双（α-呋喃羧酸根）氧钒（IV）在脂肪细胞中的抗脂解作用
The antilipolytic action of bis(alpha-furancarboxylato)oxovanadium(IV) in adipocytes.
作者信息
Gao Lihui, Niu Yanfen, Liu Weiping, Xie Mingjin, Liu Xu, Chen Zhihe, Li Ling
机构信息
Yunnan Pharmacological Laboratories of Natural Products, Kunming Medical College, Kunming, PR China.
出版信息
Clin Chim Acta. 2008 Feb;388(1-2):89-94. doi: 10.1016/j.cca.2007.10.014. Epub 2007 Oct 18.
BACKGROUND
Previously, bis(alpha-furancarboxylato)oxovanadium(IV)(BFOV) exhibited potent hypoglycemic activity in diabetic animals. We evaluated the effects of BFOV on lipolysis in isolated rat adipocytes and lipid metabolism in fat-fed/streptozotocin (STZ)-induced diabetic rats, an animal model of type 2 diabetes.
METHODS
Antilipolytic action of BFOV was investigated by observing free fatty acids (FFA) release in isolated rat adipocytes treated with epinephrine and forskolin. Diabetic rats were induced by high-fat feeding plus STZ injection (25 mg/kg, i.p.). The rats were randomly divided into non-diabetic, diabetic, diabetic-BFOV (0.02, 0.06 and 0.2 mmol/kg) and diabetic-vanadyl sulfate group. All substances were given intragastrically to rats for 4 weeks. The concentrations of blood glucose, serum lipid and leptin, as well as body weight and food intake were determined.
RESULTS
FFA release from adipocytes treated with epinephrine was markedly inhibited by BFOV and vanadyl sulfate, with the IC(50) values of 0.30+/-0.20 and 0.46+/-0.26 mmol/l, respectively, but not by insulin. Whereas, the inhibition of vanadyl compounds on FFA release triggered by forskolin in adipocytes were not observed. BFOV dose-dependently reduced serum triglycerides and FFA concentrations when compared with untreated diabetic rats (P<0.05), while it did not influence cholesterol concentrations, similar to vanadyl sulfate. Serum leptin concentration was also decreased both in the BFOV- and vanadyl sulfate-treated diabetic group (P<0.05). Moreover, BFOV markedly reduced blood glucose concentration and food intake (P<0.05), but it did not change the body weight of diabetic rats.
CONCLUSION
BFOV has an antilipolytic action in adipocytes mediated by catecholamines. This action was distinct from that of insulin and also not related to inhibiting the activity of adenylate cyclase. In vivo, BFOV could improve dyslipidemia and leptin sensitivity in fat-fed/STZ-diabetic rats.
背景
此前，双（α-呋喃甲酸根）氧钒（IV）（BFOV）在糖尿病动物中表现出强大的降血糖活性。我们评估了BFOV对分离的大鼠脂肪细胞中脂解作用以及对高脂喂养/链脲佐菌素（STZ）诱导的糖尿病大鼠（一种2型糖尿病动物模型）脂质代谢的影响。
方法
通过观察用肾上腺素和福斯高林处理的分离大鼠脂肪细胞中游离脂肪酸（FFA）的释放来研究BFOV的抗脂解作用。通过高脂喂养加STZ注射（25mg/kg，腹腔注射）诱导糖尿病大鼠。将大鼠随机分为非糖尿病组、糖尿病组、糖尿病 - BFOV组（0.02、0.06和0.2mmol/kg）和糖尿病 - 硫酸氧钒组。所有物质均经胃内给予大鼠4周。测定血糖、血脂和瘦素浓度以及体重和食物摄入量。
结果
BFOV和硫酸氧钒显著抑制肾上腺素处理的脂肪细胞中FFA的释放，IC（50）值分别为0.30±0.20和0.46±0.26mmol/l，但胰岛素无此作用。然而，未观察到钒化合物对福斯高林引发的脂肪细胞中FFA释放的抑制作用。与未治疗的糖尿病大鼠相比，BFOV剂量依赖性地降低血清甘油三酯和FFA浓度（P<0.05），而它对胆固醇浓度无影响，与硫酸氧钒相似。BFOV和硫酸氧钒处理的糖尿病组血清瘦素浓度也降低（P<0.05）。此外，BFOV显著降低血糖浓度和食物摄入量（P<0.05），但它并未改变糖尿病大鼠的体重。
结论
BFOV在儿茶酚胺介导的脂肪细胞中具有抗脂解作用。该作用与胰岛素不同，也与抑制腺苷酸环化酶的活性无关。在体内，BFOV可改善高脂喂养/STZ诱导的糖尿病大鼠的血脂异常和瘦素敏感性。
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