从澳洲栗种子提取物中分离得到的具有 DPP-IV 抑制活性的生物碱的降血糖作用：实验验证和分子对接研究。
Antihyperglycemic activity with DPP-IV inhibition of alkaloids from seed extract of Castanospermum australe: Investigation by experimental validation and molecular docking.
机构信息
Department of Biochemistry, Patna University, Patna 800005, Bihar, India.
出版信息
Phytomedicine. 2012 Dec 15;20(1):24-31. doi: 10.1016/j.phymed.2012.09.009. Epub 2012 Oct 10.
The antidiabetic actions of Castanospermum australe Cunn., seed (CAS) extract were evaluated in Poloxamer-407 (PX-407) induced T2DM rats. The CAS extract (100 and 150 mg/kg body weight) was administered orally once a day for 5 weeks after the animals were confirmed diabetic. A significant increase in blood glucose, HbA₁c and serum insulin levels were observed in T2DM rats in comparison to citrate control rats. Treatment with CAS extract in T2DM rats reduced the elevated levels of blood glucose, HbA₁c and insulin with significant (p≤0.001) improvement in OGT. The CAS extract treatment also increased (p≤0.001) the K(ITT) and prevented increase in HOMA-R level in T2DM rats. The DPP-IV inhibitory potential of CAS extract showed IC₅₀ value of 13.96 μg/ml whilst the standard Diprotin A displayed the IC₅₀ value of 1.543 μg/ml. Molecular docking of the three reported alkaloids from the seeds of C. australe showed comparable DPP-IV inhibition with berberine. Our data suggest that CAS extract (150 mg/kg body weight) normalizes hyperglycemia in T2DM rats with strong DPP-IV inhibitory potential. The molecular docking showed that among the three alkaloids of seed extract 7-Deoxy-6-epi-castanospermine is a potent DPP-IV inhibitor similar to berberine.
澳洲金粟兰（Castanospermum australe Cunn.）种子提取物的抗糖尿病作用在聚氧乙烯山梨醇酐单月桂酸酯（PX-407）诱导的 T2DM 大鼠中进行了评估。在动物确诊糖尿病后，CAS 提取物（100 和 150 mg/kg 体重）每天口服给药一次，连续 5 周。与柠檬酸盐对照大鼠相比，T2DM 大鼠的血糖、HbA₁c 和血清胰岛素水平显著升高。与 T2DM 大鼠相比，CAS 提取物治疗可降低升高的血糖、HbA₁c 和胰岛素水平，OGT 显著改善（p≤0.001）。CAS 提取物治疗还可增加（p≤0.001）K（ITT），并防止 T2DM 大鼠中 HOMA-R 水平升高。CAS 提取物的 DPP-IV 抑制潜力显示 IC₅₀值为 13.96 μg/ml，而标准二肽基肽酶-IV（DPP-IV）抑制剂 Diprotin A 显示 IC₅₀值为 1.543 μg/ml。从澳洲金粟兰种子中分离的三种生物碱的分子对接显示与小檗碱具有相当的 DPP-IV 抑制作用。我们的数据表明，CAS 提取物（150 mg/kg 体重）可使 T2DM 大鼠的高血糖正常化，具有很强的 DPP-IV 抑制潜力。分子对接显示，种子提取物中的三种生物碱中，7-去氧-6-表金粟兰碱是一种有效的 DPP-IV 抑制剂，与小檗碱相似。
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