Evaluating cytotoxic effect of  the extracted compounds from Ehretia asperula Zoll. & Mor stem on several cancer cell lines

This paper reports the cytotoxic effect on several cancer cell lines of the stem extracts and of some isolated compounds from Ehretia asperula. All the extracts exhibited cytotoxic effects on at least one cancer cell line. The n-hexane extract showed potent cytotoxic activity on Hep-G2, MCF-7 and HeLa cell lines with IC50 values of 28.3 g/ml, 14.42 g/ml and 18.59 g/ml, respectively, while the methanolic, ethyl acetate and water extracts exhibited toxicity towards MCF-7 cells with IC50 values of 16.45 g/ml, 13.4 g/ml and 39.78 g/ml, respectively. 06 compounds have been isolated from the ethyl acetate fraction of Ehretia asperula stem. Methyl caffeate has a strong cytotoxicity against Hep-G2, HeLa and MCF-7 cancer cell lines with IC50 values of 2.83 g/ml, 3.38 g/ml and 4.4 g/ml, respectively. Oresbiusin B was active against Hep-G2 with IC50 value of 9.89 g/ml. The other compounds including coniferaldehyde, 9′-methoxydehydrodiconiferyl alcohol and vanillic acid did not have any cytotoxic effect on the tested cancer cell lines. So, the obtained results have suggested possibility of using the potential Ehretia asperula extracts as health food for preventing and curing cancer diseases. Keywords: Ehretia asperula, methyl caffeate, oresbiusin B, Cancer cell lines. Citation: Vu Thi Nguyet, Nguyen Tien Đat, Le Mai Huong, Tran Thi Hong Ha, Nguyen Hong Chuyen, Nguyen Thi Hang4, Đang Đinh Kim, 2018. Evaluating cytotoxic effect of the extracted compounds from ehretia asperula zoll. & mor stem on several cancer cell lines.Tap chi Sinh hoc, 40(2): 145153. https://doi.org/10.15625/0866-7160/v40n2.12955. *Corresponding author: [email protected]

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NEW QUINAZOLINONE DERIVATIVES: SYTHESIS AND IN VITRO CYTOTOXIC ACTIVITY

Vietnam Journal of Science and Technology ◽

10.15625/2525-2518/58/1/14391 ◽

2020 ◽

Vol 58 (1) ◽

pp. 12

Author(s):

Tran Khac Vu

Keyword(s):

Cytotoxic Activity ◽

Cell Lines ◽

Cancer Cell ◽

Cytotoxic Effect ◽

Cancer Cell Lines ◽

Ic50 Values ◽

Quinazolinone Derivatives ◽

Bioassay Result ◽

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The paper presents a simple synthesis of new quinazolinone derivatives 13a-i. Synthesized derivatives were tested for their cytotoxic effect against three cancer cell lines including SKLU-1, MCF-7 and HepG-2. The bioassay result showed that only compound 13e exhibited significant cytotoxic effect against cancer cell lines tested with IC50 values of 9.48, 20.39 and 18.04 µg/ mL, respectively.

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A New Pyrrolidone Alkaloid and Other Constituents from Rourea oligophlebia Stems

Journal of Chemistry ◽

10.1155/2021/6659106 ◽

2021 ◽

Vol 2021 ◽

pp. 1-5

Author(s):

Thuc Ngoc Dinh ◽

Mai Vu Thi Ha ◽

Luong Ngo Xuan ◽

Huan Trinh Thi ◽

Huong Nguyen Thi ◽

...

Keyword(s):

Antimicrobial Activity ◽

Cell Lines ◽

Cancer Cell ◽

Protocatechuic Acid ◽

Cancer Cell Lines ◽

Coniferyl Alcohol ◽

Hep G2 ◽

Phytochemical Study ◽

Ic50 Values ◽

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Phytochemical study of Rourea oligophlebia stems led to the isolation of a new 2-pyrrolidone alkaloid (R,S)-N-(5-hydroxyl-pyrrolidin-2-one-1-yl)acetamide (1), together with 14 known compounds including friedelin (2), friedanol (3), taraxerol (4), vanillin (5), coniferyl aldehyde (6), apigenin (7), 7α-hydroxy-3β-sitosterol (8), coniferyl alcohol (9), scopoletin (10), emodin (11), protocatechuic acid (12), catechin (13), procyanidin A1 (14), and (E)-2,3,5,4’-tetrahydroxystilbene-2-β-D-glucoside (15). Several isolated compounds were evaluated for cytotoxicity and antimicrobial activity. Compound 11 exhibited good antimicrobial activity on Gram (+) strains and moderate cytotoxicity against KB, Hep-G2, and LU cancer cell lines. Compounds 6 and 8–10 showed selective activity on HepG-2 and MCF-7 over KB and LU cancer cell lines, while compound 7 exhibited similar effects on KB, HepG-2, and MCF-7 cell lines with IC50 values of 36.46 ± 0.81, 32.00 ± 0.58, and 32.03 ± 0.61 µg/mL, respectively.

