In vitro cytotoxic potential of Yacon (Smallanthus sonchifolius) against HT-29, MCF-7 and HDFn cell lines

Extracts from natural products, especially microorganisms, have served as a valuable source of diverse molecules in many drug discovery efforts and led to the discovery of several important drugs. Identification of microbial strains having promising biological activities and purifying the bio-molecules responsible for the activities, have led to the discovery of many bioactive molecules. Extracellular, as well as intracellular, extracts of the metabolites of thirty-six bacterial and twenty-four fungal isolates, grown under unusual conditions such as high temperature, high salt and low sugar concentrations, were in vitro tested for their cytotoxic potential on various cancer cell lines. The extracts were screened on HeLa and MCF-7 cell lines to study the cytotoxic potential. Nuclear staining and flow cytometric studies were carried out to assess the potential of the extracts in arresting the cell cycle. The crude ethylacetate extract of isolate F-21 showed promising results by MTT assay with IC50 as low as 20.37±0.36 µg/mL on HeLa, and 44.75±0.81 µg/mL on MCF-7 cells, comparable with Cisplatin. The isolate F-21 was identified as Aspergillus sp. Promising results were also obtained with B-2C and B-4E strains. Morphological studies, biochemical tests and preliminary chemical investigation of the extracts were also carried out.

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Cytotoxic potential of ethanol extract of Parquetina nigrescens on MCF-7, C4-2WT, HT 29 and HTC 116 cell lines

African Journal of Pharmacy and Pharmacology ◽

10.5897/ajpp2018.4947 ◽

2018 ◽

Vol 12 (23) ◽

pp. 310-318

Author(s):

M. Onyegeme-Okerenta Blessing ◽

Agyare Christian ◽

D. Bradshaw Tracey ◽

A. Spriggs Keith

Keyword(s):

Cell Lines ◽

Ethanol Extract ◽

Cytotoxic Potential ◽

Ht 29 ◽

Mcf 7

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Proanthocyanidins reduce cellular function in the most globally diagnosed cancers in vitro

PeerJ ◽

10.7717/peerj.9910 ◽

2020 ◽

Vol 8 ◽

pp. e9910

Author(s):

Sarah Albogami

Keyword(s):

Cell Lines ◽

Cancer Cell ◽

Colorimetric Assay ◽

Human Cancer ◽

Cancer Cell Lines ◽

Trypan Blue Exclusion Method ◽

Apoptotic Nucleus ◽

Ht 29 ◽

Mcf 7

Background Growing evidence indicates that proanthocyanidins (PACs) may be effective in treating and preventing various cancers. The fundamental mechanism of PACs inhibiting the proliferation at cellular and molecular levels in most of the cancer types remains unclear. Objective The anticancer efficacy of PACs was investigated in vitro using three human cancer cell lines: human colorectal adenocarcinoma (HT-29), human breast carcinoma (MCF-7), and human prostatic adenocarcinoma (PC-3). Methods Cytotoxicity was evaluated by MTT assay, while cell proliferation was measured by trypan blue exclusion method. Cell migration was measured by wound healing assay, and DAPI staining was used to evaluate apoptotic nucleus morphology. RT-PCR was used to analyze the expression of Bax and Bcl-2, and caspase enzyme activity assay was measured by caspase colorimetric assay. Results PACs could inhibit both cellular viability and proliferation in a concentration- and time-dependent fashion in all investigated cells. Further, all tested cells showed similarly decreased migration after 24- and 48-h PAC treatment. We observed increased apoptotic nucleus morphology in treated cells (p ≤ 0.01). BAX expression significantly increased in HT-29 (p < 0.01), PC-3(p < 0.01), and MCF-7 (p < 0.05) cells, while BCL-2 expression significantly declined (p < 0.05). Caspase activities were significantly increased in all tested cancer cell lines after 24-h PAC treatment. Conclusion PACs may have potential therapeutic properties against colorectal, breast, and prostate cancer.

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Synthesis and In Vitro Cytotoxic Activity of Chromenopyridones

International Journal of Medicinal Chemistry ◽

10.1155/2013/984329 ◽

2013 ◽

Vol 2013 ◽

pp. 1-7 ◽

Cited By ~ 1

Author(s):

Balwinder Singh ◽

Vishal Sharma ◽

Gagandeep Singh ◽

Rakesh Kumar ◽

Saroj Arora ◽

...

