Synergistic Anticancer Activity of Ornithogalum umbellatum and Ruta graveolens on HCT-116

Abstract In this study, ultrasonically driven biosynthesis of zinc oxide nanoparticles (ZnO NPs) using Swietenia macrophylla seed ethyl acetate fraction (SMEAF) has been reported. X-ray powder diffraction (XRD) and Fourier-transform infrared spectroscopy (FTIR) analyses confirmed the presence of a pure hexagonal wurtzite structure of ZnO. Field emission scanning electron microscope images revealed the formation of uniquely identifiable uniform rice-shaped biologically synthesized ZnOSMEAF particles. The particle sizes of the biosynthesized NPs ranged from 262 to 311 nm. The underlying mechanisms for the biosynthesis of ZnOSMEAF under ultrasound have been proposed based on FTIR and XRD results. The anticancer activity of the as-prepared ZnOSMEAF was investigated against HCT-116 human colon cancer cell lines via methyl thiazolyl tetrazolium assay. ZnOSMEAF exhibited significant anticancer activity against colon cancer cells with higher potency than ZnO particles prepared using the chemical method and SMEAF alone. Exposure of HCT-116 colon cancer cells to ZnOSMEAF promoted a remarkable reduction in cell viability in all the tested concentrations. This study suggests that green sonochemically induced ZnO NPs using medicinal plant extract could be a potential anticancer agent for biomedical applications.

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Phytochemical analysis and anticancer activity of seaweed Eucheuma Sp. against colon HCT-116 cells

10.1063/1.5096719 ◽

2019 ◽

Author(s):

Priscilla Aya Maheswari Subroto ◽

Ade Arsianti ◽

Trivani Putri ◽

Elvira Lesmana

Keyword(s):

Anticancer Activity ◽

Phytochemical Analysis ◽

Hct 116 ◽

Hct 116 Cells

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Synthesis, Anticancer Activity, and Preliminary Pharmacokinetic Evaluation of 4,4-Disubstituted Curcuminoid 2,2-bis(Hydroxymethyl)Propionate Derivatives

Molecules ◽

10.3390/molecules25030479 ◽

2020 ◽

Vol 25 (3) ◽

pp. 479 ◽

Cited By ~ 2

Author(s):

Der-Yen Lee ◽

Yu-Chi Hou ◽

Jai-Sing Yang ◽

Hui-Yi Lin ◽

Tsu-Yuan Chang ◽

...

Keyword(s):

Anticancer Activity ◽

Functional Groups ◽

Hydrolysis Product ◽

Structure Activity Relationship ◽

Ester Hydrolysis ◽

Activity Relationship ◽

Structure Activity ◽

Hct 116 ◽

Pharmacokinetic Evaluation

Compound 1 is a curcumin di-O-2,2-bis(hydroxymethyl)propionate that shows significant in vitro and in vivo inhibitory activity against MDA-MB-231 cells with eight to ten-fold higher potency than curcumin. Here, we modified the α-position (C-4 position) of the central 1,3-diketone moiety of 1 with polar or nonpolar functional groups to afford a series of 4,4-disubstituted curcuminoid 2,2-bis(hydroxymethyl)propionate derivatives and evaluated their anticancer activities. A clear structure–activity relationship of compound 1 derivatives focusing on the functional groups at the C-4 position was established based on their anti-proliferative effects against the MDA-MB-231 and HCT-116 cell lines. Compounds 2–6 are 4,4-dimethylated, 4,4-diethylated, 4,4-dibenzylated, 4,4-dipropargylated and 4,4-diallylated compound 1, respectively. Compounds 2m–6m, the ester hydrolysis products of compounds 2–6, respectively, were synthesized and assessed for anticancer activity. Among all compound 1 derivatives, compound 2 emerged as a potential chemotherapeutic agent for colon cancer due to the promising in vivo anti-proliferative activities of 2 (IC50 = 3.10 ± 0.29 μM) and its ester hydrolysis product 2m (IC50 = 2.17 ± 0.16 μM) against HCT-116. The preliminary pharmacokinetic evaluation of 2 implied that 2 and 2m are main contributors to the in vivo efficacy. Compound 2 was further evaluated in an animal study using HCT-116 colon tumor xenograft bearing nude mice. The results revealed a dose-dependent efficacy that led to tumor volume reductions of 27%, 45%, and 60% at 50, 100, and 150 mg/kg doses, respectively. The established structure–activity relationship and pharmacokinetic outcomes of 2 is the guidance for future development of 4,4-disubstituted curcuminoid 2,2-bis(hydroxymethyl)- propionate derivatives as anticancer drug candidates.

