scholarly journals Phytochemical screening and anticancer activity of the aerial parts extract of Xanthium strumarium L. on HepG2 cancer cell line

2021 ◽  
Vol 7 (1) ◽  
Author(s):  
Hai Trieu Ly ◽  
Trieu Minh Truong ◽  
Thi Thu Huong Nguyen ◽  
Hoang Dung Nguyen ◽  
Yuxia Zhao ◽  
...  

Abstract Background Cancer is one of the most considerable concerns because of increasing the death rate all over the world. Recent studies have disclosed that plant extracts exhibit anticancer activity through various mechanisms. Xanthium strumarium has been used by Vietnamese in herbal medicines to support the medication of infirmities. This study is to consider the secondary metabolites, antioxidant and anticancer capacities of extract from the aerial parts (stems and leaves) of X. strumarium (AP-XS). Methods AP-XS was analyzed for the presence of phytochemicals via qualitative chemical tests and determined total polyphenol and flavonoid contents. DPPH (1,1-diphenyl-2-picrylhydrazyl) quenching assay and sulforhodamine B (SRB) assay were selected to investigate antioxidant capacity and anti-proliferative activity, respectively. Besides, acridine orange-ethidium bromide (AO-EB) dual staining was applied to evaluate the ability to induce apoptosis on HepG2 cancer cells. Results Results of present study indicated that AP-XS contains the main phytochemicals such as flavonoids, tannins, saponins, alkaloids, and triterpenes. Ethanol extract had highest content of polyphenol (84.86 mg gallic acid equivalent/g dry mass), and exhibited the great total antioxidant property (IC50 = 184.13 μg/mL) and anti-proliferative activity on HepG2 cancer cells (IC50 = 81.69 μg/mL). Furthermore, the characteristics of apoptosis including shrinkage of the cell and apoptotic bodies were found following 60 h of AP-XS extract treatment through AO-EB dual staining. Conclusion The data suggest that AP-XS extract had antioxidant potential and anti-proliferative effect. The anti-proliferative property was considered to have an association with a rising of apoptosis. These results were reliable for further research on X. strumarium as a source of phytochemicals with anticancer activity potential for cancer therapeutics.

2020 ◽  
Vol 20 (18) ◽  
pp. 1929-1941
Author(s):  
Heba A. Elhady ◽  
Hossa F. Al-Shareef

Background and Objective: Due to the well-documented anti-proliferative activity of 2-thiohydantoin incorporated with pyrazole, oxadiazole, quinazoline, urea, β-naphthyl carbamate and Schiff bases, they are noteworthy in pharmaceutical chemistry. Methods: An efficient approach for the synthesis of a novel series of 2-thiohydantoin derivatives incorporated with pyrazole and oxadiazole has proceeded via the reaction of the acyl hydrazide with chalcones and/or triethyl orthoformate. Schiff bases were synthesized by the reaction of the acyl hydrazide with different aromatic aldehydes. Moreover, Curtius rearrangement was applied to the acyl azide to obtain the urea derivative, quinazoline derivative, and carbamate derivative. Results: The synthesized compounds structures were discussed and confirmed depending on their spectral data. The anticancer activity of these heterocyclic compounds was evaluated against the breast cancer cell line (MCF-7), where they showed variable activity. Compound 5d found to have a superior anticancer activity, where it has (IC50 = 2.07 ± 0.13 μg/mL) in comparison with the reference drug doxorubicin that has (IC50 = 2.79 ± 0.07 μg / mL). Then compound 5d subjected to further studies such as cell cycle analysis and apoptosis. Apoptosis was confirmed by the upregulation of Bax, downregulation of Bcl-2, and the increase of the caspase 3/7percentage. Conclusion: Insertion of pyrazole, oxadiazole and, quinazoline moieties with 2-thiohydantoin moiety led to the enhancement of its anti-proliferative activity. Hence they can be used as anticancer agents.


