scholarly journals In Vitro Cytotoxic Potential of Plant Terpenes and Selected Medicinal Plants of Pakistan against NIH 3T3 Cell Line.

2018 ◽  
Vol 24 (S) ◽  
pp. 853-858
Author(s):  
Shazia Kanwal Malik ◽  
Maqsood Ahmed ◽  
Farah Khan
Keyword(s):  
Medicinal Plants ◽  
Cell Line ◽  
Acid Methyl Ester ◽  
Hexadecanoic Acid ◽  
Cytotoxic Potential ◽  
Reference Drug ◽  
Animal Trials ◽  
Diphenyl Tetrazolium Bromide ◽  
Nih 3T3

Background: Medicinal plants are used in anticancer therapies from ages. The very first time we have not only screened anticancer medicinal plants from Pakistan but also identified anticancer plant terpenes. This study will definitely pave the way towards anticancer drug development after animal trials. Materials and Methods | This study was based on ethanolic extraction of fruits/seed of 25 plants. The cytotoxic potential of extracts and plant terpenes was evaluated against mouse fibroblasts (NIH 3T3) cell line by using MTT (3- [4, 5-dimethylthiazole-2-yl]-2, 5-diphenyl-tetrazolium bromide) assay and compared with cyclohexamide. Results | Ethanolic extracts were nontoxic against NIH3T3 cell line. On the basis of the % inhibition plants were graded as B.lycium, 48% > T.bellerica, 47% > C.verum, 45% > Z.tenuior, 39% > H. adenophyllum, 38% > C. carandas, 31% > C.behen, 29% > P. juliflora, 28% & P.granatum, 28% W.somnifera, 27% > E.cheiri, 26% > S. potatorum, 24% & M.incana, 24% > D. peregrina, 21% & B.lanzan, 21% > L. maldivica, 20% > F. lyrata, 18% > F.arabica, 16% & R. indica, 16% > C.absus, 13% & C.paniculatus, 13%. > C. diurnum, 12% > J.mimosifolia, 11% > D.malabarica, 8% > C. speciosa, 3% as compared to the reference drug Cyclohexamide, 70%. Whereas the maximum % inhibition was exhibited by n-Hexadecanoic acid (88%), followed by Hexadecanoic acid, methyl ester (16%) and Methyl decanoate displayed 11%. C50 of n-Hexadecanoic acid and Cyclohexamide was 3.1±0.2 and 0.8±0.2 respectively. Conclusion| Plant extracts and terpenes was found to be inactive against 3T3 cell line.

scholarly journals Assessment of the in Vitro Antiprotozoal and Cytotoxic Potential of 20 Selected Medicinal Plants from the Island of Soqotra

Molecules ◽  
2012 ◽  
Vol 17 (12) ◽  
pp. 14349-14360 ◽  
Author(s):  
Ramzi Mothana ◽  
Nawal Al-Musayeib ◽  
An Matheeussen ◽  
Paul Cos ◽  
Louis Maes
Keyword(s):  
Medicinal Plants ◽  
Cytotoxic Potential

scholarly journals Evaluation of cytotoxic potential of L-asparaginase from Scopulariopsis brevicaulis on cell lines in vitro

Biomedicine ◽  
2020 ◽  
Vol 39 (2) ◽  
pp. 254-257
Author(s):  
D’Souza Renita Maria ◽  
Abraham Asha
Keyword(s):  
Cell Line ◽  
Gel Filtration ◽  
Positive Control ◽  
Enzyme Concentration ◽  
Cytotoxic Potential ◽  
3T3l1 Cell ◽  
Maximum Inhibition ◽  
Scopulariopsis Brevicaulis ◽  
Mcf7 Cell Line

Introduction and Aim: This study reports the cytotoxic potential of L-Asparaginase isolated from the fungus Scopulariopsis brevicaulis. Materials and Methods: Extracellular L- Asparaginase was isolated from Scopulariopsis brevicaulis and purified by ammonium sulfate precipitation, followed by dialysis, ion exchange and gel filtration chromatography. Varying concentrations (31.25, 62.5, 125, 250, 500 µg/ml) of purified L-Asparaginase was tested on MCF7, HeLa, HepG2 and 3T3L1cell lines by MTT assay. Curcumin was maintained as a positive control. Results: Minimum inhibition of 23.57% was observed at an enzyme concentration of 31.25 µg/ml and maximum inhibition (66.41%) was observed at 500 µg/ml against MCF7 cell line. Minimum inhibition of 2.87% was observed at an enzyme concentration 31.25 µg/ml and maximum inhibition (58.49%) was observed at 500 µg/ml against HeLa cell line. Minimum inhibition of 4.58% was shown at an enzyme concentration of 31.25 µg/ml and maximum inhibition (46.14 %) was observed at 500 µg/ml against HepG2 cell line. Minimum inhibition of 1.4% was shown by enzyme concentration 31.25 µg/ml and maximum inhibition (50.9%) was observed at 500 µg/ml against 3T3L1 cell line. Conclusion: We report for the first time the cytotoxic potential of L-Asparaginase from Scopulariopsis brevicaulis.  

