scholarly journals Cytotoxic Activity of Pentacyclic Triterpene-3-Heptadecanoate Ester against Hela Cell Line and Its Docking Study

2017 ◽  
Vol 1 (1) ◽  
pp. 12
Author(s):  
Sri Mulyani Mulyadi ◽  
Tri Yuliati ◽  
Maulana Tegar ◽  
Imam Ardhila

Pentacyclic triterpene-3-heptadecanoate (12,13-dihydro-α-amyrin-20,30-en-3-heptadecanoate)ester refers to the compound as a result of reaction between pentacyclic triterpene-3-ol(12,13-dihydro-α-amyrin-20,30-en-3-ol) and heptadecanoic acid. This research was aimed to conductcytotoxicity test of pentacyclic triterpene-3-heptadecanoate; 12,13-dihydro-α-amyrin-20,30-en-3-oland 12,13-dihydro-α-amyrin-20,30-en-3-acetate esters against Hela cell line. The activity assay wascarried out using MTT method. The results indicated that IC50 value of 12,13-dihydro-α-amyrin-3-heptadecanoate; 12,13-dihydro-α-amyrin-20,30-en-3-acetate and 12,13-dihydro-α-amyrin-20,30-en-3-ol were 111.0, 151.1 and 944.4 μg/ml, respectively. The compound of 12,13-dihydro-α-amyrin-20,30-en-3-heptadecanoate had the lowest IC50 value, suggesting it has a potency to be synthesized as ananticancer drug.

2019 ◽  
Vol 6 (1) ◽  
pp. 30-32
Author(s):  
Poonkodi K ◽  
Mini R ◽  
Vimaladevi K ◽  
Prabhu V ◽  
Anusuya M ◽  
...  

The present investigation is carried out to study the invitro cytotoxicity of ethanol extract of Syzygium samarangense leaves on HeLa cell line by using MTT assay. Ethanol extract of S. samarangense showed concentration dependent activity on HeLa cell line with IC50 value of 40.5 μg/ml which shows that ethanol extract of S. samarangense posses significant cytoxicity.Moreover the preliminary phytochemical screening showed the presence of fatty acids, alkaloids, flavonoids, terphenoids, saponins, tannins and steroids which are responsible for its cytotoxicity. There are only a few reports are available for cytotoxicity of ethanol extract of S. samarangense.


Author(s):  
Anif Nur Artanti ◽  
Umi Hanik Pujiastuti ◽  
Fea Prihapsara ◽  
Rita Rakhmawati

As one of the leading causes of death in worldwide, cervical cancer requires the effective therapies to reduce its mortality rate. One of the chemotherapy agents that frequently used in the treatment is cisplatin. However, due to drug resistance and its side effects, an agent that can be combined with cisplatin is needed. Parijoto fruit (Medinilla speciosa Reinw.ex.Bl) contains secondary metabolites compounds that have potential as anticancer. The study aims to determine the cytotoxic effect of methanol extract of Parijoto fruit calculated from the IC50 value and the synergicity of the combinational treatment with cisplatin evaluated from the Combination Index (CI) value and its cell viability by using MTT assay. Results showed that methanol extract of Parijoto fruit (MEP) performed cytotoxic effect on HeLa cell line with IC50 of 209.6 μg/mL while the value of IC50 of cisplatin against HeLa cells amounted to 12.8 μg/mL. The combination of 26.205 ppm (1/8 IC50) of MEP and 1.601 ppm (1/8 IC50) of Cisplatin performed synergistic effect on HeLa cell line with the CI value of 0.69. From the above results, it can be concluded that MEP is potential as co-chemotherapy agent based on the synergistic cytotoxicity effect with cisplatin.Keyword: cytotoxic, Medinilla speciosa, cisplatin, co-chemotherapy, MTT