Author(s):  
Kavitha K

 Objective: In recent years, herbal plants have been got more attention due to their diverse presence of phytochemicals and its biological properties. Hepatocellular carcinoma is one of the major worldwide problems primarily caused by hepatitis B and C virus infection. End-stage liver cancer treatment options are limited, thus requiring expensive liver transplantation which is not available in many countries.Methods: In the present study, the Mucuna pruriens seed extract was analyzed for phytochemicals, antioxidant activity, total phenols, and total flavonoids content. The seed extract was further analyzed for its anticancer activity by culturing liver cancer cell line. The above protocols were done by standard methods.Results: The seed extract of M. pruriens revealed more number of phytochemicals in different organic solvents. 1,1- Diphenyl- 2- picrylhydrozyl scavenging activity of plant extract was more in ethanol extract (98.051±0.547) among all other solvents. The total phenols and flavonoids content in ethanol extract were 46.442±0.353 mg gallic acid equivalent/g and 2.254±0.647 mg - quercetin equivalent /g, respectively. IC50 value of 3-(4, 5-dimethythiazol-2-yl)-2, 5-diphenyl tetrazolium bromide (MTT) analysis of Hep-2 cell line was 150 (μg/ml).Conclusion: The present study revealed about the phytochemical contents and antioxidant potential of M. pruriens seeds. Further, the MTT analysis proved that the seed extract was effective against cancer cells and also used to treat many diseases.


Marine Drugs ◽  
2020 ◽  
Vol 18 (4) ◽  
pp. 191
Author(s):  
Ambre Dezaire ◽  
Christophe H. Marchand ◽  
Marine Vallet ◽  
Nathalie Ferrand ◽  
Soraya Chaouch ◽  
...  

High-throughput screening assays have been designed to identify compounds capable of inhibiting phenotypes involved in cancer aggressiveness. However, most studies used commercially available chemical libraries. This prompted us to explore natural products isolated from marine-derived fungi as a new source of molecules. In this study, we established a chemical library from 99 strains corresponding to 45 molecular operational taxonomic units and evaluated their anticancer activity against the MCF7 epithelial cancer cell line and its invasive stem cell-like MCF7-Sh-WISP2 counterpart. We identified the marine fungal Paradendryphiella salina PC 362H strain, isolated from the brown alga Pelvetia caniculata (PC), as one of the most promising fungi which produce active compounds. Further chemical and biological characterizations of the culture of the Paradendryphiella salina PC 362H strain identified (-)-hyalodendrin as the active secondary metabolite responsible for the cytotoxic activity of the crude extract. The antitumor activity of (-)-hyalodendrin was not only limited to the MCF7 cell lines, but also prominent on cancer cells with invasive phenotypes including colorectal cancer cells resistant to chemotherapy. Further investigations showed that treatment of MCF7-Sh-WISP2 cells with (-)-hyalodendrin induced changes in the phosphorylation status of p53 and altered expression of HSP60, HSP70 and PRAS40 proteins. Altogether, our study reveals that this uninvestigated marine fungal crude extract possesses a strong therapeutic potential against tumor cells with aggressive phenotypes and confirms that members of the epidithiodioxopiperazines are interesting fungal toxins with anticancer activities.


2020 ◽  
Vol 15 (8) ◽  
pp. 1934578X2094554
Author(s):  
Chao Tong ◽  
Ri-Hui Chen ◽  
Ding-Cheng Liu ◽  
De-Sheng Zeng ◽  
Hui Liu

A new neolignan, (7 S,8 R)- threo-1′-[3′-hydroxy-7-(4-hydroxy-3,5-dimethoxyphenyl)-8-hydroxymethyl-7,8-dihydrobenzofuran]acrylaldehyde (1), along with 5 known compounds 2-6, were isolated from the fruits of Xanthium strumarium. Their structures were elucidated by extensive spectroscopic methods. All the isolates were evaluated for in vitro cytotoxicity against human cancer cell lines, including human hepatoma cell line (HepG2), human breast cancer cell line (MCF-7), human colon cancer cell line (HCT-116), and human gastric cancer cell line (SGC-7901). Among them, compounds 1 and 3 showed selective cytotoxicity on HepG2 cancer cells with half-maximal inhibitory concentration (IC50) values of 10.2 ± 1.2 and 18.3 ± 1.6 μM, respectively. Moreover, compound 5 also exhibited moderate cytotoxicity against MCF-7 cancer cells with an IC50 value of 20.5 ± 1.3 μM.


