School of Chemical Engineering and Pharmaceutics, Henan University of Science and Technology, Luoyang 471023, China.
Life Science and Environmental Science Research Center of Harbin University of Commerce, Harbin 150025, China.
Molecules. 2018 Dec 26;24(1):72. doi: 10.3390/molecules24010072.
The discovery and search for new antimicrobial molecules from insects and animals that live in polluted environments is a very important step in the scientific search for solutions to the current problem of antibiotic resistance. Previously, we have reported that the secondary metabolite with the antibacterial action discovered in scorpion. The current study further isolated three new compounds from karsch, while compounds and possessed 5,22-cholestadienol derivatives whose structure demonstrated broad spectrum bactericide activities. To explore the antibacterial properties of these new compounds, the result shows that compound inhibited bacterial growth of both and in a bactericidal rather than a bacteriostatic manner (MBC/MIC ratio ≤ 2). Similarly, with compound , a ratio of MBC/MIC ≤ 2 indicates bactericidal activity inhibited bacterial growth of Remarkably, this suggests that two compounds can be classified as bactericidal agents against broad spectrum bactericide activities for 5,22-cholestadienol derivatives from karsch. The structures of compounds ⁻ were established by comprehensive spectra analysis including two-dimensional nuclear magnetic resonance (2D-NMR) and high-resolution electrospray ionization-mass spectrometry (HRESI-MS) spectra. The antibacterial mechanism is the specific binding (various of bonding forces between molecules) using compound or as a ligand based on the different receptor proteins'-2XRL or 1Q23-active sites from bacterial ribosome unit A, and thus prevent the synthesis of bacterial proteins. This unique mechanism avoids the cross-resistance issues of other antibacterial drugs.
从生活在污染环境中的昆虫和动物中发现和寻找新的抗菌分子，是解决当前抗生素耐药性问题的科学探索中的一个非常重要的步骤。此前，我们已经报道了在蝎子中发现的具有抗菌作用的次生代谢物。本研究进一步从 karsch 中分离出三种新化合物，其中化合物 和 具有 5,22-胆甾二烯醇衍生物的结构，表现出广谱杀菌活性。为了探索这些新化合物的抗菌特性，结果表明化合物 以杀菌而非抑菌的方式（MBC/MIC 比值≤2）抑制 和 的细菌生长。同样，对于化合物 ，MBC/MIC 比值≤2 表明杀菌活性抑制 5,22-胆甾二烯醇衍生物的广谱杀菌活性的细菌生长。从 karsch 中得到的两种化合物可以被归类为具有广谱杀菌活性的杀菌剂。化合物 ⁻ 的结构通过综合光谱分析（包括二维核磁共振（2D-NMR）和高分辨率电喷雾电离质谱（HRESI-MS）光谱）确定。抗菌机制是基于细菌核糖体单位 A 中不同的受体蛋白'-2XRL 或 1Q23-活性位点，将化合物 或 作为配体特异性结合（分子间各种键合力），从而阻止细菌蛋白质的合成。这种独特的机制避免了其他抗菌药物的交叉耐药问题。
