以大黄酸为原料,通过不同的连接基团,将其与生物素、叶酸偶联得到10个目标化合物,其结构经~1 H NMR、MRR、MS确证。采用噻唑蓝(MTT)比色法测试目标化合物对肝癌细胞HepG2的体外增殖抑制活性,结果显示,所合成的10个目标化合物抑制HepG2...以大黄酸为原料,通过不同的连接基团,将其与生物素、叶酸偶联得到10个目标化合物,其结构经~1 H NMR、MRR、MS确证。采用噻唑蓝(MTT)比色法测试目标化合物对肝癌细胞HepG2的体外增殖抑制活性,结果显示,所合成的10个目标化合物抑制HepG2细胞的活性优于大黄酸,且大多数化合物的活性强于阳性对照药氟尿嘧啶(5-FU)。展开更多
A series of novel glyco-gambogic acid（GA） compounds were synthesized and evaluated for their in vitro anti-proliferative activity against human hepatocellular carcinoma（HCC） cells.All compounds showed much better ...A series of novel glyco-gambogic acid（GA） compounds were synthesized and evaluated for their in vitro anti-proliferative activity against human hepatocellular carcinoma（HCC） cells.All compounds showed much better aqueous solubility（0.92- 1.89 mg/mL） than GA（0.013 mg/mL）,and displayed potent inhibition on HCC cells（IC_（50）：0.21-12.23μmol/L） and little affects on non-tumor liver cells（IC_（50）：42.56-86.43μmol/L）,suggesting that glyco-GA compounds selectively inhibit HCC proliferation,and may be promising candidates for further intensive study.展开更多
Considering that high levels of nitric oxide(NO) exert anti-cancer effect and the derivatives of oleanolic acid(OA) have shown potent anti-cancer activity, new O^2-vinyl diazeniumdiolate-based NO releasing derivatives...Considering that high levels of nitric oxide(NO) exert anti-cancer effect and the derivatives of oleanolic acid(OA) have shown potent anti-cancer activity, new O^2-vinyl diazeniumdiolate-based NO releasing derivatives(5a–l, 11a–l) of OA were designed, synthesized, and biologically evaluated in the present study. These derivatives could release different amounts of NO in liver cells. Among them, 5d, 5i, 5j, 11g, 11h, and 11j released more NO in SMMC-7721 cells and displayed stronger proliferative inhibition against SMMC-7721 and Hep G2 cells than OA and other tested compounds. The most active compound 5j showed almost 20-fold better solubility than OA in aqueous solution, released larger amounts of NO in liver cancer cells than that in normal ones, and exhibited potent anti-hepatocellular carcinoma activity but little effect on the normal liver cells. The inhibitory activity against the cancer cells was significantly diminished upon addition of an NO scavenger, suggesting that NO may contribute, at least in part, to the activity of 5j.展开更多
文摘以大黄酸为原料,通过不同的连接基团,将其与生物素、叶酸偶联得到10个目标化合物,其结构经~1 H NMR、MRR、MS确证。采用噻唑蓝(MTT)比色法测试目标化合物对肝癌细胞HepG2的体外增殖抑制活性,结果显示,所合成的10个目标化合物抑制HepG2细胞的活性优于大黄酸,且大多数化合物的活性强于阳性对照药氟尿嘧啶(5-FU)。
基金supported by a grant from the Nature and Science Foundation of Department of Education,Anhui province(No.KJ2010A204)
文摘A series of novel glyco-gambogic acid（GA） compounds were synthesized and evaluated for their in vitro anti-proliferative activity against human hepatocellular carcinoma（HCC） cells.All compounds showed much better aqueous solubility（0.92- 1.89 mg/mL） than GA（0.013 mg/mL）,and displayed potent inhibition on HCC cells（IC_（50）：0.21-12.23μmol/L） and little affects on non-tumor liver cells（IC_（50）：42.56-86.43μmol/L）,suggesting that glyco-GA compounds selectively inhibit HCC proliferation,and may be promising candidates for further intensive study.
基金supported by grants from the National Natural Science Foundation of China(Nos.81273378 and 21372261)
文摘Considering that high levels of nitric oxide(NO) exert anti-cancer effect and the derivatives of oleanolic acid(OA) have shown potent anti-cancer activity, new O^2-vinyl diazeniumdiolate-based NO releasing derivatives(5a–l, 11a–l) of OA were designed, synthesized, and biologically evaluated in the present study. These derivatives could release different amounts of NO in liver cells. Among them, 5d, 5i, 5j, 11g, 11h, and 11j released more NO in SMMC-7721 cells and displayed stronger proliferative inhibition against SMMC-7721 and Hep G2 cells than OA and other tested compounds. The most active compound 5j showed almost 20-fold better solubility than OA in aqueous solution, released larger amounts of NO in liver cancer cells than that in normal ones, and exhibited potent anti-hepatocellular carcinoma activity but little effect on the normal liver cells. The inhibitory activity against the cancer cells was significantly diminished upon addition of an NO scavenger, suggesting that NO may contribute, at least in part, to the activity of 5j.
