetite, anti-fibrosis and liver function recovery effect, with quick, short course, the effect is stable specialty. Indian scholar Saraswat et al found that ursolic acid (5-20 mg·kg) has protective effects on hepatotoxicity induced by CC1 in rats. The pretreatment with ursolic acid can significantly increase the survival rate of rat hepatocytes, and it is observed in the experiment that ursolic acid has anti-cholestasis effect, and the bile flow and its contents are increased. It is speculated that the mechanism of action of ursolic acid on injured hepatocytes may be similar to that of the isomer oleanolic acid, which is to protect and stabilize the biofilm system of hepatocyte membrane and organelles, making them transparent and active. The transport function returned to normal, and the movement and distribution of ions and water inside and outside the cell also recovered, and the regenerative capacity was successively restored, which promoted the repair of necrotic hepatocytes in the central region of the hepatic lobules. The research and development of “New anti-hepatitis Chinese medicine ursolic acid and its preparations†has made significant progress. It was included in the national “863†program in 2002, and received 1 million yuan from the national research funding, becoming a national-level major research project (2002AA2Z3217). ). 2 Anti-tumor effect Ursolic acid is also resistant to a variety of carcinogenic and carcinogenic substances. It has been found that ursolic acid can significantly inhibit the proliferation of HL-60 cells and induce apoptosis; it can phagocytosis of macrophages in mice. Significantly increased, can inhibit the proliferation of human tongue squamous cell carcinoma cell line TSCCa, the inhibitory amount of half growth of TSCCa cells is about 12.5 μmol·L-1, which shows a certain dose-effect relationship within 24 hours; in situ hybridization shows bear The inhibitory effect of fruit acid on TSCCa cells is related to the inhibition of in situ expression of nuclear transcription factors. . In vivo tests have shown that ursolic acid can significantly enhance the body's immune function. It shows that arbutic acid has a wide anti-tumor effect, and ursolic acid is very likely to become a low-toxic and effective new anti-cancer drug.