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海洋来源真菌 sp. SCSIO41203 的新型代谢产物作为 PC-3 细胞中的 Methuosis 诱导剂具有体外抗肿瘤活性。

Novel Metabolites from the Marine-Derived Fungus sp. SCSIO41203 Show Promising In Vitro Antitumor Activity as Methuosis Inducers in PC-3 Cells.

机构信息

CAS Key Laboratory of Tropical Marine Bio-Resources and Ecology, Guangdong Key Laboratory of Marine Materia Medica, South China Sea Institute of Oceanology, Chinese Academy of Sciences, Guangzhou 510301, China.

Pharmacy School, Guilin Medical University, Guilin 541004, China.

出版信息

Mar Drugs. 2024 May 14;22(5):218. doi: 10.3390/md22050218.

Abstract

Two new cytochalasin derivatives, peniotrinins A () and B (), three new citrinin derivatives, peniotrinins C-E (, , ), and one new tetramic acid derivative, peniotrinin F (), along with nine structurally related known compounds, were isolated from the solid culture of sp. SCSIO41203. Their structures, including the absolute configurations of their stereogenic carbons, were fully elucidated based on spectroscopic analysis, quantum chemical calculations, and the calculated ECD. Interestingly, is the first example of a rare 6/5/5/5/6/13 hexacyclic cytochalasin. We screened the above compounds for their anti-prostate cancer activity and found that compound had a significant anti-prostate cancer cell proliferation effect, while compounds and showed weak activity at 10 μM. We then confirmed that compound exerts its anti-prostate cancer effect by inducing methuosis through transmission electron microscopy and cellular immunostaining, which suggested that compound might be first reported as a potential anti-prostate methuosis inducer.

摘要

从 sp. SCSIO41203 的固体培养物中分离得到了两个新的细胞松弛素衍生物,分别为 peniotrinin A () 和 B (), 三个新的桔青霉素衍生物,peniotrinin C-E (,, ), 和一个新的四元酸衍生物,peniotrinin F (), 以及 9 个结构相关的已知化合物。根据光谱分析、量子化学计算和计算的 ECD,它们的结构,包括其手性碳原子的绝对构型,都得到了充分的阐明。有趣的是, 是罕见的 6/5/5/5/6/13 六元环细胞松弛素的第一个例子。我们筛选了上述化合物对前列腺癌细胞增殖的抑制活性,发现化合物 对前列腺癌细胞增殖有显著的抑制作用,而化合物 和 在 10 μM 时显示出较弱的活性。随后,我们通过透射电子显微镜和细胞免疫染色证实化合物 通过诱导细胞自噬发挥其抗前列腺癌细胞的作用,这表明化合物 可能是第一个被报道为潜在的抗前列腺细胞自噬诱导剂的化合物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2270/11123344/63e2d09196b1/marinedrugs-22-00218-g001.jpg

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