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Effect of Selected Silyl Groups on the Anticancer Activity of 3,4-Dibromo-5-Hydroxy-Furan-2(5H)-one Derivatives

Pharmaceuticals ◽

10.3390/ph14111079 ◽

2021 ◽

Vol 14 (11) ◽

pp. 1079

Author(s):

Radoslaw Kitel ◽

Anna Byczek-Wyrostek ◽

Katarzyna Hopko ◽

Anna Kasprzycka ◽

Krzysztof Walczak

Keyword(s):

Anticancer Activity ◽

Cancer Cells ◽

Systematic Investigation ◽

Silyl Group ◽

Silyl Groups ◽

Clonogenic Potential ◽

Hct 116 ◽

Hct 116 Cells ◽

Silicon Based ◽

The Impact

The pharmacological effects of carbon to silicon bioisosteric replacements have been widely explored in drug design and medicinal chemistry. Here, we present a systematic investigation of the impact of different silyl groups on the anticancer activity of mucobromic acid (MBA) bearing furan-2(5H)-one core. We describe a comprehensive characterization of obtained compounds with respect to their anticancer potency and selectivity towards cancer cells. All four novel compounds exert stronger antiproliferative activity than MBA. Moreover, 3b induce apoptosis in colon cancer cell lines. A detailed investigation of the mechanism of action revealed that 3b activity stems from the down-regulation of survivin and the activation of caspase-3. Furthermore, compound 3b attenuates the clonogenic potential of HCT-116 cells. Interestingly, we also found that depending on the type of the silyl group, compound selectivity towards cancer cells could be precisely controlled. Collectively, we demonstrated the utility of silyl groups for adjusting both the potency and selectivity of silicon-containing compounds. These data reveal a link between the types of silyl group and compound potency, which could have bearings for the design of novel silicon-based anticancer drugs.

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A new triazine based π-conjugated mesoporous 2D covalent organic framework: itsin vitroanticancer activities

Chemical Communications ◽

10.1039/c8cc07289b ◽

2018 ◽

Vol 54 (81) ◽

pp. 11475-11478 ◽

Cited By ~ 13

Author(s):

Sabuj Kanti Das ◽

Snehasis Mishra ◽

Krishnendu Manna ◽

Utpal Kayal ◽

Supratim Mahapatra ◽

...

Keyword(s):

Colorectal Carcinoma ◽

Anticancer Activity ◽

Cell Line ◽

Covalent Organic Framework ◽

Hct 116 ◽

Line P ◽

Organic Framework

A new 2D π-conjugated COF, TrzCOF has been synthesized and it showed excellent anticancer activity for the colorectal carcinoma HCT-116 cell line.

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STEROLS BIOACTIVITY OF RUTA GRAVEOLENS L. AND MURRAYA PANICULATA L.

International Journal of Pharmacy and Pharmaceutical Sciences ◽

10.22159/ijpps.2017v9i2.15790 ◽

2017 ◽

Vol 9 (2) ◽

pp. 103

Author(s):

Doha H. Abou Baker ◽

Eman A. Ibrahim ◽

Ahmed Kandeil ◽

Farouk K. El Baz

Keyword(s):

Anticancer Activity ◽

Antioxidant Activities ◽

Diclofenac Sodium ◽

Radical Scavenging ◽

A549 Cells ◽

Ruta Graveolens ◽

Plant Leaves ◽

Standard Drug ◽

Murraya Paniculata ◽

Anti Inflammatory

Objective: Ruta graveolens L. (R. graveolens) and Murraya paniculata L. (M. paniculata) are medicinal plants belonging to Rutaceae family have many uses in traditional medicine. The aim of the present study was to investigate sterols bioactivity of the two Rutaceae plant leaves.Methods: Sterols of the two Rutaceae plant leaves were identified using GC/MS. The antioxidant activities of the sterols of these herbs were evaluated by three different methods; free radical scavenging using 2,2′-Azino-bis (3-ethylbenzthiazoline-6-sulfonic acid) (ABTS), 1,1-Diphenyl-2-picryl-hydrazyl (DPPH) and total antioxidant activity. The anticancer activity of the sterols was determined by MTT assay against colorectal cancer HCT116, breast cancer MCF7, liver cancer HepG2 and lung cancer A549 cell lines. Anti-inflammatory activity was evaluated using albumin denaturation assay and antiviral activities against H5N1 virus were carried out using plaque reduction assay.Results: GC/MS assay showed β-Sitosterol (36%) as the most abundant sterols of R. graveolens followed by stigmasterol (18%), while stigmasterol (25.2%) was the most abundant one of M. paniculata steroids. The anti-inflammatory potential of R. graveolens steroids was significantly higher than that of diclofenac sodium (standard drug). M. paniculata sterols have higher antiviral activity (IC50= 0.15 of µg/ml) than R. graveolens sterols (IC50= 7.8 of µg/ml). The sterols of R. graveolens showed anticancer activity against MCF7 and A549 cells with inhibition 84.3 and 81%, at 100 µg/ml respectively. While M. paniculata sterols showed 77.3% inhibition against A549 cells.Conclusion: The current study suggests that the sterols of M. paniculata have more anti-viral activity than R. graveolens sterols which showed more anticancer and anti-inflammatory activities.

