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In vitro antioxidant, anti-inflammatory, and anticancer activities of methanolic extract and its metabolites of whole plant Cardiospermum canescens Wall
Future Journal of Pharmaceutical Sciences ( IF 3.4 ) Pub Date : 2020-05-11 , DOI: 10.1186/s43094-020-00028-y
Alekhya Ketha , Girija Sastry Vedula , A. V. S. Sastry

Traditionally, the whole plant of Cardiospermum canescens has wide applications in the management of oxidative stress and inflammation in Africa and Asia. The present study investigated the antioxidant, anti-inflammatory, xanthine oxidase (XO) inhibitory, and anticancer activities of metabolites present in the crude methanolic extract of whole plant C. canescens (CCE). Chemical examination of CCE revealed the presence of six known compounds (1–6). From the results of in vitro studies, it can confirm that CCE exhibited notably inhibition of DPPH and superoxide free radicals, along with COX-1, COX-2, 5-LOX, and XO enzymes. Compounds 2 and 3 showed significant inhibition of DPPH and superoxide free radicals. Also, compound 2 exhibited good inhibition of COX-1 and COX-2 enzyme with IC50 of 87.0 and 88.0 μg/mL. Furthermore, CCE exhibited significant inhibition of 5-LOX and XO enzymes with IC50 of 42.5 and 56.0 μg/mL, respectively, while standard with IC50 of 42.5 and 56.0 μg/mL, respectively. Among the test series of cancer cell lines, compounds 2, 3, and CCE showed a significant percentage of cell growth lysis of DLD-1 with IC50 values of 52.5, 72.5, and 32.5 μg/mL, respectively. Besides, all the metabolites and CCE showed a very weak degree of specificity against NHME, indicates less toxicity to normal cells. To conclude, the results of the present study indicated that the methanolic extract from the whole plant of C. canescens displayed antioxidant activity by inhibiting DPPH and superoxide free radicals; anti-inflammatory effects by regulating enzymes COX-1, COX-2, 5-LOX, and XO; and anticancer activity by inhibiting the growth of MCF-7, DLD-1, HeLa, and A549. These activities can link to natural active compounds 2 and 3. This study supports the traditional uses of the root of C. canescens. These data findings suggest that C. canescens can be a promising natural source of biological medicines for oxidative stress, inflammation, gout, and cancer.

中文翻译:

在体外抗氧化,抗炎,和甲醇提取物的抗癌活性和它的整株植物的代谢物倒地铃属藜

传统上,整个欧洲菜豆(Cardiospermum canescens)在非洲和亚洲的氧化应激和炎症管理中具有广泛的应用。本研究调查了整株C. canescens(CCE)粗甲醇提取物中存在的代谢物的抗氧化剂,抗炎剂,黄嘌呤氧化酶(XO)抑制性和抗癌活性。CCE的化学检查显示存在六种已知化合物(1-6)。从体外研究的结果可以证实,CCE与COX-1,COX-2、5-LOX和XO酶一起对DPPH和超氧化物自由基具有明显的抑制作用。化合物2和3显示出对DPPH和超氧化物自由基的显着抑制。此外,化合物2表现出对COX-1和COX-2酶的良好抑制,IC50为87.0和88.0μg/ mL。此外,CCE对5-LOX和XO酶显示出显着抑制作用,IC50分别为42.5和56.0μg/ mL,而标准品的IC50分别为42.5和56.0μg/ mL。在一系列癌细胞系的测试中,化合物2、3和CCE表现出显着百分比的DLD-1细胞生长裂解,IC50值分别为52.5、72.5和32.5μg/ mL。此外,所有的代谢产物和CCE对NHME的特异性都非常弱,对正常细胞的毒性较小。综上所述,本研究结果表明,整个C. canescens植物的甲醇提取物通过抑制DPPH和超氧自由基表现出抗氧化活性。通过调节酶COX-1,COX-2、5-LOX和XO的抗炎作用;通过抑制MCF-7,DLD-1,HeLa和A549的生长来发挥抗癌活性。这些活性可以与天然活性化合物2和3关联。这项研究支持了C. canescens根的传统用途。这些数据发现表明,C。canescens可能是有希望的天然药物,可用于氧化应激,炎症,痛风和癌症。
更新日期:2020-05-11
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