Natural Products Research Unit, Centre of Excellence for Innovation in Chemistry (PERCH-CIC), Department of Chemistry, Faculty of Science, Khon Kaen University , Khon Kaen, 40002, Thailand.
J Agric Food Chem. 2012 Oct 3;60(39):9834-41. doi: 10.1021/jf302433r. Epub 2012 Sep 21.
Tuberculosis (TB) is one of the chronic infectious diseases caused by Mycobacterium tuberculosis that causes about 2-3 million deaths per year. Isoniazid and rifampicin are examples of first line drugs used for TB treatment; however, they are potentially hepatotoxic. More effective and safer drugs are urgently needed, especially from natural products. Basidiomycete mushrooms are known as important sources of pharmaceutically active metabolites including an anti-TB agent. In this work, the chemical constituents of the edible mushroom Astraeus odoratus were isolated and investigated for antibacterial activity against M. tuberculosis H(37)Ra. The cytotoxic activity against cancerous cell lines was also evaluated. Four new lanostane triterpenes, astraodoric acids A-D, and new 5-hydroxyhypaphorine have been isolated together with four known compounds. The structures were elucidated by NMR spectroscopic methods, HR-ESI-MS results, and X-ray crystallographic analysis. Astraodoric acids A and B exhibited moderate antibacterial (MICs of 50 and 25 μg/mL) and cytotoxic activities (IC(50) values of 34.69 and 18.57 μg/mL against KB and 19.99 and 48.35 μg/mL against NCI-H187), respectively. The results of this study show that A. odoratus could be a significant natural source for safer antitubercular and anticancer agents.
结核病（TB）是由结核分枝杆菌引起的慢性传染病之一，每年导致约 200 万至 300 万人死亡。异烟肼和利福平是用于结核病治疗的一线药物示例；然而，它们有潜在的肝毒性。迫切需要更有效和更安全的药物，特别是来自天然产物的药物。担子菌蘑菇被认为是具有药用活性代谢物的重要来源，包括一种抗结核病药物。在这项工作中，从可食用蘑菇 Astraeus odoratus 中分离出化学成分，并研究其对结核分枝杆菌 H(37)Ra 的抗菌活性。还评估了对癌细胞系的细胞毒性活性。分离得到了四种新的羊毛甾烷三萜，即 astraodoric 酸 A-D，以及一种新的 5-羟基hypaphorine，以及四种已知化合物。通过 NMR 光谱方法、HR-ESI-MS 结果和 X 射线晶体学分析阐明了结构。Astraodoric 酸 A 和 B 表现出中等的抗菌活性（MIC 分别为 50 和 25 μg/mL）和细胞毒性活性（对 KB 的 IC50 值分别为 34.69 和 18.57 μg/mL，对 NCI-H187 的 IC50 值分别为 19.99 和 48.35 μg/mL）。这项研究的结果表明，A. odoratus 可能是更安全的抗结核和抗癌药物的重要天然来源。
