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Antioxidant, Anti-Inflammatory and Anticancer Activities of the Methanolic Extract of Thottea siliquosa: An In Vitro and In Silico Study
Recent Patents on Anti-Cancer Drug Discovery ( IF 2.8 ) Pub Date : 2021-07-31 , DOI: 10.2174/1574892816666210401143750
Amrutha Koottasseri 1 , Amal Babu 1 , Anna Augustin 1 , Joice Tom Job 1 , Arunaksharan Narayanankutty 1
Affiliation  

Background: Oxidative stress and inflammation are the predominant cause of chronic diseases, including multiple forms of cancers. Prevention of oxidative stress and inflammation is considered to be a target for preventing these disorders due to their significant roles in various degenerative diseases. Various natural products and plant extracts prevent the process of free radical- induced damages.

Objective: The present study evaluated the biological properties of Thottea siliquosa, belonging to the family Aristolochiaceae, which is a traditionally used Ayurvedic plant.

Methods: Antioxidant assays carried out were DPPH, FRAP, hydrogen peroxide scavenging, and hemolysis inhibition assay; nitric oxide and lipoxygenase inhibition assays were used for anti-inflammatory studies. Anticancer activity was evaluated using human endometrial and breast cancer cells by MTT assay. Bioactive compounds present in T. siliquosa were identified by LCMS and each was docked with various cancer targets, including EGFR, VEGFR, GST, COX2, and Lipooxygenase.

Results: The results of the present study showed antioxidant properties of the methanolic crude extract of T. siliquosa as DPPH radical scavenging (110.40 ± 4.5 μg/mL), FRAP capacity (41.1 ± 6.2), and peroxide scavenging (233.4 ± 14.2 μg/mL). Besides, anti-inflammatory properties were also evident in terms of nitric oxide radical scavenging (28.76± 3.9 μg/mL) and lipoxygenase inhibition (39.2 ± 3.2 μg/mL) assays. In silico analysis confirmed the inhibitory potential of the bioactive compounds of T. siliquosa against cancer drug targets such as EGFR, VEGFR, and inflammatory enzymes cyclooxygenase as well as lipooxygenase. Further, the anticancer activity of the extract has been identified against human endometrial and breast cancer cells. The possible mechanism of anticancer action of the extract is mediated through the apoptosis induction mechanism acting through increased caspase and APAF-1 expressions.

Conclusion: The study thus concludes that T. siliquosa showed significant antioxidant, anti-inflammatory and anticancer properties. Further studies together with a bioassay-guided fractionation may identify possible bioactive compounds.



中文翻译:

Thottea siliquosa 甲醇提取物的抗氧化、抗炎和抗癌活性:体外和计算机研究

背景:氧化应激和炎症是慢性疾病的主要原因,包括多种癌症。预防氧化应激和炎症被认为是预防这些疾病的目标,因为它们在各种退行性疾病中的重要作用。各种天然产品和植物提取物可防止自由基引起的损伤过程。

目的:本研究评估了 Thottea siliquosa 的生物学特性,它属于马兜铃科,是一种传统上使用的阿育吠陀植物。

方法:进行的抗氧化试验为DPPH、FRAP、过氧化氢清除、溶血抑制试验;一氧化氮和脂氧合酶抑制测定用于抗炎研究。通过MTT测定使用人子宫内膜和乳腺癌细胞评估抗癌活性。LCMS 鉴定了 T. siliquosa 中存在的生物活性化合物,每种化合物都与各种癌症靶标对接,包括 EGFR、VEGFR、GST、COX2 和脂氧合酶。

结果:本研究的结果表明,长叶松树甲醇粗提物的抗氧化特性为 DPPH 自由基清除 (110.40 ± 4.5 μg/mL)、FRAP 容量 (41.1 ± 6.2) 和过氧化物清除 (233.4 ± 14.2 μg/毫升)。此外,抗炎特性在一氧化氮自由基清除(28.76±3.9 μg/mL)和脂氧合酶抑制(39.2±3.2 μg/mL)测定方面也很明显。计算机分析证实了 T. siliquosa 的生物活性化合物对癌症药物靶标(如 EGFR、VEGFR 和炎症酶环加氧酶以及脂加氧酶)的抑制潜力。此外,提取物对人类子宫内膜和乳腺癌细胞的抗癌活性已被确定。

结论:该研究因此得出结论,T. siliquosa 显示出显着的抗氧化、抗炎和抗癌特性。进一步的研究与生物测定指导的分级分离可以确定可能的生物活性化合物。

更新日期:2021-07-31
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