当前位置：
X-MOL 学术
›
Chem. Res. Toxicol.
›
论文详情
Our official English website, www.x-mol.net, welcomes your
feedback! (Note: you will need to create a separate account there.)
Metabolic Interaction between Ammonia and Baicalein.
Chemical Research in Toxicology ( IF 3.7 ) Pub Date : 2020-07-03 , DOI: 10.1021/acs.chemrestox.0c00205 Shuwei Zhang 1 , Ronghui Wang 1 , Yantao Zhao 1 , Fakir Shahidullah Tareq 1 , Shengmin Sang 1
Chemical Research in Toxicology ( IF 3.7 ) Pub Date : 2020-07-03 , DOI: 10.1021/acs.chemrestox.0c00205 Shuwei Zhang 1 , Ronghui Wang 1 , Yantao Zhao 1 , Fakir Shahidullah Tareq 1 , Shengmin Sang 1
Affiliation
|
Ammonia is treated as a primary waste product of cellular metabolism in vivo and can contribute to the alteration of neurotransmission, oxidative stress, and cerebral edema and astrocyte swelling when its concentration in the brain is high. The objective of this study was to determine whether bioactive polyphenol baicalein had the capacity to trap ammonia in vitro and in vivo. Under in vitro conditions, baicalein rapidly reacted with ammonia to generate two monoaminated products and one diaminated product under different reaction times. These three major aminated products were purified from the reaction mixture, and their structures were characterized as 5-NH2-baicalein, 6-NH2-baicalein, and 5,6-di-NH2-baicalein based on the analysis of their HR-MS and 1D- and 2D-NMR data. In mice, both 5-NH2-baicalein and 6-NH2-baicalein were detected in 24 h fecal and urine samples collected from mice treated with baicalein (200 mg/kg) through oral gavage, and 6-NH2-baicalein was also detected in mouse plasma and brain samples collected at 0.5 h after baicalein treatment. Significant amounts of 6-NH2-baicalein were detected in all mouse samples including feces, urine, plasma, and brain. The levels of 6-NH2-baicalein in feces and urine were significantly higher than those of 5-NH2-baicalein. Furthermore, the average level of 6-NH2-baicalein was very close to that of baicalein (3.62 vs 3.77 ng/g) in mouse brain, suggesting it is possible that baicalein has the capacity to be absorbed rapidly into the circulation system and then cross the blood-brain barrier into the brain to detoxify ammonia in the blood and brain. In conclusion, this study confirmed that baicalein, a flavonoid with a vic-trihydroxyl structure on the A-ring, has the potential to detoxify ammonia and treat ammonia-associated chronic diseases.
中文翻译：
氨和黄芩素之间的代谢相互作用。
氨被视为体内细胞代谢的主要废物，当其在大脑中的浓度高时，会导致神经传递、氧化应激、脑水肿和星形胶质细胞肿胀的改变。这项研究的目的是确定生物活性多酚黄芩素是否具有在体外和体内捕获氨的能力。在体外条件下，黄芩素与氨迅速反应，在不同的反应时间下生成两种单胺化产物和一种二胺化产物。从反应混合物中纯化出这三种主要的胺化产物，其结构表征为5-NH 2 -黄芩素、6-NH 2-baicalein 和 5,6-di-NH 2 -baicalein 基于对它们的 HR-MS 和 1D-和 2D-NMR 数据的分析。在小鼠中，5-NH 2 -baicalein和6-NH 2在从与黄芩素（200毫克/千克）通过口服强饲法处理的小鼠中收集24小时的粪便和尿液样本中检测到-baicalein和6-NH 2 -baicalein是还在黄芩素处理后 0.5 小时收集的小鼠血浆和脑样本中检测到。在包括粪便、尿液、血浆和大脑在内的所有小鼠样本中都检测到了大量的 6-NH 2 -黄芩素。粪便和尿液中6-NH 2 -黄芩素的含量显着高于5-NH 2 -黄芩素。此外，6-NH 2的平均水平-baicalein 与小鼠大脑中的黄芩素非常接近（3.62 vs 3.77 ng/g），这表明黄芩素有可能被迅速吸收到循环系统中，然后穿过血脑屏障进入大脑，解毒血液和大脑中的氨。总之，这项研究证实黄芩素是一种在 A 环上具有vic-三羟基结构的黄酮类化合物，具有解毒氨和治疗氨相关慢性疾病的潜力。
更新日期：2020-08-17
中文翻译：
氨和黄芩素之间的代谢相互作用。
氨被视为体内细胞代谢的主要废物，当其在大脑中的浓度高时，会导致神经传递、氧化应激、脑水肿和星形胶质细胞肿胀的改变。这项研究的目的是确定生物活性多酚黄芩素是否具有在体外和体内捕获氨的能力。在体外条件下，黄芩素与氨迅速反应，在不同的反应时间下生成两种单胺化产物和一种二胺化产物。从反应混合物中纯化出这三种主要的胺化产物，其结构表征为5-NH 2 -黄芩素、6-NH 2-baicalein 和 5,6-di-NH 2 -baicalein 基于对它们的 HR-MS 和 1D-和 2D-NMR 数据的分析。在小鼠中，5-NH 2 -baicalein和6-NH 2在从与黄芩素（200毫克/千克）通过口服强饲法处理的小鼠中收集24小时的粪便和尿液样本中检测到-baicalein和6-NH 2 -baicalein是还在黄芩素处理后 0.5 小时收集的小鼠血浆和脑样本中检测到。在包括粪便、尿液、血浆和大脑在内的所有小鼠样本中都检测到了大量的 6-NH 2 -黄芩素。粪便和尿液中6-NH 2 -黄芩素的含量显着高于5-NH 2 -黄芩素。此外，6-NH 2的平均水平-baicalein 与小鼠大脑中的黄芩素非常接近（3.62 vs 3.77 ng/g），这表明黄芩素有可能被迅速吸收到循环系统中，然后穿过血脑屏障进入大脑，解毒血液和大脑中的氨。总之，这项研究证实黄芩素是一种在 A 环上具有vic-三羟基结构的黄酮类化合物，具有解毒氨和治疗氨相关慢性疾病的潜力。
京公网安备 11010802027423号