Using antimalarials to treat osteoporosis

C&I Issue 11, 2023

Read time: 1-2 mins


AI identifies an effective secondary use for an artemisinin derivative.

Chinese researchers have used AI algorithms to show that an antimalarial drug could treat osteoporosis. In studies on mice, the drug appeared to reverse bone loss related to the disease.

In the search to find new applications for known drugs, Zhengwei Xie and colleagues from Peking University International Cancer Institute developed a machine learning algorithm to investigate how small-molecule drugs affect gene expression. In this case, they used it to see how effectively selected small-molecule drugs reversed changes to gene expression associated with osteoporosis. Specifically, they looked at what compounds altered genes involved in the differentiation of bone marrow mesenchymal stem cells (BMMSCs).

BMMSCs are the precursors of osteoblasts, cells, which create new bone tissue in areas that are growing or need repair. In people with osteoporosis, osteoblasts tend to turn into fat-creating cells while osteoclasts, cells, which dissolve and break down old or damaged bone cells, become overactive. Current treatments for osteoporosis focus mainly on inhibiting osteoclasts but more recently researchers have been looking at whether osteoblasts could be reprogrammed to build bone again.

The program predicted that one of the best compounds at reversing gene effects associated with osteoporosis would be dihydroartemisinin (DHA), a derivative of a compound called artemisinin found in the sweet wormwood plant (ACS Cent. Sci., doi: 10.1021/acscentsci.3c00794) and a traditional Chinese medicine. Several artemisinin-derived compounds are recommended for malaria treatment by the World Health Organization as part of combination therapies.

When mice with induced osteoporosis were fed DHA extract daily for six weeks, the researchers found significantly reduced bone loss in their femurs and nearly completely preserved bone structure.

They also experimented with injections of DHA-loaded nanoparticles once a week for eight weeks and found that bones of mice with osteoporosis that received the treatment were similar to those of the control group. Further testing suggested that DHA interacted with BMMSCs to boost osteoblast production.