scholarly journals EVALUATION OF IN VITRO ANTICANCER ACTIVITY OF AERIAL PARTS OF AVICENNIA ALBA PLANT METHANOLIC EXTRACT AGAINST HELA AND MCF-7 CELL LINES

2021 ◽  
pp. 73-79
Author(s):  
RA ZERUBABEL MICHAEL
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Mtt Assay ◽  
Methanolic Extract ◽  
Inhibitory Effect ◽  
Mangrove Plant ◽  
Standard Drug ◽  
Ic50 Values ◽  
Avicennia Alba ◽  
Mcf 7

Objective: The current study emphasizes the effects of stem and leaf methanolic extract of mangrove plant Avicennia alba on human tumor cell lines HeLa and MCF-7. Method: The collected mangrove plant sample was subjected to extraction with methanol and screened for anticancer activity according to 3-(4,5-dimethythiazol- 2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay method. The ability of the plant extract to inhibit the proliferation of HeLa and MCF-7 cell lines procured from NCCS Pune was compared parallel to inhibitory effect of standard drug Cisplatin. The spectrophotometric optical densities obtained were plotted on graph and consecutive data were obtained to depict the inhibitory effect and IC50 values. The histopathology studies were also done for a clear insight to understand the depth of inhibition microscopically. Results: The MTT assay performed illustrates the plant samples with different concentrations (10, 20, 25, 30, and 50 μg) showed significant inhibitory effect on comparison with the standard drug Cisplatin. The IC50 values and the inhibitory OD values elucidate effective projection of plant as a potential source of anticancer activity based on comparative study. The histopathology studies revealed an insight to a clearer picture of how the cells growth was controlled. It was found that the methanolic extract of A. alba exhibited more activity against HeLa cell lines than MCF-7 cell lines. Conclusion: The synergistic effect of various phytochemicals present in the methanolic plant extract played a significant role in establishing the plant as a significant anticancer source.

Synthesis, In Silico and In Vivo Evaluation of Novel 1, 3, 4-Thiadiazole Analogues as Novel Anticancer Agents

2020 ◽  
Vol 17 (4) ◽  
pp. 434-444 ◽  
Author(s):  
Swathi Krishna ◽  
Byran Gowramma ◽  
Manal Mohammed ◽  
Rajagopal Kalirajan ◽  
Lakshman Kaviarasan ◽  
...  
Keyword(s):  
Vero Cell ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Binding Interaction ◽  
Standard Drug ◽  
Discovery Studio ◽  
Vero Cell Lines ◽  
Mcf 7

Background: 1,3,4-thiadiazole is a lead molécule which is versatile for a wide variety of biological activities and in continuation of our interest in establishing some novel heterocyclic compounds for antitumor activity. Objective: The objective of the study was to synthesize series of 5-(1,3-benzodioxol-5-yl)-1,3,4- thiadiazol-2-amine derivative and evaluated for their possible in vitro and in vivo anticancer activity. Methods: The synthesis of 2-aminonaphthoxy-1,3,4-thiadiazole and 5-(1,3-benzodioxol-5-yl)-1,3,4- thiadiazol-2-amine as intermediates were carried out by cyclization method. A mixture of thiosemicarbazide and naphthoxyacetic acid/piperonylic acid and phosphoryl chloride were subjected to cyclization with phosphorous oxychloride to obtain compound 3. Further compounds 1 and 3 were reacted with different aromatic aldehydes in methanol to form compounds 2a-e and 4a-e. The compounds 2a-e and 4a-e were characterized for the melting points, IR, Proton NMR and Mass spectra. The compounds were further evaluated for their anticancer activity. The docking study was performed using Discovery studio 4.1 (Accelrys) software against DNA-binding domain of STAT3. The compounds were analyzed for the ligand-protein binding interaction(s) by molecular docking into the active site of STAT3β using the CDOCKER protocol of Discovery studio (v4.1). Results: The title compounds were screened for in vitro anticancer on human breastadenocarcinoma cells (MCF-7 and Vero). Compounds 4c, 4d and 2d against MCF 7 and 4d against Vero cell lines were found to be the most active dérivatives with IC50 values of 1.03, 2.81 and 3.45 µg/ml against MCF 7 and 31.81 µg/ml against Vero cell lines, respectively. Conclusion: From the in vivo anticancer studies, it was concluded that the synthesized compounds 4c and 4d displayed anticancer activity comparable to the standard drug, while the rest of the compounds demonstrated mild potency for anticancer studies.