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Anticancer Effect and Phytochemical Profile of the Extract from Achillea ketenoglui against Human Colorectal Cancer Cell Lines

Anti-Cancer Agents in Medicinal Chemistry ◽

10.2174/1871520621666210908110422 ◽

2021 ◽

Vol 21 ◽

Author(s):

İlknur Çınar Ayan ◽

Sümeyra Çetinkaya ◽

Hatice Gül Dursun ◽

Canan Eroğlu Güneş ◽

Seda Şirin

Keyword(s):

Colorectal Cancer ◽

Cell Cycle ◽

Antioxidant Activity ◽

Anticancer Activity ◽

Cell Lines ◽

Cancer Cell ◽

Caspase 3 ◽

Caspase 9 ◽

Hct 116 ◽

Ht 29

Background: In the treatment of colorectal cancer (CRC), the search for new antineoplastic drugs with fewer side effects and more effectiveness continues. A significant part of these pursuits and efforts focus on medicinal herbs and plant components derived from these plants. A. ketenoglui is one of these medicinal plants, and its anticancer potential has never been studied before. Methods: The phenolic and flavonoid content, and antioxidant activity of A. ketenoglui extracts were determined. The phytochemical profiling and quantification analysis of major components were performed by HPLC-ESI-Q-TOF-MS. Cytotoxicity, proliferation, apoptosis and cell cycle were evaluated to reveal the anticancer activity of the extract on CRC cells (HCT 116 and HT-29). The determined anticancer activity was confirmed by mRNA (RT-qPCR) and protein (Western blotting) analyzes. Results: A. ketenoglui methanol extract was found to have high phenolic (281.89±0.23) and flavonoid (33.80±0.15) content and antioxidant activity (IC50 40.03±0.38). According to the XTT assay, the extract has strong cytotoxic activity (IC50 350 µM in HCT 116 and IC50 263 µM in HT-29 cell line). The compounds most commonly found in the plant are, in descending order, chlorogenic acid, apigenin, genistin, baicalin, eupatorin, casticin, and luteolin. In flowcytometric analysis, the extract was found to induce greater apoptosis and cell cycle arrest in both cell lines than in both control and positive control (casticin). According to the results of the mRNA expression analysis, the extract treatment upregulated the expression of the critical genes of the cell cycle and apoptosis, such as p53, p21, caspase-3, and caspase-9. In protein expression analysis, an increase in caspase-3 and p53 expression was observed in both cell lines treated with the extract. In addition, caspase-9 expression was increased in HT-29 cells. Conclusion: The findings show that A. ketenoglui has an anticancer potential by inducing apoptosis and arresting the cancer cell cycle and may be promising for CRC therapy. This potential of the plant is realized through the synergistic effects of its newly identified components.

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Anticancer Activity of Mixed Doxorubicin and Pravastatin in Nanoemulsions Against HCT 116 Colon Cancer Cells

International Journal of Drug Delivery Technology ◽

10.25258/ijddt.v7i1.8918 ◽

2017 ◽

Vol 7 (1) ◽

Author(s):

Mayson Alkhatib ◽

Retnowati . ◽

Amalia F.

Keyword(s):

