Brine shrimp lethality assay ‘an effective prescreen’: Microwave-assisted synthesis, BSL toxicity and 3DQSAR studies-based designing, docking and antitumor evaluation of potent chalcones

Nazir, Samina; Ansari, Farzana Latif; Hussain, Tajammul; Mazhar, Kehkashan; Muazzam, Ambreen Gul; Ul-Haq, Zaheer; Makhmoor, Talat; Noureen, Humera; Mirza, Bushra

doi:10.3109/13880209.2013.777930

Cited by 19 publications

(13 citation statements)

References 41 publications

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“…A 1 = absorbance of extract/standard. (10,20,40,80, 100 μg/ml). The control sample consisted of 0.5 mL of RBCs mixed with hypotonic-buffered saline alone.…”

Section: Determination Of Anti-oxidant Activitymentioning

confidence: 96%

“…Studies have found very good relationship between this simple, inexpensive, and bench-top assay and the antitumor potential of the cytotoxic compounds [10]. So, BSLB might be helpful as a preliminary screening in the antitumor drug designing and synthesis expeditions [10].…”

Section: Introductionmentioning

confidence: 96%

“…This assay has been extensively used for different studies such as for preliminary toxicity screening of plant extracts, detection of fungal toxins, plant extract toxicity, heavy metals, cyanobacteria toxins, pesticides, and cytotoxicity testing of dental materials [9]. Studies have found very good relationship between this simple, inexpensive, and bench-top assay and the antitumor potential of the cytotoxic compounds [10]. So, BSLB might be helpful as a preliminary screening in the antitumor drug designing and synthesis expeditions [10].…”

Section: Introductionmentioning

confidence: 99%

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Bioactivity evaluations of leaf extract fractions from young barley grass and correlation with their phytochemical profiles

Panthi

Subba

Raut

et al. 2020

BMC Complement Med Ther

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Background: The pressed juice of Barley Grass (BG) has become very popular among people for various assumed benefits along with many testimonies of people who have been healed from various ailments such as anemia, cancer, GI problems by consuming BG. The aim of our research was to validate the claims of its medicinal values such as chemo-protective action, high anti-oxidants, RBC membrane stabilization activity, and toxicity level. Methods: Extracts of hexane, ethyl acetate and methanol were quantitatively estimated for total phenolic contents (TPC) and total flavonoid contents (TFC). The same extracts were assessed for their antioxidative potentials with the use of DPPH free radical scavenging assay followed by determination of HRBC membrane stabilization method, Brine Shrimp Lethality Assay (BSLA) and GC-MS analysis. Results: All the extracts showed high TPC and TFC along with the stronger correlation with the antioxidant activity of the extracts suggesting phenolics and flavonoids contents of the extract might be attributed to showing antioxidant activity. The methanolic and ethyl acetate extracts of the plant also showed remarkable antiinflammatory activity where methanolic extracts had the lowest EC50. During Brine Shrimp Lethality Assay, all extracts of BG were found to be bioactive and the degree of lethality was found to be concentration dependent. The GC-MS analysis of the methanolic extract of BG revealed 23 compounds which are reported to possess different biological activities. Conclusion: The study reveals the strong antioxidant and RBC membrane stabilization activity of BG. The Brine Shrimp Lethality Assay found extracts to be bioactive suggesting extracts as a promising candidate for plantderived anti-tumor compounds. Further, studies are needed to validate the data on cancer cell lines.

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“…A 1 = absorbance of extract/standard. (10,20,40,80, 100 μg/ml). The control sample consisted of 0.5 mL of RBCs mixed with hypotonic-buffered saline alone.…”

Section: Determination Of Anti-oxidant Activitymentioning

confidence: 96%

Section: Introductionmentioning

confidence: 96%

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Bioactivity evaluations of leaf extract fractions from young barley grass and correlation with their phytochemical profiles

Panthi

Subba

Raut

et al. 2020

BMC Complement Med Ther

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“…Their structures, bearing two benzene rings (A and B), are linked by an enone bridge. They have demonstrated antiproliferative activity against cancer cells, including breast cancer [13][14][15] . Mai et al described chalcone was effective against ERpositive breast cancer cells (MCF-7 line) targeting 20 apoptotic markers 16 .…”

