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Chemical constituents from the roots of Kadsura coccinea with their protein tyrosine phosphatase 1B and acetylcholinesterase inhibitory activities

机译:来自Kadsura Coccinea的根源的化学成分及其蛋白质酪氨酸磷酸酶1B和乙酰胆碱酯酶抑制活性

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摘要

Kadsura coccinea (Lem.) A. C. Smith has been used as a tonic, decongestant, and digestive agent. The roots are also employed in traditional medicine to treat chronic enteritis, acute gastritis, duodenal ulcers, rheumatic pain in bone, and traumatic injuries. In the present study, we have described the biological evaluation of constituents from the roots of K. coccinea with PTP1B and AChE inhibitory activities for the first time in literature. A new compound ( 1 ), kadcoccilactone T, and 24 known ones ( 2 ? 25 ) were isolated and identified using spectroscopic methods. All the isolates were examined for PTP1B and AChE inhibitory activities. Compounds 4 and 8 expressed strong PTP1B inhibition with IC_(50)values of 1.57?±?0.11 and 3.99?±?1.08?μM, respectively. Apparently, these compounds were further studied for PTP1B enzyme kinetic analysis. The result indicated that compounds 4 and 8 exhibited mixed-type inhibition with the Κ _(i)values of 4.97 and 3.26?μM, respectively.
机译:Kadsura Coccinea(LEM)A. C.史密斯已被用作滋补,减料和消化剂。 根源还用于传统医学,治疗慢性肠炎,急性胃炎,十二指肠溃疡,骨骼的风湿疼痛和创伤性损伤。 在本研究中,我们已经描述了PTP1B中K.Coccinea的根源的成分的生物学评估,并在文献中首次疼痛抑制活动。 分离新的化合物(1),kadcoCcallacterOnt和24种已知的(2→25)并使用光谱方法鉴定。 检查所有分离株的PTP1B和ACHE抑制活动。 化合物4和8表达了强的PTP1B抑制,IC_(50)值分别为1.57Ω±0.11和3.99?±1.08?μm。 显然,对PTP1B酶动力学分析进行了这些化合物。 结果表明,化合物4和8分别表现出与κ_(i)值的混合型抑制,分别为4.97和3.26Ωμm。

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