在天津举办的新闻发布会上，南开大学生命科学学院贡红日教授与中科院饶子和院士带领的研究团队，成功揭示了抗结核药物贝达喹啉(BDQ)及其衍生物TBAJ-587作用于结核分枝杆菌ATP合成酶的分子机理。这一研究成果对于理解贝达喹啉的抗结核作用机制，以及开发更有效的抗耐药结核病药物具有重要意义。
#### 研究背景
结核病作为全球范围内的一大公共卫生挑战，近年来耐药结核病的出现和蔓延，使得传统抗结核药物的疗效大打折扣。贝达喹啉作为一种新型抗结核药物，因其独特的抗菌谱和对耐药菌株的活性而受到广泛关注。然而，对其作用机制的深入了解，对于优化其临床应用和开发新型抗结核药物至关重要。
#### 研究发现
研究团队通过结构生物学、生物化学和分子生物学等多学科交叉方法，解析了贝达喹啉及其衍生物与结核分枝杆菌ATP合成酶的复合物结构。结果显示，这些药物通过特异性结合ATP合成酶的特定位点，干扰了细菌的能量代谢过程，从而达到抑制细菌生长的目的。尤其值得关注的是，TBAJ-587展现出比贝达喹啉更优异的抗菌活性，其分子机制的研究为设计更高效、选择性更强的抗结核药物提供了新思路。
#### 研究意义
这一研究成果不仅为理解贝达喹啉及其衍生物的抗结核作用机制提供了科学依据，也为未来抗结核药物的研发提供了新的靶点和策略。通过深入研究ATP合成酶这一关键的细菌代谢节点，有望开发出针对耐药结核病的新型药物，为全球结核病防治工作注入新的活力。同时，该研究对于提升我国在抗感染药物领域的话语权和创新能力具有重要意义，标志着我国在结核病防治研究领域取得了关键突破。
此研究不仅对医学界和公共卫生领域具有深远影响，也为全球对抗结核病的挑战提供了新的解决方案。随着研究的深入，未来有望在临床应用中展现出更为显著的疗效和潜力，为全球结核病防治贡献力量。
英语如下：
### Chinese Research Team Reveals Mechanism of Anti-Tuberculosis Drug Bedaquiline and Overcomes Treatment Challenges for Drug-Resistant Tuberculosis
At a press conference held in Tianjin, Professor Gong Hongri from the School of Life Sciences at Nankai University, led by a research team including Academicians of the Chinese Academy of Sciences, Dr. Liu Zehu, successfully elucidated the molecular mechanism of how the anti-tuberculosis drug bedaquiline and its derivatives interact with the ATP synthase of Mycobacterium tuberculosis. This breakthrough is of great significance for understanding the antitubercular action of bedaquiline, as well as for the development of more effective drugs against drug-resistant tuberculosis.
#### Research Background
Tuberculosis, a major public health challenge worldwide, has seen an increase in drug-resistant strains, significantly reducing the efficacy of traditional anti-tuberculosis drugs. Bedaquiline, as a novel anti-tuberculosis drug, has attracted considerable attention due to its unique antibacterial spectrum and its effectiveness against drug-resistant strains. However, a deeper understanding of its mechanism of action is crucial for optimizing its clinical application and for the development of new anti-tuberculosis drugs.
#### Research Findings
Utilizing interdisciplinary approaches such as structural biology, biochemistry, and molecular biology, the research team elucidated the complex structures of bedaquiline and its derivatives in combination with the ATP synthase of Mycobacterium tuberculosis. The results showed that these drugs specifically bind to the targeted sites of the ATP synthase, disrupting the bacterial energy metabolism process, thereby inhibiting bacterial growth. Notably, TBAJ-587 demonstrated superior antibacterial activity compared to bedaquiline, suggesting new avenues for the design of more efficient and selective anti-tuberculosis drugs.
#### Research Significance
This research not only provides a scientific basis for understanding the antitubercular mechanism of bedaquiline and its derivatives, but also opens new perspectives for the development of future anti-tuberculosis drugs. By delving into the critical bacterial metabolic node, ATP synthase, there is potential to develop novel drugs specifically targeting drug-resistant tuberculosis, revitalizing global efforts in tuberculosis prevention and control. Moreover, this study underscores the importance of China’s contribution to the field of antimicrobial drug development, marking a significant advancement in tuberculosis prevention and control research in China.
This research, with its profound implications for the medical community and public health, also provides a new solution to the global challenge of tuberculosis. As the research progresses, it is anticipated to exhibit more significant therapeutic effects and potential in clinical applications, contributing to global efforts in tuberculosis prevention and control.
【来源】http://www.chinanews.com/life/2024/07-08/10248105.shtml
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