| Clinical Studies | Abstract |
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Inhibition of steroid 5 alpha-reductase by specific aliphatic unsaturated fatty acids.
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Human or rat microsomal 5 alpha-reductase activity, as measured by enzymic conversion of testosterone into 5 alpha-dihydrotestosterone or by binding of a competitive inhibitor, [3H]17 beta-NN-diethulcarbamoyl-4-methyl-4-aza-5 alpha-androstan-3-one ([3H]4-MA) to the reductase, is inhibited by low concentrations (less than 10 microM) of certain polyunsaturated fatty acids. The relative inhibitory potencies of unsaturated fatty acids are, in decreasing order: gamma-linolenic acid greater than cis-4,7,10,13,16,19-docosahexaenoic acid = cis-6,9,12,15-octatetraenoic acid = arachidonic acid = alpha-linolenic acid greater than linoleic acid greater than palmitoleic acid greater than oleic acid greater than myristoleic acid. Other unsaturated fatty acids such as undecylenic acid, erucic acid and nervonic acid, are inactive. The methyl esters and alcohol analogues of these compounds, glycerols, phospholipids, saturated fatty acids, retinoids and carotenes were inactive even at 0.2 mM. The results of the binding assay and the enzymic assay correlated well except for elaidic acid and linolelaidic acid, the trans isomers of oleic acid and linoleic acid respectively, which were much less active than their cis isomers in the binding assay but were as potent in the enzymic assay. gamma-Linolenic acid had no effect on the activities of two other rat liver microsomal enzymes: NADH:menadione reductase and glucuronosyl transferase. gamma-Linolenic acid, the most potent inhibitor tested, decreased the Vmax. and increased Km values of substrates, NADPH and testosterone, and promoted dissociation of [3H]4-MA from the microsomal reductase. gamma-Linolenic acid, but not the corresponding saturated fatty acid (stearic acid), inhibited the 5 alpha-reductase activity, but not the 17 beta-dehydrogenase activity, of human prostate cancer cells in culture. These results suggest that unsaturated fatty acids may play an important role in regulating androgen action in target cells.
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Cytosolic phospholipase A2-driven PGE2 synthesis within unsaturated fatty acids-induced lipid bodies of epithelial cells.
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Cytoplasmic lipid bodies (also known as lipid droplets) are intracellular deposits of arachidonic acid (AA), which can be metabolized for eicosanoid generation. PGE2 is a major AA metabolite produced by epithelial cells and can modulate restoration of epithelium homeostasis after injury. We studied lipid body biogenesis and their role in AA metabolic pathway in an epithelial cell line derived from normal rat intestinal epithelium, IEC-6 cells. Lipid bodies were virtually absent in confluent IEC-6 cells. Stimulation of confluent IEC-6 cells with unsaturated fatty acids, including AA or oleic acid (OA), induced rapid lipid body assembly that was independent on its metabolism to PGE(2), but dependent on G-coupled receptor-driven signaling through p38, PKC, and PI3 K. Newly formed lipid bodies compartmentalized cytosolic phospholipase (cPL)A(2)-alpha, while facilitated AA mobilization and synthesis of PGE(2) within epithelial cells. Thus, both lipid body-related events, including highly regulated biogenesis and functional assembly of cPLA (2)-alpha-driven enhanced AA mobilization and PGE(2)production, may have key roles in epithelial cell-driven inflammatory functions, and may represent relevant therapeutic targets of epithelial pathologies.
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Emu oil(s): a source of non-toxic transdermal anti-inflammatory agents in aboriginal medicine.
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The 'oil' obtained from emu fat can be a very effective inhibitor of chronic inflammation in rats when applied dermally (with a skin penetration enhancer). Assays for this activity using the adjuvant-induced arthritis model have shown: i. Considerable variability in potency of some commercial oil samples; ii. Little or no correlation of activity with colour or linolenic acid (18:3) content of the oil; iii. Relative stability of some active oils (to heat, ageing at room temperature); iv. The bulk of the anti-inflammatory activity was present in a low triglyceride fraction; and v. Potential arthritis-suppressant/immunoregulant activity of these active fractions. These studies point to the need for more rigid quality control before considering such a (now proven) traditional medicine as a complementary therapy.Repeated applications of selected oils did not induce any of the more prominent side-effects associated with NSAIDs (e.g. platelet inhibition, gastrotoxicity) or certain anti-arthritic drugs (proteinuria, leukopenia).
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Anti-inflammatory activity and healing-promoting effects of topical application of emu oil on wound in scalded rats
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OBJECTIVE:
To investigate the effects of topical application of emu oil on wound healing in scalded rats.
METHODS:
In 144 male Wistar rats with 10%; total body surface superficial II degree scald treated on a random basis with physiological saline, povidone iodine and emu oil, respectively, the changes of the wound were observed and the wound tissue and blood samples harvested at different times after injury for evaluation of histopathological changes, total tissue water content (measured by wet:dry weight ratios), and tumor necrosis factor (TNF)-alpha levels in the wound tissue and plasma by enzyme-linked immunosorbent assay (ELISA). The general condition of the wound healing was also observed.