Synthesis and Biological Evaluation of New Quinoline-Based Thiazolyl Hydrazone Derivatives as Potent Antifungal and Anticancer Agents

2018 ◽  
Vol 15 (2) ◽  
pp. 193-202 ◽  
Author(s):  
Ali Erguc ◽  
Mehlika Dilek Altintop ◽  
Ozlem Atli ◽  
Belgin Sever ◽  
Gokalp Iscan ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Mtt Assay ◽  
Anticancer Agents ◽  
Mouse Embryonic Fibroblast ◽  
Biological Evaluation ◽  
Diffusion Method ◽  
Breast Adenocarcinoma ◽  
Nih 3T3 ◽  
Mcf 7

Background: In medicinal chemistry, thiazoles have gained great importance in antifungal and anticancer drug design and development. Objectives: The aim of this study was to synthesize new quinoline-based thiazolyl hydrazone derivatives and evaluate their anticandidal and anticancer effects. Methods: New thiazolyl hydrazone derivatives were evaluated for their anticandidal effects using disc diffusion method. Ames MPF assay was carried out to determine the genotoxicity of the most effective antifungal derivative. MTT assay was also performed to assess the cytotoxic effects of the compounds on A549 human lung adenocarcinoma, HepG2 human hepatocellular carcinoma, MCF- 7 human breast adenocarcinoma and NIH/3T3 mouse embryonic fibroblast (healthy) cell lines. Methods: Results: 4-(4-Fluorophenyl)-2-(2-((quinolin-4-yl)methylene)hydrazinyl)thiazole (4) showed antifungal activity against Candida albicans and Candida krusei in the concentration of 1 mg/mL. In MTT and Ames MPF tests, it was determined that compound 4 did not show cytotoxic and genotoxic effects. MTT assay indicated that 4-(naphthalen-2-yl)-2-(2-((quinolin-4-yl)methylene) hydrazinyl)thiazole (10) showed more selective anticancer activity than cisplatin against A549 and MCF-7 cell lines. Besides, 4-(4-chlorophenyl)-2-(2-((quinolin-4-yl)methylene)hydrazinyl)thiazole (5) exhibited more selective anticancer activity than cisplatin against HepG2 cell line. Conclusion: Due to their high selectivity index, these compounds are considered as candidate compounds to participate in further research.

Design, Synthesis of novel coumarin conjugated acetamides as promising anticancer agents: An in-silico and in-vitro approach.

2020 ◽  
Vol 20 ◽  
Author(s):  
Mamatha S. V ◽  
S. L. Belagali ◽  
Mahesh Bhat ◽  
Vijay M. Kumbar
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Mtt Assay ◽  
Anticancer Agents ◽  
In Silico ◽  
Active Sites ◽  
Biological Activities ◽  
Biological Evaluation ◽  
Mcf 7

Background: Coumarin and benzophenone possess a vast sphere of biological activities whereas thiazoles display various pharmacological properties. Hence we focused on incorporation of coumarin and thiazole core to the benzophenone skeleton to enhance the bioactivity anticipating their interesting biological properties. Objective: The objective of the current work is synthesis and biological evaluation of a novel series of coumarin fused thiazole derivatives. Methods: A novel series of Coumarin conjugated thiazolyl acetamide hybrid derivatives were synthesized by multistep reaction sequence and were characterized by the FT-IR, LCMS and NMR spectral techniques. The newly synthesized compounds were screened for anticancer activity by in-silico and in-vitro methods. The cytotoxicity of the synthesized unique compounds had been executed for two different cancer cell lines MCF-7 (Breast cancer) and KB (Oral cancer) in comparison with standard paclitaxel by MTT assay. Results: The compound 7f is the potent motif with an acceptable range of IC 50 values for anticancer activity were 63.54 µg/ml and 55.67 µg/ml, against the MCF-7 and KB cell lines, respectively. Molecule docking model revealed that this compound formed three conventional hydrogen bonds with the active sites of the amino acids MET 769, ARG 817 and LYS 721. Conclusion: Compound 7f with two methyl groups on the phenoxy ring and one 4-position methoxy group on the benzoyl ring, showed a significant cytotoxic effect. An advantageous level of low toxicity against normal cell line (L292) by MTT assay was determined.

