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The microbial secondary metabolites are always the main source of the natural drugs. The historical paradigm of the deep ocean as a biological 'desert' has shifted to one of a 'rainforest' owing to the isolation of many novel microbes and their associated bioactive compounds. A high quality microbial and its natural product library are crucial for successful drug and other screenings. However, how to build up the library efficiently is still faced with many bottlenecks. To overcome the difficulties and limitations, we reviewed the following strategies: (1) diversifying microbial sources and dereplication; (2) diversifying gene sources and dereplication; (3) diversifying microbial metabolite sources and dereplication; (4) novel methods and technologies for bioactive secondary metabolites, especially the high-throughput synergy screening for multi-target drugs. Bioactive compounds isolated using the above chemical microbiology strategies have not only shown importance in biotechnological and pharmaceutical applications but also increased our understanding of the diversity of microbe, ecosystem functions and the exploitable biology.

Bioactive small molecules play a crucial role in maintaining structural and functional homeostasis of cardiovascular system. However, systemic research pattern is rare because of the multiple forms, diverse effects and complicated interaction of these molecules. Therefore firstly, they can be classified into different single 'families' according to their internal relationships. Secondly, studies may be focused on the network of members within each 'family' as well as network among different 'families', especially the physiological and pathological significance of each member in the cardiovascular diseases. Lastly, efforts should be made to establish a primary and simple regulation network as the strategy of researches on biology of cardiovascular systems, and to promote the transition to a network covering more complicated multiplex 'families', even the whole body.