Antioxidant, Anti-Inflammatory and Cytotoxic Activities of Jasminum multiflorum (Burm. F.) Andrews Leaves towards MCF-7 Breast Cancer and HCT 116 Colorectal Cell Lines and Identification of Bioactive Metabolites

Author(s):  
Seham Salah El-Hawary ◽  
Hala M. EL-Hefnawy ◽  
Samir Mohamed Osman ◽  
Mohamed A. El-Raey ◽  
Fatma Alzahraa Mokhtar ◽  
...  

Background: The plants of high phenolic contents are perfect antioxidant and anti-inflammatory candidates and participate in biological studies as effective agents towards different cancer cell lines. Objective: To investigate the antioxidant, anti-inflammatory, and cytotoxic activities of the hydromethanolic leaf extract of Jasminum multiflorum (Burm. f.) Andrews. (J. multiflorum), and phenolic profiling of the extract. Methods: The antioxidant activity for the extract was estimated using β-Carotene-linoleic and ferric reducing antioxidant power (FRAP) assays. The anti-inflammatory activity was evaluated by histamine release assay. Cytotoxicity of J. multiflorum was performed using a neutral red uptake assay towards breast cancer (MCF-7) and colorectal cancer (HCT 116) cell lines. Phenolic profiling of the leaves was characterized using high performance liquid chromatography coupled to photodiode array detector-mass spectroscopy-mass spectroscopy (HPLC-PDA-MS/MS), and chromatographic isolation and identification of the isolated compounds were performed using spectroscopic and NMR data, and virtual docking was performed to the isolated compounds against HSP90 (HEAT SHOCK PROTEIN 90). Results : At a concentration of 75 µg mL-1, J. multiflorum extract showed high antioxidant power; 68.23±0.35 % inhibition and 60.30±0.60 a TEAC (µmol Trolox g-1) for β-Carotene-linoleic assay and FRAP assay; respectively, and possessed anti-inflammatory activity with IC50 67.2 µg/ml. J. multiflorum showed high cytotoxic activity with IC50 of 24.81 µg/ml and 11.38 µg/ml for MCF-7 and HCT 116 cell lines, respectively. HPLC-PDA-MS/MS analysis tentatively identified 39 compounds; major compounds are secoiridoid glycosides, kaempferol, and quercetin glycosides, in addition to simple phenylethanoid compounds. Isolation of active metabolites was performed and led to the isolation and identification of four compounds. On the basis of docking study using HSP90 legend, kaempferol neohesperidoside showed a high cytotoxic potential supported by a high affinity score towards HSP90 legend protein. Conclusion: Jasminum multiflorum is a good candidate to isolate cytotoxic agents.

2018 ◽  
Vol 8 (3) ◽  
pp. 159 ◽  
Author(s):  
Meghan Fragis ◽  
Abdulmonem I. Murayyan ◽  
Suresh Neethirajan

Background: Breast cancer is the most commonly diagnosed cancer and the second leading cause of cancer deaths among Canadian women. Cancer management through changes in lifestyle, such as increased intake of foods rich in dietary flavonoids, have been shown to decrease the risk associated with breast, liver, colorectal, and upper-digestive cancers in epidemiologic studies. Onions are high in flavonoid content and one of the most common vegetables. Additionally, onions are used in most Canadian cuisines.Methods: We investigated the effect of five prominent Ontario grown onion (Stanley, Ruby Ring, LaSalle, Fortress, and Safrane) extracts on two subtypes of breast cancer cell lines: a triple negative breast cancer line MDA-MB-231 and an ER+ breast cancer line MCF-7.Results: These onion extracts elicited strong anti-proliferative, anti-migratory, and cytotoxic activities on both the cancer cell lines. Flavonoids present in these onion extracts induced apoptosis, cell cycle arrest in the G2/M phase, and a reduction in mitochondrial membrane potential at dose-dependent concentrations. Onion extracts were more effective against MDA-MB-231 compared to the MCF-7 cell line. Conclusion: In this study, we investigated the extracts synthesized from Ontario-grown onion varieties in inducing anti-migratory, cytostatic, and cytotoxic activities in two sub-types of human breast cancer cell lines. Anti-tumor activity of these extracts depends upon the varietal and can be formulated into nutraceuticals and functional foods for the wellbeing of cancer patients. Overall, the results suggest that onion extracts are a good source of flavonoids with anti-cancerous properties.Keywords: onion extracts; flavonoids; anti-proliferative; breast cancer; cytotoxic activity


Author(s):  
Bruna Alexandre Oliveira da Silva ◽  
Isabela Spido Dias ◽  
Luís Eduardo Sarto ◽  
Elba Pereira de Gois ◽  
Claudia Torres ◽  
...  

