Medicinal and Process Chemistry Division, CSIR - Central Drug Research Institute, Lucknow 226 001, U.P., India.
Eur J Med Chem. 2013 Nov;69:439-48. doi: 10.1016/j.ejmech.2013.09.002. Epub 2013 Sep 12.
Andrographis paniculata, native to Taiwan, Mainland China and India, is a medicinal herb, which possesses various biological activities including anti-atherosclerosis. Andrographolide (1) has been identified as one of the active constituents against atherosclerosis. In continuation of our drug discovery program we synthesized few novel derivatives of 1 to improve their antidyslipidemic, LDL-oxidation and antioxidant activity. The tosylated derivative 7 has been turned out to be more potent than the parent compound and comparable activity with marketed antidyslipidemic drugs.
穿心莲原产于中国台湾、中国大陆和印度，是一种药用草本植物，具有多种生物活性，包括抗动脉粥样硬化。穿心莲内酯（1）已被确定为抗动脉粥样硬化的有效成分之一。在我们的药物发现计划中，我们合成了一些 1 的新型衍生物，以提高其抗血脂异常、LDL 氧化和抗氧化活性。对甲苯磺酰基衍生物 7 的活性强于母体化合物，与市售的抗血脂异常药物相当。
