Cytotoxic Activities of Some Mono and Bis Mannich Bases Derived from Acetophenone in Brine Shrimp Bioassay

2011 ◽  
Vol 52 (11) ◽  
pp. 840-843
Author(s):  
Halise Gul ◽  
Mustafa Gul ◽  
Osmo Hänninen
Author(s):  
Deedarul Hyder Sani ◽  
Ali Newaz Munna ◽  
Mohammad Salim ◽  
Md. Jahangir Alam ◽  
Md. Jahangir Alam

Background: Diabetes mellitus is the most occurring non-communicable disease resulting in a high blood glucose level. There has been an immense interest in the development of alternative medicines for diabetes treatment, specifically screening functional foods for phytochemicals with the capability of delaying or preventing glucose absorption through digestive enzymes (e.g. α-amylase) inhibition. So, the development of α-amylase inhibitors derived from natural food products is an alternative way to prevent diabetes mellitus Objective: In this study, organic solvent extracts of the Arachis hypogaea (Peanut) and Cinnamomum tamala (Indian bay leaf /Tejpata) were used to investigate their potential α-amylase inhibition and cytotoxic activities through α-amylase inhibition assay and brine shrimp lethality bioassay respectively Method: The α-amylase inhibition assay was performed using the 3,5-dinitrosalicylic acid method for different concentrations of plant extracts. The optical density (OD) of the solutions were measured to determine the inhibition activity at 540 nm using a spectrophotometer. The cytotoxicity of the plant extracts was measured using brine shrimp (Artemia salina) lethality bioassay Results: Among the different organic solvent extracts, peanut seed ethanol extract showed the highest α-amylase inhibition activity (67.68±8.67%) at 1.25 μg/mL concentration with an IC50 value of 0.61 μg/mL which is very close to standard α-amylase inhibitor Acarbose (72.34±4.23%) with an IC50 value of 0.32 μg/mL while acetone extract of Indian bay leaf exhibited the lowest inhibition activity (47.75±1.63%) with an IC50 value of 1.42 μg/mL at the same concentration. Besides, the maximum cytotoxic activity was found in acetone extract of peanut shell with an LC50 value of 57.87 μg/mL whereas ethanol extract of peanut seed showed the lowest cytotoxicity with an LC50 value of 413.90 μg/mL Conclusion: The result of the present work clearly indicates the potentiality of peanut seed ethanol extract to be used in the management of hyperglycemia as it significantly inhibits α-amylase activity while showing less cytotoxic activities


2010 ◽  
Vol 39 (42) ◽  
pp. 10203 ◽  
Author(s):  
Amanda P. Neves ◽  
Gustavo B. da Silva ◽  
Maria D. Vargas ◽  
Carlos B. Pinheiro ◽  
Lorenzo do C. Visentin ◽  
...  

2009 ◽  
Vol 64 (7-8) ◽  
pp. 518-520 ◽  
Author(s):  
Yin Lu ◽  
Shaoyuan Chen ◽  
Ben Wang

Eleven strains of endophytic fungi which habitat in an endangered, Chinese endemic medicinal plant, Dysosma pleiantha (Hance) Woodson, were isolated and tested for their cytotoxic activity using the brine shrimp lethality bioassay. Six isolates were found to exhibit some cytotoxic activity. Extracts of F1273, F1276, and F1280, which were identified as Trichoderma citrinoviride, Chaetomium globosum and Ascomycete sp., in particular, showed most potent activity with LC50 values of 4.86, 7.71, and 14.88 μg/ml, respectively. These results indicate that endophytic fungi of Dysosma pleiantha could be a promising source for antitumour agents.


2015 ◽  
Vol 16 (2) ◽  
pp. 131-135
Author(s):  
M Sekendar Ali ◽  
Kazi Omar Faruq ◽  
Atiqul Islam ◽  
AMM Nurullah ◽  
Kazi Ashfak Ahmed Chowdhury ◽  
...  

