关键词: Peniophora sp. anti-prostate methuosis inducer citrinin cytochalasins marine fungus peniotrinin

Mesh : Humans Antineoplastic Agents / pharmacology chemistry isolation & purification Male PC-3 Cells Prostatic Neoplasms / drug therapy pathology Cell Proliferation / drug effects Cytochalasins / pharmacology chemistry isolation & purification Aquatic Organisms Cell Line, Tumor Molecular Structure

来  源:   DOI:10.3390/md22050218   PDF(Pubmed)

Abstract:
Two new cytochalasin derivatives, peniotrinins A (1) and B (2), three new citrinin derivatives, peniotrinins C-E (4, 5, 7), and one new tetramic acid derivative, peniotrinin F (12), along with nine structurally related known compounds, were isolated from the solid culture of Peniophora 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, 1 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 3 had a significant anti-prostate cancer cell proliferation effect, while compounds 1 and 2 showed weak activity at 10 μM. We then confirmed that compound 3 exerts its anti-prostate cancer effect by inducing methuosis through transmission electron microscopy and cellular immunostaining, which suggested that compound 3 might be first reported as a potential anti-prostate methuosis inducer.
摘要:
两种新的细胞松弛素衍生物,青霉素A(1)和B(2),三种新的桔霉素衍生物,peniotrininsC-E(4,5,7),和一种新的四胺酸衍生物,peniotrininF(12),连同9种结构相关的已知化合物,从Peniophorasp.的固体培养物中分离出来。SCSIO41203.他们的结构,包括它们的立体碳的绝对构型,基于光谱分析充分阐明,量子化学计算,和计算的ECD。有趣的是,1是罕见的6/5/5/5/6/13六环细胞松弛素的第一个例子。我们筛选了上述化合物的抗前列腺癌活性,发现化合物3具有显著的抗前列腺癌细胞增殖作用,而化合物1和2在10μM时显示弱活性。然后我们通过透射电镜和细胞免疫染色证实了化合物3通过诱导瘤形成发挥其抗前列腺癌作用,这表明化合物3可能首先被报道为潜在的抗前列腺甲基营养诱导物。
公众号