Szapary Philippe O, Wolfe Megan L, Bloedon LeAnne T, Cucchiara Andrew J, DerMarderosian Ara H, Cirigliano Michael D, Rader Daniel J
Department of Medicine, University of Pennsylvania School of Medicine, Philadelphia 19104-6021, USA.
JAMA. 2003 Aug 13;290(6):765-72. doi: 10.1001/jama.290.6.765.
Herbal extracts from Commiphora mukul (guggul) have been widely used in Asia as cholesterol-lowering agents, and their popularity is increasing in the United States. Recently, guggulsterones, the purported bioactive compounds of guggul, have been shown to be potent antagonists of 2 nuclear hormone receptors involved in cholesterol metabolism, establishing a plausible mechanism of action for the hypolipidemic effects of these extracts. However, there are currently no published safety or efficacy data on the use of guggul extracts in Western populations.
To study the short-term safety and efficacy of 2 doses of a standardized guggul extract (guggulipid, containing 2.5% guggulsterones) in healthy adults with hyperlipidemia eating a typical Western diet.
Double-blind, randomized, placebo-controlled trial using a parallel design, conducted March 2000-August 2001.
A total of 103 ambulatory, community-dwelling, healthy adults with hypercholesterolemia in the Philadelphia, Pa, metropolitan area.
Oral, 3 times daily doses of standard-dose guggulipid (1000 mg), high-dose guggulipid (2000 mg), or matching placebo.
Percentage change in levels of directly measured low-density lipoprotein cholesterol (LDL-C) after 8 weeks of therapy. Secondary outcome measures included levels of total cholesterol, high-density lipoprotein cholesterol (HDL-C), triglycerides, and directly measured very low-density lipoprotein cholesterol (VLDL-C), as well as adverse events reports and laboratory safety measures including electrolyte levels and hepatic and renal function.
Compared with participants randomized to placebo (n = 36), in whom levels of LDL-C decreased by 5%, both standard-dose guggulipid (n = 33) and high-dose guggulipid (n = 34) raised levels of LDL-C by 4% (P =.01 vs placebo) and 5% (P =.006 vs placebo), respectively, at 8 weeks, for a net positive change of 9% to 10%. There were no significant changes in levels of total cholesterol, HDL-C, triglycerides, or VLDL-C in response to treatment with guggulipid in the intention-to-treat analysis. While guggulipid was generally well tolerated, 6 participants treated with guggulipid developed a hypersensitivity rash compared with none in the placebo group.
Despite plausible mechanisms of action, guggulipid did not appear to improve levels of serum cholesterol over the short term in this population of adults with hypercholesterolemia, and might in fact raise levels of LDL-C. Guggulipid also appeared to cause a dermatologic hypersensitivity reaction in some patients.
没药树（guggul）的草药提取物在亚洲已被广泛用作降胆固醇药物，在美国其受欢迎程度也在不断提高。最近，没药甾酮，据称是没药的生物活性化合物，已被证明是参与胆固醇代谢的两种核激素受体的有效拮抗剂，为这些提取物的降血脂作用建立了一个合理的作用机制。然而，目前尚无关于没药提取物在西方人群中使用的安全性或有效性数据发表。
研究两种剂量的标准化没药提取物（guggulipid，含2.5%没药甾酮）对食用典型西方饮食的健康高脂血症成年人的短期安全性和有效性。
2000年3月至2001年8月进行的双盲、随机、安慰剂对照试验，采用平行设计。
宾夕法尼亚州费城大都市地区共有103名非卧床、居住在社区的健康高胆固醇血症成年人。
口服，每日3次，标准剂量的guggulipid（1000毫克）、高剂量的guggulipid（2000毫克）或匹配的安慰剂。
治疗8周后直接测量的低密度脂蛋白胆固醇（LDL-C）水平的百分比变化。次要观察指标包括总胆固醇、高密度脂蛋白胆固醇（HDL-C）、甘油三酯水平以及直接测量的极低密度脂蛋白胆固醇（VLDL-C）水平，以及不良事件报告和实验室安全指标，包括电解质水平以及肝肾功能。
与随机分配到安慰剂组（n = 36）的参与者相比，安慰剂组LDL-C水平下降了5%，标准剂量的guggulipid组（n = 33）和高剂量的guggulipid组（n = 34）在8周时LDL-C水平分别升高了4%（与安慰剂组相比P = 0.01）和5%（与安慰剂组相比P = 0.006），净正向变化为9%至10%。在意向性分析中，guggulipid治疗后总胆固醇、HDL-C、甘油三酯或VLDL-C水平无显著变化。虽然guggulipid一般耐受性良好，但与安慰剂组无人出现相比，有6名接受guggulipid治疗的参与者出现了过敏性皮疹。
尽管有合理的作用机制，但在这群高胆固醇血症成年人中，guggulipid在短期内似乎并未改善血清胆固醇水平，实际上可能会提高LDL-C水平。Guggulipid在一些患者中似乎也会引起皮肤过敏反应。
