scholarly journals Hypoglycemic active principles from the leaves of Bauhinia holophylla: Comprehensive phytochemical characterization and in vivo activity profile

PLoS ONE ◽  
2021 ◽  
Vol 16 (9) ◽  
pp. e0258016
Author(s):  
Luiz Leonardo Saldanha ◽  
Aislan Quintiliano Delgado ◽  
Laurence Marcourt ◽  
Nathalia Aparecida de Paula Camaforte ◽  
Priscilla Maria Ponce Vareda ◽  
...  

Bauhinia holophylla leaves, also known as "pata-de-vaca", are traditionally used in Brazil to treat diabetes. Although the hypoglycemic activity of this medicinal plant has already been described, the active compounds responsible for the hypoglycemic activity have not yet been identified. To rapidly obtain two fractions in large amounts compatible with further in vivo assay, the hydroalcoholic extract of B. holophylla leaves was fractionated by Vacuum Liquid Chromatography and then purified by medium pressure liquid chromatography combined with an in vivo Glucose Tolerance Test in diabetic mice. This approach resulted in the identification of eleven compounds (1–11), including an original non-cyanogenic cyanoglucoside derivative. The structures of the isolated compounds were elucidated by nuclear magnetic resonance and high-resolution mass spectrometry. One of the major compounds of the leaves, lithospermoside (3), exhibited strong hypoglycemic activity in diabetic mice at the doses of 10 and 20 mg/kg b.w. and prevents body weight loss. The proton nuclear magnetic resonance (1H NMR) quantification revealed that the hydroalcoholic leaves extract contained 1.7% of lithospermoside (3) and 3.1% of flavonoids. The NMR analysis also revealed the presence of a high amount of pinitol (4) (9.5%), a known compound possessing in vivo hypoglycemic activity. The hypoglycemic properties of the hydroalcoholic leaves extract and the traditional water infusion extracts of the leaves of B. holophylla seem thus to be the result of the activity of three unrelated classes of compounds. Such results support to some extent the traditional use of Bauhinia holophylla to treat diabetes.

1985 ◽  
Vol 5 (2) ◽  
pp. 267-274 ◽  
Author(s):  
Hiroyuki Kato ◽  
Kyuya Kogure ◽  
Hitoshi Ohtomo ◽  
Muneshige Tobita ◽  
Shigeru Matsui ◽  
...  

Evaluation of ischemic brain injury in experimental cerebral infarction in gerbils and rats was performed by means of both proton nuclear magnetic resonance imaging ([1H]NMR-CT) and various histochemical analyses. In vivo nuclear magnetic resonance (NMR) imaging was carried out employing saturation recovery, inversion recovery, and spin echo pulse sequences. Spatial resolution of the images was excellent. The ischemic lesions were detected with a remarkable contrast in inversion recovery and spin echo images within a few hours after insult. Those changes in NMR images consistently corresponded with the various retrospective histochemical observations, especially with methods related to brain edema (K+ staining) rather than structural (enzymatic) studies. Calculated T1 and T2 relaxation times indicated the evolution of the edema state in the brain in situ. They correlated excellently with the retrospective water content measurement. As a result, detailed characterization of the edema state induced by cerebral ischemia was possible in vivo using [1H]NMR imaging.


2021 ◽  
Author(s):  
Sait SARI ◽  
Mehmet YILMAZ

Abstract Novel acrylamide and methacryloyl carrying piperazine-dihydrofuran derivatives ( 3a-p ) were designed and obtained from radical cyclizations of unsaturated piperazine derivatives ( 1a-f ) with 1,3-dicarbonyl compounds ( 2a-c ) mediated by Mn(OAc) 3 . Structures of obtained compounds were confirmed with 1 H NMR (proton nuclear magnetic resonance), 13 C NMR (Carbon-13 nuclear magnetic resonance), HRMS (High resolution mass spectrometry), FTIR (Fourier-transform infrared spectroscopy and melting point analysis. Inhibitory activites of all piperazine-dihydrofuran compounds were evaluated against AChE (Acetylcholinesterase) by Ellman method and test results showed that 3a , 3c , 3j and 3l are most active AChEI’s (AChE inhibitors) of our work with IC 50 (half-maximal inhibitory concentration) values of 2.62, 5.29, 1.17 and 3.90 µM, respectively. Furthermore, ligand-protein interactions and inhibitory activity mechanisms of 3a and 3j were investigated by molecular docking. Finally, in silico molecular property and ADME (absorption, distribution, metabolism and excretion) of potential AChEI’s (AChE inhibitor) were predicted by PreADMET and Molinspiration webservers. It can be concluded that the lead compound 3j show excellent inhibiton and satisfactory druglike characteristics.


2021 ◽  
Vol 12 ◽  
Author(s):  
Sylvana Vilca-Melendez ◽  
Malin V. Uthaug ◽  
Julian L. Griffin

While psychedelics may have therapeutic potential for treating mental health disorders such as depression, further research is needed to better understand their biological effects and mechanisms of action when considering the development of future novel therapy approaches. Psychedelic research could potentially benefit from the integration of metabonomics by proton nuclear magnetic resonance (1H NMR) spectroscopy which is an analytical chemistry-based approach that can measure the breakdown of drugs into their metabolites and their metabolic consequences from various biofluids. We have performed a systematic review with the primary aim of exploring published literature where 1H NMR analysed psychedelic substances including psilocin, lysergic acid diethylamide (LSD), LSD derivatives, N,N-dimethyltryptamine (DMT), 5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT) and bufotenin. The second aim was to assess the benefits and limitations of 1H NMR spectroscopy-based metabolomics as a tool in psychedelic research and the final aim was to explore potential future directions. We found that the most current use of 1H NMR in psychedelic research has been for the structural elucidation and analytical characterisation of psychedelic molecules and that no papers used 1H NMR in the metabolic profiling of biofluids, thus exposing a current research gap and the underuse of 1H NMR. The efficacy of 1H NMR spectroscopy was also compared to mass spectrometry, where both metabonomics techniques have previously shown to be appropriate for biofluid analysis in other applications. Additionally, potential future directions for psychedelic research were identified as real-time NMR, in vivo1H nuclear magnetic resonance spectroscopy (MRS) and 1H NMR studies of the gut microbiome. Further psychedelic studies need to be conducted that incorporate the use of 1H NMR spectroscopy in the analysis of metabolites both in the peripheral biofluids and in vivo to determine whether it will be an effective future approach for clinical and naturalistic research.


Sign in / Sign up

Export Citation Format

Share Document