The present study was designed to investigate the thrombolytic activity and cytotoxic potential of the methanolic extract of bark of Terminalia bellerica Roxb. The cytotoxicity was assessed with the brine shrimp lethality bioassay and thrombolytic effect with human blood. The brine shrimp lethality bioassay was used to evaluate cytotoxicity (LC50 = 3.21 ?g/ml) compared to vincristine of sulphate (LC50 = 0.512 ?g /ml). It was also evaluated as thrombolytic agent as compared to streptokinase. It has significant thrombolytic activity (32.95%) compared to standard streptokinase (70%). DOI: http://dx.doi.org/10.3329/bpj.v16i2.22293 Bangladesh Pharmaceutical Journal 16(2): 131-135, 2013


Author(s):  
Emine Erdag

Aims: In this study, a series of new Mannich bases of 2(3H)-benzoxazolone derivatives containing substituted cyclic amine moieties with a potential to show cytotoxic activity have been prepared. In order to develop effective anticancer agents against various cancer cell lines, it is essential to study the structure activity relationship and the effect of different substituents on the activity of heterocyclic scaffolds which were known to have cytotoxic activities. Study Design: In silico and experimental design. Place and Duration of Study: Pharmaceutical Chemistry Department, Faculty of Pharmacy, Near East University, Nicosia, Cyprus, between January 2019- September 2020. Methodology: In this work, 2(3H)-benzoxazolone derivatives were prepared by Mannich reaction. The synthesis and structural characterization of the compounds were performed experimentally by FT-IR, 1H NMR, 13C NMR spectra and elemental analysis. In silico prediction of cell line cytotoxicity with PASS based CLC-Pred tool was performed to predict cytotoxicity of the compounds against different tumor cell lines. Results: In silico prediction results for the compounds showed that all benzoxazolone derivatives have cytotoxic activity against different cell lines and tumor types. It was clearly understood that the cytotoxicity of the compounds was affected by the substituents on their piperazine moieties and by the substituents on benzoxazolone core structure. Conclusion: In conclusion, newly synthesized Mannich bases of benzoxazolone derivatives were reported for the first time which may have a potential to show anticancer activities at different cancer cell lines. The efficiency of new compounds against cancer could be found via PASS based CLC-Pred database and could be further investigated by in vivo experimental cytotoxicity studies in the future to design new anticancer drug candidates.


Marine Drugs ◽  
2018 ◽  
Vol 16 (12) ◽  
pp. 519 ◽  
Author(s):  
Yuan-Ming Zhou ◽  
Guang-Lin Ju ◽  
Lin Xiao ◽  
Xiang-Fei Zhang ◽  
Feng-Yu Du

On the basis of the ‘one strain, many compounds’ (OSMAC) strategy, chemical investigation of the marine-derived fungus Trichothecium roseum resulted in the isolation of trichomide cyclodepsipeptides (compounds 1–4) from PDB medium, and destruxin cyclodepsipeptides (compounds 5–7) and cyclonerodiol sesquiterpenes (compounds 8–10) from rice medium. The structures and absolute configurations of novel (compounds 1, 8, and 9) and known compounds were elucidated by extensive spectroscopic analyses, X-ray crystallographic analysis, and ECD calculations. All isolated compounds were evaluated for cytotoxic, nematicidal, and antifungal activities, as well as brine shrimp lethality. The novel compound 1 exhibited significant cytotoxic activities against the human cancer cell lines MCF-7, SW480, and HL-60, with IC50 values of 0.079, 0.107, and 0.149 μM, respectively. In addition, it also showed significant brine shrimp lethality, with an LD50 value of 0.48 μM, and moderate nematicidal activity against Heterodera avenae, with an LC50 value of 94.9 μg/mL. This study constitutes the first report on the cytotoxic and nematicidal potential of trichomide cyclodepsipeptides.


Author(s):  
Asim Debnath ◽  
Mohammad Salim ◽  
Md Faruque Miah ◽  
Rezaul Karim ◽  
Md Jahangir Alam

Invertase, the key enzyme responsible for sucrose hydrolysis. Inhibition of invertase can decrease the postprandial blood sugar level in diabetic patients and keep the blood glucose level normal where cytotoxicity to fast-growing cells like those of brine shrimp (Artemia salina) nauplii is a great measurement for further important drug development. This study was aimed to investigate potential anti-diabetic and cytotoxic activities of the ethanol and acetone extracts of Swietenia macrophylla leaves, Syzygium cumini and Trigonella foenum-graecum seeds. Invertase inhibition activities of S. macrophylla leaves, S. cumini, and T. foenum-graecum seeds were measured by spectrophotometrically using standard protocols and cytotoxicity were measured by brine shrimp lethality bioassay. Among the plant extracts, all ethanol extracts showed higher invertase inhibition activities than all acetone extracts. S. cumini seed ethanol extract showed the highest invertase inhibition activity whereas S. macrophylla leaves acetone extract showed the lowest invertase inhibition activity. The maximum toxicity was observed in ethanol extract of T. foenum-graecum seed whereas the lowest toxicity was observed in acetone extract of S. macrophylla leaves. Both ethanol and acetone extract of T. foenum-graecumseeds showed significant cytotoxic activities. This investigation suggested that S. cumini and T. foenum-graecum seeds possess potential antidiabetic activities and T. foenum-graecum seeds have potential cytotoxicity.


