scholarly journals TLC-Bioautographic Evaluation for High-Throughput Screening and Identification of Free Radical Scavenging and Antidiabetic Compounds from Traditional Unani Medicinal Plant: Citrullus colocynthis Schrad

2020 ◽  
Vol 103 (3) ◽  
pp. 669-677 ◽  
Author(s):  
Rabea Parveen ◽  
Nausheen Khan ◽  
Sultan Zahiruddin ◽  
Mohammad Ibrahim ◽  
Varisha Anjum ◽  
...  
Keyword(s):  
Free Radical ◽  
Medicinal Plant ◽  
Ethyl Acetate ◽  
Bioactive Compounds ◽  
High Throughput ◽  
High Throughput Screening ◽  
Antidiabetic Activity ◽  
Antioxidant Compounds ◽  
Citrullus Colocynthis ◽  
Tlc Bioautography

Abstract Background: Interest in the antioxidant and antidiabetic activity of natural products are growing vastly in the modern world. Thin layer chromatography-bioautography-mass spectroscopy (TLC-bioautography-MS) plays an important role in chemico-biological screening of natural sources. TLC combined with 2, 2-Diphenyl-1-picrylhydrazyl (DPPH) free radical, α-amylase and α-glucosidase bioassay were used to evaluate antioxidant and antidiabetic activities, respectively, in different extracts of Citrullus colocynthis (Hanzal), a well-known traditional Indian Unani medicinal plant. Objective: To develop a TLC-bioautographic-MS method for DPPH, α-amylase, and glucosidase inhibitors in different extract of C. colocynthis fruits. Method: Fruits of C. colocynthis were successively extracted with toluene, dichloromethane, ethyl acetate, methanol, and water. TLC solvents were developed, and bioautographic-MS analysis was carried out to identify the antioxidant and antidiabetic compounds. Results: HPTLC fingerprinting analysis showed maximum numbers of band separated in dichloromethane and ethyl acetate extracts of C. colocynthis, fourteen and thirteen at 254 and 366 nm, respectively. Whereas six and five separated bands were observed in toluene extract at 254 and 366 nm, respectively showed minimum numbers of metabolites. Based on TLC-bioautography-MS, maximum number of antioxidant compounds were identified in dichloromethane extract. Except aqueous extract of C. colocynthis, all the extracts have shown antidiabetic activity. On the other hand, there were no antioxidant compounds in methanolic extract of C. colocynthis. Conclusions: The results of this study reveal that TLC-bioautography-MS–guided strategy used to identify antioxidant and antidiabetic compounds of C. colocynthis is very useful technique for high-throughput screening of bioactive compounds. Highlights: TLC-MS bioautography is a simple and fast to enables bioactive compounds present in extracts.

scholarly journals Sustainable Biosynthesis of Antioxidants from Koji Rice Fermented with Aspergillus flavus Using Microwave-Assisted Extraction

2021 ◽  
Vol 11 (1) ◽  
pp. 430
Author(s):  
Hassan Hadi Mehdi Al Rubaiy ◽  
Ammar Altemimi ◽  
Ali Khudair Jaber Al Rikabi ◽  
Naoufal Lakhssassi ◽  
Anubhav Pratap-Singh
Keyword(s):  
Ethyl Acetate ◽  
Aspergillus Flavus ◽  
Bioactive Compounds ◽  
Ethylenediaminetetraacetic Acid ◽  
Ethyl Acetate Extract ◽  
Antioxidant Properties ◽  
Antioxidant Compounds ◽  
Microwave Assisted Extraction ◽  
Microwave Assisted ◽  
Assisted Extraction