Author(s):  
CHIDAMBARARAJAN P ◽  
KEERTHANA V ◽  
PRIYADHARSHINI K, ◽  
SAKTHIVEL B

Objective: The aim of the present investigation was to determine the in vitro antioxidant and anticancer activity of the ethanol extract of Ulva lactuca L. Methods: The present study was to investigate the antioxidant and anticancer activity of U. lactuca L. The extract of U. lactuca L. was extracted by ethanol and subject to analysis. An in vitro antioxidant activity of the ethanol extract of U. lactuca L. was performed by 1, 1-diphenyl-2-picrylhydrazyl free radical scavenging assay. Simultaneously anticancer activity was also performed using blood cancer (MOLT-3) cell line, and the species showed a strong selective cell proliferation inhibition of the cancer cell line. Results: The scavenging activity was measured and determined to be 78.5%. This might be due to high polyphenolic compounds and flavonoid contents of the extract, which showed maximum growth inhibition of 74.4%. Conclusion: Thus, the study concludes that the constituents of seaweeds can act as potent in treating various diseases and can be used as an alternative for therapeutic treatment.


Author(s):  
Nenavath Vinay ◽  
Darling Chellathai David

Background: Cancer is rapidly evolving life-threatening ailment in the mankind due to changes in daily food intake and lifestyle changes. Oral carcinoma is 6th major cause of cancer death in the world and it is third major reason of cancer mortality in India. Every cell in the human body requires glucose for its metabolic energy. Besides normal cell, cancer cells also require the glucose for its endurance and multiplication. SGLT2 inhibitors which are aimed at diabetes therapy exhibited anticancer properties also in colon and pancreatic cancer lines. Present study aim is to evaluate the anticancer activity of SGLT2 inhibitors against oral cancer cell by MTT Assay.Methods: To evaluate the anticancer activity of SGLT2 inhibitors MTT Cytotoxic assay is performed as per standard protocols. Cancer cells were plated in 24-well plates and incubated at 370C with 5% CO2 condition. After convergence, samples are added to the plates in various concentrations and allowed to incubate then they are detached from the plates and cleansed with the reagents. The wells are coated with the dye and incubated. Later samples are analysed in UV-spectrophotometer.Results: Cytotoxic assay showed decrease in cell viability with increasing dose of SGLT2 inhibitors. IC50 values were determined graphically. The IC50 value of dapagliflozin is 400µg/ml and canagliflozin is 250µg/ml respectively after 24 hours of Assessment.Conclusions: The results of the current study give us an evidence that SGLT2 inhibitors dapagliflozin and canagliflozin exhibits anticancer property in Oral Cancer cell line.


2019 ◽  
Vol 2 (2) ◽  
pp. 31-35
Author(s):  
Rosidah Rosidah ◽  
Poppy Anjelisa Zaitun Hasibuan ◽  
Ginda Haro ◽  
Denny Satria

Breast cancer is one of the world's leading cause of death in women. Due to the resistance of chemotherapeutic agents, there is a continuous need to search of natural products with anticancer activity.  The use of natural products  is expected to increase the effectiveness  and decrease side effect. The purpose of this study was to investigate the anticancer activity of ethanol extract of andaliman fruits (EEAF) towards 4T1 cells. Extracts were prepared by maceration using solvent ethanol 96%. 4T1 cells were grown in culture medium DMEM then given by EEAF and doxorubicin. Cytotoxic test in vitro was done by MTT method [3-(4,5-dimetiltiazol-2-il) -2.5 difeniltetrazolium bromide] which is then analyzed using SPSS 21. The results from this study showed that the cytotoxic results (IC50) after treatment with EEAF and doxorubicin were 54.48 ± 0.22 µg/mL dan 0.80 ± 0.02 µg/mL.Based on the result above, we conclude that EEAF has cytotoxic activity towards 4T1 cancer cells. Key words: andaliman fruits, Zanthoxylum acanthopodium DC., ethanol extract, breast cancer, 4T1 cell line.