RESULTS:
After application of emu oil, the swelling and effusion of the burn wound were alleviated and evidences of wound infection or adverse effects were not observed. Pathological examination showed that emu oil could alleviate topical inflammation, which was particularly obvious on days 1 and 3 after injury as compared with the other two groups. On day 3 after injury, water content and TNF-alpha level in the tissues was markedly decreased with the application of emu oil (P<0.05), with a significant correlation between their changes (P<0.001) and shortened wound healing time (P<0.05). Pathological examination showed that emu oil could promote epithelialization and differentiation of various epidermal layers.
CONCLUSION:
Emu oil has topical anti-inflammatory activity in rats with superficial II degree scald, possibly in association with decreased levels of the proinflammatory cytokines in the tissues and can promote wound healing by inhibiting local secondary inflammation.
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Effect of emu oil on auricular inflammation induced with croton oil in mice.
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OBJECTIVE:
To determine the acute anti-inflammatory effects of topically applied emu oil.
ANIMALS:
96 male CD-1 mice assigned randomly to 4 groups, each comprising 24 mice.
PROCEDURE:
To induce auricular inflammation, 50 microl of a solution comprising 10 microl of croton oil dissolved in 1 ml of acetone was applied to the inner surface of the left auricle (pinna). One hour later, 3 or 5 microl of emu oil (low- and high-dose groups, respectively) or 5 microl of porcine oil (oil-control) was applied to the left pinna. Control mice remained untreated. Six mice per group were euthanatized 3, 6, 12, and 24 hours after induction of inflammation. Specimens of auricular tissue (ear plugs) were obtained, using a 6-mm biopsy punch. Magnitude of swelling was calculated as the weight difference between left (inflamed) and right (noninflamed) ear plugs; degree of edema was determined as the difference between wet and dry weights of the left ear plug.
RESULTS:
Magnitude of swelling was significantly reduced at 6 and 12 hours in mice treated with emu or porcine oil, compared with controls. The greatest reduction in swelling was detected in the high-dose emu group at 6 hours. Compared with controls, degree of edema was significantly reduced at 6 hours only in the high-dose group, whereas by 12 hours, all groups treated with oils had significantly less edema than controls. At 24 hours, magnitude of swelling and degree of edema did not differ among groups.
CONCLUSION:
Topically applied emu oil significantly reduced severity of acute auricular inflammation induced by croton oil in mice.
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Promotion of second intention wound healing by emu oil lotion: comparative results with furasin, polysporin, and cortisone.
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Previous studies showed that twice-daily application of emu oil lotion (mixture of emu oil/fat, vitamin E, and botanical oil) immediately after creation of full-thickness skin defects delayed wound healing 6 days later, perhaps owing to its antiinflammatory actions. If administration was delayed for 48 hours, a two-fold promotion of wound contraction, epithelialization, and infiltration of organized granulation tissue was observed. In the present study, emu oil lotion was applied to full-thickness skin defects in rodents 24 hours after surgery. Six days postoperatively, wound contraction and infiltration of fronts of epithelialized and granulation tissue were assessed. Results indicated a two-fold promotion of all of the above parameters with emu oil lotion. No such effects were exerted by pure emu oil, furasin, cortaid, or polysporin. Data obtained indicate promise for emu oil lotion as an aid in treating full-thickness skin defects if applied after the major postinflammatory stages of wound healing have transpired.
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Moisturizing and cosmetic properties of emu oil: a pilot double blind study.
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Summary:
Cosmetic and moisturizing properties of emu oil were assessed in a double blind clinical study. Emu oil in comparison to mineral oil was found overall to be more cosmetically acceptable. Furthermore, it appears that emu oil in comparison to mineral oil has better moisturizing properties, superior texture, and lower incidence of comedogenicity, but probably because of the small sample size these differences, were not found to be statistically significant. Neither of the oils were found to be irritating to the skin. Finally, emu oil fatty acid composition was studied by gas chromatography and was found to have high concentration of nonpolar monounsaturated fatty acids, which may explain emu oil's ability to penetrate easily through the stratum corneum barrier.
Introduction:
The emu, a large flightless bird, Dromaius novaehollandiae, is probably best known for being on Australia's coat of arms opposite the kangaroo. In the past few years commercial emu breeding has become a multi-million dollar industry in the United States, Australia, and other countries. Emu oil derived from emu fat was being used by the Aborigines for healing and pain control long before British ships landed on the eastern shores of Australia.
A number of Australian investigators (George Hobday, M.D., a dermatologist and Peter Ghosh, Ph.D., FRSC at the University of Sydney) claimed that emu oil has anti-inflammatory and skin penetrating properties. Recently the Australian Department of health classified emu oil as a pharmaceutical product1 and registered emu oil in the Therapeutic Goods Registry2. Finally an official Australian government publication stated "the oil (emu) will find uses in the pharmaceutical and cosmetic industries". We performed an extensive literature search (Medline, Index Medicus) and could not find a single report in scientific peer reviewed literature dealing with either emu oil or the cosmetic pharmaceutical properties of its composition1. A pilot double blind study was conducted to assess cosmetic properties of emu oil - namely its moisturizing and skin penetrating properties, texture and odor, and irritancy and comedogenicity potential. The emu oil was compared in this study to mineral oil, a synthetic oil that is widely used in the United States as an emulsifier and lubricant in topical cosmetical and pharmaceutical preparations.
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