长春花生物碱的抗糖尿病和抗氧化特性。

Antidiabetic and antioxidant properties of alkaloids from Catharanthus roseus (L.) G. Don.

机构信息

Department of Chemistry, Faculty of Science, University of Malaya, Kuala Lumpur 50603, Malaysia.

出版信息

Molecules. 2013 Aug 15;18(8):9770-84. doi: 10.3390/molecules18089770.

Catharanthus roseus (L.) G. Don is a herbal plant traditionally used by local populations in India, South Africa, China and Malaysia to treat diabetes. The present study reports the in vitro antioxidant and antidiabetic activities of the major alkaloids isolated from Catharanthus roseus (L.) G. Don leaves extract. Four alkaloids--vindoline I, vindolidine II, vindolicine III and vindolinine IV--were isolated and identified from the dichloromethane extract (DE) of this plant's leaves. DE and compounds I-III were not cytotoxic towards pancreatic β-TC6 cells at the highest dosage tested (25.0 µg/mL). All four alkaloids induced relatively high glucose uptake in pancreatic β-TC6 or myoblast C2C12 cells, with III showing the highest activity. In addition, compounds II-IV demonstrated good protein tyrosine phosphatase-1B (PTP-1B) inhibition activity, implying their therapeutic potential against type 2 diabetes. III showed the highest antioxidant potential in ORAC and DPPH assays and it also alleviated H₂O₂-induced oxidative damage in β-TC6 cells at 12.5 µg/mL and 25.0 µg/mL.

长春花（Catharanthus roseus (L.) G. Don）是一种草药植物，传统上被印度、南非、中国和马来西亚的当地居民用于治疗糖尿病。本研究报告了从长春花（Catharanthus roseus (L.) G. Don）叶片提取物中分离得到的主要生物碱的体外抗氧化和抗糖尿病活性。从该植物叶片的二氯甲烷提取物（DE）中分离并鉴定出四种生物碱 - 长春碱 I、长春质碱 II、长春新碱 III 和长春文碱 IV。DE 和化合物 I-III 在最高测试剂量（25.0 µg/mL）下对胰腺 β-TC6 细胞均无细胞毒性。这四种生物碱均能在胰腺β-TC6 或成肌细胞 C2C12 细胞中诱导较高的葡萄糖摄取，其中 III 的活性最高。此外，化合物 II-IV 对蛋白酪氨酸磷酸酶-1B（PTP-1B）表现出良好的抑制活性，暗示它们具有治疗 2 型糖尿病的潜力。III 在 ORAC 和 DPPH 测定中表现出最高的抗氧化潜力，并且在 12.5 µg/mL 和 25.0 µg/mL 时还能减轻 H₂O₂诱导的β-TC6 细胞氧化损伤。