Project "Research and development of aptamer-triptolide conjugate for treatment of rheumatoid arthritis (RA) ",which is jointly carried out by Institute for Advancing Translational Medicinein Bone & Joint Diseases, Hong Kong Baptist University and Institute of Basic Research in Clinical Medicine, China Academy of Chinese Medical Sciences, has won the support from the National Science and Technology Major Projects for"Major New Drugs Innovation and Development" in 2013. The research fund is￥1,500,000, the period is three years, and the principle investigator is Prof. Aiping Lu.

Triptolide (TP) is a major active compound derived from anti-RA herb Tripterygium wilfordii Hook F. However, its severe hepatotoxicity is the bottle neck for clinical translation in anti-RA therapy.Therefore, this project aims to address the bottle neck by conjugating TP withspecific aptamer through pH-sensitive linker. Specific aptamer helps to reduce the exposure of TP to liver cells and facilitate TP selectively targeting fibroblast-like synoviocytes (FLS). PH-sensitive linker between TP and aptamercan maintain the aptamer-TP conjugates at physiological pH but rupture in the acidic environment within FLS. This project hopes to provide efficient and safe aptamer-TP conjugate in treating RA. At the same time, the application of this project may play a big promoting role in researching and developing of other herb ingredients with similar characteristics (effective but toxic).