Author(s):  
Jamilah Abbas

The anticancer activities of medicinal plants from Indonesia’s tropical rainforests were investigated against Hela cell line. Maytenfoliol from leaves of Calophyllumtetrapterum 3-epibetulinic acid from stem bark of C. tomentosum Wight and D.A-friedo-oleanan-3-on from stem bark of C. moonii showed anticancer activity. The compound 3-epibetulinic acid showed the more potent anticancer activity than maytenfoliol and D.A-friedo-oleanan-3- with thean IC50 value were 3.17 μg/mL, 4.89 μg/mL and 5.63 μg/mL, respectively.Keywords: Anticancer evaluation, Hela cell line, Calophyllumtetrapterum. C. tomentosum Wight and C. moonii


Author(s):  
Renjini Haridas

Cancer is a group of diseases caused by loss of cell cycle control. Cancer is associated with abnormal uncontrolled cell growth. The study was aimed to evaluation of the anticancer activity of the Malaxis rheedei Sw. on the HeLa cell line and MCF- 7cell line. The whole plant part of the Malaxis rheedei methanolic extract were tested for its inhibitory effect on HeLa Cell Line and MCF- 7cell line. The cytotoxicity of Malaxis rheedei on HeLa cell and MCF- 7cell line were evaluated by the MTT assay. Malaxis rheedei methanolic extract has significant cytotoxicity effect on MCF- 7cell line in concentration range between 18.75 to 300 µg/ml by using MTT assay and study also showed that inhibitory action on HeLa cell line inconcentration range between 18.75 to 300 µg/ml by using MTT assay. Methanol extract of  the whole plant part of Malaxis rheedei was found to be 7.3%, 16.6%,  25.4%, 36.3% and 47.1%toxic in HeLa cell line and 7.9%, 13.9%, 26%, 48.4% and 66.3% toxic in MCF- 7cell line. IC50 value of Malaxis rheedei on MCF- 7cell was  167.76  µg/ml and IC50 value of Malaxis rheedei on HeLa Cell was not found by MTT assay. From the performed assay, methanol extract of these drug shows greater activity on MCF- 7cell line and little activity on HeLa cell line and that mean Malaxis rheedei can be used as anticancer activity.Keywords: Cytotoxicity Activity, MTT Assay, Malaxis rheedei Sw. , HeLa CellLine, MCF- 7Cell Line.


2020 ◽  
Vol 16 ◽  
Author(s):  
Jamshed Iqbal ◽  
Ayesha Basharat ◽  
Sehrish Bano ◽  
Syed Mobasher Ali Abid ◽  
Julie Pelletier ◽  
...  

Aims: The present study was conducted to examine the inhibitory effects of synthesized sulfonylhydrazones on the expression of CD73 (ecto-5′-NT). Background: CD73 (ecto-5′-NT) represents the most significant class of ecto-nucleotidases which are mainly responsible for dephosphorylation of adenosine monophosphate to adenosine. Inhibition of CD73 played an important role in the treatment of cancer, autoimmune disorders, precancerous syndromes, and some other diseases associated with CD73 activity. Objective: Keeping in view the significance of CD73 inhibitor in the treatment of cervical cancer, a series of sulfonylhydrazones (3a-3i) derivatives synthesized from 3-formylchromones were evaluated. Methods: All sulfonylhydrazones (3a-3i) were evaluated for their inhibitory activity towards CD73 (ecto-5′-NT) by the malachite green assay and their cytotoxic effect was investigated on HeLa cell line using MTT assay. Secondly, most potent compound was selected for cell apoptosis, immunofluorescence staining and cell cycle analysis. After that, CD73 mRNA and protein expression were analyzed by real-time PCR and Western blot. Results: Among all compounds, 3h, 3e, 3b, and 3c were found the most active against rat-ecto-5′-NT (CD73) enzyme with IC50 (µM) values of 0.70 ± 0.06 µM, 0.87 ± 0.05 µM, 0.39 ± 0.02 µM and 0.33 ± 0.03 µM, respectively. These derivatives were further evaluated for their cytotoxic potential against cancer cell line (HeLa). Compound 3h and 3c showed the cytotoxicity at IC50 value of 30.20 ± 3.11 µM and 86.02 ± 7.11 µM, respectively. Furthermore, compound 3h was selected for cell apoptosis, immunofluorescence staining and cell cycle analysis which showed promising apoptotic effect in HeLa cells. Additionally, compound 3h was further investigated for its effect on expression of CD73 using qRT-PCR and western blot. Conclusion: Among all synthesized compounds (3a-3i), Compound 3h (E)-N'-((6-ethyl-4-oxo-4H-chromen-3-yl) methylene)-4-methylbenzenesulfonohydrazide was identified as most potent compound. Additional expression studies conducted on HeLa cell line proved that this compound successfully decreased the expression level of CD73 and thus inhibiting the growth and proliferation of cancer cells.


