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Triterpenic Acids Present in Hawthorn Lower Plasma Cholesterol by Inhibiting Intestinal ACAT Activity in Hamsters.
- 1
- Unilever Food and Health Research Institute, Unilever R&D Vlaardingen, P.O. Box 114, 3130 AC Vlaardingen, The Netherlands.
Abstract
Hawthorn (Crataegus pinnatifida) is an edible fruit used in traditional Chinese medicine to lower plasma lipids. This study explored lipid-lowering compounds and underlying mechanisms of action of hawthorn. Hawthorn powder extracts inhibited acylCoA:cholesterol acyltransferase (ACAT) activity in Caco-2 cells. The inhibitory activity was positively associated with triterpenic acid (i.e., oleanolic acid (OA) and ursolic acid (UA)) contents in the extracts. Cholesterol lowering effects of hawthorn and its potential additive effect in combination with plant sterol esters (PSE) were further studied in hamsters. Animals were fed a semi-synthetic diet containing 0.08% (w/w) cholesterol (control) or the same diet supplemented with (i) 0.37% hawthorn dichloromethane extract, (ii) 0.24% PSE, (iii) hawthorn dichloromethane extract (0.37%) plus PSE (0.24%) or (iv) OA/UA mixture (0.01%) for 4 weeks. Compared to the control diet, hawthorn, PSE, hawthorn plus PSE and OA/UA significantly lowered plasma non-HDL (VLDL + LDL) cholesterol concentrations by 8%, 9%, 21% and 6% and decreased hepatic cholesterol ester content by 9%, 23%, 46% and 22%, respectively. The cholesterol lowering effects of these ingredients were conversely associated with their capacities in increasing fecal neutral sterol excretion. In conclusion, OA and UA are responsible for the cholesterol lowering effect of hawthorn by inhibiting intestinal ACAT activity. In addition, hawthorn and particularly its bioactive compounds (OA and UA) enhanced the cholesterol lowering effect of plant sterols.
Figure 1
HPLC profile of the triterpenic acids in the dichloromethane extract of the dried hawthorn fruit powder is depicted. Dried hawthorn fruit powder was extracted sequentially with ethanol by using Soxhlet extractor at 80°C, followed by a dichloromethane extraction of the dried ethanol extract. Signal detection was carried out at 210 nm. Peak numbers: 1, (unknown); 2, OA; 3, UA; and 4, (unknown).
Evid Based Complement Alternat Med. 2011;2011:801272.
Figure 2
Hepatic FC and CE concentrations of hamsters fed the control and treatment diets for 4 weeks. A 300 mg portion of liver tissue from each animal was homogenized. Lipids were extracted using the method described by Bligh and Dyer and total cholesterol and FC were measured enzymatically. Concentration of CE was calculated as the difference between total cholesterol and FC. Data are presented as mean ± SE (n = 20 animals per group). *P < .01 as compared to control.
Evid Based Complement Alternat Med. 2011;2011:801272.
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