Purpose: Breast cancer is the most common female malignancy and melanoma is the most lethal type of skin cancer. Traditional therapy for cancer treatment is far from satisfactory due to drug resistance and side effects, thus a search for new medicines is being emphasized. Palladium(II) complexes have been reported as anticancer potential agents. In this work, the anticancer activities and cell death induction of a new series of square-planar palladium(II) complexes were evaluated against MCF-7 and MDA-MB-435 cancer cells. Methods: MCF-7 (breast carcinoma) and MDA-MB-435 (melanoma) cells were cultivated, and treated with ligand and Pd(II) complexes. Cell growth, migration and adhesion inhibition, morphological alterations, cell death induction and, DNA interaction upon treatment were studied. Results: Pd(II) complexes exhibited both short and long-term antiproliferative effects on both cell lines, reducing by 80% cell growth in the SRB assay and abolishing long-term proliferation, estimated by the clonogenic assay. Complexes reduced significantly (p < 0.05) cell migration and adhesion when compared to the control group. Complexes induced morphological alterations in cell lines and significant (p<0.05) cellular shrinkage. Cell death was induced and the complexes were able to interact with DNA, inducing cleavage of double-stranded DNA, which may account for the complexes cytotoxic effects, observed against both MCF-7 and MDA-MB-435 cells. Conclusion: Overall, the complexes exhibited cytotoxic activities and induced cell death. These observations emphasize an anticancer role with a potential therapeutic value for Pd(II) complexes to improve the outcome of patients with breast cancer and melanoma.


2020 ◽  
Vol 10 (4) ◽  
pp. 411-428
Author(s):  
Eman F. Ahmed ◽  
Amany A. Sleem ◽  
Fawkeya A. Abbas ◽  
Azza M. El-Shafae ◽  
Maher M. El-Domiaty

Background: The literature survey revealed that there are no sufficient phytochemical and biological studies on the roots and rhizomes of Prosopis farcta (Banks & Sol.) J. F. Macbr., therefore, the present work is concerned with the phytochemical and biological evaluation of this plant. Methods: The shade-dried roots and rhizomes were powdered together, extracted by 85% ethanol and subjected to phytochemical investigation. Biologically, the antioxidant, antidiabetic, cytotoxic, antiallergic and antimicrobial activities were evaluated. Results: The phytochemical investigation resulted in the isolation of 14 compounds including the fatty acid derivative, threo- methyl 9, 10-dihydroxyoctadecanoate (5), that is isolated for the first time from a natural source, in addition to the identification of 72 compounds by HPLC-PDA-ESIMS/ MS analysis including organic acids and their derivatives, flavonoids, anthraquinones and lignan derivatives. Biologically, threo- methyl 9, 10-dihydroxyoctadecanoate (5) exerted a potent cytotoxic effect against human lung carcinoma (A-549) and human colon carcinoma (HCT-116) cell lines. The total alcoholic extract showed a potent DPPH scavenging activity, a significant decrease in the blood glucose level in alloxan-induced diabetic rats and a mild antibacterial effect against Bacillus subtilis, Staphylococcus aureus (G +ve bacteria) and Escherichia coli (G –ve bacteria). Conclusion: This is the first report on the isolation and identification of threo- methyl 9, 10- dihydroxyoctadecanoate (5) from a natural source, and this novel compound exhibited potent cytotoxic activities against A-549 and HCT-116 cell lines. Moreover, this is the first HPLC-PDA-ESIMS/ MS profiling for this plant.