Colon Cancer ◽

Anticancer Activity ◽

Cancer Cells ◽

Therapeutic Potential ◽

Morphological Changes ◽

Weight Ratio ◽

Nuclear Staining ◽

Colon Cancer Cells ◽

Fixed Weight ◽

Hct 116

Combining drugs with different mechanism of action in nanocarriers is becoming a promising strategy in cancer therapy. In the present study, the anticancer activity of the combination of doxorubicin (DOX) and pravastatin (PRV) loaded in nanoemulsions (NEs) was evaluated in HCT 116 colon cancer cells. The NE formulas (NEa and NEb) consisted of different weight fractions of the surfactant mixture of Eumulgin HRE 40/ Soya phosphatidylcholine/ sodium oleate at a fixed weight ratio of 3.5:3.0:3.5, cholesterol (CHO), Tris- HCl buffer (pH 7.22), and 1-octanol. The cytotoxicity of the drug formulas, loaded in either water or NEs, was assessed through 3-(4, 5 Dimethylthiazole- 2-yl)-2, 5-diphenyl tetrazolium bromide (MTT) assay, while the mechanism of cell death was determined by observing the morphological changes of treated cells under light microscope and identifying apoptosis by using the ApopNexin FITC kit and DAPI nuclear staining. It has been found that reducing the concentration of DOX from 15 to 7.5µM by formulating it with 7.5µM of PRV in NEa (NEa (1 DOX:1 PRV)) has preserved its cytotoxicity against HCT-116 cancer cells. The present study proved that the combination of the PRV and DOX loaded in NEa formulations improved the therapeutic potential of both of PRV and DOX as anticancer drugs.

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In Vitro Anticancer Activity of Au, Ag Nanoparticles Synthesized Using Commelina nudiflora L. Aqueous Extract Against HCT-116 Colon Cancer Cells

Biological Trace Element Research ◽

10.1007/s12011-016-0666-7 ◽

2016 ◽

Vol 173 (2) ◽

pp. 297-305 ◽

Cited By ~ 32

Author(s):

Palaniselvam Kuppusamy ◽

Solachuddin J. A. Ichwan ◽

Putri Nur Hidayah Al-Zikri ◽

Wastuti Hidayati Suriyah ◽

Ilavenil Soundharrajan ◽

...

Keyword(s):

Colon Cancer ◽

Anticancer Activity ◽

Cancer Cells ◽

Aqueous Extract ◽

Ag Nanoparticles ◽

Colon Cancer Cells ◽

Hct 116

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PHYTOCHEMICAL COMPOSITION AND ANTICANCER ACTIVITY OF SEAWEEDS ULVA LACTUCA AND EUCHEUMA COTTONII AGAINST BREAST MCF-7 AND COLON HCT-116 CELLS

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2016.v9i6.13798 ◽

2016 ◽

Vol 9 (6) ◽

pp. 115 ◽

Cited By ~ 5

Author(s):

Ade Arsianti Arsianti ◽

Fadilah Fadilah ◽

Kusmardi Suid ◽

Fatmawaty Yazid ◽

Lies Kurniati Wibisono ◽

...

Keyword(s):

Colorectal Cancer ◽

Positive Result ◽

Ethyl Acetate ◽

Anticancer Activity ◽

Ulva Lactuca ◽

Phytochemical Composition ◽

Hct 116 ◽

Hct 116 Cells ◽

Eucheuma Cottonii ◽

Mcf 7

Objective: this study is aimed to develop marine resources which is focused on the determination of phytochemical composition and exploration of seaweeds Ulva Lactuca and Eucheuma cotonii, as a potential anti-breast cancer and anti-colorectal cancer agents. Methods: Seaweeds Ulva Lactuca collected from Parangtritis beach, Yogyakarta, Central Java, Indonesia. Whereas Eucheuma cottonii collected from Salemo island, South Sulawesi, Indonesia. Seaweeds U. lactuca and E. cottonii were macerated in organic solvents, n-hexane, chloroform, ethyl acetate and ethanol, respectively. After maceration for three days, the mixture was filtered, the filtrate was concentrated by rotary evaporator. The concentrated extract of n-hexane, ethyl acetate, ethanol and chloroform were then analyzed by thin layer chromatography. Phytochemical test of the concentrated extract were conducted to identify the metabolites containing in the seaweeds. Furthermore, the cytotoxic activity of the n-hexane, ethyl acetate, ethanol and chloroform extract of Ulva Lactuca and Eucheuma cotonii were evaluated as a growth inhibitor of breast MCF-7 and colorectal HCT-116 cancer cells by MTT cell proliferation assay. Results: Phytochemical test for the concentrated extracts of Ulva Lactuca showed the positive result for metabolites of steroids, glycosides, flavonoid,and tannin. While the concentrated extracts of E. cottonii showed positive result for metabolites of steroids, glycosides, and flavonoid. Both concentrated extracts of Ulva lactuca and Eucheuma cotonii exhibited anticancer activity against breast MCF-7 and colorectal HCT-116 cells with IC50 ranging of 21 µg/mL to 99 µg/mL . Conclusion: Our results clearly demonstrate seaweeds Ulva Lactuca and Eucheuma cotonii as a promising candidates for the new anti-breast and anti-colorectal cancer agents. Keywords: Phytochemistry, Ulva Lactuca, Eucheuma cotonii , anticancer, breast MCF-7, colorectal HCT-116

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