scholarly journals EVALUATION AND COMPARISON OF CYTOTOXIC EFFECT OF VILAZODONE HYDROCHLORIDE WITH 5-FLUOROURACIL IN HT-29 BOWEL CANCER CELL LINE

2019 ◽  
pp. 124-127
Author(s):  
LATHA PRIYA A ◽  
ANUSHA D ◽  
DARLING CHELLATHAI K ◽  
HEMALATHA A ◽  
JEGAN MOHAN Y
Keyword(s):  
Cell Line ◽  
Cytotoxic Effect ◽  
Depressive Disorders ◽  
Cancer Cell Line ◽  
Test Sample ◽  
Standard Drug ◽  
Drug Sample ◽  
Diphenyl Tetrazolium Bromide ◽  
Ht 29

Objectives: Vilazodone hydrochloride is a novel selective serotonin reuptake inhibitor (SSRI) used to treat major depressive disorders. There are only sparse data available to know about the SSRI’s and its association with colon cancer. This study aims to evaluate and compare the in vitro cytotoxic effect of vilazodone with 5-fluorouracil (5-FU) in HT-29 cell line. Methods: Cell viability was tested by the 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay (Mosmann, 1983). Test sample and standard drug in variable concentrations were added to the HT-29 cell lines for incubation over 24 h under ideal conditions. After washing the test and standard drug sample from the well with saline, MTT was added and incubated for 4 h. Dimethyl sulfoxide of 1 ml was added in all wells after incubation with MTT. The absorbance at 570 nm was measured with an ultraviolet - spectrophotometer. Results: The values were tabulated, and the graph was plotted to find the IC-50 value (inhibitory concentration at 50%) which was struck at 28.5 μg/ml and12. 8 μg/ml for vilazodone hydrochloride and 5-FU, respectively. Conclusion: The results show that vilazodone hydrochloride has good anticancer property comparable with 5-FU, which would probably play a role as a cytotoxic agent in tumor cells. The proposed mechanism of action could be by activation of caspase-3 enzyme, thereby increasing apoptosis and indicates its use in coexisting depression and colon carcinoma. Other mechanism includes suppression of oncogene p53, which can be confirmed by future studies.

scholarly journals In VitroUltramorphological Assessment of Apoptosis on CEMss Induced by Linoleic Acid-Rich Fraction fromTyphonium flagelliformeTuber

2011 ◽  
Vol 2011 ◽  
pp. 1-12 ◽  
Author(s):  
Syam Mohan ◽  
Ahmad Bustamam ◽  
Siddig Ibrahim ◽  
Adel S. Al-Zubairi ◽  
Mohammed Aspollah ◽  
...  
Keyword(s):  
Linoleic Acid ◽  
Cell Line ◽  
Chromatin Condensation ◽  
Terminal Deoxynucleotidyl Transferase ◽  
Gas Chromatography Mass Spectrometry ◽  
Cancer Therapies ◽  
Hexadecanoic Acid ◽  
Dna Breaks ◽  
Cellular Dna

The plantTyphonium flagelliforme, commonly known as “rodent tuber” in Malaysia, is often used as a health supplement and traditional remedy for alternative cancer therapies, including leukemia. This study aimed to evaluatein vitroanti-leukemic activity of dichloromethane extract/fraction number 7 (DCM/F7) fromT. flagelliformetuber on human T4 lymphoblastoid (CEMss) cell line. The DCM extract of tuber has been fractionated by column chromatography. The obtained fractions were evaluated for its cytotoxicity toward CEMss cells as well as human primary blood lymphocytes (PBLs). Assessment of apoptosis produced by the most active fraction was evaluated by various microscopic techniques and further confirmation of apoptosis was done by terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL) assay. Phytochemical screening was done by gas chromatography-mass spectrometry (GC-MS). The results shows that 7 out of 12 fractions showed significant cytotoxicity against the selected cell line CEMss, in which fractions DCM/F7, DCM/F11 and DCM/F12 showed exceptional activity with 3, 5 and 6.2 μg ml−1, respectively. Further studies in the non-cancerous PBL exhibited significant selectivity of DCM/F7 compared to other fractions. Cytological observations showed chromatin condensation, cell shrinkage, abnormalities of cristae, membrane blebbing, cytoplasmic extrusions and formation of apoptotic bodies as confirmed collectively by double-staining of acridine orange (AO)/propidium iodide (PI), SEM and TEM. In addition, DCM/F7 has increased the cellular DNA breaks on treated cells. GC-MS revealed that DCM/F7 contains linoleic acid, hexadecanoic acid and 9-hexadecanoic acid. The present results indicate thatT. flagelliformepossess a valuable anti-leukemic effect and was able to produce distinctive morphological features of cell death that corresponds to apoptosis.

