On September 4, 2018, the team led by Professor He Yun of Chongqing University’s School of Pharmaceutical Sciences has published a paper titled “Total Synthesis and Antimicrobial Evaluation of Natural Albomycins against Clinical Pathogens” in Nature Communications (a sub-journal of Nature, with influence factor in 2018 of 12.35) run by Springer Nature, in collaboration with the Affiliated Children’s Hospital of Chongqing Medical University and Gates Foundation Global Health Drug Discovery Institute of Tsinghua University. Professor He Yun is the corresponding author of the paper. Lin Zihua, Xu Xiaobo and Zhao Sheng, doctoral students of the research group led by Professor He Yun, are parallel first authors. Chongqing University is the first author and the only corresponding author employer. All experiment work has been done by Chongqing University’s teams.
The wide use of antibiotics, in particular the misuse of antibiotics, has resulted in serious bacterial drug resistance that has become one of the most challenging problems in clinic treatment. The emergence and wide spread of multiple resistant bacteria and even “super bacteria” are now threatening human beings’ health. It is therefore urgently needed to develop new types of antibiotics.
Albomycins (or Grisein as it was called at the beginning) is a natural product with prominent anti-bacterial activity obtained by separating the metabolite of Streptomyces griseus in 1947. It is composed of the Siderophore and thioglycosides (such as SB-217452), which are very important for growth of harmful bacteria.
Chemical construction of Albomycins
The paper describes the first total synthesis of Albomycins δ1, δ2 and ε, and includes activity test of the three natural products. In particular, the Albomycins δ2 has demonstrated outstanding anti-bacterial activity. The minimum inhibitory concentration is generally lower than ciprofloxacin, vancomycin and penicillin that are highly accessible from the market. It also has satisfactory inhibitory activity for multiple resistant bacteria MARSA obtained through clinic separation, with the minimum inhibitory activity of 0.25μg/mL. The anti-bacterial activity against streptococcus pneumoniae even reaches the nanogram/ml level. In addition, early researches have indicated that the Albomycins are quite safe. As such, the compounds are very likely to be developed into drugs that are effective in fighting against bacterial resistance. The School of Pharmaceutical Science is now taking the lead to build up a pharmaceutical platform centering on bacterial resistance to develop Albomycins compounds and other new type antibiotics to cope with the bacterial resistance.
Related research work has drawn wide coverage from Nature, Chemical and Engineering News, the journal of American Chemical Journal with history of nearly 100 years, Chinese Science News, Xinhua News Agency, the Paper, Bioworld, BioArt and other domestic and foreign journals and media.
Link of the Professor He Yun’s research group: http://www.iddts.com/
Link of the paper: https://www.nature.com/articles/s41467-018-05821-1.pdf