Molecules ◽  
2019 ◽  
Vol 24 (20) ◽  
pp. 3738 ◽  
Author(s):  
Alminderej ◽  
Elganzory ◽  
El-Bayaa ◽  
Awad ◽  
El-Sayed

New 1,3,4-thiadiazole thioglycosides linked to substituted arylidine systems were synthesized via glycosylation of the prepared 1,3,4-thiadiazole thiol compounds. Click strategy was also used for the synthesis of new 1,3,4-thiadiazole and 1,2,3-triazole hybrid glycosides by reaction of the acetylenic derivatives with different glycosyl azids followed by deacetylation process. The cytotoxic activities of the prepared compounds were studied against HCT-116 (human colorectal carcinoma) and MCF-7 (human breast adenocarcinoma) cell lines using the MTT assay. The results showed that the key thiadiazolethione compounds 2 and 3, the triazole glycosides linked to p-methoxyarylidine derivatives 14 and 15 in addition to the free hydroxyl glycoside 20 were found potent in activity comparable to the reference drug doxorubicin against MCF-7 human cancer cells. The acetylenic derivative 2 and glycoside 20 were also found highly active against HCT-116 cell lines.


2012 ◽  
Vol 13 (8) ◽  
pp. 4075-4079 ◽  
Author(s):  
Mohammed Hadi Al-Douh ◽  
Hayder B. Sahib ◽  
Hasnah Osman ◽  
Shafida Abd Hamid ◽  
Salizawati M. Salhimi

2016 ◽  
Author(s):  
◽  
Kabange Kasumbwe

Coumarins are naturally occurring α-benzopyrone derivatives known for their pharmacological properties such as anticoagulant, antimicrobial, anticancer, antioxidant, anti-inflammatory and antiviral properties. The pharmacological, biochemical, and curative applications of coumarins depend on the substitution around the coumarin core structure. In the present study, seven halogenated coumarins CMRN1 - CMRN7 were synthesized and evaluated for mosquito larvicidal, repellancy , and insecticidal activity against Anopheles arabiensis. Furthermore, the antimicrobial properties of compounds CMRN1 - CMRN7 were evaluated by assessing the bacterial and fungicidal activities using the disc diffusion method. The anti-inflammatory properties were evaluated using the 5-lipoxygenase kit assay. The evaluation of the safe use of the compounds was determined using the Brine shrimp lethal test. The potential carcinogenic properties of the studied compounds was done using the Salmonella mutagenicity test. The anti-cancer property of the studied compounds was evaluated against UACC62 (Melanoma), MCF-7 (Breast cancer), and PBMC (Peripheral blood mononuclear) cell lines using of MTT assay. The apoptotic potential of the synthesized coumarin was evaluated against UACC62 (Melanoma) cell by assessing their morphological changes, membrane change, mitochondria membrane potential, and caspase-3 activity using the Annexin V-PI staining, JC-1, caspase-3 enzyme kits, respectively, on flow cytometer. The results were compared to a known anti-cancer drug, doxorubicin. The results showed that compounds CMRN1, CMRN2, CMRN4, CMRN5 and CMRN7 exerted 100% larval mortality within 24 h of exposure. All halogenated coumarins reversibly knocked down adult mosquitoes but did not kill them after 24 h of exposure. Furthermore, the adulticidal activity of the compounds was considered only mild to moderate. The antimicrobial activity of the synthetized coumarins CMRN1 - CMRN7 were assessed against E. coli, K. pneumoniae, S. marcescens, S. faecalis, B. cereus, B. coagulans, B. stearothermophilus, C. freundii, S. aureus and M. luteus bacteria and three yeast cultures, C. albicans, C. utilis, S. cerevisiae as well as two fungal species, A. flavus and A. niger. Compounds CMRN1 and CMRN2 showed bacterial growth inhibition for all the tested species except K. pneumonia and B. stearothermophilus. Compounds CMRN4 and CMRN7 showed moderate bacterial inhibition against B. cereus, M. luteus and S. aureus. The anti-inflammatory activity of the coumarins analogues showed that 1 mg/mL of the compounds CMRN1, CMRN2, CMRN4 and CMRN5 displayed moderate anti-inflammatory activity when compared to the positive control, 15-lapoxygenase. The cytotoxicity results of the studied synthetized coumarins displayed selective activity towards the cancer cell lines used in this study. Our studies showed that CMRN1, CMRN2, CMRN4, and CMRN5 had significant cytotoxity effect against UACC-62 (Melanoma) and MCF-7 ( Breast) cancer cells with an inhibitory concentration (IC50) which displayed significant cytotoxicity effect, in particular CMRN4 and CMRN5. These compounds CMRN1- CMRN7 showed no toxicity effect against PBMCs cell line. The mechanism of cell death, that is, necrosis or apoptosis induced by the coumarins was investigated against UACC-62 (Melanoma). We found that CMRN1, CMRN2, CMRN4, CMRN5 induced morphological changes, characteristic of apoptosis . Annexin V kit showed that CMRN1, CMRN2 and CMRN5 showed early apopotosis and late apoptosis was particularly higher for compound CMRN4. The disruption of the mitochondria membrane was noticed to be greater in CMRN1 and CMRN5 when compared to the positive control doxorubicin. Compound CMRN4 produced high levels of caspase-3 positive compared to the control. The coumarin compounds showed no mutagenicity and were also found to be non-toxic to brine shrimps. In conclusion, compounds CMRN1, CMRN2, CMRN4, CMRN5 and CMRN7 are potential larvicidal agents because they exhibited close to 100% activity within 24 h. Furthermore, the anti-cancer efficiency of compounds CMRN1, CMRN2, CMRN4, and CMRN5, is enough qualification for them to be optimized for increase anticancer potency.


