Essential phospholipids

Cleves, A.E., McGee, T Whitters, E. A., Champion, K.M., Aitken, J.R., Dowhan, W., Goebl, M., and Bankaitis, VA., 1991b, Mutations in the CDP-choline pathway for phospholipid biosynthesis bypass the requirement for an essential phospholipid transfer protein. Cell 64 789-800. 

EPL In a pilot study, it was possible to achieve recompensation and lasting stabilization in 9 out of 10 patients suffering from severe liver insufficiency by i.v. administration of a new galenic form of polyenylphos-phatidylcholine. (32) This clinical result might be supported by the finding that a considerable deterioration in liver function was associated with a deficit of essential phospholipids (= EPL). (15) (s. p. 865)... 

EPL The substance known as essential phospholipid is the highly purified fraction of phosphatidylcholine with polyunsaturated fatty acids in positions Ci and C2 (= PPC), whereby 1,2 dilinoleylphosphatidylcholine is the main active ingredient. This exact biochemical definition is important, since similar substances do not display the effects of EPL as far as cell protection against toxic substances and inhibition of fibrosis are concerned — as was shown in many experimental and clinical studies. Recommended dosage 3 X 300 mg/day over a longer period of time. (72, 74) (s. p. 865)... 

Prevention of fibrosis is of particular importance. Three substances have already proved their worth in the inhibition of fibrosis essential phospholipids (EPL or PPC), silymarin and UDCA. The antifibrogenic effect of EPL has been demonstrated repeatedly in experiments it is based upon the stimulation of collagenase. (s. fig. 40.3) The antifibrogenic efficacy of silymarin is attributed to the proven inhibition and transformation of Ito cells as well as the reduction in gene expression of ECM and TGF-p. (s. tab. 40.13) Recently, an antifibrogenic effect of UDCA in alcoholic liver disease was also reported. 

Essential phospholipids 3. Glycyrrhizin 4. Silymarin 5. Various herbal preparations ... 

Essential phospholipids are a highly purified phosphatidylcholine fraction containing essential (unsaturated) fatty acids, especially linoleic acid (about 70%), in the... 

The combination of essential phospholipids and silymarin is of special clinical interest because of the cellular targets and modes of action of these two drugs. (268-273) (s. fig. 40.3) (s. tab. 40.13) In patients with chronic hepatitis, a combined EPL-silymarin substance was applied with success (269). Thus, the available results of clinical studies suggest the following indications ... 

Geetha, J., Manjula, R., S lathi, S., Usha, K. Efficacy of essential phospholipid substance of Soya bean oil and Phyllanthus niruri in acute viral hepatitis. J. Gen. Med. (India) 1992 4 53-58... 

Gonciarz, Z., Besser, R, Lelek, E., Gundermann, K.J., Johannes, K.J. Randomized placebo-controlled double blind trial on essential phospholipids in the treatment of fatty liver associated with diabetes. Med. Chir. Dig. 1988 17 61-65... 

Ilic, V., Kordac, V., Alvarez, S.Z. Clinical experience with long-term administration of essential phospholipids in chronic active hepatitis. Review of 3 double-blind studies, (tschech.) Cas. Lek. Ces. 1992 131 801 -804... 

Knntz, E. The essential phospholipids in hepatology. Experimental and clinical experiences. Progr. Hepatol. Pharmacol. 1995 1 156—167... 

Machoy-Mokrzynska, A., Put, A., Ceglecka, M., Mysliwie, Z. Influence of essential phospholipids (EPL) on selected biochemical parameters of lipid metabolism in rats chronically exposed to ammonium fluoride vapours. Eluoride 1994 27 201 -204... 

Since we felt that these observations do not constitute absolute proof that phosphatidylserine is the essential phospholipid in native Na-K ATPase preparations, we have applied another approach. Membranes of jE. coli contain an enzyme, which catalyses the conversion of phosphatidylserine into phosphatidylethanolamine (Kanfer and Kennedy, 1964 Dowhan et al., 1974). Treatment of Na-K ATPase preparations by this enzyme could remove phosphatidylserine without removing any other phospholipids. There is, however, a technical complication the isolated phosphatidylserine decarboxylase requires a non-ionic detergent, such as Triton-X-100, for activity, but this detergent inactivates Na-K ATPase. We were able to overcome this problem, since inorganic phosphate and EDTA reduce the inactivating effect of Triton-X-100 on Na-K ATPase. In order to eliminate the effects of factors present in the phosphatidylserine decarboxylase preparation, we have always used a preheated phosphatidylserine decarboxylase preparation as a control. 

For this reason we have tried to improve the sensitivity of the approach by prior removal of an important part of less essential phospholipids. Extraction of lyophilized cattle brain Na-K ATPase with n-hexane leads to removal of all cholesterol and of 68% (SE 1.8, n=5) of the phospholipids (Fig. 1). There is relatively little difference in extractability of the individual phospholipids, varying from 77% (SE 4.0, n=5) for phosphatidylserine to 61%... 

The lipids of the membrane are essentially phospholipids and sterols. They are amphiphilic molecules, i.e. possessing a hydrophilic and a hydrophobic part. 

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