RB-2 and RB-4 are two structural analogs of polyacetylene from Radix Bupleuri that show antidepressant effects. However, no metabolic data are available to elucidate their systemic homeostasis. Mass spectrometry combined with liver microsomes and recombinant drug-metabolizing enzymes were performed to profile the biotransformations of RB-2/RB-4 in vitro and in vivo. Oxidation should be the major metabolic pathways for them in phase I, while CYP2C9 and CYP2E1 was the major contributor. In phase II, conjugational groups usually combined with the metabolites from phase I. This study provides an important reference basis for the safety evaluation and rational application of RB-2/RB-4.

2019-11-01·Microbial Pathogenesis3区 · 医学

Isolation of flavonoids from the flowers of Rhynchosia beddomei Baker as prominent antimicrobial agents and molecular docking

3区 · 医学

Article

作者: Bhaskar, Baki Vijaya ; Gunasekar, Duvvuru ; Zyryanov, Grigory V ; Rao, Veeramallu Lakshmana ; Venkateswarlu, Nagam ; Rammohan, Aluru

Rhynchosia beddomei Baker (R. beddomei) is a viscous hairy under shrub, belongs to the family of Fabaceae and widely distributed in Deccan and Carnatic regions of South India. In the present investigation, four flavonoids such as an isoflavone, 5,7-dihydroxy-4'-methoxyisoflavone (RB-1), a flavonol, quercetin-7-O-methylether (RB-2), two flavone C-glycosides, isovitexin (RB-3) and 5,7,3',4'-tetrahydroxy-6-C-β-d-glucopyranosyl flavone (RB-4) were isolated from the flowers of R. beddomei Baker through bioassay guided fractionation. Subsequently, antimicrobial activity of compounds against drug resistant gram positive and negative bacteria and fungi revealed RB-2 and RB-4 have shown highest minimal inhibition concentrations against Pseudomonas aeruginosa and Candida albicans. RB-2 and RB-4 enclosed OH groups at 5th position on the ring A, 3' and 4' ortho dihydroxyl groups positioned on the ring B and accomplished efficacious antibacterial activity. In addition, Docking studies perceptible that RB-4 conferred highest binding energy of -10.5 kcal/mol and exhibited eloquent polar and non-polar interactions with active site residues of N-Myristoyltransferase (Nmt) of Candida albicans while binding energy of -7.5 kcal/mol was recorded for peptidyldeformylase (PaPDF) of Pseudomonas aeruginosa. Moreover, these compounds obey Lipinski's rule of five and exerts good drug likeness properties and might be ratified as lead molecules for further investigations to prevent panicking microbial infections.

2018-07-01·Chemosphere2区 · 环境科学与生态学

Immobilization of peroxidase on polypyrrole-cellulose-graphene oxide nanocomposite via non-covalent interactions for the degradation of Reactive Blue 4 dye

2区 · 环境科学与生态学

Article

作者: Husain, Qayyum ; Ahmad, Masood ; Ali, Misha ; Sultana, Saima

In the present study novel polypyrrole-cellulose-graphene oxide nanocomposite (PCeGONC) was employed for the immobilization of ginger peroxidase (GP) via simple adsorption mechanism. Immobilization of enzyme on the obtained support resulted in enhancement of the enzyme activity. The recovery of activity was 128% of the initial activity. Consequently, in 3 h stirred batch treatment, PCeGONC bound GP exhibited higher decolorization efficiency (99%) for Reactive Blue 4 (RB 4) dye as compared to free GP (88%). The immobilized GP exhibited higher operational stability and retained approximately 72% of its initial activity even after ten sequential cycles of dye decolorization in batch process. The kinetic characterization of PCeGONC bound GP revealed slightly lower K_m and 3.3 times higher V_max compared to free GP. Degraded products were identified on the basis of GC-MS analysis and degradation pathway was proposed accordingly which confirms enzymatic breakdown of RB 4 into low molecular weight compounds. Genotoxic assessment of GP treated RB 4 revealed significant reduction of its genotoxic potential. In-silico analysis identified that binding site of PCeGONC on enzyme is distinct and lies far away from the active site of the enzyme. Furthermore, it also revealed higher affinity of 1-hydroxybenzotriazole (a redox mediator) and RB 4 for PCeGONC bound enzyme as compared to the free enzyme. This is in consensus with the observed decrease in K_m of the immobilized GP.

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适应症	最高研发状态	国家/地区	公司	日期
高肿瘤突变负荷肿瘤	临床1期	中国	瑞阳（苏州）生物科技有限公司	2021-03-18
淋巴瘤	临床1期	中国	瑞阳（苏州）生物科技有限公司	2021-03-18
MSI-H 癌症	临床1期	中国	瑞阳（苏州）生物科技有限公司	2021-03-18