Department of Microbial Technology, School of Biological Sciences, Madurai Kamaraj University, Madurai, Tamil Nadu, India.
Department of Organic Chemistry, School of Chemistry, Madurai Kamaraj University, Madurai, Tamil Nadu, India.
J Appl Microbiol. 2019 Nov;127(5):1468-1478. doi: 10.1111/jam.14410. Epub 2019 Sep 2.
Medicinal plant-associated endophytic fungi are important sources of precious bioactive compounds, contributing more than 80% of the natural drugs for various ailments. The present study was aimed at evaluating the anticancer activity of the crystallized compound alternariol methyl ether (AME) against hepatocellular carcinoma (HCC) both in vitro and in vivo from an endophytic fungus residing in the medicinal plant Vitex negundo.
The secondary metabolites from the endophytic fungus Alternaria alternata MGTMMP031 were isolated. Purification and characterization of the compound was performed and the potential compound was identified as AME. The crystal structure of AME was unambiguously confirmed by X-ray analysis. AME has been checked for its antibacterial and anticancer properties which showed its effectiveness against various bacteria and demonstrated marked anti-proliferative activity against the human HCC cells (HUH-7) both in vitro and in vivo. Mode of actions included cell cycle arrest, reducing the level of markers enzymes of liver cancer and preventing tumour growth.
Alternariol methyl ether acts as a potential therapeutic target against HCC. The compound was isolated and the crystal structure was obtained for the first time from the endophytic fungus A. alternata MGTMMP031. In the present study, the crystallized structure of AME was obtained by slow evaporation technique. It can be concluded that AME acts as a potential therapeutic target against HCC.
Endophytic fungi residing in the medicinal plants have strong biological significance and bioactive compounds from these fungi provide better therapeutic targets against diseases.
药用植物相关内生真菌是珍贵生物活性化合物的重要来源，为各种疾病提供了超过 80%的天然药物。本研究旨在从药用植物荆条中栖息的内生真菌中评估结晶化合物 alternariol 甲基醚 (AME) 的抗癌活性，包括体外和体内实验。
从内生真菌链格孢Alternaria alternata MGTMMP031 中分离出次级代谢产物。对化合物进行了纯化和表征，鉴定出潜在的化合物为 AME。AME 的晶体结构通过 X 射线分析得到明确确认。AME 已被检查其抗菌和抗癌特性，结果表明其对各种细菌有效，并在体外和体内显示出对人肝癌细胞（HUH-7）的显著抗增殖活性。作用模式包括细胞周期停滞、降低肝癌标志物酶水平和阻止肿瘤生长。
Alternariol 甲基醚可作为治疗 HCC 的潜在治疗靶点。该化合物是从内生真菌 A. alternata MGTMMP031 中分离出来的，其晶体结构也是首次获得。在本研究中，通过缓慢蒸发技术获得了 AME 的结晶结构。可以得出结论，AME 可作为治疗 HCC 的潜在治疗靶点。
栖息在药用植物中的内生真菌具有很强的生物学意义，这些真菌中的生物活性化合物为疾病提供了更好的治疗靶点。
