Dose escalation of a curcuminoid formulation.
Dose escalation of a curcuminoid formulation.
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DOI：
10.1186/1472-6882-6-10
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发表时间：
2006-03-17
影响因子：
--
通讯作者：
Brenner, Dean E
中科院分区：
文献类型：
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作者：
Lao, Christopher D;Ruffin, Mack T 4th;Brenner, Dean E
背景：姜黄素是从姜黄中提取的主要黄色素，姜黄是印度和东南亚常用的香料，具有广泛的抗癌和防癌作用。然而，关于姜黄素在人体内的药理和毒理学的系统研究还很少。方法：采用剂量递增研究，以确定单一剂量的标准化粉末提取物，均匀研磨的姜黄素(C3复合商标，Sabinsa公司)的最大耐受量和安全性。健康志愿者的剂量从500毫克递增到12,000毫克。结果：24名受试者中有7名(30%)只经历了似乎与剂量无关的轻微毒性。500、1,000、2,000、4,000、6,000或8,000毫克受试者的血清中未检测到姜黄素。在两名服用10,000或12,000 mg姜黄素的受试者中检测到低水平的姜黄素。结论：姜黄素在高单次口服剂量下的耐受性良好。鉴于实现姜黄素或其代谢产物的全身生物利用度可能不是结直肠癌化学预防所必需的，这些发现值得进一步研究其作为长期化学预防药物的有效性。
BACKGROUND: Curcumin is the major yellow pigment extracted from turmeric, a commonly-used spice in India and Southeast Asia that has broad anticarcinogenic and cancer chemopreventive potential. However, few systematic studies of curcumin's pharmacology and toxicology in humans have been performed.METHODS: A dose escalation study was conducted to determine the maximum tolerated dose and safety of a single dose of standardized powder extract, uniformly milled curcumin (C3 Complextrade mark, Sabinsa Corporation). Healthy volunteers were administered escalating doses from 500 to 12,000 mg.RESULTS: Seven of twenty-four subjects (30%) experienced only minimal toxicity that did not appear to be dose-related. No curcumin was detected in the serum of subjects administered 500, 1,000, 2,000, 4,000, 6,000 or 8,000 mg. Low levels of curcumin were detected in two subjects administered 10,000 or 12,000 mg.CONCLUSION: The tolerance of curcumin in high single oral doses appears to be excellent. Given that achieving systemic bioavailability of curcumin or its metabolites may not be essential for colorectal cancer chemoprevention, these findings warrant further investigation for its utility as a long-term chemopreventive agent.