Keyword(s):

Cytotoxic Activity ◽

Cell Lines ◽

Cancer Cell ◽

Human Cancer ◽

Cancer Cell Lines ◽

Hep G2 ◽

Cytotoxic Potential ◽

Human Cancer Cell Lines ◽

Mcf 7

Novel substituted chromenopyridones (3a–j and 6a–d) were synthesized and evaluated in vitro for the cytotoxic activity against various human cancer cell lines such as prostate (PC-3), breast (MCF-7), CNS (IMR-32), cervix (Hela), and liver (Hep-G2). preliminary cytotoxic screening showed that all the compounds possess a good to moderate inhibitory activity against various cancer cell lines. Particularly, compound 6b bearing allyl moiety displayed a significant cytotoxic potential in comparison to standard drugs.

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APRICOXIB

The Professional Medical Journal ◽

10.29309/tpmj/18.4781 ◽

2018 ◽

Vol 25 (12) ◽

pp. 1915-1922

Author(s):

Fatima Rizvi ◽

Syed Mahboob Alam ◽

Farah Asad ◽

Hina Shams

Keyword(s):

Breast Cancer ◽

Cell Line ◽

Cell Lines ◽

Mtt Assay ◽

Cytotoxic Effects ◽

Inflammatory Conditions ◽

Ic50 Value ◽

Ht 29 ◽

Mcf 7

Background: Breast cancer is most frequently diagnosed cancer globally but there is not any ideal economical and safer agent that not only decreases the progression but also resolve complexities associated with breast cancer such as inflammatory conditions. There was strong link between inflammation and cancer specially breast cancer. Thus by inhibiting the COX enzyme may inhibit the progression of cancer beside of its role in inflammatory conditions of breast. Study Design: Interventional In Vitro trial. Setting: Department of Pharmacology in alliance with PCMD. Period: The duration of study from April 2016 to February 2017. Methodology: For this purpose we used five cancerous lines MCF-7, MDA-MB-231, MCF-10, HT-29 and Hela cell lines. For demonstrating the cytotoxic effects of Apricoxib we used MTT assay (for all cell Lines) and Trypan blue dye exclusion assay (Primarily for MCF-7 cell lines). For calculation of minimum dose required for exert cytotoxic effects of Apricoxib and its selectivitytowards cancerous cells of breast tissue we calculated its IC50 value and Selectivity Index (SI) by MTT assay. Results: Apricoxib significantly reduce the viability of MCF-7, MDA-MB-231, Hela, HT-29 as assessed by MTT assay in dose dependent manner (χ2 (2) = 26.483, p<0.001), (χ2 (2) = 26.49, p<0.001), (χ2 (2) = 26.062, p<0.001) and (χ2 (2) = 26.062, p<0.001) respectively. However Apricoxib had non-significant effects on % viability of MCF-10 cell line (χ2 (2) = 4.167, p=0.654) as assessed by MTT assay. Furthermore Apricoxib had lowest IC50 value against MCF-7 cell line. Conclusion: This study demonstrated that beside of primarily anti-inflammatory effects Apricoxib have additional benefits in term of exerting the cytotoxic effects (in vitro) on cancerous cell lines as indicated by reducing the % viability and reducing the Absorbance value of test sample as compare to control. This opens the newer path for researcher to evaluate different aspects of Apricoxib in field of chemotherapy.

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In vitro and in silico studies of the interaction of three tetrazoloquinazoline derivatives with DNA and BSA and their cytotoxicity activities against MCF-7, HT-29 and DPSC cell lines

International Journal of Biological Macromolecules ◽

10.1016/j.ijbiomac.2016.09.113 ◽

2017 ◽

Vol 94 ◽

pp. 85-95 ◽

Cited By ~ 25

Author(s):

Maryam Mohamadi ◽

Asadollah Hassankhani ◽

S. Yousef Ebrahimipour ◽

Masoud Torkzadeh-Mahani

Keyword(s):

Cell Lines ◽

In Silico ◽

In Silico Studies ◽

Cytotoxicity Activities ◽

Ht 29 ◽

Mcf 7

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Evaluation of in vitro cytotoxic activity of different solvent extracts of Clerodendrum thomsoniae Balf.f and its active fractions on different cancer cell lines

Future Journal of Pharmaceutical Sciences ◽

10.1186/s43094-021-00206-6 ◽

2021 ◽

Vol 7 (1) ◽

Author(s):