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Cytotoxic effect of γ-sitosterol from Kejibeling (Strobilanthes crispus) and its mechanism of action towards c-myc gene expression and apoptotic pathway

Medical Journal of Indonesia ◽

10.13181/mji.v23i4.1085 ◽

2015 ◽

Vol 23 (4) ◽

pp. 203-8 ◽

Cited By ~ 11

Author(s):

Susi Endrini ◽

Asmah Rahmat ◽

Patimah Ismail ◽

Y.H. Taufiq-Yap

Keyword(s):

Cell Lines ◽

Cancer Cell ◽

Cytotoxic Effect ◽

Cancer Cell Lines ◽

Liver Cancer Cell ◽

Apoptotic Pathway ◽

Strobilanthes Crispus ◽

Ic50 Values ◽

Chang Liver ◽

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Background: This study aimed to analyze the cytotoxicity effect of γ-sitosterol isolated from “Kejibeling” (Strobilanthes crispus), a medicinal plant, on several cancer cell lines. The mechanisms of the effects were studied through the expression of cancer-caused gene, c-myc and apoptotic pathways.Methods: This in vitro study was done using human colon cancer cell lines (Caco-2), liver cancer cell lines (HepG2), hormone-dependent breast cancer cell lines (MCF-7) and the normal liver cell lines (Chang Liver). The cytotoxic effect was measured through MTT assay and the potential cytotoxic value was calculated by determining the toxic concentration which may kill up to 50% of the total cell used (IC50). Meanwhile, the cytotoxic mechanism was studied by determining the effect of adding γ-sitosterol to the c-myc gene expression by reverse transciptase-polymerase chain reaction (RT-PCR). The effect of γ-sitosterol through apoptotic pathway was studied by using terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL) assay.Results: γ-sitosterol was cytotoxic against Caco-2, HepG2, and MCF-7 with IC50-values of 8.3, 21.8, and 28.8 μg/mL, respectively. There were no IC50-values obtained from this compound against Chang Liver cell line. This compound induced apotosis on Caco-2 and HepG2 cell lines and suppressed the c-myc genes expression in both cells.Conclusion: γ-sitosterol was cytotoxic against colon and liver cancer cell lines and the effect was mediated by down-regulation of c-myc expression and induction of the apoptotic pathways.

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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 ◽

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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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Design, Synthesis, and Antitumor Activity of Olmutinib Derivatives Containing Acrylamide Moiety

Molecules ◽

10.3390/molecules26103041 ◽

2021 ◽

Vol 26 (10) ◽

pp. 3041

Author(s):

Xiaohan Hu ◽

Sheng Tang ◽

Feiyi Yang ◽

Pengwu Zheng ◽

Shan Xu ◽

...

Keyword(s):

Antitumor Activity ◽

Cell Lines ◽

Cancer Cell ◽

Antitumor Agents ◽

Cancer Cell Lines ◽

Design Synthesis ◽

Structure Activity ◽

Excellent Activity ◽

Ic50 Values ◽

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Two series of olmutinib derivatives containing an acrylamide moiety were designed and synthesized, and their IC50 values against cancer cell lines (A549, H1975, NCI-H460, LO2, and MCF-7) were evaluated. Most of the compounds exhibited moderate cytotoxic activity against the five cancer cell lines. The most promising compound, H10, showed not only excellent activity against EGFR kinase but also positive biological activity against PI3K kinase. The structure–activity relationship (SAR) suggested that the introduction of dimethylamine scaffolds with smaller spatial structures was more favorable for antitumor activity. Additionally, the substitution of different acrylamide side chains had different effects on the activity of compounds. Generally, compounds H7 and H10 were confirmed as promising antitumor agents.

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The Effect of Fatty Acids on Ciprofloxacin Cytotoxic Activity in Prostate Cancer Cell Lines. Does Lipid Component Enhance Anticancer Ciprofloxacin Potential?

