PGE2-16,16-dimethyl

Mechanisms of cytoprotection have been the subject of a symposium and a review,Interest has centred on the "mucus-bicarbonate barrier" as prostaglandins have been shown to stimulate bicarbonate secretion in both stomach and duodenum of rats, cats and dogs. In the dog PGE2, 16,16-dimethyl PGE2, 2a stable prostacyclin... 

PGE andDenvatives. PGE2 and several related PGs protect against radiation injury in the rodent intestine with respect to both crypt clonogen survival and LD Q g Protection of hemopoietic tissue has also been reported using the exogenous CEU-S assay (215), and 40 p.m of 16,16-dimethyl PGE2... 

The plant is strongly aromatic on account of an essential oil which comprises cis-a-ocimene (25.11%), 3,7-dimethyl-l,6-octadien-3 ol (16.85%), and trans-nerolidol (13.89%), hence the use of the plant in aromatherapy. A methanolic extract of bark of Litsea cubeba (Lour.) Pers. and its fractions (0.01 mg/mL) from bark inhibit NO and PGE2 production in LPS-activated RAW 264.7 macrophages without significant cytotoxicity at less than 0.01 mg/mL concentration. The methanol extract decreased the enzymatic activity of myeloperoxidase (0.05 mg/mL). These findings suggest that L. cubeba is beneficial for inflammatory conditions and may contain compound(s) with anti-inflammatory properties (63). Can we expect the vasorelaxant laurotetanine (64) isolated from the plant to exert such activity ... 

Rush B, Merritt MV, Kaluzny M, et al. 1986. Studies on the mechanism of the protective action of 16,16-dimethyl PGE2 in carbon tetrachloride induced acute hepatic injury in the rat. Prostaglandins 32 439-455. 

Using various doses, dose-response curves can be established and potency ratios calculated. 16,16-dimethyl PGE2 was found to be the most active compound and can be used as standard to estimate the diarrhoeic side effect potential of candidate compound. 

Robert, A., Magerlein, B. J., 15-Methyl PGE2 and 16,16-dimethyl PGE2. Potent inhibitors of gastric secretion, Adv. Biosci. 1973, 9, 247-253. 

GSTM2-2—Dopa o-quinones, PGH2 to PGE2, DCNB-high, CDNB-high, aminochrome, 2-cyano-l,3-dimethyl-lnitroso-guanidine. 

PGE-dependent heterologous desensitization has also been shown to occur in rat liver. Treatment of rats with 16,16-dimethyl PGE2 caused a loss in the ability of rat liver membranes to synthesize cAMP when stimulated by glucagon, NaF or forskolin. This general loss of adenylate cyclase activity correlated with decreased levels of as measured both by reconstitution of cyclase stimulatory activity into the cyc membrane system and by the amount of cholera toxin substrate. Since 16,16-dimethyl PGE2 appears to act via hepatic stimulatory PGE receptors ° this derivative may act via this receptor to cause a decreased level of and perhaps also cyclase catalytic activity. 

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