(Lauraceae) is an endemic plant in Taiwan. One new carboline alkaloid, demethoxydaibucarboline A (), two new eudesmanolide-type sesquiterpenes, methyl-neolitacumone A (), neolitacumone E (), and twelve known compounds (-) were isolated from the root of Their structures were elucidated by spectroscopic analysis. Glucuronidation represents a major metabolism process of detoxification for carcinogens in the liver. However, intestinal bacterial β-Glucuronidase (βG) has been considered pivotal to colorectal carcinogenesis. To develop specific bacterial-βG inhibitors with no effect on human βG, methanolic extract of roots of was selected to evaluate their anti-βG activity. Among the isolates, demethoxydaibucarboline A () and quercetin () showed a strong bacterial βG inhibitory effect with an inhibition ratio of about 80%. Methylneolitacumone A () and epicatechin () exhibited a moderate or weak inhibitory effect and the enzyme activity was less than 45% and 74%, respectively. These four compounds specifically inhibit bacterial βG but not human βG. Thus, they are expected to be used for the purpose of reducing chemotherapy-induced diarrhea (CID). The results suggest that the constituents of have the potential to be used as CID relief candidates. However, further investigation is required to determine their mechanisms of action.
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http://dx.doi.org/10.3390/molecules25215170 | DOI Listing |
Anal Bioanal Chem
November 2024
Fujian Key Laboratory of Drug Target Discovery and Structural and Functional Research, School of Pharmacy, Fujian Medical University, Fuzhou, 350004, China.
α-Glucosidase (α-Glu) is implicated in the progression and pathogenesis of type II diabetes (T2D). In this study, we developed a rapid colorimetric technique using platinum nanoparticles stabilized by chitosan (Ch-PtNPs) to detect α-Glu activity and its inhibitor. The Ch-PtNPs facilitate the conversion of 3,3',5,5'-tetramethylbenzidine (TMB) into oxidized TMB (oxTMB) in the presence of dissolved O.
View Article and Find Full Text PDFExp Mol Med
February 2023
Department of Biomedical Sciences, Asan Medical Center, University of Ulsan College of Medicine, Seoul, 05505, South Korea.
Int J Pharm
November 2022
School of Pharmacy, The University of Jordan, Amman, Jordan. Electronic address:
The objective of this study was to develop and evaluate an effective topical formulation to promote corneal epithelial wound healing. Ascorbyl glucoside (AA-2G), a stable prodrug of AA, was formulated in solid in oil (S/O) nanodispersions by emulsifying AA-2G solutions in cyclohexane using Span 85 as an emulsifying agent and freeze-drying emulsions to produce AA-2G - surfactant complex. The complexes were then dispersed in castor oil to produce S/O nanodispersions which were evaluated in terms of their particle size, polydispersity index, encapsulation efficiency, morphology, physical stability as well as the transcorneal permeation and accumulation of AA-2G.
View Article and Find Full Text PDFSheng Wu Gong Cheng Xue Bao
July 2022
Institute of Biomedicine, Jinan University, Guangzhou 510632, Guangdong, China.
-ascorbic acid 2-glucoside (AA-2G) is a derivative of -ascorbic acid (-AA). Compared with -AA, it has good stability and is easily decomposed by enzyme in the human body. α-Glucosidase (AG) was the first enzyme found capable of producing AA-2G.
View Article and Find Full Text PDFBiosens Bioelectron
October 2022
State Key Laboratory of Electroanalytical Chemistry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun, Jilin, 130022, China; School of Applied Chemistry and Engineering, University of Science and Technology of China, Hefei, Anhui, 230026, China. Electronic address:
A facile and sensitive method for sensing α-glucosidase (α-glu) and screening its inhibitors based on fluorescence monitoring of water-solute silicon-containing nanoparticles (Si CNPs) was proposed and demonstrated. Such fluorescent nanoparticles can be easily produced by mixing (3-aminopropyl) trimethoxysilane (APTMS) and ascorbate sodium (AS) (both without fluorescence signals) at room temperature and pressure. If the ascorbate sodium was replaced by L-ascorbic acid-2-O-α-D-glucopyranosyl (AA2G), which can be hydrolyzed into the former by α-glu, the fluorescence "turn-on" biosensor for α-glu activity can be established.
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