A structure-based approach was used to optimize our new class of quinoline LXR modulators leading to phenyl acetic acid substituted quinolines 15 and 16. Both compounds displayed good binding affinity for LXRbeta and LXRalpha and were potent activators in LBD transactivation assays. The compounds also increased expression of ABCA1 and stimulated cholesterol efflux in THP-1 cells. Quinoline 16 showed good oral bioavailability and in vivo efficacy in a LDLr knockout mouse model for lesions.

The pharmacological importance of cannabidiol (CBD) has been in study for several years. CBD is the major nonpsychoactive constituent of plant Cannabis sativa and its administration is associated with reduced side effects. Currently, CBD is undergoing a lot of research which suggests that it has no addictive effects, good safety profile and has exhibited powerful therapeutic potential in several vital areas. It has wide spectrum of action because it acts through endocannabinoid receptors; CB1 and CB2 and it also acts on other receptors, such as GPR18, GPR55, GPR 119, 5HT1A, and TRPV2. This indicates its therapeutic value for numerous medical conditions because of its neuroprotective and immunomodulatory properties. Potential therapeutic applications of CBD include, analgesic, anti-inflammatory, anxiolytic, anti-arthritic, anti-depressant, anti-Alzheimer disease, anti-ischemic, neuroprotective, and anti-fibrotic. More promising areas appear to include diabetes and cancer where CBD exhibits lesser side effects and more therapeutic benefits as compared to recent available medical therapies. Hence, CBD is a promising substance for the development of new drug. However further research and clinical studies are required to explore its complete potential.

No abstract

This study evaluates the antioxidant activity of Ranunculus muricatus and isolation and structure elucidation of the active constituents. The aerial parts of the plants were shade dried at room temperature and powdered and extracted with methanol. The free radical scavenging activity was evaluated by 1,1-diphenyl-2-picryl-hydrazyl (DPPH) assay. The percentage scavenging activity was determined based on the percentage of DPPH radical scavenged. Column chromatography was used in order to isolate the active compounds. Spectral techniques UV, IR, 1H NMR, 13CNMR and HREI-MS were used for the structure elucidation of the isolated compounds. Two isolated compounds, A (caffeoyl-β-d-glucopyranoside) and B (1,3-dihydroxy-2-tetracosanoylamino-4-(E)-nonadecene), exibited a significant antioxidant activity as showed by DPPH radical scavenging method. Percentage inhibition for compound A (at 0.5 mM) was 82.67 ± 0.19 with IC50 of 93.25 ± 0.12 (μM), and for compound B (at 0.5 mM) was 69.23 ± 0.19 with IC50 of 183.34 ± 0.13 (μM). Quercetin was used as standard control. It was conclued from the present study that caffeoyl-β-d-glucopyranoside and 1,3-dihydroxy-2-tetracosanoylamino-4-(E)-nonadecene isolated from methanol extract of aerial parts of Ranunculus muricatus posses antioxidant activity.

No abstract