Li Zhaoping, Seeram Navindra P, Lee Rupo, Thames Gail, Minutti Chayo, Wang He-Jing, Heber David
Center for Human Nutrition, David Geffen School of Medicine, University of California, Los Angeles, CA90095-1742, USA.
J Altern Complement Med. 2005 Dec;11(6):1031-8. doi: 10.1089/acm.2005.11.1031.
It is now accepted that inhibition of cholesterol biosynthesis is effective in the primary and secondary prevention of heart disease. However, the perceived side-effects on muscle and liver reduce the general acceptance of statin drug therapy as well as compliance over the long term, which is necessary for prevention efforts to be successful. Chinese red yeast rice (CRYR) is a supplement containing lovastatin (monacolin K), eight other monacolins, pigments, tannins, and other phytochemicals. The authors previously reported on a double- blind placebo-controlled trial of CRYR supplement in 80 individuals demonstrating a significant decrease in cholesterol levels from 250 mg/dL to 210 mg/dL over 8 weeks independent of diet. The current study compared the pharmacokinetics of CRYR with lovastatin at the same bioeffective dose for lowering cholesterol.
Eleven (11) healthy volunteers were randomized to a crossover study taking 2400 mg CRYR or 20 mg of lovastatin.
The Cmax and area under the curve (AUC) of lovastatin were 22.42 ng/mL, and 80.47 higher than CRYR (p = 0.001 and 0.002, respectively). The Cmax for lovastatin hydroxy-acid was 36.63 ng/mL higher than the Cmax of CRYR hydroxy-acid (p = 0.001). The AUC of lovastatin hydroxy-acid was 258.5 greater than that of CRYR (p = 0.001).
The results suggested that the effect of CRYR on the cholesterol concentration might be caused by the additive and/or synergistic effects of monacolin K with other monacolins and substances in CRYR. It may lead to the ultimate development of a botanical supplement based on CRYR.
目前已公认抑制胆固醇生物合成在心脏病的一级和二级预防中有效。然而，他汀类药物疗法对肌肉和肝脏的副作用被认为会降低其总体接受度以及长期依从性，而长期依从性对于预防措施取得成功是必要的。中国红曲米（CRYR）是一种含有洛伐他汀（莫纳可林K）、其他八种莫纳可林、色素、单宁和其他植物化学物质的补充剂。作者之前报道了一项针对80名个体的CRYR补充剂双盲安慰剂对照试验，结果表明在不考虑饮食的情况下，8周内胆固醇水平从250mg/dL显著降至210mg/dL。本研究比较了CRYR与洛伐他汀在相同生物等效剂量下降低胆固醇的药代动力学。
11名健康志愿者被随机分配到一项交叉研究中，分别服用2400mg CRYR或20mg洛伐他汀。
洛伐他汀的Cmax和曲线下面积（AUC）分别为22.42ng/mL和80.47，高于CRYR（分别为p = 0.001和0.002）。洛伐他汀羟酸的Cmax比CRYR羟酸的Cmax高36.63ng/mL（p = 0.001）。洛伐他汀羟酸的AUC比CRYR的AUC大258.5（p = 0.001）。
结果表明，CRYR对胆固醇浓度的影响可能是由莫纳可林K与CRYR中其他莫纳可林及物质的相加和/或协同作用引起的。这可能会最终促成基于CRYR的植物性补充剂的开发。
