基于 HPTLC-DPPH 生物指纹图谱从 Abrus precatorius L. 中分离和鉴定未被描述的黄酮类化合物及其细胞毒性评价

IF 3.4 Q2 PHARMACOLOGY & PHARMACY
Hafsa I. Ansari, Ranjitsinh C. Dabhi, Pooja G. Trivedi, Milan S. Thakar, Jayesh J. Maru, Gaurang M. Sindhav
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引用次数: 0

摘要

天然衍生化合物作为药物和原料药开发的先导结构发挥着巨大作用。因此,需要从自然界中分离和鉴定化合物,以缓解威胁生命的疾病。A. precatorius L. 属于豆科植物,其药用价值很高。因此,本研究采用 HPTLC-DPPH 生物层析技术,努力从 APHA 提取物中分离出具有生物活性的实体。在 TLC 板上分离出的所有化合物中,Rf = 0.67 的化合物(APSP-3)显示出了显著的抗氧化活性,因此,APSP-3 被进一步分离、纯化,并使用 1D 和 2D NMR、FTIR、HPLC-MS/MS 和元素分析等多种分析方法进行结构表征。此外,还分别采用标准的 DPPH 和比色法 MTT 评估了 APHA 提取物和 APSP-3 的抗氧化性和细胞毒性。根据 HPTLC-DPPH 生物层析技术,对分离出的化合物 APSP-3 进行了抗氧化性研究。发现 APSP-3 具有新颖性,光谱数据显示了其合理的结构;7-羟基-3,5-二甲氧基-2-(4-((3,4,5-三羟基-6-(羟甲基)四氢-2H-吡喃-2-基)氧基)苯基)-4H-色烯-4-酮。此外,与标准抗坏血酸(75.19 ± 1.5 µg/mL)相比,APSP-3 的自由基清除活性更高,IC50 = 38.70 ± 3.5 µg/mL。细胞毒性评估显示,APHA 提取物对 HepG2、MCF-7 和 HCT116 细胞株的 IC50 值分别为 122.09 µg/mL、122.61 µg/mL和 48.08 µg/mL,而 APSP-3 对 HepG2、MCF-7 和 HCT116 细胞株的 IC50 值分别为 96.75、61.67 和 47.61 µg/mL。总之,HPTLC 引导的生物层析技术从 APHA 提取物中捕获了具有抗氧化功效的新黄酮实体。从细胞毒性中获得的 IC50 值建立了一种剂量-反应关系,有助于确定某种物质开始产生毒性效应的浓度。这一基本信息对于确定医疗和制药应用中的安全剂量水平至关重要。此外,在评估其他生物活性方面的研究涉及硅学和体内研究,必须为临床影响提供有前景的可靠描述。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Isolation and characterization of undescribed flavonoid from Abrus precatorius L. based on HPTLC-DPPH bioautography and its cytotoxicity evaluation

Background

Naturally derived compounds play a tremendous role as a drug as well as lead structure for the development of APIs. Therefore, isolation and characterization of compounds from nature are needed to alleviate life-threatening diseases. A. precatorius L. belongs to the family Leguminosae and is valued for its medicinal properties. Therefore, in this study, efforts are being made to isolate bioactive entity based on HPTLC-DPPH bioautography from APHA extract. Among all the separated compounds on TLC plate, the one (APSP-3) at Rf = 0.67 showed significant antioxidant activity, and hence, APSP-3 was further subjected to isolation, purification, and structural characterization using diverse analytical modus operandi such as 1D and 2D NMR, FTIR, HPLC–MS/MS, and elemental analysis. In addition, antioxidant and cytotoxicity evaluation of APHA extract and APSP-3 was pursued by standard DPPH and colorimetric MTT assays, respectively.

Results

Antioxidative isolated compound APSP-3 was scrutinized based on HPTLC-DPPH bioautography. The APSP-3 was found novel and spectroscopic data revealed the plausible structure; 7-hydroxy-3,5-dimethoxy-2-(4-((3,4,5-trihydroxy-6-(hydroxymethyl) tetrahydro-2H-pyran-2-yl)oxy) phenyl)-4H-chromen-4-one. Moreover, APSP-3 ascribed higher free radical scavenging activity with IC50 = 38.70 ± 3.5 µg/mL than standard ascorbic acid (75.19 ± 1.5 µg/mL). Cytotoxicity evaluation of APHA extract exhibited IC50 value 122.09 µg/mL for HepG2, 122.61 µg/mL for MCF-7, and 48.08 µg/mL for HCT116 cell lines, while APSP-3 displayed IC50 values 96.75 for HepG2, 61.67 for MCF-7, and 47.61 µg/mL for HCT116 cell lines.

Conclusions

In a nutshell, HPTLC-directed bioautography leads to the capturing of new flavonoid entity having antioxidant potency from APHA extract. The IC50 values obtained from cytotoxicity establish a dose–response relationship helping to determine the concentration at which a substance begins to exhibit toxic effects. This fundamental information is crucial for establishing safe dosage level in medical and pharmaceutical applications. Further, research engrossed in assessing other bioactivities involving in silico and in vivo studies obliged to offer a promising and secure portrayal for clinical implications.

Graphical abstract

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来源期刊
自引率
0.00%
发文量
44
审稿时长
23 weeks
期刊介绍: Future Journal of Pharmaceutical Sciences (FJPS) is the official journal of the Future University in Egypt. It is a peer-reviewed, open access journal which publishes original research articles, review articles and case studies on all aspects of pharmaceutical sciences and technologies, pharmacy practice and related clinical aspects, and pharmacy education. The journal publishes articles covering developments in drug absorption and metabolism, pharmacokinetics and dynamics, drug delivery systems, drug targeting and nano-technology. It also covers development of new systems, methods and techniques in pharmacy education and practice. The scope of the journal also extends to cover advancements in toxicology, cell and molecular biology, biomedical research, clinical and pharmaceutical microbiology, pharmaceutical biotechnology, medicinal chemistry, phytochemistry and nutraceuticals.
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