目的 研究糖復(fù)康寧提取物對鈉離子-葡萄糖協(xié)同轉(zhuǎn)運(yùn)體2（SGLT2）的抑制作用及對二型糖尿病大鼠的降糖作用。方法 通過由轉(zhuǎn)染試劑Lipo 3 000介導(dǎo)的轉(zhuǎn)基因方法構(gòu)建SGLT2過表達(dá)的HEK293細(xì)胞株，考察0.01、0.03、0.1、0.3、1.0、3.0 mg/mL糖復(fù)康寧提取物對SGLT2介導(dǎo)的α-甲基吡喃葡萄糖苷（¹⁴C-AMG）攝入的抑制作用；應(yīng)用高糖高脂飼料和鏈脲佐菌素制備二型糖尿病動(dòng)物模型，ig低、高劑量（162、324 mg/kg）糖復(fù)康寧提取物，每天給藥1次，連續(xù)給藥5周，每周測定空腹血糖值，給藥結(jié)束后測定糖耐量。結(jié)果 與對照組比較，0.1、0.3、1.0、3.0 mg/mL的糖復(fù)康寧提取物對SGLT2介導(dǎo)的¹⁴C-AMG攝入均有顯著抑制作用（P<0.05），IC₅₀為0.119 mg/mL；與模型組比較，ig 162、324 mg/kg糖復(fù)康寧提取物35 d后，二型糖尿病大鼠的空腹血糖顯著降低（P<0.05、0.01），糖耐量也明顯改善（P<0.05）。結(jié)論 糖復(fù)康寧提取物對二型糖尿病大鼠發(fā)揮顯著降糖作用，其機(jī)制可能與抑制SGLT2對葡萄糖的重吸收相關(guān)。

Objective To research the inhibition of Tangfu Kangning extracts to SGLT2 and the antidiabetic effects to mice with type Ⅱ diabetic. Method The SGLT2 overexpressed cell line (HEK293-SGLT2) was transfected through Lipo3000. The inhibitory effects of 0.01, 0.03, 0.1, 0.3, 1, and 3 mg/mL of Tangfu Kangning extracts on SGLT2 mediated ¹⁴C-AMG intake were investigated. The animal model of type two diabetes was prepared with high glucose and high fat diet and streptozotocin, ig low and high dose (162, 324 mg/kg) Tangfu Kangning extract to mice, once daily, continuous for five weeks, the fasting blood glucose was measured weekly, and the glucose tolerance was measured after the end of the administration. Result Compared with control group, the TangFuKangNing extract of 0.1, 0.3, 1.0, and 3.0 mg/mL had significant inhibitory effects on SGLT2 mediated ¹⁴C-AMG intake (P<0.05) and IC₅₀ was 0.119 mg/mL. The fasting blood glucose (FBG) of type Ⅱ diabetes mice treated with the two dosages (162 and 324 mg/kg)of Tangfu Kangning extracts for 35 d were significantly lower than model group (P<0.05 and 0.01). The glucose tolerances of mice treated with Tangfu Kangning extract were also improved (P<0.05). Conclusion Tangfu Kangning extracts have significant hypoglycemic effect on type two diabetes rats, and its mechanism may be related to inhibiting the reabsorption of glucose by SGLT2.

國家自然科學(xué)基金重點(diǎn)項(xiàng)目（81430096）；天津市科技支撐重點(diǎn)項(xiàng)目（17YFZCSY01170）；國家青年自然科學(xué)基金（81503154）