Synthesis of 2-Substituted 4-Arylidene-5(4H)-oxazolones as Potential Cytotoxic Agents in the Presence of Lemon Juice as a Biocatalyst

2020 ◽  
Vol 22 (9) ◽  
pp. 625-634 ◽  
Author(s):  
Malavattu G. Prasad ◽  
Chapala V. Lakshmi ◽  
Naresh K. Katari ◽  
Krishnan Anand ◽  
Manojit Pal ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Cell Line ◽  
Anticancer Agents ◽  
Human Colon ◽  
Malignant Cell ◽  
Lemon Juice ◽  
Cytotoxic Agents ◽  
Reference Drug ◽  
Initial Objective

Background: The oxazolone class of compounds is known to exert a profound effect on malignant cell proliferation, tumor angiogenesis and /or on the established neoplastic vasculature. Additionally, these compounds are generally known to have a low tendency to interact with DNA which is not common with most of the conventional cytotoxic agents. Thus, this class of compounds is of particular interest for the discovery and development of patient-friendly anticancer agents. Objective: The initial objective of this study was to synthesize and evaluate 2-substituted 4-arylidene- 5(4H)-oxazolones for their potential anticancer properties. Methods: A simple, mild and non-hazardous synthetic methodology has been developed for the preparation of 2-substituted 4-arylidene-5(4H)-oxazolones. The methodology involved lemon juice mediated condensation of N-acyl glycine derivatives including hippuric acid with arylaldehydes in PEG-400 under ultrasound irradiation. All the synthesized compounds were screened via an MTT assay for their potential cytotoxic properties in vitro using the cancerous cell lines e.g. K562 (human chronic myeloid leukemia), Colo-205 (human colon carcinoma), and A549 (human lung carcinoma) and a non-cancerous HEK293 (human embryonic kidney) cell line. Results: Compounds 3a, 3c and 3i showed promising growth inhibition against A549 cell line but no significant effects on HEK293 cell line, indicating their selectivity towards cancer cells. Moreover, their IC50 values suggested that all these compounds were comparable to the reference drug doxorubicin indicating their potential against lung cancer. Conclusion: he 4-arylidene-5(4H)-oxazolone framework presented here could be a new template for the design and discovery of potential anticancer agents especially for lung cancer.

Natural chemical entities as bioactive moiety from weaver ant, Oecophylla smaragdina: An in vitro and in silico Study

2020 ◽  
Vol 17 ◽  
Author(s):  
Suchismeeta Behera ◽  
Priyanka Dash ◽  
Amulyaratna Behera ◽  
Chinmaya Chidananda Behera ◽  
Prafulla Kumar Mohanty
Keyword(s):  
Methyl Ester ◽  
Inhibitory Activity ◽  
In Silico ◽  
Acid Methyl Ester ◽  
Hexane Extract ◽  
Bioactive Molecules ◽  
Hexadecanoic Acid ◽  
Acid Methyl ◽  
In Silico Study

Background: Since time immemorial the ethnic community of Mayrubhanj District, Odisha, India has preferred to Olecophylla smaragdina as traditional medicine for their multiple ailments. Hence, the objective of the investigation is to scientifically examine the myth behind ethno-zoological claims using chemometric analysis as well as in vitro and in silico study. Methods: The maceration method was used for the extraction of O. smaragdina using hexane and methanol. In this study, various bioactive compounds of O. smaragdina were identified through GC MS analysis followed by an antimicrobial activity. The species was further studied for their binding modes for in silico inhibition of a choice of bacterial proteins using Biovia Discovery studio software. Results: Tetradecanoic acid, hexadecanoic acid, methyl ester, hexadecenoic acid, n-hexadecanoic acid, 9-octadecenoic acid, methyl ester, oleic acid, 9-octadecenamide are some important bioactive constituents identified through GCMS analysis. The hexane extract was found to be maximum inhibitory activity against Staphyllococus aureus. The % inhibitory activity of hexane and methanolic extract against S. aureus at a concentration of 400 μg/mL was found to be 90 and 83%, respectively. The high inhibitory capacity of the n-hexane extract was comparable to the standard drug Gentamycin which further supported the high receptor binding affinity of identified compound Octadecanoic acid towards Tyrosol-t RNA synthetase of staphylococcus aureus (PDB ID: 1JIK). Conclusion: Interestingly, this is probably the first report that the obtained bioactive molecules from O. smaragdina showed that binding site identification to carry out molecular docking studies and results showed that the better affinity to bind with suitable targeted moiety.

