Abstract：
Penicilloneines A (1) and B (2) are the first reported quinolone-citrinin hybrids. They were isolated from the starfish-derived fungus Penicillium sp. GGF16-1-2, and their structures were elucidated using spectroscopic, chemical, computational, and single-crystal X-ray diffraction methods. Penicilloneines A (1) and B (2) share a common 4-hydroxy-1-methyl-2(1H)-quinolone unit; however, they differ in terms of citrinin moieties, and these two units are linked via a methylene bridge. Penicilloneines A (1) and B (2) exhibited antifungal activities against Colletotrichum gloeosporioides, with lethal concentration 50 values of 0.02 and 1.51 μg/mL, respectively. A mechanistic study revealed that 1 could inhibit cell growth and promote cell vacuolization and consequent disruption of the fungal cell walls via upregulating nutrient-related hydrolase genes, including putative hydrolase, acetylcholinesterase, glycosyl hydrolase, leucine aminopeptidase, lipase, and beta-galactosidase, and downregulating their synthase genes 3-carboxymuconate cyclase, pyruvate decarboxylase, phosphoketolase, and oxalate decarboxylase.
摘要：
青霉素A（1）和B（2）是最早报道的喹诺酮-citrinin杂种。它们是从海星衍生的真菌青霉中分离出来的。GGF16-1-2，它们的结构用光谱学阐明，化学,计算，和单晶X射线衍射方法。青霉素A（1）和B（2）共享一个共同的4-羟基-1-甲基-2（1H）-喹诺酮单元；然而，它们在桔霉素部分方面不同，这两个单元通过亚甲基桥连接。青霉素A（1）和B（2）对炭疽病具有抗真菌活性，致死浓度50值为0.02和1.51μg/mL，分别。一项机制研究表明，1可以通过上调与营养相关的水解酶基因来抑制细胞生长并促进细胞空泡化和随后的真菌细胞壁破坏，包括推定的水解酶，乙酰胆碱酯酶，糖基水解酶，亮氨酸氨基肽酶，脂肪酶,和β-半乳糖苷酶,并下调它们的合成酶基因3-羧酸环化酶，丙酮酸脱羧酶,磷酸转酮酶，和草酸脱羧酶.
