ABSTRACT
A new lignan, named pouzolignan P (1), together with 14 known ones (2 - 15) were isolated from the roots of Pouzolzia zeylanica (L.) Benn. Their structures were deduced based on the detailed spectroscopic analysis. All the isolates were evaluated for their inhibitory activities toward the ATP citrate lyase (ACLY). Among them, four lignans, isopouzolignan K (3), gnemontanins E (5), gnetuhainin I (6), and styraxlignolide D (15) showed excellent ACLY inhibitory effect with IC50 values of 9.06, 0.59, 2.63, and 7.62 µM, respectively. These compounds were further evaluated for their cholesterol-lowing effects on ox-LDL-induced high-cholesterol HepG2 cells. Compound 15 emerges as the most potent ACLY inhibitor, which significantly decreased the TC level in a dose-dependent manner. In addition, molecular docking simulations elucidated that 15 formed a strong hydrogen-bond interaction with Glu599 of ACLY, which was an important site responsible for the enzyme catalytic activity.
Subject(s)
ATP Citrate (pro-S)-Lyase , Lignans , ATP Citrate (pro-S)-Lyase/chemistry , Molecular Docking Simulation , Enzyme Inhibitors/pharmacology , CholesterolABSTRACT
Three new acetophenones, named cynwilforones A-C (1-3), together with cynandione A (4) were isolated from the root bark of Cynanchum wilfordii (Maxim.) Hemsl. Their structures were deduced based on spectroscopic analysis and chemical methods. Compounds 1 and 4 exhibited potential hypoglycemic effects through inhibition of hepatic gluconeogenesis by down-regulating the expression of phosphoenolpyruvate carboxykinase and glucose-6-phosphatase. This is the first report that acetophenones from the root bark of C. wilfordii possesses potential hypoglycemic activity in vitro.
Subject(s)
Acetophenones/isolation & purification , Cynanchum/chemistry , Hypoglycemic Agents/pharmacology , Acetophenones/chemistry , Acetophenones/pharmacology , Animals , Biphenyl Compounds/isolation & purification , Cells, Cultured , Mice , Plant Bark/chemistry , Plant Roots/chemistryABSTRACT
Under the traditional processing theory "wine processing could promote the efficacy", Rhubarb after wine processing could treat the upper energizer diseases such as red swelling, and breath sores. Processing changes the medicinal properties of rhubarb, and thus results in different focuses in clinical application. In this study, a sensitive and specific method was developed for the determination of aloe-emodin, rhein and emodin in rats tissue. Rhubarb raw materials and its wine processed decoction were given to SD rats respectively by gavage administration, and then the contents of aloe-emodin, rhein and emodin in the tissues (heart, lung, brain, liver, kidney) were determined by HPLC-MS to explore the effect of wine processing on free anthraquinones in rat tissues. Experimental results showed that wine processing can significantly change the distribution of aloe emodin, rhein and emodin in rats in vivo, and the distribution of these components was increased in heart and lung tissues.There was no significant change of distribution in the liver and the kidney as compared with raw product group, and these three ingredients were not detected in the brain, indicating that aloe-emodin, rhein, emodin can not pass through the blood brain barrier.Therefore, wine processing had greater effect on distribution of free anthraquinones in rat tissues.This also verified the theory of traditional Chinese medicine, providing experimental basis for rhubarb processing mechanism.
