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一种新型天然(-)-羟基柠檬酸提取物(HCA-SX)用于体重管理的安全性和有效性概述。

An overview of the safety and efficacy of a novel, natural(-)-hydroxycitric acid extract (HCA-SX) for weight management.

作者信息

Preuss H G, Rao C V S, Garis R, Bramble J D, Ohia S E, Bagchi M, Bagchi D

机构信息

Department of Physiology, Medicine and Pathology Georgetown University Medical Center, Washington, DC 20057, USA.

出版信息

J Med. 2004;35(1-6):33-48.

Abstract

Garcinia cambogia-derived (-)-hydroxycitric acid (HCA) is a safe, natural supplement for weight management. HCA is a competitive inhibitor of ATP citrate lyase, a key enzyme which facilitates the synthesis of fatty acids, cholesterol and triglycerides. Previous studies in our laboratories have demonstrated the superior bioavailability of a novel calcium-potassium salt of HCA derived from Garcinia cambogia (HCA-SX, Super CitriMax). Greater bioavailability of HCA-SX was observed when taken on an empty stomach. HCA-SX was also shown to exhibit concentration-dependent release of serotonin in isolated rat brain cortex, which may explain its appetite suppressive action. Acute oral, acute dermal, primary dermal irritation, primary eye irritation and 90-day chronic toxicity studies, as well as Ames bacterial reverse mutation and mouse lymphoma tests, were assessed to determine the safety of HCA-SX. In the 90-day toxicity study, dose- and time-dependent effects of HCA-SX were assessed on body weight, selected organ weights, hepatic and testicular lipid peroxidation and DNA fragmentation, hematology and clinical chemistry, and histopathology in male and female Sprague-Dawley rats. No remarkable toxicity results were detected, demonstrating the safety of HCA-SX. Furthermore, clinical studies to evaluate the safety and efficacy of HCA-SX over a period of eight weeks were conducted in 60 human volunteers. Subjects were given a 2,000 kcal diet/day, participated in a 30 min walking exercise program 5 days/week and given an oral dose of placebo or 4666.7 mg HCA-SX (providing 2,800 mg HCA) in three equally divided doses 30-60 min before meals, Body weight, BMI, lipid profiles, serum leptin, serotonin and excretion of urinary fat metabolites were determined at 0, 4 and 8 weeks of treatment. At the end of 8 weeks, body weight and BMI decreased by 5.4% and 5.2%, respectively. Food intake, total cholesterol, LDL, triglycerides and serum leptin levels were significantly reduced, while HDL and serotonin levels, and excretion of urinary fat metabolites (a biomarker of fat oxidation) significantly increased. No significant adverse effects were reported. These results demonstrate the safety, bioavailability and efficacy of HCA-SX in weight management.

摘要

藤黄果提取物(-)-羟基柠檬酸(HCA)是一种用于体重管理的安全天然补充剂。HCA是ATP柠檬酸裂解酶的竞争性抑制剂,ATP柠檬酸裂解酶是促进脂肪酸、胆固醇和甘油三酯合成的关键酶。我们实验室之前的研究表明,一种源自藤黄果的新型HCA钙钾盐(HCA-SX,超级藤黄果提取物)具有卓越的生物利用度。空腹服用时,HCA-SX的生物利用度更高。HCA-SX还被证明能在离体大鼠脑皮层中呈现浓度依赖性的血清素释放,这可能解释了其食欲抑制作用。我们进行了急性口服、急性皮肤、原发性皮肤刺激、原发性眼刺激和90天慢性毒性研究,以及艾姆斯细菌回复突变试验和小鼠淋巴瘤试验,以确定HCA-SX的安全性。在90天毒性研究中,评估了HCA-SX对雄性和雌性斯普拉格-道利大鼠的体重、选定器官重量、肝脏和睾丸脂质过氧化及DNA片段化、血液学和临床化学指标以及组织病理学的剂量和时间依赖性影响。未检测到显著的毒性结果,证明了HCA-SX的安全性。此外,在60名人类志愿者中进行了为期八周的临床研究,以评估HCA-SX的安全性和有效性。受试者每天摄入2000千卡的饮食,每周5天参加30分钟的步行锻炼计划,并在饭前30 - 60分钟口服一剂安慰剂或4666.7毫克HCA-SX(提供2800毫克HCA),分三次等量服用。在治疗的第0、4和8周测定体重、体重指数、血脂谱、血清瘦素、血清素和尿脂肪代谢产物的排泄情况。在8周结束时,体重和体重指数分别下降了5.4%和5.2%。食物摄入量、总胆固醇、低密度脂蛋白、甘油三酯和血清瘦素水平显著降低,而高密度脂蛋白和血清素水平以及尿脂肪代谢产物(脂肪氧化的生物标志物)的排泄显著增加。未报告明显的不良反应。这些结果证明了HCA-SX在体重管理方面的安全性、生物利用度和有效性。

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