Cytotoxic and Antibacterial Preussomerins from the Mangrove Endophytic Fungus Lasiodiplodia theobromae ZJ-HQ1

Two new chlorinated preussomerins,
chloropreussomerins A and B (1 and 2), together
with nine known preussomerin analogues, 3–11, were obtained from the endophytic fungus Lasiodiplodia
theobromae ZJ-HQ1. Their structures were elucidated by a
combination of spectroscopic analyses. The absolute configurations
of 1 and 2 were both determined by single-crystal
X-ray diffraction using Cu Kα radiation. Chloropreussomerins
A and B (1 and 2) are the first chlorinated
compounds in the preussomerin family, and preussomerin M (3) is reported for the first time as a natural product. Compounds 1 and 2 showed potent in vitro cytotoxicity against A549 and MCF-7 human cancer cell lines, with
IC50 values ranging from 5.9 to 8.9 μM, and compounds 4–7 exhibited significant bioactivity
against A549, HepG2, and MCF-7 human cancer cell lines, with IC50 values of 2.5–9.4 μM. In the antibacterial
assay, compounds 1, 2, 5–7, and 11 exhibited significant activities against Staphylococcus aureus, with MIC values between 1.6 and 13
μg/mL.

从内生真菌Lasiodiplodia theobromae ZJ-HQ1中提取了两种新的氯化普鲁索梅林，即氯普鲁索梅林A和B（1和2），以及九种已知的普鲁索梅林类似物（3-11）。通过光谱分析方法确定了其结构。1和2的绝对构型通过使用Cu Kα辐射的单晶X射线衍射方法进行确定。氯普鲁索梅林A和B（1和2）是普鲁索梅林家族中的首次发现的氯化化合物，而普鲁索梅林M（3）则首次作为天然产物被报道。化合物1和2在体外对A549和MCF-7人癌细胞系表现出显著的细胞毒性，IC50值在5.9至8.9 μM之间，化合物4-7对A549、HepG2和MCF-7人癌细胞系显示出显著的生物活性，IC50值在2.5至9.4 μM之间。在抗菌实验中，化合物1、2、5-7和11对金黄色葡萄球菌显示出显著的活性，最小抑菌浓度（MIC）值在1.6至13 μg/mL之间。