ABSTRACT
Abstract Gut bacterial β-glucuronidase (GUS) can reactivate xenobiotics that exert enterohepatic circulation- triggered gastrointestinal tract toxicity. GUS inhibitors can alleviate drug-induced enteropathy and improve treatment outcomes. We evaluated the inhibitory effect of Polygonum cuspidatum Siebold & Zucc. and its major constituents against Escherichia coli GUS (EcGUS), and characterized the inhibitory mechanism of each of the components. Trans-resveratrol 4'-O-β-D-glucopyranoside (HZ-1) and (-)-epicatechin gallate (HZ-2) isolated from P. cuspidatum were identified as the key components and potent inhibitors. These two components displayed strong to moderate inhibitory effects on EcGUS, with Ki values of 9.95 and 1.95 μM, respectively. Results from molecular docking indicated that HZ-1 and HZ-2 could interact with the key residues Asp163, Ser360, Ile 363, Glu413, Glu504, and Lys 568 of EcGUS via hydrogen bonding. Our findings demonstrate the inhibitory effect of P. cuspidatum and its two components on EcGUS, which supported the further evaluation and development of P. cuspidatum and its two active components as novel candidates for alleviating drug-induced damage in the mammalian gut.
ABSTRACT
A popliteal nerve block may be used to provide anesthesia and extended analgesia of the lower extremity, to ameliorate severe and long lasting postoperative pain. The aim of this study was to elucidate the anatomical location of tibial (TN) and common peroneal (CPN) nerves in the popliteal crease for effective nerve block. Fifty fresh specimens from 27 adult Chinese cadavers (16 males and 11 females, age range from 35 to 87 years) were investigated. Twenty-two cadavers were used to identify nerve locations and 5 cadavers were used to determine the depths of nerves in cross section. TN was found to be located at 50% from the most lateral point of the popliteal crease at 1.4 cm deep to the surface. In 20% of the 50 specimens, the medial sural cutaneous nerve branched out below or at the popliteal crease, whereas the CPN was located at 26.0% from the most lateral point of the popliteal crease and at 0.7 cm deep to the surface. Furthermore, in 6.0% of specimens the lateral sural cutaneous nerve branched out below or at the popliteal crease. This study suggests that the TN and CPN leave the sciatic nerve at variable distances from the popliteal crease. However, we believe that the results of the present study about the location of TN and CPN at the popliteal crease offer a good guide to optimal nerve block.
El bloqueo nervioso poplíteo puede ser utilizado para proporcionar anestesia y analgesia prolongada del miembro inferior y para aliviar el dolor postoperatorio severo y duradero. El objetivo fue determinar la localización anatómica de los nervios tibial (NT) y fibular común (NFC) en el pliegue poplíteo para un bloqueo nervioso efectivo. Se utilizaron 50 miembros inferiores frescos pertenecientes a 27 cadáveres adultos chinos (16 hombres y 11 mujeres, rango de edad entre 35-87 años). Se utilizaron 22 cadáveres para identificar la localización de los nervios y los 5 restantes para determinar la profundidad de los nervios en una sección transversal. El NT se encontró en el 50% de los casos desde el punto más lateral del pliegue poplíteo a 1,4 cm de la superficie. En el 20% de 50 muestras, el nervio cutáneo sural medial se ramificó por debajo o en el pliegue poplíteo, mientras que el NFC se encontró en el 26% de los casos desde el punto más lateral del pliegue poplíteo a 0,7 cm de la superficie. Además, en el 6% de las muestras, el nervio cutáneo sural lateral se ramificó por debajo o en el pliegue poplíteo. Nuestros resultados sugieren que el NT y NFC emergen del nervio ciático a distancias variables del pliegue poplíteo. Creemos que los resultados sobre la ubicación de NT y NFC en el pliegue poplíteo ofrecen una buena guía para el adecuado bloqueo nervioso.