Title : Synthesis and anti-hypoxia activity of salidroside
Abstract:
High altitude reaction is a common disease unique to the plateau area, with common symptoms such as dizziness, headache, insomnia, loss of appetite, fatigue, and difficulty in breathing. In China, especially in Tibet, the plant has been an important source of substances for the treatment of various diseases, especially those related to oxidative stress. Rhodiola rosea is a traditional herb used in Chinese Tibetan medicine to treat plateau hypoxia. Modern research shows that salidroside is the main active ingredient of Rhodiola rosea, which has pharmacological activities such as improving blood microcirculation, reducing myocardial oxygen consumption and anti-fatigue. Due to the scarcity and low content of natural resources as well as the complexity of the extraction process, it can be obtained by chemical synthesis, biosynthesis, and biocatalytic (enzymatic) synthesis. The key step of chemical synthesis is the coupling of substituted phenylethanol with glucose pentaacetate, which is a low-cost and fast method, and is a feasible measure to advance the industrial production of salidroside. The in vitro study revealed that the HUVECs and EA.hy 926 cells treated with conditioned medium from osteoblast cells (MG-63 cells) treated with salidroside or treated directly with salidroside showed enhanced proliferation, migration and capillary structure formation. However, supplementation with an anti-VEGF antibody during the treatment of endothelial cells (ECs) significantly reversed the pro-angiogenic effect of salidroside. Moreover, salidroside upregulated HIF-1α expression and increased its transcriptional activity, consequently upregulating VEGF expression at the mRNA and protein levels. In addition, in vivo analysis demonstrated that it can stimulate endothelial sprouting from metatarsal bones. Thus, the experimental results show that the pro-angiogenic effects of salidroside involve HIF-1α-VEGF signalling by coordinating the coupling of angiogenesis-osteogenesis in the bone environment. Based on the structure of salidroside, it is promising to carry out the design of novel compounds and the evaluation of anti-hypoxia activity, and then develop new and efficient drugs for the prevention and treatment of plateau hypoxia injury.
Audience Takeaway Notes:
- Common symptoms and treatment of high altitude reaction.
- Methods of constructing models of hypoxic injury and studying the mechanism of action of anti-hypoxic injury.
- Stimulate research thinking and open up new research areas.