scholarly journals Biological Evaluation ofPupalia lappaceafor Antidiabetic, Antiadipogenic, and Hypolipidemic Activity BothIn VitroandIn Vivo

Scientifica ◽  
2016 ◽  
Vol 2016 ◽  
pp. 1-9 ◽  
Author(s):  
Vivek Kumar ◽  
Parag Jain ◽  
Kalpana Rathore ◽  
Zabeer Ahmed
Keyword(s):  
Cell Line ◽  
Reference Group ◽  
Lipid Level ◽  
Biological Evaluation ◽  
Diabetic Rats ◽  
Hypolipidemic Activity ◽  
Albino Rats ◽  
Reference Drug

Objective. The present study assesses the effect ofPupalia lappacea(L.) Juss. (Amaranthaceae) (PL) leaves ethanolic extract on adipocytes, blood glucose level, and lipid level in streptozotocin (STZ) induced diabetic rats.Materials and Methods. Male Albino rats were rendered diabetic by a single moderately sized dose of STZ (45 mg/kg, intraperitoneally) at once before starting the treatment. Animals were divided into five groups: normoglycemic control, diabetic control, reference group (glibenclamide, 5.0 mg/kg), AS001 (250 mg/kg extract), and AS002 (500 mg/kg extract) each containing six animals forin vivostudy. Antidiabetic and hypolipidemic activity of extract were determined byin vivomethod on STZ induced diabetic rats. Antiadipogenic activity was determined byin vitromethod on 3T3-L1 cell line in comparison to simvastatin as reference drug.Result. The extract showed significant fall in fasting serum glucose (FSG), that is, 234.68 and 211.61 mg/dL, in STZ induced diabetic animals for dose groups AS001 and AS002, respectively. ThePLextract also exhibited noteworthy antiadipogenic activity on 3T3-L1 cell line. The value of inhibitory concentration (IC50) ofPLextract to reduce adipocyte cells was found to be 662.14 μg/mL.Conclusion. ThePLextract exhibited significant antiadipogenic, antidiabetic, and hypolipidemic activities.

scholarly journals Pyrazole Incorporated New Thiosemicarbazones: Design, Synthesis and Investigation of DPP-4 Inhibitory Effects

Molecules ◽  
2020 ◽  
Vol 25 (21) ◽  
pp. 5003
Author(s):  
Belgin Sever ◽  
Hasan Soybir ◽  
Şennur Görgülü ◽  
Zerrin Cantürk ◽  
Mehlika Dilek Altıntop
Keyword(s):  
Cell Line ◽  
Aromatic Aldehydes ◽  
Docking Studies ◽  
Phenyl Isothiocyanate ◽  
Inhibitory Effects ◽  
Dipeptidyl Peptidase 4 ◽  
Ic50 Value ◽  
In Silico Studies ◽  
Nih 3T3

Dipeptidyl peptidase-4 (DPP-4) inhibition has been recognized as a promising approach to develop safe and potent antidiabetic agents for the management of type 2 diabetes. In this context, new thiosemicarbazones (2a–o) were prepared efficiently by the reaction of aromatic aldehydes with 4-[4-(1H-pyrazol-1-yl)phenyl]thiosemicarbazide (1), which was obtained via the reaction of 4-(1H-pyrazol-1-yl)phenyl isothiocyanate with hydrazine hydrate. Compounds 2a–o were evaluated for their DPP-4 inhibitory effects based on a convenient fluorescence-based assay. 4-[4-(1H-pyrazol-1-yl)phenyl]-1-(4-bromobenzylidene)thiosemicarbazide (2f) was identified as the most effective DPP-4 inhibitor in this series with an IC50 value of 1.266 ± 0.264 nM when compared with sitagliptin (IC50 = 4.380 ± 0.319 nM). MTT test was carried out to assess the cytotoxic effects of compounds 2a–o on NIH/3T3 mouse embryonic fibroblast (normal) cell line. According to cytotoxicity assay, compound 2f showed cytotoxicity towards NIH/3T3 cell line with an IC50 value higher than 500 µM pointing out its favourable safety profile. Molecular docking studies indicated that compound 2f presented π-π interactions with Arg358 and Tyr666 via pyrazole scaffold and 4-bromophenyl substituent, respectively. Overall, in vitro and in silico studies put emphasis on that compound 2f attracts a great notice as a drug-like DPP-4 inhibitor for further antidiabetic research.

