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  • Yang et al studied anti inflammatory and

    2020-07-29

    Yang et al. studied anti-inflammatory and antioxidant activities of methanol extract of the fruits of Foeniculum vulgare (F. vulgare) traditionally used to treat inflammatory diseases. Four coumarins viz scopoletin 13, 8-methoxypsoralen 14, bergapten 15 and imperatorin 16 were isolated. Although four coumarins isolated from the fruits of F. vulgare provide effective anti-inflammatory and antioxidant activities, imperatorin was found to be most potent [46]. Shokoohinia et al. studied acetone extracts of Prangos ferulacea (Apiaceae), a perennial plant found in the Middle-East, where it RS 127445 HCl mg is commonly used as an antispasmodic and anti-inflammatory agent and is a rich source of coumarins. Several coumarins from P. ferulacea were isolated and screened and isoimperatorin 17 was found to be a cyclooxygenase-2 inhibitor [47]. Hemshekhar et al. reported a significant amelioration of the upregulated non-enzymic inflammatory markers such as TNF-α, IL-1β, IL-6, COX-2 and PGE2 [48] by 4-methyl esculetin 18. Hwang et al. reported Phenylpropanoids and coumarins isolated from Ailanthus altissima were screened for COX-1/COX-2 inhibition. These findings suggested that new synthetic phenylpropanoid derivatives good activity and were potential selective COX-2 inhibitors [49]. 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 RS 127445 HCl mg 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 absorption 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].