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Evaluation of epicoprostanol: a major sterol of ambergris for antiinflammatory and antipyretic activities.
Abstract
The major sterol of epicoprostanol was isolated from ambergris by flash column chromatography. Its identity as epicoprostanol was confirmed by 'HNMR and 1 3 ~spec-tros~copy~. ~ Epicoprostanol was studied for its anti-inflammatory and antipyretic activities. Epicoprostanol produced a significant inhibition of carrageenan induced paw oedema. The study on antipyretic activity showed, that epicoprostanol produced a significant reduction of yeast-induced hyperthermia in rat.
... A primary screening profile regarding the cholinergic and/or adrenergic effects of some fractions of ambergris has been reported earlier 13 , and a few reports regarding the effects of ambrein on the cardiovascular system 14 , blood glucose level 15 , edema 16 and mode of action in antinociception 17 have been published from the same laboratory. Similarly, Epicoprostanol has been evaluated from the same laboratory for some hormonal levels, anti-inflammatory and antipyretic activity, changes in plasma biochemistry, protection against experimental models of insulitis and smooth muscle responses have already been published 10,[18][19][20][21][22][23] . ...
The current study evaluated the effects of ambergris on some endocrine hormones, serum lipids, body weights and appetite. A total forty subjects were recruited to receive randomly 415 mg /day of either ambergris (Am; n=20) or placebo (PL; = 20) for 4 weeks. Blood samples were used for the assessments of serum lipids, testosterone, estradiol, growth hormone (GH), prolactin, insulin, thyroxin (T4), and cortisol. Data show significant increase in testosterone, estradiol, prolactin, insulin, cortisol, thyroxin (T4) levels and body weights after ambergris dosing only while growth hormone showed non-significant changes in both groups. A significant increase in total cholesterol (Tc), low density lipoprotein cholesterol (LDLc) and high density lipoprotein cholesterol (HDLc) while significant decrease in triglycerides (TGs) levels in ambergris group were observed. We conclude that ambergris ingestion resulted in; increase of both sexual desire and body weights due to its effect on some endocrine hormones.
Ambergris is the pathological (the only source) secretion of the intestine sperm whale Physeter macrocephalus syn. Physeter catodon belonging to the family Physeteridae. Ambergris has been found only rarely for centuries, as jetsam on beaches all over the world known as Baltic amber. Ambrein is the major constituent of ambergris and responsible for its various pharmacological activities like breakdown of the relatively scentless ambrein through oxidation produces ambroxan and ambrinol, the main odor components of ambergris. Other amber originated from pine plants resin known as sucinum; other amber known as compressed amber, made of small pieces and small stones that melted together under high pressure.
Epicoprostanol (3-alpha-hydroxy-5 beta-cholestanol) has been studied for its effects on blood glucose and plasma insulin levels in rodents. Epicoprostanol significantly induced hypoglycemia and increased insulin levels in rat blood plasma by 88% and 66% compared to that of control after 2 h and 4 h of acute treatment at 100 mg/kg dose. It also highly significantly lowered blood glucose levels in a dose dependent manner at 50, 100 and 200 mg/kg doses when administered to alloxan-rendered moderately diabetic rats after 120 and 240 min of treatment. Similarly, epicoprostanol, with the same dosage regimen, caused hypoglycemia in streptozotocin-induced severe diabetic rats, to a similar extent at the same time-points. However, the lowest dose (10 mg/kg) failed to produce a striking effect in either of the diabetic groups. In normoglycemic rats, plasma insulin levels were affected significantly after a single dose (100 mg/kg) of epicoprostanol. In contrast, diabetic animals suffering from insulitis showed a significant decline in hyperglycemia, strongly suggesting an insulin-like action of epicoprostanol. It seems likely that epicoprostanol acts through a mechanism other than hyperinsulinemia.
Ambrein and epicoprostanol were evaluated for their antioxidant potential in vitro by chemiluminescence (CL), as well as in vivo using lipid peroxides and glutathione levels as indicators in liver tissue of rats treated with adriamycin (doxorubicin) a well known free radicals producing drug. In the in vitro test, the inhibition in CL by ambrein was dose dependent. Both the high concentrations of ambrein (20–40 μg/ml) inhibited CL response significantly (P < 0.05 and P < 0.01, respectively) when compared to control. Similarly two low concentrations (5–20 μg/ml) of epicoprostanol inhibited CL significantly (P < 0.001 and P < 0.01, respectively) in comparison of DMSO control. The high concentration (40 μg/ml) of epicoprostanol behaved exceptionally and caused an increase in CL response that was more than control and significantly (P < 0.001) higher than both the low concentrations. In the in vivo studies adriamycin treatment significantly (P < 0.05) increased malondialdehyde (MDA) and decreased non-protein sulfhydryl (NP-SH) contents in the liver tissue of mice after 5 days treatment. Ambrein (25 and 50 mg/kg) treatment as a solo therapy at both the dose levels significantly (P < 0.001) decreased MDA contents in the liver tissue. On the other hand, in the combined treatment the high dose effectively prevented any rise in MDA contents and it remained around the levels of ambrein alone. In the same experiment, adriamycin declined NP-SH contents significantly (P < 0.001). Ambrein alone at both the dose levels caused a decline (P < 0.01) in NP-SH contents when compared to adriamycin group. But in the combined treatment this decline in NP-SH was significantly (P < 0.05) different from adriamycin alone.
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