ABSTRACT
Rosmarinic acid (RA), commonly found in Nepetoidae subfamily of Lamiaceae family, possesses various biological activities. To expand its application, RA was modified by esterification with methyl (me), propyl (pro), and hexyl (hex) alcohols and then tested antibacterial, α-glucosidase inhibitory, and lipid accumulation suppression activities. Consequently, RA derivatives enhanced antibacterial activity, especially the RA-pro and RA-hex, which effectively inhibited the growth of Bacillus cereus rather than tannic acid, a natural antibacterial agent. RA-hex also inhibited α-glucosidase inhibitory activity greater than luteolin. By computational molecular docking, dihydroxyphenyl group and hexyl group were selected as essential groups for interaction with the active site of α-glucosidase through hydrogen bonding and hydrophobic interaction, contributing to the great inhibitory activity. Furthermore, RA-pro and RA-hex effectively suppressed lipid accumulation of 3T3-L1 cells, superior to EGCG, a well-known anti-obesity phytochemical. These biological effects of RA derivatives commonly attributed to hydrophobicity, hydrogen bonding, and steric bulkiness of the side chain. PRACTICAL APPLICATIONS: Rosmarinic acid (RA), a fundamental compound in the family Lamiaceae, is one of powerful naturally occurring antioxidants as well as other biological activities. Furthermore, its abundance in nature was also high in amount in the plant kingdom. So, natural RA can be one of possible natural resources for creating potent natural drugs and biologically useful substances after chemical modification. Studies on various biological activities may intensively expand usage and application of RA. In this study, RA was derivatized to corresponding ester such as methyl, propyl, and hexyl alcohols with higher hydrophobicity, and found great antibacterial, α-glucosidase inhibitory, and lipid accumulation suppression activities. RA-pro and RA-hex significantly suppressed lipid accumulation and cell differentiation. Therefore, RA derivatives with multiple biological activities have the potential to be applied in the food and pharmaceutical industries as food ingredients and supplements.
Subject(s)
Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/pharmacology , Cinnamates/chemistry , Cinnamates/pharmacology , Depsides/chemistry , Depsides/pharmacology , Glycoside Hydrolase Inhibitors/chemistry , Glycoside Hydrolase Inhibitors/pharmacology , Lipid Metabolism/drug effects , 3T3-L1 Cells , Animals , Bacillus cereus/drug effects , Bacillus cereus/growth & development , Esters/chemistry , Esters/pharmacology , Lipids , Mice , Molecular Docking Simulation , Structure-Activity Relationship , alpha-Glucosidases/chemistry , Rosmarinic AcidABSTRACT
OBJECTIVES: Atherosclerotic stenosis of the middle cerebral artery (MCA) is one of the causes of ischemic stroke, but aside from investigations using magnetic resonance angiography (MRA), studies evaluating stenosis are rare. The purpose of this study was to assess dynamic changes of MCA cross section between the systolic and diastolic phases in patients with cerebral infarction using 3·0-Tesla magnetic resonance imaging (3T MRI). METHODS: We assessed 12 stroke patients with M1 stenosis in the MCA and 12 healthy volunteers. We measured MCA cross sections (proximal/distal to stenosis and on the stenosis) in the systolic and diastolic phases by synchronizing imaging with heartbeats, as well as the maximum flow velocity by using cine-phase contrast (PC) MRI. Each patient also underwent conventional MRA. RESULTS: Differences in cross sections between systolic and diastolic phases were significantly smaller in the stenosed artery compared to the distal (P < 0·05) and proximal areas (P < 0·01) in stroke patients. The difference in maximal blood velocity between systolic and diastolic phases at the M1 stenosis was significantly larger than that in the area proximal to the stenosis (P < 0·05). DISCUSSION: We clearly demonstrated dynamic cross-sectional changes in the stenotic areas by 3T MRI, suggesting hemodynamic shear stress, which may further enhance MCA atherosclerosis.
Subject(s)
Intracranial Arteriosclerosis/pathology , Magnetic Resonance Imaging/methods , Middle Cerebral Artery/pathology , Adult , Aged , Aged, 80 and over , Brain Ischemia/pathology , Brain Ischemia/physiopathology , Constriction, Pathologic , Female , Humans , Intracranial Arteriosclerosis/physiopathology , Magnetic Resonance Angiography , Magnetic Resonance Imaging/instrumentation , Male , Middle Aged , Middle Cerebral Artery/physiopathology , Stroke/pathology , Stroke/physiopathologyABSTRACT
The purpose of this study was to improve the visualization of long-axis black-blood imaging of the carotid arteries. We experimented on phantom and in-vivo study of 3 dimension (3D) inversion recovery T(1) turbo field echo combined with phase sensitive inversion recovery (PSIR-3D IR-T(1)TFE) at 3.0 Tesla. As a result, the contrast has been improved by calculated images of PSIR-3D IR-T(1)TFE set to inversion time (TI) 350 ms that is shorter than null point of blood. This displays that the contrast between blood and tissues can be improved when the longitudinal magnetization of blood is a negative. Therefore, the visualization of long-axis black-blood imaging of the carotid arteries has been improved by the calculated images of PSIR-3D IR-T(1)TFE set to TI that is shorter than null point of blood.
