Eutymeroterpenoids A–G with cytotoxic and anti-inflammatory activity from the fungus Eutypella scoparia GZU-4-19Y

IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL
Jingxin He , Binglin Chang , Shiting He , Die Yan , Yuwei Zhou , Jingnan Li , Zhongqiu Liu , Hui Cui , Yena Liu
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引用次数: 0

Abstract

Eutymeroterpenoids A–G (17), seven new eremophilane-type sesquiterpenoids, together with one known compound cryptosphaerolide (8), were isolated from marine-derived Eutypella scoparia GZU-4-19Y. Their structures were established by analysis of their NMR data and electronic circular dichroism calculations. All of them featured the unique 11‑carbon alkyl chain were rarely found in natural sesquiterpenoids. The isolates were evaluated for their anti-cancer and anti-inflammatory activities in vitro. Compounds 4, 5, 7 and 8 exhibited moderate cytotoxic activities against two human cancer cell lines (HT29 and HepG2). In addition, compounds 5 and 8 displayed good inhibitory activities against lipopolysaccharide-induced NO production in RAW264.7 cells with IC50 values of 26.9 and 13.7 μM, respectively, comparable to that of the positive control indomethacin (IC50 value = 24.2 μM). Western blot analysis further indicated that compounds 5 and 8 decreased the level of pro-inflammatory enzymes iNOS and COX-2.
具有细胞毒和抗炎活性的茯苓真蝶萜类A-G
从海产莨菪真typella scoparia GZU-4-19Y中分离到7个新戊二烯型倍半萜类A-G(1-7)和1个已知化合物隐球内酯(8)。通过核磁共振数据分析和电子圆二色性计算确定了它们的结构。它们都具有独特的11碳烷基链,这在天然倍半萜类中很少发现。对分离物进行了体外抗癌和抗炎活性评价。化合物4、5、7和8对两种人类癌细胞(HT29和HepG2)具有中等的细胞毒活性。化合物5和8对脂多糖诱导的RAW264.7细胞NO生成具有良好的抑制作用,IC50值分别为26.9和13.7 μM,与阳性对照吲哚美辛(IC50值为24.2 μM)相当。Western blot分析进一步表明,化合物5和8降低了促炎酶iNOS和COX-2的水平。
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来源期刊
Fitoterapia
Fitoterapia 医学-药学
CiteScore
5.80
自引率
2.90%
发文量
198
审稿时长
1.5 months
期刊介绍: Fitoterapia is a Journal dedicated to medicinal plants and to bioactive natural products of plant origin. It publishes original contributions in seven major areas: 1. Characterization of active ingredients of medicinal plants 2. Development of standardization method for bioactive plant extracts and natural products 3. Identification of bioactivity in plant extracts 4. Identification of targets and mechanism of activity of plant extracts 5. Production and genomic characterization of medicinal plants biomass 6. Chemistry and biochemistry of bioactive natural products of plant origin 7. Critical reviews of the historical, clinical and legal status of medicinal plants, and accounts on topical issues.
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