Cancers ◽

10.3390/cancers14020409 ◽

2022 ◽

Vol 14 (2) ◽

pp. 409

Author(s):

Alicja Chrzanowska ◽

Wioletta Olejarz ◽

Grażyna Kubiak-Tomaszewska ◽

Andrzej K. Ciechanowicz ◽

Marta Struga

Keyword(s):

Prostate Cancer ◽

Fatty Acids ◽

Cell Lines ◽

Cancer Cell ◽

Cytotoxic Effect ◽

Cancer Cell Lines ◽

Lncap Cells ◽

Ic50 Values ◽

Late Apoptosis ◽

Pc3 Cells

Purpose: To assess cytotoxic effect of ciprofloxacin conjugates with fatty acids on prostate cancer cells (LNCaP and DU-145) with different hormone sensitivity, based on previous promising results from the PC3 cells. Methods: Cytotoxicity were estimated using MTT and LDH tests, whereas its mechanisms were estimated by apoptosis and IL-6 assays. The intensity of proteins involved in lipid metabolism was determined using ML-CS assay. Results: The hormone insensitive DU-145 cells were more vulnerable than the hormone sensitive LNCaP cells. The IC50 values for oleic (4), elaidic (5) and docosahexaenoic acid (8) conjugates were 20.2 µM, 17.8 µM and 16.5 µM, respectively, in DU-145 cells, whereas in LNCaP cells IC50 exceeded 20 µM. The strong conjugate cytotoxicity was confirmed in the LDH test, the highest (70.8%) for compound (5) and 64.2% for compound (8) in DU-145 cells. This effect was weaker for LNCaP cells (around 60%). The cytotoxic effect of unconjugated ciprofloxacin and fatty acids was weaker. The early apoptosis was predominant in LNCaP while in DU-145 cells both early and late apoptosis was induced. The tested conjugates decreased IL-6 release in both cancer cell lines by almost 50%. Proteomic analysis indicated influence of the ciprofloxacin conjugates on lipid metabolic proteins in prostatic cancer. Conclusion: Our findings suggested the cytotoxic potential of ciprofloxacin conjugates with reduction in proteins involved in prostate cancer progress.

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Cytotoxic Sterols from Philippine Mushrooms

Asian Journal of Chemistry ◽

10.14233/ajchem.2020.22591 ◽

2020 ◽

Vol 32 (5) ◽

pp. 1197-1202

Author(s):

Consolacion Y. Ragasa ◽

Glenn G. Oyong ◽

Maria Carmen S. Tan ◽

Mariquit M. De Los Reyes ◽

Maria Ellenita G. De Castro

Keyword(s):

Cell Lines ◽

Cancer Cell ◽

Human Cancer ◽

Dermal Fibroblast ◽

Cancer Cell Lines ◽

Cytotoxic Activities ◽

Cell Viability Assay ◽

Ic50 Values ◽

Ht 29 ◽

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Ergosterol peroxide (1) and ergosterol (2) were commonly isolated as the major compounds of Philippine mushrooms. Sterols 1 and 2 from the dichloromethane extract of Geastrum triplex and Termitomyces clypeatus, respectively, were evaluated for their cytotoxic activities against four human cancer cell lines, viz., breast cancer (MCF-7), colon cancer (HT-29), leukemia (THP-1), and small lung cell carcinoma (H69PR), and a human normal cell line, human dermal fibroblast-neonatal (HDFn), using the PrestoBlue® cell viability assay. Compounds 1 and 2 exhibited the strongest activities against HT-29 with IC50 values of 1.79 and 2.98 μg/mL, respectively, while Zeocin gave an IC50 of 4.89 μg/mL. These compounds also exhibited strong antiproliferative effects against MCF-7 with IC50 values of 4.13 for 1 and 4.20 μg/mL for compound 2, comparable to Zeocin with IC50 = 3.68 μg/mL. Only moderate cytotoxicity resulted when compounds 1 and 2 were tested against H69PR with IC50 values of 7.78 and 6.83 μg/mL, respectively, while Zeocin exhibited an IC50 of 9.81 μg/mL. Furthermore, compounds 1 and 2 showed no effects against THP-1 (IC50 > 100 μg/mL), while Zeocin showed an IC50 of 4.73 μg/mL. Although compounds 1 and 2 have been reported to exhibit different bioactivities in previous studies, the cancer cell lines tested and/or the polarities of the solvents for extraction varied. Therefore, comparisons of the cytotoxic activities of compounds 1 and 2 with earlier studies could not be made extensively.

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