2017 ◽  
Vol 2017 ◽  
pp. 1-9 ◽  
Author(s):  
María José Vallejo ◽  
Lizeth Salazar ◽  
Marcelo Grijalva

Medicinal and aromatic plants (MAPs) are known and have been long in use for a variety of health and cosmetics applications. Potential pharmacological usages that take advantage of bioactive plant-derived compounds’ antimicrobial, antifungal, anti-inflammatory, and antioxidant properties are being developed and many new ones explored. Some phytochemicals could trigger ROS-mediated cytotoxicity and apoptosis in cancer cells. A lot of effort has been put into investigating novel active constituents for cancer therapeutics. While other plant-derived compounds might enhance antioxidant defenses by either radical scavenging or stimulation of intracellular antioxidant enzymes, the generation of reactive oxygen species (ROS) leading to oxidative stress is one of the strategies that may show effective in damaging cancer cells. The biochemical pathways involved in plant-derived bioactive compounds’ properties are complex, and in vitro platforms have been useful for a comprehensive understanding of the mechanism of action of these potential anticancer drugs. The present review aims at compiling the findings of particularly interesting studies that use cancer cell line models for assessment of antioxidant and oxidative stress modulation properties of plant-derived bioactive compounds.


2020 ◽  
Vol 25 (1) ◽  
pp. 21
Author(s):  
Wulandari Wulandari ◽  
Muthi’ Ikawati ◽  
Edy Meiyanto

Pentagamavunone‐0 (PGV‐0) or 2,5‐bis(4’‐hydroxy‐3‐methoxybenzylidine)‐cyclopentanone is a curcumin analogue that exhibits anticancer activity in breast cancer cells. However, most of previous reports are limited to the use of two‐dimensional (2D) cell culture. The use of three‐dimensional (3D) cell culture model in cancer research can represent the real condition of cancer growth in patients better than the 2D culture. The purpose of this study was to determine the anticancer activity of PGV‐0 on a 3D model of HCC 1954 breast cancer cells. HCC 1954 cells were grown in the 3D culture in the presence of PGV‐0, and the spheroid formation and growth of formed spheroids were observed using microscope at 24 and 96 h, respectively. The cytotoxic effects were measured by MTT assay. PGV‐0 inhibited the formation and growth of spheroids at the concentration as low as 60 µM. The cytotoxic effect of PGV‐0 appeared in a dose‐dependent manner with the IC50 value of 70.9 µM. The results of this study indicate that PGV‐0 has an anticancer activity on a 3D model of HCC 1954 breast cancer cell line. Therefore, the result supported the potency of PGV‐0 as cancer chemopreventive agent.


Molecules ◽  
2019 ◽  
Vol 24 (13) ◽  
pp. 2489 ◽  
Author(s):  
Leon M. Larcher ◽  
Tao Wang ◽  
Rakesh N. Veedu

MicroRNAs (miRNAs) are short non-coding RNAs that are involved in the regulation of gene expression. Previous reports showed an over-expression of miRNA-21 (miR-21) in various cancer cells, and its up-regulation is closely related to cancer initiation, proliferation and metastasis. In this work, we envisioned the development of novel antimiRzymes (anti-miRNA-DNAzyme) that are capable of selectively targeting and cleaving miR-21 and inhibit its expression in cancer cells using the DNAzyme technique. For this purpose, we have designed different antimiRzyme candidates by systematically targeting different regions of miR-21. Our results demonstrated that RNV541, a potential arm-loop-arm type antimiRzyme, was very efficient (90%) to suppress miR-21 expression in U87MG malignant glioblastoma cell line at 200 nM concentration. In addition, RNV541 also inhibited miR-21 expression (50%) in MDA-MB-231 breast cancer cell line. For targeted delivery, we conjugated RNV541 with a transferrin receptor (TfR) targeting aptamer for TfR-mediated cancer cell delivery. As expected, the developed chimeric structure efficiently delivered the antimiRzyme RNV541 into TfR positive glioblastoma cells. TfR aptamer-RNV541 chimeric construct showed 52% inhibition of miR-21 expression in U87MG glioblastoma cells at 2000 nM concentration, without using any transfection reagents, making it a highly desirable strategy to tackle miR-21 over-expressed malignant cancers. Although these are in vitro based observations, based on our results, we firmly believe that our findings could be beneficial towards the development of targeted cancer therapeutics where conventional therapies face several challenges.


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