Diaphorin, a polyketide produced by a bacterial symbiont of the Asian citrus psyllid, kills various human cancer cells
Diaphorin, a polyketide produced by a bacterial symbiont of the Asian citrus psyllid, kills various human cancer cells
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DOI：
10.1371/journal.pone.0218190
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发表时间：
2019-06-10
期刊：
影响因子：
3.7
通讯作者：
Okamura, Keiko
中科院分区：
文献类型：
--
作者：
Nakabachi, Atsushi;Okamura, Keiko
Diaphorin是由Betaproteobacteria（Betaproteobacteria）产生的一种聚酮化合物，是一种由植物汁液吸吮昆虫亚洲柑橘木虱Diaphorina citri（半翅目：Liviidae）窝藏的细胞器样防御共生体。黄递素属于pederin家族，这是一组与pederin共享其大部分核心结构的化合物，其特征在于由N-酰基缩醛胺桥接的两个二氢吡喃环。该家族的大多数成员具有有效的抗肿瘤活性，使其成为有希望的抗癌药物候选者。本研究评估了心肌黄蛋白对39种人类癌细胞系的抗肿瘤活性的治疗潜力，这些细胞系包括乳腺癌、脑癌、结肠癌、肺癌、皮肤癌、卵巢癌、肾癌、胃癌和前列腺癌。结果表明，黄递素对所有39种癌细胞系都具有抑制活性。GI 50、TGI和LC 50值的范围分别为0.28 μ M-2.4 μ M、1.6 μ M-11 μ M和7.5 μ M-> 100 μ M。这些值是pederin家族中最高的，表明黄藤素的抗癌活性比其他pederin同类物温和。黄递素的抑制作用在不同的癌症类型之间存在显著差异。最大差异约为10倍，这与大多数其他pederin同源物相似。
Diaphorin is a polyketide produced by Candidatus Profftella armatura (Betaproteobacteria), an organelle-like defensive symbiont harbored by a plant sap-sucking insect, Asian citrus psyllid Diaphorina citri (Hemiptera: Liviidae). Diaphorin belongs to the pederin family, a group of compounds that share much of their core structure with that of pederin, which is characterized by two dihydropyran rings bridged by an N-acyl aminal. Most members of this family have potent antitumor activity, making them promising anticancer drug candidates. The present study assessed the therapeutic potential of diaphorin for its antitumor activity against 39 human cancer cell lines including those from breast, brain, colon, lung, skin, ovary, kidney, stomach, and prostate. The results showed that diaphorin had inhibitory activity against all 39 cancer cell lines tested. The GI50, TGI, and LC50 values ranged from 0.28 mu M-2.4 mu M, 1.6 mu M -11 mu M, and 7.5 mu M-> 100 mu M, respectively. These values are among the highest in the pederin family, indicating that the anticancer activity of diaphorin is milder than those of other pederin congeners. The inhibitory effects of diaphorin significantly differed among the distinct cancer types. The maximum difference was about 10-fold, which was similar to those of most other pederin congeners.