scholarly journals Determination of the Wound Healing Potentials of Medicinal Plants Historically Used in Ghana

2017 ◽  
Vol 2017 ◽  
pp. 1-6 ◽  
Author(s):  
Sara H. Freiesleben ◽  
Jens Soelberg ◽  
Nils T. Nyberg ◽  
Anna K. Jäger
Keyword(s):  
Wound Healing ◽  
Medicinal Plants ◽  
Plant Species ◽  
Cold Water ◽  
Water Extract ◽  
Scratch Assay ◽  
3T3 Fibroblasts ◽  
Nih 3T3 ◽  
Wound Healing Activity

The present study was carried out to investigate the wound healing potentials of 17 medicinal plants historically used in Ghana for wound healing. Warm and cold water extracts were prepared from the 17 dried plant species and tested in vitro in the scratch assay with NIH 3T3 fibroblasts from mice. The wound healing scratch assay was used to evaluate the effect of the plants on cell proliferation and/or migration in vitro, as a test for potential wound healing properties. After 21 hours of incubation increased proliferation and/or migration of fibroblasts in the scratch assay was obtained for 5 out of the 17 plant species. HPLC separation of the most active plant extract, which was a warm water extract of Philenoptera cyanescens, revealed the wound healing activity to be attributed to rutin and a triglycoside of quercetin. The present study suggests that Allophylus spicatus, Philenoptera cyanescens, Melanthera scandens, Ocimum gratissimum, and Jasminum dichotomum have wound healing activity in vitro.

scholarly journals Dispirooxindoles Based on 2-Selenoxo-Imidazolidin-4-Ones: Synthesis, Cytotoxicity and ROS Generation Ability

2021 ◽  
Vol 22 (5) ◽  
pp. 2613
Author(s):  
Vladimir K. Novotortsev ◽  
Maxim E. Kukushkin ◽  
Viktor A. Tafeenko ◽  
Dmitry A. Skvortsov ◽  
Marina A. Kalinina ◽  
...  
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
In Vitro Cytotoxicity ◽  
Selectivity Index ◽  
Azomethine Ylides ◽  
Ros Generation ◽  
Cytotoxic Action ◽  
Diphenyl Tetrazolium Bromide

A regio- and diastereoselective synthesis of two types of dispiro derivatives of 2-selenoxoimidazolidin-4-ones, differing in the position of the nitrogen atom in the central pyrrolidine ring of the spiro-fused system—namely, 2-selenoxodispiro[imidazolidine-4,3′-pyrrolidine-2′,3″-indoline]-2″,5-diones (5a-h) and 2-senenoxodispiro[imidazolidine-4,3′-pyrrolidine-4′,3″-indoline]-2″,5-diones (6a-m)—were developed based on a 1,3-dipolar cycloaddition of azomethine ylides generated from isatin and sarcosine or formaldehyde and sarcosine to 5-arylidene or 5-indolidene-2-selenoxo-tetrahydro-4H-imidazole-4-ones. Selenium-containing dispiro indolinones generally exhibit cytotoxic activity near to the activity of the corresponding oxygen and sulfur-containing derivatives. Compounds 5b, 5c, and 5e demonstrated considerable in vitro cytotoxicity in the 3-(4,5-dimethylthiazol-2-yl)2,5-diphenyl tetrazolium bromide (MTT) test (concentration of compounds that caused 50% death of cells (CC50) 7.6–8.7 μM) against the A549 cancer cell line with the VA13/A549 selectivity index 5.2–6.9 and compound 6e—against the MCF7 cancer cell line (CC50 20.6 μM, HEK293T/A549 selectivity index 1.6); some compounds (5 and 6) increased the level of intracellular reactive oxygen species (ROS) in the experiment on A549 and PC3 cells using platinized carbon nanoelectrode. The tests for p53 activation for compounds 5 and 6 on the transcriptional reporter suggest that the investigated compounds can only have an indirect p53-dependent mechanism of action. For the compounds 5b, 6b, and 6l, the ROS generation may be one of the significant mechanisms of their cytotoxic action.

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