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从灰树花中提取的黄嘌呤氧化酶抑制羊毛甾烷类化合物。

Xanthine oxidase inhibitory lanostanoids from Ganoderma tsugae.

机构信息

Faculty of Pharmacy, College of Pharmacy, Kaohsiung Medical University, Kaohsiung 80708, Taiwan.

出版信息

Fitoterapia. 2013 Sep;89:231-8. doi: 10.1016/j.fitote.2013.06.006. Epub 2013 Jun 13.

Abstract

Two new lanostanoids, 3α-acetoxy-22-oxo-5α-lanosta-8,24-dien-21-oic acid, named tsugaric acid D (1) and 16α-hydroxy-3-oxo-5α-lanosta-6,8,24(24(1))-trien-21-oic acid, named tsugaric acid E (2) were isolated from the fruit bodies of Ganoderma tsugae. The structures 1 and 2 were determined by spectroscopic methods. Compound 1 and known compounds 3 and 6 exhibited significant inhibitory effects on xanthine oxidase (XO) activity with an IC50 values of 90.2±24.2, 116.1±3.0, and 181.9±5.8 μM, respectively. Known compound 5 was able to protect human keratinocytes against damage induced by UVB light, which showed 5 could protect keratinocytes from photodamage. The 1 and 5 μM 1 combined with 5 μM cisplatin, respectively, enhanced the cytotoxicity induced by cisplatin. It suggested that 1 and 5 μM 1 combined with low dose of cisplatin may enhance the therapeutic efficacy of cisplatin and reduce side effect and cisplatin resistant.

摘要

从云芝(Ganoderma tsugae)的子实体中分离得到两个新的羊毛甾烷类化合物,分别命名为 tsugaric 酸 D(1)和 tsugaric 酸 E(2)。化合物 1 和 2 的结构通过光谱方法确定。化合物 1 和已知化合物 3 和 6 对黄嘌呤氧化酶(XO)活性表现出显著的抑制作用,其 IC50 值分别为 90.2±24.2、116.1±3.0 和 181.9±5.8 μM。已知化合物 5 能够保护人角质形成细胞免受 UVB 光诱导的损伤,表明 5 可以保护角质形成细胞免受光损伤。1 和 5 μM 的 1 分别与 5 μM 的顺铂联合使用,增强了顺铂诱导的细胞毒性。这表明 1 和 5 μM 的 1 联合低剂量顺铂可能增强顺铂的治疗效果,并降低副作用和顺铂耐药性。

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