Evaluation of biological activities of Barbarea integrifolia and isolation of a new glucosinolate derivated compound

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Merve Badem ◽  
Sıla Ozlem Sener ◽  
Seyda Kanbolat ◽  
Nuriye Korkmaz ◽  
Sermet Yildirmiş ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Total Phenolic Content ◽  
Phenolic Content ◽  
Methanolic Extract ◽  
Biological Activities ◽  
Total Phenolic ◽  
Chloroform Fraction ◽  
Aqueous Fraction ◽  
Mcf 7

Abstract The aim of the present study is to determine the potent biological activities and carry out isolation studies on Barbarea integrifolia. The antioxidant capacity of the species was evaluated by total phenolic content, FRAP, CUPRAC, and DPPH radical scavenging activity. Anticancer activity studies were performed by MTT assay in MDA-MB-231, MCF-7, Hep3B, PC-3, A549, HCT116, L-929 cell lines. It was observed that the remaining aqueous fraction has higher total phenolic content while higher activity in the CUPRAC and FRAP assays was displayed for the methanolic extract and chloroform fraction. The extracts showed anticancer activity as compared with vincristine. It was observed that chloroform fraction has the highest anticancer activity on MCF-7 cell line, while ethyl acetate fraction has the highest anticancer activity on Hep-3B and A549 cell lines. Methanolic extract has the highest anticancer activity on HCT116 and MDA-MB-23 cell lines. The isolation studies have been performed using several chromatographic methods. The chemical structures of compounds have been identified by means of 1H NMR, 13C NMR, 2D-NMR, and MS. Five major compounds, one steroid (β-Sitosterol), one phenolic acid (Rosmarinic acid), one flavonol heteroside (kaempferol 7-O-α-l-rhamnoside-3-O-β-d-(2-O-β- d -glucosyl)-β-d-glucoside), and two glucosinolates (Gluconasturtiin, Gluconasturtiin choline salt) have been isolated.

scholarly journals SYNTHESIS, CHARACTERIZATION, AND ANTICANCER ACTIVITY OF SOME NOVEL ACRIDINE DERIVATIVES

2020 ◽  
pp. 166-169
Author(s):  
SWETHA PADIGELA ◽  
BHAGAVAN RAJU RM ◽  
RAJENDRA PRASAD VVS
Keyword(s):  
Spectral Analysis ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Mtt Assay ◽  
Chloroacetyl Chloride ◽  
Mass Spectral Analysis ◽  
Mass Spectral ◽  
Acridine Derivatives ◽  
Mcf 7

Objective: The objective of the study was to synthesize and evaluate the anticancer activity of some novel acridine derivatives. Methods: The present works involve condensation of acridine and various 2, 4-Thiazolidine-2,4-dione derivatives (2a–2h) with chloroacetyl chloride to give a novel acridine derivatives (5a–5l), respectively. Results: All the newly synthesized molecules (5a–5l) were characterized by FTIR, H1-NMR, and mass spectral analysis along with physical data. The biological potentials of the new synthesized compounds are evaluated for their in vitro anticancer activity by MTT assay. Conclusion: The synthesized compounds 5a, 5f, and 5h exhibited good anticancer activity against MCF-7 and SKVO3 cancer cell lines at a concentration of 0.5 mg/mL-1.

scholarly journals Design, Synthesis and in vitro Anticancer Evaluation of New 2H-benzo[b][1,4]thiazin-3(4H)-one Based 1,2,3-Triazoles

2019 ◽  
Vol 31 (11) ◽  
pp. 2647-2652 ◽  
Author(s):  
O. Rajender ◽  
S. Narsimha ◽  
N. Vasudeva Reddy
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Broad Spectrum ◽  
Moderate Activity ◽  
Design Synthesis ◽  
Triazole Derivatives ◽  
Cuaac Reaction ◽  
Ic50 Values ◽  
Mcf 7

