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Strain Screening, Marine Active Compounds Targeted Isolating from the Fungus Library under the Guidance of the Antitubercular Activity

Antitubercular Activity,Marine fungus

Strain Screening, Marine Active Compounds Targeted Isolating from the Fungus Library under the Guidance of the Antitubercular Activity

Rong Chao^{1, 2}, Yang-Yang Guo^{1, 2}, Qun Zhang^{1, 2}, Mei-Yan Wei^{1, 2}, Wei-Feng Xu^{1, 2}, Xue-Mei Hou^{1, 2}, Chang-Yun Wang^{1, 2}, Chang-Lun Shao*<sup>1, 2

1</sup> Key Laboratory of Marine Drugs, The Ministry of Education of China, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, People’s Republic of China.

² Laboratory for Marine Drugs and Bioproducts, Qingdao National Laboratory for Marine Science and Technology, Qingdao 266237, People’s Republic of China.

* Email: shaochanglun@163.com.



Tuberculosis (TB/tuberculosis) is one of the multiple diseases that cause human deaths. It is a bacterial infection disease caused by Mycobacterium tuberculosis (Mtb/Mycobacterium tuberculosis). Tuberculosis has always been one of the most serious public health challenges in the world.^[1] The first-line anti-tuberculosis drugs such as rifampicin, isoniazid, pyrazinamide and ethambutol have reduced mortality. However, M. tuberculosis has appeared multidrug resistance and extensive drug resistance worldwide. Therefore, the research and development of new antitubercular drugs has become one of the key research directions in the field of drug research and development. ^[2] The special characteristics of marine ecosystems such as high pressure, high salt, hypoxia, and low light have created huge biodiversity and unique chemical diversity of marine organisms. Marine natural products have been widely studied as important sources of marine drugs.^[3]

In our previous work, the small fungus library containing 106 marine-derived fungi was constructed involving 1 phylum, 5 classes, 15 orders, 23 families, 40 genera. Under the guidance of the antitubercular activity, the ethyl acetate extracts of fungi CHNSCLM-0585 and CHNSCLM-0606 from the library showed good anti-M. tuberculosis activities at the concentration of 50 μg/mL. Further, the EtOAc extracts of these two fungi were subjected to silica gel vacuum liquid chromatography (VLC) to afford five fractions (Fr.1−Fr.5), and the Fr. 2 of fungus CHNSCLM-0606 showed significant antitubercular at the concentration of 1 μg/mL. Further investigations are focused on the discovery and isolation of antitubercular marine natural products from the fungus CHNSCLM-0606.

This work was supported by the Program of National Natural Science Foundation of China (Nos. U1706210, 41776141, 41906090, 42006092 and 41322037), the Program of Natural Science Foundation of Shandong Province of China (No. ZR2019BD047), the Marine S&T Fund of Shandong Province for Pilot National Laboratory for Marine Science and Technology (Qingdao) (No. 2018SDKJ0403-2), and the Taishan Scholars Program, China (No. tsqn20161010).

References

1. World Health Organization. Global Tuberculosis Report 2020. https://www.who.int/health-topics/tuberculosis#tab=tab_1


2. Xuemei Hou, Changyun Wang, William H. Gerwick, and Changlun Shao. Marine Natural Products as Potential Anti-Tubercular Agents. European Journal of Medicinal Chemistry, 2019, 165, 273–292.


3. Bin Yang, Jingxia Huang, Xuefeng Zhou, Xiuping Lin, Juan Liu, Shengrong Liao, Junfeng Wang, Fengan Liu, Huaming Tao, and Yonghong Liu. The fungal Metabolites with Potential Antiplasmodial Activity. Current Medicinal Chemistry, 2018, 25, 3796‒3825.