PCR-Based Data and Secondary Metabolites as Chemotaxonomic Markers in High-Throughput Screening for Bioactive Compounds from Fungi

Secondary metabolites from fungi organisms have extensive past and present use in the treatment of many diseases and serve as compounds of interest both in their natural form and as templates for synthetic modification. Through high throughput screening (HTS) and bioassay-guided isolation, we isolated two bioactive compounds hamigerone (1) and radicinol (2). These compounds were isolated from fungusBipolaris papendorfii, isolated from the rice fields of Dera, Himachal Pradesh, India. The structures of the compounds were established on the basis of spectroscopic data, namely, NMR (1H,13C, mass, and UV). Both compounds were found to be antiproliferative against different cancer cells. Furthermore we have also noted that both compounds showed increase in apoptosis by favorably modulating both tumor suppressor protein (p53) and antiapoptic protein (BCL-2), and in turn increase caspase-3 expression in cancer cells. This is the first report of these compounds from fungusBipolaris papendorfiiand their anticancer activity.

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

Methods and Principles in Medicinal Chemistry - Data Mining in Drug Discovery ◽

10.1002/9783527655984.ch06 ◽

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

Journal of AOAC International ◽

10.5740/jaoacint.19-0287 ◽

2020 ◽

Vol 103 (3) ◽

pp. 669-677 ◽

Cited By ~ 2

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.

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Screening and synthesis: high throughput technologies applied to parasitology

Parasitology ◽

10.1017/s0031182004007073 ◽

2004 ◽

Vol 128 (S1) ◽

pp. S71-S79 ◽

Cited By ~ 2

Author(s):

R. E. MORGAN ◽

N. J. WESTWOOD

Keyword(s):

Bioactive Compounds ◽

High Throughput ◽

High Throughput Screening ◽

Target Identification ◽

Protein Target ◽

Genome Projects

High throughput technologies continue to develop in response to the challenges set by the genome projects. This article discusses how the techniques of both high throughput screening (HTS) and synthesis can influence research in parasitology. Examples of the use of targeted and phenotype-based HTS using unbiased compound collections are provided. The important issue of identifying the protein target(s) of bioactive compounds is discussed from the synthetic chemist's perspective. This article concludes by reviewing recent examples of successful target identification studies in parasitology.

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