A series of novel 2H-benzo[b][1,4]thiazin-3(4H)-one derived from 1,4-disubstituted 1,2,3-triazole derivatives (4a-j and 5a-j) were synthesized using Cu(I) catalyzed azide alkyne cyclization (CuAAC) reaction of the compounds 2 and 3 with various aromatic azides. The examination of in vitro anticancer activity revealed that the compounds 4d and 5d were found to possess a broad spectrum of anticancer activity against three cell lines MCF-7, HeLa and IMR-32 with IC50 values ranging from 26.28 ± 1.5 to 32.06 ± 0.3 M mL-1, respectively. The remaining compounds have shown good to moderate activity against the tested cell lines.

scholarly journals The Anticancer Activity of Phytoconstituents of the Stem of Bouea macrophylla

2021 ◽  
Vol 14 (4) ◽  
pp. 1955-1964
Author(s):  
Tarso Rudiana ◽  
Nani Suryani ◽  
Dimas D. Indriatmoko ◽  
Yusransyah Yusransyah ◽  
Muhammad A. Hardiyanto ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cancer Cells ◽  
Cell Line ◽  
Cell Lines ◽  
Metastatic Breast ◽  
Alveolar Epithelial Cells ◽  
Ic50 Values ◽  
Stem Extract ◽  
Mcf 7

Gandaria (Bouea macrophylla Griff) is a typical Asian plant that is commonly found in In-donesia with various secondary metabolite compounds such as phenolic, flavonoid and ter-penoid. The purpose of this study was to isolate secondary metabolites from the stem extract of B. macrophylla and determine their activity against cancer cells MCF-7, A549, MDA-MB 231 and HCC-1954. The isolation of the compounds was conducted using various chromatographic techniques, the determination of the chemical structure of the isolates was performed using physicochemical methods including mass spectrometer and nuclear magnetic resonance, the determination of anticancer activity was carried out using 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium (MTS) i.e. MCF-7 and A549 cell lines; and dimetiltiazol-2-il) -2,5-diphenyltetrazolium bromide (MTT) for MDA-MB 231 and HCC-1954 cell lines. Four compounds namely stigmasterol (1), fustin (2), garbanzol (3) and methyl galat (4) were successfully isolated from the stem extract of B. macrophylla, which was obtained from Serang Regency, Indonesia. These compounds were then tested their anticancer activity against the cancer cells of Michigan Cancer Foundation-7 (MCF-7), human alveolar epithelial cells (A549), human breast cancer cell line-1954 (HCC-1954) and M.D. Anderson-Metastatic Breast-231 (MDA-MB-231). The results of anticancer test indicated that based on the IC50 values for all compounds tested, the compounds 2 and 4 were more active on HCC-1954 cell with IC50 values of 134.35 ± 44.62 and 153.69 ± 12.54 µg/mL, respectively, while the compound 3 was found to be the most active against MDA-MB-231 cell line with IC50 value of 233.41 ± 91.57 µg/mL

scholarly journals The influence of a single and double biotinylation of xanthohumol on its anticancer activity

2019 ◽  
Author(s):  
Monika Stompor ◽  
Marta Świtalska ◽  
Joanna Wietrzyk
Keyword(s):  
Breast Cancer ◽  
Anticancer Activity ◽  
Cancer Cells ◽  
Cell Lines ◽  
Growth Inhibitor ◽  
Breast Cancer Cell Lines ◽  
Active Growth ◽  
Ic50 Values ◽  
4T1 Breast Cancer ◽  
Mcf 7

