Vivek-Ananth R P, Sahoo Ajaya Kumar, Baskaran Shanmuga Priya, Samal Areejit
The Institute of Mathematical Sciences (IMSc), Chennai600113, India.
Homi Bhabha National Institute (HBNI), Mumbai400094, India.
ACS Omega. 2023 Jan 10;8(3):3102-3113. doi: 10.1021/acsomega.2c06428. eCollection 2023 Jan 24.
Medicinal fungi, including mushrooms, have well-documented therapeutic uses. In this study, we perform a cheminformatics-based investigation of the scaffold and structural diversity of the secondary metabolite space of medicinal fungi and, moreover, perform a detailed comparison with approved drugs, other natural product libraries, and semi-synthetic libraries. We find that the secondary metabolite space of medicinal fungi has similar or higher scaffold diversity in comparison to other natural product libraries analyzed here. Notably, 94% of the scaffolds in the secondary metabolite space of medicinal fungi are not present in the approved drugs. Further, we find that the secondary metabolites, on the one hand, are structurally far from the approved drugs, while, on the other hand, they are close in terms of molecular properties to the approved drugs. Lastly, chemical space visualization using dimensionality reduction methods showed that the secondary metabolite space has minimal overlap with the approved drug space. In a nutshell, our results underscore that the secondary metabolite space of medicinal fungi is a valuable resource for identifying potential lead molecules for natural product-based drug discovery.
药用真菌,包括蘑菇,其治疗用途有充分的文献记载。在本研究中,我们基于化学信息学对药用真菌次生代谢产物空间的支架和结构多样性进行了调查,此外,还与已批准药物、其他天然产物库和半合成库进行了详细比较。我们发现,与这里分析的其他天然产物库相比,药用真菌的次生代谢产物空间具有相似或更高的支架多样性。值得注意的是,药用真菌次生代谢产物空间中94%的支架在已批准药物中不存在。此外,我们发现,次生代谢产物一方面在结构上与已批准药物相差甚远,而另一方面,它们在分子性质方面与已批准药物相近。最后,使用降维方法进行的化学空间可视化显示次生代谢产物空间与已批准药物空间的重叠最小。简而言之,我们的结果强调药用真菌的次生代谢产物空间是基于天然产物的药物发现中识别潜在先导分子的宝贵资源。