V. K. Muhammed Ashraf ◽

V. K. Kalaichelvan ◽

V. V. Venkatachalam ◽

R. Ragunathan

Keyword(s):

Cell Lines ◽

Cancer Cell ◽

Cytotoxic Effect ◽

Cancer Cell Lines ◽

Phytochemical Analysis ◽

Hep G2 ◽

Ht 29 ◽

Mcf 7 ◽

Ethyl Acetate Extracts

AbstractBackgroundClerodendrumis a genus of about 500 species belongs to the family Lamiaceae. Many species of this genus have been proved for the treatment of various diseases. This study was aimed to evaluate the cytotoxic effect of different solvents and their most active fractions ofClerodendrum thomsoniaeBalf.f. in different human cancer cell lines. Aerial parts of the plant were subjected to Soxhlet extraction. Phytochemical analysis was done by using standard tests. In vitro anti-cancer activity on MCF-7, Hep-G2, A549, HT-29, MOLT-4, Hela, and Vero cell lines were evaluated by MTT assay.ResultsPhytochemical analysis confirmed the presence of most of the phytoconstituents in ethyl acetate extracts and the same extracts were found to be more cytotoxic activity to cancer cell lines MCF-7,Hep-G2,A549,HT–29, MOLT-4, and Hela with IC50values 29.43 ± 1.44 μg/ml, 43.22 ± 1.02 μg/ml, 56.93 ± 1.41 μg/ml, 60.68 ± 1.05 μg/ml, 69.83 ± 1.33 μg/ml, and 40.02 ± 1.14 μg/ml respectively, while it had no cytotoxic effect on normal Vero cells IC50= 367.5 ± 1.03 μg/ml. Ethyl acetate extracts were selected for the fractionation and MCF-7 cell line was used repeat MTT assay and found that fraction F5 was the most active fraction with IC5017.33 ± 0.54 μg/ml.ConclusionThese findings have proved thatClerodendrum thomsoniaeBalf.f. have significant cytotoxicity especially for breast cancer cell lines. Further studies are required for the isolation of constituents and to explore the mechanism of action.

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

Letters in Drug Design & Discovery ◽

10.2174/1570180815666181004114125 ◽

2020 ◽

Vol 17 (5) ◽

pp. 563-573 ◽

Cited By ~ 2

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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In Vitro Antitumor Evaluation of Some Hybrid Molecules Containing Coumarin and Quinolinone Moieties

Anti-Cancer Agents in Medicinal Chemistry ◽

10.2174/1871520619666190930143856 ◽

2020 ◽

Vol 19 (16) ◽

pp. 2010-2018

Author(s):

Youstina W. Rizzk ◽

Ibrahim M. El-Deen ◽

Faten Z. Mohammed ◽

Moustafa S. Abdelhamid ◽

Amgad I.M. Khedr

Keyword(s):

Cell Cycle ◽

Cell Lines ◽

Cancer Cell ◽

Anticancer Agents ◽

Topoisomerase Ii ◽

Cancer Cell Lines ◽

Bax Protein ◽

Hybrid Molecules ◽

Mcf 7

Background: Hybrid molecules furnished by merging two or more pharmacophores is an emerging concept in the field of medicinal chemistry and drug discovery. Currently, coumarin hybrids have attracted the keen attention of researchers to discover their therapeutic capability against cancer. Objective: The present study aimed to evaluate the in vitro antitumor activity of a new series of hybrid molecules containing coumarin and quinolinone moieties 4 and 5 against four cancer cell lines. Materials and Methods: A new series of hybrid molecules containing coumarin and quinolinone moieties, 4a-c and 5a-c, were synthesized and screened for their cytotoxicity against prostate PC-3, breast MCF-7, colon HCT- 116 and liver HepG2 cancer cell lines as well as normal breast Hs-371 T. Results: All the synthesized compounds were assessed for their in vitro antiproliferative activity against four cancer cell lines and several compounds were found to be active. Further in vitro cell cycle study of compounds 4a and 5a revealed MCF-7 cells arrest at G2 /M phase of the cell cycle profile and induction apoptosis at pre-G1 phase. The apoptosis-inducing activity was evidenced by up-regulation of Bax protein together with the downregulation of the expression of Bcl-2 protein. The mechanism of cytotoxic activity of compounds 4a and 5a correlated to its topoisomerase II inhibitory activity. Conclusion: Hybrid molecules containing coumarin and quinolinone moieties represents a scaffold for further optimization to obtain promising anticancer agents.

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