Section: Introductionmentioning

confidence: 99%

Antiproliferative activity and p53 upregulation effects of chalcones on human breast cancer cells

Santos

Anselmo

Oliveira

et al. 2019

Journal of Enzyme Inhibition and Medicinal Chemistry

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Chalcones are valuable structures for drug discovery due to their broad bioactivity spectrum. In this study, we evaluated 20 synthetic chalcones against estrogen-receptor-positive breast cancer cells (MCF-7 line) and triple-negative breast cancer (TNBC) cells (MDA-MB-231 line). Antiproliferative screening by MTT assay resulted in two most active compounds: 2-fluoro-4'-aminochalcone (11) and 3-pyridyl-4'-aminochalcone (17). Their IC 50 values ranged from 13.2 to 34.7 mM against both cell lines. Selected chalcones are weak basic compounds and maintained their antiproliferative activity under acidosis conditions (pH 6.7), indicating their resistance to ion-trapping effect. The mode of breast cancer cells death was investigated and chalcones 11 and 17 were able to induce apoptosis rather than necrosis in both lines. Antiproliferative target investigations with MCF-7 cells suggested 11 and 17 upregulated p53 protein expression and did not affect Sp1 protein expression. Future studies on chalcones 11 and 17 can define their in vivo therapeutic potential.

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“…Brine shrimp lethality (BSL) assay has been shown to have a good correlation with other antitumor assays. The BSL model has proved helpful as a preliminary screening model in the drug design and synthesis of cytotoxic compounds (Nazir et al, 2013). The lethality of the extracts on the brine shrimps was classified by Padmaja et al (2002).…”

Section: Discussionmentioning

confidence: 99%

Phytochemical, antioxidant, brine shrimp lethality and antiproliferative analyses of Solanum dasyphyllum schum. & thonn. leaf and fruit extracts [Solanaceae]

2019

Savannah Vet J

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Introduction: Solanum dasyphyllum is an edible egg plant belonging to Solanaceae family. The fruit and leaf of S. dasyphyllum are traditionally used to relief swellings and oedema. In this study, we investigated the phytochemical constituents, DPPH antioxidant activity, brine shrimp lethality and cytotoxicity on human cancer cell lines of the leaf and fruit extracts of S. dasyphyllum. Methods: The leaf and fruit extracts of S. dasyphyllum were subjected to phytochemical screening, in vitro antioxidant assay using DPPH, brine shrimp lethality (BSL) bioassay and MTT colorimetric assay using human cancer cell lines. Results: The leaf and fruit of S. dasyphyllum tested positive for the presence of alkaloids, tannins, saponins and cardiac glycosides. Extract of the leaf (IC50 of 274.6±2.45 and LC50 of 406.0±7.41) and fruit (278.2±2.68 µg/mL and 766.7±9.14 µg/mL) displayed weak DPPH radical scavenging activity and brine shrimp lethality (BSL) compared to ascorbic acid (IC50=20.2±0.36 µg/mL) and cyclophosphamide (LC50 of 98.76±0.15 µg/mL) respectively. Compared to the fruits extracts, the leaf extract was found to be more cytotoxic with CC50 of 28.46±1.42, 2.99±0.15 and 23.33±2.7 µg/mL on the human cancer cell lines Rd, Hep-2c and the normal cell line, Vero, respectively in the MTT colorimetric assay. Significance: The leaf and fruit extracts of S. dasyphyllum had weak DPPH activity and elicited mild cytotoxicity in BSL assay. However, the leaf extract of displayed a higher cytotoxicity than the fruit extract on human cancer line used in the study.

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Brine shrimp lethality assay ‘an effective prescreen’: Microwave-assisted synthesis, BSL toxicity and 3DQSAR studies-based designing, docking and antitumor evaluation of potent chalcones

Cited by 19 publications

References 41 publications

Bioactivity evaluations of leaf extract fractions from young barley grass and correlation with their phytochemical profiles

Bioactivity evaluations of leaf extract fractions from young barley grass and correlation with their phytochemical profiles

Antiproliferative activity and p53 upregulation effects of chalcones on human breast cancer cells

Phytochemical, antioxidant, brine shrimp lethality and antiproliferative analyses of Solanum dasyphyllum schum. & thonn. leaf and fruit extracts [Solanaceae]

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