The present study proposes microwave-assisted extraction as a sustainable technique for the biosynthesis of bioactive compounds from rice fermented with Aspergillus flavus (koji). First, fermentation conditions (i.e., pH from 3–12, five temperatures from 20–40 °C, and four culture-fermentation media viz. wheat, wheat bran, malt and rice) were optimized for producing microbial bioactive compounds. Microwave extraction was performed at 2450 MHz and 500 W for 20, 30, and 40 s with seven solvents (distilled water, ethyl acetate, hexane, ethanol, chloroform, diethyl ether, and methanol). The obtained results revealed that ethyl acetate is the most appropriate solvent for extraction. Effects of this ethyl acetate extract were compared with a commercial synthetic antioxidant. Antioxidant properties were enhanced by preventing the oxidation of the linoleic acid (C18H32O2) with an inhibition rate (antioxidant efficacy) of 73.13%. Notably, the ferrous ion binding ability was marginally lower when compared to the disodium salt of ethylenediaminetetraacetic acid (EDTA). Additionally, the obtained total content of phenolic compounds in the ethyl acetate extract of fermented rice (koji) by Aspergillus flavus was 232.11 mg based on gallic acid/mL. Antioxidant compounds in the ethyl acetate extract of fermented rice showed stability under neutral conditions, as well as at high temperatures reaching 185 °C during 2 h, but were unstable under acidic and alkaline conditions. The results demonstrate the efficacy of novel microwave-assisted extraction technique for accelerating antioxidant production during rice fermentation.

scholarly journals Recent Advances in In-Vitro Assays for Type 2 Diabetes Mellitus: An Overview

2020 ◽  
Vol 16 (1) ◽  
pp. 13-23
Author(s):  
Nazmina Vhora ◽  
Ujjal Naskar ◽  
Aishwarya Hiray ◽  
Abhijeet S. Kate ◽  
Alok Jain
Keyword(s):  
Type 2 Diabetes ◽  
Drug Discovery ◽  
High Throughput ◽  
High Throughput Screening ◽  
Antidiabetic Activity ◽  
Screening Methods ◽  
Selection Of

BACKGROUND: A higher rate of attenuation of molecules in drug discovery has enabled pharmaceutical companies to enhance the efficiency of their hit identification and lead optimization. Selection and development of appropriate in-vitro and in-vivo strategies may improve this process as primary and secondary screening utilize both strategies. In-vivo approaches are too relentless and expensive for assessing hits. Therefore, it has become indispensable to develop and implement suitable in-vitro screening methods to execute the required activities and meet the respective targets. However, the selection of an appropriate in-vitro assay for specific evaluation of cellular activity is no trivial task. It requires thorough investigation of the various parameters involved. AIM: In this review, we aim to discuss in-vitro assays for type 2 diabetes (T2D), which have been utilized extensively by researchers over the last five years, including target-based, non-target based, low-throughput, and high-throughput screening assays. METHODS: The literature search was conducted using databases including Scifinder, PubMed, ScienceDirect, and Google Scholar to find the significant published articles. DISCUSSION and CONCLUSION: The accuracy and relevance of in-vitro assays have a significant impact on the drug discovery process for T2D, especially in assessing the antidiabetic activity of compounds and identifying the site of effect in high-throughput screening. The report reviews the advantages, limitations, quality parameters, and applications of the probed invitro assays, and compares them with one another to enable the selection of the optimal method for any purpose. The information on these assays will accelerate numerous procedures in the drug development process with consistent quality and accuracy.

scholarly journals Isolation of bioactive compounds from Bergenia ciliata (haw.) Sternb rhizome and their antioxidant and anticholinesterase activities

2019 ◽  
Vol 19 (1) ◽  
Author(s):  
Roheena Zafar ◽  
Habib Ullah ◽  
Muhammad Zahoor ◽  
Abdul Sadiq
Keyword(s):  
Free Radicals ◽  
Free Radical ◽  
Ethyl Acetate ◽  
Silica Gel ◽  
Bioactive Compounds ◽  
Crude Extract ◽  
Radical Scavenging ◽  
Ethyl Acetate Fraction ◽  
Free Radical Scavenging ◽  
Total Phenolic

