Hawthorn Berries
Hawthorn Berries are gathered from the small tree Crataegus oxyacantha and C. monogyna of the family Rosaceae. Also known as Mayblossom and Whitehorn, Hawthorn was known to Dioscorides in the first century AD, but was not widely used until recent times. Currently about three dozen different preparations containing extracts of Hawthorn are marketed in Germany.
Hawthorn is described in most modern herbals as a valuable treatment for various heart ailments and circulatory disorders, as well acting as a mild astringent to be used for treating sore throats. Hawthorn is most often used to protect against the beginning stages of heart disease for mild heart muscle weakness, pressure and tightness of the chest, and mild arrhythmia. It is also used as a tonic for an aging heart.
The active constituents of hawthorn are flavonoids, oligomeric procyanidins, Crataegus acids and catechin monomers. Some of the therapeutic benefit of Crataegus is due to the antioxidant activity of its various compounds. In one study, the antioxidant activity of various compounds in Crataegus were studied. The most efficient in decreasing order: epicatechin> hyperoside>B2 dimer with the IC50 values expressed in mg/l. These values are less than those from N-actylcysteine, glutathione or mensa (Arzneim.-Forsch./Drug Res 46 (II), 1086
1089, 1996 ).
Tincture of Crataegus was administered to rats fed an atherosclerotic diet. here was significant increase in binding of I-LDL to the liver plasma membranes thought to occur by an up-regulation of LDL receptors. Bile acid excretion increased and hepatic cholesterol synthesis was depressed. This means that the cholesterol in LDL was used in bile acid production not new synthesized cholesterol (Rajendran, et al Atherosclerosis 123, 235-241, 1996).
In an animal study, the release of lactate dehydrogenase from rat hearts was released at a significantly lower rate at onset of reperfusion. The effect was similar to that of the drugs trimetazidine and mepacrine. It has also been found that pretreatment with Crataegus extract produced a reduction in the necrotic zone by a factor of five to six (S. Mackdessi Arsneim.-Forsch/Drug Res. 46 (I) 25-27 1996). Hawthorn's action is not immediate, but develops very slowly, apparently it has a direct effect on the heart itself, especially in cases of heart damage.
The effect of Crataegus extract on contraction and energy turnover was studied on rat cardiomyocytes. When compared to drugs such as isoprenaline, ouabain or elevation of extracellular CA++ concentration, the effects of hawthorn were significantly more economical with respect to the energetics of the myocytes. The extract also prolonged the apparent refractory period in the presence and absence of isoprenaline. This indicates a good antiarrhythmic potential ( S. Popping et al Areneim.-Frosch/Drug Res. 45 (II) 1157-1160, 1995).
Coleus Forskohlii
Coleus Forskohlii contains the compound forskolin which has been shown to be a potent intracellular cAMP (Cyclic Adenosine Monophosphate) elevator. Increased intracellular levels of cAMP are associated with: inhibition of platelet activating factor (PAF), mast cell degranulation, histamine release, relaxation of smooth muscle and arteries, and increased force of contraction in the heart muscle. Forskolin not only acts on cAMP. It also has inhibitory activity on membrane transport and channel proteins.
One of the principal events of heart disease, strokes and peripheral vascular disease is the formation of thromboses. An initiating factor of these clots is the excess activation of PAF. PAF starts a cascade of events that result in clinical symptoms. Forskolin interferes with the binding of PAF to its binding sites. Platelets treated with forskolin exhibited a 30-40% decrease in PAF binding when exposed to PAF (Wong et al (1993) Eur. J. Pharmacol 245:55-61). This activity was not the result of increased cAMP.
Intracellular cAMP is able to regulate the expression of cell receptors. Forskolin was able to down-regulate the mRNA expression and PAF receptor binding similar to oxLDL (Stengel et al (1997) Arterioscler Thromb Vas Biol.17:954-962). PAF is thought to be a contributing factor to atherogenesis. Forskolin’s ability to reduce blood pressure and treat hypertension is through its ability to increase cAMP. The increased cAMP causes the smooth muscles in the arteries to relax. Forskolin has also been found to improve contractility of the heart.
Forskolin’s ability to raise intracellular cAMP and other unelucidated activities makes it useful in the treatment of cardiovascular diseases of hypertension, atherosclerosis, congestive heart failure and angina.
Lutein & Zeaxanthin
There are over 500 naturally occurring carotenoids. Human blood contains between 7 and 20 of these carotenoids. The most abundant being beta-carotene, lutein, zeaxanthin, beta-cryptoxanthin, alpha-carotene and lycopene in that order. Epidemiological studies have shown an inverse relationship between carotenoid consumption and the development of some cancers and macular degeneration. Carotenoids are considered to be lipophilic antioxidant constituents of the blood.
Coronary Heart Disease (CHD) and the formation of atherosclerotic lesions is thought to occur from free radical oxidation of cholesterol rich LDL. The resistance of LDL to oxidative stress is a determining factor in atherogenesis. Lutein and zeaxanthin are stereoisomers of each other and are chemically di-hydroxy carotenoids. On a molar basis lutein is 10 times more effective as an antioxidant than vitamin E when incorporated into LDL in vitro (Chopra et al (1994) Proc. Nutr. Soc. 53:18A). Lutein differs from vitamin E in not only being able to trap lipid peroxyl radicals but can also trap singlet oxygen species. Beta-carotene, in contrast is inactive and slightly pro-oxidant at atmospheric pressure.
A 1995 study compared the difference in CHD between populations in Belfast, Ireland and Toulouse, France (A.N. Howard et al (1996) Internat. J. Vit. Nutr. Res. 66:113-118). People in Toulouse have a much lower incidence of CHD. Plasma levels of antioxidant vitamins and carotenoids were compared. The major difference was in the concentrations of plasma carotenoids. In both sexes, lutein levels were two times higher in France than those in Ireland. Cigarette smoke exposure has been linked to an increase in atherosclerosis. In a 1996 study, human plasma was exposed to the gas phase of cigarette smoke (G. J. Handelman et al Am. J. Clin. Nutr. 63: 559-565). Most of the lipophilic antioxidants were depleted after exposure. Of the carotenoids, lycopene was most susceptible with lutein and zeaxanthin being next. Lutein and zeaxanthin are di-hydroxy carotenoids that are found in highest concentration in dark green leafy vegetables. Beta-carotene reduces their absorption from the intestine (D. Kostic et al (1995) Am. J. Clin. Nutr. 62:604-10). When absorbed, they concentrate in HDL. Lutein and zeaxanthin also accumulate in the macula of the eye and in the lung where they act as antioxidants and have a role in preventing macular degeneration and lung cancer. Their antioxidant properties help to reduce CHD via reduction of atherosclerosis by helping LDL to resist free radical oxidation. They are also involved in buffering the damage caused by cigarette smoke. Lutein and zeaxanthin are included in this formula because of their specific antioxidant function in being anti-atherosclerotic.
