摘要
Some glucosidase inhibitors show antitumor metastasis and anti-HIV activities and are also clinically useful for the treatment of diabetes,besides andrographolide derivative have been proven to be potent an α-glucosidase inhibitor.In order to investigate the double effect of glucosidase inhibition activity,a new diterpene lactone derivative 2 was synthesized via reduction of compound 1 which was one of the constitutions of Andrographis Pamicutate(Brum) Nees.The structure of compound 2 was confirmed with X-ray diffraction analysis,NMR,IR,HR-MS and so on.Compound 2 shows a selective α-glucosidase inhibitory activity with inhibition of 49.6% at 100 μmol/L,and the mother 1 has no inhibition activity(100 μmol/L).The results indicate that the double bond can affect the α-glucosidase inhibition activity of andrographolide.
Some glucosidase inhibitors show antitumor metastasis and anti-HIV activities and are also clinically useful for the treatment of diabetes, besides andrographolide derivative have been proven to be potent an α- glucosidase inhibitor. In order to investigate the double effect of glucosidase inhibition activity, a new diter- pene lactone derivative 2 was synthesized v/a reduction of compound 1 Which was one of the constitutions of Pamicutate (Brum) Nees. The structure of compound 2 was confirmed with X-ray diffraction α-nalysis, NMR, IR, HR-MS and so on. Compound 2 shows a hibition of 49. 6% at 100 μmol/L, and the mother 1 has no selective α-glucosidase inhibitory activity with ininhibition activity( 100 μmol/L). The results indicate that the double bond can affect the α-glucosidase inhibition activity of andrographolide.
出处
《高等学校化学学报》
SCIE
EI
CAS
CSCD
北大核心
2007年第7期1304-1306,共3页
Chemical Journal of Chinese Universities
基金
国家自然科学基金(批准号:20472075)资助