Author(s):  
Ying Qian ◽  
Yingnian Yu ◽  
Xingruo Cheng ◽  
Jianhong Luo ◽  
Haiyang Xie ◽  
...  

RSC Advances ◽  
2017 ◽  
Vol 7 (9) ◽  
pp. 5282-5296 ◽  
Author(s):  
Marija S. Jeremić ◽  
Hubert Wadepohl ◽  
Vesna V. Kojić ◽  
Dimitar S. Jakimov ◽  
Ratomir Jelić ◽  
...  

Two new Rh(iii)–ed3a complexes [Rh(ed3a)(OH2)]·H2O and Na[Rh(ed3a)Cl]·H2O have shown good antitumor activity, especially against HeLa cell line.


2018 ◽  
Author(s):  
◽  
Kola Augustus Oluwafemi

This work focuses on the design, synthesis and evaluation of imine-containing heterocyclic and acyclic compounds with special focus on their bioactivity against parasitic protozoans (P. falciparum and T. brucei) - given the context of drug resistance in the treatment of malaria and Human African sleeping sickness and the fact that several bioactive organic compounds have been reported to possess the imino group. Starting from 2-aminopyridine, novel #-alkylated-5-bromo-7-azabenzimidazoles and substituted 5-bromo-1-(carbamoylmethy)-7-azabenzimidazole derivatives were prepared, and their bioactivity against parasitic protozoans was assessed. NMR spectra of the substituted 5- bromo-1-(carbamoylmethy)-7-azabenzimidazole derivatives exhibited rotational isomerism, and a dynamic NMR study was used in the estimation of the rate constants and the free- energies of activation for rotation. The free-energy differences between the two rotamers were determined and the more stable conformations were predicted. Novel 2-phenyl-7-azabenzimidazoles were also synthesised from 2-aminopyridine. A convenient method for the regioselective formylation of 2,3-diaminopyridines into 2-amino- 7-(benzylimino)pyridine analogues of 2-phenyl-7-azabenzimidazole was developed, and some of the resulting imino derivatives were hydrogenated to verify the importance of the imino moiety for bioactivity. The 2-phenyl-7-azabenzimidazoles and the 2-amino-7- (benzylimino)pyridine analogues were screened for their anti-protozoal activity and their cytotoxicity level was determined against the HeLa cell line. In order to validate the importance of the pyridine moiety, novel #-(phenyl)-2- hydroxybenzylimines, #-(benzyl)-2-hydroxybenzylimines and (±)-trans-1,2-bis[2- hydroxybenzylimino]cyclohexanes were also synthesized and screened for activity against the parasitic protozoans and for cytotoxicity against the HeLa cell line. The biological assay results indicated that these compounds are not significantly cytotoxic and a good number of them show potential as lead compounds for the development of new malaria and trypanosomiasis drugs.


2016 ◽  
Vol 27 (suppl_9) ◽  
Author(s):  
A. Fani-Pakdel ◽  
S.H. Forouzmand ◽  
S.H. Mousavi ◽  
V. Vazifedan ◽  
M. Nourbakhsh ◽  
...  

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