2021 ◽  
Author(s):  
Shangxian Luan ◽  
Yingying Gao ◽  
Xiaoxia Liang ◽  
Li Zhang ◽  
Qiang Wu ◽  
...  

Abstract Aconitine linoleate (1) is a lipo-diterpenoid alkaloid, isolated from Aconitum sinchiangense W. T. Wang. The study aimed at investigating the anti-proliferative efficacy and the underlying mechanisms of 1 against MCF-7 and MCF-7/ADR cells, as well as obvious the safety evaluation in vivo. The cytotoxic activities of 1 were measured in vitro. Also, we investigated the latent mechanism of 1 by cell cycle analysis in MCF-7/ADR cells, and Topo I, Topo IIα inhibition assay. Molecular docking is done by Discovery Studio 3.5 and Autodock vina 1.1.2. Finally, the acute toxicity of 1 was detected on mice. 1 exhibited significant anti-tumor activity against both MCF-7 and MCF-7/ADR cells, with IC50 value of 7.58 and 7.02 µM, which is 2.38 times and 5.05 times more active, respectively than etoposide in both cell lines, and being 9.63 times more active than adriamycin in MCF-7/ADR cell lines. The molecular docking and topo inhibition test found that it's a selective inhibitor of topoisomerase Ⅱα. Moreover, activation of damage response pathway of the DNA leads to cell cycle arrest at G0G1phase. Furthermore, the in vivo acute toxicity of 1 in mice displayed lower toxicity than aconitine, with LD50 of 2.2×105nmol/Kg and only slight pathological changes in liver and lung tissue, 489 times safer than aconitine. In conclusion, compared with aconitine, 1 has more significant anti-proliferative activity against MCF-7 and MCF-7/ADR cells, and greatly reduces in vivo toxicity, which suggesting this kind of lipo-alkaloids are powerful and promising antitumor compounds for breast cancer.


2019 ◽  
Vol 16 ◽  
Author(s):  
Alaa M. Abo Alnaja ◽  
Thoraya. A. Farghaly ◽  
Heba S. A. El-zahabi ◽  
Mohamed R. Shaaban

Background: Azolopyrimidines are imposed on the arena of drugs treated for cancer. The urgent need to discover new selective anticancer agents, paved the way to explore the antitumor significance of such fused systems. From synthetic point of view, Microwave- facilitated technique for synthesis is very strongly associated with green method in chemistry field. Aim: Our aim is to synthesis of bioactive compounds and using docking simulation run by MOE program to explore the binding mode of the most active enzyme inhibitor among the target compounds. Method: In addition to the use of conventional heating, the MARS system of CEM utilized for Microwave irradiation that is equipped with a multi-mode platform with a magnetic stirring plate and a rotor that allows the parallel processing of many vessels per batch. All the synthesized compounds were tested for their anticancer activity against hepatic cancer (HePG-2), breast cancer (MCF-7) and colon cancer (HCT-116). Screening against the cancer cell lines was performed, using doxorubicin as a reference drug. Docking studies were conducted using MOE software. Result: A novel series of fluorinated fused-pyrimidine namely, pyrazolopyrimidine, triazolopyrimidine and pyrimidobenzimidazole were designed and synthesized conventionally and under microwave irradiations The mechanistic pathways as well as the structure of all products were debated and demonstrated based on all possible spectral data. In-vitro examination of the novel prepared derivatives versus the three different human cancer cell lines [hepatic cancer (HePG-2), breast cancer (MCF-7) and colon cancer (HCT-116)] was evaluated to estimate their actual activity. Conclusion: We have developed a simple, facile, and efficient procedure for the formation of new series of azolopyrimidines. All spectra of all products were investigated deliberately to confirm their structures. The anti-cancer activity has been examined against three cancer cell lines e.g. HepG-2, MCF-7 and HCT116. Molecular modeling study was carried out in order to rationalize the in vitro anti-tumor results.


