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  • Abha et al reported Natural coumarinolignoids isolated from


    Abha et al. reported Natural coumarinolignoids isolated from the seeds of Cleome viscosa consist of a racemic mixture of cleomiscosins A 19, B 20 and C 21 and were screened for anti-inflammatory activity through mol. docking and QSAR studies by using reported in vivo activity of Swiss albino mice. Based on docking binding affinity, a possible mechanism of action has been hypothesized which constitute toll-like receptors (TLR-4), cluster of differentiation mols. (CDs), iNOS, COX-2 and STAT-6 proteins. It was rather interesting to find that the 3D topology of the active site of COX-2 from the docking was in good agreement with QSAR model and in silico ADME/T parameters. Cleomiscosins also showed compliance with 95% of in silico ADME/T properties of available drugs, e.g. serum protein binding, blood-brain barrier, CNS activity, HERG K+ channel activity, apparent Caco-2 permeability, apparent MDCK permeability, skin permeability and human oral pde-5 inhibitors in GI. Besides, toxicity screening study suggests that cleomiscosin molecules possess no toxicity risk parameters [50]. Kohna et al. reported methyl galbanate 2 molecule for the inhibition of a inflammatory mediator, nitric oxide (NO), produced by inducible NO synthase (iNOS) reported as one of the possible causes of neurodegeneration. Methyl galbanate 2 was isolated from Ferula szowitsiana DC. Methyl galbanate was found to attenuate COX-2 mRNA expression only slightly, but significantly. The author further suggests that Me galbanate may be useful for developing a new drug against neurodegenerative diseases [51]. Ma et al. reported isolation and purification of five kinds of coumarin compounds from Angelica gigas Nakai by using recycling-preparative HPLC and identified them as decursin 22, decursinol angelate 23, 7-demethylsuberosine 24, marmesin 25, and decursinol 26 by NMR analyses. The anti-inflammatory activities of the purified compounds were evaluated and compared using the NO concentration assay and western blot analysis on LPS-stimulated RAW 264.7 cells. NO production was significantly suppressed by all the compounds in a dose-dependent manner among which compounds 22, 23, and 24 showed very good activities with IC50 values of 7.4, 6.5, and 7.6μg/mL, respectively. Treatment with compounds 24–26 effectively suppressed the expression levels of iNOS, IL-1β, and COX-2, which are responsible for promoting the inflammatory process [52]. Anti-inflammatory effects of two coumarins, columbianetin 27 and libanoridin 28 isolated from Corydalis heterocarpa in lipopolysaccharide (LPS)-stimulated HT-29 human colon carcinoma cells were studied by Kang et al., further 28 inhibited the protein expression levels of inflammatory mediators such as inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), tumor necrosis factor-α (TNF-α), and interleukin-1β (IL-1β) in a dose-dependent manner in LPS-stimulated HT-29 cells, while 28 showed no activity, Furthermore, it was observed that LPS-induced transcription activity of NF-κB was inhibited by 28. As a result of this study, 28 was found to be a potential anti-inflammatory agent [53]. Taechowisan et al. reported in vitro anti-inflammatory action of 5,7,4′-trimethoxy-4-phenylcoumarin 29 and 5,7-dimethoxy-4-phenylcoumarin 30 produced by Streptomyces aureofaciens CMUAc130. The effects of the two coumarins were investigated on the formation of NO, PGE2, and TNF-α and also on inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) in lipopolysaccharide (LPS)-induced murine macrophage RAW 264.7 cells. The data obtained were consistent with the modulation of iNOS enzyme expression. A similar effect was also observed whilst LPS-induced PGE2 release and COX-2 expression were tested. The inhibitory effects were concentration.-dependent. The 5,7,4′-Trimethoxy-4-phenylcoumarin and 5,7-dimethoxy-4-phenylcoumarin also mildly but significantly reduced the formation of TNF-α [54], [55].