Abstract
Seven new xanthones, diaporthones A−G (1−7), together with 13 known analogues, including five mono- (8−14) and six dimeric xanthones (15−20), were obtained from the ascidian-derived fungus Diaporthe sp. SYSU-MS4722. Their planar structures were established by extensive spectroscopic analyses, including 1D and 2D NMR and high-resolution mass spectrometry (HR-ESIMS). The absolute configurations of 1−7 were clearly identified by X-ray crystallographic analysis and calculation of the ECD Spectra. Compounds 15−20 showed significant anti-inflammatory activity with IC50 values between 6.3 and 8.0 μM. In addition, dimeric xanthones (15−20) showed selective cytotoxicity against T98G cell lines with IC50 values ranging from 19.5 to 78.0 μM.
Highlights
Temozolomide (TMZ) as the first-line therapy drug is used for the treatment of glioma; at least 50% of TMZ-treated patients and more than 90% of recurrent gliomas show no response to TMZ [6,7]
SYSU-MS4722 was performed on the repeated silica gel and Sephadex LH-20 column chromatography, followed formed on the repeated silica gel and Sephadex LH-20 column chromatography, followed by semipreparative HPLC to afford seven new xanthones, diaporthones A−H (1−7)
IR data were carried out on a Fourier transformation infrared spectrometer coupled with an EQUINOX 55 infrared microscope (Bruker, Rheinstetten, Germany)
Summary
Glioma is a fatal disease of the central nervous system having an incidence rate of 3.20 per 100,000 people [1–3]. Due to limitations of the blood–brain barrier, only four drugs, including lomustine, carmustine, temozolomide, and bevacizumab, have been approved by FDA to treat glioma in the past four decades [4,5]. Temozolomide (TMZ) as the first-line therapy drug is used for the treatment of glioma; at least 50% of TMZ-treated patients and more than 90% of recurrent gliomas show no response to TMZ [6,7]. It is an urgent need to find more anti-glioma agents for the treatment of glioma. Anti-glioma molecules of marine origin have attracted many scientific research institutes or pharmaceutical companies’ attention.
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