Karanjin,一种具有抗非小细胞肺癌癌症细胞实验模型抗癌活性的有前景的生物活性化合物。

IF 2.6 4区 医学 Q3 CHEMISTRY, MEDICINAL Anti-cancer agents in medicinal chemistry Pub Date : 2024-01-01 DOI:10.2174/0118715206255557231024095245
Gourav Kumar, Dev Mani Pandey, Manik Ghosh, Stefano Dall'Acqua, Rashmi Gupta, Nishi Prakash Tiwari, Usman Mohd Siddique, Leena Vishwakrama, Sunil Kant Guleri, Uma Ranjan Lal, Supriya Dubey
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引用次数: 0

摘要

目的:本研究的目的是分离具有抗癌性质的叶提取物,并研究分离物在非小细胞肺癌癌症细胞系中的分子靶点。背景:在我们早期的研究中,裙带菜叶提取物已显示出潜在的抗癌活性。因此,在寻找生物活性化合物的过程中,我们从先前的研究中纯化了最有潜力的活性提取物。此外,还对分离的化合物卡兰津的抗癌特性进行了研究,旨在促进细胞凋亡和抑制生长。方法:采用柱色谱法从叶氯仿提取物中分离纯化复方卡兰津。然后使用FTIR、质谱和NMR对纯化的组分进行表征。基于MTT的细胞毒性测定用于分析细胞毒性,而荧光染色用于细胞凋亡和活性氧抑制定量。此外,实时PCR测定用于确定卡兰津给药诱导的细胞毒性的分子作用机制。结果:卡兰津对A549细胞的抗癌活性显著,IC50值为4.85μM。根据预测的分子通路研究,卡兰津通过凋亡抑制癌症细胞的增殖,凋亡受外源性通路蛋白FAS/FADD/Caspase 8/3/9的控制。KRAS和依赖性基因表达的下调也阻止了细胞增殖。结论:卡兰津是一种对非小细胞肺癌癌症细胞有潜在作用的化合物。观察了H2O2诱导细胞凋亡和抑制活性氧的分子机制,认为卡兰津具有药用和抗氧化特性。
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Karanjin, A Promising Bioactive Compound Possessing Anti-cancer Activity against Experimental Model of Non-small Cell Lung Cancer Cells.

Aims: The aim of this study is to isolate the Millettia pinnata (Karanj) leaf extract for pure compound with anticancer properties and to study the molecular target of the isolates in non-small cell lung cancer cell lines.

Background: In our earlier research Millettia pinnata leaf extract has demonstrated potential anticancer activities. Thus, in pursuit of the bioactive compounds, the most potential active extract from our previous study was purified. Furthermore, the anticancer properties of the isolated compound karanjin was studied and aimed for apoptosis and restraining growth.

Methods: A novel method was developed through column chromatography for isolation and purification of the compound karanjin from leaf chloroform extract. The purified component was then characterised using FTIR, mass spectrometry, and NMR. An MTT-based cytotoxicity assay was used to analyse cell cytotoxicity, whereas fluorescence staining was used for apoptosis and reactive oxygen species inhibition quantification. Furthermore, the real-time PCR assay was used to determine the molecular mechanism of action in cells causing cytotoxicity induced by karanjin dosing.

Results: The anticancer activity of karanjin in A549 cell line exhibited prominent activity revealing IC50 value of 4.85 μM. Conferring the predicted molecular pathway study, karanjin restrains the proliferation of cancer cells through apoptosis, which is controlled by extrinsic pathway proteins FAS/FADD/Caspases 8/3/9. Downregulation of KRAS and dependent gene expression also stopped cell proliferation.

Conclusion: Karanjin has been identified as a compound with potential effect in non-small cell lung cancer cells. Molecular mechanism for apoptosis and inhibition of reactive oxygen species induced through H2O2 were observed, concluding karanjin have medicinal and antioxidant properties.

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来源期刊
Anti-cancer agents in medicinal chemistry
Anti-cancer agents in medicinal chemistry ONCOLOGY-CHEMISTRY, MEDICINAL
CiteScore
5.10
自引率
3.60%
发文量
323
审稿时长
4-8 weeks
期刊介绍: Formerly: Current Medicinal Chemistry - Anti-Cancer Agents. Anti-Cancer Agents in Medicinal Chemistry aims to cover all the latest and outstanding developments in medicinal chemistry and rational drug design for the discovery of anti-cancer agents. Each issue contains a series of timely in-depth reviews and guest edited issues written by leaders in the field covering a range of current topics in cancer medicinal chemistry. The journal only considers high quality research papers for publication. Anti-Cancer Agents in Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments in cancer drug discovery.
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