Abstract Background Bergenia ciliata is a medicinal plant used for the treatment of diarrhea, vomiting, fever, cough, diabetes, cancer, pulmonary disorders and wound healing. Methods In this study, Bergenia ciliata crude extract, subfractions, and isolated compounds were evaluated for their antioxidant and anticholinesterase potential. The free radical scavenging capacities of the extracts determined using DPPH and ABTS assays. The anticholinesterase potentials were determined using acetylcholine esterase and butyryl choline esterase enzymes. To determine the phytochemical composition, the extracts were subjected to HPLC analysis and silica gel column isolation. Based on HPLC fingerprinting results, the ethyl acetate fraction was found to have more bioactive compounds and was therefore subjected to silica gel column isolation. As a result, three compounds; pyrogallol, rutin, and morin were isolated in the pure state. The structures of the isolated compounds were elucidated using spectroscopic techniques like 1H-NMR, IR and UV-Visible. Results The crude extract showed maximum anticholinesterase (acetylcholinesterase = 90.22 ± 1.15% and butyrylcholinesterase = 88.22 ± 0.71%) and free radical scavenging (87.37 ± 2.45 and 83.50 ± 0.70% respectively against DPPH and ABTS radicals) potentials. The total phenolic contents (expressed as equivalent of gallic acid; mgGAE/g) were higher in ethyl acetate fraction (80.96 ± 1.74) followed by crude extract (70.65 ± 0.86) while the flavonoid contents (expressed as quercetin equivalent; mgQE/g) and were higher in crude extract (88.40 ± 1.12) followed by n-butanol fraction (60.10 ± 1.86). The isolated bioactive compounds pyrogallol, rutin, and morin were found active against ABTS and DPPH free radicals. Amongst them, pyrogallol was more active against both free radicals. Reasonable anticholinesterase activities were recorded for pyrogallol against selected enzymes. Conclusion The extracts and isolated compounds showed antioxidant and acetylcholinesterase inhibitory potentials. It was concluded that this plant could be helpful in the treatment of oxidative stress and neurological disorders if used in the form of extracts.

Aptamer‐based high‐throughput screening model for medicinal plant drugs against SGIV

2020 ◽  
Vol 43 (11) ◽  
pp. 1479-1482 ◽  
Author(s):  
Mingzhu Liu ◽  
Hehe Xiao ◽  
Siting Wu ◽  
Qing Yu ◽  
Pengfei Li
Keyword(s):  
Medicinal Plant ◽  
High Throughput ◽  
High Throughput Screening ◽  
Screening Model ◽  
Plant Drugs

scholarly journals A Recent Optimization and Advancement in the Development of Microwave-Assisted Extraction of Microbial Bioactive Compounds

2019 ◽  
Author(s):  
Hassan Hadi Mehdi AL Rubaiy ◽  
Ammar Altemimi ◽  
Ali Khudair Jaber Al Rikabi ◽  
Uttpal Anand ◽  
Naoufal Lakhssassi
Keyword(s):  
Ethyl Acetate ◽  
Bioactive Compounds ◽  
Ethyl Acetate Extract ◽  
Antioxidant Properties ◽  
Total Content ◽  
Antioxidant Compounds ◽  
Assisted Extraction ◽  
Alkaline Conditions ◽  
The Stability ◽  
Neutral Conditions

The current study aims to study the optimal fermentation conditions for producing microbial bioactive compounds. The microwave parameters consist on 2450 MHz, and 500-watt for 20, 30, and 40 seconds. The solubility of solvents was tested for the extraction of antioxidant compounds from fermented rice (Koji) by A. flavus, Ethyl acetate was the best solvent used for extraction purposes. Antioxidant properties were differentiated by blocking the oxidation of the linoleic acid with an inhibition rate of 73.13% at a concentration of 200 mg/mL, in addition to increasing its effectiveness for free radical extraction and reduction strength by increasing concentrations gradually. The bond ability to irons was lower compared to the EDTA-2Na, in addition to the obtained total content corresponding to phenolic compounds in the ethyl acetate extract of fermented rice (Koji) by A. flavus was 232.11 mg, on the basis of galic acid/mg. The stability of the antioxidant compounds of the ethyl acetate extract of fermented rice (Koji) by A. flavus was also studied; showing stability under neutral conditions, as well as at high temperatures (185 °C during two hours). However, no stability was obtained under acidic and alkaline conditions.

The Role of Data Mining in the Identification of Bioactive Compounds via High-Throughput Screening

2013 ◽  
pp. 131-154
Author(s):  
Kamal Azzaoui ◽  
John P. Priestle ◽  
Thibault Varin ◽  
Ansgar Schuffenhauer ◽  
Jeremy L. Jenkins ◽  
...  
Keyword(s):  
Data Mining ◽  
Bioactive Compounds ◽  
High Throughput ◽  
High Throughput Screening
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