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北部湾珊瑚来源真菌节菱孢GXIMD 02501 产生的破骨细胞生成抑制性酚类衍生物。

Osteoclastogenesis inhibitory phenolic derivatives produced by the Beibu Gulf coral-associated fungus Acremonium sclerotigenum GXIMD 02501.

机构信息

Institute of Marine Drugs, Guangxi University of Chinese Medicine, Nanning 530200, China.

State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources, School of Chemistry and Pharmaceutical Sciences, Guangxi Normal University, Guilin 541004, China.

出版信息

Fitoterapia. 2022 Jun;159:105201. doi: 10.1016/j.fitote.2022.105201. Epub 2022 Apr 27.

DOI:10.1016/j.fitote.2022.105201
PMID:35489580
Abstract

Three new chlorinated orsellinic aldehyde derivatives, orsaldechlorins A - C (1-3) and a naturally new brominated orsellinic acid (7), along with ten known biosynthetically related phenolic (4-6, 8-13) and cyclohexanone (14) derivatives, were identified from the Beibu Gulf coral-derived fungus Acremonium sclerotigenum GXIMD 02501. Their structures were determined by spectroscopic data interpretation and comparison with those reported in the literature. Several of them showed inhibition of lipopolysaccharide (LPS)-induced NF-κB activation in RAW 264.7 macrophages at 20 μM. Moreover, the two new potent inhibitors (1 and 2) suppressed RANKL-induced osteoclast differentiation without cytotoxicity in bone marrow macrophages cells (BMMs). Our findings reveal that the phenolic compounds could be potential candidates for the prevention and treatment of osteolytic bone diseases.

摘要

从北部湾珊瑚来源的真菌棘孢木霉 GXIMD 02501 中鉴定出三种新的氯化奥索利醛衍生物(orsaldechlorins A-C(1-3))和一种天然的新的溴化奥索利酸(7),以及十种已知的生物合成相关的酚类(4-6、8-13)和环己酮(14)衍生物。它们的结构通过光谱数据分析和解构与文献报道的结构进行了确定。其中一些化合物在 20 μM 时表现出对脂多糖(LPS)诱导的 RAW 264.7 巨噬细胞中 NF-κB 激活的抑制作用。此外,两种新的强效抑制剂(1 和 2)在骨髓巨噬细胞(BMMs)中没有细胞毒性的情况下抑制了 RANKL 诱导的破骨细胞分化。我们的发现表明,这些酚类化合物可能是预防和治疗溶骨性骨疾病的潜在候选药物。

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