Key Laboratory of Yunnan Insect Drug R&D, College of Pharmaceutical Sciences of Dali University, Wanhua Road, Dali 671000, China.
Fitoterapia. 2012 Apr;83(3):568-85. doi: 10.1016/j.fitote.2011.12.028. Epub 2012 Jan 10.
Twenty-nine phenolic compounds were isolated from the root bark of fresh (Yunnan) ginger and their structures fully characterized. Selected compounds were divided into structural categories and twelve compounds subjected to in-vitro assays including DPPH radical scavenging, xanthine-oxidase inhibition, monoamine oxidase inhibition, rat-brain homogenate lipid peroxidation, and rat pheochromocytoma PC12 cell and primary liver cell viability to determine their antioxidant and cytoprotective properties. Isolated compounds were also tested against nine human tumor cell lines to characterize anticancer potency. Several diarylheptanoids and epoxidic diarylheptanoids were effective DPPH radical scavengers and moderately effective at inhibiting xanthine oxidase. An enone-dione analog of 6-shogaol (compound 2) was isolated and identified to be most effective at protecting PC12 cells from H₂O₂-induced damage. Almost all tested compounds inhibited lipid peroxidation. Three compounds, 6-shogaol, 10-gingerol and an enone-diarylheptanoid analog of curcumin (compound 6) were identified to be cytotoxic in cell lines tested, with KB and HL60 cells most susceptible to 6-shogaol and the curcumin analog with IC₅₀<10 μM. QSAR analysis revealed cytotoxicity was related to compound lipophilicity and chemical reactivity. In conclusion, we observed distinct compounds in fresh ginger to have biological activities relevant in diseases associated with reactive oxygen species.
从新鲜（云南）姜的根皮中分离出 29 种酚类化合物，并对其结构进行了全面表征。选择的化合物分为结构类别，对其中 12 种化合物进行了体外测定，包括 DPPH 自由基清除、黄嘌呤氧化酶抑制、单胺氧化酶抑制、大鼠脑匀浆脂质过氧化、大鼠嗜铬细胞瘤 PC12 细胞和原代肝细胞活力，以确定其抗氧化和细胞保护特性。分离得到的化合物也针对 9 个人类肿瘤细胞系进行了测试，以表征其抗癌潜力。几种二芳基庚烷和环氧化二芳基庚烷是有效的 DPPH 自由基清除剂，对黄嘌呤氧化酶的抑制作用也较强。6-姜烯酮（化合物 2）的烯酮-二酮类似物被分离出来并鉴定为最有效地保护 PC12 细胞免受 H₂O₂诱导的损伤。几乎所有测试的化合物都抑制脂质过氧化。三种化合物，6-姜烯酮、10-姜酚和姜黄素的烯酮-二芳基庚烷类似物（化合物 6）被鉴定为在测试的细胞系中具有细胞毒性，其中 KB 和 HL60 细胞对 6-姜烯酮和姜黄素类似物最敏感，IC₅₀<10 μM。QSAR 分析表明，细胞毒性与化合物的亲脂性和化学反应性有关。总之，我们在新鲜生姜中观察到不同的化合物具有与活性氧相关疾病相关的生物学活性。
