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J Enzyme Inhib Med Chem ; 35(1): 1372-1378, 2020 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-32571102


Gut microbial ß-glucuronidase (GUS) is a potential therapeutic target to reduce gastrointestinal toxicity caused by irinotecan. In this study, the inhibitory effects of 17 natural cinnamic acid derivatives on Escherichia coli GUS (EcGUS) were characterised. Seven compounds, including caffeic acid ethyl ester (CAEE), had a stronger inhibitory effect (IC50 = 3.2-22.2 µM) on EcGUS than the positive control, D-glucaric acid-1,4-lactone. Inhibition kinetic analysis revealed that CAEE acted as a competitive inhibitor. The results of molecular docking analysis suggested that CAEE bound to the active site of EcGUS through interactions with Asp163, Tyr468, and Glu504. In addition, structure-activity relationship analysis revealed that the presence of a hydrogen atom at R1 and bulky groups at R9 in cinnamic acid derivatives was essential for EcGUS inhibition. These data are useful to design more potent cinnamic acid-type inhibitors of EcGUS.

Zhonghua Liu Xing Bing Xue Za Zhi ; 34(11): 1068-70, 2013 Nov.
Artículo en Chino | MEDLINE | ID: mdl-24517935


OBJECTIVE: To study the prevalence and characteristics of blood pressure (BP) among children and adolescents at normal weight but with abdominal obesity. METHODS: Using data from the 'Student physical fitness and health surveillance 2010 project' in Shandong province, a total of 38 816 students aged 7-17 years were selected to participate in this study. Stature, body weight, waist circumference(WC), systolic blood pressure(SBP)and diastolic blood pressure(DBP) of these subjects were measured. Body weight status and abdominal obesity were defined by body mass index (BMI) and WC, respectively. RESULTS: In total, the proportions of thinness, normal weight, overweight and obesity defined by BMI were 5.37%, 72.47%, 12.92% and 9.24% respectively. 5.86% of the children and adolescents with normal weight had abdominal obesity, with normal weighted girls (7.19%) having higher prevalence of abdominal obesity than boys(4.33%)(P < 0.01). The Z-scores of SBP and DBP for both boys and girls were all significantly higher in the normal weight but with abdominal obesity groups than in both normal weight and WC groups (P < 0.01). CONCLUSION: Children and adolescents under normal weight but with abdominal obesity had higher BP level need to be identified and considered as high-risk individuals. Related intervention programs should also be targeted to this population.

Obesidad Abdominal/epidemiología , Obesidad Abdominal/fisiopatología , Adolescente , Presión Sanguínea , Índice de Masa Corporal , Peso Corporal , Niño , China/epidemiología , Femenino , Humanos , Masculino , Estudiantes , Circunferencia de la Cintura