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Hypothesis/purpose: The aim of the present study was to evaluate in vivo the potential anti-ischemic and antiatheromatic activity of Chios Mastic gum, the resin of the trunk and branches of "Pistacia lentiscus var. chia", used since antiquity in traditional Greek medicine. The main compounds of mastic are triterpenes, possessing phytosterol-like structures. This led to the hypothesis that mastic and particularly its neutral fraction, enriched in phytosterol-like compounds, possess antiatheromatic activities., Methods: Total Mastic Extract without Polymer (TMEWP) and the neutral mastic fraction (NMF) were administered orally for 6 weeks to normal fed and to cholesterol fed rabbits in the form of sunflower oil solution. All the animals were randomly divided into 6 groups, anesthetized and subjected to 30min ischemia of the heart, followed by 3h reperfusion: At the end of the experiment the area at risk and the infarct zone were determined with the aid of fluorescent particles and triphenyl tetrazolium chloride staining, and small segments of the ascending and descending aorta and the heart were taken for histologic examination. Blood samples were collected at different time points of ischemia and reperfusion, for malondialdehyde (MDA) evaluation as an index of lipid peroxidation, for total and LDL cholesterol determination and for evaluation of oxidized LDL., Results: In the normal fed animals the NMF and the TMEWP reduced significantly the infarct size, while in the hypercholesterolemic rabbits both treatments were ineffective. Atherosclerosis was detected in all the animals fed cholesterol enriched diet in the form of subintimal accumulation of lipids and foamy macrophages. There was no detection of atherosclerosis in Groups treated with TMEWP and NMF, which both reduced the total cholesterol levels by 47 and 88% respectively, whilst had not effect on LDL oxidation. TMEWP and NMF reduced the MDA concentration in normal fed rabbits, but had no effect on MDA levels in cholesterol fed animals. TMEWP and NMPF reduce the infarct size in normal animals and possess significant antiatheromatic and hypolipidemic activities in rabbits fed cholesterol enriched diet., (Copyright © 2016 Elsevier GmbH. All rights reserved.)

Background: Guggul, herbal extract from resin of the Commiphora mukul tree, is widely used in Asia as a cholesterol-lowering agent based on Indian Ayurvedic medicine. Its popularity for this use is increasing in the US and Western Europe. Guggulsterones, the presumed bioactive compounds of guggul, may antagonise two nuclear hormone receptors involved in cholesterol metabolism, which is a possible explanation for hypolipidemic effects of these extracts. However, publications of efficacy data on the use of guggul extracts in Western populations are scarce., Objective: To study the efficacy of a guggul-based formulation (short: guggul) on blood lipids in healthy adults with moderately increased cholesterol., Methods: Double-blind, randomised, placebo controlled trial in Norwegian general practice. 43 women and men, age 27-70, with moderately increased cholesterol, randomised to use 2160mg guggul (4 capsules) daily, or placebo for 12 weeks., Outcome Measures: Mean change in total cholesterol, low-density lipoprotein cholesterol (LDL-C), triglycerides, high-density lipoprotein cholesterol (HDL-C) and total cholesterol/HDL-C ratio compared with baseline. Lipids were analysed at baseline, and at 6 and 12 weeks. In addition, unexpected events and adverse effects were recorded., Results: Two dropouts, one withdrawal, and incomplete lab results for six persons left 34 participants to accomplish the trial (18-guggul, 16-placebo) with complete lab test data. After 12 weeks, mean levels of total cholesterol and HDL-C in the active group were significantly reduced compared with the placebo group. However, the mean levels of LDL-C, triglycerides, and total cholesterol/HDL-C ratio between the two groups did not change significantly. Ten guggul users (vs. four in the placebo group) reported side effects: mild gastrointestinal discomfort (n=7), possible thyroid problems (n=2), and generalized skin rash (n=1). The latter resulted in withdrawal from trial., Conclusions: Even if total cholesterol and HDL-C were significantly reduced, the clinical magnitude of this remains obscure. More and larger studies are needed to establish effects and safety of guggul-based formulations in the treatment for hypercholesterolemia.

There are indications that treatment of hypercholesterolemia by means of drugs reduce risk of atherosclerosis in patients with increased concentrations of atherogenic lipoproteins. Such therapy should be initiated only after satisfactory exclusion of secondary causes of hyperlipoproteinemia, and should be regarded as an adjunct to appropriate dietary therapy. Drug therapy should be strongly considered in patients with total cholesterol above 8-9 mmol/l on diet therapy only. Drug therapy should be considered at even lower concentrations of cholesterol when coronary heart disease is present and in familial forms of hyperlipidemia when increased risk of atherosclerosis has been documented. In patients with increased plasma concentrations of total cholesterol the drugs of choice are agents which enhance the rate of LDL catabolism (resins) or reduce the rate of LDL synthesis (nicotinic acid). Fibrates should be used when triglycerides and cholesterol are both increased. HMG CoA reductase inhibitors offer considerable promise in the therapy of patients with primary hypercholesterolemia. Probucol may be used in combination with other drugs, particularly when xanthomas are present in patients with familial hypercholesterolemia.

In 16 children heterozygous for familial hypercholesterolemia, two- to three-year therapy with diet and cholestyramine resin (16 gm/day) was assessed in terms of effectiveness, practicality, and safety. All 16 children had previously taken a low-cholesterol (less than 300 mg/day), polyunsaturate-rich (P/S ratio, 1.5:1) diet and choeltyramine resin (12 gm/day) for 12 months. In this study, the cholestyramine resin dose was increased to 16 gm/day, and follow-up was maintained through months 13 through 18, 19 through 24, 25 through 30, and 31 through 36. Eleven children had good drug adherence (four packs of cholestyramine per day) and five children had fair adherence (two to three packs per day). Plasma total cholesterol and low-density lipoprotein (LDL) cholesterol levels were not significantly lowered on the drug-plus-diet regimen as compared to diet alone in five children with fair drug adherence. For children with good drug adherence, mean plasma cholesterol level was lowered below levels achieved on diet alone by 13% (months 13 through 18), 12% (months 19 through 24), 12% (months 25 through 30), and 11% (months 31 through 36) (P less than .05). Reduction in plasma cholesterol level was no greater with 16 than with 12 gm of cholestyramine per day. There were no group changes in mean plasma triglyceride levels. Cholestyramine resin, when added to diet and maintained for two to three years effects a significant reduction in total and LDL cholesterol levels in about 60% of children heterozygous for familial hypercholesterolemia. Continued reinforcement of both diet and drug adherence is necessary in the face of gradual increments in plasma cholesterol level with time.