2015 ◽  
Vol 14 (1) ◽  
pp. 55-59 ◽  
Author(s):  
Fahrima Islam ◽  
Amir Hossain ◽  
Md Golam Hossain ◽  
Gazi Md Monjur Murshid ◽  
Md Mustafizur Rahman

Ethanolic extract of the root of Typha angustata was evaluated for antioxidant, analgesic and cytotoxic activities. T. angustata extract exhibited DPPH free radical scavenging activity with IC50 value of 124.96 ± 0.93 ?g/ml. The total phenolic and tannin content were found to be 596.73 ± 1 mg GAE/100 g and 319.68 ± 64 mg GAE/100 g of dried plant material, respectively. Analgesic activity was determined using acetic acid induced writhing inhibition in mice model. The root extract, at doses of 250 mg/kg and 500 mg/kg body weight, showed inhibition of writhing reflex by 33.55% (p < 0.01) and 56.78% (p<0.001), respectively. Cytotoxicity of the extract was measured by brine shrimp lethality bioassay where the LC50 against brine shrimp nauplii was found to be 41.54?g/ml.Dhaka Univ. J. Pharm. Sci. 14(1): 55-59, 2015 (June)


2013 ◽  
Vol 41 (2) ◽  
pp. 155-158
Author(s):  
TM Quadery ◽  
F Islam ◽  
M Ahsan ◽  
CM Hasan

A methanolextract of the leaves of Parabaena sagitatta Miers and its petroleum ether, carbon tetrachloride, dichloromethane, ethylacetate and aqueous soluble partitionates were evaluated for antioxidant activity by 1,1-diphenyl-2-picrylhydrazyl (DPPH), Folin-Ciocalteau reagent and phosphomolybdenum total antioxidant assays by using butylated hydroxytolune (BHT) and ascorbic acid as standards. The dichloromethane soluble fraction demonstrated the presence of significant amount of phenolic compounds 61.06 ± 0.54 mg GAE/g of extract and also has moderate antioxidant activity IC50 50.62 ± 0.25 ?g/ml. A positive correlation (R2), 0.969 was observed between total phenolic content and total antioxidant activity of P. sagitatta. The general toxicity was determined by brine shrimp lethality bioassay where the dichloromethane LC50DOI: http://dx.doi.org/10.3329/bjb.v41i2.13441 Bangladesh J. Bot. 41(2): 155-158, 2012 (December)


2013 ◽  
Vol 11 (2) ◽  
pp. 117-120
Author(s):  
ATM Zafrul Azam ◽  
Abdullah Al Hasan ◽  
Md Gias Uddin ◽  
Mohammad Mehedi Masud ◽  
Choudhury Mahmood Hasan

The methanol extract (ME) of the powdered bark of Glochidion multiloculare and its six vacuum liquid chromatographic (VLC) fractions (Fa-f) were investigated for antimicrobial, cytotoxic and antioxidant activities. Only fractions Fc and Fd showed mild antimicrobial activity. Significant free radical (DPPH) scavenging activity was found in Ff (IC50 value = 9.27±0.117 ?g/ml). The total phenolic content was measured involving Folin-Ciocalteu reagent and it was the highest in fraction Fe (187.00±1.74 mg of GAE/gm of sample). Cytotoxicity (LC50) by brine shrimp lethality bioassay was found to be significant for Fb (0.023±0.001 ?g/ml), Fc (0.3±0.01 ?g/ml) and Fd (0.117±0.0015 ?g/ml). DOI: http://dx.doi.org/10.3329/dujps.v11i2.14560 Dhaka Univ. J. Pharm. Sci. 11(2): 117-120, 2012 (December)


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