Department of Natural Products, National Institute of Pharmaceutical Education and Research (NIPER), S.A.S. Nagar, Punjab 160062, India.
National Agri-Food Biotechnology Institute (NABI), S.A.S. Nagar, Punjab 160071, India.
J Ethnopharmacol. 2017 Feb 2;197:138-146. doi: 10.1016/j.jep.2016.07.070. Epub 2016 Jul 26.
As an effort to identify newer anti-obesity lead(s) we have selected 13 plant materials from the six plant species which have been reported in Indian Ayurvedic medicine as remedy against complications affecting glucose and lipid homeostasis.
In vitro screening of six Indian Ayurvedic medicinal plants on anti-adipogenic and pancreatic lipase (PL) inhibition potential followed by bioactivity guided isolation from most active plant material.
In vitro anti-adipogenic assay using 3T3-L1 preadipocytes and pancreatic lipase (PL) inhibition assay were performed for hexanes, dichloromethane, ethyl acetate and methanolic extracts of all the plant materials. Bioactivity guided isolation approach was used to identify active constituent for anti-adipogenesis and PL inhibition assay. Inhibition of lipid accumulation and adipogenic transcription factor was measured by oil Red 'O' staining and quantitative real-time PCR method respectively.
Ethyl acetate extract of Oroxylum indicum bark was found to be most active in screening of anti-adipogenesis (59.12±1.66% lipid accumulation as compared to control at 50μg/mL dose) and PL inhibition (89.12±6.87% PL inhibition at 250μg/mL dose) assays. Further, three bioactive flavonoids were isolated and identified as oroxylin A, chrysin and baicalein from O. indicum bark. Oroxylin A, chrysin, and baicalein were inhibited lipid accumulation in 3T3-L1 preadipocytes (75.00±5.76%, 70.21±4.23% and 77.21±5.49% lipid accumulation respectively in comparison to control at 50μM dose) and PL enzyme (69.86±2.96%, 52.08±2.14% and 45.06±2.42% PL inhibition respectively at 250μg/mL dose). In addition, oroxylin A and chrysin also inhibited PPARγ and C/EBPα, major adipogenic transcription factors, in 3T3L-1 preadipocytes during adipogenesis process at 50μM dose.
The present study augurs the anti-obesity potential of well practiced Ayurvedic herb O. indicum and its flavonoids.
为了寻找新的抗肥胖先导化合物，我们从印度阿育吠陀医学中报道的六种植物中选择了 13 种植物材料，这些植物被报道可治疗影响葡萄糖和脂质稳态的并发症。
对六种印度阿育吠陀药用植物进行体外筛选，以评估其抗脂肪生成和胰腺脂肪酶（PL）抑制潜力，然后从最有效的植物材料中进行基于生物活性的分离。
使用 3T3-L1 前脂肪细胞进行体外抗脂肪生成测定和胰腺脂肪酶（PL）抑制测定，对所有植物材料的正己烷、二氯甲烷、乙酸乙酯和甲醇提取物进行测定。采用生物活性导向分离法，鉴定抗脂肪生成和 PL 抑制测定的活性成分。通过油红'O'染色和定量实时 PCR 法分别测定脂质积累和脂肪生成转录因子的抑制。
发现 Oroxylum indicum 树皮的乙酸乙酯提取物在筛选抗脂肪生成（与 50μg/mL 剂量的对照相比，脂质积累减少 59.12±1.66%）和 PL 抑制（在 250μg/mL 剂量下 PL 抑制 89.12±6.87%）测定中最有效。此外，从 O. indicum 树皮中分离并鉴定出三种生物活性黄酮类化合物，即黄连甲素、白杨素和黄芩素。黄连甲素、白杨素和黄芩素在 3T3-L1 前脂肪细胞中抑制脂质积累（与 50μM 剂量的对照相比，分别为 75.00±5.76%、70.21±4.23%和 77.21±5.49%）和 PL 酶（与 250μg/mL 剂量的对照相比，分别为 69.86±2.96%、52.08±2.14%和 45.06±2.42%）。此外，黄连甲素和白杨素还在 3T3L-1 前脂肪细胞的脂肪生成过程中抑制 PPARγ 和 C/EBPα，这两种主要的脂肪生成转录因子，在 50μM 剂量下。
本研究预示着实践良好的阿育吠陀草药 O. indicum 及其类黄酮具有抗肥胖的潜力。