Two biotinylated derivatives of the main hop chalcone xanthohumol (1) were prepared by a one-step synthesis via esterification using biotin and 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (EDC×HCl) and 4-dimethylaminopyridine (DMAP) as coupling reagents. The products were characterized spectroscopically and their antiproliferative activity toward MCF-7, MCF-10A, HepG2, MDA-MB-231, 4T1 and Balb/3T3 cell lines was investigated using the SRB assay. For all three tested compounds the best activity was noted in the case of human (MCF-7) and mice (4T1) breast cancer cell lines (IC50 values < 9 μM). Both biotinylated derivatives showed slightly higher anticancer activity than xanthohumol (1) towards all types of tested breast cancer cells. Double biotinylated xanthohumol (3) proved to be the most active in inhibiting cell growth, with IC50 values equal to 5.35 ± 1.5 μM for 4T1 and 8.03 ± 0.53 µM for MCF-7 cell lines. Compound 3 was also more active than 1 and 2 against liver cancer cells HepG2 (IC50 = 17.37 ± 5.1 μM), while the IC50 values for 1 and 2 were equal to 21.5 ± 2.7 and 22.1 ± 3.9 µM, respectively. 4‑O‑biotinylxanthohumol (2) was the second most active growth inhibitor, particularly with respect to MCF-7 (IC50 = 6.19 ± 1.7 μM) and 4T1 (IC50 = 6.64 ± 0.4 μM) cell lines. Our preliminary study on biotinylated xanthohumol (1) have shown that this type of functionalization is an effective method for the production of active biomolecules and study on this area should be continued thereby extending their applications.

Isolation of New Glycosides from Anemarrhena Asphodeloides Rhizome and Screening of their Anticancer Activity

2019 ◽  
Vol 16 (6) ◽  
pp. 474-477 ◽  
Author(s):  
Pham Van Khang ◽  
Nguyen Thi Hien Lan ◽  
Le Quang Truong ◽  
Mai Thi Minh Chau ◽  
Mai Xuan Truong ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Spectral Data ◽  
Cell Lines ◽  
Cancer Cell ◽  
Spectroscopic Analysis ◽  
2D Nmr ◽  
Ic50 Values ◽  
Nmr Techniques ◽  
Inhibitory Activities ◽  
Anemarrhena Asphodeloides

In this report, two new steroidal glycosides were isolated and determined from n-butanol fraction of A.asphodeloides. The structures were confirmed in comparison with the spectral data of known compounds by using different spectroscopic analysis approaches including 1D & 2D-NMR techniques and HRMS. The anti-proliferation screening against cancer cell lines A549 and HeLa indicated that compound 1 exhibited good inhibitory activities with IC50 values of 0.79 and 0.55 &#181;g/mL, respectively.

(Substituted)-benzo[b]thiophene-4-carboxamide Synthesis and Antiproliferative Activity Study

2020 ◽  
Vol 17 (5) ◽  
pp. 563-573 ◽  
Author(s):  
Chandrakant Dhondiram Pawar ◽  
Dattatraya Navnath Pansare ◽  
Devanand Baburao Shinde
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Proliferative Activity ◽  
Thiophene Ring ◽  
Amide Group ◽  
Peptide Coupling ◽  
Ic50 Value ◽  
Important Building Block ◽  
Mcf 7

Background: Thiophene ring forms important building block in medicinal chemistry. Literature reveals that thiophene ring in combination with different groups shows different activity. By keeping these things in mind we have designed and synthesized a new series of amide and sulfonamide coupled thiophene. A series of novel substituted 3-sulfamoylbenzo[b]thiophene-4- carboxamide molecules containing sulfonamide and amide group were designed, synthesized and used for anti-proliferative activity study. Methods: The final compounds 16-36 were synthesized by using series of reactions comprising sulfonation, sulfonamide coupling, hydrolysis and peptide coupling. The yields of compounds 16- 36 are in the range of 90-98%. The structures of the synthesized compounds were elucidated and confirmed by 1H NMR, 13C NMR, LCMS and the purity was checked through HPLC analysis. The compounds were further tested for their in vitro anticancer activity against a series of cell lines A549, HeLa, MCF-7 and Du-145. Results: The intermediates 8-13, 15 and final compounds 16-36 were synthesized in good yields. The synthesized compounds were further tested for their anticancer activity and most of compounds showed moderate to good anticancer activity against all four cell lines. Conclusion: We have synthesized 21 compounds and were screened for anticancer activity against MCF-7, HeLa, A-549 and Du-145 cancer cell lines. Most of the compounds were active for tested cell lines with IC50 value in the range of 1.81 to 9.73 μM. The compounds 18, 19, 21, 25, 30, 31 and 33 are most active in cell line data with IC50 value in the range of 1.81 to 2.52 μM.

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