2021 ◽  
Vol 11 (8) ◽  
pp. 3510
Author(s):  
Loubna El Fakir ◽  
Kaoutar Bouothmany ◽  
Amal Alotaibi ◽  
Mohammed Bourhia ◽  
Riaz Ullah ◽  
...  

The current research was conducted to investigate the chemical profile, antiproliferative, and antioxidant activities of methanol extracts obtained by two different methods including maceration and Soxhlet from Berberis hispanica Boiss. & Reut. Antiproliferative activities were evaluated by the MTT (3-(4, 5-dimethylthiazolyl-2)-2, 5-diphenyltetrazolium bromide) assay in four human cancer cell lines including prostate (LnCap and 22 RV1) and breast cancer (MDA-MB-231 and MCF7). The antioxidant power was evaluated by DPPH ((2,2-diphenyl-1-picryl-hydrazyl-hydrate), ABTS (2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid), and FRAPS (Ferric reducing antioxidant power) tests. The chemical composition was conducted by gas chromatography-mass spectrometry (GC-MS) after methylation. Total phenolic and flavonoid contents were assessed using the Folin–Ciocalteu method. The phytochemical analysis showed that the tested extracts possessed inserting potentially active compounds. The MTT test revealed that both extracts (maceration and Soxhlet) reduced cell viability in all cell lines tested. In breast cancer cell lines MDA-MB-231 and MCF-7, the IC50 values obtained by maceration were 16.55 ± 0.58 and 17.95 ± 0.58 µg/mL, respectively. These values were slightly lower than those obtained with the Soxhlet extract toward MDA-MB-231 (19.93 ± 0.74 µg/mL) and MCF-7 (20.22 ± 0.89 µg/mL). Regarding prostate cancer cells 22 RV and LnCap, the IC50 values obtained by maceration extract (22 RV: 11.75 ± 0.35 µg/mL; LnCap: 11.91 ± 0.54 µg/mL) were also slightly lower than those obtained with Soxhlet (22 RV: 13.47 ± 0.52 µg/mL; LnCap: 19.64 ± 1.05 µg/mL). The antioxidant activity showed that the studied extracts had considerable antioxidant activity (DPPH, FRAP, and ABTS) with particular attention to the extract obtained with maceration. The Berberis hispanica Bois. and Reut. can serve society as it provides potentially bioactive compounds that may find application in the medical sector to control such diseases.


2021 ◽  
Vol 14 (1) ◽  
Author(s):  
Endalkachew Nibret ◽  
Sonja Krstin ◽  
Michael Wink

Abstract Objective We investigated the anti-proliferative or cytotoxic activities of five nutraceutical compounds: allyl isothiocyanate, β-carotene, caffeine, capsaicin, and lupanine that we consume respectively, for example, from mustard seeds, carrot, coffee, pepper, and lupin seeds against cancer cell lines (human colon: HCT 116 p53 wild type, HCT 116 p53−/− and lymphoblastic: CEM/CCRF, CEM/ADR5000). Result Out of the five compounds tested in vitro, capsaicin and β-carotene were more cytotoxic than the other three compounds against the four cancer cell lines. The most potent nutraceutical compound was capsaicin and it exerted its highest cytotoxicity against HCT 116 p53−/− with IC50 value of 19.67 ± 0.06 µM. It is worth considering capsaicin for further development of anticancer drug against both colon and leukemia cancer types.


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