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Enhanced Production and Anticancer Properties of Photoactivated Perylenequinones.
Journal of Natural Products ( IF 3.3 ) Pub Date : 2020-08-10 , DOI: 10.1021/acs.jnatprod.0c00492 Zeinab Y Al Subeh 1 , Huzefa A Raja 1 , Susan Monro 2 , Laura Flores-Bocanegra 1 , Tamam El-Elimat 3 , Cedric J Pearce 4 , Sherri A McFarland 2, 5 , Nicholas H Oberlies 1
Journal of Natural Products ( IF 3.3 ) Pub Date : 2020-08-10 , DOI: 10.1021/acs.jnatprod.0c00492 Zeinab Y Al Subeh 1 , Huzefa A Raja 1 , Susan Monro 2 , Laura Flores-Bocanegra 1 , Tamam El-Elimat 3 , Cedric J Pearce 4 , Sherri A McFarland 2, 5 , Nicholas H Oberlies 1
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Hypocrellins and hypomycins are naturally occurring fungal perylenequinones with potential photodynamic activity against cancer and microbial diseases. This project pursued three lines of research. First, the production of perylenequinones was enhanced by investigating the effect of culture medium and light exposure on their biosynthesis. Solid-fermentation cultures on rice medium allowed for enhanced production of hypocrellins as compared to Cheerios or oatmeal medium. Alternatively, increased production of hypomycins, which are structurally related to the hypocrellins, was observed on oatmeal medium. In both cases, light exposure was an essential factor for the enhanced biosynthesis. In addition, this led to the discovery of two new perylenequinones, ent-shiraiachrome A (5) and hypomycin E (8), which were elucidated based on spectroscopic data. Finally, the photocytotoxic effects of both classes of compounds were evaluated against human skin melanoma, with EC50 values at nanomolar levels for hypocrellins and micromolar levels for hypomycins. In contrast, both classes of compounds showed reduced dark toxicity (EC50 values >100 μM), demonstrating promising phototherapeutic indices.
中文翻译：
增强光活化苝醌的生产和抗癌特性。
竹红菌素和下霉素是天然存在的真菌苝醌，具有对抗癌症和微生物疾病的潜在光动力活性。该项目进行了三个研究方向。首先，通过研究培养基和光照对其生物合成的影响来提高苝醌的产量。与Cheerios或燕麦片培养基相比，大米培养基上的固体发酵培养物可以提高竹红菌素的产量。另外，在燕麦培养基上观察到次霉素产量增加，次霉素在结构上与次红菌素相关。在这两种情况下，光照都是增强生物合成的重要因素。此外，还发现了两种新的苝醌，ent -shiraiachrome A ( 5 ) 和次霉素 E ( 8 )，并根据光谱数据对其进行了阐明。最后，评估了两类化合物针对人类皮肤黑色素瘤的光细胞毒性作用，竹红菌素的 EC 50值为纳摩尔水平，下霉素的 EC 50 值为微摩尔水平。相比之下，两类化合物均表现出降低的暗毒性（EC 50值>100 μM），展现出有前景的光疗指数。
更新日期：2020-08-28
中文翻译：
增强光活化苝醌的生产和抗癌特性。
竹红菌素和下霉素是天然存在的真菌苝醌，具有对抗癌症和微生物疾病的潜在光动力活性。该项目进行了三个研究方向。首先，通过研究培养基和光照对其生物合成的影响来提高苝醌的产量。与Cheerios或燕麦片培养基相比，大米培养基上的固体发酵培养物可以提高竹红菌素的产量。另外，在燕麦培养基上观察到次霉素产量增加，次霉素在结构上与次红菌素相关。在这两种情况下，光照都是增强生物合成的重要因素。此外，还发现了两种新的苝醌，ent -shiraiachrome A ( 5 ) 和次霉素 E ( 8 )，并根据光谱数据对其进行了阐明。最后，评估了两类化合物针对人类皮肤黑色素瘤的光细胞毒性作用，竹红菌素的 EC 50值为纳摩尔水平，下霉素的 EC 50 值为微摩尔水平。相比之下，两类化合物均表现出降低的暗毒性（EC 50值>100 μM），展现出有前景的光疗指数。
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