School of Pharmaceutical Sciences, Xiamen University , South Xiangan Road, Xiamen, Fujian 361102, China.
J Agric Food Chem. 2014 Jun 25;62(25):5993-6000. doi: 10.1021/jf501724a. Epub 2014 Jun 17.
Worldwide, many different grains are infected by various fungi that may produce trichothecene mycotoxins. Fungi that produce trichothecenes, as well as the trichothecenes themselves, are potential problems for public health. On the other hand, trichothecenes possess multiple biological activities. Reduced toxicity may result in their applications in the pharmaceutical field. Two new trichothecenes along with seven known trichothecenes were isolated from an endophyte of the herb plant Ajuga decumbens. Their structures were deduced from 1D and 2D NMR data. The results of MTT assays revealed that new trichothecene 2',3'-epoxymyrothecine A, 1, and myrothecine A, 3, exhibited much lower toxicity compared to other trichothecenes. New trichothecene 2',3'-epoxymyrothecine A, 1, could induce phosphorylation of JNK (c-Jun N-terminal protein kinase) protein and the PARP (poly ADP-ribose polymerase) cleavage, and eventually induce apoptosis in cancer cells. These results point out the possibility for application of trichothecenes as chemotherapeutic agent.
在全球范围内，许多不同的谷物受到各种可能产生单端孢霉烯族毒素的真菌的感染。产生单端孢霉烯的真菌以及单端孢霉烯本身都是公共卫生的潜在问题。另一方面，单端孢霉烯具有多种生物活性。降低其毒性可能会导致其在制药领域的应用。从草本植物 Ajuga decumbens 的内生真菌中分离得到两种新的单端孢霉烯和七种已知的单端孢霉烯。它们的结构是根据 1D 和 2D NMR 数据推断出来的。MTT 测定结果表明，新的单端孢霉烯 2',3'-环氧表木贼碱 A,1 和表木贼碱 A,3 的毒性明显低于其他单端孢霉烯。新的单端孢霉烯 2',3'-环氧表木贼碱 A,1 可诱导 JNK（c-Jun N-末端蛋白激酶）蛋白磷酸化和 PARP（多聚 ADP-核糖聚合酶）裂解，最终诱导癌细胞凋亡。这些结果表明单端孢霉烯类化合物作为化疗药物的应用具有可能性。
