Mathi Pardhasaradhi, Nikhil Kumar, Ambatipudi Nagavamsikrishna, Roy Partha, Bokka Venkata Raman, Botlagunta Mahendran
Biomedical research Laboratory, Department of Biotechnology, K L University, Green fields, Vaddeswaram, Guntur 522 502, AndhraPradesh, India.
Molecular Endocrinology Laboratory, Department of Biotechnology, Indian Institute of Technology Roorkee, Roorkee 247 667, Uttarakhand, India.
Bioinformation. 2014 Mar 19;10(3):144-51. doi: 10.6026/97320630010144. eCollection 2014.
Sophora interrupta belongs to the family of Fabaceae and the species in this genus have a diverse medicinal importance as a folk medicine for preventing many ailments including cancer. In order to evaluate the anticancer activity of S.interrupta, we have performed in vitro anti-oxidant, anti-inflammatory, anti-proliferative, and cell based anticancer activity in MCF-7 and PC-3 cell lines. Secondary metabolites of S.interrupta were used to identify anticancer compounds using Open Eye software. The antioxidant activity of the S.interrupta root ethylacetate (SEA) extract at 100 µg/ml is equal to that of ascorbic acid at 50 µg/ml. The antiinflammatory activity of SEA is half of that of diclofenac at 50 µg/ml. Anticancer activity was detected by measuring the mitochondrial dehydrogenase activity (MTT assay). The half maximal inhibitory concentrations (IC50) for MCF-7 and PC-3 cell lines are 250 and 700 µg/ml respectively. This was supported by the morphological changes such as membrane blebbing, cell detachment and rounded cell morphology when compared to the parental cells. In addition, we observed few green cells (live) over red cells (dead) based on the uptake of acridine orange and ethidium bromide dyes. Kaempferol-3-O-b-D-glucopyranoside, a Secondary metabolite of S.interrupta form 6 hydrogen bond interactions with Arg 202, Gln 207, Gly 227, Gly 229, Thr 231 and Ala 232 human DEAD box RNA helicase, DDX3 protein and is equivalent to crystal structure of adenosine mono phosphate to DDX3. Overall, it suggests that the SEA extract has anticancer compounds, and it can be used to enhance death receptor mediated cancer cell death.
苦豆子属于豆科，该属植物作为预防包括癌症在内的多种疾病的民间药物，具有多种药用价值。为了评估苦豆子的抗癌活性，我们在MCF-7和PC-3细胞系中进行了体外抗氧化、抗炎、抗增殖和基于细胞的抗癌活性实验。使用Open Eye软件，利用苦豆子的次生代谢产物来鉴定抗癌化合物。苦豆子根乙酸乙酯（SEA）提取物在100μg/ml时的抗氧化活性与50μg/ml的抗坏血酸相当。SEA的抗炎活性是50μg/ml双氯芬酸的一半。通过测量线粒体脱氢酶活性（MTT法）检测抗癌活性。MCF-7和PC-3细胞系的半数最大抑制浓度（IC50）分别为250和700μg/ml。与亲代细胞相比，膜泡形成、细胞脱离和细胞形态变圆等形态学变化支持了这一结果。此外，基于吖啶橙和溴化乙锭染料的摄取，我们观察到活细胞（绿色）比死细胞（红色）少。苦豆子的次生代谢产物山柰酚-3-O-β-D-吡喃葡萄糖苷与人类DEAD盒RNA解旋酶DDX3蛋白的Arg 202、Gln 207、Gly 227、Gly 229、Thr 231和Ala 232形成6个氢键相互作用，与腺苷单磷酸与DDX3的晶体结构相当。总体而言，这表明SEA提取物含有抗癌化合物，可用于增强死亡受体介导的癌细胞死亡。
