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Highly oxygenated lanostane triterpenoids from Ganoderma applanatum as a class of agents for inhibiting lipid accumulation in adipocytes.
Bioorganic Chemistry ( IF 4.5 ) Pub Date : 2020-09-03 , DOI: 10.1016/j.bioorg.2020.104263
Hai-Guo Su 1 , Qian Wang 1 , Lin Zhou 2 , Xing-Rong Peng 2 , Wen-Yong Xiong 3 , Ming-Hua Qiu 2
Affiliation  

Ganoderma triterpenoids (GTs), a class of major active constituents in Ganoderma species, play an important role in the anti-obesity effect of Ganoderma fungi. In the study, seventeen new highly oxygenated lanostane triterpenoids, ganoapplanoids A–Q (117), together with five previously reported compounds (1822), were isolated from the fruiting bodies of Ganoderma applanatum. Their structures were confirmed by comprehensive spectroscopic analyses, single-crystal X-ray diffraction and Mo2(OAc)4 induced CD cotton effect. Structurally, compound 6 represents the first example of 2-norlanostane triterpenoid possessing an unusual semiacetal moiety. Furthermore, isolates (15, 711, 1322, 3a) were evaluated for regulatory effects on lipid accumulation by 3T3-L1 adipocytes model. Among them, compounds 11 and 17 exhibited significant potency in blunted adipogenesis activities dose-dependently. Meanwhile, compounds 11 and 17 reduced triglyceride (TG) and total cholesterol (TC) levels in the adipocytes. These results supported that the highly oxygenated lanostane triterpenoids from G. applanatum may serve as agents for inhibiting the lipid accumulation in adipocytes and the G. applanatum provided an important source for searching new drugs to treat obesity.



中文翻译:

来自灵芝的高度氧化的羊毛脂三萜类化合物,作为一类抑制脂肪细胞中脂质蓄积的药物。

灵芝三萜类物质(GTs)是灵芝物种中的一类主要活性成分,在灵芝真菌的抗肥胖作用中起着重要作用。在研究中,17个新高度氧化羊毛甾烷三萜类化合物,ganoapplanoids A-Q(1 - 17),加上5种先前报道的化合物(18 - 22),从子实体中分离树舌。通过全面的光谱分析,单晶X射线衍射和Mo 2(OAc)4诱导的CD棉效应证实了它们的结构。从结构上讲,化合物6代表具有不寻常的半缩醛部分的2-降冰片烷三萜的第一个实例。此外,分离物(1 - 57 - 1113 - 22图3a),用于对脂质积聚调节作用进行了评价由3T3-L1脂肪细胞的模型。在它们之中,化合物1117在钝化的脂肪生成活性中显示出显着的剂量依赖性效力。同时,化合物1117降低了脂肪细胞中的甘油三酸酯(TG)和总胆固醇(TC)水平。这些结果支持了高氧化的羊毛脂三萜类化合物从青苹果可以作为抑制脂肪细胞中脂质蓄积的药物,青苹果为寻找新的治疗肥胖的药物提供了重要来源。

更新日期:2020-09-10
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