Curcumin Pharmacokinetic and Pharmacodynamic Evidences in Streptozotocin-Diabetic Rats Support the Antidiabetic Activity to Be via Metabolite(s).
Curcumin Pharmacokinetic and Pharmacodynamic Evidences in Streptozotocin-Diabetic Rats Support the Antidiabetic Activity to Be via Metabolite(s).
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DOI：
10.1155/2015/678218
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发表时间：
2015
期刊：
影响因子：
--
通讯作者：
Brunetti IL
中科院分区：
文献类型：
--
作者：
Gutierres VO;Campos ML;Arcaro CA;Assis RP;Baldan-Cimatti HM;Peccinini RG;Paula-Gomes S;Kettelhut IC;Baviera AM;Brunetti IL
本研究采用液相色谱法测定大鼠血浆中姜黄素的浓度，并研究富含姜黄素的酸奶对链脲佐菌素糖尿病大鼠糖耐量和胰岛素敏感性的影响。姜黄素检测的分析方法在10至500 ng/mL范围内呈线性。静脉注射姜黄素10 mg/kg后，血浆中姜黄素的Cmax和达峰时间（tmax）分别为3.14 ± 0.9 μg/mL和5 min。和0.06 ± 0.01 μg/mL和14分钟（500 mg/kg，p.o.）。消除半衰期为8.64 ± 2.31（i. v.）和32.70 ± 12.92（p.o.）分钟口服生物利用度为0.47%。本实验观察了正常大鼠和糖尿病大鼠分别饮用酸奶（NYOG和DYOG）后糖耐量和胰岛素敏感性的变化。并用掺入酸奶中的90 mg/kg/天姜黄素处理（分别为NC 90和DC 90）。治疗15 d后，DC 90大鼠的葡萄糖耐量和胰岛素敏感性较对照组显著改善，这可能与骨骼肌AKT磷酸化水平和GLUT 4转位增加有关。这些发现至少可以部分解释富含姜黄素的酸奶对糖尿病的益处，并证实姜黄素代谢物负责抗糖尿病活性的证据。
This study measures the curcumin concentration in rat plasma by liquid chromatography and investigates the changes in the glucose tolerance and insulin sensitivity of streptozotocin-diabetic rats treated with curcumin-enriched yoghurt. The analytical method for curcumin detection was linear from 10 to 500 ng/mL. The C max and the time to reach C max (t max) of curcumin in plasma were 3.14 ± 0.9 μg/mL and 5 minutes (10 mg/kg, i.v.) and 0.06 ± 0.01 μg/mL and 14 minutes (500 mg/kg, p.o.). The elimination half-time was 8.64 ± 2.31 (i.v.) and 32.70 ± 12.92 (p.o.) minutes. The oral bioavailability was about 0.47%. Changes in the glucose tolerance and insulin sensitivity were investigated in four groups: normal and diabetic rats treated with yoghurt (NYOG and DYOG, resp.) and treated with 90 mg/kg/day curcumin incorporated in yoghurt (NC90 and DC90, resp.). After 15 days of treatment, the glucose tolerance and the insulin sensitivity were significantly improved in DC90 rats in comparison with DYOG, which can be associated with an increase in the AKT phosphorylation levels and GLUT4 translocation in skeletal muscles. These findings can explain, at least in part, the benefits of curcumin-enriched yoghurt to diabetes and substantiate evidences for the curcumin metabolite(s) as being responsible for the antidiabetic activity.
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影响因子：
6.1
作者：
Deng, Yea-Tzy;Chang, Tsai-Wen;Lin, Jen-Kun
通讯作者：
Lin, Jen-Kun
影响因子：
3.6
作者：
Gutierres, Vania O.;Pinheiro, Clara M.;Brunetti, Iguatemy L.
通讯作者：
Brunetti, Iguatemy L.
影响因子：
8.9
作者：
Aggarwal BB
通讯作者：
Aggarwal BB
影响因子：
2.5
作者：
Cheng, Tse-Chou;Lin, Chian-Shiung;Cheng, Juei-Tang
通讯作者：
Cheng, Juei-Tang
影响因子：
5.8
作者：
Khalil, Najeh Maissar;Frabel do Nascimento, Thuane Castro;Mainardes, Rubiana Mara
通讯作者：
Mainardes, Rubiana Mara